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Небесная энциклопедия

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

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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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 6600. Отображено 100.
05-01-2012 дата публикации

Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme

Номер: US20120004206A1
Автор: Bryan K. Sorensen, Dariusz Wodka, James T. Link, Marina A. Pliushchev
Принадлежит: Dariusz Wodka, Link James T, Pliushchev Marina A, Sorensen Bryan K

The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.

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Номер записи: 1
23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Автор: Hiroki Fukudome, Hiroshi Moritani, Takahiro Nigawara, Takeshi Hanazawa, Tomoaki Kawano, Yasuhiro Yonetoku
Принадлежит: Astellas Pharma Inc

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

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Номер записи: 2
22-03-2012 дата публикации

Metallo-beta-lactamase inhibitors

Номер: US20120071457A1
Автор: Akihiro Morinaka, Ken Chikauchi, Mizuyo Ida, Takao Abe, Toshiaki Kudo, Yukiko Hiraiwa
Принадлежит: Individual

A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.

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Номер записи: 3
29-03-2012 дата публикации

Methods for Identifying Autophagy Inducing Compounds

Номер: US20120077705A1
Автор: Junying Yuan
Принадлежит: Harvard College

This invention pertains to screening methods for identifying autophagy inducing compounds.

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Номер записи: 4
10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Автор: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
Принадлежит: Kyowa Hakko Kirin Co Ltd

An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R 5 represents optionally substituted aryl or the like, Z represents —N═CHR 6 R 7 or the like, R 6 and R 7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R 101 and R 102 together form ═O, and R 103 and R 104 represent H, or R 101 and R 104 together from a bond, and R 102 and R 103 together form a bond.

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Номер записи: 5
05-07-2012 дата публикации

Zinc cluster

Номер: US20120172601A1
Автор: Hideki Nara, Takahiro Fujiwara, Yoshimasa Matsushima
Принадлежит: Takasago International Corp

Disclosed is a novel zinc cluster compound represented by general formula (1): Zn 4 O (OCOR) 6 (RCOOH) n , wherein R represents an alkyl group which has 1 to 4 carbon atoms and may be substituted with a halogen atom, and n represents 0.1 to 1, and also disclosed are a method for producing the compound and a reaction using the compound.

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Номер записи: 6
30-08-2012 дата публикации

Selective calcium channel modulators

Номер: US20120220564A1
Автор: Eric Simonson, Hassan Pajouhesh, Michael E. Grimwood, Yongbao Zhu, Yuanxi Zhou
Принадлежит: Zalicus Pharmaceuticals Ltd

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an aπl ring as shown in formula (I).

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Номер записи: 7
06-09-2012 дата публикации

Compositions and methods useful for treating diseases

Номер: US20120225851A1
Автор: Andrew F. Kolodziej, Michael H. Cardone, Xiang Y. Yu
Принадлежит: Eutropics Pharmaceuticals Inc

The present invention relates to a chemotherapeutic cancer treatment in which compounds of Formula Ia′, Ib′, Ic′, or II′ (referred to as a group as BH3Is) are administered to a mammal for the treatment of B-cell Lymphoma or other hematopoietic cancers, including diseases associated with MCL-1. In another aspect, the invention provides a method for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds selected from the group consisting of compounds or Formula Ia, Ib, Ic, or II in combination with other therapies, for example, a class of therapeutics known as 26S proteosome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with pharmaceutical compositions comprising one or more compounds of Formula Ia′, Ib′, Ic′, or II′. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.

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Номер записи: 8
13-09-2012 дата публикации

Methods of treating emesis using growth hormone secretagogues

Номер: US20120232113A1
Автор: William J. Polvino, William R. Mann
Принадлежит: Helsinn Therapeutics Us Inc

The present invention relates to methods of treating or preventing emesis and improving a subject's ASAS score by administering to the subject an effective amount of a growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof.

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Номер записи: 9
08-11-2012 дата публикации

Inhibitors of Atypical Protein Kinase C and Their Use in Treating Hedgehog Pathway-Dependent Cancers

Номер: US20120283194A1
Автор: Anthony Oro, Scott X. Atwood
Принадлежит: Leland Stanford Junior University

Methods and compositions are provided for modulating Hedgehog (Hh) pathway signaling in a cell. Aspects of the methods include methods for inhibiting Hh pathway-promoted cancer proliferation and/or metastasis that is promoted by Hh pathway signaling, methods for treating cancers promoted by Hh pathway signaling, and methods for screening candidate agents for the ability to treat a cancer promoted by Hh pathway signaling. In addition, reagents and kits thereof that find use in practicing the subject methods are provided.

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Номер записи: 10
03-01-2013 дата публикации

Cyclic amine bace-1 inhibitors having a benzamide substituent

Номер: US20130004518A1
Автор: Andrew Stamford, Corey Strickland, Douglas W. Hobbs, Jared N. Cumming, Jeffrey F. Lowrie, Johannes H. Voight, Kurt W. Saionz, Samuel Chackalamannil, Suresh D. Babu, Tao Guo, Thuy X.H. Le, Ulrich Iserloh, Yan Xia, Ying Huang, Yusheng Wu
Принадлежит: Merck Sharp and Dohme LLC

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is R is —C(O)—N(R 27 )(R 28 ) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

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Номер записи: 11
10-01-2013 дата публикации

Substituted phenyl compounds

Номер: US20130012711A1
Автор: Simon Gessler, Theo Wollmann
Принадлежит: SANOFI SA

The present invention relates to novel substituted phenyl compounds of the formula and to a process for making them. The compounds can be used as intermediates for making 6-substituted-1-(2H)-isoquinolinone derivatives.

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Номер записи: 12
14-02-2013 дата публикации

Chemoselective enrichment for compound isolation

Номер: US20130041106A1
Автор: Antoinette Odendaal, Darci Trader, Erin E. Carlson
Принадлежит: Indiana University Research And Technology Corp

Chemoselective isolation of hydroxyl group-containing and carboxyl group-containing compounds is accomplished via formation of polymeric silyl ethers and polymeric siloxyl esters, respectively. Preparation of chemoselective polymeric reagents for capture of hydroxyl group containing compounds and carboxyl group containing compounds is described.

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Номер записи: 13
14-03-2013 дата публикации

N-piperidinyl acetamide derivatives as calcium channel blockers

Номер: US20130065926A1
Автор: Hassan A. Pajouhesh, Jason Tan, Lingyun Zhang, Michael Edward Grimwood, Nagasree Chakka, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Yuanxi Zhou
Принадлежит: Zalicus Pharmaceuticals Ltd

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).

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Номер записи: 14
04-04-2013 дата публикации

HETEROCYCLIC COMPOUND AND H1 RECEPTOR ANTAGONIST

Номер: US20130085127A1
Автор: Aotsuka Tomoji, Hasumi Koichi, Ishitani Kouki, Kanazawa Hashime, Nishimoto Takahiro, Okada Makoto, Yoshida Miwa
Принадлежит: ASKA Pharmaceutical Co., Ltd

A heterocyclic compound useful as an antiallergic agent is provided. 3. A heterocyclic compound or a salt thereof according to claim 1 , whereinthe ring A is a benzene ring or an aromatic 5- or 6-membered heterocyclic ring;the ring B is an aliphatic 4- to 10-membered heterocyclic ring;{'sup': '1', 'sub': '1-4', 'Ris a straight chain or branched chain Calkylene group;'}{'sup': 2a', '2b, 'sub': 1-6', '1-6', '1-6', '1-6, 'Rand Rare the same or different and each are a benzene ring which may have at least one substituent selected from the group consisting of a halogen atom, a Calkyl group, a haloCalkyl group, a Calkoxy group and a haloCalkoxy group;'}{'sub': 1-4', '1-4', '1-4, 'Z is a hydroxyl group; a Calkoxy group; an amino group; or an N-substituted amino group in which the nitrogen atom has at least one substituent selected from the group consisting of a Calkyl group and a Calkyl-carbonyl group; and'}when G is CH, X is an oxygen atom and n is 1; when G is N, n is 0.4. A heterocyclic compound or a salt thereof according to claim 1 , whereinthe ring A is an aromatic heterocyclic ring containing at least one hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom;the ring B is an aliphatic 5- or 6-membered heterocyclic ring;{'sup': '1', 'sub': '1-3', 'Ris a straight chain or branched chain Calkylene group;'}{'sup': 2a', '2b, 'sub': 1-3', '1-3', '1-3', '1-3, 'Rand Rare the same or different and each are a benzene ring which may have at least one substituent selected from the group consisting of a fluorine atom, a chlorine atom, a Calkyl group, a haloCalkyl group, a Calkoxy group and a haloCalkoxy group; and'}{'sub': 1-3', '1-3', '1-3, 'Z is a hydroxyl group; a Calkoxy group; an amino group; or an N-substituted amino group in which the nitrogen atom has at least one substituent selected from the group consisting of a Calkyl group and a Calkyl-carbonyl group.'}5. A heterocyclic compound or a salt thereof according to claim 1 , ...

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Номер записи: 15
06-06-2013 дата публикации

Novel hydroxamates as therapeutic agents

Номер: US20130142758A1
Автор: Chitra Baskaran, Erik J. Verner, James Robinson, Joseph J. Buggy, Martin Sendzik
Принадлежит: Pharmacyclics LLC

The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

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Номер записи: 16
06-06-2013 дата публикации

COMPOUNDS AND THEIR USE AS IKACH BLOCKERS

Номер: US20130143858A1
Автор: Bostrom Jonas, Emtenas Hans, Granberg Kenneth, Llinas Antonio, Mogemark Mickael
Принадлежит: AstraZeneca AB

The invention relates to compounds according to Formula I: 111-. (canceled)1516-. (canceled) The present invention relates to a novel class of compounds which are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current, i.e. IKACh blockers.The invention also relates to processes for preparing such compounds, to pharmaceutical compositions containing them, to the use of such compounds and to methods for their therapeutic use, particularly in the treatment of cardiac arrhythmias.The normal electrophysiologic behaviour of the heart is determined by ordered propagation of excitatory stimuli that result in rapid depolarization of the cardiac cell, followed by a slower repolarization. The sum of these events creates the cardiac action potential in individual myocytes. Cardiac rhythm disturbances can be caused by abnormalities of impulse generation, propagation or the duration and configuration of such individual cardiac action potentials. The action potentials are generated by the integrated activity of specific ion currents through various transmembrane spanning ion channels with specific selectivity for individual ions (e.g. potassium, sodium, calcium, see Grant AO. Circ. Arrhythmia Electrophysiol. 2009; 2:185-194). The majority of these ion channels have been cloned and thus, their molecular components are known. This knowledge has enabled a more effective search for selective ion channel blockers, as specific ion channel targets can be recombinantly over-expressed in mammalian cells and be used for high capacity screening.Electrophysiological studies in the early 1950s showed the importance of the movement of K out of the cell to produce repolarization after the rapid depolarizing spike. Over the last 60 years, the introduction of single channel recording techniques and molecular cloning has resulted in a deeper understanding of cardiac repolarization and of the ...

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Номер записи: 17
27-06-2013 дата публикации

HEXAFLUOROISOPROPYL CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION

Номер: US20130165422A1
Автор: BARTSCH Regine, CHEURET Dorothee, EVEN Luc, Hoornaert Christian, Jeunesse Jean, MARGEUT Frank
Принадлежит: SANOFI

The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): 2. The compound of formula (I) according to claim 1 , wherein:{'sup': '1', 'Rrepresents a phenyl, naphthyl, indanyl, benzoxazole, benzisoxazole, benzimidazole, benzotriazole, oxadiazole, indazole, isoxazole, pyridine, pyrazine, pyrimidine, thienyl, thiazole, benzothiophene, indole, dihydrobenzodioxane, benzothiadiazole, pyrazole, dihydrobenzoxazine or indoline group;'}{'sup': '2', 'sub': 3', '3', '2', '2', '2', '2', '2, 'Rrepresents one or more groups chosen from a halogen atom or a methyl, trifluoromethyl, methoxy, trifluoromethoxy, cyano, oxo, CHNHCO, CHSO, NHCO, NHSOand pyrrolidine-SOgroup;'}{'sup': '3', 'Rrepresents a group chosen from a phenyl and an oxazole; and also the compound 2,2,2-trifluoro-1-(trifluoromethyl)ethyl 4-{[3-(2-methylpyrimidin-4-yl)benzenesulphonylamino]methyl}piperidine-1-carboxylate,'}in the form of the base or of an addition salt with an acid.3. The compound of formula (I) according to claim 1 , wherein:{'sub': 2', '2', '2', '2', '3', '2, 'Z represents a bond or a CH, (CH), CH═CH, C≡C, OCHor OC(CH)group,'}in the form of the base or of an addition salt with an acid.4. The compound of formula (I) according to claim 1 , wherein:{'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '3', '2, 'A represents a bond, an oxygen atom, a sulphur atom, an OCHgroup, an O—(CH)group, an NH, NHCHor NH(CH)group, an SOor CO group, a CONH group, a CONHCHor CONH(CH)group, an SONH group, an SONHCHor SONH(CH)group, an SONHCO, SONHCONH or SONHCONHCHgroup, an OCONH group, an NHCONH group, an NHCONHCHgroup, an N(CH)CONHCH, NHCONH(CH)or N(CH)CONH(CH)group or an SON(CH)CHgroup,'}in the form of the base or of an addition salt with an acid.5. The compound of formula (I) according claim 1 , wherein m and n represent 1 claim 1 , in the form of the base or of an addition salt with an ...

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Номер записи: 18
11-07-2013 дата публикации

CHIRAL AUXILIARIES

Номер: US20130178612A1
Автор: Shimizu Mamoru, Wada Takeshi
Принадлежит: CHIRALGEN, LTD.

Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries. 2. The compound or a salt thereof according to claim 1 , wherein Rand Rare hydrogen atom or an alkyl group claim 1 , Ris phenyl group claim 1 , Rand Rare hydrogen atom or an alkyl group claim 1 , and Y is —C(R)(R)— (Rand Rare independently hydrogen atom or an alkyl group claim 1 , and when Rrepresents an alkyl group claim 1 , Rmay bind with the phenyl group represented by Rto form a ring) claim 1 , o-phenylene group claim 1 , or naphthalene-1 claim 1 ,2-diyl group.8. The method according to claim 7 , wherein 3% dichloroacetic acid (DCA) in dichloromethane is used for the acidic condition in the step (c).9. The method according to claim 7 , wherein claim 7 , as the modification of phosphorus atom claim 7 , a group represented by X (X represents an alkylthio group which may have a substituent claim 7 , an alkenylthio group which may have a substituent claim 7 , an alkynylthio group which may have a substituent claim 7 , an arylthio group which may have a substituent claim 7 , thiol group claim 7 , an alkoxy group which may have a substituent claim 7 , —BH claim 7 , —Se claim 7 , an alkyl group which may have a substituent claim 7 , an alkenyl group which may have a substituent claim 7 , an alkynyl group which may have a substituent claim 7 , an aryl group which may have a substituent claim 7 , an acyl group which may have a substituent claim 7 , or —N(R)(R) (Rand Rindependently represent hydrogen atom claim 7 , an alkyl group which may have a substituent claim 7 , an alkenyl group which may have a substituent claim 7 , an alkynyl group which may have a substituent claim 7 , or an aryl group which may have a substituent) is introduced on the phosphorus atom.11. The compound or a salt thereof according to ...

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Номер записи: 19
25-07-2013 дата публикации

BENZYL SULFONAMIDE DERIVATIVES AS RORC MODULATORS

Номер: US20130190288A1
Автор: FAUBER Benjamin, Rene Olivier
Принадлежит: Genentech, Inc.

Compounds of the formula I: 2. The compound of claim 1 , wherein n is 0 or 1.3. The compound of claim 1 , wherein X claim 1 , X claim 1 , Xand Xare CR.4. The compound of claim 1 , wherein m is from 0 to 2 and each Ris independently: Calkyl; halo; Calkoxy; cyano; halo-Calkyl; or halo-Calkoxy.5. The compound of claim 1 , wherein Ris: Calkyl; Ccycloalkyl; or Ccycloalkyl-Calkyl; each of which may be optionally substituted one or more times with R.6. The compound of claim 1 , wherein Ris Ccycloalkyl.7. The compound of claim 1 , wherein Ris cyclobutyl.8. The compound of claim 1 , wherein Rand Rare hydrogen.9. The compound of claim 1 , wherein Rand Rare hydrogen.11. The compound of claim 1 , wherein Y is N.12. The compound of claim 1 , wherein Z is —CRR—.13. The compound of claim 1 , wherein Y is CH.14. The compound of claim 1 , wherein Z is —NR—.15. The compound of claim 1 , wherein p is 2.16. The compound of claim 1 , wherein q is 2.17. The compound of claim 1 , wherein each Ris indepently: hydrogen; Calkyl; or halo.18. The compound of claim 1 , wherein Rand Rare hydrogen.19. The compound of claim 1 , wherein Ris acetyl.22. The compound of claim 1 , wherein A is: pyrrolidin-1-yl; 4-hydroxy-piperidin-1-yl; 2-methoxy-ethylamino; morpholin-4-yl; 4-methyl-piperazin-1-yl; 2-hydroxy-ethylamino; 3-oxo-piperazin-1-yl; 2-dimethylamino-ethylamino; 4-(dimethylaminocarbonyl)-piperidin-1-yl; 4-methoxymethyl-piperidin-1-yl; 4-hydroxymethyl-piperidin-1-yl; 4-(aminocarbonyl)-piperidin-1-yl; 4-(dimethylamino)-piperidin-1-yl; 4-(cyanomethyl)-piperidin-1-yl; 3-hydroxy-pyrrolidin-1-yl; 4-(methanesulfonyl)-piperazin-1-yl; 4-acetyl-piperazin-1-yl; 4-methoxy-piperidin-1-yl; 3-hydroxy-piperidin-1-yl; 3-(aminocarbonyl)-pyrrolidin-1-yl; 1 claim 1 ,1-Dioxo-thiomorpholin-4-yl; 4-(methoxycarbonyl)-piperazin-1-yl; 4-(methylcarbonylamino)-piperidin-1-yl; 3-methanesulfonyl-pyrrolidin-1-yl; 3-hydroxy-azetidin-1-yl; 4-(ethoxycarbonyl)-piperazin-1-yl; 3-(aminocarbonyl)-azetidin-1-yl; 3-( ...

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Номер записи: 20
01-08-2013 дата публикации

Alkaloid aminoester derivatives and medicinal composition thereof

Номер: US20130196978A1
Автор: Antonio Caligiuri, Gabriele Amari, Mauro Riccaboni
Принадлежит: Chiesi Farmaceutici SpA

Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.

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Номер записи: 21
08-08-2013 дата публикации

Compositions and methods for enhancing immune responses to vaccines

Номер: US20130202630A1
Автор: Alain P. ROLLAND, Joel D. Enas, Jukka Hartikka, Sean M. Sullivan
Принадлежит: Vical Inc

The disclosure provides adjuvants, immunogenic compositions, and methods useful for vaccination and immune response. In particular, the disclosure provides a class of adjuvants comprising cationic lipid:co-lipid mixtures and methods for delivering formulated compositions.

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Номер записи: 22
08-08-2013 дата публикации

NAPHT-2-YLACETIC ACID DERIVATIVES TO TREAT AIDS

Номер: US20130203727A1
Автор: Babaoglu Kerim, Bacon Elizabeth, Bjornson Kyla, Guo Hongyan, Halcomb Randall L., Hrvatin Paul, Link John O., Liu Hongtao, McFadden Ryan, Mitchell Michael L., Roethle Paul, Taylor James, Trenkle James D., Vivian Randall W., Xu Lianhong
Принадлежит: Gilead Sciences, Inc.

The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I). 2. The compound of wherein Ris (C-C)alkyl claim 1 , (C-C)alkenyl or —O(C-C)alkyl wherein any (C-C)alkyl or (C-C)alkenyl of Ris optionally substituted with one or more groups selected from —O(C-C)alkyl claim 1 , halo claim 1 , oxo and —CN; and wherein Ris H.4. The compound of wherein Ris selected from:{'sub': 1', '6', '2', '6', '1', '6', '3', '7', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'a) aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and heteroaryl is optionally substituted with one or more groups each independently selected from halo, (C-C)alkyl, (C-C)alkenyl, (C-C)haloalkyl, (C-C)cycloalkyl, —OH, —O(C-C)alkyl, —SH, —S(C-C)alkyl, —NH, —NH(C-C)alkyl and —N((C-C)alkyl), wherein (C-C)alkyl is optionally substituted with hydroxy, —O(C-C)alkyl, cyano or oxo;'}{'sub': 3', '14', '3', '14', '3', '7, 'sup': 1', '1, 'b) (C-C)carbocycle, wherein (C-C)carbocycle is optionally substituted with one or more Zgroups, wherein two Zgroups together with the atom or atoms to which they are attached optionally form a (C-C)carbocycle or heterocycle; and'}{'sup': 7', '1, 'c) aryl, heteroaryl and fused-heterocycle, wherein any aryl, heteroaryl and fused-heterocycle is substituted with one or more Zgroups and optionally substituted with one or more Zgroups.'}5. The compound of wherein Ris selected from:{'sub': 1', '6', '2', '6', '1', '6', '3', '7', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'a) aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and ...

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Номер записи: 23
08-08-2013 дата публикации

CYTOKINE INHIBITORS

Номер: US20130203815A1
Автор: Bandgar Babasaheb Pandurang, Totre Jalindar Vasant
Принадлежит: Piramal Enterprises Limited

The present invention provides compounds represented by general formula (I): 2. The compound of formula (I) according to claim 1 , wherein{'sub': '1', 'Ris selected from hydrogen or alkyl;'}{'sub': '2', 'Rat each occurrence is independently selected from hydrogen, halogen, hydroxy, alkyl or alkoxy; and'}T is phenyl; which is unsubstituted or substituted by at least one group selected from halogen, hydroxy, alkyl, haloalkyl, alkoxy, carboxy, amino, nitro or cyano;or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof.6. The compound of formula (I) according to claim 1 , wherein{'sub': '1', 'Ris selected from hydrogen or alkyl;'}{'sub': '2', 'Rat each occurrence is independently selected from hydrogen, halogen, hydroxy, alkyl or alkoxy; and'}T is 5 or 6 membered heteroaryl; wherein the heteroaryl is unsubstituted or substituted by at least one group selected from; halogen, hydroxy, alkyl, haloalkyl, alkoxy, carboxy, amino, nitro or cyano;or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof.14. The compound of formula (I) according to claim 1 , wherein the compound is:(+/−)3-(2-Chlorophenyl)-1-(2-hydroxy-3-(2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4,6-dimethoxy-phenyl)prop-2-en-1-one hydrochloride,(−)3-(2-Chlorophenyl)-1-(2-hydroxy-3-(2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4,6-dimethoxy-phenyl)prop-2-en-1-one,(+)3-(2-Chlorophenyl)-1-(2-hydroxy-3-(2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4,6-dimethoxy-phenyl)prop-2-en-1-one,(+/−)3-(3-Bromophenyl)-1-(2-hydroxy-3-(2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4,6-dimethoxy-phenyl)prop-2-en-1-one,(+/−)3-(2,4-Dimethoxy-phenyl)-1-(2-hydroxy-3-(2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4,6-dimethoxy-phenyl)prop-2-en-1-one,(+/−)1-(2-Hydroxy-3-(2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4,6-dimethoxyphenyl)-3-m-tolylprop-2-en-1-one,(+/−)1-(2-Hydroxy-3-(2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4,6-dimethoxy-phenyl)-3-o-tolylprop-2-en-1-one,(+/−)1-(2-Hydroxy-3-(2-(hydroxymethyl ...

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Номер записи: 24
31-10-2013 дата публикации

Psyllid Attractants and Their Uses

Номер: US20130287727A1
Автор: Dimitratos Spiros, Woods Daniel F.
Принадлежит: Inscent, Inc.

The present specification discloses psyllid attractants, compositions comprising such attractants, lures, traps and other devices using such attractants, methods and uses to attract, capture and/or kill psyllids using such attractants, compositions and/or lures, traps and/or other devices, and methods and uses for monitoring a psyllid population using such attractants, compositions and/or lures, traps and/or other devices. 156-. (canceled)62. The compound of claim 57 , wherein the compound has a binding affinity for a psyllid OBP or SAP having an equilibrium dissociation constant of less than 0.500 nM claim 57 , less than 0.450 nM claim 57 , less than 0.400 nM claim 57 , less than 0.350 nM claim 57 , less than 0.300 nM claim 57 , less than 0.250 nM claim 57 , less than 0.200 nM claim 57 , less than 0.150 nM claim 57 , less than 0.100 nM claim 57 , or less than 0.050 nM.63. A composition comprising one or more of the compounds as defined in .64. The composition of claim 57 , wherein the composition is a liquid composition claim 57 , a semi-solid composition claim 57 , or a solid composition.65. A device comprising one or more of the compounds as defined in .66. A method of capturing psyllids claim 57 , the method comprising using one or more of the compounds as defined in to attract the psyllids to a device claim 57 , thereby capturing the psyllids.67. A method of killing psyllids claim 57 , the method comprising using one or more of the compounds as defined in to attract the psyllids to a device claim 57 , thereby killing the psyllids.68. A method of monitoring a psyllid population claim 57 , the method comprising a) using one or more of the compounds as defined in to attract psyllids to a device claim 57 , thereby capturing the psyllids; b) counting the psyllids to determine a number of captured psyllids; and c) performing a statistical analysis on the number of captured psyllids in order to determine the psyllid population claim 57 , thereby monitoring the psyllid ...

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Номер записи: 25
31-10-2013 дата публикации

DIAZENIUMDIOLATE HETEROCYCLIC DERIVATIVES

Номер: US20130289003A1
Автор: Ali Amjad, Baker Robert K., Dellureficio James, Guo Zhiqiang, Henderson Timothy J., Lo Michael Man-Chu, Metzger Edward, Shah Shrenik K., Wang Jun, WHITEHEAD Brent, Yan Lin
Принадлежит:

A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy. 4. A compound of claim 1 , wherein Ris hydrogen claim 1 , —C(O)OH claim 1 , or —C(O)OCH claim 1 , or a pharmaceutically acceptable salt thereof.5. A compound of claim 1 , wherein Ris hydrogen claim 1 , or a pharmaceutically acceptable salt thereof.6. A compound of claim 1 , wherein Ris —CDCalkyl claim 1 , —C(CH) claim 1 , —CHCH claim 1 , or —CH(CH).8. A compound of claim 1 , wherein Ris hydrogen claim 1 , —CH claim 1 , C(O)OCH claim 1 , —C(O)OH claim 1 , phenyl claim 1 , or a pharmaceutically acceptable salt thereof.9. A compound of claim 1 , wherein Ris hydrogen or —CH claim 1 , or a pharmaceutically acceptable salt thereof.10. A compound of claim 1 , wherein Rand Rare attached to the same carbon atom and together form ═O claim 1 , or a pharmaceutically acceptable salt thereof.16. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHor —CH.17. A compound of claim 1 , wherein Rand R claim 1 , together with the N atom to which they are attached claim 1 , form a 5- or 6-membered heterocyclic ring containing 1 N atom claim 1 , which ring is unsubstituted or substituted with —CHOH.18. A compound of claim 1 , wherein Rtogether with R claim 1 , forms ═O.19. A compound of claim 1 , which is{'sup': '2', 'O-[(3R)-1-(tert-butoxycarbonyl)pyrrolidin-3-yl]1-(N-tert-butyl-N-methylamino)diazen-1-ium-1,2-diolate,'}{'sup': '2', 'O-[(3S)-1-(tert-butoxycarbonyl)pyrrolidin-3-yl]1-(N-tert-butyl-N-methylamino)diazen-1-ium-1,2-diolate,'}{'sup': '2', 'O-[(3R)-1-(tert-butoxycarbonyl)pyrrolidin-3-yl]1-(N-tert-butyl-N-ethylamino)diazen-1-ium-1,2-diolate,'}{'sup': '2', 'O-[(3R)-1-(tert-butoxycarbonyl)pyrrolidin-3-yl]1-(N-tert-butyl-N- ...

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Номер записи: 26
31-10-2013 дата публикации

4-(p-QUINONYL)-2-HYDROXYBUTANAMIDE DERIVATIVES FOR TREATMENT OF MITOCHONDRIAL DISEASES

Номер: US20130289034A1
Автор: Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader
Принадлежит: Edison Phamaceuticals Inc

Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

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Номер записи: 27
14-11-2013 дата публикации

Substituted 2-Aminoacetamides and the Use Thereof

Номер: US20130303568A1
Автор: CAI Sui Xiong, LAN Nancy C., Wang Yan
Принадлежит:

The invention is directed to substituted 2-aminoacetamides represented by formula (II): 2. The method according to claim 1 , wherein A1 and A2 are both optionally substituted aryl moieties.3. The method according to claim 1 , wherein{'sub': 1', '2', '2', '1-6', '1-4, 'Aand Aare phenyl moieties, that Ais optionally substituted by one or two substituents independently selected from the group consisting of hydrogen, Calkyl, halogen, hydroxy, Calkoxy or trifluoromethyl;'}{'sub': 1', '2, 'Rand Rare hydrogen;'}{'sub': 3', '4, 'Rand Rare methyl;'}{'sub': 5', '6', '7', '1-6', '3-7, 'R, Rand Rare independently hydrogen, Calkyl, or Ccycloalkyl; and'}{'sub': '2', 'X is O, S, CH, or NH.'}4. The method according to claim 1 , wherein said compound is selected from the group consisting of:2-(4-(2-fluorobenzyloxy)benzylamino)-2-methyl-propanamide;2-(4-(4-fluorophenoxy)benzylamino)-2-methyl-propanamide;2-(4-(3,4-methylenedioxyphenoxy)benzylamino)-2-methyl-propanamide;2-(4-(3,4-methylenedioxybenzyloxy)benzylamino)-2-methyl-propanamide;2-(4-cyclohexyloxybenzylamino)-2-methyl-propanamide;2-(4-(5,6,7,8-tetrahydro-2-naphthoxy)benzylamino)-2-methyl-propanamide;2-(4-(2-adamantanoxy)benzylamino)-2-methyl-propanamide;2-(4-(4-chloro-2-fluorophenoxy)benzylamino)-2-methyl-propanamide;2-(4-(2,4-difluorophenoxy)benzylamino)-2-methyl-propanamide;2-(4-(3,4-difluorophenoxy)benzylamino)-2-methyl-propanamide;2-(4-(6-bromo-4-fluorophenoxy)benzylamino)-2-methyl-propanamide;2-(4-(4-nitrophenoxy)benzylamino)-2-methyl-propanamide;2-(4-(4-tetrahydropyranoxy)benzylamino)-2-methyl-propanamide;2-(4-(3,5-difluorophenoxy)benzylamino)-2-methyl-propanamide,2-(4-(4-chlorophenoxy)benzylamino)-2-methyl-propanamide;2-(4-(4-methylphenoxy)benzylamino)-2-methyl-propanamide;2-(4-(2-chloro-4-fluorophenoxy)benzylamino)-2-methyl-propanamide;2-(4-(5-indanoxy)benzylamino)-2-methyl-propanamide;2-(4-cycloheptoxybenzylamino)-2-methyl-propanamide;2-(4-(1-methyl-4-piperidinoxy)benzylamino)-2-methyl-propanamide;2-(4-(exo-2- ...

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Номер записи: 28
21-11-2013 дата публикации

DITERPENOID DERIVATIVES ENDOWED OF BIOLOGICAL PROPERTIES

Номер: US20130310423A1
Автор: Bianchi Giuseppe, Cerri Alberto, Ferrandi Mara, Ferrari Patrizia, Gobbini Mauro, Torri Marco
Принадлежит: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.

The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients. 2. The compound according to claim 1 , wherein Rrepresents —CH═NOR.3. The compound according to claim 1 , wherein Ris amino-(Ci-C6)alkyl or heterocycloalkyl.4. A medicament comprising an effective amount of the compound according to .5. (canceled)6. A method according to wherein cardiovascular disorder is hypertension.7. The method according to wherein hypertension is caused by the effects of endogenous ouabain.8. A method of treatment of a patient affected by cardiovascular disorder claim 1 , hypertension claim 1 , heart failure claim 1 , cardiac hypertrophy claim 1 , renal failure claim 1 , glomerulosclerosis claim 1 , proteinuria and vascular stenosis after vascular surgery claim 1 , comprising administering to said patient an effective amount of a compound according to .9. A pharmaceutical composition comprising a compound according to together with a pharmaceutically acceptable excipient.11. The medicament according to claim 4 , wherein said effective amount comprises from about 0.1 to about 50% by weight.12. The medicament according to claim 4 , wherein said effective amount comprises from about 1 to about 40% by weight.13. The method according to claim 8 , wherein said effective amount comprises from 0.001 mg/kg to 10 mg/kg.14. The method according to claim 8 , wherein said effective amount comprises from 0.05 mg/kg to 50 mg/kg. The present invention relates to new diterpenoid derivatives, process for their preparation, and to pharmaceutical compositions containing them for the prevention and/or treatment of cardiovascular disorders, obstructive vascular ...

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Номер записи: 29
05-12-2013 дата публикации

Protease Activated Receptor 2 (PAR2) Antagonists

Номер: US20130324556A1
Автор: Boyd Joe William, Higginbottom Michael, MEO Paul, Mountford David Mark, Savory Edward Daniel, Simpson Iain
Принадлежит:

A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof 2. A compound according to wherein Rand Rare independently selected from H claim 1 , Calkyl claim 1 , or cyclopropyl claim 1 , each of which Calkyl claim 1 , or cyclopropyl being optionally substituted with one or more substituents independently selected from fluoro and Calkoxy4. A compound according to wherein the ring comprising Z and Y is optionally substituted with one more substituents independently selected from fluoro claim 1 , C-alkyl claim 1 , C-alkoxy claim 1 , fluoro-C-alkyl and fluoro-C-alkoxy.7. A compound according to any wherein Ris hydrogen.8. A compound according to wherein W is an optionally substituted phenyl ring.9. A compound according to wherein the Rsubstituent is optionally substituted with one or more fluoro substituents10. A compound according to wherein Ris H.11. A compound according to wherein Ris H or methyl.12. A compound according to wherein Ris H or methyl.14. (canceled)15. A compound according to wherein U═O.16. A compound according to wherein X is independently selected from —C(O)— claim 1 , —(CHR)— claim 1 , —N(R)— or claim 1 , in either orientation claim 1 , —(CHCHR)—.17. A compound according to wherein Q is independently selected from —O— claim 1 , —S— claim 1 , —N(R)— claim 1 , —C(O)— claim 1 , C(H)(OH)— claim 1 , —(CHR)— or claim 1 , in either orientation claim 1 , —(CHCHR)—.18. A compound according to wherein X is independently selected from —C(O)— claim 1 , —(CHR)— claim 1 , or —N(R).19. A compound according to wherein Q is independently selected from —O— claim 1 , —N(R)— claim 1 , —C(O)— claim 1 , C(H)OH)— claim 1 , —(CHR)—.20. A compound as claimed in selected from:(4-{[(4-Benzylpiperidin-1-yl)carbonylamino]methyl}phenyl)methanaminium chloride;2,2,2-Trifluoroacetic acid; N-{[4-(aminomethyl)phenyl]methyl}-4-[(4-methoxyphenyl)methyl]piperidine-1-carboxamide:2,2,2-Trifluoroacetic acid; N-{[4-(aminomethyl)phenyl]methyl}-4-[(3- ...

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Номер записи: 30
12-12-2013 дата публикации

NOVEL IMINOSUGARS AND THEIR APPLICATIONS

Номер: US20130331578A1
Автор: Dwek Raymond, Kiappes J. L., Laing Peter, POLLOCK Stephanie, Zitzmann Nicole
Принадлежит:

Iminosugar compounds are described that have inbuilt delivery features by virtue of covalent incorporation of a tocopherol moiety, or alternative moieties that are analogues of tocopherol or select analogues of cholesterol, or its antagonist “Ezitimibe”; and are likely to have broad spectrum antiviral activity. The compounds differ from previous iminosugar compounds, even lipophillic ones, being more hydrophobic and resembling fats and oils in their partition behavior in vivo into lipid phases of lipoproteins, cellular lipid droplet organelles and biological membranes. These features confer a number of unique delivery attributes in vivo, favorable to the therapy of virus infections involving cells of the lymphoid system and the liver, in particular, but these features are also favorable in general for the treatment of virus infections of man and animals. 3. The compound of claim 1 , wherein Ris Calkyl.6. The compound of claim 5 , wherein Xare each methyl and Ris Calkyl.7. The compound of claim 1 , wherein Ware each H.11. The method of claim 9 , wherein Y is O.15. The method of claim 14 , further comprising deprotecting R—Z—Y—R—OPto form R—Z—Y—R—OH claim 14 , wherein Pis an alcohol protecting group.16. The method of claim 15 , further comprising reacting R—Z—OH with PO—R—OPto form R—Z—Y—R—OP claim 15 , wherein Pis an alcohol protecting group.21. The compound of claim 18 , wherein Z is a cholesterol derivative.22. The compound of claim 18 , wherein Z is a diacylglyceryl derivative.26. The compound of claim 23 , wherein Z is a cholesterol derivative.27. The compound of claim 23 , wherein Z is a diacylglyceryl derivative. This application claims priority from U.S. Provisional Application No. 61/656,265, filed Jun. 6, 2012, the contents of which are hereby incorporated by reference in their entirety into the present disclosure.The present application relates to novel iminosugars and their methods of making and use and in particular, to novel deoxynojimimycin based ...

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Номер записи: 31
19-12-2013 дата публикации

METHOD FOR PRODUCING DI(ARYLAMINO)ARYL COMPOUND AND SYNTHETIC INTERMEDIATE THEREFOR

Номер: US20130338358A1
Автор: Akiba Takahiro, Hirasawa Shun, Kobayashi Koji, KONDOH Yutaka, Obitsu Kazuyoshi, Orii Ryoki, Takahama Vuji, Takeguchi Kazuhiro
Принадлежит: Astellas Pharma Inc.

Provided is a method for producing a di(arylamino)aryl compound that has superior inhibitory activity against the kinase activities of EML4-ALK fusion protein and mutant EGFR protein and is useful as an active ingredient in pharmaceutical compositions for cancer treatment. The production method includes no purification step using silica gel column chromatography or no step possibly producing a mutagenic mesylate ester as a by-product, greatly improves overall yield, and is high yield and low cost and suitable for the industrial production of pharmaceutical products. Also provided is a synthetic intermediate that is useful in the production method. 9. The compound according to or a salt thereof claim 8 , wherein Lv is a leaving group selected from the group consisting of halogen claim 8 , sulfonyloxy groups claim 8 , lower alkylsulfanyl and lower alkylsulfonyl.10. The compound according to claim 9 , wherein Lv is halogen.11. The compound according to claim 10 , wherein Lv is Cl and Rand Rare both methyl groups.12. The compound according to or a salt thereof claim 7 , wherein Raand Raare both methyl groups.14. The compound according to claim 13 , wherein Rband Rbare both methyl groups.15. The method according to claim 5 , wherein the compound of Formula (9) is cyanuric chloride.16. The method according to claim 1 , further comprising a purification step including crystallization of the compound of Formula (1). The present invention relates to a method for producing N-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}-N′-[2-(propane-2-sulfonyl)phenyl]-1,3,5-triazine-2,4-diamine (hereinafter, referred to as “compound of Formula (1)” in some cases), and to a synthetic intermediate therefor.We have already reported that the compound of Formula (1) has high inhibitory activity against EML4-ALK fusion protein kinase and mutant EGFR protein kinase and is useful as an active ingredient in pharmaceutical compositions for cancer treatment (Patent Document 1). ...

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Номер записи: 32
02-01-2014 дата публикации

DIMETHYL-BENZOIC ACID COMPOUNDS

Номер: US20140005222A1
Автор: BLANCO-PILLADO Maria-Jesus, Fisher Matthew Joseph, Kuklish Steven Lee, VETMAN Tatiana Natali
Принадлежит:

The present invention provides a compound of the Formula II: 3. A compound or salt according to wherein Ris CH.4. A compound or salt according to wherein X is N.5. A compound or salt according to wherein Ris H and Ris OH.8. Hydrated compound according to .9. The hydrated compound according to characterized by a substantial peak in the X-ray diffraction spectrum claim 8 , at diffraction angle 2-theta claim 8 , of 9.0° claim 8 , in combination with two or more peaks at diffraction angle 2-theta selected from the group consisting of 5.8° claim 8 , 8.5° claim 8 , 9.8° claim 8 , 11.6° claim 8 , 11.8° claim 8 , 17.5° claim 8 , and 24.2°.10. A method of treating osteoarthritis in a patient claim 1 , comprising administering to a patient in need of such treatment an effective amount of a compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to .11. A method of treating rheumatoid arthritis in a patient claim 1 , comprising administering to a patient in need of such treatment an effective amount of a compound or pharmaceutically acceptable salt thereof claim 1 , according to .12. A method of treating pain associated with osteoarthritis or rheumatoid arthritis in a patient claim 1 , comprising administering to a patient in need of such treatment an effective amount of a compound or a pharmaceutically acceptable salt thereof claim 1 , according to .13. A pharmaceutical composition claim 1 , comprising a compound or a pharmaceutically acceptable salt thereof according to in combination with one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , or excipients. The present invention relates to novel dimethyl-benzoic acid compounds, to pharmaceutical compositions comprising the compounds, to methods of using the compounds to treat physiological disorders, and to intermediates and processes useful in the synthesis of the compounds.The present invention is in the field of treatment of inflammatory conditions, such as arthritis, ...

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Номер записи: 33
06-02-2014 дата публикации

MODULATORS OF SEROTONIN RECEPTORS

Номер: US20140038934A1
Автор: Brock Shireman T., Carruthers Nicholas I., Jablonowski Jill A., Tran Vi T.
Принадлежит: Janssen Pharmaceutica NV

Certain biphenyl compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases. 122.-. (canceled)24. A method according to claim 23 , wherein the disease claim 23 , disorder claim 23 , or condition is selected from the group consisting of: sleep disorders claim 23 , depression/anxiety claim 23 , generalized anxiety disorder claim 23 , schizophrenia claim 23 , bipolar disorders claim 23 , cognitive disorders claim 23 , mild cognitive impairment claim 23 , Alzheimer's disease claim 23 , Parkinson's disease claim 23 , psychotic disorders claim 23 , phobic disorders claim 23 , obsessive-compulsive disorder claim 23 , mood disorders claim 23 , post-traumatic stress claim 23 , migraine claim 23 , pain claim 23 , eating disorders claim 23 , obesity claim 23 , sexual dysfunction claim 23 , metabolic disturbances claim 23 , hormonal imbalance claim 23 , hot flushes associated with menopause claim 23 , alcohol abuse claim 23 , drug abuse claim 23 , drug addiction claim 23 , alcohol addiction claim 23 , nausea claim 23 , inflammation claim 23 , centrally mediated hypertension claim 23 , sleep/wake disturbances claim 23 , jetlag claim 23 , and circadian rhythm abnormalities.26. A method according to claim 25 , wherein the disease claim 25 , disorder claim 25 , or condition is selected from the group consisting of: sleep disorders claim 25 , depression/anxiety claim 25 , generalized anxiety disorder claim 25 , schizophrenia claim 25 , bipolar disorders claim 25 , cognitive disorders claim 25 , mild cognitive impairment claim 25 , Alzheimer's disease claim 25 , Parkinson's disease claim 25 , psychotic disorders claim 25 , phobic disorders claim 25 , obsessive-compulsive disorder claim 25 , mood disorders claim 25 , post-traumatic stress disorder claim 25 , pain claim 25 , alcohol abuse claim 25 , drug abuse claim 25 , drug addiction claim 25 , and alcohol addiction.27. A method according to claim 25 , wherein the disease claim 25 , disorder claim 25 , ...

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Номер записи: 34
06-02-2014 дата публикации

Serotonin receptor modulator

Номер: US20140038943A1
Автор: Brock T. Shireman, Chandravadan R. Shah, Devin M. Swanson, Jill A. Jablonowski, Nicholas I. Carruthers, Vi Tran, Victoria Wong, Wenying Chai
Принадлежит: Janssen Pharmaceutica NV

Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.

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Номер записи: 35
06-03-2014 дата публикации

HETEROCYCLIC COMPOUND

Номер: US20140066420A1
Автор: KAKU Tomohiro, KAMAURA Masahiro, KASAI Shizuo
Принадлежит: Takeda Pharmaceutical Company Limited

The present invention relates to 2. The compound according to claim 1 , wherein ring A is benzene optionally further substituted;{'sup': '1', 'sub': '3-6', 'Ris an optionally substituted branched Calkyl group;'}{'sup': '1', 'sub': '2', 'Xis O, S, SO, SOor NH;'}{'sup': '2', 'sub': '1-3', 'Xis a bond or a Calkylene group;'}ring B is piperidine;{'sup': '3', 'Xis CO; and'}{'sup': '2', 'Ris an acyl group or an optionally substituted hydrocarbon group.'}3. The compound according to claim 1 , wherein ring A is benzene optionally further substituted by 1 to 3 substituents selected from the group consisting of (1) a halogen atom claim 1 , (2) an optionally halogenated Calkyl group and (3) an optionally halogenated Calkoxy group.4. The compound according to claim 1 , wherein Ris an isopropyl group or a tert-butyl group.5. The compound according to claim 1 , wherein Xis O.6. The compound according to claim 1 , wherein Xis a bond or methylene.8. The compound according to claim 1 , wherein Xis CO.9. The compound according to claim 1 , wherein Ris an acyl group or an optionally substituted hydrocarbon group.1126-. (canceled)27. {4-[(2-tert-Butyl-4-chlorophenoxy)methyl]piperidin-1-yl}(oxo)acetic acid or a salt thereof.28. [4-(2-tert-butylphenoxy)piperidin-1-yl](oxo)acetic acid or a salt thereof.29. {4-[(2-tert-butylphenoxy)methyl]piperidin-1-yl}(oxo)acetic acid or a salt thereof.30. A pharmaceutical composition comprising the compound according to and a pharmacologically acceptable carrier. The present invention relates to a novel heterocyclic compound, which is useful as an agent for the prophylaxis or treatment of diabetes and the like; and the like.Retinol binding protein 4 (hereinafter sometimes to be abbreviated as “RBP4”) is known to be a sole blood retinol transport protein mainly produced in the liver. In recent years, moreover, RBP4 is suggested to be an insulin resistance-inducing factor from the following literatures and the like.(1) Since RBP4 expression increases in ...

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Номер записи: 36
13-03-2014 дата публикации

AROMATIC AMIDES AS POTENTIATORS OF BIOEFFICACY OF ANTI-INFECTIVE DRUGS

Номер: US20140073595A1
Автор: GUPTA Pankaj, JOHRI Rakesh Kamal, Khan Inshad Ali, KHOSA Anita, KOUL Jawahir Lal, Koul Surrinder, KUMAR Ashwani, MIRZA Zahid Mehmood, PANDITA Monika, Qazi Ghulam Nabi, SHARMA Subhash Chander, TANEJA Subhash Chandra, TIKOO Ashok Kumar, VERMA Vijeshwar
Принадлежит: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH

The present invention relates to an aromatic substituted pentadienoic acid amides and there use in combination of specific amounts of aromatic amides i.e. 4-alkyl-5-(substituted phenyl)-2(E),4(E)-pentadienoic acid amides, its geometrical isomers or their dihydro or tetrahydro derivatives and an anti-infective drug useful in potentiating the bioefficacy of antiinfective drug. The combination of the present invention is useful in the treatment of certain infections and disease at lower concentration of anti-infectives necessary to inhibit the growth of microbial strains and may also find applications in reducing the resistance in microorganisms. 132-. (canceled)37. The method of claim 33 , wherein the potentiating compound is in the form of a pharmaceutically acceptable salt selected from hydrochloride claim 33 , acetate claim 33 , succinate claim 33 , and maleate.38. The method of wherein NRRtogether (R+R) represent an amino acid radical comprising at least one of alaninyl claim 33 , leucinyl claim 33 , phenylalaninyl claim 33 , tyrosinyl claim 33 , glycylglycinyl claim 33 , alanylalaninyl or prolinyl; or a heterocyclic amine radical comprising at least one of piperidinyl claim 33 , pyrrolidinyl claim 33 , morpholinyl claim 33 , piperazinyl claim 33 , N-methylpiperazinyl claim 33 , pyrrolyl claim 33 , imidazolyl claim 33 , or oxazolyl.39. The method of claim 33 , wherein the bacterial cell comprises a gram positive bacterium.40Staphylococcus speciesBacillus. The method of wherein the gram positive bacterium comprises at least one of and species.41. The method as claimed in claim 33 , wherein the bacterial cell comprises a gram negative bacterium.42Pseudomonas species, E. coliSalmonella. The method of wherein the gram negative bacterium comprises at least one of and species.43mycobacterium. The method of claim 33 , wherein the bacterial cell comprises species.44. The method of claim 33 , wherein the composition further comprises an effective amount of an anti- ...

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Номер записи: 37
20-03-2014 дата публикации

Novel Compositions for Preventing and/or Treating Degenerative Disorders of the Central Nervous System

Номер: US20140080871A1
Автор: Boyd Robert, LEE GARY, Rybczynski Philip
Принадлежит: AMICUS THERAPEUTICS, INC.

The present invention provides novel compounds as well as compositions and methods using the same for preventing and/or treating degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Parkinson's disease. 122-. (canceled)301. A pharmaceutical composition comprising the compound of claim and at least one pharmaceutically acceptable carrier.352. A pharmaceutical composition comprising the compound of claim and at least one pharmaceutically acceptable carrier.363. A pharmaceutical composition comprising the compound of claim and at least one pharmaceutically acceptable carrier. The present invention provides novel compounds, known as pharmacological chaperones, as well as compositions and methods using the same for preventing and/or treating degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Parkinson's disease.Many degenerative disorders of the central nervous system are associated with pathologic aggregation of proteins or lipids. For example, synucleinopathies are a group of diseases that arise from disruption of synuclein protein homeostasis. In particular, alpha-synuclein aggregation is associated with pathological conditions characterized by Lewy bodies, such as Parkinson's disease, dementia with Lewy bodies, and multiple system atrophy. Likewise, alpha-synuclein fragment, non-Abeta component, is found in amyloid plaques of Alzheimer's disease. Recently, enhancement of glucocerebrosidase (beta-glucosidase; GCase) activity in the brain has been shown to prevent accumulation of synuclein in the brain (Sean Clark, Ying Sun, You-Hai Xu, Gregory Grabowski, and Brandon Wustman, “A biochemical link between Gaucher and Parkinson's disease and a potential new approach to treating synucleinopathies: a pharmacological chaperone for beta-glucocerebrosidase prevents accumulation of alpha-synuclein in a ...

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Номер записи: 38
27-03-2014 дата публикации

Novel Compositions for Preventing and/or Treating Lysosomal Storage Disorders

Номер: US20140086896A1
Автор: Boyd Robert, LEE GARY, Rybczynski Philip
Принадлежит: AMICUS THERAPEUTICS, INC.

The present invention provides novel compositions as well as methods for preventing and/or treating lysosomal storage disorders. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease. 120-. (canceled)29. The method of claim 21 , further comprising administering an effective amount of at least one other therapeutic agent.30. The method of claim 21 , wherein the lysosomal storage disease is Niemann-Pick disease.31. The method of claim 21 , wherein the lysosomal storage disease is Gaucher's disease.32. The method of claim 23 , further comprising administering an effective amount of at least one other therapeutic agent.33. The method of claim 32 , wherein at least one other therapeutic agent is imiglucerase or 1 claim 32 ,5-(butylimino)-1 claim 32 ,5-dideoxy-D-glucitol.35. The method of claim 34 , further comprising administering an effective amount of at least one other therapeutic agent.36. The method of claim 35 , wherein at least one other therapeutic agent is imiglucerase or 1 claim 35 ,5-(butylimino)-1 claim 35 ,5-dideoxy-D-glucitol.38. The kit of claim 37 , wherein the lysosomal storage disorder is Gaucher's disease. The present invention provides novel compounds, known as pharmacological chaperones, as well as methods using the same for preventing and/or treating lysosomal storage disorders. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease.Lysosomal storage disorders are caused by a defect in lysosomal function that results in accumulation of substances within the lysosome of cells. This defect is usually a consequence of deficiency of a single enzyme required for the metabolism of lipid, glycogen, glycoprotein, or mucopolysaccharide. Gaucher's disease, the most common lysosomal storage disorder, is characterized by accumulation of the glycolipid glucocerebroside (also known as glucosylceramide). Symptoms of Gaucher's disease include enlarged spleen and liver, ...

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Номер записи: 39
10-04-2014 дата публикации

C17-ALKANEDIYL AND ALKENEDIYL DERIVATIVES OF OLEANOLIC ACID AND METHODS OF USE THEREOF

Номер: US20140100227A1
Автор: Anderson Eric, BENDER Christopher F., Jiang Xin, Visnick Melean
Принадлежит: REATA PHARMACEUTICALS, INC.

Disclosed herein are novel C17-alkanediyl and alkenediyl derivatives of oleanolic acid, including those of the formula: 5. The compound of claim 1 , wherein the bond between carbon atoms a and b is a single bond.6. The compound of claim 1 , wherein the bond between carbon atoms a and b is a double bond.7. The compound of claim 1 , wherein Y is a covalent bond.8. The compound of claim 1 , wherein Y is —CH—.9. The compound of claim 1 , wherein Y is —C(O)—.10. The compound of claim 1 , wherein Y is —O—.11. The compound of claim 1 , wherein Ris —H.12. The compound of claim 1 , wherein Ris methyl.13. The compound of claim 1 , wherein Ris —H.14. The compound of claim 1 , wherein Ris —OH.15. The compound of claim 1 , wherein Ris amino.16. The compound of claim 1 , wherein Ris alkyl.17. (canceled)18. The compound of claim 1 , wherein Ris heterocycloalkyl.19. (canceled)20. The compound of claim 1 , wherein Ris substituted heterocycloalkyl.21. (canceled)22. The compound of claim 1 , wherein Ris acyl.23. (canceled)24. The compound of claim 1 , wherein Ris substituted acyl.25. (canceled)26. The compound of claim 1 , wherein Ris alkoxy.27. (canceled)28. The compound of claim 1 , wherein Ris aryloxy.29. (canceled)30. The compound of claim 1 , wherein Ris aralkoxy.31. (canceled)32. The compound of claim 1 , wherein Ris substituted acyloxy.33. The compound of claim 32 , wherein Ris —OC(O)NHCHCH.34. The compound of claim 1 , wherein Ris heterocycloalkoxy.35. (canceled)36. The compound of claim 1 , wherein Ris alkylamino.37. (canceled)38. The compound of claim 1 , wherein Ris substituted alkylamino.39. The compound of claim 38 , wherein Ris 2 claim 38 ,2 claim 38 ,2-trifluoroethylamino claim 38 , —NHCHC(O)OCHor —NHCHC(O)OH.40. The compound of claim 1 , wherein Ris dialkylamino.41. (canceled)42. The compound of claim 1 , wherein Ris alkoxyamino.43. (canceled)44. The compound of claim 1 , wherein Ris arylamino.45. (canceled)46. The compound of claim 1 , wherein Ris aralkylamino.47. ( ...

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Номер записи: 40
04-01-2018 дата публикации

ANTIOXIDANT INFLAMMATION MODULATORS: OLEANOLIC ACID DERIVATIVES WITH AMINO AND OTHER MODIFICATIONS AT C-17

Номер: US20180002277A1
Автор: Anderson Eric, Jiang Xin, Visnick Melean
Принадлежит: REATA PHARMACEUTICALS, INC.

This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: 1257-. (canceled)259264-. (canceled)266. The method of claim 265 , wherein Ris hydrogen.267. The method of claim 265 , wherein Ris alkylor substituted alkyl.268. The method of claim 265 , wherein Ris alkylsulfonyl claim 265 , arylsulfonyl claim 265 , aralkylsulfonyl claim 265 , heteroarylsulfonyl claim 265 , heteroaralkylsulfonyl claim 265 , or a substituted version of any of these groups.269. The method of claim 265 , wherein Ris acylor substituted acyl.270. The method of claim 269 , wherein Ris substituted acyl.272. The method of claim 271 , wherein Ris hydrogen.273. The method of claim 271 , wherein Ris alkylor substituted alkyl.274. The method of claim 271 , wherein Ris alkylsulfonyl claim 271 , arylsulfonyl claim 271 , aralkylsulfonyl claim 271 , heteroarylsulfonyl claim 271 , heteroaralkylsulfonyl claim 271 , or a substituted version of any of these groups.275. The method of claim 271 , wherein Ris acylor substituted acyl.276. The method of claim 271 , wherein Ris substituted acyl.278. The method of claim 277 , wherein the acylation agent is an acyl halide or an anhydride.279. The method of claim 277 , wherein the acylation agent is an acyl halide.280. The method of claim 277 , wherein the acylation agent is an acyl chloride.281. The method of claim 258 , wherein the modification is conducted in a medium comprising a solvent.282. The method of claim 281 , wherein the solvent is benzene or dichloromethane.283. The method of claim 258 , wherein the modification is conducted in the presence of a base.284. The method of claim 283 , wherein the base is NEt. The present application is a continuation of U.S. patent application Ser. No. 14/753,297, filed Jun. 29, 2015, now U.S. Pat. No. 9,670,147, which is a continuation of U.S. patent application Ser. No. 13/861,208, filed Apr. 11, 2013, now U.S. Pat. No. 9,102,681, which is a continuation of U.S. patent application ...

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Номер записи: 41
04-01-2018 дата публикации

STERICALLY HINDERED ALKYL AND OXYALKYL AMINE LIGHT STABILIZERS

Номер: US20180002285A1
Автор: Armstrong Paul B., Hoy Charles J., Hunt William J., Iyer Suresh, Klun Thomas P., Nachtigal Alan K., Petrin Jason T., Pokorny Richard J., Roehrig Mark A., Spagnola Joseph C.
Принадлежит:

Compounds having hindered amine and oxyalkyl amine light stabilizers can mitigate the adverse effects of actinic radiation, such as visible and ultraviolet light, on polymers and copolymers. Polymers and copolymers derived from such compounds. Articles, such as coated articles and molded articles, containing such polymers or compounds. 3. The compound of claim 2 , wherein each G is Cto Calkylene.4. The compound of claim 2 , wherein each G is Cto Calkylene.6. The compound of claim 1 , wherein o is 1-3.7. The compound of claim 1 , wherein each q is hydrocarbon polyradical.8. The compound of claim 1 , wherein q+o+r is from 2 to 5.9. The compound of claim 1 , wherein q+o+r is from 2 to 3.10. The compound of claim 1 , wherein each Eis NH.11. The compound of claim 1 , wherein each Eis O.12. The compound of claim 1 , wherein p is 1-2.13. The compound of claim 1 , wherein r is 1-2.14. The compound of claim 1 , wherein q is 0.15. A polymer or copolymer derived from or blended with a compound of .16. An article comprising a compound of or a polymer of . The present disclosure relates to sterically hindered alkyl amine and sterically hindered oxyalkyl amine compounds.Compounds containing sterically hindered alkyl amines or sterically hindered oxyalkyl amines, and particularly the moietywherein Ris alkyl, Ris alkyl, Ris H or alkyl, Ris H or alkyl, Ris H or alkyl, Ris H or alkyl, Ris alkyl, and Ris alkyl are known in the art. When A is alkyl, such compounds are known as hindered amine light stabilizers, or HALS; when A is oxyalkyl, such compounds are known as NORHALS.The utility of HALS and NORHALS as radical scavengers and polymer stabilizers and is well recognized in the art, and is described in, for example, the Journal of Macromolecular Science Part A, 35:7, 1327-36 (1998) and The Journal of Macromolecular Science Part A, 38:2, 137-58 (2001), as well as in JP 2001270859, U.S. Pat. No. 4,983,737 (Grant), and U.S. Pat. No. 5,442,071 (Grant). Such compounds are known to protect ...

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Номер записи: 42
01-01-2015 дата публикации

Photoresist composition, resist pattern-forming method, acid diffusion control agent, and compound

Номер: US20150004544A1
Автор: Hayato Namai
Принадлежит: JSR Corp

A photoresist composition containing: a polymer including an acid-labile group; a radiation-sensitive acid generator; and an acid diffusion control agent that contains a compound represented by a formula (1). In the formula (1), R 1 , R 2 and R 3 each independently represent a hydrogen atom or a monovalent hydrocarbon group having 1 to 10 carbon atoms. A represents a group having a valency of n that is obtained by combining: a hydrogen atom, a linear hydrocarbon group having 1 to 30 carbon atoms, an alicyclic hydrocarbon group having 3 to 30 carbon atoms or a combination thereof; —O—, —CO—, —COO—, —SO 2 O—, —NRSO 2 —, —NRSO 2 O—, —NRCO— or a combination thereof; and n nitrogen atoms as a binding site to the carbonyl group in the formula (1), in which a sum of atomic masses of the atoms constituting A is no less than 120. n is an integer of 1 to 4.

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Номер записи: 43
27-01-2022 дата публикации

ANALOGS OF PRIDOPIDINE, THEIR PREPARATION AND USE

Номер: US20220023280A1
Автор: Kaljuste Kalle, Laos Marit, Maasalu Ants, Päri Malle, Schmidt Malle
Принадлежит:

This invention provides a composition comprising pridopidine or pharmaceutically acceptable salt thereof and at least one of compounds 1-8: 2. The method of claim 1 , wherein the method comprises treating claim 1 , slowing the progression claim 1 , lessening the decline claim 1 , delaying onset of symptoms or slowing the progression of symptoms of Huntington disease claim 1 , wherein the Huntington disease is an early stage Huntington disease.3. The method of claim 1 , wherein the method comprises treating claim 1 , slowing the progression claim 1 , lessening the decline claim 1 , delaying onset of symptoms or slowing the progression of symptoms of ALS.4. The method of claim 1 , wherein the method comprises treating claim 1 , slowing the progression claim 1 , lessening the decline claim 1 , delaying onset of symptoms or slowing the progression of symptoms of dystonia claim 1 , wherein the dystonia is a severe dystonia.5. The method of claim 1 , wherein the method treating claim 1 , slowing the progression claim 1 , lessening the decline claim 1 , delaying onset of symptoms or slowing the progression of symptoms of Rett Syndrome.6. The method of claim 1 , wherein the method comprises treating claim 1 , slowing the progression claim 1 , lessening the decline claim 1 , delaying onset of symptoms or slowing the progression of symptoms of a mitochondrial disease or dysfunction claim 1 , wherein the mitochondrial disease or dysfunction is Lysosomal Storage Disease (LSD) claim 1 , leukodystrophies or a vanishing white matter (VWM) disease.7. The method of claim 1 , wherein the composition comprises pridopidine or a pharmaceutically acceptable salt thereof and at least one of compound 1 claim 1 , compound 4 claim 1 , pharmaceutically acceptable salt thereof or combination thereof.8. The method of claim 1 , wherein the composition comprises pridopidine or a pharmaceutically acceptable salt thereof and compound 1 or pharmaceutically acceptable salt thereof.9. The method of ...

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Номер записи: 44
14-01-2016 дата публикации

H3 ANTAGONISTS CONTAINING PHENOXYPIPERIDINE CORE STRUCTURE

Номер: US20160009645A1
Автор: BALÁZS Ottília, BARTÁNÉ SZALAI Gizella, KISS Béla, NAGY Noémi, Schmidt Eva, WÁGNER Gábor András
Принадлежит:

The present invention relates to new histamine H(H) receptor subtype selective ligands of the general formula (I) and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and the use of these compounds as medicaments for treatment and/or prevention of conditions which require modulation of Hreceptors. The invention also cover the combinations of a compound of the general formula (I) and an acetylcholinesterase inhibitor. 2. Compounds of the general formula (I) according to wherein Rand Rtogether with the adjacent nitrogen atom form an optionally substituted 5-membered heterocyclic group.3. Compounds of the general formula (I) according to wherein Rand Rtogether with the adjacent nitrogen atom form a 2-methyl-pyrrolidine ring.4. Compounds of the general formula (I) according to wherein Rand Rtogether with the adjacent nitrogen atom form a 2-(R)-methyl-pyrrolidine ring.5. Compounds of the general formula (I) according to wherein the meaning of Ris —C(═O)R claim 1 , wherein the meaning of Ris C-Cstraight or branched alkyl group claim 1 , or C-Ccycloalkyl group optionally substituted with C-Calkyl group.6. A compound of selected from the group consisting of4-{4-[3-(piperidin-1-yl)-propoxy]-phenoxy}-piperidine-1-carboxylic acid tert-butyl ester,1-{3-[4-(piperidin-4-yl-oxy)-phenoxy]-propyl}-piperidine dihydrochloride salt,1-(4-{4-[3-(piperidin-1-yl)-propoxy]-phenoxy}-piperidin-1-yl)-ethanone hydrochloride salt,cyclobutyl-(4-{4-[3-(piperidin-1-yl)-propoxy]-phenoxy}-piperidin-1-yl)-methanone hydrochloride salt,(1-methyl-cyclopropyl)-(4-{4-[3-(piperidin-1-yl)-propoxy]-phenoxy}-piperidin-1-yl)-methanone hydrochloride salt,ethyl-4-{4-[3-(piperidin-1-yl)-propoxy]-phenoxy}-piperidine-1-carboxylate hydrochloride salt,N-ethyl-4-{4-[3-(piperidin-1-yl)-propoxy]-phenoxy}-piperidine-1-carboxamide,N-ethyl-N-methyl-4-{4-[3-(piperidin-1-yl ...

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Номер записи: 45
11-01-2018 дата публикации

THERAPEUTIC COMPOUNDS AND USES THEREOF

Номер: US20180009735A1
Автор: Albrecht Brian K., Audia James Edmund, CÔTÉ Alexandre, Duplessis Martin, Gehling Victor S., Good Andrew Charles, Harmange Jean-Christophe, LEBLANC Yves, Nasveschuk Christopher G., Taylor Alexander M., Vaswani Rishi G.
Принадлежит:

Provided herein are compounds of formula I: 23-. (canceled)4. The compound of claim 1 , wherein X is —CH— claim 1 , —CHCH— or —CHCHCH—.79-. (canceled)11. The compound of claim 1 , wherein X is or —N(R)C(R)—.1214-. (canceled)15. The compound of claim 1 , wherein Ris hydrogen claim 1 , halo claim 1 , heteroaryl claim 1 , —OR claim 1 , CN claim 1 , —C(O)—N(R)or —C(O)—OR claim 1 , wherein any heteroaryl of Ris optionally substituted with one or more Rgroups.1618-. (canceled)2022-. (canceled)2425-. (canceled)27. (canceled)2933-. (canceled)36. (canceled)40. (canceled)42. (canceled)43. A method of treating cancer in an animal comprising administering to the animal in need thereof a compound of formula I or a pharmaceutically acceptable salt thereof as described in .44. A method of treating an LSD1-mediated disorder in an animal comprising administering to the animal in need thereof a compound of formula I or a pharmaceutically acceptable salt thereof as described in .4549-. (canceled)50. A method of increasing efficacy of a cancer treatment comprising a cytotoxic agent in an animal comprising administering to the animal an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof as described in .51. (canceled)52. A method of delaying or preventing development of cancer resistance to a cytotoxic agent in an animal claim 1 , comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof as described in .53. A method of extending the duration of response to a cancer therapy in an animal claim 1 , comprising administering to the animal undergoing the cancer therapy a compound of formula I or a pharmaceutically acceptable salt thereof claim 1 , as described in claim 1 , wherein the duration of response to the cancer therapy when the compound of formula I is administered is extended over the duration of response to the cancer therapy in the absence of the administration of the compound of formula I or ...

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Номер записи: 46
14-01-2021 дата публикации

HISTONE DEACETYLASE INHIBITORS

Номер: US20210009519A1
Автор: Bhagwat Shripad, Bridges Alexander, Luedtke Gregory
Принадлежит:

Provided herein are compounds and methods for inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3). 2. The compound of claim 1 , wherein ring A is a 4-7 membered heterocycloalkyl ring containing one nitrogen ring atom or a 7-9 membered bicyclic heterocycloalkyl ring containing one nitrogen ring atom; Z is O claim 1 , NR claim 1 , S claim 1 , or SO; Ris Calkyl claim 1 , Chydroxyalkyl claim 1 , or Calkylene-Ccycloalkyl; Ris H claim 1 , F claim 1 , Cl claim 1 , or CH; Ris H claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkylene-Ccycloalkyl claim 1 , C(O)Calkyl claim 1 , or C(O)Calkylene-Ccycloalkyl; and Ris H or Calkyl.3. The compound of or claim 1 , wherein ring A is a 7-9 membered bicyclic heterocycloalkyl ring containing one nitrogen ring atom.4. The compound of or claim 1 , wherein ring A is a 4-7 membered heterocycloalkyl ring containing one nitrogen ring atom.5. The compound of any one of to claim 1 , wherein Z is O or NR.6. The compound of any one of to claim 1 , wherein Ris Calkyl claim 1 , Chydroxyalkyl claim 1 , C(O)Calkyl claim 1 , Calkylene-Ccycloalkyl claim 1 , or Calkylene-Cheterocycloalkyl having 1 or 2 heteroatoms selected from O claim 1 , S claim 1 , N claim 1 , and N(Calkyl).7. The compound of any one of to claim 1 , wherein Ris H claim 1 , Calkyl claim 1 , Chydroxyalkyl claim 1 , Calkylene-Ccycloalkyl claim 1 , or Calkylene-Cheterocycloalkyl having 1 or 2 heteroatoms selected from O claim 1 , S claim 1 , N claim 1 , and N(Calkyl).8. The compound of claim 7 , wherein Ris Calkyl claim 7 , Chydroxyalkyl claim 7 , Calkylene-Ccycloalkyl claim 7 , or Calkylene-Cheterocycloalkyl having 1 or 2 heteroatoms selected from O claim 7 , S claim 7 , N claim 7 , and N(Calkyl).9. The compound of claim 7 , wherein Ris Calkyl claim 7 , Chydroxyalkyl claim 7 , or Calkylene-Ccycloalkyl.10. The compound of claim 7 , wherein Ris H.11. The compound of claim 7 , wherein Ris a Calkyl.12. The compound of claim 7 , wherein Ris methyl claim 7 , ...

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Номер записи: 47
14-01-2021 дата публикации

Benzamide compounds

Номер: US20210009543A1
Автор: Ahmed Abdi Samatar, Joseph Robert Pinchman, Kevin Duane Bunker, Peter Qinhua HUANG, Rakesh Kumar Sit
Принадлежит: Recurium IP Holdings LLC, Zeno Management Inc

Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as cancer and tumors, as well as viral infections such as HIV.

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Номер записи: 48
10-01-2019 дата публикации

Urea derivative and use therefor

Номер: US20190010117A1
Автор: Hideyuki Tsutsui, Hiroyuki Meguro, Keiichi Okimura, Masashi Yamamoto, Mie Kaino, Syuji UDAGAWA, Tomohide Masuda, Yukihiro Nishio, Yuko Kubota, Yumiko SEKIYA
Принадлежит: TORAY INDUSTRIES INC

A compound has inhibitory activity on Discoidin Domain Receptor 1. The compound includes a urea derivative represented by the formula below or a pharmaceutically acceptable salt thereof.

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Номер записи: 49
09-01-2020 дата публикации

COMPOUNDS AND METHODS FOR TREATING CANCER

Номер: US20200010418A1
Автор: BRADNER James, ERB Michael, Qi Jun
Принадлежит:

The present application relates to compounds comprising an ester, a thioester, or a hydrazide moiety and methods of synthesizing these compounds. The present application also relates to pharmaceutical compositions containing the compounds and methods of treating cell proliferative disorders mediated by the Hh signaling pathway, such as cancer, by administering the compounds and pharmaceutical compositions to subjects in need thereof. 18. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.19. A method of modulating the SMO claim 1 , comprising contacting the SMO with a compound of or a pharmaceutically acceptable salt thereof.20. A method of treating a disorder mediated by the Hh signaling pathway claim 1 , comprising administering to a subject in need thereof claim 1 , a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof. This application is a divisional application of U.S. application Ser. No. 15/577,845, now allowed, which is a U.S. National Phase application, filed under 35 U.S.C. § 371, of International Application No. PCT/US2016/035641, filed on Jun. 3, 2016, which claims priority to, and the benefit of U.S. Provisional Application No. 62/171,783, filed on Jun. 5, 2015, the contents of each of which are incorporated herein by reference in their entireties.Aberrant regulation of the Hedgehog (Hh) signaling pathway drives several cancers, including medulloblastoma (MB) and Basal Cell Carcinoma (BCC), and is often caused by mutations to Patched (PTCH) or Smoothened (SMO) (Amakye et al., 19, 1410 (2013)). Loss of function mutations to PTCH in the germline are responsible for Gorlin syndrome (also known as nevoid basal cell carcinoma syndrome, NBCCS), a serious genetic disorder that predisposes an individual to several forms of cancer, including MB and BCC (Gorlin, Genet. Med. 6, 530 (2004)). Fortunately, SMO has proved ...

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Номер записи: 50
21-01-2016 дата публикации

AMINO- OR AMMONIUM-CONTAINING SULFONIC ACID, PHOSPHONIC ACID AND CARBOXYLIC ACID DERIVATIVES AND THEIR MEDICAL USE

Номер: US20160016981A1
Автор: Braxmeier Tobias, Friedrichson Tim, Jennings Gary, Knölker Hans-Joachim, Schlechtingen Georg
Принадлежит: GLYCOREGIMMUNE, INC.

The present invention relates to amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives, in particular the compounds of formula 1, 2, 3, 4, 5 or 6, and their medical use, including their use in the treatment, prevention or amelioration of an inflammatory, autoimmune and/or allergic disorder.

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Номер записи: 51
18-01-2018 дата публикации

Process for the synthesis of difluoromethyl ether-based compounds

Номер: US20180016227A1
Автор: Abdelmalik Slassi, Peter Dove
Принадлежит: Trillium Therapeutics ULC

The present application relates to a novel process for the preparation of difluoromethyl ether-based derivatives from, for example, aliphatic and aromatic hydroxyl precursors, compositions comprising these compounds and their use, in particular as precursors for medicines for the treatment of diseases, disorders or conditions. In particular, the present application includes the process of preparing compounds of Formula (I), and compositions and uses thereof:

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Номер записи: 52
15-01-2015 дата публикации

Compounds and methods for treating leukemia

Номер: US20150018355A1
Автор: Angelo A. Cardoso, Mark R. Kelley, Melissa L. Fishel
Принадлежит: Indiana University Research And Technology Corp

Compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating leukemia. In particular, compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating acute lymphoblastic leukemia (ALL) in its various forms.

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Номер записи: 53
24-01-2019 дата публикации

N-sulfonyl benzamide derivative with heterocyclic substituent, preparation method therefor and pharmaceutical application thereof

Номер: US20190023654A1
Автор: Dong Huang, Fusheng ZHOU, Jing Xie, Jinzhu ZHAO, Jiong Lan, Qiang Lv, Yi Hu
Принадлежит: Shanghai Haiyan Pharmaceutical Technology Co Ltd, Yangtze River Pharmaceutical Group Co Ltd

The present invention discloses an N-sulfonyl benzamide derivative with a heterocyclic substituent, and a preparation method therefor and a pharmaceutical application thereof. More specifically, the invention discloses a compound represented by formula (II) or a pharmaceutically acceptable salt, stereoisomer, solvent compound, or prodrug thereof, and a preparation method therefor and an application thereof. Refer to the specification for definitions of each group in the

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Номер записи: 54
24-01-2019 дата публикации

METHOD FOR PRODUCING KAKEROMYCIN AND DERIVATIVES THEREOF

Номер: US20190023667A1
Автор: ISHIKAWA Teruhiko, IWAMI Morita
Принадлежит:

Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): This patent application is a divisional of copending U.S. patent application Ser. No. 15/554,002, filed on Aug. 27, 2017, which the U.S. national phase of International Patent Application No. PCT/JP2016/055891, filed on Feb. 26, 2016, which claims the benefit of Japanese Patent Application No. 2015-039363, filed Feb. 27, 2015, the disclosures of which are incorporated herein by reference in their entireties for all purposes.The present invention relates to a production method of kakeromycin and a derivative thereof.In recent years, along with an increase in elderly people, progress of advanced medicine, immunodeficiency of late stage cancer patients and the like, infections with fungi have been increasing. These infections provide serious effects, often causing death. Since there are not many kinds of existing antifungal agents, and their toxicity is high, the mother nucleus of a new antifungal agent, which is different from that of conventional medicaments, has been desired. In addition, since the use of antifungal agents causes increased emergence of resistant bacteria, the development of a new medicament has been earnestly desired. While candin-based antifungal agents show low toxicity, since the molecular weight thereof is large, reactivity with serum poses problems. Azole-based antifungal agents have a problem in that administration at a high concentration is difficult in view of the toxicity thereof. Therefore, an effective, low-molecular-weight compound showing low reactivity with serum and low toxicity has been strongly desired.Conventionally, in search of a pharmaceutical product seed compound from microbial metabolites, terrestrial separation sources have been mainly harvested and subjected ...

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Номер записи: 55
24-01-2019 дата публикации

METHOD FOR PRODUCING KAKEROMYCIN AND DERIVATIVES THEREOF

Номер: US20190023668A1
Автор: ISHIKAWA Teruhiko, IWAMI Morita
Принадлежит:

Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): This patent application is a divisional of copending U.S. patent application Ser. No. 15/554,002, filed on Aug. 27, 2017, which the U.S. national phase of International Patent Application No. PCT/JP2016/055891, filed on Feb. 26, 2016, which claims the benefit of Japanese Patent Application No. 2015-039363, filed Feb. 27, 2015, the disclosures of which are incorporated herein by reference in their entireties for all purposes.The present invention relates to a production method of kakeromycin and a derivative thereof.In recent years, along with an increase in elderly people, progress of advanced medicine, immunodeficiency of late stage cancer patients and the like, infections with fungi have been increasing. These infections provide serious effects, often causing death. Since there are not many kinds of existing antifungal agents, and their toxicity is high, the mother nucleus of a new antifungal agent, which is different from that of conventional medicaments, has been desired. In addition, since the use of antifungal agents causes increased emergence of resistant bacteria, the development of a new medicament has been earnestly desired. While candin-based antifungal agents show low toxicity, since the molecular weight thereof is large, reactivity with serum poses problems. Azole-based antifungal agents have a problem in that administration at a high concentration is difficult in view of the toxicity thereof. Therefore, an effective, low-molecular-weight compound showing low reactivity with serum and low toxicity has been strongly desired.Conventionally, in search of a pharmaceutical product seed compound from microbial metabolites, terrestrial separation sources have been mainly harvested and subjected ...

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Номер записи: 56
24-01-2019 дата публикации

METHOD FOR PRODUCING KAKEROMYCIN AND DERIVATIVES THEREOF

Номер: US20190023669A1
Автор: ISHIKAWA Teruhiko, IWAMI Morita
Принадлежит:

Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): 1. A compound represented by the formula (6):whereinR is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group,{'sup': '4', 'Ris an optionally substituted hydrocarbon group or an optionally substituted hydrocarbon-oxy group, and'}n is 0 or 1, This patent application is a divisional of copending U.S. patent application Ser. No. 15/554,002, filed on Aug. 27, 2017, which the U.S. national phase of International Patent Application No. PCT/JP2016/055891, filed on Feb. 26, 2016, which claims the benefit of Japanese Patent Application No. 2015-039363, filed Feb. 27, 2015, the disclosures of which are incorporated herein by reference in their entireties for all purposes.The present invention relates to a production method of kakeromycin and a derivative thereof.In recent years, along with an increase in elderly people, progress of advanced medicine, immunodeficiency of late stage cancer patients and the like, infections with fungi have been increasing. These infections provide serious effects, often causing death. Since there are not many kinds of existing antifungal agents, and their toxicity is high, the mother nucleus of a new antifungal agent, which is different from that of conventional medicaments, has been desired. In addition, since the use of antifungal agents causes increased emergence of resistant bacteria, the development of a new medicament has been earnestly desired. While candin-based antifungal agents show low toxicity, since the molecular weight thereof is large, reactivity with serum poses problems. Azole-based antifungal agents have a problem in that administration at a high concentration is difficult in view of the toxicity thereof. Therefore, an ...

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Номер записи: 57
02-02-2017 дата публикации

FUCOSIDASE INHIBITORS

Номер: US20170029376A1
Автор: Isbell Sara Louise, Ko Amanda Anne, Zankel Todd C.
Принадлежит: RAPTOR PHARMACEUTICALS INC.

The present disclosure relates, in general, to compounds useful as inhibitors of fucosidase enzymes, and to methods and compositions for the treatment of tumors or cancers, such as liver disorders and liver tumors (e.g., hepatocellular carcinoma), with a compound as disclosed herein. 2. The compound of claim 1 , wherein X claim 1 , X claim 1 , and Xare OH claim 1 , R is methyl claim 1 , and/or Ris H.3. (canceled)4. (canceled)5. The compound of claim 1 , wherein Ris —NRC(O)Ror —C(O)NRR.6. (canceled)7. (canceled)8. The compound of claim 1 , wherein G is selected from the group consisting of optionally substituted indolyl claim 1 , benzothiophenyl claim 1 , fluorenyl claim 1 , indenyl claim 1 , dihydro indenyl claim 1 , and phenyl.13. (canceled)15. (canceled)16. (canceled)18. (canceled)20. The method of claim 19 , wherein the tumor or cancer is liver cancer claim 19 , breast cancer claim 19 , melanoma claim 19 , lung cancer claim 19 , leukemia claim 19 , pancreatic cancer claim 19 , gastric cancer claim 19 , colorectal cancer claim 19 , and head and neck cancer.21. The method of claim 19 , wherein the compound reduces tumor metastasis in a subject claim 19 , the treatment results in a decrease in tumor size in the subject claim 19 , and/or the treatment results in a reduction of alpha-fetoprotein levels in blood of the subject compared to levels before treatment.22. The method of claim 19 , wherein the tumor is a result of hepatocellular carcinoma claim 19 , hepatitis virus infection claim 19 , cirrhosis claim 19 , toxic liver damage claim 19 , and hereditary hemochromatosis.23. (canceled)24. (canceled)25. (canceled)26. The method of claim 19 , wherein the compound is administered intravenously claim 19 , optionally wherein the compound is administered via the hepatic artery.27. (canceled)28. The method of claim 19 , wherein the compound is administered in combination with a second agent claim 19 , optionally wherein the second agent is selected from the group ...

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Номер записи: 58
02-02-2017 дата публикации

1,1,1-TRIFLUORO-3-HYDROXYPROPAN-2-YL CARBAMATE DERIVATIVES AND 1,1,1-TRIFLUORO-4-HYDROXYBUTAN-2-YL CARBAMATE DERIVATIVES AS MAGL INHIBITORS

Номер: US20170029390A1
Автор: "ONEIL STEVEN VICTOR", BECK ELIZABETH MARY, Brodney Michael Aaron, BUTLER CHRISTOPHER RYAN, GILBERT ADAM MATTHEW, Helal Christopher John, Johnson Douglas Scott, MCALLISTER LAURA ANN, MONTGOMERY JUSTIN IAN, ROGERS BRUCE NELSEN, VERHOEST PATRICK ROBERT, WEBB DAMIEN
Принадлежит: PFIZER INC.

The present invention provides, in part, compounds of Formula I: 3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein the compound of Formula I is a compound of I-a1.4. The compound of claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , wherein Rand R claim 3 , together with the N atom to which they are attached claim 3 , form 4- to 14-membered heterocycloalkyl that is substituted with Rand optionally substituted with one or more independently selected R.8. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein each of Rand Ris H.9. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris H or R; and Ris —P(═O)(OR)(OR).10. The compound of any one of claims claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , wherein the moiety of “—N(R)(R)” is a moiety of Formula a-46-1; Ris -L-Ror -L-R; and each of Land Lis —C(═O)— or —S(═O)—.11. A compound of selected from the group consisting of:(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl (1α,5α,6α)-6-[1-(5-methoxypyridin-2-yl)-1H-pyrazol-3-yl]-3-azabicyclo[3.1.0]hexane-3-carboxylate;(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl (1α,5α,6α)-6-[1-(4-fluorophenyl)-1H-pyrazol-3-yl]-3-azabicyclo[3.1.0]hexane-3-carboxylate;(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl 4-[(4-fluorophenyl)sulfonyl]-1-oxa-4,9-diazaspiro[5.5]undecane-9-carboxylate;(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl 4-(phenylsulfonyl)-1-oxa-4,9-diazaspiro[5.5]undecane-9-carboxylate;(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl (3S)-3-[(phenylsulfonyl)amino]-1-oxa-8-azaspiro[4.5]decane-8-carboxylate;(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl (3R)-3-[(phenylsulfonyl)amino]-1-oxa-8-azaspiro[4.5]decane-8-carboxylate;(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl 4-[(3-fluorophenyl)sulfonyl]-1-oxa-4,9-diazaspiro[5.5]undecane-9-carboxylate;(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl (3R)-3-[methyl(phenylsulfonyl)amino]-1-oxa-8-azaspiro[4.5]decane-8- ...

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Номер записи: 59
01-02-2018 дата публикации

Compounds for their use as drugs for the treatment and/or the prevention of infection(s) caused by biofilm-forming bacteria

Номер: US20180030047A1
Автор: Agnieszka KYZIOL, Agnieszka MACHUL, Cyril NICOLAS, Diana MIKOLAJCZYK, Estelle GALLIENNE-BOIVINEAU, Grazyna Stochel, Magdalena Strus, Olivier Martin, Piotr B. Heczko
Принадлежит: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS, Universite dOrleans, UNIWERSYTET JAGIELLONSKI

Disclosed are compounds of the following formula I: wherein: m represents an integer being equal to 0, 1, 2, 3, 4, 5 or 6, X represents a simple bond or a radical —CHR 1 — wherein R 1 represents: a hydrogen atom, or a linear or branched, possibly interrupted by up to 3 heteroatoms selected from O, S or N and/or possibly substituted, (C 1 -C 12 )-alkyl, R 2 , R 3 and R 4 represent independently from each other: a hydrogen atom, or a linear or branched (C 1 -C 12 )-alkyl or (C 1 -C 12 )-acyl R 5 represents: a hydrogen atom, or a linear or branched, possibly substituted, (C 1 -C 13 )-alkyl possibly interrupted by up to 3 heteroatoms selected from O, S or N, R 6 represents: a hydrogen atom, or a linear or branched possibly substituted (C 1 -C 12 )-alkyl, possibly substituted and possibly interrupted by up to 3 heteroatoms selected from O, S or N, for their use as antibacterial drugs.

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Номер записи: 60
31-01-2019 дата публикации

PHENYL DERIVATIVE

Номер: US20190030010A1
Автор: KAKUUCHI Akito, KUSUMI Kensuke, NAGANAWA Atsushi, NONAKA Shigeyuki, Otsuki Kazuhiro, SEKIGUCHI Tetsuya, SHINOZAKI Koji, Yamamoto Hiroshi
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

The compound of the formula (I-1): 2. The method according to claim 1 , wherein the ring 1 and the ring 2 each independently are (1) a benzene claim 1 , (2) cyclohexane or (3) pyridine ring.3. The method according to claim 1 , wherein the compound of formula (I-A) is 2-{4-[3-(4-fluorophenoxy)-5-{[(4-hydroxy-4-isobutyl-1-piperidinyl)carbonyl]amino}phenoxy]phenyl}-2-methylpropanoic acid or a salt thereof.4. The method according to claim 1 , wherein the protecting group T comprises a carbonyl group.5. The method according to claim 4 , wherein the protecting group T is a 2 claim 4 ,2 claim 4 ,2-trichloroethoxycarbonyl (Troc) group claim 4 , a phenoxycarbonyl group claim 4 , or a p-nitrophenoxycarbonyl group.6. The method according to claim 2 , wherein the compound of formula (I-A) is 2-{4-[3-(4-fluorophenoxy)-5-{[(4-hydroxy-4-isobutyl-1-piperidinyl)carbonyl]amino}phenoxy]phenyl}-2-methylpropanoic acid or a salt thereof.7. The method according to claim 1 , wherein the ring 1 and the ring 2 each independently are a benzene.8. The method according to claim 2 , wherein the ring 1 and the ring 2 each independently are a benzene.9. The method according to claim 1 , wherein the base is selected from the group consisting of pyridine claim 1 , triethylamine claim 1 , dimethylaniline claim 1 , dimethylaminopyridine claim 1 , diisopropylethylamine claim 1 , or a mixture thereof.10. The method according to claim 1 , wherein the organic solvent is selected from N claim 1 ,N-dimethylacetamide claim 1 , chloroform claim 1 , dichloromethane claim 1 , diethyl ether claim 1 , tetrahydrofuran claim 1 , and a mixture thereof.11. The method according to claim 2 , wherein the base is selected from the group consisting of pyridine claim 2 , triethylamine claim 2 , dimethylaniline claim 2 , dimethylaminopyridine claim 2 , diisopropylethylamine claim 2 , or a mixture thereof.12. The method according to claim 2 , wherein the organic solvent is selected from N claim 2 ,N-dimethylacetamide claim 2 ...

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Номер записи: 61
31-01-2019 дата публикации

ANALOGS OF PRIDOPIDINE, THEIR PREPARATION AND USE

Номер: US20190030016A1
Автор: Kaljuste Kalle, Laos Marit, Maasalu Ants, Päri Malle, Schmidt Malle
Принадлежит: TEVA PHARMACEUTICAL INDUSTRIES LTD.

This invention provides an isolated compound having the structure: 17. A pharmaceutical composition comprising an amount of pridopidine and at least one of Compound 1 , Compound 2 , Compound 3 , Compound 4 , Compound 5 , Compound 6 , and Compound 7 whereina) Compound 1 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, orb) Compound 2 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, orc) Compound 3 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, ord) Compound 4 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, ore) Compound 5 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, orf) Compound 6 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, org) Compound 7 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method.18. The pharmaceutical composition of claim 17 , whereina) Compound 1 is present in the pharmaceutical composition in an amount not more than 0.15 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, orb) Compound 2 is present in the pharmaceutical composition in an amount not more than 0.15 area-% relative to the concentration of pridopidine, based on a determination by an HPLC ...

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Номер записи: 62
30-01-2020 дата публикации

ANALOGS OF PRIDOPIDINE, THEIR PREPARATION AND USE

Номер: US20200030308A1
Автор: Kaljuste Kalle, Laos Marit, Maasalu Ants, Päri Malle, Schmidt Malle
Принадлежит:

This invention provides an isolated compound having the structure: 2. The composition of claim 1 , wherein the composition comprises pridopidine and at least one of compound 1 claim 1 , compound 4 or combination thereof.3. The composition of claim 1 , wherein the composition comprises pridopidine salt claim 1 , wherein the salt is hydrochloride claim 1 , hydrobromide claim 1 , nitrate claim 1 , perchlorate claim 1 , phosphate claim 1 , sulphate claim 1 , formate claim 1 , acetate claim 1 , aconate claim 1 , ascorbate claim 1 , benzenesulphonate claim 1 , benzoate claim 1 , cinnamate claim 1 , citrate claim 1 , embonate claim 1 , enantate claim 1 , fumarate claim 1 , glutamate claim 1 , glycolate claim 1 , lactate claim 1 , maleate claim 1 , malonate claim 1 , mandelate claim 1 , methane-sulphonate claim 1 , naphthalene-2-sulphonate claim 1 , phthalate claim 1 , salicylate claim 1 , sorbate claim 1 , stearate claim 1 , succinate claim 1 , tartrate or toluene-p-sulphonate salt.4. The composition of claim 1 , in the form of a capsule claim 1 , a tablet claim 1 , a pill claim 1 , a powder claim 1 , a granule claim 1 , a liquid solution or a liquid suspension.5. The composition of claim 1 , in an oral dosage unit form.6. The composition of claim 5 , wherein the oral dosage unit form comprises between 22.5-315 mg pridopidine.7. The composition of claim 6 , wherein the oral dosage unit form comprises between 45-250 mg pridopidine.8. The composition of claim 7 , wherein the oral dosage unit form comprises between 45-135 mg pridopidine.9. The composition of claim 8 , wherein the oral dosage unit form comprises between 90-315 mg pridopidine.10. The composition of claim 6 , wherein the oral dosage unit form comprises about 22.5 mg pridopidine claim 6 , about 45 mg pridopidine claim 6 , about 67.5 mg pridopidine claim 6 , about 90 mg pridopidine claim 6 , about 100 mg pridopidine claim 6 , about 112.5 mg pridopidine claim 6 , about 125 mg pridopidine claim 6 , about 135 mg ...

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Номер записи: 63
30-01-2020 дата публикации

WATER-SOLUBLE COMPOSITION, PRODUCTION METHOD FOR CURED PRODUCT THEREOF, AND CURED PRODUCT THEREOF, AND ACYL PHOSPHINATE

Номер: US20200032021A1
Автор: Hara Kenji, Irisawa Masatomi
Принадлежит: ADEKA CORPORATION

Provided are: a water-soluble composition which has excellent storage stability and is adaptable to a wide range of light sources and capable of forming a highly fine pattern; a method of producing a cured product of the same; a cured product of the same; and an acylphosphinate. The water-soluble composition contains: an acylphosphinate (A) represented by Formula (I) below, wherein Xrepresents an aryl group having 6 to 15 carbon atoms; Xrepresents a linear alkyl group having 1 to 8 carbon atoms or the like; A represents an alkali metal ion or the like; and m represents a number of 1 to 3; and a compound (B) having a group represented by Formula (II) below, wherein Rrepresents a hydrogen atom or the like; Zrepresents an oxygen atom or the like; Rrepresents a hydrogen atom or the like; Zrepresents an alkylene group having 1 to 6 carbon atoms; n represents a number of 0 to 30; * means a bond; and, when the compound (B) has plural groups represented by Formula (II), plural Rs, Zs, Zs and n's are each optionally the same or different. 2. The water-soluble composition according to claim 1 , wherein Xin the Formula (I) is a 2 claim 1 ,4 claim 1 ,6-trimethylphenyl group.3. The water-soluble composition according to claim 1 , wherein claim 1 , in the Formula (I) claim 1 , Xis a phenyl group and A is NHYYY.4. The water-soluble composition according to claim 1 , wherein{'sup': m+', '+', '1', '2', '3, 'A in the Formula (I) is NHYYY, and'}{'sup': 1', '2', '3, 'at least one hydrogen atom of Y, Yand Yis substituted with a hydroxy group.'}5. The water-soluble composition according to claim 1 , wherein Zin the Formula (II) is —NR—.6. The water-soluble composition according to claim 1 , further comprising a coloring agent (C).7. A method of producing a cured product claim 1 , comprising curing the water-soluble composition according to by irradiation with light or heating.8. A cured product obtained from the water-soluble composition according to .10. The acylphosphinate according to ...

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Номер записи: 64
04-02-2021 дата публикации

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Номер: US20210032195A1
Автор: Govek Steven P., Nagasawa Johnny Y., Smith Nicholas D.
Принадлежит:

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity. 1131-. (canceled)134. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:ring B is phenyl; orring B is monocyclic 6-membered heteroaryl selected from pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.136. The compound of claim 134 , or a pharmaceutically acceptable salt or solvate thereof claim 134 , wherein:ring D is phenyl; orring D is monocyclic heteroaryl selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl; or{'sub': 2', '8, 'ring D is a monocyclic heterocycle that is a monocyclic C-Cheterocycloalkyl containing at least 1 N atom in the ring that is selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidine-2,5-dionyl, piperidinyl, piperidin-2-onyl, piperazinyl, morpholinyl, thiomorpholinyl, and azepanyl.'}138. The compound of claim 136 , or a pharmaceutically acceptable salt or solvate thereof claim 136 , wherein:{'sup': 3', '10, 'Lis absent, —O—, —S—, —CH═CH—, —C≡C—, or —NR—.'}139. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:{'sub': 3', '8, 'ring A is C-Ccycloalkyl'}140. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:{'sub': 2', '8, 'ring A is C-Cheterocycloalkyl.'}141. The compound of claim 140 , or a pharmaceutically acceptable salt or solvate thereof claim 140 , wherein:{'sub': 2', '8', '5', '8', '5', '8', '5', '8', '5', '8, 'ring A is a monocyclic C-Cheterocycloalkyl or a bicyclic C-Cheterocycloalkyl ...

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Номер записи: 65
04-02-2021 дата публикации

COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9

Номер: US20210032214A1
Автор: Barta Thomas E., Bourne Jonathan William, Bowers Simeon, Pandey Anjali
Принадлежит:

The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I). 2. (canceled)4. (canceled)5. (canceled)6. (canceled)7. The compound of claim 1 , wherein m is 1.8. The compound of claim 1 , wherein m is 0 or 1.9. The compound of claim 1 , wherein Ris hydrogen.10. (canceled)11. The compound of any preceding claim claim 1 , wherein Ris hydrogen or Calkyl optionally substituted with halo or hydroxy.12. (canceled)13. The compound of claim 1 , wherein Ris halo claim 1 , Calkyl claim 1 , or aryl claim 1 , wherein Calkyl or aryl is optionally substituted with 1 to 3 halo.14. The compound of claim 1 , wherein Ris chlorine or fluorine.15. The compound of claim 1 , wherein Ris CF.16. (canceled)17. (canceled)19. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of .21. A method of treating a disease or condition mediated claim 18 , at least in part claim 18 , by PCSK9 claim 18 , the method comprising administering to a patient in need thereof a compound of .22. The method of claim 20 , wherein the disease or condition is a cardiovascular disease claim 20 , a metabolic disease claim 20 , or hypocholesterolemia.23. The method of claim 22 , wherein the cardiovascular disease is coronary disease claim 22 , hypertension claim 22 , hypercholesterolemia claim 22 , or atherosclerosis.24. The method of claim 22 , the metabolic disease is diabetes.25. The method of claim 24 , wherein the patient has elevated plasma levels of low density lipoprotein cholesterol.26. (canceled)27. A method of inhibiting the activity of PCSK9 claim 1 , the method comprising binding a compound of to PCSK9 claim 1 , thereby inhibiting the activity of PCSK9. This application is a continuation of U.S. application Ser. No. 16/078,578, filed Aug. 21, 2018, which is the U.S. National Stage of ...

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Номер записи: 66
08-02-2018 дата публикации

ETHYLENEDIAMINETETRAACETIC ACID BIS(AMIDE) DERIVATIVES AND THEIR RESPECTIVE COMPLEXES WITH MN(II) ION FOR USE AS MRI CONTRAST AGENT

Номер: US20180036436A1
Автор: BARANYAI Zsolt, GARDA Zoltán, GHIANI Simona, KÁLMÁN Ferenc Krisztián, KRUSPER László, MAIOCCHI Alessandro, TIRCSÓ Gyula, TOTH Imre
Принадлежит: BRACCO IMAGING S.P.A.

The present invention relates to novel substituted ethylenediaminetetraacetic acid bisamide derivatives, their complexes with Mn(II) ion and the use thereof as contrast agents for Magnetic Resonance Imaging (MRI) analysis. 2. The compound according to claim 1 , wherein n is 2.3. The compound according to claim 1 , wherein Rand Rare alkyl groups and only one of them is substituted by the carboxyl group.4. The compound according to claim 1 , wherein Rand R claim 1 , taken together with the adjacent N atom claim 1 , form a 5 membered unsubstituted aromatic ring.5. The compound according to claim 1 , wherein Rand R claim 1 , taken together with the adjacent N atom claim 1 , form a 6-7 membered unsubstituted saturated ring.6. The compound according to claim 1 , wherein Rand R claim 1 , taken together with the adjacent N atom claim 1 , form a 6 membered saturated ring substituted by one hydroxyl and one additional moiety selected from the group consisting of methyl claim 1 , hydroxymethyl claim 1 , cyclopentylmethylene claim 1 , and cyclohexylmethylene.7. The compound according to claim 6 , wherein the methyl or hydroxymethyl moiety is at an ortho position and the hydroxyl moiety is at a meta position.8. The compound according to claim 6 , wherein the methyl or hydroxymethyl moiety is at a meta position and the hydroxyl moiety is at the other meta position or at the para position.9. The compound according to claim 1 , wherein Rand R claim 1 , taken together with the adjacent N atom claim 1 , form a 5-6 membered saturated ring substituted by a carboxyl moiety.10. The compound according to claim 9 , wherein the carboxyl is at a meta or the para position.11. The compound according to claim 1 , wherein Rand R claim 1 , taken together with the adjacent N atom claim 1 , form a 6 membered saturated ring substituted by an aminocarbonyl moiety which is in turn substituted at the aminocarbonyl nitrogen by bis(hydroxymethyl)methyl [—CH(CHOH)] claim 1 , 2 claim 1 ,3 claim 1 ,4 claim ...

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Номер записи: 67
08-02-2018 дата публикации

PIPERIDINE DERIVATIVES AND LIQUID-CRYSTALLINE MEDIUM

Номер: US20180037820A1
Автор: ENGEL Martin, Fortte Rocco, GOETZ Achim, Kodek Thorsten, MAAG Sabrina
Принадлежит: Merck Patent GmBH

Disclosed are compounds of the formula I, liquid-crystalline media comprising the compounds of formula I, and the use of these liquid-crystalline media in liquid-crystal displays. 2. The compound according to claim 1 , where{'sup': 1', '2, 'sub': '2', 'Spand Spare each independently alkylene having 1 to 12 carbon atoms which is optionally mono- or polysubstituted by F, Cl or CN, and in which one or more nonadjacent CHgroups are optionally each independently replaced by —O—, —S—, —NH—, —CO—, —COO—, —OCO—, —OCO—O—, —CH═CH— or —C≡C—.'}4. A method for stabilization of a liquid-crystalline medium claim 1 , comprising adding to said liquid-crystalline medium the compound according to .5. A process for preparing the compound according to claim 1 , comprising a reaction of 4-hydroxy-2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethylpiperidinyloxyl.6. A liquid-crystalline medium comprising{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a) one or more compounds according to and'}b) one or more mesogenic compounds.9. The liquid-crystalline medium according to claim 6 , wherein the total concentration of the one or more compounds of the formula I in the overall medium is 5000 ppm or less.10. An electrooptical display or electrooptical component comprising a liquid-crystalline medium according to .11. The compound according to claim 1 , where{'sub': '2', 'B is trans-1,4-cyclohexylene in which one or more nonadjacent CHgroups are optionally replaced by —O— and/or —S— and in which one or more hydrogen atoms are optionally replaced by F, or 1,4-phenylene in which one or two nonadjacent CH groups are optionally replaced by N and in which one or more hydrogen atoms are optionally replaced by L.'}12. The compound according to claim 1 , where{'sup': '0', 'sub': '2', 'Zis a single bond, —CFO— or —COO—.'}13. The compound according to claim 1 , where{'sup': 1', '2, 'sub': 2', 'p1', '2', '2', 'q1', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'Spand Sp, in each case independently, are, ...

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Номер записи: 68
08-02-2018 дата публикации

NOVEL LOW MOLECULAR WEIGHT CYCLIC AMINE CONTAINING CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY

Номер: US20180037893A1
Автор: Beutner Gregory L., Stanton Matthew G.
Принадлежит: Sirna Therapeutics, Inc.

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA. 2. A lipid nanoparticle comprising a cationic lipid according to .3. The lipid nanoparticle according to further comprises an oligonucleotide.4. The lipid nanoparticle according to wherein the oligonucleotide is siRNA or miRNA.5. The lipid nanoparticle according to wherein the oligonucleotide is siRNA. This application is a Continuation of U.S. patent application Ser. No. 14/719,513 filed, May 22, 2015, which is a Continuation of U.S. patent application Ser. No. 13/883,487 filed May 3, 2013, now U.S. Pat. No. 9,0678,82 issued Jun. 30, 2015, which is 371 National Phase Entry of International Patent Application No. PCT/US2011/058498 filed on Oct. 31, 2011, which claims benefit under 35 U.S.C. § 119(e) of the U.S. Provisional Application No. 61/410,472, filed Nov. 5, 2010, the contents of each of which are incorporated herein by reference in their entirety.The instant application contains a Sequence Listing which has been submitted electronically in ASCII format and is hereby incorporated by reference in its entirety. Said ASCII copy, created on Aug. 26, 2017 is named MRLMIS00047WOPCTSEQ.txt and is 3,671 bytes.The present invention relates to novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in ...

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Номер записи: 69
07-02-2019 дата публикации

PIPERIDINE DERIVATIVE

Номер: US20190040039A1
Автор: HARIGUCHI Norimitsu, Ishikawa Shunpei, Kawano Yoshikazu, Matsuba Miki, MATSUMOTO Makoto, SHIMIZU Hiroshi, TAKEMURA Isso
Принадлежит: OTSUKA PHARMACEUTICAL CO., LTD.

The purpose of the present invention is to provide a compound having excellent antibacterial activity against , multidrug-resistant tuberculosis bacteria, and/or non-tuberculous acid-fast bacteria. A compound represented by formula [I]: 2. The compound according to claim 1 , wherein Ring A is an optionally substituted 6-membered monocyclic hydrocarbon ring claim 1 , optionally substituted 6-membered monocyclic heterocycle claim 1 , optionally substituted 7- to 12-membered bicyclic hydrocarbon ring claim 1 , or optionally substituted 7- to 12-membered bicyclic or tricyclic heterocycle claim 1 , the heterocycle group comprising as a ring member atom 1 to 5 heteroatoms independently selected from the group consisting of nitrogen claim 1 , oxygen claim 1 , and sulfur;a substituent of Ring A is at least one group independently selected from the group consisting of:(1) halogen,(2) —CN,{'sub': '2', '(3) —NO,'}(4) ═N—OH,(5) —OH,(6) ═O,(7) ═S,{'sub': '1-6', 'claim-text': (i) halogen,', '(ii) —OH,', {'sup': a', 'a, 'sub': '1-6', '(iii) —COORwherein Ris hydrogen or Calkyl,'}, {'sub': '6-10', '(iv) —Caryl, and'}, {'sup': b', 'c', 'b', 'c, 'sub': '1-6', '(v) —CONRRwherein Rand Rare each independently hydrogen or Calkyl,'}], '(8) Calkyl optionally substituted with at least one group independently selected from the group consisting of{'sub': '1-6', '(9) Calkoxy optionally substituted with the same or different at least one halogen,'}{'sup': d', 'd, 'sub': 1-6', '1-6, '(10) —CORwherein Ris —OH, Calkyl, or Calkoxy,'}{'sub': '1-6', '(11) Calkyl-S—,'}{'sup': e', 'e, 'sub': 1-6', '1-6', '6-10', '7-12, '(12) —NHCORwherein Ris hydrogen, Calkyl, Calkoxy, Caryl, or Caralkyl,'}{'sup': b', 'c', 'b', 'c, '(13) —CONRRwherein Rand Rare the same as defined above,'}{'sup': b', 'c', 'b', 'c, '(14) —NRRwherein Rand Rare the same as defined above,'}{'sub': '6-10', '(15) Caryl optionally substituted with the same or different at least one halogen,'}{'sub': '6-10', '(16) Caryl-O—,'}{'sub': '7-12', '( ...

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Номер записи: 70
12-02-2015 дата публикации

Cinnamic acid hydroxyamides as inhibitors of histone deacetylase 8

Номер: US20150045367A1
Автор: Erik Verner, Sriram Balasubramanian, Wei Chen
Принадлежит: Pharmacyclics LLC

Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

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Номер записи: 71
06-02-2020 дата публикации

PRODRUGS OF GAMMA-HYDROXYBUTYRIC ACID, COMPOSITIONS AND USES THEREOF

Номер: US20200039917A1
Автор: Xiang Jia-Ning, Xu Xuesong, Zhang Xuan
Принадлежит:

The present disclosure discloses prodrugs of gamma-hydroxybutyric acid as well as compositions and uses thereof. 2. The composition of claim 1 , wherein the composition is a solid.3. The composition of claim 1 , wherein the composition further comprises a solvent for dissolving or dispersing the compound.4. The composition of claim 3 , wherein the solvent comprises water.5. The composition of claim 1 , wherein the composition is in a liquid dosage form.6. The composition of claim 1 , wherein the composition further comprises a flavoring agent claim 1 , sucrose claim 1 , lactose claim 1 , cellulose sugar claim 1 , mannitol claim 1 , maltitol claim 1 , dextran claim 1 , sorbitol claim 1 , starch claim 1 , agar claim 1 , alginates claim 1 , chitins claim 1 , chitosans claim 1 , pectins claim 1 , tragacanth gum claim 1 , gum arabic claim 1 , gelatins claim 1 , collagens claim 1 , casein claim 1 , albumin claim 1 , synthetic or semi-synthetic polymers or glycerides claim 1 , methyl cellulose claim 1 , hydroxypropylmethyl-cellulose claim 1 , or polyvinylpyrrolidone.7. The composition of claim 1 , wherein the composition further comprises a polymeric excipient.8. The composition of claim 1 , wherein the composition comprises a tablet claim 1 , a caplet claim 1 , a capsule claim 1 , a gel cap claim 1 , granules claim 1 , a pill claim 1 , a powder claim 1 , a lozenge claim 1 , a sachet claim 1 , a cachet claim 1 , a suspension claim 1 , an emulsion claim 1 , a solution claim 1 , a slurry claim 1 , or a syrup.9. The composition of claim 1 , wherein the composition is formulated in a unit dosage form.10. The composition of claim 9 , wherein the unit dosage form has a weight from 0.5 grams to 30 grams.11. The composition of claim 10 , wherein the composition is in a liquid dosage form.12. The composition of claim 11 , further comprising a pH adjusting agent selected from sodium hydroxide claim 11 , hydrochloric acid claim 11 , or malic acid.13. The composition of claim 1 , ...

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Номер записи: 72
15-02-2018 дата публикации

PHENYL DERIVATIVE

Номер: US20180042908A1
Автор: KAKUUCHI Akito, KUSUMI Kensuke, NAGANAWA Atsushi, NONAKA Shigeyuki, Otsuki Kazuhiro, SEKIGUCHI Tetsuya, SHINOZAKI Koji, Yamamoto Hiroshi
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

The compound of the formula (I-1): 1. A method of preventing and/or treating a S1P2-mediated disease , comprising administering to a mammal an effective amount of 2-{4-[3-(4-fluorophenoxy)-5-{[(4-hydroxy-4-isobutyl-1-piperidinyl)carbonyl]amino}phenoxy]phenyl}-2-methylpropanoic acid , or a salt thereof.2. The method according to claim 1 , wherein the S1P2-mediated disease is a disease resulting from vascular constriction claim 1 , fibrosis claim 1 , peripheral arterial occlusive disease claim 1 , hepatitis claim 1 , hepatic cirrhosis claim 1 , or hepatic failure.3. The method according to claim 2 , wherein the disease resulting from vascular constriction is cerebral vasospastic disease claim 2 , cardiac vasospastic disease claim 2 , coronary vasospastic disease claim 2 , hypertension claim 2 , pulmonary hypertension claim 2 , myocardial infarction claim 2 , angina claim 2 , arrhythmia claim 2 , portal hypertension claim 2 , varix claim 2 , or ischemia-reperfusion injury.4. The method according to claim 2 , wherein the fibrosis is pulmonary fibrosis claim 2 , hepatic fibrosis claim 2 , kidney fibrosis claim 2 , myocardial fibrosis claim 2 , or skin fibrosis. This is a Divisional of U.S. patent application Ser. No. 15/089,690 filed Apr. 4, 2016 (allowed), which is a Divisional of U.S. patent application Ser. No. 14/592,100 filed Jan. 8, 2015 (issued as U.S. Pat. No. 9,340,499 on May 17, 2016), which is a Continuation of U.S. application Ser. No. 14/347,178 filed Mar. 25, 2014 (issued as U.S. Pat. No. 8,975,409 on Mar. 10, 2015), which is a National Stage Entry of PCT International Application No. PCT/JP2012/074968 filed Sep. 27, 2012, which claims benefit of Japanese Patent Application No. 2011-213987 filed Sep. 29, 2011 of which disclosures are incorporated herein by reference in their entirety.The present invention relates to a compound represented by the formula (I-1):wherein all the symbols have the same meanings as described hereinbelow, and a salt thereof, a ...

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Номер записи: 73
18-02-2016 дата публикации

N-ACYLOXYSULFONAMIDE AND N-HYDROXY-N-ACYLSULFONAMIDE DERIVATIVES

Номер: US20160046570A1
Автор: BROOKFIELD Frederick Arthur, COURTNEY Stephen Martin, FROST Lisa Marie, KALISH Vincent Jacob, Sutton Art, Toscano John P.
Принадлежит:

The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy. 2. The compound of claim 1 , wherein L is —SO—.3. The compound of claim 1 , wherein Y is aryl and said aryl is unsubstituted or substituted with one or more substituents independently selected from W.4. The compound of claim 1 , wherein Y is aryl and said aryl is unsubstituted or substituted with one or two substituents independently selected from W.5. The compound of claim 1 , wherein Y is phenyl and said phenyl is unsubstituted or substituted with one or more substituents independently selected from W.6. The compound of claim 1 , wherein W is halo or —SO.7. The compound of claim 1 , wherein W is chloro claim 1 , bromo or —SO.8. The compound of claim 1 , wherein R is alkyl or phenyl claim 1 , wherein said alkyl and phenyl are unsubstituted or substituted with one or more halos.9. The compound of claim 2 , wherein Y is alkyl and said alkyl is unsubstituted or substituted with one or more substituents independently selected from W.10. The compound of claim 2 , wherein Y is alkyl and said alkyl is unsubstituted or substituted with one or more halos.11. The compound of claim 9 , wherein R is alkyl or phenyl claim 9 , wherein said alkyl and phenyl are unsubstituted or substituted with one or more substituents independently selected from halo claim 9 , nitro claim 9 , alkylsulfonyl and trihalomethyl.12. The compound of claim 1 , wherein the ...

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Номер записи: 74
18-02-2016 дата публикации

Therapeutic compounds and compositions

Номер: US20160046579A1
Автор: Giovanni Cianchetta, Janeta Popovici-Muller, Robert Zahler, Sheldon Cao, Xiaolei Wang, Zhixiong Ye
Принадлежит: Agios Pharmaceuticals Inc

Compounds of general formula (I) and compositions comprising compounds of general formula (I) that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.

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Номер записи: 75
16-02-2017 дата публикации

New Method for Preparing Isofagomine and Its Derivatives

Номер: US20170044102A1
Автор: Rybczynski Philip J., Sheth Kamlesh
Принадлежит:

A method for preparing isofagomine, its derivatives, intermediates and salts thereof using novel processes to make isofagomine from D-(−)-arabinose and L-(−)-xylose. 1. A method for preparing isofagomine , its derivatives , or acid salts thereof , comprising:protecting the anomeric hydroxyl group of D-(−)-arabinose with a protecting group to form a glycoside;further protecting by converting said protected glycoside to an acetonide using a ketal or ketone;converting said acetonide to an alkoxide and reacting with an alkylating agent to form an ether;converting said ether to a diol having two protecting groups;further protecting said diol using selective etherification to form a triprotected arabinose derivative;converting said arabinose derivative to a triprotected xylose derivative using an activated system;converting said xylose derivative to a triprotected nitrile using an activated system;converting said nitrile using catalytic hydrogenation.28-. (canceled)9. The method of claim 1 , wherein the protecting group is selected from benzyl claim 1 , methoxybenzyl claim 1 , chlorobenzyl claim 1 , diphenylmethyl claim 1 , methyl claim 1 , ethyl claim 1 , isopropyl or cyclohexylmethyl.10. The method of claim 1 , wherein the ketone or ketal is selected from acetone claim 1 , 2-butanone claim 1 , benzophenone claim 1 , cyclohexanone claim 1 , acetophenone claim 1 , or their corresponding dialkylketals.11. The method of claim 1 , wherein the activated system is selected from p-toluenesulfonate claim 1 , methanesulfonate claim 1 , and trifluoromethanesulfonate13. The method of claim 12 , wherein the protecting group is benzyl.14. The method of claim 12 , wherein the ketone or ketal is selected from acetone claim 12 , 2 claim 12 ,2-dimethoxypropane claim 12 , or combinations thereof.15. The method of claim 12 , wherein the leaving group is trifluoromethanesulfonate. This application claims the benefit of U.S. Provisional Application Ser. No. 60/939,519, filed May 22, 2007, ...

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Номер записи: 76
16-02-2017 дата публикации

Compounds for treating viral infections

Номер: US20170044181A1
Автор: Dongsik Park, Hee-Young Kim, Jaeheon Lee, Jaewon Yang, Jeongjin KWON, Jihyun Choi, Jong Yeon Hwang, Marc P. Windisch, Suyeon JO
Принадлежит: INSTITUT PASTEUR KOREA

The present invention relates to small molecule compounds and their use in the treatment of diseases, in particular viral diseases, in particular hepatitis C virus (HCV).

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Номер записи: 77
15-02-2018 дата публикации

Biguanide compound and use thereof

Номер: US20180044283A1
Автор: Hong Bum Lee, Hong Woo Kim, Hye Jin Heo, Jae Kap Jeong, Ji Ae KOOK, Ji Sun Lee, Sung Wuk Kim
Принадлежит: IMMUNOMET THERAPEUTICS INC

The present invention relates to a guanidine compound and a use thereof, and more specifically, to a guanidine derivative showing excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence; a preparation method thereof; and a pharmaceutical composition containing the same as an active ingredient. Compared to existing drugs, the guanidine derivative according to the present invention shows excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence even with small doses, and may thus be effectively used in preventing or treating various cancers such as uterine cancer, breast cancer, stomach cancer, brain cancer, rectal cancer, colorectal cancer, lung cancer, skin cancer, blood cancer, liver cancer, etc., inhibiting cancer cell proliferation and cancer metastasis.

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Номер записи: 78
19-02-2015 дата публикации

Novel Compounds For Preventing And/Or Treating Lysosomal Storage Disorders And/Or Degenerative Disorders Of The Central Nervous System

Номер: US20150050263A1
Автор: Boyd Robert, Rybczynski Philip J., Sheth Kamlesh
Принадлежит:

Described are novel salts of the compound (3R,4R,5S)-5-(difluoromethyl) piperidine-3,4-diol, as well as methods of using the same for preventing and/or treating lysosomal storage disorders and/or degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease and/or Parkinson's disease. 1. A fumarate salt of (3R ,4R ,5S)-5-(difluoromethyl)piperidine-3 ,4-diol or a solvate or prodrug thereof.2. The fumarate salt of claim 1 , wherein the fumarate salt has a molar ratio of active ingredient to fumaric acid of about 1:1.3. The fumarate salt of claim 1 , wherein the fumarate salt has a molar ratio of active ingredient to fumaric acid of about 2:1.6. A polymorph of the fumarate salt of having an X-ray diffraction pattern of or .7. A pharmaceutical composition comprising the fumarate salt of and at least one pharmaceutically acceptable carrier.8. A method for preventing and/or treating Parkinson's disease in a patient at risk for developing or diagnosed with the same claim 7 , which comprises administering to the patient an effective amount of the pharmaceutical composition of .9. The method of claim 8 , which comprises administering the pharmaceutical composition in combination with an effective amount of a second therapeutic agent selected from the group consisting of carbidopa claim 8 , levodopa claim 8 , dopamine receptor agonists claim 8 , anticholinergics claim 8 , MAO inhibitors claim 8 , and COMT inhibitors.10. A method for preventing and/or treating Gaucher's disease in a patient at risk for developing or diagnosed with the same claim 7 , which comprises administering to the patient an effective amount of the pharmaceutical composition of .11. The method of claim 10 , which comprises administering the pharmaceutical composition in combination with an effective amount of a second therapeutic agent selected from the group consisting of human recombinant β-glucocerebrosidase ...

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Номер записи: 79
03-03-2022 дата публикации

ANTHRANILIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT OF HUMAN CANCERS

Номер: US20220064133A1
Автор: HERSHBERGER Paul, IV Otto, Maloney Patrick, MOOTS Holly, PEDDIBHOTLA Satyamaheshwar, Phanstiel
Принадлежит:

A method and apparatus for transferring an image of predetermined length onto a substrate by selective energization of a row of printing elements in a printhead of a printing apparatus. Operational characteristics of the printing apparatus are determined, and the image is rendered such that the number of rows of the pixels in the rendered image is no greater than the maximum number of rows of pixels which can be printed in the length of the image given the operational characteristics of the printing apparatus. Additional rows of pixels may be printed between pairs of rows of printed which correspond to consecutive rows in the rendered image. The pixel content of each additional row is a function of the pixel content of the adjacent pairs of rows.

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Номер записи: 80
25-02-2021 дата публикации

Immunomodulator compounds

Номер: US20210052514A1
Автор: Christopher Lange, Darren J. Mcmurtrie, JU Yang, Penglie Zhang, Rajinder Singh, Sreenivas Punna, Viengkham Malathong
Принадлежит: Chemocentryx Inc

including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

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Номер записи: 81
25-02-2016 дата публикации

Novel compounds

Номер: US20160052898A1
Автор: Andrea Hagebarth, Anja Richter, Daniel Basting, Dirk Schneider, Eckhard Bender, Florian Puehler, Franziska SIEGEL, Kai Thede, Ludwig Zorn, Manfred Möwes, Ningshu Liu, Philip Lienau, Stefan Golz, Ursula MÖNNING, William Johnston Scott
Принадлежит: Bayer Pharma AG

The present invention relates to substituted N-biphenyl-3-acetylamino-benzamides and N-[3-(acetylamino)phenyl]-biphenyl-carboxamides of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disorder, as a sole agent or in combination with other active ingredients.

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Номер записи: 82
23-02-2017 дата публикации

AUTOPHAGY INDUCING COMPOUNDS AND USES THEREOF IN TREATING AUTOPHAGY ASSOCIATED DISEASES

Номер: US20170050929A1
Автор: Ma Dawei, Yuan Junying, Zhang Lihong
Принадлежит:

This invention pertains to screening methods for identifying autophagy inducing compounds. 2. The pharmaceutical composition of claim 1 , wherein said composition further comprises a pharmaceutically acceptable carrier.3. The pharmaceutical composition of claim 1 , wherein said autophagy associated disease is a disease caused by misfolded protein aggregates.414-. (canceled)15. A method of treating an autophagy associated disease in a subject claim 1 , said method comprising administering to said subject a pharmaceutical composition according to in an amount effective to treat said disease claim 1 , wherein the autophagy associated disease is selected from the group consisting of Alzheimer's disease claim 1 , Parkinson's disease claim 1 , amyotrophic lateral sclerosis claim 1 , Huntington's disease claim 1 , spinocerebellar ataxia claim 1 , oculopharyngeal muscular dystrophy claim 1 , prion diseases claim 1 , fatal familial insomnia claim 1 , alpha-1 antitrypsin deficiency claim 1 , dentatorubral pallidoluysian atrophy claim 1 , frontal temporal dementia claim 1 , progressive supranuclear palsy claim 1 , x-linked spinobulbar muscular atrophy claim 1 , neuronal intranuclear hyaline inclusion disease claim 1 , and cancer claim 1 , thereby treating said disease in said subject.1619-. (canceled)20. The method of claim 15 , wherein said autophagy inducing compound is selected from the group comprising Loperamide claim 15 , Amiodarone claim 15 , Niguldipine claim 15 , Pimozide claim 15 , Nicardipine claim 15 , Penitrem A claim 15 , Fluspirilene claim 15 , Trifluoperazine claim 15 , and pharmaceutically acceptable salts thereof.2240-. (canceled) This application claims priority to Chinese Application No. 200710046992.1, filed on Oct. 12, 2007, the entire contents of which are hereby incorporated herein by reference.This invention pertains to autophagy inducing compounds that are useful in treating or preventing autophagy associated diseases, e.g., diseases caused by ...

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Номер записи: 83
22-02-2018 дата публикации

N-acyloxysulfonamide and n-hydroxy-n-acylsulfonamide derivatives

Номер: US20180050985A1
Автор: Art Sutton, Frederick Arthur Brookfield, John P. Toscano, Lisa Marie Frost, Stephen Martin Courtney, Vincent Jacob Kalish
Принадлежит: Cardioxyl Pharmaceuticals Inc, JOHNS HOPKINS UNIVERSITY

The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected, from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.

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Номер записи: 84
22-02-2018 дата публикации

CATIONIC LIPID

Номер: US20180051285A1
Автор: KASUYA Yuji, Koizumi Makoto, NIWA Takako, Onishi Yoshiyuki, Tamura Masakazu
Принадлежит:

The present invention provides a compound represented by the formula (Ia) as a novel cationic lipid that forms a lipid particle and also provides a lipid particle comprising the compound. The present invention further provides a nucleic acid lipid particle containing the lipid particle, and a pharmaceutical composition containing the nucleic acid lipid particle as an active ingredient. 2. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein Rand Rare each independently a C-Calkyl group.3. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein both Rand Rare methyl groups.4. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein Ris a C-Calkyl group.5. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein Ris a methyl group.6. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein{'sup': '1', 'sub': 17', '19', '1', '7', '17', '19', '1', '7, 'Lis a C-Calkyl group optionally substituted with a C-Calkanoyloxy group or a C-Calkenyl group optionally substituted with a C-Calkanoyloxy group.'}7. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein Lis a heptadecenyl group claim 1 , an octadecenyl group claim 1 , a nonadecenyl group claim 1 , a heptadecadienyl group claim 1 , an octadecadienyl group claim 1 , a nonadecadienyl group claim 1 , a heptadecatrienyl group claim 1 , an octadecatrienyl group claim 1 , or a nonadecatrienyl group optionally substituted with a C-Calkanoyloxy group.8. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein Lis a (R)-11-acetyloxy-cis-8-heptadecenyl group claim 1 , a cis-9-octadecenyl group (oleyl group) claim 1 , a cis-8 claim 1 ,11-heptadecadienyl group claim 1 , a cis-9 claim 1 ,12-octadecadienyl group (linoleyl group) claim 1 , a cis-10 claim 1 ,13-nonadecadienyl group claim 1 , or a cis-6 claim 1 ,9 claim 1 ,12-octadecatrienyl group (linolenyl group).9. The lipid of or a ...

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Номер записи: 85
13-02-2020 дата публикации

RESIST COMPOSITION AND PATTERNING PROCESS

Номер: US20200050105A1
Автор: Fujiwara Takayuki, Hatakeyama Jun, OHASHI Masaki
Принадлежит: SHIN-ETSU CHEMICAL CO., LTD.

A resist composition comprising a base polymer and a quencher in the form of an amine compound having an iodized aromatic ring bonded to the nitrogen atom via a divalent hydrocarbon group offers a high sensitivity and minimal LWR or improved CDU, independent of whether it is of positive or negative tone. 1. A resist composition comprising a base polymer and a quencher , the quencher being an amine compound having an iodine-substituted aromatic ring bonded to the nitrogen atom via a C-Cdivalent hydrocarbon group which may contain at least one moiety selected from ester bond and ether bond.3. The resist composition of claim 1 , further comprising an acid generator capable of generating a sulfonic acid claim 1 , imide acid or methide acid.4. The resist composition of claim 1 , further comprising an organic solvent.6. The resist composition of which is a chemically amplified positive resist composition.7. The resist composition of wherein the base polymer is free of an acid labile group.8. The resist composition of which is a chemically amplified negative resist composition.10. The resist composition of claim 1 , further comprising a surfactant.11. The resist composition of claim 1 , further comprising a quencher other than the amine compound.12. A process for forming a pattern comprising the steps of applying the resist composition of onto a substrate claim 1 , baking to form a resist film claim 1 , exposing the resist film to high-energy radiation claim 1 , and developing the exposed resist film in a developer.13. The process of wherein the high-energy radiation is ArF excimer laser radiation of wavelength 193 nm or KrF excimer laser radiation of wavelength 248 nm.14. The process of wherein the high-energy radiation is EB or EUV of wavelength 3 to 15 nm. This non-provisional application claims priority under 35 U.S.C. § 119(a) on Patent Application No. 2018-150050 filed in Japan on Aug. 9, 2018, the entire contents of which are hereby incorporated by reference.This ...

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Номер записи: 86
23-02-2017 дата публикации

CURVED LIQUID CRYSTAL DISPLAY AND METHOD OF MANUFACTURING THE SAME

Номер: US20170052412A1
Автор: BAE Ji Hong, OH Keun Chan, PARK Heung Shik
Принадлежит:

A curved liquid crystal display comprises, a first curved substrate; a second curved substrate facing the first curved substrate; a liquid crystal layer disposed between the first curved substrate and the second curved substrate; a first curved liquid crystal alignment layer disposed between the liquid crystal layer and the first curved substrate and containing a light stabilizer; and a second curved liquid crystal alignment layer disposed between the liquid crystal layer and the second curved substrate. 1. A curved liquid crystal display comprising:a first curved substrate;a second curved substrate facing the first curved substrate;a liquid crystal layer disposed between the first curved substrate and the second curved substrate;a first curved liquid crystal alignment layer disposed between the liquid crystal layer and the first curved substrate and containing a light stabilizer; anda second curved liquid crystal alignment layer disposed between the liquid crystal layer and the second curved substrate.2. The curved liquid crystal display of claim 1 , wherein the second curved liquid crystal alignment layer does not contain the light stabilizer.3. The curved liquid crystal display of claim 2 , wherein the second curved liquid crystal alignment layer comprises a reactive mesogen and an amount of the reactive mesogen is higher in the second curved liquid crystal alignment layer than an amount in the first curved liquid crystal alignment layer.4. The curved liquid crystal display of claim 2 , wherein the second curved liquid crystal alignment layer has a multilayer structure including a 2-1curved liquid crystal alignment layer and a 2-2curved liquid crystal alignment layer comprising a reactive mesogen claim 2 , and an amount of the reactive mesogen in the 2-2curved liquid crystal alignment layer is higher than an amount in the 2-1curved liquid crystal alignment layer.6. The curved liquid crystal display of claim 5 , wherein in the Chemical Formula 1 claim 5 , Z1 to Z3 ...

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Номер записи: 87
26-02-2015 дата публикации

Cycloalkyl Amine Compounds

Номер: US20150057443A1
Автор: Heal Jonathan R., Huxley Philip, Todd Richard S.
Принадлежит:

Cycloalkyl amine compounds of Formula (I), 2. The compound of claim 1 , wherein Rand Rare both H claim 1 , and R claim 1 , R claim 1 , Rand Rare all H.3. (canceled)5. The compound of claim 4 , wherein Ris H.7. (canceled)9. The compound of claim 1 , wherein ring A is unsubstituted.10. The compound of claim 1 , wherein ring A is substituted with one or more C-Calkyl.11. The compound of claim 10 , wherein ring A is substituted with one C-Calkyl.12. The compound of claim 1 , wherein ring A is optionally substituted C-Ccycloalkyl.13. The compound of claim 12 , wherein the compound is of Formula (Ia) or (Ib) and ring A is unsubstituted cyclobutyl.14. The compound of claim 12 , wherein the compound is of Formula (Ic) and ring A is unsubstituted cyclopentyl.15. The compound of claim 12 , wherein the compound is of Formula (Ic) and ring A is optionally substituted cyclobutyl.16. The compound of claim 2 , wherein each of Rand R claim 2 , independently claim 2 , is H claim 2 , halo claim 2 , or cyano.17. The compound of claim 16 , wherein at least one of Rand Ris halo.18. The compound of claim 17 , wherein each of Rand Ris chloro.19. The compound of claim 16 , wherein Rand R claim 16 , together with the carbon atoms to which they are attached claim 16 , form phenyl claim 16 , pyridyl claim 16 , pyrrolyl claim 16 , furanyl claim 16 , thienyl claim 16 , thiazolyl claim 16 , oxazolyl claim 16 , imidazolyl claim 16 , pyrazolyl claim 16 , isoxazolyl claim 16 , triazolyl claim 16 , oxadiazolyl claim 16 , pyridazinyl claim 16 , pyrazinyl claim 16 , or pyrimidyl.20. The compound of claim 2 , wherein one of Rand Ris H and the other is C-Calkyl optionally substituted with halo or is C-Ccycloalkyl optionally substituted with C-Calkyl.21. The compound of claim 20 , wherein the other of Rand Ris isopropyl or t-butyl claim 20 , optionally substituted with one or more halo groups.22. The compound of claim 1 , wherein one of Rand Ris C-Calkyl optionally substituted with halo and the other is ...

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Номер записи: 88
15-05-2014 дата публикации

NOVEL COMPOUNDS AS HISTAMINE H3 RECEPTOR LIGANDS

Номер: US20140135304A1
Автор: Ahmad Ishtiyaque, Deshpande Amol Dinakar, Dwarampudi Adi Reddy, Gangadasari Narasimhareddy, Jasti Venkateswarlu, Jayarajan Pradeep, Kambhampati Ramasastri, Kandikere Vishwottam Nagaraj, Mulla Mohmadsadik Abdulhamid, Nirogi Ramakrishna, Saraf Sangram Keshari, Shinde Anil Karbhari
Принадлежит: SUVEN LIFE SCIENCES LIMITED

The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. 2. The compound as claimed in claim 1 , wherein Rrepresents hydrogen claim 1 , halogen claim 1 , haloalkyl claim 1 , hydroxy or alkyl.3. The compound according to claim 1 , which is selected from the group consisting of:N-[4-(1-Cyclobutyl piperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide dihydrochloride;2-[4-(1-Cyclobutyl piperidin-4-yloxy)phenylamino]-1-(morpholin-4-yl)ethanone hydrochloride;N-[4-(1-Cyclobutyl piperidin-4-yloxy)-2-fluoro-phenyl]-2-(morpholin-4-yl)acetamide dihydrochloride;N-[4-(1-Cyclobutyl piperidin-4-yloxy)benzyl]morpholine-4-yl amide;N-[4-(1-Cyclobutyl piperidin-4-yloxy)-3-fluoro phenyl]-2-(morpholin-4-yl)acetamide;N-[4-(1-Cyclobutyl piperidin-4-yloxy)-2-methyl phenyl]-2-(3,3-difluoro pyrrolidin-1-yl)acetamide;N-[4-(1-Cyclobutyl piperidin-4-yloxy)-2-trifluoromethyl phenyl]-2-(piperidin-1-yl)acetamide;N-[4-(1-Cyclopentyl piperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide;N-[4-(1-Cyclobutyl piperidin-4-yloxy)-2-trifluoromethyl phenyl]-2-(morpholin-4-yl)acetamide;N-[4-(1-Isopropyl piperidin-4-yloxy)-2-methyl phenyl]-2-(pyrrolidin-1-yl)acetamide;N-[4-(1-Cyclobutyl piperidin-4-yloxy)-2-methyl phenyl]-2-(pyrrolidin-1-yl)acetamide;N-[4-(1-Cyclopentyl piperidin-4-yloxy)-2-methyl phenyl]-2-(piperidin-1-yl)acetamide;N-[4-(1-Cyclobutyl piperidin-4-yloxy)-2-methyl phenyl]-2-(piperidin-1-yl)acetamide;N-[4-(1-Cyclobutyl piperidin-4-yloxy)phenyl]-N-methyl-2-(morpholin-4-yl)acetamide;N-[4-(1-Cyclopentyl piperidin-4-yloxy)-2-methyl phenyl]-2-(R-2-methylpyrrolidin-1-yl)acetamide;N-[4-(1-Cyclobutyl piperidin-4-yloxy)-2-methyl phenyl]-2-(R-2-methyl pyrrolidin-1-yl)acetamide;N-[4-(1-Cyclobutyl piperidin-4-yloxy)-2-methoxy phenyl]-2-(morpholin-4-yl)acetamide;N-[4-(1-Cyclobutyl piperidin-4-yloxy)-2-trifluoromethyl phenyl]-2-(4-hydroxy piperidin-1-yl)acetamide;N-[4-(1-Cyclobutyl piperidin-4-yloxy)phenyl]-2-(4-hydroxy ...

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Номер записи: 89
03-03-2016 дата публикации

Compounds and liquid-crystalline medium

Номер: US20160060528A1
Автор: Achim Goetz, Detlef Pauluth, Ingo ALMEROTH, Martin Engel, Rocco Fortte, Sabrina Maag, Thomas MERGNER, Thorsten Kodek
Принадлежит: Merck Patent GmBH

The invention relates to compounds of the formula I, in which X 1 , X 2 , Sp, and R are as defined herein, and to the use thereof in liquid-crystal media, but also to the use of these liquid-crystal media in liquid-crystal displays, and also to liquid-crystal displays of this type per se.

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Номер записи: 90
01-03-2018 дата публикации

Derivatives of sobetirome

Номер: US20180057472A1
Автор: Andrew PLACZEK, James Matthew MEINIG, Sky Ferrara, Tapasree BANERJI, Thomas S. Scanlan
Принадлежит: Oregon Health Science University

Ester derivatives of sobetirome with enhanced CNS distribution are disclosed.

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Номер записи: 91
17-03-2022 дата публикации

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Номер: US20220081390A1
Автор: Govek Steven P., Nagasawa Johnny Y., Smith Nicholas D.
Принадлежит:

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity. 4. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring B is phenyl.5. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring B is monocyclic 6-membered heteroaryl selected from pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.7. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring D is phenyl.8. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring D is monocyclic heteroaryl selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.11. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:{'sub': 2', '8, 'ring D is a monocyclic heterocycle that is a monocyclic C-Cheterocycloalkyl containing at least 1 N atom in the ring that is selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidine-2,5-dionyl, piperidinyl, piperidin-2-onyl, piperazinyl, morpholinyl, thiomorpholinyl, and azepanyl.'}12. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:{'sup': 3', '2', '4', '4', '2, 'Lis —X-L- or -L-X—;'}{'sup': 2', '10', '10', '10', '10', '10, 'sub': 2', '2', '2', '2, 'Xis absent, —O—, —S—, —S(═O)—, —S(═O)—, —S(═O)NR—, —CH—, —CH═CH—, —C≡C—, —C(═O)—, —C(═O)O—, —OC(═O)—, —C(═O)NR—, —NRC(═O)—, —NRS(═O)—, or —NR—;'}{'sup': '4', 'sub': '2', 'Lis absent or —CH—.'}13. The compound of any one of - , or a pharmaceutically ...

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Номер записи: 92
08-03-2018 дата публикации

Compounds, compositions and methods useful for cholesterol mobilization

Номер: US20180064718A1
Автор: Jean-Louis Henri Dasseux, Ronald Barbaras
Принадлежит: Cerenis Therapeutics Holding SA

The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.

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Номер записи: 93
08-03-2018 дата публикации

METHOD FOR PRODUCING 1-(4-HYDROXYPHENYL)-4-(4-TRIFLUOROMETHOXYPHENOXY)PIPERIDINE OR SALT THEREOF

Номер: US20180065931A1
Автор: ASAHINA Aya, MIYAKE Masahiro, Okada Takahiro
Принадлежит: OTSUKA PHARMACEUTICAL CO., LTD.

The present invention provides a method for producing 1-(4-hydroxyphenyl)-4-(4-trifluoromethoxyphenoxy)piperidine or a salt thereof, the method including the step of heating hydroquinone and 4-(4-trifluoromethoxyphenoxy)piperidine. This method can produce 1-(4-hydroxyphenyl)-4-(4-trifluoromethoxyphenoxy)piperidine or a salt thereof in an industrially advantageous manner. 2. The production method according to claim 1 , wherein the hydroquinone represented by Formula (2) or a salt thereof is used in an amount of 2 to 10 moles per mole of the 4-(4-trifluoromethoxyphenoxy)piperidine represented by Formula (3) or a salt thereof.3. The production method according to claim 1 , wherein the heating step comprises heating at 150° C. or more.4. The production method according to claim 1 , wherein the heating step is performed under solvent-free conditions.9. A method for producing the compound represented by Formula (9) or a salt thereof by using 1-(4-hydroxyphenyl)-4-(4-trifluoromethoxyphenoxy)piperidine or a salt thereof claim 1 ,the method comprising:{'claim-ref': {'@idref': 'CLM-00006', 'claim 6'}, 'steps (c2) and (c3) according to .'}10. A method for producing the compound represented by Formula (9) or a salt thereof by using 1-(4-hydroxyphenyl)-4-(4-trifluoromethoxyphenoxy)piperidine or a salt thereof claim 1 ,the method comprising:{'claim-ref': {'@idref': 'CLM-00007', 'claim 7'}, 'steps (c1), (c2), and (c3) according to .'}11. A method for producing the compound represented by Formula (9) or a salt thereof by using 1-(4-hydroxyphenyl)-4-(4-trifluoromethoxyphenoxy)piperidine or a salt thereof claim 1 ,the method comprising:{'claim-ref': {'@idref': 'CLM-00008', 'claim 8'}, 'step (b1) according to .'} The present invention relates to a method for producing 1-(4-hydroxyphenyl)-4-(4-trifluoromethoxyphenoxy)piperidine or a salt thereof, and use thereof.1-(4-Hydroxyphenyl)-4-(4-trifluoromethoxyphenoxy)piperidine and salts thereof are compounds that are useful as an ...

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Номер записи: 94
08-03-2018 дата публикации

1,1,1-TRIFLUORO-3-HYDROXYPROPAN-2-YL CARBAMATE DERIVATIVES AND 1,1,1-TRIFLUORO-4-HYDROXYBUTAN-2-YL CARBAMATE DERIVATIVES AS MAGL INHIBITORS

Номер: US20180065943A1
Автор: "ONEIL STEVEN VICTOR", BECK ELIZABETH MARY, Brodney Michael Aaron, BUTLER CHRISTOPHER RYAN, GILBERT ADAM MATTHEW, Helal Christopher John, Johnson Douglas Scott, MCALLISTER LAURA ANN, MONTGOMERY JUSTIN IAN, ROGERS BRUCE NELSEN, VERHOEST PATRICK ROBERT, WEBB DAMIEN
Принадлежит: PFIZER INC.

The present invention provides, in part, compounds of Formula I: 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein the compound is a compound of I-a1.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each of Rand Ris independently H or methyl.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each of Rand Ris H.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H or R; and Ris —P(═O)(OR)(OR).9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.10. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein:{'sup': 8', '1', '11', '2', '12', '3', '13', '4', '14, 'Ris -L-R, -L-R, -L-R, or -L-R;'}{'sup': 1', '2', '3', '4', '21', '22', '23', '21', '22', '23', '21', '22', '21', '22, 'sub': 2', '2', '2', '2', '2', '2, 'each of L, L, L, and Lis independently absent, —(CRR)—, —C(═O)—, —S(═O)—, —S(═O)—NR—, —S(═O)—(CRR)—, —S(═O)—NR—(CRR)—, or —S(═O)—(CRR)—;'}{'sup': 21', '22, 'sub': '1-3', 'each of Rand Ris independently H, Calkyl, or cyclopropyl;'}{'sup': 11', '31, 'Ris 5- to 6-membered heteroaryl optionally substituted with one or more independently selected R;'}{'sup': 12', '31, 'Ris 5- to 6-membered heterocycloalkyl optionally substituted with one or more independently selected R;'}{'sup': 13', '33, 'Ris phenyl optionally substituted with one or more independently selected R; and'}{'sup': 14', '34, 'sub': '3-8', 'Ris Ccycloalkyl optionally substituted with one or more independently selected R.'}11. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris -L-R claim 4 , -L-R claim 4 , -L-R claim 4 , or -L-R; and each of each of L claim 4 , L claim 4 , L claim 4 , and Lis —S(═O)— or —C(═O)—.12. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris —S(═O ...

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Номер записи: 95
17-03-2016 дата публикации

4-(p-QUINONYL)-2-HYDROXYBUTANAMIDE DERIVATIVES FOR TREATMENT OF MITOCHONDRIAL DISEASES

Номер: US20160075638A1
Автор: JANKOWSKI Orion D., MOLLARD Paul, SHRADER William D., WESSON Kieron E.
Принадлежит:

Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed. 2. (canceled)4. The compound of claim 3 , where R claim 3 , R claim 3 , R claim 3 , and Rare methyl; or a salt claim 3 , a stereoisomer claim 3 , or a mixture of stereoisomers thereof.5. The compound of claim 3 , where Ris hydrogen and Ris C-Calkyl substituted with hydroxy claim 3 , alkoxy or —C(O)O—C-Calkyl; or a salt claim 3 , a stereoisomer claim 3 , or a mixture of stereoisomers thereof.6. The compound of claim 3 , where Ris hydrogen and Ris independently selected from C-C6 alkyl substituted with —NRR′ claim 3 , where Rand R′ are independently selected from the group consisting of hydrogen claim 3 , C-C-alkyl claim 3 , C-C-haloalkyl claim 3 , aryl claim 3 , aryl-C-C-alkyl claim 3 , heteroaryl claim 3 , heterocyclyl claim 3 , —C(O)—H claim 3 , —C(O)—C-C-alkyl claim 3 , —C(O)-aryl and —C(O)—C-C-alkyl-aryl; or a salt claim 3 , a stereoisomer claim 3 , or a mixture of stereoisomers thereof.7. The compound of claim 6 , where Ris hydrogen and Ris independently selected from C-C-6 alkyl substituted with heterocyclyl or heteroaryl group; or a salt claim 6 , a stereoisomer claim 6 , or a mixture of stereoisomers thereof.8. The compound of ...

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Номер записи: 96
17-03-2016 дата публикации

GLYCOLIPID INHIBITION USING IMINOSUGARS

Номер: US20160075651A1
Автор: ALONZI Dominic, BUTTERS Terry, Dwek Raymond A., KIAPPES John, Laing Peter, POLLOCK Stephanie, Ramstedt Urban, Zitzmann Nicole
Принадлежит:

The application provides iminosugars with a high activity and specificity for inhibiting ceramide glucosyltransferase. 1. A method of inhibiting ceramide glucosyltransferase and/or lowering a glycolipid concentration comprising administering to a subject in need thereof an effective amount of N-(9-Methoxynonyl)deoxynojirimycin or a pharmaceutically acceptable salt thereof.3. The method of claim 2 , wherein Ris a substituted or unsubstituted butyl claim 2 , pentyl claim 2 , hexyl claim 2 , heptyl claim 2 , or octyl group.4. The method of claim 2 , wherein Z is NH.5. The method of claim 2 , wherein at least one of Xis selected from NO claim 2 , Nor NH.7. The method of claim 6 , wherein{'sub': 1', '2', '5, 'Ris —(CH)—;'}{'sub': '1-4', 'Ware H;'}{'sub': 1', '2, 'Xis NO;'}{'sub': 3', '3, 'Xis N;'}{'sub': 2', '4', '5, 'X, X, and Xare H;'}{'sub': '2', 'Y is —(CH)—; and'}Z is NH.8. The method of claim 6 , wherein{'sub': 1', '2', '5, 'Ris —(CH)—;'}{'sub': '1-4', 'Ware H;'}{'sub': 1', '3', '2, 'Xand Xare NO;'}{'sub': 2', '4', '5, 'X, X, and Xare H;'}{'sub': '2', 'Y is —(CH)—; and'}Z is NH.10. The method of claim 9 , wherein R′ is an unsubstituted or substituted alkyl group having from 1 to 12 carbon atoms.11. The method of claim 10 , wherein R′ is an alkyl group substituted with from 1 to 3 oxygen atoms.12. The method of claim 11 , wherein R′ is (CH2)—O—(CH) claim 11 , where n is 5-8 and m is 0-4.13. The method of claim 10 , wherein R′ is an amino-substituted alkyl group.14. The method of claim 13 , wherein R′ is (CH)—NH—(CH) claim 13 , where p is 5-8 and q is 0-215. The method of claim 9 , wherein at least one of Xis halogen or halogenated alkyl.192918. The method of any one of - claims 1 , and claims 1 , wherein the subject is a subject with a disease or condition for which inhibiting ceramide glucosyltransferase and/or lowering a glycolipid concentration is beneficial claims 1 , wherein said administering results in treatment of said disease or condition.20. The method of ...

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Номер записи: 97
24-03-2022 дата публикации

N-BENZYL-N-ARYLSULFONAMIDE DERIVATIVE AND PREPARATION AND USE THEREOF

Номер: US20220089555A1
Автор: HU Xiuai, HU Yongzhou, WANG Xiaolu, Ye Qing
Принадлежит: Hangzhou Yirui Pharmaceutical Technology Co., Ltd

The invention provides an N-benzyl-N-arylsulfonamide derivative, which is an N-benzyl-N-arylsulfonamide compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof. The N-benzyl-N-arylsulfonamide derivative is obtained by condensing a substituted nitrobenzene with 5- or 6-membered nitrogen-containing aliphatic heterocycle (the ring B), reducing the nitro group to an amino group, and subjecting the amino group to reductive amination, sulfonamidation; or by subjecting a substituted nitrobenzene to nitro reduction, reductive amination and sulfonamidation, and condensing the resultant intermediate with 5- or 6-membered nitrogen-containing aliphatic heterocycle (the ring B). It has been experimentally demonstrated that the N-benzyl-N-arylsulfonamide derivative of the invention can specifically bind to Kv1.3 potassium channel and inhibit or decrease its activity, and is useful in the treatment of autoimmune diseases caused by abnormal activation of the Kv1.3 potassium channel in human or animals. The invention further provides a medicament or a pharmaceutical composition comprising the N-benzyl-N-arylsulfonamide derivative. 4. The N-benzyl-N-arylsulfonamide derivative according to claim 1 , characterized in that the N-benzyl-N-arylsulfonamide derivative is selected from the group consisting of the following compounds:ethyl 4-(2-cyano-4-((4-fluoro-N-propylphenyl)sulfonamido)phenyl) piperazin-1-formate,ethyl 4-(2-cyano-4-(N-(4-fluorobenzyl)propanesulfonamido)phenyl) piperazin-1-formate,ethyl 4-(2-cyano-4-(N-isobutylphenylsulfonamido)phenyl)piperazin-1-formate,N-(3-cyano-4-(4-hydroxypiperidin-1-yl)phenyl)-N-(4-fluorobenzyl) propane-1-sulfonamide,4-(2-cyano-4-(N-(4-fluorobenzyl)propyl)phenyl)-N,N-dimethyl piperazin-1-formamide,ethyl 4-(4-(N-benzylpropanesulfonamido)2-cyanophenyl)piperazin-1-formate,ethyl 4-(2-cyano-4-(N-(3-fluorobenzyl)propanesulfonamido)phenyl) piperazin-1-formate,ethyl 4-(4-(4-(N-(4-chlorobenzyl)propanesulfonamido)2- ...

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Номер записи: 98
07-03-2019 дата публикации

PYRIDINE COMPOUND AND USE THEREOF

Номер: US20190071403A1
Автор: Fukushima Yusuke, Inoue Hiroki, Iwata Jun, KAMADA Takuya, KOBAYASHI Tomomi, KOUBORI Shinya, MUNEI Youhei, NAKAMURA Yuka, Nishimura Satoshi, Tanaka Tetsuya, Teranishi Takaaki, UESUSUKI Shinya
Принадлежит: NIPPON SODA CO., LTD.

The present invention provides a compound represented by formula (I) (in the formula, Rto Reach represent a hydrogen atom, an unsubstituted or G-substituted C1-6 alkyl group or the like, A represents an oxygen atom or the like, Cy represents a C6-10 aryl group or the like), an N-oxide compound thereof, a tautomer or salt thereof. The present invention also provides an agricultural and horticultural fungicide, harmful organism control agent and insecticidal/acaricidal agent containing at least one compound selected from the group consisting of a compound represented by formula (I), a tautomer and salt thereof, as an active ingredient. 2. An agricultural and horticultural fungicide comprising as an active ingredient at least one selected from the group consisting of the pyridine compound claim 1 , the N-oxide compound thereof claim 1 , and the tautomer and salt thereof according to .3. A harmful organism control agent comprising as an active ingredient at least one selected from the group consisting of the pyridine compound claim 1 , the N-oxide compound thereof claim 1 , and the tautomer and salt thereof according to .4. (canceled)5. (canceled) The present invention relates to a pyridine compound and use thereof such as agricultural and horticultural fungicides, harmful organism control agents, insecticidal agents or acaricidal agents, or the like.Priority is claimed on Japanese Patent Application No. 2016-046046, filed Mar. 9, 2016, the content of which is incorporated herein by reference.In cultivation of agricultural and horticultural crops, a large number of control agents for crop diseases have been proposed. Most of those proposed control agents are not always satisfactory because the controlling effect thereof is insufficient, the use thereof is restricted due to the emergence of drug-resistant pathogenic bacteria, phytotoxicity or pollution to plants occurs, or the toxicity to livestocks and fish and the environmental impact were great. Therefore, an ...

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Номер записи: 99
05-03-2020 дата публикации

BIARYL PIPERIDINE AMIDE COMPOUNDS AND METHODS OF USE THEREOF

Номер: US20200071305A1
Автор: CLEMENTS James Lindsay, Hangauer, JR. David G., SMOLINSKI Michael P., URGAONKAR Sameer
Принадлежит:

The present application is directed to biaryl piperidine amide compounds, or pharmaceutically acceptable salts, solvates, and prodrugs thereof, and methods of use thereof. 114.-. (canceled)17. The method of further comprising modulating subsequent biochemical pathways culminating in cellular activation.18. The method of further comprising modulating production of a responsive cytokine.19. The method of claim 16 , wherein the antigen receptor is a T cell receptor.20. (canceled)25. The method according to claim 15 , wherein Ris selected from hydrogen claim 15 , halogen claim 15 , C-Calkyl claim 15 , C-Chaloalkyl claim 15 , OH claim 15 , O(C-Calkyl) claim 15 , OCF claim 15 , OCFH claim 15 , OCFH claim 15 , CN claim 15 , N claim 15 , NO claim 15 , NH claim 15 , NH(C-Calkyl) claim 15 , and N(C-Calkyl).26. The method according to claim 25 , wherein Ris selected from hydrogen claim 25 , halogen claim 25 , and CN.27. The method according to claim 15 , wherein Ris selected from hydrogen claim 15 , halogen claim 15 , C-Calkyl claim 15 , C-Chaloalkyl claim 15 , OH claim 15 , O(C-Calkyl) claim 15 , OCF claim 15 , OCFH claim 15 , OCFH claim 15 , CN claim 15 , NH claim 15 , NH(C-Calkyl) claim 15 , and N(C-Calkyl).28. The method according to claim 27 , wherein Ris selected from hydrogen claim 27 , halogen claim 27 , C-Calkyl claim 27 , OH claim 27 , and O(C-Calkyl).29. The method according to claim 15 , wherein Ris selected from hydrogen claim 15 , halogen claim 15 , C-Calkyl claim 15 , C-Chaloalkyl claim 15 , OH claim 15 , O(C-Calkyl) claim 15 , OCF claim 15 , OCFH claim 15 , OCFH claim 15 , CN claim 15 , NH claim 15 , NH(C-Calkyl) claim 15 , N(C-Calkyl) claim 15 , S(O)NRR claim 15 , C(O)NRR claim 15 , COR claim 15 , and COOR.30. The method according to claim 29 , wherein Ris selected from hydrogen claim 29 , halogen claim 29 , C-Calkyl claim 29 , C-Chaloalkyl claim 29 , OH claim 29 , O(C-Calkyl) claim 29 , CN claim 29 , S(O)NRR claim 29 , C(O)NRR claim 29 , COR claim 29 , and ...

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Номер записи: 100