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Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Применить Всего найдено 1249. Отображено 100.
28-03-2013 дата публикации

ORAL PARTICULATE ANTITUMOR PREPARATION

Номер: US20130078309A1
Автор: Ogata Tetsuo, Ohnishi Yoshito
Принадлежит: TAIHO PHARMACEUTICAL CO., LTD.

An oral particulate antitumor preparation, which allows safe intake of antitumor agents, handling of which could be in many cases dangerous due to their high pharmacological activity, and has a stability equivalent to that of capsules or tablets, is provided. An oral particulate antitumor preparation, in which a particulate composition containing an antitumor agent is coated with a saccharide other than a cellulose derivative. 1. An oral particulate antitumor preparation , comprising a particulate composition containing an antitumor agent comprising (a) tegafur , (b) gimeracil , and (c) oteracil potassium , wherein the particulate composition is coated with a saccharide other than a cellulose derivative or mannitol.2. The oral particulate antitumor preparation according to claim 1 , wherein the saccharide is a monosaccharide or an oligosaccharide.3. The oral particulate antitumor preparation according to claim 1 , wherein the saccharide is a sugar alcohol or a disaccharide.4. The oral particulate antitumor preparation according to claim 1 , wherein the saccharide is sucrose.5. The oral particulate antitumor preparation according to claim 1 , having a dosage form of a granular preparation.6. The oral particulate antitumor preparation according to claim 1 , wherein the antitumor agent is an orally administrable form.7. The oral particulate antitumor preparation according to claim 1 , comprising (a) tegafur claim 1 , (b) gimeracil and (c) oteracil potassium at a molar ratio of 1:0.4:1.8. The oral particulate antitumor preparation according to claim 1 , comprising 0.5% to 15% by mass of tegafur in the particulate preparation coated with a coating film.9. The oral particulate antitumor preparation according to claim 1 , comprising 5% to 10% by mass of tegafur in the particulate preparation coated with a coating film. The present application is continuation of U.S. Ser. No. 12/810,540, filed Jun. 25, 2010, which is a National Stage (371) of PCT/JP08/03991, filed Dec.26, ...

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Номер записи: 1
18-04-2013 дата публикации

Biguanide Compositions and Methods of Treating Metabolic Disorders

Номер: US20130095140A1
Автор: Baron Alain D., Beeley Nigel R. A., Fineman Mark S.
Принадлежит: Elcelyx Therapeutics, Inc.

Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use. 2. A composition according to claim 1 , wherein{'sub': 2', '3', '4', '5', '6', '7, 'R, R, R, R, Rand Rare independently selected from H, methyl, ethyl, propyl or isopropyl; and'}{'sub': '1', 'Ris selected fromH,{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkenyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkynyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 3', '7', '2', '6, 'Cto Ccycloalkyl, Cto Cheterocycloalkyl, where the heterocycle comprises one or two hetero atoms selected from O, S, or N,'}{'sub': 4', '12, 'Cto Calkylcycloalkyl,'}{'sub': 3', '11, 'Cto Calkylheterocycloalkyl, where the heterocycle comprises one or two hetero atoms selected from O, S, or N and wherein N is present in the heterocyclic ring, the nitrogen atom may be in the form of an amide, carbamate or urea,'}phenyl, substituted phenyl, naphthyl, substituted naphthyl,alkylphenyl, alkylsubstituted phenyl, alkylnaphthyl, alkylsubstituted naphthyl,pyridyl, furanyl, thiophenyl, pyrrollyl, oxazolyl, isoxazolyl, thiazolyl, diazolyl, pyrazolyl ...

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Номер записи: 2
16-05-2013 дата публикации

BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE

Номер: US20130123263A1
Автор: Bayliss Tracy, Do Steven, Follkes Adrian, Goldsmith Paul, Goldsmith Richard, Heffron Tim, Kolesnikov Aleksandr, Olivero Alan G., Pegg Neil, Siu Michael, Staben Steven, Sutherlin Daniel P., Zhu Bing-Yan
Принадлежит:

Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomer solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 2. The method of wherein Xis N and Xis S.3. The method of wherein Xis S and Xis CR.6. The method of wherein the compound of formula I is selected from:N2-(2-chlorophenyl)-N2,N8,N8-trimethyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepine-2,8-dicarboxamide;7-acetamido-N-(2-chlorophenyl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepine-2-carboxamide;N2-(2-chlorophenyl)-N8-(3-(diethylamino)propyl)-N2-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepine-2,8-dicarboxamide;N-(2-chlorophenyl)-7-cyano-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepine-2-carboxamide;N-(2-chlorophenyl)-N-(2-hydroxyethyl)-4,5-dihydrobenzo[b]thieno[2,3-d]oxepine-2-carboxamide;N-(2-chloro-4-fluorophenyl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepine-2-carboxamide;N-(2,4-dichlorophenyl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepine-2-carboxamide;2-(4-isopropyl-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)-4,5-dihydrobenzo[b]thieno[2,3-d]oxepine-8-carboxamide;1-(2-(4-(2-chlorophenyl)-4H-1,2,4-triazol-3-yl)-4,5-dihydrobenzo[b]thieno[2,3-d]oxepin-8-yl)-3-methylurea;methyl 2-(4-(2-chlorophenyl)-4H-1,2,4-triazol-3-yl)-4,5-dihydrobenzo[b]thieno[2,3-d]oxepin-8-ylcarbamate;7-bromo-N-(2-chlorophenyl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepine-2-carboxamide;N-(2-(4-(2-chlorophenyl)-4H-1,2,4-triazol-3-yl)-4,5-dihydrobenzo[b]thieno[2,3-d]oxepin-8-yl)acetamide;N-(4-(3-amino-5-methyl-1H-pyrazole-1-carbonyl)-2-chlorophenyl)-N-(2-hydroxyethyl)-4,5-dihydrobenzo[b]thieno[2,3-d] ...

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Номер записи: 3
16-05-2013 дата публикации

COMPOSITIONS AND METHODS FOR TREATMENT OF INFLAMMATORY BOWEL DISORDERS AND INTESTINAL CANCERS

Номер: US20130123264A1
Автор: Browning Darren D.
Принадлежит:

Compositions and formulations useful for treating inflammatory bowel diseases, intestinal cancers, and improving the integrity of the luminal surface of the gastrointestinal tract are disclosed. Typically, the composition increases level of cGMP in the intestinal mucosa or increases the activity of a PKG, preferably PKG2, in the intestinal mucosa. Preferably, the composition includes a phosphodiesterase type 5 (PDE5) inhibitor and is targeted to the intestinal mucosa, for example by enteric coating or attachment of an intestinal specific targeting moiety. 1. A method of treating an intestinal or bowel disorder comprising administering to a subject an effective amount of a composition that increases cGMP level in the intestinal mucosa or increases the activity of a PKG in intestinal mucosa to reduce one or more symptoms of the intestinal bowel disorder.2. The method of wherein the composition comprises one or more phosphodiesterase 5 inhibitors.3. The method of wherein the phosphodiesterase 5 inhibitor is vardenafil.4. The method of wherein the intestinal bowel disorder is an inflammatory bowel disease.5. The method of wherein the inflammatory bowel disease is selected from the group consisting of Crohn's disease claim 4 , ulcerative colitis claim 4 , necrotizing enterocolitis claim 4 , collagenous colitis claim 4 , lymphocytic colitis claim 4 , ischaemic colitis claim 4 , diversion colitis claim 4 , Behçet's disease claim 4 , and indeterminate colitis. Symptoms of inflammatory disorders include abdominal pain claim 4 , vomiting claim 4 , diarrhea claim 4 , rectal bleeding claim 4 , severe internal cramps/muscle spasms in the region of the pelvis claim 4 , weight loss claim 4 , arthritis claim 4 , pyoderma gangrenosum claim 4 , and primary sclerosing cholangitis.6. The method of wherein one or more of the symptoms is selected from the group consisting of abdominal pain claim 4 , vomiting claim 4 , diarrhea claim 4 , rectal bleeding claim 4 , severe internal cramps/ ...

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Номер записи: 4
23-05-2013 дата публикации

TREATMENT OF TYPE 2 DIABETES

Номер: US20130131065A1
Автор: Bolze Sébastien, Cravo Daniel, Fouqueray Pascale, Hallakou-Bozec Sophie
Принадлежит:

The present invention relates to triazine derivatives of Formula I for their use in the treatment of Type 2 diabetes, and to compositions comprising said triazine derivatives. 111.-. (canceled)13. The method according to claim 12 , wherein at least one of R5 and R6 is a hydrogen atom.14. The method according to claim 12 , wherein R6 is a methyl group claim 12 , and R5 is a hydrogen atom.15. The method according to claim 12 , wherein R1 and R2 are methyl groups and R3 and R4 are hydrogen atoms.16. The method according to claim 12 , wherein the triazine derivative is selected in the group consisting of 2-amino-3 claim 12 ,6-dihydro-4-dimethylamino-6-methyl-1 claim 12 ,3 claim 12 ,5-triazine claim 12 , a racemic form claim 12 , tautomer claim 12 , enantiomer claim 12 , diastereoisomer and epimer thereof claim 12 , and a pharmaceutically acceptable salt thereof.17. The method according to claim 12 , wherein the triazine derivative is selected in the group consisting of (+)-2-amino-3 claim 12 ,6-dihydro-4-dimethylamino-6-methyl-1 claim 12 ,3 claim 12 ,5-triazine and a pharmaceutically acceptable salt thereof.18. The method according to claim 12 , wherein the triazine derivative is selected in the group consisting of (−)-2-amino-3 claim 12 ,6-dihydro-4-dimethylamino-6-methyl-1 claim 12 ,3 claim 12 ,5-triazine and a pharmaceutically acceptable salt thereof.19. The method according to claim 17 , wherein the pharmaceutically acceptable salt is hydrochloride.20. The method according to claim 12 , wherein the subject to be treated has pre-diabetes.21. The method according to claim 12 , wherein the subject to be treated is at an early stage of type 2 diabetes.22. The method according to claim 12 , wherein the subject to be treated has gestational diabetes. The present invention relates to triazine derivatives or compositions comprising the same for their use in the treatment of type 2 diabetes mellitus, in particular to delay the onset of type 2 diabetes or slow down its ...

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Номер записи: 5
23-05-2013 дата публикации

TREATMENT OF TYPE 1 DIABETES

Номер: US20130131066A1
Автор: Bolze Sébastien, Cravo Daniel, Fouqueray Pascale, Hallakou-Bozec Sophie
Принадлежит: POXEL

The present invention relates to triazine derivatives of formula (I) for their use in the treatment of type 1 diabetes mellitus, and to compositions comprising said triazine derivatives. 115.-. (canceled)17. The method according to claim 16 , wherein at least one of R5 and R6 is a hydrogen atom.18. The method according to claim 16 , wherein R6 is a methyl group and R5 is a hydrogen atom.19. The method according to claim 16 , wherein R1 and R2 are methyl groups and R3 and R4 are hydrogen atoms.20. The method according to claim 16 , wherein the triazine derivative is selected in the group consisting of 2-amino-3 claim 16 ,6-dihydro-4-dimethylamino-6-methyl-1 claim 16 ,3 claim 16 ,5-triazine claim 16 , a racemic form claim 16 , tautomer claim 16 , enantiomer claim 16 , diastereoisomer and epimer thereof claim 16 , and a pharmaceutically acceptable salt thereof.21. The method according to claim 16 , wherein the triazine derivative is selected in the group consisting of (+)-2-amino-3 claim 16 ,6-dihydro-4-dimethylamino-6-methyl-1 claim 16 ,3 claim 16 ,5-triazine and a pharmaceutically acceptable salt thereof.22. The method according to claim 16 , wherein the triazine derivative is selected in the group consisting of (−)-2-amino-3 claim 16 ,6-dihydro-4-dimethylamino-6-methyl-1 claim 16 ,3 claim 16 ,5-triazine and a pharmaceutically acceptable salt thereof.23. The method according to claim 21 , wherein the pharmaceutically acceptable salt is hydrochloride.24. The method according to claim 16 , wherein the subject to be treated is a patient at risk of developing type 1 diabetes.25. The method according to claim 16 , wherein the subject to be treated is a patient at an early stage of type 1 diabetes.26. The method according to claim 16 , wherein the treatment is to delay the onset of type 1 diabetes or slow down its progression.27. The method according to claim 16 , wherein the subject to be treated is an adult who suffers from Latent Autoimmune Diabetes of Adult.28. The ...

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Номер записи: 6
30-05-2013 дата публикации

COMPOUNDS AND COMPOSITIONS FOR OSSIFICATION AND METHODS RELATED THERETO

Номер: US20130137634A1
Автор: Borden Scott D., Sangadala Sreedhara
Принадлежит: EMORY UNIVERSITY

The disclosure relates to compounds and compositions for forming bone and methods related thereto. In one embodiment, the disclosure relates to a composition comprising a compound disclosed herein, such as 2,4-diamino-1,3,5-triazine derivatives or salts thereof, for use in bone growth processes. In a typical embodiment, a bone graft composition is implanted in a subject at a site of desired bone growth or enhancement. 1. A bone graft composition comprising a 2 ,4-diamino-1 ,3 ,5-triazine derivative or salt thereof.3. The bone graft composition of claim 1 , wherein the 2 claim 1 ,4-diamino-1 claim 1 ,3 claim 1 ,5-triazine derivative is a compound selected from the group consisting of:1-benzyl-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine;1-(4-methoxybenzyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine;1-(3-methoxybenzyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine;1-(4-chlorophenyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine;1-(3-chlorophenyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine;1-(3-chloro-4-methoxyphenyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine;1-(3-chloro-4-methylphenyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine;1-(4-bromo-2-fluorophenyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine;1-(2-bromo-4-methylphenyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine;6,6-dimethyl-1-(4-methyl-3-nitrophenyl)-1,6-dihydro-1,3,5-triazine-2,4-diamine;1-(3-chloro-4-fluorophenyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine;1-(3-chloro-5-fluorophenyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine;2-chloro-4-(4,6-diamino-2,2-dimethyl-1,3,5-triazin-1(2H)-yl)phenol;1-(2-chloro-5-methoxyphenyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine; and1-(2-chloro-4-methylphenyl)-4,6-diamino-1,2-dihydro-2,2-dimethyl-1,3,5-triazine or salts thereof.4. The bone graft composition of claim 1 , further comprising a growth factor.5. The bone graft composition of claim 4 , wherein the growth factor is a ...

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Номер записи: 7
06-06-2013 дата публикации

METHODS FOR PRESERVING AND/OR INCREASING RENAL FUNCTION USING XANTHINE OXIDOREDUCTASE INHIBITORS

Номер: US20130143886A1
Автор: Lademacher Christopher, MacDonald Patricia, Whelton Andrew
Принадлежит: TAKEDA PHARMACEUTICALS U.S.A., INC.

The present invention relates to methods of preserving or increasing renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof. The present invention also relates to methods of increasing renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof. 1. A method of preserving renal function in a subject in need thereof , the method comprising the step of:administering to the subject a therapeutically effective amount of at least one compound, wherein said at least one compound is a xanthine oxidoreductase inhibitor or a pharmaceutically acceptable salt thereof.2. The method of claim 1 , wherein the xanthine oxidoreductase inhibitor is selected from the group consisting of: 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methylthiazole-5-carboxylic acid claim 1 , 2-[3-cyano-4-(3-hydroxy-2-methylpropoxy)phenyl]-4-methyl-5-thiazolecarboxylic acid claim 1 , 2-[3-cyano-4-(2-hydroxy-2-methylpropoxy)phenyl]-4-methyl-5-thiazolecarboxylic acid claim 1 , 2-(3-cyano-4-hydroxyphenyl)-4-methyl-5-thiazolecarboxylic acid claim 1 , 2-[4-(2-carboxypropoxy)-3-cyanophenyl]-4-methyl-5-thiazolecarboxylic acid claim 1 , 1-(3-cyano-4-(2 claim 1 ,2-dimethylpropoxy)phenyl)-1H-pyrazole-4-carboxylic acid claim 1 , 1-3-cyano-4-(2 claim 1 ,2-dimethylpropoxy)phenyl]-1H-pyrazole-4-carboxylic acid claim 1 , pyrazolo[1 claim 1 ,5-a]-1 claim 1 ,3 claim 1 ,5-triazin-4-(1H)-one claim 1 , 8-[3-methoxy-4-(phenylsulfinyl)phenyl]-sodium salt (±) claim 1 , 3-(2-methyl-4-pyridyl)-5-cyano-4-isobutoxyphenyl)-1 claim 1 ,2 claim 1 ,4-triazole and a pharmaceutically acceptable salt thereof.3. The method of claim 1 , wherein the subject has hyperuricemia claim 1 , gout claim 1 , acute gouty arthritis claim 1 , chronic gouty joint disease claim 1 , tophaceous gout claim 1 , uric acid nephropathy or ...

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Номер записи: 8
13-06-2013 дата публикации

METHODS AND COMPOSITIONS FOR TREATING A SUBJECT FOR CENTRAL NERVOUS SYSTEM (CNS) INJURY

Номер: US20130150351A1
Автор: Carmichael Stanley T., Clarkson Andrew N., Huang Ben, Mody Istvan
Принадлежит:

Methods for treating a central nervous system (CNS) injury in a subject are provided. As of the methods include administering to the subject an effective amount of gamma aminobutyric acid (GABA) receptor signaling inhibitor to treat the subject for the CNS injury. Also provided are compositions useful in embodiments of the methods. Methods and compositions of the invention find use in the treatment of a variety of different CNS injuries, including but not limited to, treating a subject for CNS injury associated with the occurrence of stroke. 2. The method according to claim 1 , wherein the compound is administered during the recovery phase after neuronal injury.3. The method according to claim 1 , wherein the compound is administered at least 3 days after neuronal injury.4. The method according to claim 3 , wherein the compound is administered at least 7 days after neuronal injury.5. The method according to claim 1 , wherein the compound is a GABA receptor signaling inhibitory ligand.6. The method according to claim 5 , wherein the inhibitory ligand is an inverse agonist or antagonist of the GABA receptor.7. The method according to claim 6 , wherein the inhibitory ligand is an imidazo-diazepine claim 6 , a triazolo-pyridazines claim 6 , a pyrazolo-triazine claim 6 , or a dihydro-2-benzothiophen-4(5H)-one compound.8. The method according to claim 6 , wherein the linked cyclic compound is a piperidinyl-isothiazole compound.9. The method according to claim 6 , wherein the inhibitory ligand is a compound of Table 1.10. The method according to claim 6 , wherein the inverse agonist is a compound selected from the group consisting of a5IA claim 6 , PWZ-029 claim 6 , 6 claim 6 ,6-Dimethyl-3-(2-hydroxyethyl)thio-1-(thiazol-2-yl)-6 claim 6 ,7-dihydro-2-benzothiophen-4(5H)-one claim 6 , RO4938581 claim 6 , and pharmaceutically acceptable salts and mixtures thereof.11. The method according to claim 6 , wherein the inhibitory ligand is a GABA receptor antagonist.12. The method ...

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Номер записи: 9
20-06-2013 дата публикации

IDENTIFICATION OF GENE EXPRESSION AS A PREDICTIVE BIOMARKER FOR LKB1 STATUS

Номер: US20130158023A1
Автор: Chopra Rajesh, Ning Yuhong L., Worland Peter, Xu Shuichan, XU Weiming
Принадлежит: SIGNAL PHARMACEUTICALS, LLC

Provided herein are methods for predicting the LKB1 status of a patient or a biological sample, comprising the measurement of particular gene expression levels relative to a set of reference levels that represent the gene expression level of a biological wild-type sample without LKB1 gene or protein loss or mutation and the gene expression level of a reference sample with LKB1 gene or protein loss or mutation. Further provided herein are methods for treating and/or preventing a cancer or a tumor syndrome in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer or a tumor syndrome, characterized by particular gene expression levels. 1. A method for predicting LKB1 gene or protein loss or mutation in a patient's cancer , comprising:a) obtaining a biological test sample from the patient's cancer;b) obtaining the gene expression level of one or more genes selected from Table 1 in said biological sample;c) comparing said gene expression level to a set of reference levels that represent the gene expression level of a biological wild-type sample without LKB1 gene or protein loss or mutation, and the gene expression level of a reference sample with LKB1 gene or protein loss or mutation;wherein the gene expression level of the biological test sample characterized by higher similarity to the gene expression level of a reference sample with LKB1 gene or protein loss or mutation, indicates an increased likelihood of an LKB1 gene or protein loss or mutation in the patient's cancer.2. The method of claim 1 , wherein the gene expression level of the biological test sample is obtained using gene mRNA measurement.3. The method of claim 1 , wherein the gene expression level of the biological test sample is obtained using RT-PCR or Affymetrix HGU133plus2.4. The method of claim 1 , wherein the comparison of gene expression levels is performed using PAMR.5. The method of claim 1 , wherein the cancer is non-small cell lung carcinoma ...

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Номер записи: 10
20-06-2013 дата публикации

N-((1R,2S,5R)-5-(TERT-BUTYLAMINO)-2-((S)-3-(7-TERT-BUTYLPYRAZOLO[1,5-A][1,3,5]TRIAZIN-4-YLAMINO)-2-OXOPYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE, A DUAL MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESSES

Номер: US20130158039A1
Автор: CARTER Percy H., Cherney Robert J.
Принадлежит:

The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: This application is a continuation of U.S. application Ser. No. 12/901,614, filed Oct. 11, 2010 which claims the benefit of U.S. Provisional Application No. 61/250,978, filed Oct. 13, 2009, the contents of which are herein incorporated by reference in their entirety.The present invention provides N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected desirable dual activity. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide:wherein R, R, R, R, andare as described herein. Compounds that are useful intermediates of the process are also provided herein. Metabolites of active compounds, pharmaceutical compositions, and use thereof are also provided herein.Chemokines are chemotactic cytokines, of molecular weight 6-15 kDa, that are released by a wide variety of cells to attract and activate, among other cell types, macrophages, T and B lymphocytes, eosinophils, basophils and neutrophils (reviewed in: Charo et al., 354:610-621 (2006); Luster, 338:436-445 (1998); and Rollins, 90:909-928 (1997)). There are two major classes of chemokines, CXC and CC, depending on whether the first two cysteines in the amino acid sequence are separated by ...

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Номер записи: 11
04-07-2013 дата публикации

PROSTAGLANDIN TRANSPORTER INHIBITORS

Номер: US20130171171A1
Автор: Chang Young-Tae, Chi Yuling, Min JaeKi, Schuster Victor L.
Принадлежит:

The present invention generally relates to prostaglandin transport. More specifically, the invention is directed to compounds that inhibit prostaglandin transport and subsequent COX-2 induction, and methods relating thereto. 112-. (canceled)1445-. (canceled)46. A method of inhibiting COX-2 in a mammal , the method comprising administering an inhibitor of prostaglandin transporter activity to the mammal.47. The method of claim 46 , wherein the inhibitor is an antisense nucleic acid claim 46 , a ribozyme or an siRNA claim 46 , wherein the antisense nucleic acid claim 46 , the ribozyme or the siRNA is specific for the mRNA of the prostaglandin transporter.48. The method of claim 46 , wherein the inhibitor is an antibody or aptamer that specifically inhibits the prostaglandin transporter.51. The method of claim 49 , wherein R2 comprises a carboxyl or phenol group.52. The method of claim 49 , wherein R2 is a C-Cstraight or branched alkyl claim 49 , a phenyl claim 49 , a fused aryl claim 49 , a fused heteroaryl claim 49 , or any combination thereof claim 49 , optionally substituted with a halogen claim 49 , a carboxyl claim 49 , an amino claim 49 , a nitro claim 49 , a SCH claim 49 , a hydroxyl claim 49 , a C-Calkoxy claim 49 , C-Cstraight or branched alkyl claim 49 , an azido claim 49 , or a combination thereof.53. The method of claim 49 , wherein R2 is a C-Cstraight or branched alkyl claim 49 , a phenyl claim 49 , a fused aryl claim 49 , or a combination of a C-Cstraight or branched alkyl and a phenyl claim 49 , optionally substituted with a halogen claim 49 , one or more hydroxyls claim 49 , a methoxy claim 49 , a nitro claim 49 , a carboxy claim 49 , or a combination thereof.56. The method of claim 46 , wherein the mammal is a human suffering from a disease or disorder at least partially mediated by a cyclooxygenase-2.57. The method of claim 56 , wherein the disease or disorder involves pain and/or inflammation.58. The method of claim 56 , wherein the disease or ...

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Номер записи: 12
04-07-2013 дата публикации

COMBINATION OF EGCG OR METHYLATED EGCG AND A PDE INHIBITOR

Номер: US20130172356A1
Автор: Tachibana Hirofumi
Принадлежит: Kyushu University, National University Corporation

Disclosed is a medicament characterized by the combination of: epigallocatechin gallate, methylated epigallocatechin gallate, or a pharmacologically permitted salt thereof; and a phosphodiesterase inhibitor. 1. A pharmaceutical composition comprising a combination of epigallocatechin gallate or a methylated epigallocatechin gallate or a pharmaceutically acceptable salt thereof and a phosphodiesterase inhibitor.2. The composition according to claim 1 , which composition is used in treatment of cancer claim 1 , allergy claim 1 , obesity claim 1 , arteriosclerosis claim 1 , inflammation claim 1 , or muscle atrophy.3. The composition according to or claim 1 , which composition is used in treatment of a 67LR-positive disease.4. The composition according to or claim 1 , wherein the phosphodiesterase inhibitor is a phosphodiesterase 3 inhibitor or phosphodiesterase 5 inhibitor.5. The composition according to or claim 1 , wherein the phosphodiesterase inhibitor is vardenafil.6. A kit for use in treatment of cancer claim 1 , allergy claim 1 , obesity claim 1 , arteriosclerosis claim 1 , inflammation claim 1 , or muscle atrophy claim 1 , the kit comprising:a) a first unit dosage form containing epigallocatechin gallate, a methylated epigallocatechin gallate, or a pharmaceutically acceptable salt thereof;b) a second unit dosage form containing a phosphodiesterase inhibitor; andc) a container device for containing the first unit dosage form and the second unit dosage form. The present invention relates to a combination of epigallocatechin gallate (hereinafter, also referred to as “EGCG”) or a methylated epigallocatechin gallate (hereinafter, also referred to as “a methylated EGCG”) and a phosphodiesterase (hereinafter, also referred to as “PDE”) inhibitor, which is useful for prevention or treatment of a disease, in particular, a disease such as malignant tumor, allergy, obesity, arteriosclerosis, inflammation, or muscle atrophy.Cancer is a disease accounting for one-third of ...

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Номер записи: 13
01-08-2013 дата публикации

Use of isoxazoline compounds and compositions in bladder cancer

Номер: US20130196996A1
Автор: John Arthur Taylor, III, Thais Sielecki-Dzurdz
Принадлежит: CPSI STOCKHOLDER TRUST

One embodiment provides a method, comprising treating or preventing at least one disease selected from the group consisting of bladder cancer, weight loss accompanying bladder cancer, bone pain accompanying bladder cancer, bladder cancer carcinoma in-situ (CIS), TA stage bladder cancer, T1 stage bladder cancer, T2 stage bladder cancer, T3 stage bladder cancer, T4 stage bladder cancer, lymph node metastasis therefrom, solid organ metastasis therefrom, bony metastasis therefrom, cachexia/anorexia associated with bladder cancer, generalized wasting syndrome associated with bladder cancer, or a combination thereof, by administering to a subject in need thereof one or more compounds described herein, prodrug thereof, salt thereof, or a combination thereof.

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Номер записи: 14
03-10-2013 дата публикации

SEPARATION OF TRIAZINE DERIVATIVES ENANTIOMERS USING TARTARIC ACID

Номер: US20130261300A1
Автор: Cravo Daniel, Helmreich Matthias
Принадлежит: POXEL

The present invention relates to a new process of separation of triazine derivatives enantiomers involving tartaric acid. 114-. (canceled)16. The process according to claim 15 , wherein at least one of Rand Ris a hydrogen atom.17. The process according to claim 16 , wherein Rand Rare both hydrogen atoms.18. The process according to claim 15 , wherein Rand Rindependently represent C1 to C3 alkyl groups.19. The process according to claim 18 , wherein at least one alkyl group is methyl.20. The process according to claim 15 , wherein the compound of formula (I) is in the form of a salt claim 15 , in particular hydrochloride salt.21. The process according to claim 15 , wherein the triazine derivative of formula (I) is chosen in the group consisting of:2-amino-3,6-dihydro-4-dimethylamino-6-methyl-1,3,5-triazine,2-amino-6-cyclohexyl-3,6-dihydro-4-dimethylamino-1,3,5-triazine,and a salt thereof.22. The process according to claim 20 , wherein the triazine derivative is 2-amino-3 claim 20 ,6-dihydro-4-dimethylamino-6-methyl-1 claim 20 ,3 claim 20 ,5-triazine hydrochloride.23. The process according to claim 15 , wherein step 1 is performed with a salt of the triazine derivative as starting material.24. The process according to claim 23 , wherein a base is present in the reaction medium.25. The process according to claim 24 , wherein the base is triethylamine.26. The process according to claim 15 , wherein step 1 is performed by the reaction of a triazine derivative of formula (I) with L-(+)-tartaric acid.27. The process according to claim 15 , wherein step 1 is performed in a solvent.28. The process according to claim 27 , wherein the solvent of step 1 is methanol.29. The process according to claim 15 , wherein step 2 is performed by filtration or by centrifugation.30. The process according to claim 15 , wherein step 3 is performed in a solvent.31. The process according to claim 30 , wherein the solvent of step 3 is ethanol.32. The process according to claim 15 , wherein step ...

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Номер записи: 15
17-10-2013 дата публикации

Composition For Prevention of Vasoactivity in the Treatment of Blood Loss and Anemia

Номер: US20130274245A1
Автор: BLUMENSTEIN Jan
Принадлежит:

The present invention relates to the prevention of cardiovascular and central nervous system side effects in mammals who receive transfusions of hemoglobin based oxygen carriers (HBOC) or stored blood products containing a concentration of hemoglobin sufficient to induce vasoconstriction, by adding a vasoactivity reducing effective amount of one or more phosphodiesterase inhibitors in combination with a calcium channel blocker and/or an alpha agonist, to the circulation, or alternatively to the HBOC or stored blood, thereby preventing the manifestation of vasoactivity attributable to the presence of free tetrameric hemoglobin (Hb). 1. A process for reducing or preventing vasoactivity induced by the introduction of a composition containing a hemoglobin based oxygen carrier (HBOC) , free hemoglobin (Hb) , stored blood products having vasoactivity inducing concentrations of free tetrameric hemoglobin , and combinations thereof comprising:combining at least one phosphodiesterase inhibitor (PDE) with an additional agent selected from the group consisting of at least one calcium channel blocker, at least one alpha antagonist, and combinations thereof, with an HBOC or Hb containing material, in an amount effective to reduce or prevent said vasoactivity.2. The process of wherein said phosphodiesterase inhibitors are selected from the group consisting of 5-(2-Propoxyphenyl)-1H-[1 claim 1 ,2 claim 1 ,3]triazolo[4 claim 1 ,5-d]pyrimidin-7(4H)-one claim 1 , 2-o-propoxyphenyl-8-azapurine-6-one claim 1 , 1-cyclopentyl-3-methyl-6-(4-pyridyl)pyrazolo[3 claim 1 ,4-d]pyrimidin-4-(5H)-one claim 1 , SCH 48936 ((+)-6a claim 1 ,7 claim 1 ,8 claim 1 ,9 claim 1 ,9a claim 1 , 10 claim 1 ,11 claim 1 ,1 1a-octahydro-2 claim 1 ,5-dimethyl-3H-pentalen(6a claim 1 ,1 claim 1 ,4 claim 1 ,5)imidazo[2 claim 1 ,1- b]purin-4(5H)-one claim 1 , 2-phenyl-8-ethoxycycloheptimidazole claim 1 , sodium 1-[6-chloro-4-(3 claim 1 ,4-methylenedioxybenzyl)-aminoquinazolin-2-y]piperidine-4-carboxylate sesquihydrate ...

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Номер записи: 16
07-11-2013 дата публикации

HIGH DRUG LOAD TABLET FORMULATION OF [(1R), 2S]-2-AMINOPROPIONIC ACID 2-[4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-5-METHYLPYRROLO[2,1-f][1,2,4]TRIAZIN-6-YLOXY]-1-METHYLETHYL ESTER

Номер: US20130296325A1
Автор: Badawy Sherif Ibrahim Farag, Bindra Dilbir S., LaMarche Keirnan Ryan, Narang Ajit S., Rao Venkatramana M., Subramanian Ganeshkumar A.
Принадлежит: BRISTOL-MYERS SQUIBB COMPANY

The present invention is directed to a high drug load tablet formulation of [(1R),2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester, and to methods of using the formulation in the treatment of cancer. The tablet is obtained by means of a wet granulation process. 2. The formulation of wherein the active pharmaceutical ingredient is included in the range of 30-80% w/w claim 1 , one or more fillers is included in the range of 15-65% w/w claim 1 , the binder is included in the range of 1-20% w/w claim 1 , one or more disintegrants is included in the range of 1-20% w/w claim 1 , and the lubricant is included in the range of 0.25-2.5% w/w.3. The formulation of wherein the active pharmaceutical ingredient is included in the range of 40-70% w/w claim 2 , one or more fillers is included in the range of 25-55% w/w claim 2 , the binder is included in the range of 2-12% w/w claim 2 , one or more disintegrants is included in the range of 2-12% w/w claim 2 , and the lubricant is included in the range of 0.75-1.5% w/w.4. The formulation of wherein the active pharmaceutical ingredient is included in about 50% w/w claim 3 , one or more fillers is included in about 24.5% w/w claim 3 , the binder is included in about 3% w/w claim 3 , one or more disintegrants is included in 3% w/w claim 3 , the glidant is included in about 0.5% w/w and the lubricant is included in about 1.0% w/w.5. The formulation of wherein the fillers and disintegrants are intragranular and extragranular.6. The formulation of wherein the fillers are selected from lactose monohydrate and microcrystalline cellulose.7. The formulation of wherein the binder is hydroxypropyl cellulose (HPC) claim 4 , polyvinyl pyrrolidone (PVP) claim 4 , starch or hydroxypropyl methylcellulose (HPMC).8. The formulation of wherein the disintegrants are selected from croscarmellose sodium claim 4 , crospovidone claim 4 , starch and sodium starch glycolate.9 ...

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Номер записи: 17
14-11-2013 дата публикации

Methods for the prevention and/or treatment of memory impairment

Номер: US20130302352A1
Автор: Orser Beverley A.
Принадлежит: THE GOVERNING COUNCIL OF THE UNIVERSITY OF TORONTO

The present invention relates to methods for the prevention and/or treatment of memory impairment and for improving memory and particularly to methods for the prevention and/or treatment of memory impairment and improving memory comprising administering an agent that decreases activity of a GABAreceptor. The present invention also relates the use of an agent that decreases activity of a GABAreceptor for preventing or treating a memory deficit and for improving memory. 1. A method for preventing or treating a memory deficit , comprising administering an agent that decreases activity of a GABAreceptor , wherein the memory deficit is induced by inflammation or IL-1β.2. The method of claim 1 , wherein the memory deficit is short-term memory loss.3. The method of claim 1 , wherein the memory deficit is long-term memory loss.4. The method of claim 1 , wherein the GABAreceptor is an α5GABAreceptor.5. The method of claim 1 , wherein the agent decreases activity of the GABAreceptor by inhibiting agonist interaction with the GABAreceptor.6. The method of claim 5 , wherein the agent is an antibody.7. The method of claim 5 , wherein the agent is an antagonist.8. The method of claim 5 , wherein the agent decreases activity of the GABAreceptor by binding to the GABAreceptor and wherein the agent is an inverse agonist selected from the group consisting of L-655 claim 5 ,708 claim 5 , MRK-016 and combinations thereof.9. The method of claim 5 , wherein the agent inhibits interaction of IL-1β with the GABAreceptor.10. A method for improving memory comprising administering an agent that decreases activity of a GABAreceptor claim 5 , wherein memory is improved following an inflammatory reaction or an increase in IL-1β expression and/or activity.11. The method of claim 10 , wherein the memory is short-term memory.12. The method of claim 10 , wherein the memory is long-term memory.13. The method of claim 10 , wherein the GABAreceptor is an α5GABAreceptor.14. The method of claim 10 , ...

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Номер записи: 18
21-11-2013 дата публикации

COMBINATION OF INSULIN WITH TRIAZINE DERIVATIVES AND ITS USE FOR TREATING DIABETES

Номер: US20130310312A1
Автор: AUDET Annick, Cravo Daniel, MESANGEAU Didier
Принадлежит:

The invention relates to a composition for use as a medicament comprising insulin in combination with at least one compound of formula (I) 115.-. (canceled)17. The method of claim 16 , wherein the composition further comprises one or more pharmaceutically acceptable adjuvants.18. The method of claim 16 , wherein the compound of formula (I) is 5 claim 16 ,6-dihydro-4-dimethylamino-2-imino-6-methyl-1 claim 16 ,3 claim 16 ,5-triazine.19. The method of claim 16 , wherein the insulin is in fixed combination with the compound of formula (I) in a single dosage unit.20. The method of claim 16 , wherein the insulin and the compound of formula (I) are in separate dosage units in a single package.21. The method of claim 16 , wherein claim 16 , as a result of the method claim 16 , glucose tolerance and/or insulin secretion in response to glucose are increased.22. The method of claim 16 , wherein the compound of formula (I) is administered in a dose range from 25 to 200 mg per kg of body weight.23. A method according to claim 16 , wherein the insulin and the compound of formula (I) are administered simultaneously.24. A method according to claim 16 , wherein the insulin and the compound of formula (I) are administered sequentially.25. The method of claim 16 , for the therapeutic treatment of a disease associated with insulin resistance.26. The method according to claim 25 , wherein the disease treated is selected from the group consisting of diabetes claim 25 , pre-diabetes claim 25 , low glucose tolerance claim 25 , hyperglycemia claim 25 , metabolic syndrome claim 25 , diabetic nephropathy claim 25 , neuropathy claim 25 , retinopathy claim 25 , arteriosclerosis and cardiovascular disease.27. The method according to claim 25 , wherein the disease treated is selected from the group consisting of insulin dependent diabetes mellitus and non-insulin dependent diabetes mellitus.28. The method according to claim 25 , wherein the compound of formula (I) and/or physiologically ...

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Номер записи: 19
28-11-2013 дата публикации

Pharmaceutical Composition Comprising (1r,4r)-6'-fluoro-N, N-dimethyl-4-phenyl-4,9' -dihydro-3'H-spiro[cyclohexane-1,1' -pyrano[3,4,b]indol]-4-amine and an Anticonvulsant

Номер: US20130317009A1
Автор: Christoph Thomas, FROSCH Stefanie, LINZ Klaus
Принадлежит: GRUENENTHAL GmbH

The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6′-fluoro-N,N-dimethyl-4-phenyl-4′,9′-dihydro-3′H-spiro[cyclohexane-1,1′-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient which is an anticonvulsant selected from the group consisting of retigabin, lamotrigine, lacosamide, levetiracetam, carbamazepine, sultiame, phenacemide, felbamate, topiramate, pheneturide, brivaracetam, selectracetam, zonisamide, stiripentol, beclamide, mexiletin, ralfinamide, methylphenobarbital, phenobarbital, primidone, barbexaclone, metharbital, ethotoin, phenyloin, amino(diphenylhydantoin) valeric acid, mephenyloin, fosphenyloin, paramethadione, trimethadione, ethadione, ethosuximide, phensuximide, mesuximide, clonazepam, lorazepam, diazepam, clobazam, oxcarbazepine, eslicarbazepine, rufinamide, valproic acid, valpromide, aminobutyric acid, progabide, tiagabine, and the physiologically acceptable salts thereof. 1. A pharmaceutical composition comprising:(a) a first pharmacologically active ingredient selected from (1r,4r)-6′-fluoro-N,N-dimethyl-4-phenyl-4′,9′-dihydro-3′H-spiro[cyclohexane-1,1′-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and(b) a second pharmacologically active ingredient which is an anticonvulsant selected from the group consisting of retigabin, lamotrigine, lacosamide, levetiracetam, carbamazepine, sultiame, phenacemide, felbamate, topiramate, pheneturide, brivaracetam, selectracetam, zonisamide, stiripentol, beclamide, mexiletin, ralfinamide, methylphenobarbital, phenobarbital, primidone, barbexaclone, metharbital, ethotoin, phenyloin, amino(diphenylhydantoin) valeric acid, mephenyloin, fosphenyloin, paramethadione, trimethadione, ethadione, ethosuximide, phensuximide, mesuximide, clonazepam, lorazepam, diazepam, clobazam, oxcarbazepine, eslicarbazepine, rufinamide, valproic acid, ...

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Номер записи: 20
06-02-2014 дата публикации

NOVEL USE FOR IMIDAZOTRIAZINONES

Номер: US20140038967A1
Автор: Hasse Birgit, Koopmans Guido
Принадлежит: ALGIAX PHARMACEUTICALS GMBH

Provided herein are compounds for use in the treatment of central nervous system (CNS)-trauma related disorders like spinal cord injuries. Pharmaceutical compositions, single unit dosage forms, and kit suitable for use for the treatment of (CNS)-trauma related disorders are also disclosed. 1. A compound for the use in treating of a central nervous system trauma related disorder , wherein the compound is an imidazotriazinone.4. The compound of claim 3 , wherein the stereoisomer of the compound is the R or S enantiomer.5. The compound of claim 3 , wherein the central nervous system trauma related disorder is selected from the group consisting of a complete spinal cord injury claim 3 , an incomplete spinal cord injury claim 3 , a spinal cord contusion claim 3 , a spinal cord compression claim 3 , a spinal cord trauma claim 3 , a spinal injury claim 3 , paraplegia claim 3 , quadriplegia claim 3 , tetraplegia claim 3 , central cord syndrome claim 3 , Brown-Séquard syndrome claim 3 , anterior cord syndrome claim 3 , conus medullaris syndrome claim 3 , cauda equina syndrome claim 3 , traumatic brain injury claim 3 , TBI claim 3 , brain injury claim 3 , brain damage claim 3 , head injury claim 3 , diffuse axonal injury (DAT) claim 3 , head trauma claim 3 , brain concussion claim 3 , brain contusion claim 3 , subdural hematoma claim 3 , epidural hematoma claim 3 , subarachnoid hemorrhage claim 3 , intracerebral hemorrhage claim 3 , or CNS compression.6. The compound of claim 3 , wherein the central nervous system trauma related disorder is a spinal cord injury.7. The compound of claim 3 , wherein the central nervous system trauma related disorder is a spinal cord contusion.8. A pharmaceutical composition for the use in the treatment of central nervous system trauma related disorders comprising an imidazotriazinone in free form or in the form of pharmaceutically acceptable salt or physiologically functional derivative claim 3 , together with pharmaceutically acceptable ...

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Номер записи: 21
20-02-2014 дата публикации

COMBINATION OF TRIAZINE DERIVATIVES AND INSULIN SENSITISERS

Номер: US20140050786A1
Автор: Cravo Daniel, MESANGEAU Didier, Moinet Gerard
Принадлежит: POXEL SAS

The present invention relates to combinations of triazine derivatives and of insulin sensitisers. 2. The pharmaceutical composition according to claim 1 , comprising a compound of the formula (I) in which R5 is hydrogen.3. The pharmaceutical composition according to claim 1 , comprising a compound of the formula (I) in which R5 and R6 are independently chosen from H and (C1-C20)alkyl groups optionally substituted by hydroxyl claim 1 , halogen claim 1 , (C1-C5)alkyl claim 1 , (C6-C14)aryloxy or trifluoromethyl.4. The pharmaceutical composition according to claim 1 , wherein R1 claim 1 , R2 claim 1 , R3 and R4 are independently chosen from H and (C1-C20)alkyl groups optionally substituted by (C1-C5)alkyl.5. (canceled)6. The pharmaceutical composition according to claim 1 , comprising a compound of the formula (I) in which R1 and R2 are a methyl group and R3 and R4 represent a hydrogen.7. The pharmaceutical composition according to claim 1 , wherein the compound of formula (I) is 2-amino-3 claim 1 ,6-dihydro-4-dimethylamino-6-methyl-1 claim 1 ,3 claim 1 ,5-triazine claim 1 , or a pharmaceutically acceptable salt thereof.8. The pharmaceutical composition according to claim 1 , wherein the compound of formula (I) is (−)-2-amino-3 claim 1 ,6-dihydro-4-dimethylamino-6-methyl-1 claim 1 ,3 claim 1 ,5-triazine claim 1 , or a pharmaceutically acceptable salt thereof.9. The pharmaceutical composition according to claim 1 , wherein the compound of formula (I) is (+)-2-amino-3 claim 1 ,6-dihydro-4-dimethylamino-6-methyl-1 claim 1 ,3 claim 1 ,5-triazine claim 1 , or a pharmaceutically acceptable salt thereof.10. The pharmaceutical composition according to claim 1 , wherein the compound of the formula (I) is in the form of a hydrochloride salt.1112-. (canceled)13. The pharmaceutical composition according to claim 1 , wherein the insulin sensitiser is selected from the group consisting of rosiglitazone and pioglitazone.14. (canceled)15. The pharmaceutical composition according to ...

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Номер записи: 22
20-02-2014 дата публикации

TREATMENT OF ERECTILE DYSFUNCTION AND OTHER INDICATIONS

Номер: US20140051707A1
Автор: Fossel Eric T.
Принадлежит: Strategic Science & Technologies, LLC

The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising a phosphodiesterase type 5 inhibitor and/or a salt thereof, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these. 1169-. (canceled)170. A transdermal patch for application to the skin of a subject , the transdermal patch comprising a composition comprising:an ionic strength of at least about 0.25 M;a stabilization polymer comprising xanthan gum;propylene glycol;a polysorbate surfactant comprising polysorbate 20; anda phosphodiesterase type 5 inhibitor and/or a salt thereof.171. The transdermal patch of claim 170 , wherein the composition further comprises a nitric oxide donor.172. The transdermal patch of claim 171 , wherein the nitric oxide donor comprises L-arginine and/or an L-arginine salt.173. The transdermal patch of claim 172 , wherein the nitric oxide donor comprises L-arginine.174. The transdermal patch of claim 172 , wherein the nitric oxide donor comprises L-arginine hydrochloride.175. The transdermal patch of claim 171 , wherein the nitric oxide donor is present at at least about 0.5% by weight of the composition.176. The transdermal patch of claim 170 , wherein the composition comprises sodium chloride.177. The transdermal patch of claim 176 , wherein the sodium chloride is present at at least about 5% by weight of the ...

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Номер записи: 23
27-03-2014 дата публикации

TAZOBACTAM ARGININE COMPOSITIONS

Номер: US20140088067A1
Автор: Damour Nicole Miller, Gu Jian-Qiao, Jurkauskas Valdas, Lai Jan-Ji, Pathare Pradip M., Terracciano Joseph
Принадлежит: Cubist Pharmaceuticals, Inc.

This disclosure provides compositions containing solid forms of tazobactam arginine, and methods of manufacturing and using these compositions. 1. A method for the treatment of bacterial infections in a mammal , comprising administering to said mammal a therapeutically effective amount of a pharmaceutical composition comprising tazobactam arginine polymorph Ia.2. The method of wherein the mammal is human.3. A method for the treatment of bacterial infections in a mammal claim 1 , comprising administering to said mammal a therapeutically effective amount of a pharmaceutical composition comprising a beta-lactam compound and tazobactam arginine polymorph Ia.4. The method of wherein the mammal is a human.5. A pharmaceutical composition comprising tazobactam arginine polymorph Ia and one or more beta-lactam compounds claim 3 , and a pharmaceutically acceptable carrier or diluent.6. A pharmaceutical composition prepared by a method comprising the step of combining tazobactam arginine polymorph Ia and a beta-lactam compound. This application is a continuation of U.S. patent application Ser. No. 13/628,742, the contents of which are incorporated herein by reference.This disclosure relates to solid forms of (2S,3S,5R)-3-((1H-1,2,3-triazol-1-yl)methyl)-3-methyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid 4,4-dioxide (tazobactam), and related compositions and methods.The crystal state of a compound may be important when the compound is used for pharmaceutical purposes. Compared with an amorphous solid, the solid physical properties of a crystalline compound may change, which may affect its suitability for pharmaceutical use. For example, a particular crystalline compound may overcome the disadvantage of other solid forms of the compound that readily absorb moisture (e.g., high hygroscopicity). For an ionic drug substance, high hygroscopicity may diminish the drug product's stability profile by a host of mechanisms, as the drug substance may have a propensity to ...

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Номер записи: 24
07-01-2016 дата публикации

PHARMACEUTICAL COMPOSITIONS OF CETP INHIBITORS

Номер: US20160000799A1
Автор: Damle Shantanu Yeshwant, Gandhi Rajesh, Nekkanti Vijay Kumar, Padhi Bijay Kumar, Raghuvanshi Rajeev Singh
Принадлежит:

The present application discloses a pharmaceutical composition comprising a class of cholesteryl ester transfer protein (CETP) inhibitors with improved oral bioavailability. The application further discloses compositions comprising a class of CETP inhibitor and at least one surfactant in the form of a solution, suspension, emulsion or a pre-concentrate. 2. (canceled)6. The composition according to claim 1 , wherein the surfactant is hydrophilic claim 1 , hydrophobic or mixtures thereof.7. The composition according to claim 1 , wherein the surfactant comprises from about 1% to about 90% weight of the composition.8. The composition according to claim 6 , wherein the hydrophilic surfactant is anionic claim 6 , cationic claim 6 , zwitterionic or non-ionic.9. The composition according to claim 8 , wherein the anionic surfactant is selected from group consisting of fatty acid salts claim 8 , bile salts claim 8 , phospholipids claim 8 , phosphoric acid esters claim 8 , carboxylates claim 8 , acyl lactylates claim 8 , alginate salts claim 8 , sulfates and sulfonates claim 8 , cationic surfactants and combinations thereof.1017-. (canceled)18. The composition according to claim 8 , wherein the cationic surfactant is selected from group comprising lauroyl carnitine claim 8 , palmitoyl carnitine claim 8 , myristoyl carnitine claim 8 , hexadecyl triammonium bromide claim 8 , decyl trimethyl ammonium bromide claim 8 , cetyl trimethyl ammonium bromide claim 8 , dodecyl ammonium chloride claim 8 , alkyl benzyldimethylammonium salts claim 8 , diisobutyl phenoxyethoxydimethyl benzylammonium salts claim 8 , alkylpyridinium salts claim 8 , betaines (trialkylglycine): lauryl betaine (N-lauryl claim 8 , N claim 8 ,N-dimethylglycine) claim 8 , ethoxylated amines: polyoxyethylene-15 coconut amine and combinations thereof.19. The composition according to claim 8 , wherein the non-ionic surfactant is selected from group comprising polyethoxylated fatty Acids claim 8 , PEG fatty acid diesters ...

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Номер записи: 25
02-01-2020 дата публикации

VACUOLE-INDUCING COMPOUNDS, METHODS OF MAKING AND USING THE SAME

Номер: US20200000789A1
Автор: Erhardt Paul W., Li Zehui, Maltese William A., Trabbic Christopher J.
Принадлежит: The University of Toledo

Vacuole- or exosome-inducing indole-based chalcone and substituted triazole-hydrazone compounds that induce endosomal vacuolization and increase exosome yield, but do not trigger growth arrest or cell death, and methods of making and using are described. 1. A method for increasing exosome production in a cell , comprising: exposing the cell to an indole-pyridinyl-propenone compound that induces endosomal vacuolization but does not trigger growth arrest or cell death.3. The method of claim 2 , wherein R═OCH; and claim 2 , R′═H claim 2 , CHCHCH claim 2 , CH(CH) claim 2 , or CHCH(CH).4. The method of claim 3 , wherein R═OCH claim 3 , and R′═CHCHCH.5. The method of claim 2 , wherein R═OH claim 2 , OCHCH claim 2 , OCH(CH) claim 2 , NHCOCHor NHCOC(CH); and claim 2 , R′═CH.6. The method of claim 5 , wherein R═OCHCH; and claim 5 , R′═CH.7. The method of claim 2 , wherein R═OCHCH; and R′═CHCHCH.8. The method of claim 1 , wherein exosomes are collected by one or more of the following: ultracentrifugation; column chromatography; size exclusion; and filtration through a device containing an affinity matrix that is selective toward exosomes.9. A method using exosomes produced by claim 1 , comprising harvesting the exosomes for use as nanocarriers for packaging and delivery of a therapeutic material to a subject in need thereof.10. The method of claim 9 , wherein the therapeutic material comprises one or more of: small molecules claim 9 , miRNAs claim 9 , and proteins.11. The method of claim 1 , wherein the cell comprises one or more of: multipotent mesenchymal stromal cells; stem cells; and claim 1 , cancer cells.12. The method of claim 1 , wherein the cell is a mammalian cell.13. A method of producing transiently expressed miRNA containing cells claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'transfecting a cell population of cells capable of producing exosomes produced according to the method of with one or more plasmids encoding miRNA;'}harvesting ...

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Номер записи: 26
02-01-2020 дата публикации

Pro-drugs of riluzole and their method of use for the treatment of amyotrophic lateral sclerosis

Номер: US20200000818A1
Автор: Allen B. Reitz, Garry Robert Smith
Принадлежит: Biohaven Pharmaceutical Holding Co Ltd

Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.

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Номер записи: 27
07-01-2016 дата публикации

COMBINATION THERAPY FOR TREATING CANCER AND METHOD FOR TREATING CANCER USING A COMBINATION THERAPY

Номер: US20160001052A1
Автор: Zucker Shoshanna
Принадлежит:

A combination therapy for treating cancer including a DNA damaging agent deliverable to cancer cells and operatively arranged to activate only under a low oxygen condition and a non-thermal plasma deliverable to cancer cells. The non-thermal plasma and the DNA damaging agent individually and in conjunction promote cell toxicity. 1. A combination therapy for treating cancer , comprising:a DNA damaging agent deliverable to cancer cells and operatively arranged to activate only under a hypoxia condition; and,a non-thermal plasma deliverable to cancer cells;wherein said non-thermal plasma and said DNA damaging agent individually and in conjunction promote cell toxicity.2. The combination therapy for treating cancer as recited in claim 1 , wherein said non-thermal plasma is generated from mixing helium gas and atmospheric gases and ionizing the mixed gases.3. The combination therapy for treating cancer as recited in claim 1 , wherein said DNA damaging agent is tirapazamine.4. The combination therapy for treating cancer as recited in claim 1 , wherein said cell toxicity is achieved via apoptosis.5. The combination therapy for treating cancer as recited in claim 1 , wherein said cell toxicity is achieved via necrosis.6. The combination therapy for treating cancer as recited in claim 1 , wherein said non-thermal plasma is deliverable via a plasma torch.7. The combination therapy for treating cancer as recited in claim 1 , wherein said DNA damaging agent is deliverable via injection.8. The combination therapy for treating cancer as recited in claim 1 , wherein said non-thermal plasma is deliverable via a plasma torch and said cancer is treated with said non-thermal plasma for at least one treatment which lasts for at least 10 seconds.9. The combination therapy for treating cancer as recited in claim 1 , wherein said cancer cells are manipulated to overexpress functional gap junctions.10. The combination therapy for treating cancer as recited in claim 1 , wherein said non- ...

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Номер записи: 28
11-01-2018 дата публикации

Compositions and Methods for Treating Metabolic Disorders

Номер: US20180008561A1
Автор: Baron Alain D., Beeley Nigel R. A., Fineman Mark S.
Принадлежит:

Methods for improving the gastrointestinal tolerability of biguanide compounds and for treating metabolic disorders and/or inducing weight loss in patients in need thereof, particularly in individuals having a contraindication for treatment with biguanide compounds, are provided comprising administering delayed release formulations of such biguanide compounds, including metformin, targeted to the small intestine. 1. A method of improving the gastrointestinal tolerability of and/or reducing gastrointestinal complications resulting from biguanide administration , comprising administering a therapeutically effective amount of a biguanide compound in a delayed-release formulation to a patient in need thereof.2. A method of treating metabolic disorders in a patient in need thereof , comprising administering a therapeutically effective amount of a biguanide compound to said patient in a delayed-release formulation , wherein said patient has a contraindication for the biguanide compound.3. The method according to claim 2 , wherein the patient has a contraindication selected from the group consisting of a hypoxic condition claim 2 , impaired lactate clearance claim 2 , and impaired clearance of the biguanide compound.4. The method according to claim 3 , wherein the patient has a hypoxic condition.5. The method according to claim 3 , wherein the patient has impaired lactate clearance.6. The method according to claim 3 , wherein the patient has impaired clearance of the biguanide compound.7. The method according to claim 3 , wherein the patient has moderate renal impairment claim 3 , severe renal impairment claim 3 , or endstage renal disease which results in impaired clearance of the biguanide compound.8. The method according to claim 3 , wherein the patient has chronic kidney disease.9. The method according to any one of the preceding claims claim 3 , wherein the patient in need thereof has hyperglycemia.10. The method according to claim 9 , wherein the hyperglycemia is ...

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Номер записи: 29
19-01-2017 дата публикации

PHARMACEUTICAL ADMINISTRATION SYSTEM FOR THE TRANSDERMAL APPLICATION OF VARDENAFIL

Номер: US20170014417A1
Автор: Lipp Ralph
Принадлежит: LIPP LIFE SCIENCES LLC

A pharmaceutical administration system for the transdermal application of at least one active agent includes vardenafil and/or a pharmaceutically acceptable salt thereof as the active agent and a pharmaceutically acceptable carrier providing a solution of the at least one active agent in the administration system. Another active agent may be testosterone. This system can be used to systemically deliver therapeutic doses of vardenafil and/or a pharmaceutically acceptable salt thereof and optionally testosterone in order to treat benign prostatic hyperplasia, erectile dysfunction, male hypogonadism, pulmonary hypertension, and/or pulmonary arterial hypertension. 1. A pharmaceutical administration system for the transdermal application of at least one active agent , comprising:vardenafil and/or a pharmaceutically acceptable salt thereof as the active agent; anda pharmaceutically acceptable carrier providing a solution of the at least one active agent in the administration system, wherein the pharmaceutically acceptable carrier comprises at least one transdermal penetration enhancer;wherein the system comprises an amount of penetration enhancer that is greater than an amount of vardenafil.2. A pharmaceutical administration system for the transdermal application of at least one active agent , comprising:vardenafil and/or a pharmaceutically acceptable salt thereof as the active agent;testosterone as another active agent; anda pharmaceutically acceptable carrier providing a solution of the at least one active agent in the administration system.3. The system according to claim 1 , wherein a content of vardenafil and/or a pharmaceutically acceptable salt thereof in the system is 0.1-15% by weight.4. The system according to claim 2 , wherein a content of testosterone in the system is 0.1-15% by weight.5. The system according to claim 1 , wherein the pharmaceutically acceptable carrier is an alcohol and/or a polyol or a mixture of alcohols and/or polyols.6. The system ...

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Номер записи: 30
28-01-2016 дата публикации

NOVEL USE FOR IMIDAZOTRIAZINONES

Номер: US20160022688A1
Автор: Hasse Birgit, Koopmans Guido
Принадлежит:

Use of compounds in the treatment of central nervous system (CNS)-trauma related disorders like spinal cord injuries. Pharmaceutical compositions, single unit dosage forms, and kit suitable for use for the treatment of (CNS)-trauma related disorders are also disclosed. 2. The method of claim 1 , wherein the stereoisomer of the compound is the R or S enantiomer.3. The method of claim 1 , wherein the central nervous system trauma related disorder is selected from the group consisting of a complete spinal cord injury claim 1 , an incomplete spinal cord injury claim 1 , a spinal cord contusion claim 1 , a spinal cord compression claim 1 , a spinal cord trauma claim 1 , a spinal injury claim 1 , paraplegia claim 1 , quadriplegia claim 1 , tetraplegia claim 1 , central cord syndrome claim 1 , Brown-Séquard syndrome claim 1 , anterior cord syndrome claim 1 , conus medullaris syndrome claim 1 , cauda equina syndrome claim 1 , traumatic brain injury claim 1 , TBI claim 1 , brain injury claim 1 , brain damage claim 1 , head injury claim 1 , diffuse axonal injury (DAI) claim 1 , head trauma claim 1 , brain concussion claim 1 , brain contusion claim 1 , subdural hematoma claim 1 , epidural hematoma claim 1 , subarachnoid hemorrhage claim 1 , intracerebral hemorrhage claim 1 , or CNS compression.4. The method of claim 1 , wherein the central nervous system trauma related disorder is a spinal cord injury. The technology provided herein relates to the novel use of imidazotriazinones derivatives in the treatment of central nervous system (CNS)-trauma related disorders.Central nervous system (CNS) trauma, caused by injuries such as spinal and head injuries, cause, when not-fatal, devastating physical and psychological effects to the human body. Many of these injuries are caused by common events such as automobile accidents, serious falls, diving accidents, crushing industrial injuries and gunshot or stab wounds.Spinal cord injury (SCI) and traumatic brain injury (TBI) cause tissue ...

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Номер записи: 31
28-01-2016 дата публикации

Triazine compound for resisting coccidiosis in chickens

Номер: US20160022689A1
Автор: FAN Chao, Fei Chenzhong, LI Tao, WANG CHUNMEI, Wang Mi, Wang Xiaoyang, Xiao Sui, XIAO Wenlong, Xue Feiqun, Zhang Depeng, Zhang Keyu, ZHANG Lifang, Zheng Wenli
Принадлежит:

This invention is involved in the field of pharmaceutical technology. It is related to a triazine compound for resisting coccidiosis in chickens, its preparation method and application. This compound has the structure below. The invented drug has good efficacy, low toxicity and is suitable for treating animal coccidiosis 2. An application of the compound mentioned in claim 1 , with the peculiarity that this compound is used to prepare drugs for resisting coccidiosis in chickens.3. A pharmaceutical composition for resisting coccidiosis in chickens claim 1 , which is characterized in comprising: a significant amount of the triazine compound as recited in claim 1 , a corresponding medicinal salt and a medicinal carrier thereof. This is a U.S. National Stage under 35 U.S.C 371 of the International Application PCT/CN2014/090460, filed Nov. 6, 2014, which claims priority under 35 U.S.C. 119(a-d) to CN 201310552795.2, filed Nov. 8, 2013.1. Field of InventionThis invention relates to a compound and its synthesis, and more particularly to a new triazine compound for resisting coccidiosis in chickens, its preparation method and applications.2. Description of Related ArtsChicken coccidiosis which is prevalent around the world is an important disease threatening intensive chicken farm. It is induced by parasites in the enterocyte.At present, there are two main methods for preventing chicken coccidiosis: vaccines and anticoccidial drugs. Although certain achievements have been made in the development and application of live coccidiosis vaccines, subunit vaccines and recombinant vaccines, the prevention and treatment of coccidiosis mainly depend on drugs. The development of anticoccidial drugs has significant effects on reducing the hazard of coccidiosis and the loss of chicken farm, and ensuring the development of poultry industry.However, drug resistance caused by the long term usage of only one type of anticoccidial drug has been a veterinary clinical problem to be solved. ...

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Номер записи: 32
17-04-2014 дата публикации

METHOD FOR SELECTING CHEMOTHERAPY FOR GASTRIC CANCER PATIENT USING COMBINATION DRUG OF TEGAFUR, GIMERACIL AND OTERACIL POTASSIUM AND EGFR INHIBITOR

Номер: US20140105893A1
Автор: Kobunai Takashi, Saito Hitoshi, Takechi Teiji
Принадлежит: TAIHO PHARMACEUTICAL CO., LTD.

A method for predicting a therapeutic effect of chemotherapy with a combination drug containing tegafur, gimeracil, and oteracil potassium in a gastric cancer patient by: 1. A method for predicting a therapeutic effect of chemotherapy with a combination drug containing tegafur , gimeracil , and oteracil potassium in a gastric cancer patient , the method comprising the steps of:(1) measuring an expression level of EGFR contained in a biological sample obtained from the patient;(2) comparing the expression level of EGFR obtained in step (1) with a corresponding predetermined cut-off point; and(3) predicting that the patient is likely to sufficiently respond to chemotherapy in which a combination drug containing tegafur, gimeracil, and oteracil potassium is used in combination with an EGFR inhibitor, when the comparison in step (2) reveals that the expression level of EGFR is greater than the cut-off point, or predicting that the patient is likely to sufficiently respond to chemotherapy in which a combination drug containing tegafur, gimeracil, and oteracil potassium is used alone, when the comparison in step (2) reveals that the expression level of EGFR is not greater than the cut-off point.2. The method of claim 1 , wherein the molar ratio of the respective active ingredients in the combination drug containing tegafur claim 1 , gimeracil claim 1 , and oteracil potassium is tegafur:gimeracil:oteracil potassium=1:0.4:1.3. The method of claim 1 , wherein the EGFR inhibitor is cetuximab.4. The method of claim 1 , wherein the chemotherapy is postoperative adjuvant chemotherapy.5. An antitumor agent comprising a combination drug containing tegafur claim 1 , gimeracil claim 1 , and oteracil potassium and an EGFR inhibitor for use in the treatment of a gastric cancer patient predicted claim 1 , according to the method of claim 1 , to be likely to sufficiently respond to chemotherapy in which the combination drug containing tegafur claim 1 , gimeracil claim 1 , and oteracil ...

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Номер записи: 33
26-01-2017 дата публикации

DIAMINOTRIAZINE DERIVATIVES AS HERBICIDES

Номер: US20170022170A1
Автор: CALO Frederick, HANZLIK Kristin, Hutzler Johannes, Kreuz Klaus, Major Julia, NEWTON Trevor William, Schachtschabel Doreen, SEITZ Thomas, Tresch Stefan, VOGT Florian
Принадлежит:

The present invention relates to diaminotriazine compounds of the formula (I) and to their use as herbicides. The present invention also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation. 117-. (canceled)19. The compound of claim 18 , wherein Ris selected from the group consisting of C-C-haloalkoxy claim 18 , C-C-alkenyloxy claim 18 , C-C-haloalkenyloxy claim 18 , C-C-alkynyloxy claim 18 , C-C-haloalkynyloxy claim 18 , (C-C-alkoxy)-C-C-alkoxy claim 18 , C-C-cycloalkoxy claim 18 , C-C-halocycloalkoxy claim 18 , (C-C-cycloalkyl)-C-C-alkoxy and (C-C-halocycloalkyl)-C-C-alkoxy.20. The compound of claim 18 , wherein Ris C-C-cycloalkoxy claim 18 , C-C-alkenyloxy claim 18 , C-C-alkynyloxy or (C-C-cycloalkyl)-C-C-alkoxy.21. The compound of claim 18 , wherein Ris selected from the group consisting of halogen claim 18 , CN claim 18 , C-C-alkoxy claim 18 , C-C-haloalkoxy claim 18 , C-C-cycloalkoxy and C-C-halocycloalkoxy.23. The compound of claim 21 , wherein R claim 21 , Rand Rare selected from the group consisting of and hydrogen and fluorine.25. The compound of claim 18 , wherein Ris H claim 18 , CN claim 18 , C-C-alkyl claim 18 , (C-C-alkoxy)-C-C-alkyl claim 18 , C-C-alkoxy claim 18 , (C-C-alkyl)carbonyl claim 18 , (C-C-cycloalkyl)carbonyl or (C-C-alkyl)sulfonyl.26. The compound of claim 25 , wherein Ris H.27. The compound of claim 18 , wherein Ris H claim 18 , CN claim 18 , C-C-alkyl claim 18 , (C-C-alkoxy)-C-C-alkyl claim 18 , (C-C-alkyl)carbonyl claim 18 , (C-C-cycloalkyl)carbonyl or (C-C-alkyl)sulfonyl.28. The compound of claim 27 , wherein Ris H.29. The compound of claim 18 , wherein Ris selected from the group consisting of hydrogen claim 18 , fluorine claim 18 , chlorine claim 18 , C-C-alkyl and C-C-alkoxy.30. The compound of claim 18 , wherein Ris selected from the group consisting of hydrogen claim 18 , fluorine claim 18 , C-C-alkyl claim 18 , C-C-haloalkyl claim 18 , C-C-alkoxy and C-C-haloalkoxy.31. The ...

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Номер записи: 34
25-01-2018 дата публикации

N2-(3,4-DIMETHYLPHENYL)-6-((4-(P-TOLYL)PIPERAZIN-1-YL)METHYL)-1,3,5-TRIAZINE-2,4-DIAMINE

Номер: US20180022715A1
Автор: Walum Erik, Wikström Per, Wilcke Mona
Принадлежит:

The compound N-(3,4-dimethylphenyl)-6-((4-(p-tolyl)piperazin-1-yl)methyl)-1,3,5-triazine-2,4-diamineor a pharmaceutically acceptable salt of said compound. The compound is useful the treatment of a condition or disorder associated with nicotinamide adenine dinucleotide phosphate oxidaseactivity. A pharmaceutical composition comprising the compound. 24.-. (canceled)5. A pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt according to and optionally a pharmaceutically acceptable excipient.616.-. (canceled)17. A method of treatment of a condition or disorder selected from endocrine disorders claim 1 , cardiovascular disorders claim 1 , respiratory disorders claim 1 , metabolism disorders claim 1 , skin disorders claim 1 , bone disorders claim 1 , neuroinflammatory and/or neurodegenerative disorders claim 1 , kidney diseases claim 1 , reproduction disorders claim 1 , diseases affecting the eye and/or the lens and/or conditions affecting the inner ear claim 1 , inflammatory disorders claim 1 , liver diseases claim 1 , pain claim 1 , cancers claim 1 , allergic disorders claim 1 , traumatisms claim 1 , septic claim 1 , hemorrhagic and anaphylactic shock claim 1 , diseases or disorders of the gastrointestinal system claim 1 , abnormal angiogenesis and angiogenesis-dependent conditions claim 1 , lung infections claim 1 , acute lung injury claim 1 , pulmonary arterial hypertension claim 1 , obstructive lung disorders claim 1 , and fibrotic lung disease claim 1 , by administering the compound N-(3 claim 1 ,4-dimethylphenyl)-6-((4-(p-tolyl)piperazin-1-yl)methyl)-1 claim 1 ,3 claim 1 ,5-triazine-2 claim 1 ,4-diamine claim 1 , or a pharmaceutically acceptable salt of said compound claim 1 , to a mammal in need of such treatment.18. The method of claim 17 , wherein the mammal is a human.19. The method of claim 17 , wherein the mammal is a non-human mammal.20. The method of claim 17 , wherein the non-human mammal is a dog or a cat.21. The ...

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Номер записи: 35
22-01-2015 дата публикации

GABAA RECEPTOR ANTAGONISTS AFFECTING GANGLION CELL FUNCTION AND VISUAL ACUITY

Номер: US20150025061A1
Автор: Karakossian Movses H.
Принадлежит:

The present invention is directed to a method of enhancing visual acuity in a subject, comprising intravitreally administering to the subject in need of such enhancement, a therapeutically effective amount of an extrasynaptic GABAreceptor antagonist. The present invention is also directed to an ocular implant comprising a therapeutically effective amount of the extrasynaptic GABAreceptor antagonist. 1. A method of enhancing visual function in a subject , comprising intravitreally administering to the subject in need of such enhancement , a therapeutically effective amount of a compound that is an extrasynaptic GABAreceptor antagonist.2. The method of claim 1 , wherein the visual function is selected from the group consisting of visual acuity claim 1 , visual field claim 1 , contrast sensitivity claim 1 , visual adaptation to differerent luminance levels claim 1 , color vision claim 1 , binocular and three dimensional vision3. The method of claim 2 , wherein the visual function is visual acuity.4. The method of claim 1 , wherein the compound is SR-95531 (Gabazine) claim 1 , or a compound selected from the group consisting of pentylenetetrazole claim 1 , bicuculline claim 1 , bilobalida claim 1 , ginkgolide B claim 1 , picrotoxin claim 1 , RO-4882224 claim 1 , RO-4938591 claim 1 , α5IA claim 1 , and RG-1662; or a pharmaceutically acceptable salt thereof.5. The method of claim 1 , wherein the compound is a benzodiazepine site inverse agonist.6. The method of claim 5 , wherein the benzodiazepine site inverse agonist is selected from the group consisting of: Ro 19-4603 claim 5 , Ro 15-4513 claim 5 , L-655 claim 5 ,708 claim 5 , TB 21007 claim 5 , and MRK 016; or a pharmaceutically acceptable salt thereof.7. The method of claim 1 , wherein the subject in need of such enhancement is one who has low/poor visual function resulting from a retinal disorder or retinal damage.8. The method of claim 3 , wherein said visual acuity is measured by sweep vision evoked potential (sVEP ...

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Номер записи: 36
23-01-2020 дата публикации

Novel compound having isocyanuric skeleton and composition in which said compound is included

Номер: US20200024241A1
Автор: Eiji Sakamoto, Hisashi Mitsuhashi, Kaori Ozawa, Masatoshi Nose, Saya Nii, Tsuneo Yamashita
Принадлежит: Daikin Industries Ltd

The invention aims to provide a novel compound to be suitably used for antifouling agents. The compound of the invention is represented by the following formula (1): wherein R 1 is a monovalent organic group containing a polyether chain; X 1 and X 2 are each individually a monovalent group; and the polyether chain is a chain represented by the following formula: —(OC 6 F 12 ) m11 —(OC 5 F 10 ) m12 —(OC 4 F 8 ) m13 —(OC 3 X 10 6 ) m14 —(OC 2 F 4 ) m15 —(OCF 2 ) m16 —, wherein m11, m12, m13, m14, m15, and m16 are each individually an integer of 0 or 1 or greater; X 10 s are each individually H, F, or Cl; and the repeating units are present in any order.

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Номер записи: 37
02-02-2017 дата публикации

Diaminotriazine Derivatives as Herbicides

Номер: US20170029383A1
Автор: CALO Frederick, HANZLIK Kristin, Hutzler Johannes, Kreuz Klaus, Major Julia, NEWTON Trevor William, Schachtschabel Doreen, SEITZ Thomas, Tresch Stefan, VOGT Florian
Принадлежит:

The present invention relates to diaminotriazine compounds of the formula (I) and to their use as herbicides. The present invention also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation. 120-. (canceled)22. The compound of claim 21 , wherein Rand Rare claim 21 , independently of each other claim 21 , selected from the group consisting of hydrogen and halogen.23. The compound of claim 21 , wherein Ris selected from the group consisting of hydrogen claim 21 , halogen and C-C-alkoxy.24. The compound of claim 21 , wherein Ris selected from the group consisting of halogen and C-C-alkoxy.25. The compound of claim 21 , wherein Rand Rare claim 21 , independently of each other claim 21 , selected from the group consisting of fluorine and C-C-alkoxy claim 21 , provided that either Ror Ris C-C-alkoxy.27. The compound of claim 21 , wherein Ris selected from the group consisting of H claim 21 , CN claim 21 , (C-C-alkyl)carbonyl claim 21 , (C-C-alkyl)sulfonyl claim 21 , C-C-alkoxy claim 21 , (C-C-alkoxy)carbonyl claim 21 , (C-C-alkylamino)carbonyl claim 21 , di(C-C-alkyl)aminocarbonyl claim 21 , (C-C-alkylamino)sulfonyl claim 21 , di(C-C-alkyl)aminosulfonyl claim 21 , wherein the aliphatic parts of the 10 aforementioned radicals are unsubstituted claim 21 , partly or completely halogenated claim 21 , phenyl claim 21 , phenylcarbonyl and phenyl-C-Calkyl claim 21 ,{'sub': 2', '1', '6', '1', '6, 'wherein phenyl in the last 3 mentioned radical is unsubstituted or substituted by 1, 2, 3, 4, or 5 identical or different substituents selected from the group consisting of halogen, CN, NO, C-C-alkoxy and C-C-haloalkoxy.'}28. The compound of claim 21 , wherein Ris selected from the group consisting of H claim 21 , CN claim 21 , C-C-alkoxy claim 21 , (C-C-alkyl)carbonyl and (C-C-alkyl)sulfonyl.29. The compound of claim 21 , wherein Ris selected from the group consisting of H claim 21 , CN claim 21 , C-C-alkoxy claim 21 , (C-C-alkyl) ...

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Номер записи: 38
02-02-2017 дата публикации

DIAMINOTRIAZINE DERIVATIVES AS HERBICIDES

Номер: US20170029384A1
Автор: CALO Frederick, HANZLIK Kristin, Hutzler Johannes, Kreuz Klaus, Major Julia, NEWTON Trevor William, Schachtschabel Doreen, SEITZ Thomas, Tresch Stefan, VOGT Florian
Принадлежит:

The present invention relates to diaminotriazine compounds of the formula (I) and to their use as herbicides. The present invention also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation. 119-. (canceled)21: The compound of claim 20 , wherein A is phenyl claim 20 , which carries a fluorine atom in the 2-position of the phenyl ring and which further carries 1 claim 20 , 2 claim 20 , 3 or 4 identical or different substituents R.22: The compound of claim 21 , wherein Ris halogen claim 21 , CN claim 21 , C-C-alkyl claim 21 , C-C-haloalkyl claim 21 , C-C-cycloalkyl claim 21 , C-C-alkynyl or C-C-alkenyl.23: The compound of claim 22 , wherein A is phenyl claim 22 , which carries a fluorine atom in the 2-position of the phenyl ring and which further carries 1 claim 22 , 2 claim 22 , 3 or 4 substituents Rselected from the group consisting of F claim 22 , Cl claim 22 , Br claim 22 , CN claim 22 , CF claim 22 , methyl claim 22 , vinyl claim 22 , ethynyl and cyclopropyl.24: The compound of claim 23 , wherein A is 2 claim 23 ,6-difluorophenyl claim 23 , 2 claim 23 ,3 claim 23 ,6-trifluorophenyl claim 23 , 2 claim 23 ,4 claim 23 ,6-trifluorophenyl claim 23 , 2 claim 23 ,3 claim 23 ,5 claim 23 ,6-tetrafluorophenyl or 2 claim 23 ,3 claim 23 ,4 claim 23 ,5 claim 23 ,6-pentafluorophenyl.25: The compound of claim 20 , wherein Ris selected from the group consisting of H claim 20 , CN claim 20 , C-C-alkyl claim 20 , (C-C-alkoxy)-C-C-alkyl claim 20 , (C-C-alkyl)carbonyl claim 20 , (C-C-alkyl)sulfonyl claim 20 , C-C-alkoxy claim 20 , (C-C-alkoxy)carbonyl claim 20 , (C-C-alkylamino)carbonyl claim 20 , di(C-C-alkyl)aminocarbonyl claim 20 , (C-C-alkylamino)sulfonyl claim 20 , di(C-C-alkyl)aminosulfonyl claim 20 , where the aliphatic parts of the 10 aforementioned radicals are unsubstituted claim 20 , partly or completely halogenated claim 20 ,{'sub': 1', '6, 'phenyl, phenylcarbonyl and phenyl-C-Calkyl,'}{'sub': 2', '1', '6', '1', '6 ...

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Номер записи: 39
02-02-2017 дата публикации

5-HT2B Antagonists

Номер: US20170029385A1
Автор: Huang Niu, LIN Xingyu, Zhou Yu
Принадлежит: National Institute of Biological Sciences, Beijing

The invention provides novel compounds and compositions comprising a 5-HTantagonist of formula I: 2. The method of wherein:{'sup': 1', '2, 'Rand Rare independently H or methyl;'}{'sup': 3', '4', '3', '4, 'Rand Rare independently C1-C3 alkyl, or Rand Rare joined to form C4-C7 cycloalkyl;'}{'sup': 5', '9, 'Rand Rare independently H, halogen, methyl or methoxyl; and'}{'sup': 6', '8', '10', '10', '10', '10', '10', '10, 'R-Rare independently H, halogen, methyl, —OR, COR, COOR, or CONRR, wherein each Ris independently H or C1-C4 alkyl.'}3. The method of wherein:{'sup': 1', '2, 'Rand Rare independently H or methyl;'}{'sup': 3', '4', '3', '4, 'Rand Rare methyl or Rand Rform cyclopentyl or cyclohexyl;'}{'sup': '5', 'Ris H, halogen, methyl or methoxyl;'}{'sup': 6', '10', '10', '10', '10', '10', '10, 'Ris H, halogen (F, Cl, Br, I), methyl, methoxyl, or —OR, COR, COOR, or CONRR, wherein each Ris independently H or C1-C4 alkyl.'}{'sup': 7', '10', '10', '10, 'Ris H, halogen, methyl, —ORor COOR, wherein each Ris independently H or C1-C3 alkyl;'}{'sup': '8', 'Ris H, halogen, methyl or methoxyl; and'}{'sup': '9', 'Ris H or methyl.'}5. The method of wherein the disorder is migraine claim 1 , irritable bowel syndrome (IBS) claim 1 , pulmonary arterial hypertension (PAH) claim 1 , fibrosis claim 1 , hepatocellular cancer claim 1 , a small intestinal neuroendocrine tumor claim 1 , a cardiovascular disorder claim 1 , or a gastrointestinal (GI) tract disorder.6. The method of further comprising the step of detecting a resultant amelioration of the disorder that is migraine claim 1 , irritable bowel syndrome (IBS) claim 1 , pulmonary arterial hypertension (PAH) claim 1 , fibrosis claim 1 , hepatocellular cancer claim 1 , a small intestinal neuroendocrine tumor claim 1 , a cardiovascular disorder claim 1 , or a gastrointestinal (GI) tract disorder.7. The method of further comprising the antecedent step of diagnosing the disorder that is migraine claim 1 , irritable bowel syndrome (IBS) ...

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Номер записи: 40
11-02-2016 дата публикации

Targeted Therapies for Cancer

Номер: US20160038492A1
Автор: David Craig, John Carpten, Mitesh Jivraj Borad
Принадлежит: Mayo Foundation for Medical Education and Research, Translational Genomics Research Institute TGen

Methods of selecting a chemotherapy regimen for treatment of cancer in a patient are disclosed. A patient genetic sample from a bilary cancer such as cholangiocarcinoma is analyzed for a mutation in ERRFI1 and a chemotherapeutic agent is selected as a result of the analysis. If a mutation in ERRFI1 is present, treatment with an inhibitor of Epidermal Growth Factor Receptor (EGFR) is shown to have inhibitory effects on tumor growth. In this manner, the chemotherapy regimen is targeted to a given mutation in a patient's cancer.

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Номер записи: 41
18-02-2016 дата публикации

NOVEL USES

Номер: US20160045507A1
Автор: WENNOGLE Lawrence
Принадлежит:

The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder. 1. A method for the prophylaxis or treatment of a CNS disease , disorder , and/or injury , wherein the method comprises the administration of an effective amount of a PDE1 inhibitor (e.g. , any compound described herein , e.g. , any compound of Formula I-XI) to a subject , wherein the administration of the PDE1 inhibitor modulates the subject's level of intracellular cAMP.13. The method according to claim 1 , wherein the CNS disease claim 1 , disorder claim 1 , or injury is a spinal cord injury.14. The method according to claim 1 , wherein the CNS disease claim 1 , disorder claim 1 , or injury relates to motor neuron trauma.15. The method according to claim 1 , wherein the CNS disease claim 1 , disorder claim 1 , or injury is selected from the group consisting of: neurological traumas and injuries claim 1 , surgery related trauma and/or injury claim 1 , retinal injury and trauma claim 1 , injury related to epilepsy claim 1 , cord injury claim 1 , spinal cord injury claim 1 , brain injury claim 1 , brain surgery claim 1 , trauma related brain injury claim 1 , trauma related to spinal cord injury claim 1 , brain injury related to cancer treatment claim 1 , spinal cord injury related to cancer treatment claim 1 , brain injury related to infection claim 1 , brain injury related to inflammation claim 1 , spinal cord injury related to infection claim 1 , spinal cord injury related to inflammation claim 1 , brain injury related to environmental toxin claim 1 , and spinal cord injury related to environmental toxin.16. The method according to claim 1 , wherein the CNS disease claim ...

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Номер записи: 42
15-02-2018 дата публикации

METHODS OF TREATMENT OF MALIGNANCIES

Номер: US20180042930A1
Автор: AMATANGELO Michael, Hu Xiaolan, THAKURTA Anjan
Принадлежит:

Provided are methods and compositions for treating a malignancy in patients carrying an IDH2 mutation. 2. The method of claim 1 , wherein the myelodysplastic syndrome is further characterized by the presence of one or more mutant alleles of one or more additional genes.3. The method of claim 1 , wherein the myelodysplastic syndrome is characterized by the presence of mutant alleles of ASXL1 and SRSF2.4. The method of claim 2 , wherein the additional gene is MPL.5. The method of claim 2 , wherein the one or more additional genes is MPL claim 2 , DNMT3A claim 2 , CSF3R claim 2 , FAT3 claim 2 , or CBL.6. The method of claim 1 , wherein the myelodysplastic syndrome is further characterized by the absence of a mutant allele of at least one other gene claim 1 , wherein the other gene is selected from the group consisting of KRAS claim 1 , TP53 claim 1 , SETBP1 claim 1 , and U2AF1.7. The method of claim 1 , wherein the myelodysplastic syndrome is further characterized by the absence of a mutant allele of at least one other gene claim 1 , wherein the other gene is selected from the group consisting of TP53 claim 1 , SETBP1 claim 1 , U2AF1 claim 1 , TCF3 claim 1 , STAG2 claim 1 , NRAS claim 1 , JAK2 and BRAF.8. The method of claim 1 , wherein the myelodysplastic syndrome is characterized by the absence of a mutant allele of KRAS claim 1 , TP53 claim 1 , SETBP1 claim 1 , and U2AF1.9. The method of claim 1 , wherein the myelodysplastic syndrome is characterized by the absence of a mutant allele of KRAS claim 1 , TP53 claim 1 , TCF3 claim 1 , and STAG2.10. The method of claim 1 , wherein the myelodysplastic syndrome is characterized by the absence of a mutant allele of SETBP1 claim 1 , NRAS claim 1 , JAK2 and BRAF.13. The method of claim 11 , wherein the myelodysplastic syndrome is further characterized by the presence of one or more mutant alleles of one or more additional genes.14. The method of claim 11 , wherein the myelodysplastic syndrome is characterized by the absence ...

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Номер записи: 43
18-02-2016 дата публикации

Sept4/ARTS AS A TUMOR SUPPRESSOR IN THE DIAGNOSIS, PROGNOSIS AND TREATMENT OF HEPATIC DISORDERS

Номер: US20160047001A1
Автор: LARISCH Sarit, STELLER Hermann
Принадлежит:

The invention relates to methods for the diagnosis and prognosis of hepatic disorder and associated pathologies as well as of a solid proliferative disorder in a mammalian subject. More specifically, the methods of the invention are based on determining the expression, methylation of ARTS as well as histone trimethylation. The invention further provides therapeutic methods for treating said disorders. 134-. (canceled)35. A method for treating , preventing , ameliorating or delaying the onset of a hepatic disorder and associated pathologies or of a solid proliferative disorder in a subject , said method comprises the steps of: (i) the level of expression of Apoptosis Related Protein in the TGF-beta Signaling Pathway (ARTS) and optionally of at least one of Survivin and α-fetoprotein (AFP) to obtain an expression value;', '(ii) Sept4/ARTS methylation level of the CpG islands at the TSS to obtain a value of Sept4/ARTS TSS methylation; and', '(iii) the level of Histone 3 trimethylation at at least one of lysine 4, lysine 9 and lysine 27 to obtain a trimethylation value of histone H3 at said lysine residues;, '(a) determining in at least one biological sample of said subject at least one of (i) if the expression value of ARTS obtained in step (a i) is any one of, positive or negative with respect to a predetermined standard expression value of ARTS or the expression value of ARTS in a control sample and optionally, determining if the expression value of at least one of Survivin and AFP is any one of, positive or negative with respect to a predetermined standard expression value of at least one of Survivin and AFP or to the expression value of at least one of Survivin and AFP in a control sample;', '(ii) if the value of Sept4/ARTS TSS methylation obtained in step (a ii) is any one of, positive or negative with respect to a predetermined standard Sept4/ARTS TSS methylation or to the Sept4/ARTS TSS methylation value in a control sample;', '(iii) if trimethylation value of ...

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Номер записи: 44
16-02-2017 дата публикации

Diaminotriazine compounds and their use as herbicides

Номер: US20170044114A1
Автор: CALO Frederick, HANZLIK Kristin, Hutzler Johannes, Kreuz Klaus, Major Julia, NEWTON Trevor William, Schachtschabel Doreen, SEITZ Thomas, SISAY Mihiret Tekeste, Tresch Stefan, VOGT Florian
Принадлежит:

The present invention relates to diaminotriazine compounds and to their use as herbicides. It also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation. 120-. (canceled)22: The compound of claim 21 , wherein Ris selected from the group consisting of halogen claim 21 , CN claim 21 , C-C-alkyl claim 21 , C-C-alkoxy and C-C-haloalkoxy claim 21 , in particular from fluorine chlorine or CN.23: The compound of claim 21 , wherein Ris selected from the group consisting of and halogen claim 21 , CN claim 21 , C-C-alkoxy and C-C-haloalkoxy and is in particular fluorine.25: The compound of claim 24 , wherein R claim 24 , Rand Rare selected from the group consisting of and hydrogen and fluorine.26: The compound of claim 21 , wherein Q is selected from the group consisting of a chemical bond claim 21 , O claim 21 , CH claim 21 , S claim 21 , S(O) and S(O).27: The compound of claim 21 , wherein Q is NR claim 21 , wherein Ris selected from H claim 21 , CN and C-C-alkyl.28: The compound of claim 21 , wherein Ar is phenyl claim 21 , which carries 1 or 2 radicals R.29: The compound of claim 21 , wherein R claim 21 , if present claim 21 , is selected from the group consisting of halogen claim 21 , CN claim 21 , C-C-alkyl claim 21 , C-C-haloalkyl claim 21 , C-C-alkoxy and C-C-haloalkoxy.30: The compound of claim 21 , wherein the moiety Ar-Q is selected from the group consisting of phenyl claim 21 , 4-methoxyphenyl claim 21 , 4-cyanophenyl claim 21 , 3-methylphenyl claim 21 , 3 claim 21 ,5-dimethylphenyl claim 21 , 3 claim 21 ,5-difluorophenyl claim 21 , 3 claim 21 ,5-dichlorophenyl claim 21 , 3 claim 21 ,5-dibromophenyl claim 21 , 3 claim 21 ,5-dimethoxyphenyl claim 21 , 3 claim 21 ,5-diethoxyphenyl claim 21 , 3 claim 21 ,5-Bis-(trifluoromethoxy)phenyl claim 21 , 3 claim 21 ,5-Bis-(trifluoromethyl)phenyl claim 21 , 3 claim 21 ,5-dicyanophenyl claim 21 , 3-fluoro-5-methylphenyl claim 21 , 3-chloro-5-methylphenyl claim 21 , 3-bromo- ...

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Номер записи: 45
19-02-2015 дата публикации

Tyrosine Kinase Inhibitor Combinations and their Use

Номер: US20150051210A1
Автор: Buckler Alan, Harbinski Fred, JEFFERY Douglas, Sanghavi Sneha, Tiedt Ralph, Wilson Christopher
Принадлежит: NOVARTIS AG

The invention relates to pharmaceutical combination product comprising (i) a MET inhibitor and (ii) an FGFR inhibitor, or a pharmaceutical acceptable salt thereof, respectively, or a prodrug thereof, respectively, and at least one pharmaceutically acceptable carrier. 1. A pharmaceutical combination comprising (i) a MET inhibitor and (ii) an FGFR inhibitor , or a pharmaceutically acceptable salt thereof , respectively , or a prodrug thereof , respectively , and at least one pharmaceutically acceptable carrier.2. The pharmaceutical combination according to for simultaneous claim 1 , separate or sequential use of the components (i) and (ii).3. The pharmaceutical combination according to in the form of a fixed combination.4. The pharmaceutical combination according to in the form or a kit of parts for the combined administration where the FGFR tyrosine kinase inhibitor and the MET tyrosine kinase inhibitor may be administered independently at the same time or separately within time intervals claim 1 , especially where these time Intervals allow that the combination partes are jointly active.5. The pharmaceutical combination according to claim 1 , wherein the MET tyrosine kinase inhibitor is selected from the group consisting of (E)-2-(1-(3-((7-fluoroquinolin-6-yl)methyl)imidazo[1 claim 1 ,2-b]pyridazin-6-yl)ethylidene)hydrazinecarboxamide and 2-fluoro-N-methyl-4-[7-quinolin-6-yl-methyl)-imidazo[1 claim 1 ,2-b]triazin-2-yl]benzamide claim 1 , or a pharmaceutically acceptable salt or prodrug thereof claim 1 , respectively claim 1 , and the FGR-R tyrosine kinase inhibitor is 3-(2 claim 1 ,6-dichloro-3 claim 1 ,5-dimethoxy-phenyl)-1-{6-[4-(4-ethylpiperazin-1-yl)-phenylamino]-pyridin-4-yl}-1-methyl-urea claim 1 , or a pharmaceutically acceptable salt or prodrug thereof.6. The pharmaceutical combination according to comprising a further co-agent claim 1 , or a pharmaceutically acceptable salt or a prdodrug thereof.7. The pharmaceutical combination according to comprising a ...

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Номер записи: 46
13-02-2020 дата публикации

LAMOTRIGINE SUSPENSION DOSAGE FORM

Номер: US20200046716A1
Автор: Jha Amit, Kumar Dinesh, Mehta Kamal Surendra, SINGH Rakesh K., Srivastava Saurabh
Принадлежит:

The present invention relates to a stable ready to use and powder for oral suspension dosage forms of Lamotrigine and its pharmaceutically acceptable salts and process of preparing such compositions. The liquid and powder for oral suspension dosage forms of Lamotrigine have been previously known only as extemporaneous preparations. Present invention relates to manufacture of liquid and powder for oral suspension dosage forms of Lamotrigine having improved physico-chemical properties with desired technical attributes. The prepared dosage forms are useful in patients having difficulties in swallowing tablets and provide physician with more options for dose titration. 1. An immediate release oral pharmaceutical powder for suspension of lamotrigine or its pharmaceutically acceptable salt , hydrate or polymorph thereof with one or more pharmaceutically acceptable excipients comprising lamotrigine present at from about 0.1% w/w to 40% w/w of the power for suspension , wherein the pH of the reconstituted composition is from 4-8 when reconstituted with water.2. The immediate release oral pharmaceutical powder for suspension of claim 1 , wherein the pH of the reconstituted composition is from 4-8 and the viscosity is from 700-1200 cps.3. The immediate release oral pharmaceutical powder for suspension of claim 1 , wherein the composition is free from microbial contamination for at least 20 days when tested according to <1111>USP-30 NF-25.4. An immediate release oral pharmaceutical powder for suspension of lamotrigine or its pharmaceutically acceptable salt claim 1 , hydrate or polymorph thereof with one or more pharmaceutically acceptable excipients comprising lamotrigine from about 0.01% w/w to 10% w/w by weight on the basis of the total weight of the composition wherein the composition exhibits in-vitro dissolution rate of more than 85% of drug release within 20 minutes when placed in a dissolution vessel filled with 900 ml of 0.1N HCL claim 1 , pH 1.2 maintained at 37±0.5° ...

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Номер записи: 47
22-02-2018 дата публикации

USE OF 4-(4-FLUORO-2-METHOXYPHENYL)-N--1,3,5-TRIAZIN-2-AMINE FOR TREATING LYMPHOMAS

Номер: US20180050040A1
Автор: ISHIDA Takashi, SCHOLZ Arne
Принадлежит:

The present invention relates to 4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A), more particularly (+)-4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A′), for use in treating lymphoma, preferably diffuse large B-cell lymphoma (DLBCL) mantle cell lymphoma, follicular lymphoma, diffuse large B-cell lymBurkitt's lymphoma, adult T-cell lymphoma (ATL) and Hodgkin's lymphoma, more preferably DLBCL and ATL. 120-. (canceled)2326-. (canceled)28: The method according to claim 27 , whereindiffuse large B-cell lymphoma, mantle cell lymphoma, follicular lymphoma, Burkitt's lymphoma, adult T-cell lymphoma or Hodgkin's lymphoma is treated.29: The method according to claim 28 , whereindiffuse large B-cell lymphoma is treated.30: The method according to claim 28 , whereinadult T-cell lymphoma is treated.31: The method according to claim 27 , wherein the enantiomer(+)-4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine or a physiologically acceptable salt thereof is used.32: The method according to claim 28 , wherein the enantiomer(+)-4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine or a physiologically acceptable salt thereof is used.33: The method according to claim 29 , wherein the enantiomer(+)-4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine or a physiologically acceptable salt thereof is used.34: The method according to claim 30 , wherein the enantiomer(+)-4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine or a physiologically acceptable salt thereof is used.35: The method according to claim 21 , whereindiffuse large B-cell lymphoma, mantle cell lymphoma, follicular lymphoma, Burkitt's lymphoma, adult T-cell lymphoma or Hodgkin's lymphoma is treated.36: The method according to claim 35 ...

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Номер записи: 48
26-02-2015 дата публикации

METHOD AND IMPROVED PHARMACEUTICAL COMPOSITION FOR ENHANCING TRANSDERMAL DELIVERY OF PDE-5 INHIBITOR

Номер: US20150057284A1
Автор: Liu Yee-Chien, Wu Pei-Ling
Принадлежит: Tritech Biopharmaceuticals Co., Ltd.

The present disclosure relates to the use of an agent that enhances transdermal delivery of a PDE-5 inhibitor. More particularly, the present disclosure provides improved method and composition that promotes transdermal delivery of a PDE-5 inhibitor for the treatment of the PDE-5 mediated conditions and/or diseases. 1. In an improved transdermal pharmaceutical composition comprising a phosphodiesterase type-5 (PDE-5) inhibitor or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient , wherein the improvement comprises ,an enhancer selected from the group consisting of cocamidopropyl betaine, sodium lauroamphoacetate, quaternium-60, isostearamidopropyl morpholine lactate, dipropylene glycol and a combination thereof; wherein the PDE-5 inhibitor and the enhancer are present in a ratio from about 20:1 to 2:1 in the improved transdermal pharmaceutical composition.2. The improved transdermal pharmaceutical composition of claim 1 , wherein the PDE-5 inhibitor is any of sildenafil claim 1 , tadalafi or vardenafil.3. The improved transdermal pharmaceutical composition of claim 2 , wherein the PDE-5 inhibitor is vardenafil.4. The improved transdermal pharmaceutical composition of claim 2 , wherein the PDE-5 and the enhancer are present in a ratio of about 5:1.5. The improved transdermal pharmaceutical composition of claim 2 , wherein the PDE-5 inhibitor is not in crystalline state.6. A method for enhancing transdermal delivery of a phosphodiesterase type-5 (PDE-5) inhibitor in a subject comprising administering to the subject the improved transdermal pharmaceutical composition of .7. The method of claim 6 , wherein the PDE-5 inhibitor is any of sildenafil claim 6 , tadalafi or vardenafil.8. The method of claim 7 , wherein the PDE-5 inhibitor is vardenafil.9. The method of claim 7 , wherein the PDE-5 and the enhancer are administered in a ratio of about 5:1.10. The method of claim 6 , wherein the PDE-5 inhibitor is not in crystalline state. 1. ...

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Номер записи: 49
28-02-2019 дата публикации

POWDER FOR ORAL SUSPENSION CONTAINING LAMOTRIGINE

Номер: US20190060237A1
Автор: Li Shoufeng, Lu Enxian
Принадлежит: AUCTA Pharmaceuticals

This document discloses a powder formulation of lamotrigine for oral administration. Also disclosed is a suspension of lamotrigine and a method of treating diseases. 1. A powder formulation suitable for reconstitution with a pharmaceutically acceptable carrier to form a stable suspension oral dosage form comprising:lamotrigine or a pharmaceutically acceptable salt thereof; anda suspending agent, wherein the suspending agent is in an amount ranging from about 0.1% to about 10% w/w in the powder formulation, further wherein the suspending agent is effective for maintaining a sedimentation volume ratio of more than about 0.8 for at least 10 hour after the powder formulation is reconstituted into an aqueous suspension.2. The powder formulation of claim 1 , wherein less than about 5% of the lamotrigine is converted to its hydrate form within about 24 hours after the powder formulation is reconstituted into the suspension.3. The powder formulation of claim 1 , wherein less than about 0.5% of the lamotrigine or the pharmaceutically acceptable salt thereof decomposes within about 24 hours after the powder formulation is reconstituted into the suspension.4. The powder formulation of claim 1 , wherein the lamotrigine or the pharmaceutically acceptable salt thereof and the suspending agent have a ratio ranging from about 10:1 to about 10:5 by weight.5. The powder formulation of claim 1 , wherein the lamotrigine or the pharmaceutically acceptable salt thereof and the suspending agent have a ration of about 5:1 by weight.6. The powder formulation of claim 1 , wherein the suspending agent is selected from the group consisting of hydrocolloid gum claim 1 , cellulosic derivative claim 1 , a polysaccharide claim 1 , alginate claim 1 , acrylic acid copolymer claim 1 , polyvmylpyrrohdone claim 1 , aluminiummagnesium silicate claim 1 , and any combination thereof.7. The powder formulation of claim 1 , wherein the suspending agent is hydrocolloid gum.8. The powder formulation of claim 1 ...

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Номер записи: 50
10-03-2016 дата публикации

USE OF PHOSPHODIESTERASE 5A INHIBITORS FOR THE TREATMENT OF MUSCULAR DYSTROPHY

Номер: US20160067246A1
Автор: Thomas Gail D., Victor Ronald G.
Принадлежит: CEDARS-SINAI MEDICAL CENTER

Described herein are methods of treating muscular dystrophy, including Becker's muscular dystrophy and Duchenne muscular dystrophy. The methods comprise administering a phosodiesterase 5A (PDE5A) inhibitor, such as tadalafil, to a subject in need thereof. Administering the PDE5A inhibitor has beneficial effects such as restoring functional sympatholysis, alleviating ischemic insult to dystrophin-deficient muscle membranes, reducing use-dependent muscle injury, and thus can slow muscular dystrophy disease progression. 1. A method of treating muscular dystrophy , comprising:providing a phosodiesterase 5A (PDE5A) inhibitor or a salt thereof; andadministering a quantity of a PDE5A inhibitor to a subject in need of treatment for muscular dystrophy.2. The method of claim 1 , wherein the muscular dystrophy is Becker muscular dystrophy (BMD).3. The method of claim 1 , wherein the muscular dystrophy is Duchenne muscular dystrophy (DMD).4. A method of restoring functional sympatholysis claim 1 , alleviating ischemic insult to dystrophin-deficient muscle membranes claim 1 , reducing use-dependent muscle injury claim 1 , or alleviating post-exercise hyperemia claim 1 , comprisingproviding a phosodiesterase 5A (PDE5A) inhibitor or a salt thereof; andadministering a quantity of a PDE5A inhibitor to a subject in need of restoring functional sympatholysis, alleviating ischemic insult to dystrophin-deficient muscle membranes, reducing use-dependent muscle injury, or alleviating post-exercise hyperemia.5. (canceled)6. (canceled)7. (canceled)8. The method of claim 1 , wherein the PDE5A inhibitor is tadalafil or a salt thereof.9. The method of claim 1 , wherein the PDE5A inhibitor is sildenafil or a salt thereof.10. The method of claim 1 , wherein the PDE5A inhibitor is vardenafil or a salt thereof.11. The method of claim 1 , wherein the subject is human.12. The method of claim 1 , wherein the subject is an adult human.13. The method of claim 1 , wherein the subject is an adult claim 1 ...

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Номер записи: 51
10-03-2016 дата публикации

Novel Substituted Bicyclic Aromatic Compounds as S-Nitrosoglutathione Reductase Inhibitors

Номер: US20160067254A1
Автор: Qiu Jian, Stout Adam, Sun Xicheng
Принадлежит:

The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same. 2. The method of wherein when Zand Zare both N claim 1 , and Zis CR claim 1 , then Ris selected from the group consisting of hydrogen claim 1 , C-Calkyl claim 1 , fluorinated C-Calkyl claim 1 , and cyano.3. The method of whereinm is selected from the group consisting of 0 and 1;{'sub': 2a', '2b', '2c', '3', '2, 'R, R, and R, are independently selected from the group consisting of hydrogen, chloro, fluoro, methyl, trifluoromethyl, cyano, methoxy, and N(CH);'}n is selected from the group consisting of 0 and 1; and{'sub': 3', '4', '4′', '4', '4′, 'Ris independently selected from the group consisting of fluoro, chloro, methyl, trifluoromethyl, cyano, methoxy, and NRR where Rand R are methyl, or alternatively together with the said N form the ring aziridin-1-yl or morpholino.'}5. The method of wherein A is COOH.7. The method of wherein when Zis N claim 6 , and Zis CR claim 6 , then Ris selected from the group consisting of hydrogen claim 6 , C-Calkyl claim 6 , fluorinated C-Calkyl claim 6 , and cyano.8. The method of whereinm is selected from the group consisting of 0 and 1;{'sub': 2a', '2b', '2c', '3', '2, 'R, R, and R, are independently selected from the group consisting of hydrogen, chloro, fluoro, methyl, trifluoromethyl, cyano, methoxy, and N(CH);'}n is selected from the group consisting of 0 and 1; and{'sub': 3', '4', '4′', '4', '4′, 'Ris independently selected from the group consisting of fluoro, chloro, methyl, trifluoromethyl, cyano, methoxy, and NRR where Rand R are methyl, or alternatively together with the said N form the ring aziridin-1-yl or morpholino.'}11. The method of wherein Ris selected from the group consisting of hydrogen claim 10 , C-Calkyl claim 10 , fluorinated C-Calkyl claim 10 , and cyano.12. The method of ...

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Номер записи: 52
08-03-2018 дата публикации

TABLET COMPOSITIONS

Номер: US20180064715A1
Автор: Altaf Syed, Bhat Sreenivas S., Burnside Scott, GU CHONG-HUI, Parikh Darshan
Принадлежит:

Provided herein is a tablet comprising 2-methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol or a pharmaceutically acceptable salt thereof. 2. The tablet of claim 1 , wherein Compound 1 is present in an amount from about 20% to about 30% by weight based on total weight of the tablet.3. The tablet of claim 1 , wherein Compound 1 is present in an amount of about 20% claim 1 , 25% or 30% by weight based on total weight of the tablet.4. The tablet of claim 1 , wherein the intragranular excipient comprises from about 30% to about 45% microcrystalline cellulose by weight based on total weight of the tablet.5. The tablet of claim 1 , wherein the intragranular excipient comprises about 34.50% claim 1 , 44.50% or 39.50% microcrystalline cellulose by weight based on total weight of the tablet.6. The tablet of claim 1 , wherein the extragranular excipient comprises from about 5% to about 25% microcrystalline cellulose by weight based on total weight of the tablet.7. The tablet of claim 1 , wherein the extragranular comprises about 20% microcrystalline cellulose by weight based on total weight of the tablet excipient.8. The tablet of claim 1 , wherein the intragranular excipient comprises a binder claim 1 , a disintegrant claim 1 , a wetting agent claim 1 , a lubricant claim 1 , a glidant and stabilizer.9. The tablet of claim 1 , wherein the intragranular excipient comprises microcrystalline cellulose claim 1 , hydroxypropyl cellulose claim 1 , sodium starch glycolate claim 1 , sodium lauryl sulfate claim 1 , magnesium stearate claim 1 , colloidal silicon dioxide and hypromellose acetate succinate.10. The tablet of claim 9 , wherein intragranular microcrystalline cellulose is present in an amount from about 30% to about 50% by weight based on total weight of the tablet claim 9 , intragranular hydroxypropyl cellulose is present from about 1.5% to 2.5% by weight based on total weight of the tablet and ...

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Номер записи: 53
08-03-2018 дата публикации

COMPOSITIONS AND METHODS FOR PROPHYLAXIS AND THERAPY FOR MENIERE'S DISEASE

Номер: US20180064716A1
Автор: Zhang Lixin
Принадлежит:

Provided are articles of manufacture, compositions and methods for prophylaxis and/or therapy for disorders involving dizziness and/or vertigo. The articles of manufacture and compositions contain lamotrigen and/or bupropion. The compositions include pharmaceutical compositions which are intended to alleviate dizziness and/or vertigo. In certain aspects the disclosure includes articles of manufacture and kits which include printed material which provides an indication that the articles or compositions are intended to be used for prophylaxis and/or therapy of Meniere's Disease or a symptom thereof. 1. A method comprising administering to an individual diagnosed with Meniere's Disease a pharmaceutical composition comprising an effective amount of lamotrigine or a pharmaceutically acceptable salt thereof such that the effective amount of the lamotrigine or the pharmaceutically acceptable salt thereof is sufficient to reduce dizziness that is caused by the Meniere's Disease in the individual.2. The method of claim 1 , wherein the lamotrigine or the pharmaceutically acceptable salt thereof is administered twice daily.3. The method of claim 2 , wherein the twice daily administration is performed for a period of at least two weeks.4. The method of claim 1 , wherein the effective amount of lamotrigine comprises between 25 mg and 400 mg.5. The method of claim 4 , wherein the effective amount of lamotrigine comprises between 25 mg and 200 mg.6. The method of claim 1 , further comprising administering to the individual an effective amount of bupropion or a pharmaceutically acceptable salt thereof to the individual such that the effective amount of the bupropion or the pharmaceutically acceptable salt thereof reduces dizziness in the individual that is not caused by the Meniere's Disease.7. The method of claim 6 , wherein the effective amount of the lamotrigine or the pharmaceutically acceptable salt thereof and the effective amount of bupropion or the pharmaceutically ...

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Номер записи: 54
29-05-2014 дата публикации

THERAPEUTIC COMPOSITIONS

Номер: US20140148460A1
Автор: CLOZEL Martine
Принадлежит: ACTELION PHARMACEUTICALS LTD.

The invention relates to a product containing the compound of formula (I) below (I) or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved. 2. The method according to claim 1 , wherein the compound of formula (I) and the compound having PDE5-inhibitory properties are administered simultaneously.3. The method according to claim 1 , wherein the compound of formula (I) and the compound having PDE5-inhibitory properties are administered separately.4. The method according to claim 1 , wherein the compound of formula (I) and the compound having PDE5-inhibitory properties are administered over a period of time.5. The method according to claim 4 , wherein the administration of the compound of formula (I) will be alternated with the administration of a compound having PDE5-inhibitory properties claim 4 , and the interval between such administration will not exceed two or three days.6. The method according to claim 5 , wherein said administration will not exceed one day.7. The method according to claim 1 , wherein the compound having PDE5-inhibitory properties is selected from sildenafil claim 1 , vardenafil claim 1 , tadalafil and udenafil.8. The method according to claim 1 , wherein the compound having PDE5-inhibitory properties is sildenafil.9. The method according to claim 1 , wherein the compound having PDE5-inhibitory properties is tadalafil.10. The method according to claim 1 , wherein the disease intended to be treated is pulmonary hypertension.11. The method according to claim 1 , wherein the disease intended to be treated is pulmonary arterial hypertension. The present invention relates to a product containing the compound of formula (I) belowor a pharmaceutically acceptable salt of this compound, in ...

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Номер записи: 55
17-03-2016 дата публикации

NOVEL IMMUNE SYSTEM MODULATORS

Номер: US20160074403A1
Автор: Lipford Grayson B., Zepp Charles M.
Принадлежит:

The present invention relates to a compound of Formula I: 2. The method of claim 1 , wherein the autoimmune disease is selected from the group consisting of cutaneous and systemic lupus erythematosus claim 1 , insulin-dependent diabetes mellitus claim 1 , rheumatoid arthritis claim 1 , multiple sclerosis claim 1 , atherosclerosis claim 1 , psoriasis claim 1 , psoriatic arthritis claim 1 , inflammatory bowel disease claim 1 , ankylosing spondylitis claim 1 , autoimmune hemolytic anemia claim 1 , Behget's syndrome claim 1 , Goodpasture's syndrome claim 1 , Graves' disease claim 1 , Guillain-Barre syndrome claim 1 , Hashimoto's thyroiditis claim 1 , idiopathic thrombocytopenia claim 1 , io myasthenia gravis claim 1 , pernicious anemia claim 1 , polyarteritis nodosa claim 1 , polymyositis/dermatomyositis claim 1 , primary biliary sclerosis claim 1 , sarcoidosis claim 1 , sclerosing cholangitis claim 1 , Sjogren's syndrome claim 1 , systemic sclerosis (scleroderma and CREST syndrome) claim 1 , Takayasu's arteritis claim 1 , temporal arteritis claim 1 , and Wegener's granulomatosis.3. The method of claim 1 , wherein the cancer is lymphoma claim 1 , pancreatic cancer claim 1 , breast cancer claim 1 , gastric carcinoma claim 1 , or lung cancer.4. The method of claim 1 , whereinX is absent or is an aryl, or heterocycle; and{'sub': 2', 'q', '1', '2', '1', '2', 'p', 'b', 'c', '1', '1, 'Q is (CH)NRR, NR(CH)NRR, OR, or SR, in which q is 0 or 1 and p is 2-4.'}5. The method of claim 1 , whereinX is absent or is aryl, or heterocycle;{'sub': 2', 'q', '1', '2', '1', '2', 'p', 'b', 'c', '1', '1, 'Q is (CH)NRR, NR(CH)NRR, OR, or SR, in which q is 0 or 1 and p is 2-4;'}{'sub': 1', '2', '1', '2', '1', '4, 'Rand Rare each independently hydrogen, alkyl, alkenyl, cycloalkyl, alkylcycloalkyl, aryl, alkylaryl, heterocycle, alkylheterocycle, or Rand Rtogether with the nitrogen atom to which they are bonded form a heterocycle, which may be optionally substituted by from one to four groups which ...

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Номер записи: 56
17-03-2016 дата публикации

Treatment of Skeletal-Related Disorders

Номер: US20160074409A1
Автор: Begley Glenn, Rothbaum Wayne
Принадлежит:

The invention relates to the prevention and/or treatment of skeletal related disorders using heteroaryl compounds. 7. The method of wherein the skeletal-related event is a bone fracture.8. The method of the skeletal-related event is spinal cord compression.9. The method of wherein the compound of Formula Ia or Ib is administered for treating a subject who has undergone bone surgery to treat a skeletal-related event.10. The method of wherein the compound of Formula II is administered for treating a subject who has undergone bone surgery to treat a skeletal-related event.11. The method of wherein the compound of Formula III is administered for treating a subject who has undergone bone surgery to treat a skeletal-related event.12. The method of wherein the compound is administered for treating a subject who has undergone bone surgery to treat a skeletal-related event.13. The method of wherein the compound is administered for treating a subject who has undergone bone surgery to treat a skeletal-related event.14. The method of wherein the compound is administered for treating a subject who has undergone bone surgery to treat a skeletal-related event.15. The method of wherein the subject is receiving radiation therapy.16. The method of wherein the subject is receiving chemotherapy.17. The method of wherein the subject is suffering from prostate cancer.18. The method of wherein the subject is suffering from multiple myeloma.19. The method of wherein the subject is suffering from breast cancer.20. The method of wherein the subject is suffering from lung cancer.21. The method of wherein Tec tyrosine kinase is also inhibited.22. The method of wherein the compound of Formula Ia or Ib covalently binds to BTK.23. The method of wherein the compound of Formula II covalently binds to BTK.24. The method of wherein the compound of Formula III covalently binds to BTK.25. The method of wherein the compound of Formula Ia or Ib non-covalently binds to BTK.26. The method of wherein the ...

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Номер записи: 57
07-03-2019 дата публикации

4-OXO-3,4-DIHYDRO-1,2,3-BENZOTRIAZINE MODULATORS OF GPR139

Номер: US20190070187A1
Автор: Hitchcock Stephen, Lam Betty, Monenschein Holger, Reichard Holly
Принадлежит:

The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: 3. The compound or pharmaceutically acceptable salt according to claim 1 , wherein m is 0.4. The compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris Calkyl.5. The compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris selected from the group consisting of methyl claim 1 , ethyl claim 1 , and isopropyl.6. The compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris methyl.7. The compound or pharmaceutically acceptable salt according to claim 1 , wherein n is 1 and Ris trifluoromethoxy.8. The compound or pharmaceutically acceptable salt according to claim 1 , wherein m is 1.9. The compound or pharmaceutically acceptable salt according to claim 1 , wherein m is 2.10. The compound according to claim 1 , which is selected from the group of compounds consisting of:2-(5-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;N-(1-(4-bromophenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;N-(1-(4-methoxyphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;N-(1-(2,4-dimethylphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;N-(1-(4-ethoxyphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;N-(1-(2,4-dimethoxyphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-(trifluoromethyl)phenyl)ethyl)acetamide;2-(6-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;2-(6-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-methoxyphenyl)ethyl)acetamide;2-(8-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;2-(8-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-methoxyphenyl)ethyl)acetamide;2-(6-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4H)- ...

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Номер записи: 58
14-03-2019 дата публикации

Biguanide Compositions and Methods of Treating Metabolic Disorders

Номер: US20190076380A1
Автор: Baron Alain D., Beeley Nigel R.A., Fineman Mark S.
Принадлежит:

Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use. 162-. (canceled)63. A method for treating diabetes in a patient in need thereof comprising administering to said patient a pharmaceutical dosage form comprising metformin or a salt thereof , wherein said pharmaceutical dosage form is adapted to have an onset of release of said metformin or a salt thereof at about pH 5.5 or above , and to provide at least 20% less relative bioavailability of metformin as measured by plasma area under curve (AUC) resulting from administration of said pharmaceutical dosage form , compared to an immediate release composition having the same amount of said metformin or a salt thereof.64. The method according to claim 63 , wherein the circulating plasma concentration of metformin resulting from administration of said pharmaceutical dosage form is below about 0.5 μg/mL.65. The method according to claim 63 , wherein the circulating plasma concentration of metformin resulting from administration of said pharmaceutical dosage form is below about 0.25 μg/mL.66. The method according to claim 63 , wherein said pharmaceutical dosage form is adapted to provide 30% less relative bioavailability of metformin compared to an immediate release composition having the same amount of said metformin or a salt thereof.67. The method according to claim 63 , wherein said pharmaceutical dosage form is adapted to provide 40% less relative bioavailability of metformin compared to an immediate release composition having the same amount of said metformin ...

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Номер записи: 59
22-03-2018 дата публикации

USE OF 4-(4-FLUORO-2-METHOXYPHENYL)-N-{3-[(S-METHYLSULFONIMIDOYL)METHYL]PHENYL}-1,3,5-TRIAZIN-2-AMINE FOR TREATING MULTIPLE MYELOMA

Номер: US20180078560A1
Автор: SCHOLZ Arne
Принадлежит: BAYER PHARMA AKTIENGESELLSCHAFT

The present invention relates to the use of 4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A), more particularly (+)-4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A′), for treating multiple myeloma. 18-. (canceled)11: The method according to claim 9 , wherein the pharmaceutical combination comprises the enantiomer (+)-4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1 claim 9 ,3 claim 9 ,5-triazin-2-amine or a physiologically acceptable salt thereof.13: The method according to claim 12 , wherein the enantiomer(+)-4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine or a physiologically acceptable salt thereof is used.14: The method according to claim 10 , wherein the pharmaceutical composition comprises the enantiomer (+)-4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1 claim 10 ,3 claim 10 ,5-triazin-2-amine or a physiologically acceptable salt thereof. The present invention relates to the use of 4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A), more particularly (+)-4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A′), for treating multiple myeloma.The family of cyclin-dependent kinase (CDK) proteins consists of members that are key regulators of the cell division cycle (cell cycle CDK's), that are involved in regulation of gene transcription (transcriptional CDK's), and of members with other functions. CDKs require for activation the association with a regulatory cyclin subunit. The cell cycle CDKs CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclinE, CDK4/cyclinD, and CDK6/cyclinD get activated in a sequential order to drive a cell into and through the cell division cycle. The transcriptional CDKs CDK9/cyclin T and CDK7/cyclin H regulate the activity of ...

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Номер записи: 60
12-06-2014 дата публикации

Composition of pi3k inhibitor and use thereof

Номер: US20140161891A1
Автор: Chen-Sheng Yeh, Chia-Cheng Hou, Dar-Bin Shieh, Wu-Chou Su
Принадлежит: Individual

The present invention is related to a composition of PI3K inhibitor, comprising: 0.01˜10 mg of PI3K inhibitor; 10˜500 mg of poly(lactic-co-glycolic acid) (PLGA) which is encapsulated onto the surface of the PI3K inhibitor and the surface is non-modified by a modifier; and the composition has a size of 10˜1000 nm. Thereby, an excellent effect on suppressing the growth of tumor cells will be achieved by the encapsulation of PI3K inhibitor into PLGA nanomaterials without any modifier on its surface, the optimization of a ratio of PI3K inhibitor to PLGA, and the accordingly slow release of the composition.

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Номер записи: 61
26-03-2015 дата публикации

COMBINATION OF KINASE INHIBITORS AND USES THEREOF

Номер: US20150087627A1
Автор: GUO XIN, Jessen Katayoun, Liu Yi, Ren Pingda, Rommel Christian, Wilson Troy Edward
Принадлежит: INTELLIKINE LLC

The present invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. 1. A method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject , comprising administering to said subject simultaneously or sequentially a combination of (a) a therapeutically effective amount of a PI3-kinase α inhibitor according to a first dosing regimen and (b) a therapeutically effective amount of an mTOR inhibitor according to a second dosing regimen , wherein the PI3-kinase α inhibitor exhibits selective inhibition of PI3-kinase α relative to one or more type I phosphatidylinositol 3-kinases (PI3-kinase) ascertained by an in vitro kinase assay , wherein the one or more type I PI3-kinase is selected from the group consisting of PI3-kinase β , PI3-kinase γ , and PI3-kinase δ , wherein each dosing regimen independently comprising repeating cycles of a treatment period followed by a rest period , wherein at least one dosing regimen has one rest period of more than 0 day , wherein the disease condition associated with PI3-kinase α and/or mTOR is selected from neoplastic condition , autoimmune disease , inflammatory disease , fibrotic disease or kidney disease.23-. (canceled)4. The method of claim 1 , wherein the neoplastic condition is selected from the group consisting of NSCLC claim 1 , head and neck squamous cell carcinoma claim 1 , pancreatic claim 1 , breast and ovarian cancers claim 1 , renal cell carcinoma claim 1 , prostate cancer claim 1 , neuroendocrine cancer claim 1 , and ...

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Номер записи: 62
31-03-2016 дата публикации

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE

Номер: US20160089374A1
Автор: Agresta Samuel V.
Принадлежит:

Provided are compounds useful for treating cancer and methods of treating cancer, for example an advanced solid tumor, such as a glioma, or angioimmunoblastic T-cell lymphoma (AITL). 1. A method of treating a solid tumor characterized by the presence of a mutant allele of isocitrate dehydrogenase 2 (IDH2) comprising administering to a subject in need thereof a therapeutically effective dose of an inhibitor of a mutant IDH2 , wherein the inhibitor is 2-Methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1 ,3 ,5-triazin-2-yl)amino]propan-2-ol or 2-Methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1 ,3 ,5-triazin-2-yl)amino]propan-2-ol methanesulfonate.2. The method of claim 1 , wherein the solid tumor is glioma claim 1 , melanoma claim 1 , chondrosarcoma claim 1 , or cholangiocarcinoma.3. A method of treating angioimmunoblastic T-cell lymphoma (AITL) characterized by the presence of a mutant allele of isocitrate dehydrogenase 2 (IDH2) comprising administering to a subject in need thereof a therapeutically effective dose of an inhibitor of a mutant IDH2 claim 1 , wherein the inhibitor is 2-Methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1 claim 1 ,3 claim 1 ,5-triazin-2-yl)amino]propan-2-ol or 2-Methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1 claim 1 ,3 claim 1 ,5-triazin-2-yl)amino]propan-2-ol methanesulfonate.4. The method of claim 1 , wherein the inhibitor is 2-Methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1 claim 1 ,3 claim 1 ,5-triazin-2-yl)amino]propan-2-ol or a crystalline form thereof 4.5. The method of claim 1 , wherein the inhibitor is 2-Methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1 claim 1 ,3 claim 1 ,5-triazin-2-yl)amino]propan-2-ol methanesulfonate or a crystalline form thereof.6. The method of claim 3 , ...

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Номер записи: 63
31-03-2016 дата публикации

TOPICAL OCULAR ANALGESIC AGENTS

Номер: US20160089375A1
Автор: Appell Kenneth C., David Karen C., Gadd Martha E., Hellberg Mark R., Klimko Peter G.
Принадлежит:

The topical ophthalmic use of certain 2,4-diamino-substituted 1,3-triazines for preventing or alleviating ocular pain in patients is disclosed. Topical ocular pharmaceutical composition are also disclosed. 4. The method of claim 1 , wherein the topical ophthalmic formulation comprises one or more ingredients selected from the group consisting of surfactants; tonicity agents; buffers; preservatives; co-solvents; and viscosity building agents.5. The method of claim 1 , wherein the therapeutically effect amount of a compound of Formula I is between 0.01-3%.6. The method of claim 5 , wherein the therapeutically effect amount of a compound of Formula I is between 0.1-1%.7. The method of claim 1 , wherein the surgical injury is postoperative photorefractive keratectomy (PRK) surgery.11. The method of claim 8 , wherein the topical ophthalmic formulation comprises one or more ingredients selected from the group consisting of surfactants; tonicity agents; buffers; preservatives; co-solvents; and viscosity building agents.12. The method of claim 8 , wherein the therapeutically effect amount of a compound of Formula I is between 0.01-3%.13. The method of claim 12 , wherein the therapeutically effect amount of a compound of Formula I is between 0.1-1%.14. The method of claim 8 , wherein the patient has trauma due to accidental injury or surgical injury claim 8 , uveitis claim 8 , dry eye claim 8 , or diabetic neuropathy. The present application is a continuation of U.S. patent application Ser. No. 14/179,932, filed on Feb. 13, 2014 (pending), which claims priority to U.S. Provisional Application Ser. No. 61/764,166, filed on Feb. 13, 2013, the disclosure of which is specifically incorporated by reference herein.The present invention is directed to compounds and methods for use as topical ocular analgesic agents. In particular embodiments, the present invention is directed to the use of certain 2,4-diamino-substituted 1,3-triazines as topical ocular analgesic agents.Pain is a ...

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Номер записи: 64
12-05-2022 дата публикации

KP372-1-INDUCED DNA DAMAGE AS A CHEMOTHERAPEUTIC APPROACH TO TREAT CANCER

Номер: US20220143033A1
Автор: PATIDAR Praveen, Viera Talysa
Принадлежит:

Disclosed herein are methods of treating a cancer that overexpresses NQO1 comprising administering KP372-1. In some embodiments, KP372-1 is administered with a polymerase inhibitor. 4. The method of claim , comprising administering the compound of Formula (I) or the pharmaceutically-acceptable salt thereof and the compound of Formula (II) or the pharmaceutically-acceptable salt thereof.5. The method of claim 1 , wherein the administering of the compound is oral.6. (canceled)7. (canceled)8. The method of claim 1 , wherein the therapeutically-effective amount of the compound is from about 50 mg to about 2000 mg.911-. (canceled)12. The method of claim 1 , wherein the condition is a cancer.13. The method of claim 12 , wherein the cancer overexpresses NQO1.14. The method of claim 12 , wherein the cancer is pancreatic cancer.15. (canceled)16. The method of claim 12 , wherein the cancer is breast cancer.17. The method of claim 12 , wherein the cancer is colon cancer.18. The method of claim 12 , wherein the cancer is cervical cancer.19. The method of claim 12 , wherein the cancer is lung cancer.20. The method of claim 1 , wherein the administering of the polymerase inhibitor is oral.21. (canceled)22. (canceled)23. The method of claim 1 , wherein the polymerase inhibitor is a poly ADP ribose polymerase (PARP) inhibitor.24. The method of claim 1 , wherein the polymerase inhibitor is a PARP1 inhibitor.25. The method of claim 1 , wherein the polymerase inhibitor is a PARP2 inhibitor.26. The method of claim 23 , wherein the PARP1 inhibitor is talazoparib or a derivative thereof.27. The method of claim 23 , wherein the PARP1 inhibitor is talazoparib tosylate.28. The method of claim 1 , wherein the therapeutically-effective amount of the polymerase inhibitor is from about 0.25 mg to about 1 mg.2933-. (canceled) This application claims the benefit of U.S. Provisional Application No. 63/111,994, filed Nov. 10, 2020, the content of which is incorporated herein by reference in its ...

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Номер записи: 65
06-04-2017 дата публикации

4-OXO-3,4-DIHYDRO-1,2,3-BENZOTRIAZINE AS MODULATORS OF GPR139

Номер: US20170095480A1
Автор: Hitchcock Stephen, Lam Betty, Monenschein Holger, Reichard Holly
Принадлежит: Takeda Pharmaceutical Company Limited

The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: 3. The method according to wherein m is 0.4. The method according to wherein Ris Calkyl.5. The method according to wherein Ris selected from the group consisting of methyl claim 1 , ethyl claim 1 , and isopropyl.6. The method according to wherein Ris methyl.7. The method according to wherein n is 1 and Ris trifluoromethoxy.8. The method according to wherein m is 1.9. The method according to wherein m is 2.10. The method according to claim 1 , wherein the compound is selected from the group of compounds consisting of:2-(5-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;N-(1-(4-bromophenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;N-(1-(4-methoxyphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;N-(1-(2,4-dimethylphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;N-(1-(4-ethoxyphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;N-(1-(2,4-dimethoxyphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-(trifluoromethyl)phenyl)ethyl)acetamide;2-(6-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;2-(6-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-methoxyphenyl)ethyl)acetamide;2-(8-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;2-(8-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-methoxyphenyl)ethyl)acetamide;2-(6-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;2-(6-chloro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;2-(6-chloro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-methoxyphenyl)ethyl)acetamide;2-(7-chloro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;2-(8-chloro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl ...

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Номер записи: 66
08-04-2021 дата публикации

Compounds and Compositions for Ossification and Methods Related Thereto

Номер: US20210100806A1
Автор: Boden Scott D., Sangadala Sreedhara
Принадлежит:

The disclosure relates to compounds and compositions for forming bone and methods related thereto. In one embodiment, the disclosure relates to a composition comprising a compound disclosed herein, such as 2,4-diamino-1,3,5-triazine derivatives or salts thereof, for use in bone growth processes. In a typical embodiment, a bone graft composition is implanted in a subject at a site of desired bone growth or enhancement. 1. A method of treating osteogenesis imperfecta comprising administering an effective amount of 1-(4-chlorophenyl)-5-isopropyl-biguanide or salt thereof to a subject in need thereof.2. The method of wherein the subject is a human subject.3. The method of wherein the subject is diagnosed with osteogenesis imperfecta.4. A method of treating osteogenesis imperfecta comprising administering an effective amount of 1-(4-chlorophenyl)-4 claim 2 ,6-diamino-1 claim 2 ,2-dihydro-2 claim 2 ,2-dimethyl-1 claim 2 ,3 claim 2 ,5-triazine or salt thereof to a subject in need thereof.5. The method of wherein the subject is a human subject.6. The method of wherein the subject is diagnosed with osteogenesis imperfecta. This application is a continuation of U.S. application Ser. No. 16/732,959 filed Jan. 2, 2020, which is a continuation of U.S. application Ser. No. 15/801,964 filed Nov. 2, 2017 that granted as U.S. Pat. No. 10,537,577 on Jan. 21, 2020, which is a continuation of U.S. application Ser. No. 15/334,030 filed Oct. 25, 2016 that granted as U.S. Pat. No. 9,808,464 on Nov. 7, 2017, which is a division of U.S. application Ser. No. 13/816,312 filed Feb. 11, 2013 that granted as U.S. Pat. No. 9,511,071 on Dec. 6, 2016, which is the National Stage Application of International Application No. PCT/US2011/048252 filed Aug. 18, 2011, which claims priority to U.S. Provisional Application No. 61/374,667 filed Aug. 18, 2010 and U.S. Provisional Application No. 61/479,910 filed Apr. 28, 2011. The entirety of each of these applications is hereby incorporated by reference for ...

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Номер записи: 67
13-04-2017 дата публикации

COMBINATIONS OF AN FGFR INHIBITOR AND AN IGF1R INHIBITOR

Номер: US20170100406A1
Автор: JOVCHEVA Eleonora, Perera Timothy Pietro Suren
Принадлежит: ASTEX THERAPEUTICS LTD

The invention relates to a combination of a FGFR inhibitor and an IGF1R inhibitor. The combination is for use in the treatment of a proliferative disorder, in particular for the treatment of cancer. The FGFR inhibitor and the IGFR inhibitor can be administered simultaneously, separately or sequentially. The invention further relates to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a combination according to the invention. 1. A combination of a FGFR inhibitor and an IGF1R inhibitor.2. The combination according to wherein the FGFR inhibitor is selected from N-(3 claim 1 ,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1 claim 1 ,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof claim 1 , and N-(2-fluoro-3 claim 1 ,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido [2 claim 1 ,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof.3. The combination according to wherein the FGFR inhibitor is N-(3 claim 2 ,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1 claim 2 ,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof.4. The combination according to wherein the FGFR inhibitor is N-(2-fluoro-3 claim 2 ,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2 claim 2 ,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof.5. The combination according to any one of the preceding claims wherein the IGF inhibitor is selected from GSK1838705A and BMS-754807.6. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a combination according to any one of the preceding claims.7. A combination as claimed in any one of to or a pharmaceutical composition as claimed in for use as a medicine.8. The use of a combination as claimed in any one of to or a pharmaceutical ...

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Номер записи: 68
04-04-2019 дата публикации

COMPOSITIONS AND METHODS FOR PROPHYLAXIS AND THERAPY FOR MENIERE'S DISEASE

Номер: US20190099428A1
Автор: Zhang Lixin
Принадлежит:

Provided are articles of manufacture, compositions and methods for prophylaxis and/or therapy for disorders involving dizziness and/or vertigo. The articles of manufacture and compositions contain lamotrigen and/or bupropion. The compositions include pharmaceutical compositions which are intended to alleviate dizziness and/or vertigo. In certain aspects the disclosure includes articles of manufacture and kits which include printed material which provides an indication that the articles or compositions are intended to be used for prophylaxis and/or therapy of Meniere's Disease or a symptom thereof. 1. A method comprising administering to an individual diagnosed with Meniere's Disease a pharmaceutical composition comprising an effective amount of lamotrigine or a pharmaceutically acceptable salt thereof such that the effective amount of the lamotrigine or the pharmaceutically acceptable salt thereof is sufficient to reduce dizziness that is caused by the Meniere's Disease in the individual , wherein the lamotrigine or the pharmaceutically acceptable salt thereof is the only bioactive compound in the pharmaceutical composition that is effective to treat the dizziness caused by the Meniere's Disease , wherein the individual is also diagnosed with phobic postural vertigo and/or chronic subjective dizziness , the method further comprising administering to the individual a pharmaceutical composition comprising an effective amount of bupropion or a pharmaceutically acceptable salt thereof such that the phobic postural vertigo and/or chronic subjective dizziness is also reduced.2. The method of claim 1 , wherein the individual is diagnosed with the phobic postural vertigo.3. The method of claim 1 , wherein the individual is diagnosed with the chronic subjective dizziness.4. The method of claim 1 , wherein the effective amount of lamotrigine comprises 25 mg to 400 mg.5. The method of claim 1 , wherein the effective amount of bupropion or the pharmaceutically acceptable salt ...

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Номер записи: 69
23-04-2015 дата публикации

NOVEL ANTITUMOR AGENT COMPRISING COMBINATION OF THREE AGENTS

Номер: US20150110864A1
Автор: Uchida Junji
Принадлежит: TAIHO PHARMACEUTICAL CO., LTD.

A primary object of the present invention is to provide a novel combination therapy that exhibits a notable antitumor effect. 1. An antitumor agent comprising a combination of oxaliplatin , paclitaxel , and a combination drug containing tegafur , gimeracil , and oteracil potassium.2. The antitumor agent according to claim 1 , wherein the combination drug contains tegafur claim 1 , gimeracil claim 1 , and oteracil potassium at a molar ratio of tegafur:gimeracil:oteracil potassium=1:0.4:1.3. The antitumor agent according to claim 1 , which is in a pharmaceutical form comprising the combination drug containing tegafur claim 1 , gimeracil claim 1 , and oteracil potassium claim 1 , a preparation containing oxaliplatin claim 1 , and a preparation containing paclitaxel.4. The antitumor agent according to claim 3 , wherein the combination drug containing tegafur claim 3 , gimeracil claim 3 , and oteracil potassium is administered by oral administration claim 3 , and the preparation containing oxaliplatin and the preparation containing paclitaxel are individually administered by an administration route selected from the group consisting of intravenously claim 3 , intramuscularly claim 3 , and subcutaneously.5. The antitumor agent according to claim 3 , wherein the combination drug containing tegafur claim 3 , gimeracil claim 3 , and oteracil potassium claim 3 , the preparation containing oxaliplatin claim 3 , and the preparation containing paclitaxel are administered simultaneously or at one or more intervals.6. The antitumor agent according to claim 1 , wherein oxaliplatin is contained at a daily dose of 80 to 150 mg/m claim 1 , paclitaxel is contained at a daily dose of 50 to 500 mg/m claim 1 , and the combination drug containing tegafur claim 1 , gimeracil claim 1 , and oteracil potassium is contained at a daily dose such that tegafur is contained in an amount of 60 to 120 mg/m.7. The antitumor agent according to claim 3 , wherein the pharmaceutical form of paclitaxel is ...

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Номер записи: 70
03-07-2014 дата публикации

DRUG FORMULATIONS HAVING IMPROVED PHARMACOKINETIC PROPERTIES

Номер: US20140186444A1
Автор: Hayauchi Yutaka, Heinig Roland, Pauli Kerstin, Serno Peter
Принадлежит:

The present application relates to novel drug formulations of vardenafil which dissolve rapidly in the mouth and lead to increased bioavailability and to a plateau-like plasma concentration profile, and to processes for their preparation. 1. Drug formulation which disintegrates rapidly in the mouth and comprises vardenafil , characterized in that at least 80% of the vardenafil dose in the substance form employed dissolves at 25° C. in 10 ml of physiological saline and , the rate of release from the drug formulation in 900 ml of physiological saline within the first 5 minutes in the USP pedal stirrer apparatus at 50 rotations per minute at 37° C. is at least 70%.2. Drug formulation according to claim 1 , comprising vardenafil in the form of a salt with an acid or vardenafil with an acid.3. Drug formulation according to claim 2 , comprising vardenafil hydrochloride or vardenafil hydrochloride trihydrate.4. Drug formulation according to claim 3 , comprising vardenafil hydrochloride or vardenafil hydrochloride trihydrate in micronized form with a mean particle size of less than 20 pm.5. Drug formulation according to claim 1 , comprising from 40% to 99% of sugar alcohols.6. Drug formulation according to in a drug packaging with a note on the information leaflet claim 1 , label or packaging box that the drug formulation is to be inserted into the oral cavity and claim 1 , after its disintegration claim 1 , to be swallowed. This application is a continuation of U.S. patent application Ser. No. 11/885,019, filed Jun. 9, 2008, set to issue as U.S. Pat. No. 8,613,950 on Dec. 24, 2013, This which application is a National Stage Application of International Application Number PCT/EP2006/001393, filed on Feb. 16, 2006, which application claims priority to German Patent Application No. 102005009240.3, filed on Mar. 1, 2005, the contents of each of which are incorporated herein by reference.The present application relates to novel drug formulations of vardenafil which disintegrate ...

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Номер записи: 71
29-04-2021 дата публикации

SOLID FORMS OF 2-(3,5-DICHLORO-4-((5-ISOPROPYL-6-OXO-1,6-DIHYDROPYRIDAZIN-3-YL)OXY)PHENYL)-3,5-DIOXO-2,3,4,5-TETRAHYDRO-1,2,4-TRIAZINE-6-CARBONITRILE

Номер: US20210122740A1
Автор: BATCHU Pavan Karthik, Jonas Marco, MIRMEHRABI Mahmoud
Принадлежит:

The present invention is directed to morphic forms, co-crystals, salts, and amorphous solid dispersions of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile. 1. A crystalline salt of 2-(3 ,5-dichloro-4-((5-isopropyl-6-oxo-1 ,6-dihydropyridazin-3-yl)oxy)phenyl)-3 ,5-dioxo-2 ,3 ,4 ,5-tetrahydro-1 ,2 ,4-triazine-6-carbonitrile (“Compound A”).2. The crystalline salt of claim 1 , characterized as having a counter-ion claim 1 , wherein the counter-ion is selected from L-lysine claim 1 , L-arginine claim 1 , 2-hydroxy-N claim 1 ,N claim 1 ,N-trimethylethan-1-aminium claim 1 , diethylamine claim 1 , ethanolamine claim 1 , ethanol-2-diethylamine claim 1 , Na claim 1 , Mg claim 1 , K claim 1 , Ca claim 1 , diethanolamine claim 1 , triethanolamine claim 1 , L-histidine claim 1 , and meglumine.3. The crystalline salt of claim 1 , wherein the counter-ion is L-lysine.4. The crystalline salt of claim 1 , wherein the counter-ion is L-arginine.5. The crystalline salt of claim 1 , wherein the counter-ion is 2-hydroxy-N claim 1 ,N claim 1 ,N-trimethylethan-1-aminium.6. The crystalline salt of claim 3 , characterized by an X-ray powder diffraction pattern including peaks at about 8.70 claim 3 , 9.22 claim 3 , 11.3 claim 3 , 17.0 claim 3 , and 24.8 degrees 2θ claim 3 , wherein the x-ray powder diffraction pattern is obtained using a Cu Kα radiation source (1.54 Å).7. The crystalline salt of claim 3 , having an X-ray diffraction pattern substantially similar to that set forth in .8. (canceled)9. The crystalline salt of claim 4 , having an X-ray diffraction pattern substantially similar to that set forth in any one of .10. (canceled)11. The crystalline salt of claim 5 , having an X-ray diffraction pattern substantially similar to that set forth in .12. (canceled)13. The crystalline salt of claim 1 , having a purity of Compound A of greater than 90% by weight.14. (canceled)15. (canceled)16. A ...

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Номер записи: 72
28-04-2016 дата публикации

TREATMENT OF OBESITY AND PULMONARY ARTERIAL HYPERTENSION

Номер: US20160113933A1
Автор: Chi Yuling, Schuster Victor L.
Принадлежит: ALBERT EINSTEIN COLLEGE OF MEDICINE, INC.

Disclosed are methods and compositions for treating pulmonary arterial hypertension and/or obesity using inhibitors of prostaglandin transporter (PGT) activity. 2. The method of claim 1 , wherein W is NR5.3. The method of claim 1 , wherein R6 is NR94. The method of claim 1 , wherein at least one of R4 claim 1 , R5 and R9 is H.5. The method of claim 1 , wherein all of R4 claim 1 , R5 and R9 are H.6. The method of claim 1 , wherein one of X1 and X2 is H claim 1 , and the other is halogen claim 1 , —CF claim 1 , —CH claim 1 , —COH claim 1 , —COCH claim 1 , —OCHor phenyl.7. The method of claim 1 , wherein one of X3 and X4 is —OH claim 1 , and the other is halogen claim 1 , —COH or —COCH.8. The method of claim 1 , wherein X7 is H claim 1 , —CFor —OCH.9. The method of claim 1 , wherein X1 is located in meta position and X2 is located in para position.10. The method of claim 1 , wherein X1 is located in ortho position and X2 is located in para position.11. The method of claim 1 , wherein X3 is in meta position and X4 is in para position.12. The method of claim 1 , wherein X5 or X6 is in meta position.13. The method of claim 1 , wherein X5 or X6 is in para position.19. The method of claim 1 , where R5 is H.21. The method of claim 1 , wherein the halogen is Br claim 1 , Cl or F.26. A method of treating a condition selected from the group consisting of obesity and pulmonary arterial hypertension comprising administering to a subject having obesity and/or pulmonary arterial hypertension a prostaglandin transporter inhibitor in an amount effective to treat obesity and/or pulmonary arterial hypertension.2729-. (canceled) This application claims the benefit of U.S. Provisional Patent Application No. 61/836,200, filed Jun. 18, 2013, the contents of which are incorporated herein by reference in their entirety.Various publications are referred to in parentheses throughout this application. Full citations for these references may be found at the end of the specification immediately ...

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Номер записи: 73
26-04-2018 дата публикации

5-HT2B Antagonists

Номер: US20180111908A1
Автор: Huang Niu, LIN Xingyu, Zhou Yu
Принадлежит: National Institute of Biological Sciences, Beijing

The invention provides novel compounds and compositions comprising a 5-HTantagonist of formula I: 2. The composition of wherein:{'sup': 1', '2, 'Rand Rare independently H or methyl;'}{'sup': 3', '4', '3', '4, 'Rand Rare independently C1-C3 alkyl, or Rand Rare joined to form C4-C7 cycloalkyl;'}{'sup': 5', '9, 'Rand Rare independently H, halogen, methyl or methoxyl; and'}{'sup': 6', '8', '10', '10', '10', '10', '10', '10, 'R-Rare independently H, halogen, methyl, —OR, COR, COOR, or CONRR, wherein each Ris independently H or C1-C4 alkyl.'}3. The composition of wherein:{'sup': 1', '2, 'Rand Rare independently H or methyl;'}{'sup': 3', '4', '3', '4, 'Rand Rare methyl or Rand Rform cyclopentyl or cyclohexyl;'}{'sup': '5', 'Ris H, halogen, methyl or methoxyl;'}{'sup': 6', '10', '10', '10', '10', '10', '10, 'Ris H, halogen (F, Cl, Br, I), methyl, methoxyl, or —OR, COR, COOR, or CONRR, wherein each Ris independently H or C1-C4 alkyl.'}{'sup': 7', '10', '10', '10, 'Ris H, halogen, methyl, —ORor COOR, wherein each Ris independently H or C1-C3 alkyl;'}{'sup': '8', 'Ris H, halogen, methyl or methoxyl; and'}{'sup': '9', 'Ris H or methyl.'}5. The composition of wherein:{'sup': 1', '2', '6', '7', '8, 'R═H, R═H, Ris Cl, R═H, R═H;'}{'sup': 1', '2', '6', '7', '8, 'R═H, R═H, Ris Br, R═H, R═H;'}{'sup': 1', '2', '6', '7', '8, 'R═H, R═H, Ris I, R═H, R═H;'}{'sup': 1', '2', '6', '7', '8, 'R═H, R═H, Ris CONHEt, R═H, R═H;'}{'sup': 1', '2', '6', '7', '8, 'R═H, R═H, Ris COOPr, R═H, R═H;'}{'sup': 1', '2', '6', '7', '8, 'R═H, R═H, Ris COOEt, R═Me, R═H;'}{'sup': 1', '2', '6', '7', '8, 'R═H, R═H, Ris COOEt, R═Me, R═Br;'}{'sup': 1', '2', '6', '7', '8, 'R═Me, R═H, Ris COOEt, R═H, R═H;'}{'sup': 1', '2', '6', '7', '8, 'R═Me, R═Me, Ris COOEt, R═H, R═H; or'}{'sup': 1', '2', '6', '7', '8, 'R═H, R═H, Ris COPr, R═H, R═H.'}9. The composition of wherein the salt is an acid addition salt derived from an inorganic acid or nontoxic organic acid.10. The composition of wherein the salt is an acid addition salt ...

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Номер записи: 74
13-05-2021 дата публикации

EXPANSION OF TUMOR INFILTRATING LYMPHOCYTES (TILS) WITH ADENOSINE A2A RECEPTOR ANTAGONISTS AND THERAPEUTIC COMBINATIONS OF TILS AND ADENOSINE A2A RECEPTOR ANTAGONISTS

Номер: US20210137930A1
Автор: FARDIS Maria
Принадлежит: Iovance Biotherapeutics, Inc.

Methods of expanding tumor infiltrating lymphocytes (TILs) in the presence of an adenosine A2A receptor (A2aR) antagonist, such as vipadenant, CPI-444 (ciforadenant), SCH58261, SYN115, ZM241385, SCH420814, a xanthine superfamily A2aR antagonist, or related adenosine receptor 2A antagonist, and uses of expanded TILs in the treatment of diseases such as cancer are disclosed herein. In addition, therapeutic combinations of TILs and A2aR antagonists, including compositions and uses thereof in the treatment of diseases such as cancer are disclosed herein. 1. A method of treating cancer with a population of tumor infiltrating lymphocytes (TILs) comprising:(a) obtaining a first population of TILs from a tumor resected from a patient by processing a tumor sample obtained from the patient into multiple tumor fragments;(b) adding the tumor fragments into a closed system;(c) performing a first expansion by culturing the first population of TILs in a cell culture medium comprising IL-2 and optionally OKT-3 to produce a second population of TILs, wherein the first expansion is performed in a closed container providing a first gas-permeable surface area, wherein the first expansion is performed for about 3-14 days to obtain the second population of TILs, wherein the second population of TILs is at least 50-fold greater in number than the first population of TILs, wherein the transition from step (b) to step (c) occurs without opening the system, and optionally the medium comprises an adenosine 2A receptor (A2aR) antagonist;(d) performing a second expansion by supplementing the cell culture medium of the second population of TILs with additional IL-2, OKT-3, and antigen presenting cells (APCs), to produce a third population of TILs, wherein the second expansion is performed for about 7-14 days to obtain the third population of TILs, wherein the third population of TILs is a therapeutic population of TILs, wherein the second expansion is performed in a closed container providing a ...

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Номер записи: 75
13-05-2021 дата публикации

SELECTING PATIENTS FOR THERAPY WITH ADENOSINE SIGNALING INHIBITORS

Номер: US20210137931A1
Автор: I Mingchao, LINGHU Bolan, MERCHANT Melinda, SACHSENMEIER Kris, XIE
Принадлежит:

Described herein are measures of the relative expression levels, within a given sample from a subject, of an ACPP transmembrane splice variant to the expression level of one or more ACPP non-transmembrane splice variant(s). The measures, designated ρ, show correlation with clinical outcome for the subject. In some cases, values of ρ exceeding a predetermined cutoff can be associated with poorer outcomes. Methods of determining ρ and assigning the predetermined cutoff value are described. Methods of treating cancer are also described. 1. A method for treating an elevated adenosine cancer in a subject , comprising:diagnosing the subject with an elevated adenosine cancer when, in a sample from the subject, a measure ρ of the relative expression levels of an ACPP TM variant to the expression level of one or more ACPP non-TM variant(s) exceeds a predetermined cutoff value; andadministering an effective amount of an adenosine signaling inhibitor to the diagnosed subject.2. The method of claim 1 , wherein the cancer is prostate cancer claim 1 , lung cancer claim 1 , bladder cancer claim 1 , or other cancer.3. The method of any one of to claim 1 , wherein the predetermined cutoff value of ρ is the median claim 1 , mean claim 1 , top quartile claim 1 , top quintile claim 1 , top decile claim 1 , or other statistical measure claim 1 , of ρ in a selected group of reference samples.4. The method of any one of to claim 1 , wherein ρ is the log 2 of the ratio of the expression level of ACPP variant 2 to the expression level of ACPP variant 1 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 claim 1 , 7 claim 1 , 8 claim 1 , 9 claim 1 , or the total expression level of a combination thereof.5. The method of any one of to claim 1 , wherein ρ is the log 2 of the ratio of the expression level of ACPP variant 2 to the expression level of ACPP variant 1.6. The method of any one of to claim 1 , wherein ρ is the log 2 of the ratio of the expression level of ACPP variant 2 to the expression ...

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Номер записи: 76
07-05-2015 дата публикации

Modulators Of TNF-Alpha Signaling

Номер: US20150126512A1
Автор: Biemann Hans-Peter, HIRTH Bradford H., KANE John L., Nahill Sharon R., Qiao Shuang, Sneddon Scott F., Vinick Frederic, Williams John M.
Принадлежит: Genzyme Corporation

The present invention provides compounds which are modulators of TNF-α signaling and methods of use thereof for treating a patient having a TNF-α mediated condition. The compounds can be represented by the following structural formulas: 2. The method of claim 1 , wherein R5 is substituted or unsubstituted benzyl.3. The method of claim 2 , wherein R5 is benzyl having one or more substituents independently selected from the group consisting of halogen claim 2 , linear C1-C4-alkoxy and branched C1-C4-alkoxy.4. The method of claim 3 , wherein R5 is benzyl having one or more substituents independently selected from the group consisting of chloro and methoxy.5. The method of claim 1 , wherein R5 is C3-C8-cycloalkyl claim 1 , C3-C8-cycloalkyl-C1-C4-alkyl or substituted or unsubstituted phenyl-C2-C4-alkyl.6. The method of claim 4 , wherein R5 is selected from the group consisting of 2-phenethyl claim 4 , cyclohexyl and cyclopentylethyl.7. The method of claim 1 , wherein R7 is phenyl having one or more substituents independently selected from the group consisting of halogen claim 1 , linear C1-C6-alkyl claim 1 , branched C1-C6-alkyl and cyclic C3-C6-alkyl and trifluoromethyl.8. The method of claim 7 , wherein R7 is phenyl having one or more substituents independently selected from the group consisting of fluoro claim 7 , chloro claim 7 , linear C1-C4-alkyl claim 7 , and branched C1-C4-alkyl. This application is a continuation application of U.S. Ser. No. 13/946,389 filed Jul. 19, 2013, which is a divisional application of U.S. Ser. No. 11/292,325, filed Dec. 1, 2005, now U.S. Pat. No. 8,518,999, which is a continuation application of U.S. Ser. No. 10/797,244, filed Mar. 10, 2004, now U.S. Pat. No. 7,034,031, which is a divisional application of U.S. Ser. No. 09/852,965, filed May 10, 2001, now U.S. Pat. No. 6,969,728, which claims the benefit of U.S. Provisional Application No. 60/203,784, filed May 12, 2000, and U.S. Provisional Application No. 60/205,213, filed May 18, ...

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Номер записи: 77
04-05-2017 дата публикации

TREATMENT OF COGNITIVE DISORDERS

Номер: US20170119775A1
Автор: Hasse Birgit, Koopmans Guido
Принадлежит:

The technology provided herein relates to the novel use of compounds for improving cognition, concentration capacity, learning capacity and/or memory retentiveness, in particularly for the treatment and/or prophylaxis of cognitive, concentration capacity, learning capacity and/or memory retentiveness disorders. 114-. (canceled)16. The method according to claim 15 , wherein the compound is a 7-(4-tert-butylcyclohexyl)-imidazotriazinone.18. The method according to claim 17 , wherein the stereoisomer of the compound is the R or S enantiomer.19. The method according to claim 15 , wherein said compound is administered at daily dosages between 0.1 mg-150 mg/body claim 15 , preferable 1 mg-100 mg/body and more preferable 2 mg-50 mg/body.20. The method according to claim 15 , wherein the diminished cognitive processes is experienced in several patient groups claim 15 , e.g. by schizophrenic claim 15 , depressive or psychotic patients and patients with attention deficit hyperactivity disorder (ADHD) claim 15 , Parkinson's disease claim 15 , mild cognitive impairment (MCI) claim 15 , dementia claim 15 , anxiety claim 15 , age associated memory impairment claim 15 , Alzheimer's Disease or post-traumatic stress disorder and in a range of neurodegenerative diseases in addition to Parkinson's Disease and Alzheimer's Disease.21. The method according to claim 15 , wherein the diminished cognitive processes refer to the difficulties with attention claim 15 , learning claim 15 , memory and executive function (relevant reactions to external stimuli). These can include: deficits in attention claim 15 , disorganized thinking claim 15 , slow thinking claim 15 , difficulty in understanding claim 15 , poor concentration claim 15 , impairment of problem solving claim 15 , poor memory claim 15 , difficulty in expressing thoughts and/or difficulty in integrating thoughts claim 15 , feelings and behaviour and extinction of irrelevant thoughts as well as attention and vigilance claim 15 , ...

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Номер записи: 78
24-07-2014 дата публикации

FLUORESCENT WHITENING AGENT AQUEOUS SOLUTIONS

Номер: US20140203212A1
Автор: "Berte Ferruccio", Alioli Paolo, Brena Marco
Принадлежит: 3V Sigma S.p.A

The present invention relates to a composition comprising a fluorescent whitening agent and a tertiary alkanolamine, a stable aqueous solution of such a composition and use of such composition for the bleaching of textile fibres or paper. 2. Composition according to claim 1 , wherein said compound of formula (I) claim 1 , Rand Rare selected in the group consisting of C-Calkyl groups and Ris a hydroxyethyl group.3. Composition according to claim 1 , wherein said compound of formula (I) is 2-(dimethylamino)ethanol.6. Compound of formula (III) according to claim 5 , wherein X′ is an ammonium ion derived from a compound of formula (I) wherein Rand Rare selected in the group consisting of C-Calkyl groups and Ris a hydroxyethyl group.7. Compound of formula (III) according to claim 5 , wherein X′ is an ammonium ion derived from 2-(dimethylamino)ethanol.9. Process for preparing a compound according to claim 6 , comprising the steps of:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'mixing a compound of formula (II) with a compound of formula (I) defined in in a suitable solvent medium; and'}reacting at a temperature between 20° C. and 100° C.10. Aqueous solution comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '3 to 20% by weight of at least one compound of formula (I) defined in or mixtures thereof;'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '6 to 40% by weight of at least one compound of formula (II) defined in or mixtures thereof;'}50 to 90% by weight of water and0 to 1% by weight of additives.11. Use of a aqueous solution according to the previous claim in the whitening treatment of paper.12. Use of a aqueous solution according to in the whitening treatment of natural claim 10 , semisynthetic or synthetic fibres. The present invention relates to a composition comprising a fluorescent whitening agent and a tertiary alkanolamine, a stable aqueous solution of such a composition and use of such composition for the bleaching of textile fibres or paper. ...

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Номер записи: 79
27-05-2021 дата публикации

OCULAR PHARMACEUTICAL COMPOSITIONS

Номер: US20210154201A1
Автор: Levin Marc H., Verkman Alan S.
Принадлежит:

The disclosure provides, inter alia, topical pharmaceutical compositions comprising active agents, methods for increasing tear production using the topical pharmaceutical compositions, and methods for treating dry eye disorders using the topical pharmaceutical compositions. 2. The method of claim 1 , wherein the patient has a dry eye disease.3. The method of claim 1 , comprising administering to the eye of the patient at least about 5 micrograms of compound A.4. The method of claim 1 , comprising:administering to the eye of the patient at least about 5 micrograms of compound C.5. The method of claim 1 , wherein the topically administering is effective to produce a concentration of the at least one active agent of at least about 500 nM in the tear fluid of the eye at about 1 hour to about 12 hours following administration.7. The method of claim 6 , wherein the patient has a dry eye disease.8. The method of claim 6 , wherein the topically administering is effective to produce a concentration of compound A of at least about 500 nM in the tear fluid of the eye at about 1 hour to about 12 hours following administration.10. The method of claim 9 , wherein the topically administering is effective to produce a concentration of the at least one active agent of at least about 500 nM in the tear fluid of the eye at about 1 hour to about 12 hours following administration.11. The method of claim 9 , comprising administering once or twice per day to the eye of the patient at least about 5 micrograms of compound A.12. The method of claim 9 , comprising administering once or twice per day to the eye of the patient at least about 5 micrograms of compound C.13. The method of claim 9 , wherein the topically administering is effective to increase tear production in the eye of the patient.15. The method of claim 14 , wherein topically administering includes topically administering once or twice per day.16. The method of claim 14 , wherein the topically administering is effective to ...

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Номер записи: 80
14-05-2015 дата публикации

THERAMUTEIN MODULATORS

Номер: US20150133441A1
Автор: Housey Gerard M.
Принадлежит:

This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein. 2. The method of wherein Xis N.3. The method of wherein Xis N.5. The method of wherein Xis N.6. The method of wherein Xis N.851-. (canceled)52. A method for determining whether a substance is an inhibitor or an activator of a theramutein which is capable of eliciting a detectable phenoresponse claim 5 , which comprises:a) incubating a first cell which expresses the theramutein at a substantially constant level with the substance;b) incubating a second cell which expresses a corresponding prototheramutein at a substantially constant level with a known inhibitor or activator of the prototheramutein;c) comparing a phenoresponse of the second cell to the known inhibitor or activator of the prototheramutein to the phenoresponse of the first cell to the substance; andd) determining that the phenoresponse of the first cell is inhibited or activated to at least the same degree as the phenoresponse of the second cell is inhibited or activated by the known inhibitor or activator of the prototheramutein, thereby identifying the substance as an inhibitor or an activator of the theramutein.53. The method of claim 52 , wherein the phenoresponse of the cell expressing the theramutein to the substance is greater than the phenoresponse of the cell expressing the prototheramutein to the known inhibitor or activator of the theramutein.54. A method for determining whether a substance is a specific inhibitor or specific activator of a theramutein claim 52 , which comprises:a) providing a test cell which ...

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Номер записи: 81
10-05-2018 дата публикации

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE

Номер: US20180125850A1
Автор: Agresta Samuel V.
Принадлежит:

Provided are compounds useful for treating cancer and methods of treating cancer, for example an advanced solid tumor, such as a glioma, or angioimmunoblastic T-cell lymphoma (AITL). 18-. (canceled)10. The method of claim 9 , wherein the crystalline form is selected from{'figref': {'@idref': 'DRAWINGS', 'FIG. 1'}, 'a) the crystalline form characterized by an X-ray powder diffraction pattern substantially similar to ,'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 2'}, 'b) the crystalline form characterized by an X-ray powder diffraction pattern substantially similar to ,'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 34'}, 'c) the crystalline form characterized by an X-ray powder diffraction pattern substantially similar to ,'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 37'}, 'd) the crystalline form characterized by an X-ray powder diffraction pattern substantially similar to ,'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 38'}, 'e) the crystalline form characterized by an X-ray powder diffraction pattern substantially similar to , and'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 39'}, 'f) the crystalline form characterized by an X-ray powder diffraction pattern substantially similar to .'}11. The method of claim 9 , wherein the solid tumor is brain tumor claim 9 , melanoma claim 9 , chondrosarcoma claim 9 , or cholangiocarcinoma.12. The method of claim 11 , wherein the brain tumor is glioma.13. The method of claim 11 , wherein the brain tumor is glioblastoma multiforme.14. The method of claim 11 , wherein the brain tumor is astrocytic tumor claim 11 , oligodendroglial tumor claim 11 , oligoastrocytic tumor claim 11 , ependymoma claim 11 , medulloblastoma; primitive neuroectodermal tumor claim 11 , schwannoma claim 11 , meningioma claim 11 , meatypical meningioma claim 11 , anaplastic meningioma; or pituitary adenoma.15. The method of claim 9 , wherein the crystalline form of 2-methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl] amino}-1 claim 9 ,3 claim 9 , ...

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Номер записи: 82
01-09-2022 дата публикации

FORMULATIONS OF AN AXL/MER INHIBITOR

Номер: US20220273663A1
Автор: Muller Francis X., Rocco William L.
Принадлежит:

The present application relates to pharmaceutical formulations and dosage forms of an AXL/MER inhibitor, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, including methods of preparation thereof, which are useful in the treatment of AXL/MER mediated diseases such as cancer. 2. The pharmaceutical formulation of claim 1 , wherein the organic acid is citric acid claim 1 , ascorbic acid claim 1 , fumaric acid claim 1 , malic acid claim 1 , sorbic acid claim 1 , or tartaric acid.3. The pharmaceutical formulation of claim 1 , wherein the organic acid is citric acid.4. The pharmaceutical formulation of claim 1 , comprising about 1 wt % to about 50 wt % of organic acid.5. The pharmaceutical formulation of claim 1 , comprising about 5 wt % to about 40 wt % of organic acid.6. The pharmaceutical formulation of claim 1 , comprising about 5 wt % to about 30 wt % of organic acid.7. The pharmaceutical formulation of claim 1 , comprising about 10 wt % to about 20 wt % of organic acid.8. The pharmaceutical formulation of claim 1 , comprising about 10 wt % or about 20 wt % of organic acid.9. The pharmaceutical formulation of claim 1 , comprising about 1 wt % to about 20 wt % of Compound I.10. The pharmaceutical formulation of claim 1 , comprising about 2 wt % to about 15 wt % of Compound I.11. The pharmaceutical formulation of claim 1 , comprising about 3 wt % or about 12 wt % of Compound I.12. The pharmaceutical formulation of claim 1 , wherein the surfactant is a poloxamer.13. The pharmaceutical formulation of claim 1 , wherein the surfactant is poloxamer 407 or poloxamer 188.14. The pharmaceutical formulation of claim 1 , wherein the surfactant is poloxamer 407.15. The pharmaceutical formulation of claim 1 , comprising about 1 wt % to about 20 wt % of surfactant.16. The pharmaceutical formulation of claim 1 , comprising about 5 wt % to about 15 wt % of surfactant.17. The pharmaceutical formulation of claim 1 , comprising about 5 wt % to about 10 wt % of ...

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Номер записи: 83
23-04-2020 дата публикации

Compounds and Compositions for Ossification and Methods Related Thereto

Номер: US20200121687A1
Автор: Boden Scott D., Sangadala Sreedhara
Принадлежит:

The disclosure relates to compounds and compositions for forming bone and methods related thereto. In one embodiment, the disclosure relates to a composition comprising a compound disclosed herein, such as 2,4-diamino-1,3,5-triazine derivatives or salts thereof, for use in bone growth processes. In a typical embodiment, a bone graft composition is implanted in a subject at a site of desired bone growth or enhancement. 1. A method of treating osteoporosis comprising administering an effective amount of 1-(4-chlorophenyl)-5-isopropyl-biguanide or salt thereof to a subject in need thereof.2. The method of wherein the subject is a human subject.3. The method of wherein the subject is diagnosed with osteoporosis.4. A method of treating osteoporosis comprising administering an effective amount of 1-(4-chlorophenyl)-4 claim 2 ,6-diamino-1 claim 2 ,2-dihydro-2 claim 2 ,2-dimethyl-1 claim 2 ,3 claim 2 ,5-triazine or salt thereof to a subject in need thereof.5. The method of wherein the subject is a human subject.6. The method of wherein the subject is diagnosed with osteoporosis. This application is a continuation of U.S. application Ser. No. 15/801,964 filed Nov. 2, 2017, which is a continuation of U.S. application Ser. No. 15/334,030 filed Oct. 25, 2016 that granted as U.S. Pat. No. 9,808,464 on Nov. 7, 2017, which is a division of U.S. application Ser. No. 13/816,312 filed Feb. 11, 2013 that granted as U.S. Pat. No. 9,511,071 on Dec. 6, 2016, which is the National Stage Application of International Application No. PCT/US2011/048252 filed Aug. 18, 2011, which claims priority to U.S. Provisional Application No. 61/374,667 filed Aug. 18, 2010 and U.S. Provisional Application No. 61/479,910 filed Apr. 28, 2011. The entirety of each of these applications is hereby incorporated by reference for all purposes.The Sequence Listing associated with this application is provided in text format in lieu of a paper copy, and is hereby incorporated by reference into the specification. The ...

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Номер записи: 84
21-05-2015 дата публикации

PARP INHIBITOR COMPOUNDS, COMPOSITIONS AND METHODS OF USE

Номер: US20150141429A1
Автор: Delahanty Greg, Wei Ling, XU Weizheng, Zhang Jie
Принадлежит: Eisai Inc.

The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects. 149-. (canceled)51. The method of claim 50 , wherein the compound is a pharmaceutically acceptable salt claim 50 , ester claim 50 , solvate or hydrate of compound 37.52. The method of claim 51 , wherein the pharmaceutically acceptable salt is the salt of an organic acid.54. The method of claim 50 , further comprising administering a chemotherapeutic agent selected from the group consisting of temozolomide claim 50 , adriamycin claim 50 , camptothecin claim 50 , carboplatin claim 50 , cisplatin claim 50 , daunorubicin claim 50 , docetaxel claim 50 , doxorubicin claim 50 , interferon-alpha claim 50 , interferon-beta claim 50 , interferon-gamma claim 50 , interleukin 2 claim 50 , irinotecan claim 50 , paclitaxel claim 50 , topotecan claim 50 , a taxoid claim 50 , dactinomycin claim 50 , danorubicin claim 50 , 4′-deoxydoxorubicin claim 50 , bleomycin claim 50 , pilcamycin claim 50 , mitomycin claim 50 , neomycin claim 50 , gentamycin claim 50 , etoposide claim 50 , 4-OH cyclophosphamide claim 50 , a platinum coordination complex claim 50 , and mixtures thereof.55. The method of claim 54 , wherein said chemotherapeutic agent is temozolomide claim 54 , or a salt ...

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Номер записи: 85
07-08-2014 дата публикации

ORALLY DISINTEGRATING TABLET COMPOSITIONS OF LAMOTRIGINE

Номер: US20140220144A1
Автор: GOSSELIN Michael, LAI Jin-Wang, Venkatesh Gopi M., Vyas Nehal H.
Принадлежит: Aptalis Pharmatech, Inc.

The compositions of the present invention composition comprise a therapeutically effective amount of particles comprising lamotrigine, in combination with granules comprising a disintegrant, and a sugar alcohol and/or a saccharide. These compositions are useful in treating epilepsy and bipolar disorder, particularly for patients with dysphagia, and to improve compliance with bipolar patients. 152.-. (canceled)53. An ODT composition consisting essentially of:a therapeutically effective amount of lamotrigine microcapsules comprising 25 or 200 mg of lamotrigine crystals having an average particle size of about 1-50 μm, coated with a taste-masking layer;a disintegrant; anda sugar alcohol, a saccharide, or both a sugar alcohol and a saccharide;wherein after a single oral administration said ODT composition provides:{'sub': 'max', 'claim-text': [{'sub': '0-24', 'an AUCin the range of 4.87 to 8.17 ng·hr/mL of lamotrigine, or'}, {'sub': max', '0-24, 'both a Cin the range of 0.276 to 0.482 ng/mL of lamotrigine and an AUCin the range of 4.87 to 8.17 ng·hr/mL of lamotrigine,'}, 'if the total amount of lamotrigine in the ODT is 25 mg, or, 'a Cin the range of 0.276 to 0.482 ng/mL of lamotrigine,'}{'sub': 'max', 'claim-text': [{'sub': '0-24', 'an AUCin the range of 36.0 to 63.6 ng·hr/mL of lamotrigine, or'}, {'sub': max', '0-24, 'both a Cin the range of 2.21 to 3.95 ng/mL of lamotrigine and an AUCin the range of 36.0 to 63.6 ng·hr/mL of lamotrigine,'}, 'if the total amount of lamotrigine in the ODT is 200 mg., 'a Cin the range of 2.21 to 3.95 ng/mL of lamotrigine,'}54. The ODT composition of claim 53 , wherein the disintegrant is selected from the group consisting of crospovidone claim 53 , sodium starch glycolate claim 53 , crosslinked sodium carboxymethyl cellulose claim 53 , low substituted hydroxypropyl cellulose claim 53 , and mixtures thereof.55. The ODT composition of claim 53 , wherein the sugar alcohol is selected from the group consisting of arabitol claim 53 , isomalt ...

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Номер записи: 86
26-05-2016 дата публикации

4-OXO-3,4-DIHYDRO-1,2,3-BENZOTRIAZINE MODULATORS OF GPR139

Номер: US20160145218A1
Автор: Hitchcock Stephen, Lam Betty, Monenschein Holger, Reichard Holly
Принадлежит:

The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: 3. The compound or pharmaceutically acceptable salt according to claim 1 , wherein m is 0.4. The compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris Calkyl.5. The compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris selected from the group consisting of methyl claim 1 , ethyl claim 1 , and isopropyl.6. The compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris methyl.7. The compound or pharmaceutically acceptable salt according to claim 1 , wherein n is 1 and Ris trifluoromethoxy.8. The compound or pharmaceutically acceptable salt according to claim 1 , wherein m is 1.9. The compound or pharmaceutically acceptable salt according to claim 1 , wherein m is 2.10. The compound according to claim 1 , which is selected from the group of compounds consisting of:2-(5-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;N-(1-(4-bromophenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;N-(1-(4-methoxyphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;N-(1-(2,4-dimethylphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;N-(1-(4-ethoxyphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;N-(1-(2,4-dimethoxyphenyl)ethyl)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)acetamide;2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-(trifluoromethyl)phenyl)ethyl)acetamide;2-(6-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;2-(6-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-methoxyphenyl)ethyl)acetamide;2-(8-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-p-tolylethyl)acetamide;2-(8-fluoro-4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-methoxyphenyl)ethyl)acetamide;2-(6-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4H)- ...

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Номер записи: 87
28-05-2015 дата публикации

Pro-drugs of riluzole and their method of use for the treatment of amyotrophic lateral sclerosis

Номер: US20150148329A1
Автор: Allen B. Reitz, Garry Robert Smith
Принадлежит: Fox Chase Chemical Diversity Center Inc

Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.

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Номер записи: 88
28-05-2015 дата публикации

SALTS OF 2-FLUORO-N-METHYL-4-[7-(QUINOLIN-6-YL-METHYL)- IMIDAZO[1,2-B][1,2,4]TRIAZIN-2-YL]BENZAMIDE AND PROCESSES RELATED TO PREPARING THE SAME

Номер: US20150148348A1
Автор: Liu Pingli, Pan Yongchun, QIAO Lei, WENG Lingkai, Zhou Jiacheng
Принадлежит:

The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof. 134-. (canceled)35. A method of inhibiting tumor growth in a patient comprising administering to said patient a therapeutically effective amount of 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1 ,2-b][1 ,2 ,4]triazin-2-yl]benzamide dihydrochloric acid salt , or a hydrate or solvate thereof.36. A method of inhibiting tumor metastasis in a patient comprising administering to said patient a therapeutically effective amount of 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1 ,2-b][1 ,2 ,4]triazin-2-yl]benzamide dihydrochloric acid salt , or a hydrate or solvate thereof.37. A method of treating cancer in a patient , wherein said cancer is associated with dysregulation of the HGF/c-MET signaling pathway , comprising administering to said patient a therapeutically effective amount of 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1 ,2-b][1 ,2 ,4]triazin-2-yl]benzamide dihydrochloric acid salt , or a hydrate or solvate thereof.38. (canceled)39. A method of treating a cancer in a patient comprising administering to said patient a therapeutically effective amount of 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1 ,2-b][1 ,2 ,4]triazin-2-yl]benzamide dihydrochloric acid salt , or a hydrate or solvate thereof wherein said cancer is lung cancer , liver cancer , colorectal cancer , gastric cancer , glioblastoma , breast cancer , or cancer of the kidney.4083-. (canceled)84. The method of claim 39 , wherein said cancer is ...

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Номер записи: 89
04-06-2015 дата публикации

Methods For Inhibiting Viruses By Targeting Cathepsin-L Cleavage Sites In The Viruses' Glycoproteins

Номер: US20150150878A1
Автор: Elshabrawy Hatem A., PRABHAKAR Bellur S.
Принадлежит:

The disclosure provides methods and compositions useful for inhibiting virus requiring membrane fusion for viral entry, specifically for inhibiting severe acute respiratory syndrome coronavirus (SARS-CoV), Ebola virus (EBOV), Hendra (HeV) and Nipah (NIV) viruses by targeting Cathepsin-L (CatL) cleavages sites in the viruses' glycoproteins. 2. A method of claim 1 , wherein each Ris hydrogen.3. A method of or claim 1 , wherein Ris C-Calkyl or —C-Calkyl-R claim 1 , wherein Ris —OR claim 1 , —SR claim 1 , or —NRR.43. A method of any one of - claims 1 , wherein Ris C-Calkyl or —C-Calkyl-R claims 1 , wherein Ris —OR claims 1 , —SR claims 1 , or —NRR.54. A method of any one of - claims 1 , wherein Rand Rare independently selected from ethyl claims 1 , i-propyl claims 1 , and t-butyl.65. A method of any one of - claims 1 , wherein Ris —CN.76. A method of any one of - claims 1 , wherein Ris —C(O)C-Calkyl claims 1 , —C(O)C-Chaloalkyl claims 1 , —C(O)C-Calkoxy claims 1 , or —C(O)C-Chaloalkoxy.8. A method of claim 7 , wherein Ris —C(O)CH.9. A method according to claim 1 , wherein the compound is:methyl 2-(N-(4,6-bis(isopropylamino)-1,3,5-triazin-2-yl)cyanamido)acetate; ormethyl 2-(N-(4-(tert-butylamino)-6-(ethylamino)-1,3,5-triazin-2-yl)cyanamido)acetate.109. The method according to any one of - wherein the virus is selected from the group consisting of: severe acute respiratory syndrome coronavirus claims 1 , Ebola virus claims 1 , Hendra virus claims 1 , and Nipah Virus.12. A method of claim 11 , wherein each Ris hydrogen.13. A method of or claim 11 , wherein m is integer 2.1413. A method of any one of - claims 11 , wherein n is an integer 1.1514. A method according to any one of - claims 11 , wherein each Rand each Rare independently halogen claims 11 , —CN claims 11 , or C-Chaloalkyl.16. A method according to claim 15 , wherein each Ris independently halogen claim 15 , and each Ris C-Chaloalkyl.17. A method according to claim 15 , wherein each Ris independently halogen ...

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Номер записи: 90
04-06-2015 дата публикации

Monocyclic Heteroaryl Cycloalkyldiamine Derivatives

Номер: US20150152087A1
Автор: SMITH Alexander Baxter, Thomas Gebhard, Van Elis Maurice
Принадлежит:

The present invention relates to monocyclic heteroaryl cycloalkyldiamine derivatives of formula (I), to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them. 2. A compound of or a pharmaceutically acceptable salt thereof claim 1 , whereinX1 is N;Y1 is NH, Y2 is N and Y3 is CH; orY1 is CH, Y2 is N and Y3 is NH;{'sub': '1-4', 'R1 is H, Calkyl, CN, or Hal; and'}{'sub': '1-4', 'R2 is H, Calkyl or Hal.'}3. A compound of or a pharmaceutically acceptable salt thereof claim 1 , whereinX1 is N;Y1 is NH; Y2 and Y3 are CH;{'sub': '1-4', 'R1 is H, Calkyl, CN, or Hal; and'}{'sub': '1-4', 'R2 is H, Calkyl or Hal.'}5. A compound in accordance to or a pharmaceutically acceptable salt thereof claim 4 , whereinX1 is CH;{'sub': '1-4', 'R1 is H, Calkyl, CN, or Hal; and'}{'sub': '1-4', 'R2 is H, Calkyl or Hal.'}6. A compound in accordance to or a pharmaceutically acceptable salt thereof claim 4 , whereinX1 is CH;R1 is H or methyl; andR2 is H or fluoro.7. A compound of or a pharmaceutically acceptable salt thereof claim 4 , whereinX1 is N;{'sub': '1-4', 'R1 is H, Calkyl, CN, or Hal; and'}{'sub': '1-4', 'R2 is H, Calkyl or Hal.'}8. A compound of or a pharmaceutically acceptable salt thereof claim 4 , whereinX1 is N;R1 is H or methyl; andR2 is H or fluoro.9. A compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein X1 is N claim 4 , and wherein R1 and R2 are both hydrogen.11. A compound of or a pharmaceutically acceptable salt thereof claim 10 , whereinR is methyl;R1 is H or methyl; andR2 is H, methyl or fluoro.13. A compound of or a pharmaceutically acceptable salt thereof claim 12 , whereinR1 is H or methyl; andR2 is H, methyl or fluoro.14. A compound of or a pharmaceutically acceptable salt thereof claim 12 , whereinR1 is H or methyl; and R2 is H.15. A compound in accordance to or a pharmaceutically acceptable salt thereof claim 1 , wherein said compound is selected from:3-((1R,2S)-2-Amino-cyclohexylamino ...

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Номер записи: 91
02-06-2016 дата публикации

ORAL PARTICULATE ANTITUMOR PREPARATION

Номер: US20160151295A1
Автор: Ogata Tetsuo, Ohnishi Yoshito
Принадлежит: TAIHO PHARMACEUTICAL CO., LTD.

An oral particulate antitumor preparation, which allows safe intake of antitumor agents, handling of which could be in many cases dangerous due to their high. pharmacological activity, and has a stability equivalent to that of capsules or tablets, is provided. An oral particulate antitumor preparation, in which a particulate composition containing an antitumor agent is coated with a saccharide other than a cellulose derivative. 1. An oral particulate antitumor preparation , comprising a particulate composition containing an antitumor agent comprising (a) tegafur , (b) gimeracil , and (c) oteracil potassium , wherein the particulate composition is coated with a saccharide other than a cellulose derivative or mannitol.2. The oral particulate antitumor preparation according to claim 1 , wherein the saccharide is a monosaccharide or an oligosaccharide.3. The oral particulate antitumor preparation according to claim 1 , wherein the saccharide is a sugar alcohol or a disaccharide.4. The oral particulate antitumor preparation according to claim 1 , wherein the saccharide is sucrose.5. The oral particulate antitumor preparation according to claim 1 , having a dosage form of a granular preparation.6. The oral particulate antitumor preparation according to claim 1 , wherein the antitumor agent is an orally administrable form.7. Toe oral particulate antitumor preparation according to claim 1 , comprising (a) tegafur claim 1 , (b) gimeracil and (c) oteracil potassium at a molar ratio of 1:0.4:1.8. The oral particulate antitumor preparation according to claim 1 , comprising 0.5% to 15% by mass of tegafur in the particulate preparation coated with a coating film.9. The oral particulate antitumor preparation according to claim 1 , comprising 5% to 10% by mass of tegafur in the particulate preparation coated with a coating film. The present application is continuation of U.S. Ser. No. 12/810,40, filed Jun. 25, 2010, which is a National Stage (371) of PCT/JP08/03991, filed Dec. 26, ...

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Номер записи: 92
02-06-2016 дата публикации

METHOD FOR PREDICTING A TREATMENT RESPONSE TO A CRHR1 ANTAGONIST AND/OR A V1B ANTAGONIST IN A PATIENT WITH DEPRESSIVE AND/OR ANXIETY SYMPTOMS

Номер: US20160153043A1
Автор: Holsboer Florian, Müller-Myhsok Bertram
Принадлежит: MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DER WISSENSCHAFTEN E.V.

The present invention relates to a method for predicting a treatment response to a corticotropin releasing hormone receptor type 1 (CRHR1) antagonist and/or a vasopressin receptor 1B (V) antagonist in a patient with depressive and/or anxiety symptoms. The present invention furthermore relates to a Vreceptor antagonist and/or CRHR1 antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a patient. Also, kits, diagnostic compositions, devices and microarrays allowing the determination of the presence or absence of at least one polymorphic variant in the AVPR1B gene in combination with the presence or absence of at least one polymorphic variant in the patient's genome excluding the AVPR1B gene in the nucleic acid sample are described. 2. The method according to claim 1 , wherein the polymorphic variant in the AVPR1B gene and/or in the patient's genome excluding the AVPR1B gene is a single nucleotide polymorphism (SNP).3. The method according to claim 2 , wherein a polymorphic variant in the AVPR1B gene is SNP rs28373064 which is represented by a single polymorphic change at position 27 of SEQ ID NO: 1 claim 2 , wherein in one or two alleles of the wild-type nucleotide A is replaced by indicator nucleotide G.4. The method according to claim 1 , wherein the at least one polymorphic variant in the patient's genome excluding the AVPR1B gene is selected from the group of biomarkers comprising:SNP rs9880583 which is represented by a single polymorphic change at position 27 of SEQ ID NO: 2, wherein in one or two alleles the wild-type nucleotide C is replaced by indicator nucleotide G,SNP rs13099050 which is represented by a single polymorphic change at position 27 of SEQ ID NO: 3, wherein in one or two alleles the wild-type nucleotide A is replaced by indicator nucleotide C,SNP rs7441352 which is represented by a single polymorphic change at position 27 of SEQ ID NO: 4, wherein in one or two alleles the wild-type nucleotide A is replaced by ...

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Номер записи: 93
01-06-2017 дата публикации

NOVEL THERAPEUTIC USES OF BENZYLIDENEGUANIDINE DERIVATIVES FOR THE TREATMENT OF PROTEOPATHIES

Номер: US20170151196A1
Автор: GUEDAT Philippe
Принадлежит:

The present invention relates to novel uses of a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, in treating a disorder associated with the PPP1R15A pathway and associated with protein misfolding stress and in particular with accumulation of misfolded proteins selected in the group of tauopathies, synucleinopathies, polyglutamine and polyalanine diseases, leukodystrophies, cystic fibrosis, multiple sclerosis, lysosomal storage disorders, amyloidosis diseases, inflammation, metabolic disorders, cardio-vascular disorders, osteoporosis, nervous system trauma, ischemia. 3. The method according to wherein Ris Cl claim 1 , Br claim 1 , Me claim 1 , or F claim 1 , more preferably claim 1 , Cl.4. The method according to wherein Ris H.5. The method according to wherein Y is CR.6. The method according to wherein Rand Rare both H.7. The method according to wherein Ris H and Ris C(O)R claim 1 , with Rbeing Me or OMe.10. The method according to wherein the compound is compound 1 or a pharmaceutically acceptable salt thereof.11. The method according to wherein the disorder is multiple sclerosis.12. The method according to wherein the disorder is a leukodystrophy claim 1 , preferably Pelizaeus-Merzbacher disease.13. The method according to wherein the disorder is CMT-1A.15. The association according to wherein Ris Cl claim 14 , Br claim 14 , Me claim 14 , or F.16. The association according to wherein Ris H.17. The association according to wherein Y is CR.18. The association according to wherein Rand Rare both H.19. The association according to Ris H and Ris C(O)R claim 14 , with Rbeing Me or OMe. The present invention relates to compounds that have potential therapeutic applications in treating disorders associated with protein misfolding stress and in particular with an accumulation of misfolded proteins. In particular, the invention provides compounds that are capable of exhibiting a protective effect against cytotoxic endoplasmic ...

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Номер записи: 94
08-06-2017 дата публикации

NOVEL PYRIDAZONES AND TRIAZINONES FOR TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION

Номер: US20170157133A1
Автор: Liang Chungen, PAN SONG, Wang Jianping, Yang Song
Принадлежит: Hoffmann-La Roche Inc.

The invention provides novel compounds having the general formula: 2. A compound of formula (I) according to claim 1 , wherein{'sup': '1', 'Ris phenyl; or phenyl substituted once or twice by methyl, fluoro, chloro, bromo, trifluoromethyl or cyano;'}{'sup': '2', 'Ris methyl;'}{'sup': 3', '4', '5, 'Ris phenyl; or phenyl substituted once or twice by methyl, fluoro, chloro, trifluoromethyl, cyano, methoxy, trifluoromethoxy, methoxycarbonyl or —C(O)—NRR, wherein'}{'sup': 4', '5, 'one of Rand Ris hydrogen, methyl or isopropyl, and the other one is isopropyl, pantanyl or cyclohexyl;'}{'sub': '2', 'claim-text': 'or pharmaceutically acceptable salts thereof.', 'a is single bond when X is CHor NH;'}3. A compound of formula (I) according to any one of to claim 1 , wherein Ris phenyl substituted once or twice by halogen or trifluoromethyl.4. A compound of formula (I) according to any one of to claim 1 , wherein Ris phenyl substituted once or twice by fluoro claim 1 , chloro or trifluoromethyl.5. A compound of formula (I) according to any one of to claim 1 , wherein Ris phenyl claim 1 , or phenyl substituted once or twice by halogen or trifluoromethyl.6. A compound of formula (I) according to any one of to claim 1 , wherein Ris phenyl claim 1 , or phenyl substituted once or twice by fluoro claim 1 , chloro or trifluoromethyl.7. A compound of formula (I) according to any one of to claim 1 , wherein X is CH.8. A compound according to or claim 1 , wherein{'sup': '1', 'Ris phenyl substituted once or twice by halogen or trifluoromethyl;'}{'sup': '2', 'sub': '1-6', 'Ris Calkyl;'}{'sup': '3', 'Ris phenyl, or phenyl substituted once or twice by halogen or trifluoromethyl;'}{'sub': '2', 'a is single bond when X is CH;'}or pharmaceutically acceptable salts thereof.9. A compound according to any one of claim 1 , or claim 1 , wherein{'sup': '1', 'Ris phenyl substituted once or twice by fluoro, chloro or trifluoromethyl;'}{'sup': '2', 'Ris methyl;'}{'sup': '3', 'Ris phenyl, or phenyl ...

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Номер записи: 95
28-08-2014 дата публикации

COMPOSITIONS AND METHODS FOR PROPHYLAXIS AND THERAPY FOR MENIERES DISEASE

Номер: US20140243342A1
Автор: Zhang Lixin
Принадлежит:

Provided are articles of manufacture, compositions and methods for prophylaxis and/or therapy for disorders involving dizziness and/or vertigo. The articles of manufacture and compositions contain lamotrigine and/or bupropion and pharmaceutically acceptable salts thereof. The compositions include pharmaceutical compositions which are intended to alleviate dizziness and/or vertigo. In certain aspects the disclosure includes articles of manufacture and kits which include printed material which provides an indication that the articles or compositions are intended to be used for prophylaxis and/or therapy of Meniere's disease or a symptom thereof. 1. An article of manufacture comprising packaging material , lamotrigine and bupropion or pharmaceutically acceptable salts thereof , provided in separate or in a single pharmaceutical formulation and contained in the packaging material , wherein the packaging material comprises printed material indicating that the lamotrigine and bupropion or pharmaceutically acceptable salts thereof is for treating Meniere's Disease and/or one or more symptoms of Meniere's Disease.2. The article of manufacture of claim 1 , wherein the lamotrigine and bupropion or pharmaceutically acceptable salts thereof are present in distinct pharmaceutical formulations.3. The article of manufacture of claim 1 , wherein the lamotrigine and bupropion or pharmaceutically acceptable salts thereof are present in the same pharmaceutical formulation.4. A method for prophylaxis and/or therapy of Meniere's Disease in an individual comprising administering to the individual lamotrigine or a pharmaceutically acceptable salt thereof and bupropion or a pharmaceutically acceptable salt thereof claim 1 , such that at least one symptom of Meniere's Disease in the individual is lessened subsequent to the administration.5. The method of claim 4 , wherein the lamotrigine and the bupropion or the pharmaceutically acceptable salts thereof are administered to the individual as ...

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Номер записи: 96
16-06-2016 дата публикации

METHOD FOR TREATING TYPE I AND TYPE II DIABETES

Номер: US20160166578A1
Автор: Kouji Hiroyuki, Odagami Takenao
Принадлежит: PRISM PHARMA CO., LTD.

The present disclosure relates generally to alpha-helix mimetic structures and specifically to alpha-helix mimetic structures that are inhibitors of β-catenin. The disclosure also relates to applications in the treatment of diabetes and diabetic conditions such as diabetic neuropathy, and pharmaceutical compositions comprising such alpha helix mimetic β-catenin inhibitors. 2. The compound of claim 1 , selected from:(6S,9S)—N-benzyl-6-(4-hydroxybenzyl)-2,9-dimethyl-8-(naphthalen-1-ylmethyl)-4,7-dioxooctahydro-1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide,(6S,9S)-2-allyl-N-benzyl-6-(4-hydroxybenzyl)-9-methyl-8-(naphthalen-1-ylmethyl)-4,7-dioxooctahydro-1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide,(6S,9S)—N-benzyl-6-(4-hydroxybenzyl)-9-methyl-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydropyrazino[2,1-c][1,2,4]oxadiazine-1(6H)-carboxamide,(6S,9S)-8-((2-aminobenzo[d]thiazol-4-yl)methyl)-N-benzyl-6-(4-hydroxybenzyl)-2,9-dimethyl-4,7-dioxooctahydro-1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide,(6S,9S)—N-benzyl-6-(4-hydroxybenzyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)octahydro-1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide,(6S,9S)-2-allyl-N-benzyl-6-(4-hydroxybenzyl)-9-methyl-4,7-dioxo-8-(quinolin-8-ylmethyl)octahydro-1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide,4-(((6S,9S)-1-(benzylcarbamoyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)octahydro-1H-pyrazino[2,1-c][1,2,4]triazin-6-yl)methyl)phenyl dihydrogen phosphate,4-(((6S,9S)-1-(benzylcarbamoyl)-2,9-dimethyl-8-(naphthalen-1-ylmethyl)-4,7-dioxooctahydro-1H-pyrazino[2,1-c][1,2,4]triazin-6-yl)methyl)phenyl dihydrogen phosphate,sodium 4-(((6S,9S)-1-(benzylcarbamoyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)octahydro-1H-pyrazino[2,1-c][1,2,4]triazin-6-yl)methyl)phenyl phosphate,sodium 4-(((6S,9S)-1-(benzylcarbamoyl)-2,9-dimethyl-4,7-dioxo-8-(naphthalen-8-ylmethyl)octahydro-1H-pyrazino[2,1-c][1,2,4]triazin-6-yl)methyl)phenyl phosphate,(6S,9S)-2-allyl-6-(4-hydroxybenzyl)-9-methyl-4,7-dioxo-N—((R)-1- ...

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Номер записи: 97
15-06-2017 дата публикации

Heteroaromatic Compounds and their Use as Dopamine D1 Ligands

Номер: US20170165270A1
Автор: "ONEIL STEVEN VICTOR", ALLEN JOHN ARTHUR, COE JOTHAM WADSWORTH, DAVOREN JENNIFER ELIZABETH, DOUNAY AMY BETH, Efremov Ivan Viktorovich, GRAY DAVID LAWRENCE FIRMAN, GUILMETTE EDWARD RAYMOND, HARRIS ANTHONY RICHARD, HELAL CHRIS JOHN, HENDERSON JACLYN LOUISE, MENTE SCOT RICHARD, NASON DEANE MILFORD, Subramanyam Chakrapani, XU WENJIAN
Принадлежит: PFIZER INC.

The present invention provides, in part, compounds of Formula I: 1. A method for treating Parkinson's disease in a human , which method comprises administering to said human a therapeutically effective amount of a D1 agonist with reduced D1R desensitization , wherein:{'sub': '50', 'the D1 agonist has an ECvalue of less than about 2 μM with respect to human D1 receptor;'}the D1 agonist desensitizes rat D1R cAMP signaling less than about 25% relative to Control, wherein Control is 0.1% DMSO in serum free neurobasal media; the percentage reduced D1R desensitization is measured by an assay using rat primary striatal neurons endogenously expressing rat D1Rs; and the assay comprises: a) pretreating rat D1Rs expressed in rat primary striatal neurons with Control for 30 minutes and then measuring the pretreated rat D1Rs′ ability in cAMP accumulation in the presence of SKF-81297 (1 μM) for 30 minutes, (b) pretreating rat D1Rs expressed in rat primary striatal neurons with 10 μM of the D1 agonist in serum free neurobasal media then measuring the pretreated rat D1Rs' ability in cAMP accumulation in the presence of SKF-81297 (1 μM) for 30 minutes, and (c) calculating percentage reduced desensitization by calculating percentage decrease in cAMP accumulation by the D1 agonist as measured in (b) relative to Control as measured in (a);the D1 agonist with reduced D1R desensitization is not a catechol derivative; andthe D1 agonist interacts significantly with the Ser188 but not significantly with the Ser202 residue of a human D1R when binding to the human D1R, wherein the interactions are measured by an assay substantially the same as the one in Example CC.2. The method of wherein the D1 agonist desensitizes rat D1R cAMP signaling less than about 20% relative to Control according to the assay as in .3. The method of wherein the D1 agonist interacts less strongly with the Asp103 residue or the Ser198 residue of the human D1R when binding to the human D1R wherein the interactions are ...

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Номер записи: 98
23-06-2016 дата публикации

1,2,4-TRIAZINE-4-AMINE DERIVATIVES

Номер: US20160175314A1
Автор: Andrews Stephen Philippe, Brown Giles Albert, Congreve Miles Stuart, Mason Jonathan Stephen, Richardson Christine Mary
Принадлежит:

According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A-Aor, particularly, the Areceptor wherein the compound of formula A1 has the structure, wherein, A represents Cyor Het; Cyrepresents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cygroup is optionally substituted by one or more Rsubstituents; Hetrepresents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cyor Het; Cyrepresents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cygroup is optionally substituted by one or more Rsubstituents; Hetrepresents a 3- to 10-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one or two rings and which Hetgroup is optionally substituted by one or more Rsubstituents 117-. (canceled)1932-. (canceled)33. The method as claimed in claim 18 , wherein A represents Cy claim 18 , Het claim 18 , Het or Het claim 18 , and Cy represents a 6-membered aromatic claim 18 , fully saturated or partially unsaturated carbocyclic ring system claim 18 , which Cy group is substituted claim 18 , in the 3-position relative to the point of attachment to the triazine ring claim 18 , with a Rsubstituent and is substituted in the 4-position relative to the point of attachment to the triazine ring claim 18 , with a ORsubstituent and is optionally further substituted by one or more additional ...

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Номер записи: 99
23-06-2016 дата публикации

Benzoguanamine compound having aminomethyl group, or salt thereof, and method for manufacturing the same

Номер: US20160176827A1
Автор: Tomoo Tsujimoto, Yutaka Kanbara
Принадлежит: Mitsubishi Gas Chemical Co Inc

A benzoguanamine compound having an amino methyl group is represented by the following Formula (1), or a salt thereof: wherein R represents a substituent selected from the group consisting of hydrogen, an alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an aryloxy group having 6 to 10 carbon atoms, a hydroxyl group, an amide group, and a halogen atom, and n is an integer of 1 to 2.

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Номер записи: 100