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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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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 2580. Отображено 100.
22-03-2012 дата публикации

Compositions and Their Use as Anti-Tumor Agents

Номер: US20120071513A1
Автор: Charles Vacin, David Kanne, Diva Chan, Donald R. James, Gary Look, John Schullek, John Ward, Richard Gless, Tina Lee, X. Michael Wang
Принадлежит: COMPASS PHARMACEUTICALS LLC

The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.

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Номер записи: 1
21-06-2012 дата публикации

Nuclear receptor binding agents

Номер: US20120157539A1
Автор: Christina Barrett, Duane D. Miller, James T. Dalton, Michael L. Mohler, Ramesh Narayanan, Seoung-Soo Hong, Yali He, Zhongzhi Wu
Принадлежит: GTx Inc

The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.

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Номер записи: 2
11-10-2012 дата публикации

Preventing or ameliorating agent for pigmentation

Номер: US20120258063A1
Автор: Chihiro Kondo, Takashi Yamasaki, Yuko Saitoh
Принадлежит: Pola Chemical Industries Inc

An object is to provide an external preparation for skin preferably usable to prevent or ameliorate pigmentation. The object is achieved by providing a preventing or ameliorating agent for pigmentation, consisting of a compound represented by the following general formula (1), an isomer thereof, and/or a pharmacologically acceptable salt thereof, and an external preparation for skin containing the same as a component: [wherein R 1 represents an unsubstituted aromatic group or an aromatic group having any substituent; R 2 represents a hydrogen atom, a linear chain or branched chain alkyl group having a number of carbon atom or atoms of 1 to 4, or an acyl group having a linear or branched alkyl chain having a number of carbon atom or atoms of 1 to 4; and R 3 represents a hydrogen atom or a linear chain or branched chain alkyl group having a number of carbon atom or atoms of 1 to 4.]

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Номер записи: 3
13-06-2013 дата публикации

NOVEL SOLID FORMS OF TACEDINALINE

Номер: US20130150450A1
Автор: Holson Edward, Stahly G. Patrick, Wagner Florence F.
Принадлежит: THE BROAD INSTITUTE, INC.

Novel solid forms of tacedinaline (4-(acetylamino)-N-(2-aminophenyl)benzamide), including crystalline tacedinaline Forms A, B, and D, a novel crystalline tacedinaline TFA salt, and amorphous tacedinaline, are disclosed. Pharmaceutical compositions comprising crystalline tacedinaline Forms A, B, and D, the novel crystalline tacedinaline TFA salt, and/or amorphous tacedinaline, and methods of treating various conditions by administering those novel solid forms, are also disclosed. 14-. (canceled)5. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering 4-(acetylamino)-N-(2-aminophenyl)benzamide comprising crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject.6. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering a pharmaceutical composition comprising crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject.7. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering 0.001 mg/kg to 50 mg/kg per day of 4-(acetylamino)-N-(2-aminophenyl)benzamide comprising crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject , for at least two consecutive days.8. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering up to 0.4 mg/kg per day of 4-(acetylamino)-N-(2-aminophenyl)benzamide crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject , for up to 14 consecutive days.9. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising ...

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Номер записи: 4
18-07-2013 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20130184343A1
Автор: Jung Pierre, Lutz William, Maienfisch Peter, Pitterna Thomas, Renold Peter, Zambach Werner
Принадлежит:

A compound of formula (I): 2. A compound according to wherein Ais C—X—Ror C—R.3. A compound according to wherein Ais C—X—Ror C—R.4. A compound according to wherein Ais C—X—Ror C—R.5. A compound according to wherein Ais C—X—Ror C—R.6. A compound according to wherein one or two of A claim 1 , A claim 1 , Aand Aare C—X—R.7. A compound according to wherein Ris hydrogen claim 1 , methyl claim 1 , ethyl or acetyl.8. A compound according to wherein Ris hydrogen claim 1 , methyl claim 1 , ethyl or acetyl.9. A compound according to wherein Gis oxygen.10. A compound according to wherein Gis oxygen.11. A compound according to wherein each Ris independently hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , allyl claim 1 , phenyl or phenyl mono-substituted by halogen or methyl.12. A compound according to wherein each X is independently oxygen or sulfur.13. A compound according to wherein each Ris independently hydrogen or methyl.14. A compound according to wherein each Ris independently hydrogen claim 1 , fluoro claim 1 , methyl or trifluoromethyl.15. A compound according to any wherein Qis 5-bromo-furan-2-yl claim 1 , 2-bromo-phenyl claim 1 , 5-bromo-pyrid-3-yl claim 1 , 2-chloro-5-nitro-phenyl claim 1 , 2-chloro-phenyl claim 1 , 3-chloro-phenyl claim 1 , 2-chloro-pyrid-3-yl claim 1 , 2-chloro-pyrid-4-yl claim 1 , 6-chloro-pyrid-3-yl claim 1 , 5-chloro-thiophen-2-yl claim 1 , 3-chloro-5-trifluoromethyl-pyrid-2-yl claim 1 , 4-cyano-phenyl claim 1 , 2 claim 1 ,5-dichloro-phenyl claim 1 , 2 claim 1 ,3-difluoro-phenyl claim 1 , 1 claim 1 ,3-dimethyl-pyrazol-5-yl claim 1 , 4-fluoro-phenyl claim 1 , 2-fluoro-pyrid-3-yl claim 1 , 2-fluoro-3-trifluoromethyl-phenyl claim 1 , 2-methyl-phenyl claim 1 , 3-methyl-pyrid-2-yl claim 1 , 2-methylthio-pyrid-3-yl claim 1 , 4-nitro-phenyl claim 1 , phenyl claim 1 , 1 claim 1 ,2 claim 1 ,3-thiadiazol-4-yl and thiophen-2-yl.16. A compound according to wherein Qis a moiety of formula (II).17. A compound according to wherein Qis 2 ...

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Номер записи: 5
18-07-2013 дата публикации

OLIGO-BENZAMIDE COMPOUNDS FOR USE IN TREATING CANCERS

Номер: US20130184345A1
Автор: Ahn Jung-Mo, RAJ Ganesh, VADLAMUDI Ratna K.
Принадлежит: The Board of Regents of the University of Texas System

The present invention provides bis- and tris-benzamide compounds in the treatment of breast, brain and ovarian cancers. 2. The method of claim 1 , wherein X is —NO.3. The method of claim 1 , wherein Y is —C(O)NH4. The method of claim 2 , wherein A claim 2 , A′ and A″ are each O.5. The method of claim 2 , wherein R claim 2 , Rand Rare independently Calkyl claim 2 , Chydroxyalkyl claim 2 , or Calkenyl.6. The method of claim 4 , wherein R claim 4 , Rand Rare independently Calkyl claim 4 , Chydroxyalkyl claim 4 , or Calkenyl.7. The method of claim 2 , wherein R claim 2 , Rand Rare independently Calkyl or Chydroxyalkyl.8. The method of claim 4 , wherein R claim 4 , Rand Rare independently Calkyl or Chydroxyalkyl.9. The method of claim 1 , wherein Y is COOCH.10. The method of claim 1 , wherein A claim 1 , A′ and A″ are each NH.11. The method of claim 9 , wherein A claim 9 , A′ and A″ are each NH.12. The method of claim 9 , wherein R claim 9 , Rand Rare independently Calkyl claim 9 , Chydroxyalkyl claim 9 , or Calkenyl.13. The method of claim 11 , wherein R claim 11 , Rand Rare independently Calkyl or Chydroxyalkyl.14. The method of claim 1 , wherein X is —NOand Y is —C(O)NH15. The method of claim 14 , wherein A claim 14 , A′ and A″ are each O.16. The method of claim 14 , wherein R claim 14 , Rand Rare independently Calkyl claim 14 , Chydroxyalkyl claim 14 , or Calkenyl.17. The method of claim 15 , wherein R claim 15 , Rand Rare independently Calkyl claim 15 , Chydroxyalkyl claim 15 , or Calkenyl.18. The method of claim 14 , wherein R claim 14 , Rand Rare independently Calkyl or Chydroxyalkyl.19. The method of claim 15 , wherein R claim 15 , Rand Rare independently Calkyl or Chydroxyalkyl.21. The method of claim 1 , wherein the tumor cell is an androgen receptor (AR)-positive tumor cell.22. The method of claim 1 , wherein the tumor cell is an estrogen receptor (ER)-positive tumor cell.23. The method of claim 1 , tumor cell is a carcinoma cell.24. The method of claim 23 , ...

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Номер записи: 6
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: 7
15-08-2013 дата публикации

ANTIVIRAL COMPOUNDS

Номер: US20130210915A1
Автор: Andersson Emma, Edlund Karin, Elofsson Mikael, Mei Ya-Fang, Öberg Christopher, Strand Marten, Wadell Göran
Принадлежит:

The present invention provides new antiviral compounds and pharmacological compositions comprising these new compounds and their use in the prophylaxis, prevention and treatment of viral infections, particularly adenovirus and herpes virus infections. 18-. (canceled)9. A compound selected from:Ethyl 2-[3-(benzoylamino)benzoylamino]benzoate2-[[3-(Benzoylamino)benzoyl]amino]benzoic acidEthyl 2-[4-(benzoylamino)benzoylamino]benzoate2-[2-(Acetylamino)benzoylamino]benzoic acid2-[2-(Trimethylacetylamino)benzoylamino]benzoic acid2-[[2-(Cyclohexanecarboxylamino)benzoyl]amino]benzoic acid2-[2-(4-Carboxybutanoylamido)benzoyl]aminobenzoic acid2-[2-(Benzylamino)benzoylamino]benzoic acid2-[2-(2-Fluorobenzoylamino)-benzoylamino]benzoic acid2-[2-(3-Fluorobenzoylamino)-benzoylamino]benzoic acid2-[2-(4-Fluorobenzoylamino)-benzoylamino]benzoic acidEthyl 2-[2-(benzoylamino)benzoylamino]benzoateEthyl 2-[2-(acetylamino)benzoylamino]benzoateEthyl 2-[2-(trimethylacetylamino)benzoylamino]benzoateEthyl 2-[[2-(cyclohexanecarboxylamino)benzoyl]amino]benzoateEthyl 2-[2-(phenylacetylamino)benzoylamino]benzoateEthyl 2-[2-(4-carboxybutanoylamido)benzoyl]aminobenzoateEthyl 2-[[2-(benzylamino)benzoyl]amino]benzoate2-[[2-(Benzoylamino)benzoyl]amino]benzoic acid2-[2-(Acetylamino)benzoylamino]benzoic acid2-[2-(Trimethylacetylamino)benzoylamino]benzoic acid2-[[2-(Cyclohexanecarboxylamino)benzoyl]amino]benzoic acid2-[2-(Phenylacetylamino)benzoylamino]benzoic acid2-[2-(4-Carboxybutanoylamido)benzoyl]aminobenzoic acid2-[2-(Benzylamino)benzoylamino]benzoic acid2-[2-(benzoylamino)benzoylamino]phenylacetic acid2-[2-(benzoylamino)phenylacetylamino]benzoic acid2-[2-(2-fluorobenzoylamino)-benzoylamino]-4-chlorobenzoic acid2-[2-(2-fluorobenzoylamino)benzoylamino]-5-chlorobenzoic acid2-[2-(2-fluorobenzoylamino)-benzoylamino]-4-methoxybenzoic acid2-[2-(2-fluorobenzoylamino)-benzoylamino]-5-methoxybenzoic acid2-[2-(2-fluorobenzoylamino)-benzoylamino]-4,5-difluorobenzoic acid2-[4-chloro-2-(2-fluorobenzoylamino)- ...

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Номер записи: 8
05-09-2013 дата публикации

AMIDE DERIVATIVE, PEST CONTROL AGENT CONTAINING THE AMIDE DERIVATIVE, AND USE OF THE AMIDE DERIVATIVE

Номер: US20130231392A1
Автор: Aoki Yoji, Daido Hidenori, Fukazawa Yasuaki, Hirabayashi Atsushi, Hirose Mai, Katsuta Hiroyuki, KAWAHARA Atsuko, Kobayashi Yumi, Nomura Michikazu, Takahashi Yusuke, TSUKADA Hidetaka
Принадлежит: MITSUI CHEMICALS ARGO, INC.

An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action. 4. The pest control agent according to claim 3 , wherein in Formula (8) claim 3 , Yrepresents a C3-C4 perfluoroalkyl group.5. The pest control agent according to claim 4 , wherein in Formula (8) claim 4 , Yand Yeach independently represent a chlorine atom claim 4 , a bromine atom claim 4 , an iodine atom claim 4 , a trifluoromethoxy group claim 4 , a trifluoromethyl group claim 4 , or a pentafluoroethyl group claim 4 , and Yand Yrepresent hydrogen atoms.6. The pest control agent according to claim 5 , wherein in Formula (8) claim 5 , Xand Xeach independently represent a hydrogen atom or a fluorine atom claim 5 , and Xand Xrepresent hydrogen atoms.7. The pest control agent according to claim 6 , wherein in Formula (8) claim 6 , Rand Reach independently represent a hydrogen atom or a methyl group.8. The pest control agent according to claim 7 , wherein in Formula (8) claim 7 , Qrepresents a phenyl group or a pyridyl group which may have a substituent selected from a group consisting of a halogen atom claim 7 , a C1 haloalkyl group claim 7 , a nitro group claim 7 , and a cyano group.9. The pest control agent according to claim 8 , wherein in Formula (8) claim 8 , the number of the substituents in Qis 1 or 2.10. The pest control agent according to claim 2 , wherein in Formula (7) claim 2 , Yrepresents a C2-C4 perfluoroalkyl group claim 2 , Yand Yrepresent hydrogen atoms claim 2 , Yand Yeach represent a halogen atom or a C1-C3 haloalkyl group claim 2 , and either Yor Yrepresents a C1-C3 haloalkyl group.11. The pest control agent according to claim 10 , wherein in Formula (7) claim 10 , Xto Xeach independently represent a hydrogen atom claim 10 , a halogen atom claim 10 , or a cyano group.13. The pest control agent according to claim 12 , wherein in Formula (9) claim 12 , Yrepresents a C2-C4 perfluoroalkyl ...

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Номер записи: 9
03-10-2013 дата публикации

GENETICALLY ENCODED INITIATOR FOR POLYMER GROWTH FROM PROTEINS

Номер: US20130261259A1
Автор: Averick Saadyah, MATYJASZEWSKI KRZYSZTOF, MEHL RYAN A.
Принадлежит: FRANKLIN AND MARSHALL COLLEGE

This invention pertains to methods for producing homogeneous recombinant proteins that contain polymer initiators at defined sites. The unnatural amino acid, 4-(2′-bromoisobutyramido)phenylalanine of formula 1, was designed and synthesized as a molecule comprising a functional group further comprising an initiator for an atom-transfer radical polymerization (‘ATRP”) that additionally would provide a stable linkage between the protein and growing polymer. We evolved a (Mj) tyrosyl-tRNA synthetase/tRNApair to genetically encode this unnatural amino acid in response to an amber codon. To demonstrate the utility of this functional amino acid, we produced Green Fluorescent Protein with the unnatural amino acid initiator of formula 1 site-specifically incorporated on its surface (GFP-1). Purified GFP-1 was then used as an initiator under standard ATRP conditions with oligo(ethylene oxide)monomethyl ether methacrylate, efficiently producing a polymer-GFP bioconjugate wherein the polymer is connected at a specifically selected site on GFP. 2. The compound of claim 1 , as described by formula 6 claim 1 , wherein R1 and R2 are independently H claim 1 , methyl claim 1 , or phenyl; X is F claim 1 , Cl claim 1 , Br claim 1 , I; or N; A is O claim 1 , S claim 1 , or NR claim 1 , wherein R is H claim 1 , methyl claim 1 , or phenyl; n is 1; or a salt thereof.6. The compound of claim 1 , wherein R1 and R2 are independently H claim 1 , methyl claim 1 , or phenyl; X is F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , or N; A is O claim 1 , S claim 1 , or NR claim 1 , wherein R is H claim 1 , methyl claim 1 , or phenyl; n is 0; or a salt thereof.14. The method of claim 13 , wherein R1 and R2 are independently H claim 13 , methyl claim 13 , or phenyl; X is F claim 13 , Cl claim 13 , Br claim 13 , I claim 13 , or N; Y is F claim 13 , Cl claim 13 , Br claim 13 , I claim 13 , or trifluoroacetate; A is O claim 13 , S claim 13 , or NR claim 13 , wherein R is H claim 13 , methyl claim 13 , ...

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Номер записи: 10
31-10-2013 дата публикации

INHIBITORS OF ALPHA4 MEDIATED CELL ADHESION

Номер: US20130289109A1
Автор: Kawaguchi Takayuki, KUME Toshiyuki, NOMURA Sumihiro, SIRCAR Ila, TSUKIMOTO Mikiko
Принадлежит:

The present invention relates to a phenylalanine derivative of Formula (I) wherein Xis a halogen atom, Xis a halogen atom, Q is a CHR— is a carboxyl group which may be esterified; or a pharmaceutically acceptable salt thereof. 2. The method according to claim 1 , wherein said condition is allergic condition or rejection after transplantation.3. The method according to claim 2 , wherein allergic condition is rhinitis.5. The method according to claim 4 , wherein Xis chlorine atom or fluorine atom claim 4 , Xis chlorine atom or fluorine atom claim 4 , and Y is a Calkyl group.6. The method according to claim 5 , wherein Xis chlorine atom or fluorine atom claim 5 , Xis chlorine atom or fluorine atom claim 5 , Q is a —CH— group claim 5 , Y is methyl group claim 5 , ethyl group claim 5 , or n-propyl group claim 5 , and COR is a carboxyl group claim 5 , methoxycarbonyl group claim 5 , ethoxycarbonyl group or tert-butoxycarbonyl group.7. The method according to claim 5 , wherein Xis fluorine atom claim 5 , Xis chlorine atom or fluorine atom claim 5 , Q is a —CH— group claim 5 , and Y is methyl group or ethyl group.8. The method according to claim 1 , wherein the compound is selected from the group consisting of N-(2 claim 1 ,6-difluorobenzoyl)-4-(2 claim 1 ,6-dimethoxy-4-ethoxymethylphenyl)-L-phenylalanine claim 1 , N-(2-chloro-6-fluorobenzoyl)-4-(2 claim 1 ,6-dimethoxy-4-ethoxymethylphenyl)-L-phenylalanine claim 1 , N-(2-chloro-6-fluorobenzoyl)-4-(2 claim 1 ,6-dimethoxy-4-methoxymethylphenyl)-L-phenylalanine claim 1 , and N-(2 claim 1 ,6-difluorobenzoyl)-4-(2 claim 1 ,6-dimethoxy-4-methoxymethylphenyl)-L-phenylalanine.9. The method according to claim 1 , wherein the compound is N-(2 claim 1 ,6-difluorobenzoyl)-4-(2 claim 1 ,6-dimethoxy-4-ethoxymethylphenyl)-L-phenylalanine. This application is a Divisional of co-pending application Ser. No. 12/962,707, filed Dec. 8, 2010, which is a Divisional of application Ser. No. 12/683,648, filed Jan. 7, 2010, which issued as U.S. Pat. ...

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Номер записи: 11
21-11-2013 дата публикации

Amide derivative, pest control agent containing the amide derivative, and use of the amide derivative

Номер: US20130310459A1
Автор: Atsuko Kawahara, Atsushi Hirabayashi, Hidenori Daido, Hidetaka Tsukada, Hiroyuki Katsuta, Mai Hirose, Michikazu Nomura, Yasuaki FUKAZAWA, Yoji Aoki, Yumi Kobayashi, Yusuke Takahashi
Принадлежит: Mitsui Chemicals Agro Inc

An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action. In the following Formula (1), A represents a carbon atom, a nitrogen atom, or the like, and K represents a non-metal atomic group necessary for forming a cyclic linking group derived from benzene or a heterocyclic. X represents a halogen atom or the like; n represents an integer of from 0 to 4. R 1 and R 2 represent hydrogen atoms, alkyl groups, or the like. T represents —C(=G 1 )-Q 1 or —C(=G 1 )-G 2 Q 2 , and G 1 to G 3 each represent oxygen atoms or the like. Q 1 and Q 2 each represent a hydrogen atom, an alkyl group, an aryl group, or the like. Y 1 and Y 5 each represent a halogen atom or the like, Y 2 and Y 4 each represent a hydrogen atom or the like, and Y 3 represents a C2-C5 haloalkyl group.

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Номер записи: 12
12-12-2013 дата публикации

COMPOUNDS AND METHODS FOR TREATING DISEASES MEDIATED BY PROTEASE ACTIVATED RECEPTORS

Номер: US20130331411A1
Автор: Dockendorff Chris, Flaumenhaft Robert, MacPherson Lawrence
Принадлежит:

The invention relates to the use of a compound of Formula I for the treatment of protease-activated receptor mediated diseases by the administration of a compound of Formula I or a prodrug or metabolite thereof. 12-. (canceled)46-. (canceled)821-. (canceled)26. The method of claim 22 , wherein the patient is in need of inhibition of platelet activation.27. The method of claim 22 , wherein the patient is in need of inhibition of thrombus formation.28. The method of claim 22 , wherein the PAR1 disease is particular proliferative diseases of endothelial cells claim 22 , fibroblasts claim 22 , nephrocytes claim 22 , osteosarcoma cells claim 22 , muscle cells claim 22 , cancer cells and/or glia cells.2930-. (canceled)31. The method of claim 22 , wherein said PAR1 mediated disease is selected from acute Myocardial Infarction claim 22 , stable angina claim 22 , unstable angina claim 22 , aortocoronary bypass surgery claim 22 , acute occlusion following coronary angioplasty and or stent placement claim 22 , transient Ischemic attacks claim 22 , cerebrovascular disease claim 22 , peripheral vascular disease claim 22 , placental insufficiency claim 22 , prosthetic heart valves claim 22 , atrial fibrillation claim 22 , anticoagulation of tubing.32. (canceled)33. The method of claim 22 , wherein said disease or disorder is selected from acute myocardial infarction claim 22 , stable angina claim 22 , unstable angina claim 22 , transient ischemic attack claim 22 , cerebrovascular disease claim 22 , peripheral vascular disease claim 22 , placental insufficiency claim 22 , thrombosis subsequent to or associated with a surgical procedure claim 22 , thrombosis associated with atrial fibrillation claim 22 , and inflammation.3436-. (canceled)37. The method of claim 22 , wherein Cyl and Gare aromatic groups and Gis an alkyl group.38. The method of claim 22 , wherein each Gand Gis a group containing at least two carbons independently selected from aliphatic claim 22 , substituted ...

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Номер записи: 13
12-12-2013 дата публикации

Proteasome Inhibitors

Номер: US20130331595A1
Автор: Danca Mihaela Diana, Olhava Edward J.
Принадлежит: Millennium Pharmaceuticals, Inc.

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The process of claim 1 , wherein the reaction of step (1) is conducted in the presence of a peptide coupling reagent.3. The process of claim 2 , wherein the peptide coupling reagent is selected from the group consisting of a carbodiimide reagent claim 2 , phosphonium reagent claim 2 , and uranium reagent.4. The process of claim 3 , wherein the peptide coupling reagent is selected from one or more of the group consisting of dicyclohexylcarbodiimide (DCC) claim 3 , 1-(3-dimethylaminopropyl-3-ethylcarbodiimide (EDC) claim 3 , benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) claim 3 , O-(1H-benzotriazol-1-yl)-N claim 3 ,N claim 3 ,N′N′-tetramethyluronium tetrafluoroborate (TBTU) and N-Hydroxybenzotriazole (HOBt).5. The process of claim 1 , wherein the reaction of step (3) is conducted in the presence of a peptide coupling reagent.6. The process of claim 5 , wherein the peptide coupling reagent is selected from the group consisting of a carbodiimide reagent claim 5 , phosphonium reagent claim 5 , and uranium reagent.7. The process of claim 6 , wherein the peptide coupling reagent is selected from one or more of the group consisting of dicyclohexylcarbodiimide (DCC) claim 6 , 1-(3-dimethylaminopropyl-3-ethylcarbodiimide (EDC) claim 6 , benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) claim 6 , O-(1H-benzotriazol-1-yl)-N claim 6 ,N claim 6 ,N′N′-tetramethyluronium tetrafluoroborate (TBTU) and N-Hydroxybenzotriazole (HOBt).8. The process of claim 1 , wherein the reaction of step (1) is conducted in the presence of a solvent comprising a polar aprotic solvent.9. The process of claim 8 , wherein the polar aprotic solvent is selected from one or more of the group ...

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Номер записи: 14
09-01-2014 дата публикации

POLYMERIZABLE MONOMER, POLYMERIC COMPOUND, CHARGE CONTROL AGENT CONTAINING THE POLYMERIC COMPOUND, AND DEVELOPER BEARING MEMBER AND TONER WHICH CONTAIN THE CHARGE CONTROL AGENT

Номер: US20140011129A1
Автор: Hirose Masashi, Inoue Kei, Murai Yasuaki, Murayama Ryuji, Sato Kazuyuki
Принадлежит: CANON KABUSHIKI KAISHA

A polymerizable monomer is provided which is represented by the following formula (1): 4. The polymeric compound according to claim 3 , wherein the unit represented by the formula (4) is a styrene derivative unit or an acrylate derivative unit.5. The polymeric compound according to claim 2 , which has a weight-average molecular weight of from 3 claim 2 ,000 to 100 claim 2 ,000.6. A charge control agent comprising the polymeric compound according to .7. A developer bearing member comprising in a surface layer thereof the charge control agent according to .8. A toner comprising a binder resin claim 6 , a colorant and the charge control agent according to .9. The toner according to claim 8 , which is produced by a suspension polymerization process.10. The toner according to claim 8 , which is produced by a suspension granulation process. The present invention relates to a novel polymerizable monomer having a salicylic acid unit, and a polymeric compound produced by polymerizing the same. The present invention also relates to a charge control agent used in recording methods making use of electrophotography or the like, and a developer bearing member and a toner which contain the same.In image forming methods as typified by an electrophotographic recording method, a developer charged electrostatically (hereinafter “toner”) flies to the surface of a photosensitive member by electrostatic force which accords with potential differences on the photosensitive member surface, and develops electrostatic latent images formed on the photosensitive member surface. Hence, it is necessary and indispensable to control charge characteristics of the toner. Then, as a method for providing the toner with proper charge characteristics, a method is known in which a binder resin of a developer bearing member (hereinafter also “developing roller”) is incorporated with a charge control agent or a method in which a charge control agent capable of providing the toner with positive charges or ...

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Номер записи: 15
06-02-2014 дата публикации

COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES

Номер: US20140039009A1
Автор: Chen Shoujun, Jiang Jun, Sun Lijun, Xia Zhiqiang, Xie Yu, Zhang Junyi
Принадлежит: Synta Pharmaceuticals Corp.

The invention relates to compounds of structural formulas (I), (VII) and (XI): 2. The compound of claim 1 , wherein L is —NR—C(O)—.37-. (canceled)910-. (canceled)11. The compound of claim 8 , wherein L is —NHC(O)—.1219-. (canceled)2127-. (canceled)29. The compound of claim 28 , wherein Rand Rare each claim 28 , independently claim 28 , a halo.30. The compound of claim 29 , wherein Ris a lower alkyl claim 29 , a lower alkoxy claim 29 , a lower alkyl sulfanyl claim 29 , a lower alkylamino claim 29 , a lower dialkylamino claim 29 , or a halo.31. The compound of claim 30 , Ris a bioisostere of an ester claim 30 , amide claim 30 , or carboxylic acid.32. The compound of claim 31 , wherein Ris a 5-membered heteroaryl.33. The compound of claim 32 , wherein Ris an optionally substituted oxazolyl claim 32 , an optionally substituted thiazolyl claim 32 , an optionally substituted 1H-tetrazolyl claim 32 , an optionally substituted 1H-imidazolyl claim 32 , an optionally substituted [1 claim 32 ,2 claim 32 ,4]oxadiazolyl claim 32 , or an optionally substituted 4H-[1 claim 32 ,2 claim 32 ,4]-triazolyl.34. The compound of claim 30 , wherein Ris a halo claim 30 , —C(O)R claim 30 , —S(O)R claim 30 , —S(O)NR claim 30 , —S(O)OR claim 30 , —P(O)(OR) claim 30 , or —P(O)(R) claim 30 , wherein:{'sub': '9', 'Ris a lower alkoxy, lower alkyl sulfanyl, or an alkoxyalkoxy;'}{'sub': '11', 'R, for each occurrence, is independently, a lower alkyl; and'}{'sub': '12', 'R, for each occurrence, is independently, H or a lower alkyl.'}35. The compound of claim 30 , wherein Rand Rare each a fluoro group.3744-. (canceled)46. The compound of claim 45 , wherein L is —NR—C(O)—.4751-. (canceled)5354-. (canceled)55. The compound of claim 52 , wherein L is —NHC(O)—.57115-. (canceled)116. A pharmaceutical composition claim 1 , comprising a pharmaceutically acceptable carrier and a compound of and optionally further comprising one or more additional therapeutic agents.117119-. (canceled)120. A pharmaceutical ...

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Номер записи: 16
02-01-2020 дата публикации

Boronate ester compounds and pharmaceutical compositions thereof

Номер: US20200002361A1
Автор: Abu J. Ferdous, Csanad M. Varga, Debra L. Mazaik, Eric L. Elliott, Michael J. Kaufman, Nobel T. Truong, Peter N. Zawaneh, Phuong M. Nguyen, Quentin J. Mccubbin, Raymond D. Skwierczynski, Sonja A. Komar-Lay, Vaithianathan Palaniappan
Принадлежит: Millennium Pharmaceuticals Inc

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

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Номер записи: 17
04-01-2018 дата публикации

BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

Номер: US20180002350A1
Автор: Elliott Eric L., Ferdous Abu J., Kaufman Michael J., Komar-Lay Sonja A., Mazaik Debra L., Mccubbin Quentin J., Nguyen Phuong M., Palaniappan Vaithianathan, Skwierczynski Raymond D., Truong Nobel T., Varga Csanad M., Zawaneh Peter N.
Принадлежит:

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The process of claim 1 , wherein the reaction of step (1) or step (3) or both is conducted in the presence of a peptide coupling reagent.3. The process of claim 2 , wherein the peptide coupling reagent is selected from the group consisting of a carbodiimide reagent claim 2 , phosphonium reagent claim 2 , and uronium reagent.4. The process of claim 3 , wherein the peptide coupling reagent is selected from one or more of the group consisting of dicyclohexylcarbodiimide (DCC) claim 3 , 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC) claim 3 , benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) claim 3 , and O-(1H-benzotriazol-1-yl)-N claim 3 ,N claim 3 ,N′ claim 3 ,N′-tetramethyluronium tetrafluoroborate (TBTU).5. The process of claim 1 , further comprising converting the carboxylic acid moiety of compound (i) to an activated ester or acid halide prior to the reaction of step (1).6. The process of claim 5 , wherein said activated ester or acid halide is an O—(N-hydroxysuccinimide) ester.7. The process of claim 1 , wherein the reaction of step (3) is conducted in the presence of a solvent.8. The process of claim 7 , wherein the solvent is tetrahydrofuran.9. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an aqueous mineral acid.10. The process of claim 9 , wherein the mineral acid is hydrochloric acid.11. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an organic boronic acid acceptor.12. The process of claim 11 , wherein the organic boronic acid acceptor is i-BuB(OH).13. The process of claim 1 , wherein the reaction of step (5) is conducted in the presence of a solvent selected from the group consisting of ...

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Номер записи: 18
13-01-2022 дата публикации

BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

Номер: US20220009948A1
Автор: Elliott Eric L., Ferdous Abu J., Kaufman Michael J., Komar-Lay Sonja A., Mazaik Debra L., Mccubbin Quentin J., Nguyen Phuong M., Palaniappan Vaithianathan, Skwierczynski Raymond D., Truong Nobel T., Varga Csanad M., Zawaneh Peter N.
Принадлежит:

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The process of claim 1 , wherein the reaction of step (1) or step (3) or both is conducted in the presence of a peptide coupling reagent.3. The process of claim 2 , wherein the peptide coupling reagent is selected from the group consisting of a carbodiimide reagent claim 2 , phosphonium reagent claim 2 , and uronium reagent.4. The process of claim 3 , wherein the peptide coupling reagent is selected from one or more of the group consisting of dicyclohexylcarbodiimide (DCC) claim 3 , l-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC) claim 3 , benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) claim 3 , and O-(1H-benzotriazol-1-yl)-N claim 3 , N claim 3 , N′N′-tetramethyluronium tetrafluoroborate (TBTU).5. The process of claim 1 , further comprising converting the carboxylic acid moiety of compound (ii) to an activated ester or acid halide prior to the reaction of step (1).6. The process of claim 5 , wherein said activated ester or acid halide is an O—(N-hydroxysuccinnimide) ester.7. The process of claim 1 , wherein the reaction of step (3) is conducted in the presence of a solvent.8. The process of claim 7 , wherein the solvent is tetrahydrofuran.9. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an aqueous mineral acid.10. The process of claim 9 , wherein the mineral acid is hydrochloric acid.11. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an organic boronic acid acceptor.12. The process of claim 11 , wherein the organic boronic acid acceptor is t-BuB(OH).13. The process of claim 1 , wherein the reaction of step (5) is conducted in the presence of a solvent selected from the group consisting of ethyl ...

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Номер записи: 19
14-01-2021 дата публикации

COMPOUND FOR MODULATING DDAH AND ADMA LEVELS, AS WELL AS METHODS OF USING THEREOF TO TREAT DISEASE

Номер: US20210009498A1
Автор: FOWLER Kerry, Singh Jaipal
Принадлежит:

Disclosed are compounds that can modulate DDAH and the amount of asymmetric dimethylarginine (ADMA) in a subject. Also provided are pharmaceutical compositions comprising these compounds, as well as methods of using these compositions to treat and/or prevent diseases associated with elevated or low levels of DDAH and ADMA. 2. The method of claim 1 , wherein Y is a substituted or unsubstituted aryl ring claim 1 , optionally wherein Y is selected from an oxazole ring claim 1 , a pyridinyl ring claim 1 , a thiazole ring claim 1 , and a thiophene ring.5. The method of claim 4 , wherein Xand Xarei) both CH;{'sub': '2', 'ii) independently O or CHor'}iii) together with the bond to which they are attached form a 3-membered carbocyclic ring.7. The method of claim 1 , wherein Xand Xtogether with the bond to which they are attached forms a 3-membered carbocyclic ring.8. (canceled)9. The method of wherein said composition is administered for treating or preventing a disease or condition associated with elevated levels of asymmetric dimethylarginine (ADMA) in a subject.10. The method of claim 9 , wherein the risk factors claim 9 , disease or condition includes hypertension claim 9 , heart failure claim 9 , pulmonary arterial hypertension claim 9 , erectile dysfunction claim 9 , coronary and peripheral arterial disease claim 9 , renal disease claim 9 , insulin resistance claim 9 , diabetes claim 9 , atrial fibrillation claim 9 , sickle cell disease claim 9 , organ damage claim 9 , sepsis claim 9 , renal failure claim 9 , endothelial dysfunction claim 9 , vascular disease claim 9 , or a combination thereof.11. The method of wherein said composition is administered for reducing fibrosis in a cell or tissue.1213-. (canceled)14. The method of claim 11 , wherein the fibrosis is associated with a fibrotic condition of the lung claim 11 , a fibrotic condition of the liver claim 11 , a fibrotic condition of the heart or vasculature claim 11 , a fibrotic condition of the kidney claim 11 , ...

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Номер записи: 20
03-02-2022 дата публикации

DP ANTAGONIST

Номер: US20220033371A1
Автор: ASADA Masaki, Hanada Keisuke, HIGUCHI Satonori, NAGANAWA Atsushi, Takeda Yasuhiro
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

An object of the present invention is to provide a DP receptor antagonist. A compound represented by general formula (I): 117-. (canceled)18. {4-Chloro-3-[(2 ,6-dimethyl-4-{2-[(2R)-oxan-2-yl]ethoxy}benzene-1-carbothioyl)amino]phenyl}acetic acid , or a pharmaceutically acceptable salt thereof. This patent application claims priority with respect to Japanese Patent Application No. 2018-175758, and the entire content of which is incorporated by reference herein.The present invention relates to a compound having DP receptor antagonistic activity, a pharmaceutically acceptable salt thereof, and a medicament containing them as an active ingredient. For details, a compound represented by general formula (I)(wherein all symbols have the same meanings as described below), or a pharmaceutically acceptable salt thereof (hereinafter referred to as the compound of the present invention), and a medicament containing them as active ingredients.Prostaglandin D2 (abbreviated as PGD2) is known as a metabolite of arachidonic acid cascade and is known to be involved in allergic diseases, sleep, hormone secretion, pain, platelet aggregation, glycogen metabolism, intraocular pressure regulation, and the like (Non Patent Literatures 1 to 11). It is known that DP receptors and CRTH2 receptors are present as PGD2 receptors, and it is known that, among which DP receptors that are present in the brain, especially in a subarachnoid space in a ventral region of the rostral basal forebrain, are related to a sleep-inducing action of PGD2 (Non Patent Literature 12). That is, in order to inhibit the sleep-inducing action of PGD2 and to be used as a therapeutic drug for sleep-wake disorders, it is necessary to have a drug having not only DP antagonistic activity but also transferability to the central nervous system.On the other hand, Patent Literature 1 describes that a compound represented by the following general formula (A) that specifically binds to and antagonizes the DP receptor.wherein ...

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Номер записи: 21
17-01-2019 дата публикации

TRIFLUOROMETHOXYLATION OF ARENES VIA INTRAMOLECULAR TRIFLUOROMETHOXY GROUP MIGRATION

Номер: US20190016670A1
Автор: Hojczyk Katarzyna N., Ngai Ming-Yu
Принадлежит: The Research Foundation for The State University of New York

The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure: 19-. (canceled)11. The process of claim 10 , wherein the second suitable solvent is chloroform claim 10 , dichloromethane claim 10 , nitromethane claim 10 , dimethylforamide claim 10 , diethyl ether claim 10 , tetrahydrofuran claim 10 , dioxane claim 10 , dichloroethane claim 10 , or hexane.12. The process of claim 10 , wherein step (b) is carried out at room temperature.13. The process of claim 10 , wherein step (b) is carried out at a temperature of 50-140° C.14. The process of claim 10 , wherein the compound is maintained in the second suitable solvent for 10-50 hours.15. The process of claim 10 , wherein A is a phenyl or pyridine.16. The process of claim 10 , wherein A is a furan claim 10 , thiophene claim 10 , pyrrole claim 10 , thiazole claim 10 , imidazole claim 10 , pyrazole claim 10 , isooxazole claim 10 , isothiazole claim 10 , naphthalene claim 10 , anthracene claim 10 , pyrimidine claim 10 , pyrazine claim 10 , pyridazine claim 10 , indole claim 10 , indoline claim 10 , benzofuran claim 10 , benzothiophene claim 10 , or quinolone.2037-. (canceled) This application claims priority of U.S. Provisional Application Nos. 62/192,789, filed Jul. 15, 2015; 62/192,462, filed Jul. 14, 2015; 62/063,246, filed Oct. 13, 2014; and 62/062,508, filed Oct. 10, 2014, the contents of each of which are hereby incorporated by reference.Throughout this application various publications are referenced. The disclosures of these documents in their entireties are hereby incorporated by reference into this application in order to more fully describe the state of the art to which this invention pertains.Fluorine atoms are often introduced into organic molecules to enhance their pharmacological properties such as solubility, metabolic and oxidative stability, lipophilicity, and bioavailability. Among the fluorine containing functional groups, ...

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Номер записи: 22
28-01-2016 дата публикации

PPAR AGONISTS

Номер: US20160023991A1
Автор: Baiga Thomas J., BOCK Mark G., Downes Michael, Embler Emi Kanakubo, Evans Ronald M., Fan Weiwei, Keana John F.W., Kluge Arthur F., Noel Joseph P., Patane Mike A.
Принадлежит:

Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases). 2. The compound of claim 1 , wherein ring B is selected from phenyl claim 1 , pyridine claim 1 , thiophene claim 1 , thiazole claim 1 , pyrazole claim 1 , oxazole claim 1 , isoxazole claim 1 , benzo[b]furan claim 1 , indazole claim 1 , piperidine claim 1 , cyclohexane claim 1 , piperidin-2-one claim 1 , piperazine-2 claim 1 ,5-dione or quinazolin-4(3H)-one.6. The compound of claim 1 , wherein:{'sup': '3', 'Ris selected from aliphatic or alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and/or'}{'sup': 2', '3', '4, 'L, Land Lare each independently selected from a bond or alkylene.'}7. The compound of claim 1 , wherein LRis isopropyl.8. The compound of claim 1 , wherein Ris furan-2-yl or furan-3-yl.11. The compound of claim 1 , wherein the compound is selected from6-(2-((N-isopropyl-[1,1′-biphenyl]-4-carboxamido)methyl)phenoxy)hexanoic acid;ethyl 6-(2-(1-(4-bromo-N-cyclopropylbenzamido)-2-(tert-butylamino)-2-oxoethyl)phenoxy)hexanoate;ethyl 6-(2-(2-(tert-butylamino)-1-(N-cyclopropyl-[1,1′-biphenyl]-4-carboxamido)-2-oxoethyl)phenoxy)hexanoate;ethyl 6-(2-(2-amino-1-(N-cyclopropyl-[1,1′-biphenyl]-4-carboxamido)-2-oxoethyl)phenoxy)hexanoate;6-(2-(2-amino-1-(N-cyclopropyl-[1,1′-biphenyl]-4-carboxamido)-2-oxoethyl)phenoxy)hexanoic acid;6-(2-(2-(tert-butylamino)-1-(N-cyclopropyl-[1,1′-biphenyl]-4-carboxamido)-2-oxoethyl)phenoxy)hexanoic acid;6-(2-((N-cyclopropyl-[1,1′-biphenyl]-4-carboxamido)methyl)phenoxy)hexanoic acid;N-(2-amino-1-(2-((6-(hydroxyamino)-6-oxohexyl)oxy)phenyl)-2-oxoethyl)-N-cyclopropyl-[1,1′-biphenyl]-4-carboxamide;6-(2-((N-cyclopropyl-4-(pyridin-4-yl)benzamido)methyl)phenoxy)hexanoic acid;6-(2-((N-cyclopropyl-4-(pyridin-3-yl)benzamido)methyl)phenoxy)hexanoic acid;6 ...

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Номер записи: 23
26-01-2017 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20170022148A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

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Номер записи: 24
26-01-2017 дата публикации

FUMARATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE

Номер: US20170022149A1
Автор: Nguyen Mark Quang
Принадлежит:

Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed. 2. The compound according to claim 1 , wherein Ris chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , and isopropyl.3. The compound according to claim 1 , wherein Ris chosen from methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl claim 1 , tert-butyl claim 1 , n-pentyl claim 1 , n-hexyl claim 1 , cyclohexyl claim 1 , cyclohexylmethyl claim 1 , phenyl claim 1 , benzyl claim 1 , substituted methyl claim 1 , substituted ethyl claim 1 , substituted n-propyl claim 1 , substituted isopropyl claim 1 , substituted n-butyl claim 1 , substituted isobutyl claim 1 , substituted tert-butyl claim 1 , substituted n-pentyl claim 1 , and substituted n-hexyl.4. The compound according to claim 1 , wherein Ris chosen from methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl claim 1 , tert-butyl claim 1 , n-pentyl claim 1 , n-hexyl claim 1 , cyclohexyl claim 1 , cyclohexylmethyl claim 1 , phenyl claim 1 , and benzyl.5. The compound according to claim 1 , wherein Xis chosen from methane-diyl claim 1 , ethane-1 claim 1 ,2-diyl claim 1 , propane-1 claim 1 ,3-diyl claim 1 , substituted methane-diyl claim 1 , substituted ethane-1 claim 1 ,2-diyl claim 1 , and substituted propane-1 claim 1 ,3-diyl.6. The compound according to claim 1 , wherein Xis chosen from methane-diyl claim 1 , ethane-1 claim 1 ,1-diyl claim 1 , ethane-1 claim 1 ,2-diyl claim 1 , 2-phenylethane-1 claim 1 ,2-diyl claim 1 , propane-1 claim 1 ,2- ...

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Номер записи: 25
23-01-2020 дата публикации

ANTHRACENE DERIVATIVES CONTAINING BENZIMIDAZOLE OR BORATE AND ORGANOELECTROLUMINESCENT DEVICE INCLUDING THE SAME

Номер: US20200028088A1
Автор: CHANG Chiou-Ling, CHIU Tien-Lung, FAN Bo-An, HOU Liang-Ju, LEE Jiun-Haw, LEUNG Man-Kit, Lin Chi-Feng
Принадлежит:

An organic light-emitting diode comprises a first electrode layer, a second electrode layer, and an organic luminescent unit disposed between the first electrode layer and the second electrode layer. The organic luminescent unit has an organic electroluminescent material containing anthracene group as shown in General Formula (1): 2. The organic light-emitting diode according to claim 1 , wherein the alkyl group is selected from the group consisting of a substituted or unsubstituted straight-chain C1˜C6 alkyl group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 alkyl group claim 1 , the cycloalkyl group is a substituted or unsubstituted C3˜C6 cycloalkyl group claim 1 , the alkoxy group is selected from the group consisting of a substituted or unsubstituted straight-chain C1˜C6 alkoxy group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 alkoxy group claim 1 , the haloalkyl group is selected from the group consisting of a substituted or unsubstituted straight-chain C1˜C6 haloalkyl group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 haloalkyl group claim 1 , the thioalkyl group is selected from the group consisting of a substituted or unsubstituted straight-chain C1˜C6 thioalkyl group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 thioalkyl group claim 1 , the silyl group is selected from the group consisting of a substituted or unsubstituted straight-chain C1˜C6 silyl group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 silyl group claim 1 , and the alkenyl group is selected from the group consisting of a substituted or unsubstituted straight-chain C2˜C6 alkenyl group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 alkenyl group.4. The organic light-emitting diode of claim 1 , wherein the organic luminescent unit comprises an organic luminescent layer.5. The organic light-emitting diode of claim 4 , wherein the organic luminescent unit further comprises a ...

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Номер записи: 26
31-01-2019 дата публикации

FLUORINE ATOM-CONTAINING COMPOUND AND USE THEREOF

Номер: US20190031600A1
Автор: ENDO Toshiyuki, NAKAZAWA Taichi
Принадлежит: NISSAN CHEMICAL INDUSTRIES, LTD.

Provided is a fluorine atom-containing compound represented by formula (1) below 2. The fluorine atom-containing compound of claim 1 , wherein each Aris independently a phenyl group substituted with 3 or more fluorine atoms which may be substituted with a cyano group claim 1 , a chlorine atom claim 1 , a bromine atom claim 1 , an iodine atom claim 1 , a nitro group claim 1 , an alkyl group of 1 to 20 carbon atoms claim 1 , a fluoroalkyl group of 1 to 20 carbon atoms or a fluoroalkoxy group of 1 to 20 carbon atoms; or a 2-(trifluoromethyl)phenyl group claim 1 , 3-(trifluoromethyl)phenyl group claim 1 , 4-(trifluoromethyl)phenyl group claim 1 , 4-ethoxy-3-(trifluoromethyl)phenyl group claim 1 , 3-fluoro-4-trifluoromethylphenyl group claim 1 , 4-fluoro-3-trifluoromethylphenyl group claim 1 , 4-fluoro-2-trifluoromethylphenyl group claim 1 , 2-fluoro-5-(trifluoromethyl)phenyl group claim 1 , 3-fluoro-5-(trifluoromethyl)phenyl group claim 1 , 3 claim 1 ,5-di(trifluoromethyl)phenyl group claim 1 , 2 claim 1 ,4 claim 1 ,6-tri(trifluoromethyl)phenyl group claim 1 , 4-(pentafluoroethyl)phenyl group claim 1 , 4-(3 claim 1 ,3 claim 1 ,3-trifluoropropyl)phenyl group claim 1 , 2 claim 1 ,3 claim 1 ,5 claim 1 ,6-tetrafluoro-4-trifluoromethylphenyl group claim 1 , 4-(perfluorovinyl)phenyl group claim 1 , 4-(perfluoropropenyl)phenyl group or 4-(perfluorobutenyl)phenyl group.3. The fluorine atom-containing compound of or claim 1 , wherein the Argroups are identical groups claim 1 ,4. The fluorine atom-containing compound of claim 1 , wherein Z is a group of formula (2).5. The fluorine atom-containing compound of claim 1 , wherein Ris a phenyl group.6. The fluorine atom-containing compound of claim 1 , wherein Rto Rare hydrogen atoms.7. A charge-transporting substance comprising the fluorine atom-containing compound of .8. A charge-transporting varnish comprising the charge-transporting substance of and an organic solvent.9. The charge-transporting varnish of claim 8 , further ...

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Номер записи: 27
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: 28
18-02-2021 дата публикации

MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF

Номер: US20210047347A1
Автор: "ONeill David John", Fetalvero Kristina Michelle, Narayan Sridhar, Saiah Eddine, Sengupta Shomit
Принадлежит:

The present invention provides compounds, compositions thereof, and methods of using the same. 131.-. (canceled)34. The method of claim 33 , wherein the pharmaceutically acceptable composition comprises a pharmaceutically acceptable carrier claim 33 , adjuvant claim 33 , or vehicle. The present invention relates to compounds and methods useful for modulating the Sestrin-GATOR2 interaction thereby selectively modulating mTORC1 activity indirectly. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.The mechanistic target of rapamycin complex 1 (mTORC1) protein kinase is a master growth regulator that senses diverse environmental cues, such as growth factors, cellular stresses, and nutrient and energy levels. When activated, mTORC1 phosphorylates substrates that potentiate anabolic processes, such as mRNA translation and lipid synthesis, and limits catabolic ones, such as autophagy. mTORC1 dysregulation occurs in a broad spectrum of diseases, including diabetes, epilepsy, neurodegeneration, immune response, suppressed skeletal muscle growth, and cancer among others (Howell et al., (2013) Biochemical Society transactions 41, 906-912; Kim et al., (2013) Molecules and cells 35, 463-473; Laplante and Sabatini, (2012) Cell 149, 274-293).Many upstream inputs, including growth factors and energy levels, signal to mTORC1 through the TSC complex, which regulates Rheb, a small GTPase that is an essential activator of mTORC1 (Brugarolas et al., (2004) Genes & Development 18, 2893-2904; Garami et al., (2003) Molecular Cell 11, 1457-1466; Inoki et al., (2003) Genes & Development 17, 1829-1834; Long et al., (2005) Current Biology 15, 702-713; Sancak et al., (2008) Science (New York, N.Y.) 320, 1496-1501; Saucedo et al., (2003) Nature cell biology 5, 566-571; Stocker et al., (2003) Nature cell biology 5, 559-565; Tee et al., (2002) Proc ...

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Номер записи: 29
18-02-2016 дата публикации

COMPOUNDS USEFUL FOR THE TREATMENT OF METABOLIC DISORDERS AND SYNTHESIS OF THE SAME

Номер: US20160046560A1
Автор: Brenman Jay E., Musso David L., Sexton Jonathan Z.
Принадлежит:

The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds. 23-. (canceled)56-. (canceled)815-. (canceled)19. An amide derivative selected from the group consisting of:3-Chloro-4-{[2-hydroxy-5-(trifluoromethyl)benzene]amido}benzoic acid,Methyl 4-[(5-tert-butyl-2-hydroxybenzene)amido]-3-chlorobenzoate,4-[(5-tert-butyl-2-hydroxybenzene)amido]-3-chlorobenzoic acid, andMethyl 3-chloro-4-[(2-hydroxy-5-methylbenzene)amido]benzoate.21. A pharmaceutical composition comprising one or more pharmaceutically acceptable carriers and a compound of claim 1 , or a pharmaceutically acceptable salt thereof.2223-. (canceled)24. The pharmaceutical composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with a pharmaceutically acceptable carrier and one or more hypoglycemic agents.25. The pharmaceutical composition of claim 24 , wherein the hypoglycemic agent is selected from the group consisting of insulin claim 24 , biguanidines claim 24 , sulfonylureas claim 24 , insulin secretagogues claim 24 , a-glycosidase inhibitors claim 24 , and β-adrenoreceptor agonists.26. (canceled)27. A method of treating a disease selected from the group consisting of non-alcoholic fatty liver disease claim 1 , metabolic syndrome claim 1 , diabetes claim 1 , Syndrome X claim 1 , a diabetes-related disorder claim 1 , obesity claim 1 , cardiovascular disease claim 1 , cerebrovascular disease claim 1 , peripheral vessel disease claim 1 , lupus claim 1 , polycystic ovary disease claim 1 , carcinogenesis claim 1 , hyperplasia and combinations thereof comprising the administration to a ...

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Номер записи: 30
01-05-2014 дата публикации

S-t-BUTYL PROTECTED CYSTEINE DI-PEPTIDE ANALOGS AND RELATED COMPOUNDS

Номер: US20140121202A1
Автор: Johnson Edward M., Lawton Daniel G.
Принадлежит: Promentis Pharmaceuticals, Inc.

S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS). 2. A pharmaceutical composition comprising at least one compound of and a pharmaceutically acceptable carrier.3. A method of treating a disease or condition of the Central Nervous System (CNS) selected from the group consisting of schizophrenia claim 1 , drug craving claim 1 , drug addiction claim 1 , bipolar disorder claim 1 , anxiety claim 1 , depression claim 1 , Parkinson's disease claim 1 , Alzheimer's disease claim 1 , cognitive dysfunction claim 1 , multiple sclerosis claim 1 , Amyotrophic lateral sclerosis (ALS) claim 1 , ischemic stroke claim 1 , HIV dementia claim 1 , and Huntington's disease comprising administering to a subject in need thereof a therapeutically effective amount of a compound of .4. The method of claim 3 , wherein said disease or condition of central nervous system is schizophrenia.5. The method of claim 3 , further comprising administering to a subject in need thereof:a) a first generation anti-psychotic agent selected from the group consisting of chlorpromazine, thioridazine, mesoridazine, loxapine, molindone, perphenazine, thiothixene, trifluoperazine, haloperidol, fluphenazine, droperidol, zuclopenthixol and prochlorperazineperphenazine, and/orb) a second generation anti-psychotic agent selected from the group consisting of amisulpride, aripiprazole, asenapine, blonanserin, clotiapine, clozapine, iloperidone, lurasidone, mosapramine, olanzapine, paliperidone, perospirone, quetiapine, remoxipride, risperidone, sertindole, sulpiride, ziprasidone, zotepine, bifeprunox (DU-127,090), pimavanserin (ACP-103), and vabicaserin (SCA-136). This invention relates to novel S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases ...

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Номер записи: 31
19-02-2015 дата публикации

Rhodium catalyst and method for producing amine compound

Номер: US20150051416A1
Автор: Hirotsugu Usutani, Masatoshi Yamada, Mitsuhisa Yamano
Принадлежит: Takeda Pharmaceutical Co Ltd

[Problem] Provision of a superior rhodium catalyst and a production method of amine compound. [Solving Means] A rhodium complex coordinated with a compound represented by the formula

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Номер записи: 32
14-02-2019 дата публикации

BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

Номер: US20190048028A1
Автор: Elliott Eric L., Ferdous Abu J., Kaufman Michael J., Komar-Lay Sonja A., Mazaik Debra L., Mccubbin Quentin J., Nguyen Phuong M., Palaniappan Vaithianathan, Skwierczynski Raymond D., Truong Nobel T., Varga Csanad M., Zawaneh Peter N.
Принадлежит:

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The process of claim 1 , wherein the reaction of step (1) or step (3) or both is conducted in the presence of a peptide coupling reagent.3. The process of claim 2 , wherein the peptide coupling reagent is selected from the group consisting of a carbodiimide reagent claim 2 , phosphonium reagent claim 2 , and uronium reagent.4. The process of claim 3 , wherein the peptide coupling reagent is selected from one or more of the group consisting of dicyclohexylcarbodiimide (DCC) claim 3 , 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC) claim 3 , benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) claim 3 , and O-(1H-benzotriazol-1-yl)-N claim 3 ,N claim 3 ,N′N′-tetramethyluronium tetrafluoroborate (TBTU).5. The process of claim 1 , further comprising converting the carboxylic acid moiety of compound (ii) to an activated ester or acid halide prior to the reaction of step (1).6. The process of claim 5 , wherein said activated ester or acid halide is an O—(N-hydroxysuccinnimide) ester.7. The process of claim 1 , wherein the reaction of step (3) is conducted in the presence of a solvent.8. The process of claim 7 , wherein the solvent is tetrahydrofuran.9. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an aqueous mineral acid.10. The process of claim 9 , wherein the mineral acid is hydrochloric acid.11. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an organic boronic acid acceptor.12. The process of claim 11 , wherein the organic boronic acid acceptor is i-BuB(OH).13. The process of claim 1 , wherein the reaction of step (5) is conducted in the presence of a solvent selected from the group consisting of ethyl ...

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Номер записи: 33
14-02-2019 дата публикации

MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF

Номер: US20190048029A1
Автор: "ONeill David John", Fetalvero Kristina Michelle, Narayan Sridhar, Saiah Eddine, Sengupta Shomit
Принадлежит:

The present invention provides compounds, compositions thereof, and methods of using the same. 131.-. (canceled)33. A pharmaceutically acceptable composition comprising a compound according to and a pharmaceutically acceptable carrier claim 32 , adjuvant claim 32 , or vehicle.34. The composition according to in combination with an additional therapeutic agent. The present invention relates to compounds and methods useful for modulating the Sestrin-GATOR2 interaction thereby selectively modulating mTORC1 activity indirectly. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.The mechanistic target of rapamycin complex 1 (mTORC1) protein kinase is a master growth regulator that senses diverse environmental cues, such as growth factors, cellular stresses, and nutrient and energy levels. When activated, mTORC1 phosphorylates substrates that potentiate anabolic processes, such as mRNA translation and lipid synthesis, and limits catabolic ones, such as autophagy. mTORC1 dysregulation occurs in a broad spectrum of diseases, including diabetes, epilepsy, neurodegeneration, immune response, suppressed skeletal muscle growth, and cancer among others (Howell et al., (2013) Biochemical Society transactions 41, 906-912; Kim et al., (2013) Molecules and cells 35, 463-473; Laplante and Sabatini, (2012) Cell 149, 274-293).Many upstream inputs, including growth factors and energy levels, signal to mTORC1 through the TSC complex, which regulates Rheb, a small GTPase that is an essential activator of mTORC1 (Brugarolas et al., (2004) Genes & amp; Development 18, 2893-2904; Garami et al., (2003) Molecular Cell 11, 1457-1466; Inoki et al., (2003) Genes & amp; Development 17, 1829-1834; Long et al., (2005) Current Biology 15, 702-713; Sancak et al., (2008) Science (New York, N.Y.) 320, 1496-1501; Saucedo et al., (2003) Nature cell biology 5, 566-571 ...

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Номер записи: 34
25-02-2016 дата публикации

3-AMIDOBENZAMIDES AND USES THEREOF FOR INCREASING CELLULAR LEVELS OF A3G AND OTHER A3 FAMILY MEMBERS

Номер: US20160052870A1
Автор: "DAquila Richard T.", Roh Meejeon, Schiltz Gary E., Song Chisu
Принадлежит: Northwestern University

Disclosed are novel benzamide compounds and the uses thereof for treating diseases and disorders in a patient in need thereof by increasing cellular levels of A3G and/or other members of the A3 family of proteins in the patient. The disclosed compounds include -benzamide compounds that may be administered to treat an HIV-1 infection or cancer in a patient. 2. The compound of claim 1 , wherein n is 0.3. The compound of claim 1 , wherein X is C.4. The compound of claim 1 , wherein Ris methoxy.6. The compound of claim 5 , wherein Ris C1-C6-alkoxy.7. The compound of claim 5 , wherein Ris H claim 5 , C1-C6-alkyl optionally substituted with C1-C6-alkoxy claim 5 , hydroxyl claim 5 , C1-C6-alkylamino claim 5 , C1-C6 dialkylamino claim 5 , phenyl claim 5 , benzyl claim 5 , benzo[1 claim 5 ,3]diox8yl claim 5 , pyridin-2-yl claim 5 , pyridin-3-yl claim 5 , pyridin-4-yl claim 5 , C3-C6-cycloalkyl optionally substituted with methyl claim 5 , C1-C6-alkoxy claim 5 , N-piperidinyl claim 5 , and tetrahydrofuran-2-yl.8. The compound of claim 5 , wherein R claim 5 , R claim 5 , R claim 5 , R claim 5 , and Rare independently selected from H claim 5 , C1-C6-alkoxy claim 5 , and halo.9. The compound of claim 5 , wherein one or more of R claim 5 , R claim 5 , are Rare methoxy.10. The compound of claim 9 , wherein one or more of Rand Rare chloro.12. A pharmaceutical composition comprising the compound of and a pharmaceutical carrier.13. The pharmaceutical composition of comprising an effective amount of the compound for increasing levels of A3G and/or other members of the A3 family of proteins after the composition is administereing to a patient in need thereof.14. A method for treating HIV-1 infection in a patient in need thereof claim 13 , the method comprising administering the pharmaceutical composition of to the patient.15. A method for treating cancer in a patient in need thereof claim 13 , the method comprising administering the pharmaceutical composition of to the patient. The ...

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Номер записи: 35
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: 36
25-02-2021 дата публикации

COMPOUNDS FOR INHIBITION OF ALPHA 4 BETA 7 INTEGRIN

Номер: US20210053967A1
Автор: BLOMGREN Peter A., Campbell Taryn L., CHANDRASEKHAR Jayaraman, Clark Christopher T., CURRIE Kevin S., KROPF JEFFREY E., Moazami Yasamin, Nava Nicole A., Patel Leena, Perry Jason K., Seeger Natalie, Stevens Kirk L., ZHAO ZHONGDONG
Принадлежит:

The present disclosure provides a compound of Formula (I): 15. The compound of claim 1 , wherein Zis N claim 1 , and each of Z claim 1 , Z claim 1 , and Zis CH.16. The compound of or claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Rand Ris independently selected from H claim 1 , and halo.17. The compound of any one of claim 1 , claim 1 , and or a pharmaceutically acceptable salt thereof claim 1 , wherein each Rand Ris H.18. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Rand Ris independently selected from H claim 1 , halo claim 1 , Calkyl claim 1 , Calkoxyl claim 1 , Chaloalkyl claim 1 , and Chaloalkoxyl.19. The compound of any one of to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Rand Ris independently selected from F claim 1 , and —CH.20. The compound of any one of to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris F claim 1 , and Ris —CH.21. The compound of any one of - claim 1 , claim 1 , and - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris 6-membered heterocyclyl optionally substituted with one to three R; and wherein each Ris independently selected from halo claim 1 , Calkyl claim 1 , and Chaloalkyl.22. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from —CH claim 1 , —CHF claim 1 , and —CF.23. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CF.27. The compound of any one of - claim 1 , claim 1 , and - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —NRR; and wherein Rand Ris independently selected from H claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , and Ccycloalkyl.29. The compound of any one of claim 1 , and claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Xis N claim 1 , and Xis O.30. The ...

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Номер записи: 37
22-05-2014 дата публикации

SUBSTITUTED 3-PHENYLPROPIONIC ACIDS AND THE USE THEREOF

Номер: US20140142069A1
Автор: BECKER-PELSTER Eva-Maria, EL SHEIKH Sherif, Hahn Michael, KNORR Andreas, Lampe Thomas, Li Volkhart Min-Jian, Schlemmer Karl-Heinz, Stasch Johannes-Peter, Stoll Friederike, Wunder Frank
Принадлежит: Bayer Intellectual Property GmbH

The present application relates to novel 3-phenylpropionic acid derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders. 4. The compound according to claim 1 , wherein the compound is(+)-3-(3-{[(2S,3R)-2-(4-tert-butylphenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}-4-chlorophenyl)propanoic acid;3-[4-Chloro-3-({4,4,4-trifluoro-3-methyl-2-[4-(2,2,2-trifluoroethyl)phenyl]butanoyl}amino)phenyl]propanoic acid;3-(4-chloro-3-{[(2S,3R)-2-(4-ethylphenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)butanoic acid;(3S)-3-(4-chloro-3-{[(4-chlorophenyl)(2,2-difluoro-cyclopentyl)acetyl]amino}phenyl)butanoic acid;(+)-3-(4-Chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)propanoic acid;(+)-(2S)-3-(4-Chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-2-methylpropanoic acid;(+)-(2S)-2-(4-Chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}benzyl)butanoic acid;3-(3-{[(3R)-2-(4-Chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}-4-fluorophenyl)-2-methylpropanoic acid;threo-3-(3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}-4-fluorophenyl)-2-methylbutanoic acid;(+)-2-(4-Chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}benzyl)-2-methylbutanoic acid;3-(4-Chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)hexanoic acid;(+)-3-(4-Chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)hexanoic acid;(+)-3-(4-Chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}-phenyl)-4,4,4-trifluorobutanoic acid;(+)-3-(4-Chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)pentanoic acid;3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl ...

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Номер записи: 38
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: 39
15-03-2018 дата публикации

INHIBITORS OF HISTONE DEACETYLASE

Номер: US20180072671A1
Автор: Haggarty Stephen J., Holson Edward, Lewis Michael C., Lundh Morten, Petryshen Tracey Lynn, Wagner Bridget, Wagner Florence Fevrier, ZHANG YAN-LING
Принадлежит:

The present invention relates to compounds of formula (I): 2. A compound of or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein{'sub': 1', '2', '3', '4', '1', '2', '3', '4, 'W, W, W, and Ware each independently selected from hydrogen, chlorine, fluorine, and deuterium, provided that at least one of W, W, W, and Wis not hydrogen;'}{'sub': 1', '5', '1', '3, 'Xand Xare each independently selected from hydrogen, halogen and C-Calkyl;'}{'sub': 2', '3', '4', 'p', 'p', '1', '8', '2', '8', '2', '8', '3', '8', '4', '8', '2', '3', '4, 'sup': 5', '6', '7', '1', '7', '3', '4', '1', '2', 'a, 'X, X, and Xare each independently selected from hydrogen, halogen, OR, C(O)R, OS(O)R, NRS(O)R, NRR, NRC(O)R, C-Calkyl, C-Calkenyl, C-Calkynyl, C-Ccycloalkyl, C-Ccycloalkenyl, aromatic ring, 3-8 membered heteroaromatic ring, and 3-8 membered saturated or partially saturated heterocyclic ring, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aromatic ring, heteroaromatic ring, and heterocyclic ring is unsubstituted or substituted with one or more Rand one or two of X, X, and Xis hydrogen;'}{'sup': a', '25', '26', '27', '28', '29, 'sub': 1', '8', '3', '2', '2, 'Ris selected from halogen, OR, C-Calkyl, CF, CHF, CHF, NRC(O)R, and NRR; or'}{'sup': 1', '26, 'sub': 1', '8, 'Rand Rare each independently selected from hydrogen and C-Calkyl;'}{'sup': 2', 'b, 'sub': 1', '8', '2', '8', '3', '8', '3', '8', '4', '8, 'Ris selected from hydrogen, C-Calkyl, C-Calkenyl, C-Calkynyl, C-Ccycloalkyl, C-Ccycloalkenyl, aromatic ring, 3-8 membered heteroaromatic ring, and 3-8 membered saturated or partially saturated heterocyclic ring, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aromatic ring, heteroaromatic ring, and heterocyclic ring are unsubstituted or substituted with one or more R;'}{'sup': 27', 'b, 'sub': 1', '8', '3', '8', '3', '8', '4', '8, 'Ris selected from hydrogen, C-Calkyl, C-Calkynyl, C-Ccycloalkyl, ...

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Номер записи: 40
07-03-2019 дата публикации

NOVEL COMPOUND HAVING BLT INHIBITORY ACTIVITY AND COMPOSITION, FOR PREVENTING OR TREATING INFLAMMATORY DISEASES, COMPRISING SAME AS ACTIVE INGREDIENT

Номер: US20190071395A1
Автор: CHOI YongSeok, GOO Ja-Il, HAN Hyo-Kyung, Kim Jae-Hong, KWON Jinsun, LEE Kyeong, WEI Jun Dong
Принадлежит:

The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases. 3. The method of claim 1 , wherein the compound represented by Formula 1 is selected from the group consisting of:tert-butyl 4-(4-(3-(N-phenylpentaneamido)prop-1-ynyl)benzoyl)piperazine-1-carboxylate;N-phenyl-N-(3-(4-(piperazine-1-carbonyl)phenyl)prop-2-ynyl)pentaneamide;N-(3-(4-(4-methylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-ethylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-isopropylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-(2-hydroxyethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-cyclohexylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-(cyclohexylmethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-isobutylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-phenyl-N-(3-(4-(4-(prop-2-ynyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)pentaneamide;N-(3-(4-(4-cyanopiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;tert-butyl 4-(4-(3-(N-(3-fluorophenyl)pentaneamido)prop-1-ynyl)benzoyl)piperazine-1-carboxylate;N-(3-fluorophenyl)-N-(3-(4-(piperazine-1-carbonyl)phenyl)prop-2-ynyl)pentaneamide;N-(3-fluorophenyl)-N-( ...

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Номер записи: 41
19-03-2015 дата публикации

Novel EP2 Receptor Agonists

Номер: US20150080400A1
Автор: Boer Rainer, Dunkern Torsten, Gavade Sandip, Hartung Simone, HESSMANN Manuela, Hoffmeyer Angelika, Jain Hiteshkumar, Keche Ashish, Makhija Mahindra, Pahl Andreas, Patel Sarvesh, Prabhu Arati, Praechter Christiane, Tiwari Manojkumar, VOLZ Jurgen, Zitt Christof
Принадлежит: TAKEDA GMBH

The compounds of formula (1) 6. A compound of formula (1) according to claim 5 , which is selected from the group consisting of(2E)-3-(3-{[(3-phenylnaphthalen-1-yl)carbonyl]amino}phenyl)prop-2-enoic acid,(2E)-3-(4-fluoro-3-{[(3-phenylnaphthalen-1-yl)carbonyl]amino}phenyl)prop-2-enoic acid,(2E)-3-(4-chloro-3-{[(3-phenylnaphthalen-1-yl)carbonyl]amino}phenyl)prop-2-enoic acid,(3-{[(3-phenylnaphthalen-1-yl)carbonyl]amino}phenoxy) acetic acid,(4-fluoro-3-{[(3-phenylnaphthalen-1-yl)carbonyl]amino}phenoxy) acetic acid,(4-chloro-3-{[(3-phenylnaphthalen-1-yl)carbonyl]amino}phenoxy) acetic acid,3-(3-{[(3-phenylnaphthalen-1-yl)carbonyl]amino}phenyl) propanoic acid,3-(4-fluoro-3-{[(3-phenylnaphthalen-1-yl)carbonyl]amino}phenyl) propanoic acid,(2E)-3-{3-[({3-[2-fluorophenyl]naphthalen-1-yl}carbonyl)amino]-4fluorophenyl}prop-2-enoic acid,(2E)-3-{3-[({3-[3-fluorophenyl]naphthalen-1-yl}carbonyl)amino]-4fluorophenyl}prop-2-enoic acid,(2E)-3-{3-[({3-[4-fluorophenyl]naphthalen-1-yl}carbonyl)amino]-4fluorophenyl}prop-2-enoic acid,(2E)-3-{3[({3-[3-(aminomethyl)phenyl]naphthalen-1-yl}carbonyl)amino]-4fluorophenyl}prop-2-enoic acid,(2E)-3-{4-fluoro-3-[({3-[2-(hydroxymethyl)phenyl]naphthalen-1-yl}carbonyl)amino]phenyl}prop-2-enoic acid,(2E)-3-{4-fluoro-3-[({3-[3-(hydroxymethyl)phenyl]naphthalen-1-yl}carbonyl)amino]phenyl}prop-2-enoic acid,(2E)-3-[4-fluoro-3-({[3-(3-fluoro-5-hydroxyphenyl)naphthalen-1yl]carbonyl}amino)phenyl]prop-2-enoic acid,3-[4-fluoro-3-({[3-(2-fluorophenyl)naphthalen-1yl]carbonyl}amino)phenyl]propanoicacid,3-[4-fluoro-3-({[3-(3-fluorophenyl)naphthalen-1-yl]carbonyl}amino)phenyl]propanoic acid,(2E)-3-(3-{[(3-{3-[(acetylamino)methyl]phenyl}naphthalen-1-yl)carbonyl]amino}-4fluorophenyl)prop-2-enoic acid,(2E)-3-[3-({[3-(3-hydroxyphenyl)naphthalen-1-yl]carbonyl}amino)phenyl]prop-2-enoic acid,(2E)-3-{3-[({3-[3-(piperazin-1-yl)phenyl]naphthalen-1-yl}carbonyl)amino]phenyl}prop-2-enoic acid,(2E)-3-[3-({[3-(morpholin-4-yl)naphthalen-1-yl]carbonyl}amino)phenyl]prop-2-enoic acid,( ...

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Номер записи: 42
22-03-2018 дата публикации

INHIBITORS OF INDOLEAMINE-2,3-DIOXYGENASE FOR THE TREATMENT OF CANCER

Номер: US20180079712A1
Автор: Balog James Aaron, Cherney Emily Charlotte, Cheruku Srinivas, Huang Audris, Kanyaboina Yadagiri, Markwalder Jay A., Nara Susheel Jethanand, Pulicharla Nagalakshmi, Roy Saumya, Seitz Steven P., Shan Weifang, Sistla Ramesh Kumar, Thangathirupathy Srinivasan, Thangavel Soodamani, Williams David K.
Принадлежит:

There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine-2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention. 2. The compound of claim 1 , wherein Y and V are each CH.3. The compound of or claim 1 , wherein Ris —COOH.4. The compound of any one of the preceding claims claim 1 , wherein one of Rand Ris H and the other is optionally substituted C-Calkyl claim 1 , optionally substituted Ccycloalkyl claim 1 , optionally substituted heterocyclyl claim 1 , or optionally substituted aryl.5. The compound of any one of to claim 1 , wherein Rand Rare each independently optionally substituted C-Calkyl.6. The compound of any one of the preceding claims claim 1 , wherein Rand Rare each H.7. The compound of any one of the preceding claims claim 1 , wherein Ris optionally substituted heterocyclyl and Ris optionally substituted C-Calkyl.8. The compound of any one of to claim 1 , wherein Rand Rare taken together with the nitrogen to which they are attached to form a 4- to 8-membered optionally substituted heterocyclic ring containing 0-3 additional heteroatoms selected from —N— claim 1 , —S— and —O—.9. The compound of any one of the preceding claims claim 1 , wherein Ris optionally substituted aryl.10. The compound of any one of to claim 1 , wherein Ris optionally substituted heteroaryl.11. The compound of any one of to claim 1 , wherein Ris optionally substituted heterocyclyl.12. A pharmaceutical composition comprising a compound of any one of the preceding claims and a pharmaceutically acceptable excipient.13. A compound of any one of to for use in therapy.14. A method of treating cancer is a patient in need of such treatment comprising administering to the patient a therapeutically effective amount of a compound according to any one of to .15. The method ...

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Номер записи: 43
24-03-2016 дата публикации

FATTY ACID ACYLATED SALICYLATES AND THEIR USES

Номер: US20160083336A1
Автор: Bemis Jean E., Jirousek Michael R., Milne Jill C., Smith Jesse J., Vu Chi B.
Принадлежит:

The invention relates to fatty acid acylated salicylate derivatives; compositions comprising an effective amount of a fatty acid acylated salicylate derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a fatty acid acylated salicylate derivative. 1. (canceled)3. (canceled)7. (canceled)8. A compound of claim 2 , wherein Q is Z.10. A compound of claim 2 , wherein m is 1 and L is —S—S— or —O—.1138-. (canceled)39. The compound of claim 2 , wherein r is 3 claim 2 , s is 5 and w is 1.40. A method of treating inflammation associated with a metabolic disorder claim 2 , the method comprising administering to a patient in need thereof an effective amount of a compound of .41. The method of claim 40 , wherein the inflammation is associated with inflammatory bowel disease.42. The method of claim 40 , wherein the inflammation is associated with muscular dystrophy.43. The method of claim 40 , wherein the inflammation is associated with cachexia.44. The method of claim 40 , wherein the inflammation is associated with Crohn's disease.45. The method of claim 40 , wherein the inflammation is associated with Type II diabetes.46. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier. This application is a continuation-in-part of U.S. application Ser. No. 12/499,779, filed Jul. 8, 2009, and claims the benefit of U.S. Provisional Application No. 61/148,658, filed Jan. 30, 2009, U.S. Provisional Application No. 61/104,363, filed Oct. 10, 2008, U.S. Provisional Application No. 61/104,364, filed Oct. 10. 2008, U.S. Provisional Application No. 61/104,366, filed Oct. 10, 2008, and U.S. Provisional Application No. 61/078,983, filed Jul. 8, 2008. The entire disclosures of those applications are relied on and incorporated into this application by reference.The invention relates to fatty acid acylated salicylate derivatives, fatty acid acylated diflunisal derivatives, and fatty ...

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Номер записи: 44
12-06-2014 дата публикации

STILBENE-BASED REACTIVE COMPOUNDS, POLYMERIC MATRICES FORMED THEREFROM, AND ARTICLES VISUALIZABLE BY FLUORESCENCE

Номер: US20140162083A1
Автор: Jelle Bruce M., Kurdyumov Aleksey V., Lockwood Nathan A., Swan Dale G.
Принадлежит: SURMODICS, INC.

The invention is directed to latent reactive and polymerizable derivatives of fluorescent stilbene-based compounds. The compounds can be used to provide articles with a fluorescence property, such as medical devices (e.g., catheters). The fluorescent compounds can be used in association with polymers, or can be incorporated into polymers, and the polymers used in a coating composition on the article surface. The compounds allow for visual or machine inspection of coating properties such as uniformity of coverage. 7. The compound of wherein Ris a C1-C4 hydrocarbylene group claim 1 , or a C2 hydrocarbylene group; wherein Ris —OH; or wherein R and R are phenyl.11. The compound of wherein Ris —C(O)—.13. The compound of where claim 1 , in subformula Ic claim 1 , RRis —C(O)R—.14. The compound of wherein Ris —NR— claim 13 , or —NRN— claim 13 , wherein Ris a C1-C8 hydrocarbylene group.16. The compound of wherein Ris NRN claim 15 , a C1-C4 hydrocarbylene group claim 15 , or —NHCHCHNH—.17. A polymer comprising the compound of .18. A polymeric matrix comprising the compound of .19. A medical device comprising a hydrophilic coating comprising the polymeric matrix of .20. A medical device comprising a hydrophilic coating claim 18 , the hydrophilic coating comprising an aryl ketone derivative of a triazinylaminostilbenesulfonic acid. The present non-provisional application claims the benefit of commonly owned provisional Application having Ser. No. 61/736,436, filed on Dec. 12, 2012, entitled STILBENE-BASED REACTIVE COMPOUNDS, POLYMERIC MATRICES FORMED THEREFROM, AND ARTICLES VISUALIZABLE BY FLUORESCENCE, which application is incorporated herein by reference in its entirety.The invention relates to hydrophilic polymeric coatings for surfaces of medical articles and hydrophilic polymer coatings that can be visualized with light.Developments in medicine have enabled the use of many non-classical surgical techniques in the treatment of diseases and disorders. For example, ...

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Номер записи: 45
26-03-2015 дата публикации

Thermoplastic polymer composition

Номер: US20150087758A1
Автор: Darin L. Dotson, Eduardo Torres, Francisco Alvarez, Haihu Qin, Sanjeev K. DEY
Принадлежит: Milliken and Co

The invention provides a compound conforming to the structure of Formula (CX) The invention also provides a thermoplastic polymer composition comprising a polyolefin polymer and a compound conforming to the structure of Formula (CX) as a nucleating agent.

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Номер записи: 46
12-03-2020 дата публикации

MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF

Номер: US20200079800A1
Автор: "ONeill David John", Fetalvero Kristina Michelle, Narayan Sridhar, Saiah Eddine, Sengupta Shomit
Принадлежит:

The present invention provides compounds, compositions thereof, and methods of using the same. 131.-. (canceled)33. A pharmaceutically acceptable composition comprising a compound according to claim 32 , and a pharmaceutically acceptable carrier claim 32 , adjuvant claim 32 , or vehicle.34. A method for treating depression in a patient in need thereof claim 33 , comprising the step of administering to said patient the composition of . The present invention relates to compounds and methods useful for modulating the Sestrin-GATOR2 interaction thereby selectively modulating mTORC1 activity indirectly. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.The mechanistic target of rapamycin complex 1 (mTORC1) protein kinase is a master growth regulator that senses diverse environmental cues, such as growth factors, cellular stresses, and nutrient and energy levels. When activated, mTORC1 phosphorylates substrates that potentiate anabolic processes, such as mRNA translation and lipid synthesis, and limits catabolic ones, such as autophagy. mTORC1 dysregulation occurs in a broad spectrum of diseases, including diabetes, epilepsy, neurodegeneration, immune response, suppressed skeletal muscle growth, and cancer among others (Howell et al., (2013) Biochemical Society transactions 41, 906-912; Kim et al., (2013) Molecules and cells 35, 463-473; Laplante and Sabatini, (2012) Cell 149, 274-293).Many upstream inputs, including growth factors and energy levels, signal to mTORC1 through the TSC complex, which regulates Rheb, a small GTPase that is an essential activator of mTORC1 (Brugarolas et al., (2004) Genes & Development 18, 2893-2904; Garami et al., (2003) Molecular Cell 11, 1457-1466; Inoki et al., (2003) Genes & Development 17, 1829-1834; Long et al., (2005) Current Biology 15, 702-713; Sancak et al., (2008) Science (New York, N ...

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Номер записи: 47
02-04-2015 дата публикации

Thermoplastic polymer composition

Номер: US20150094406A1
Автор: Chi-Chun Tsai, Darin L. Dotson, Eduardo Torres, Francisco Alvarez, Haihu Qin, John W. Miley, Mary Angela COOLEY, Sanjeev K. DEY
Принадлежит: Milliken and Co

The invention provides a thermoplastic polymer composition comprising a polyolefin polymer and a nucleating agent. The nucleating agent comprises a compound conforming to the structure of Formula (I) The invention also provides a series of compounds encompassed by the structure of Formula (I).

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Номер записи: 48
19-06-2014 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20140171310A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

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Номер записи: 49
19-03-2020 дата публикации

Method for producing optically active substance, optically active substance, method for producing chiral molecule, and chiral molecule

Номер: US20200087227A1
Автор: Katsuhiko Tomooka, Kazunobu Igawa
Принадлежит: Daicel Corp, Kyushu University NUC

Provided is a method for producing an optically active substance, the method including an asymmetric induction, wherein an asymmetry inducer is allowed to act on a chiral molecule having a half-life of enantiomeric excess of shorter than 10 hours, thereby increasing abundance of one enantiomer of the chiral molecule. According to this method, one enantiomer of a chiral molecule that is susceptible to racemization can be selectively and efficiently obtained.

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Номер записи: 50
26-03-2020 дата публикации

Compounds and Methods for Inhibiting CPY26 Enzymes

Номер: US20200093788A1
Автор: Board Johnathan, Cameron Donald Andrew, Maheta Ashishkumar Jayantilal, Petkovich Martin, Petkovich Toni Kristian, Singh Suneel, Snieckus Victor
Принадлежит:

Compounds described herein are inhibitors of retinoic acid inducible P450 (CYP26) enzymes, and are useful for treating diseases that are responsive to retinoids. Certain compounds have retinoid activity, are resistant to CYP26-mediated catabolism, and are used for treating diseases that are responsive to retinoids. 2. The compound of claim 1 , wherein Rand Rare H claim 1 , and Ris methyl.3. The compound of claim 1 , wherein n is 1.4. The compound of claim 1 , wherein Rand Rare methyl.5. The compound of claim 1 , wherein Rand Rare each Cand they form a ring.7. A method of treating a disease or condition in a mammal claim 1 , comprising administering an inhibitor of the breakdown of RA claim 1 , comprising a compound of Formula (1) of .8. The method of claim 7 , wherein the disease or condition is a skin disease.9. The method of claim 8 , wherein the skin disease is actinic keratosis claim 8 , arsenic keratosis claim 8 , inflammatory and non-inflammatory acne claim 8 , psoriasis claim 8 , ichthyosis and other keratinization claim 8 , hyperproliferative disorders of the skin claim 8 , eczema claim 8 , atopic dermatitis claim 8 , Darriers disease claim 8 , lichen planus claim 8 , glucocorticoid damage claim 8 , or steroid atrophy.10. The method of claim 7 , wherein the compound is applied as a topical antimicrobial claim 7 , a skin anti pigmentation agent claim 7 , to treat and reverse the effects of age and photo damage to the skin.11. The method of claim 7 , wherein the method of treating a disease or condition in a mammal claim 7 , further comprises preventing cancerous or precancerous conditions.12. The method of claim 11 , wherein the condition is premalignant or malignant hyperprolifertive diseases claim 11 , cancer of the breast claim 11 , skin claim 11 , prostate claim 11 , cervix claim 11 , uterus claim 11 , colon claim 11 , bladder claim 11 , esophagus claim 11 , stomach claim 11 , lung claim 11 , larynx claim 11 , oral cavity claim 11 , blood claim 11 , ...

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Номер записи: 51
26-03-2020 дата публикации

BIODEGRADABLE DIETHANOLAMINE DERIVATIVE CHELATING AGENT AND PREPARATION PROCESS THEREOF

Номер: US20200095192A1
Автор: KAEOTHIP SOPHON, PORNSURIYASAK PAPAPIDA
Принадлежит: PTT Global Chemical Public Company Limited

The present invention relates to a new diethanolamine derivative chelating agent having a high water solubility, a good chelating property, and biological degradation. The said new chelating agent can be prepared from reaction of diethanolamine and cyclic anhydride compound using lewis acid as the catalyst. The said process is uncomplicated, and does not use a severe condition, and also reduces the use of harmful chemicals. 4. The diethanolamine derivative chelating agent according to claim 3 , wherein n is 1.6. A process for preparing the diethanolamine derivative chelating agent according to claim 1 , wherein said process comprises the following steps:a) mixing diethanolamine and cyclic anhydride compound in equivalent mole ratio from 1:1 to 1:5 in organic solvent; andb) adding lewis acid catalyst into mixture obtained from a).7. The process for preparing the diethanolamine derivative chelating agent according to claim 6 , wherein the organic solvent in step a) can be selected from 1 claim 6 ,4-dioxane claim 6 , 1 claim 6 ,2-dichloroethane claim 6 , dichloromethane claim 6 , or mixture thereof.8. The process for preparing the diethanolamine derivative chelating agent according to claim 7 , wherein the organic solvent in step a) is dichloromethane.9. The process for preparing the diethanolamine derivative chelating agent according to claim 6 , wherein the cyclic anhydride compound in step a) is selected from maleic anhydride claim 6 , succinic anhydride claim 6 , glutaric anhydride claim 6 , or phthalic anhydride.10. The process for preparing the diethanolamine derivative chelating agent according to claim 9 , wherein the cyclic anhydride compound is selected from maleic anhydride claim 9 , succinic anhydride claim 9 , or phthalic anhydride.11. The process for preparing the diethanolamine derivative chelating agent according to claim 6 , wherein the equivalent mole ratio between diethanolamine and cyclic anhydride compound is from 1:2 to 1:5.12. The process for ...

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Номер записи: 52
26-03-2020 дата публикации

GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO

Номер: US20200095259A1
Автор: Ashweek Neil, Beaton Graham, Chen Mi, Coon Timothy Richard, Ewing Todd, Jiang Wanlong, Lowe Richard, Moree Willy, Rowbottom Martin, Smith Nicole, Wade Warren, Zhao Liren, Zhu Yun-Fei
Принадлежит:

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: 129.-. (canceled)30. The compound that is 3-(2-{[4-chloro-3-(4-cyano-6-trifluoromethyl-pyridin-3-yl)-benzoyl]-methyl-amino}-phenoxy)-propionic acid , or a pharmaceutically acceptable salt thereof.31. A pharmaceutical composition comprising the compound of claim 30 , or a pharmaceutically acceptable salt thereof claim 30 , and a pharmaceutically acceptable carrier or diluent.32. The compound that is 4-(2-{[4-chloro-3-(4-cyano-6-trifluoromethyl-pyridin-3-yl)-benzoyl]-methyl-amino}-3-methyl-phenoxy)-butyric acid claim 30 , or a pharmaceutically acceptable salt thereof.33. A pharmaceutical composition comprising the compound of claim 32 , or a pharmaceutically acceptable salt thereof claim 32 , and a pharmaceutically acceptable carrier or diluent. This application is a continuation of U.S. patent application Ser. No. 15/210,470, filed Jul. 14, 2016, which is a continuation of U.S. patent application Ser. No. 14/592,690, filed Jan. 8, 2015, now issued as U.S. Pat. No. 9,422,310 on Aug. 23, 2016, which is a continuation of U.S. patent application Ser. No. 13/910,961 filed Jun. 5, 2013, now issued as U.S. Pat. No. 8,952,161 on Feb. 10, 2015, which is a continuation of U.S. patent application Ser. No. 13/293,943 filed Nov. 10, 2011, now issued as U.S. Pat. No. 8,481,738 on Jul. 9, 2013, which is a divisional of U.S. patent application Ser. No. 12/594,809, filed Feb. 22, 2010, now issued as U.S. Pat. No. 8,084,614 on Dec. 27, 2011, which application is a U.S. national stage application filed under 35 U.S.C. § 371 of International Patent Application No. PCT/US2008/059438, accorded an international filing date of Apr. 4, 2008, which claims the benefit of U.S. Provisional Application No. 60/910,621, filed Apr. 6, 2007, all of which applications are incorporated herein by reference in ...

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Номер записи: 53
12-04-2018 дата публикации

PROTEASOME INHIBITORS

Номер: US20180099984A1
Автор: Danca Mihaela Diana, Olhava Edward J.
Принадлежит:

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The method of claim 1 , wherein Zand Zare each hydroxy.3. The method of claim 1 , wherein Zand Ztogether form a moiety derived from a boronic acid complexing agent.6. The method of claim 1 , wherein the compound of formula (I) is selected from:[(1R)-1-({[(2,3-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(5-chloro-2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,5-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,5-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-bromobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chloro-5-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,4-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,5-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,4-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chloro-4-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,3-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,4-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-chloro-2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1 ...

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Номер записи: 54
21-04-2016 дата публикации

PROCESSES FOR MAKING PONATINIB AND INTERMEDIATES THEREOF

Номер: US20160108053A1
Автор: Kannapan Jayaraman, Kovi Ravishanker, PATEL Rajesh A., Thakor Sanjay F.
Принадлежит: Apicore US LLC

Novel synthetic approaches to make 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide, intermediates and pharmaceutically acceptable salts thereof are provided. 2. The method according to wherein X is Br.3. The method according to wherein P is CH claim 1 , tosyl claim 1 , mesyl claim 1 , carboxybenzyl claim 1 , benzyl or amino.4. The method according to wherein the step of deprotecting the piperazine ring comprises N-methylation with methyl iodide.5. The method according to wherein the step of forming a piperazine ring comprises treatment of the N-(4-(aminomethyl)-3-(trifluoromethyl)phenyl)-3-(imidazo[1 claim 1 ,2-b]pyridazin-3-ylethynyl)-4-methylbenzamide with 2-chloro-N-(2-chloroethyl)-N-methylethanamine.6. The method according to wherein the step of forming a piperazine ring comprises treatment of the N-(4-(aminomethyl)-3-(trifluoromethyl)phenyl)-3-(imidazo[1 claim 1 ,2-b]pyridazin-3-ylethynyl)-4-methylbenzamide with a 2-chloro-N-(2-chloroethyl)-N-substituted derivative of the formula (VI) wherein P is a protecting group and subsequently deprotecting the piperazine ring.7. The method according to wherein the step of deprotection of the piperazine ring is carried out in an acid claim 1 , base and under hydrogenation conditions.8. The method according to wherein the acid is selected from the group consisting of concentrated sulfuric acid claim 7 , HBr in acetic acid claim 7 , HBr in water and trifluoroacetic acid.9. The process according to wherein the hydrogenation is carried out using hydrogen pressure and a catalyst.10. The process according to wherein the catalyst comprises palladium and/or Raney nickel.12. The method according to wherein P is CH claim 11 , tosyl claim 11 , mesyl claim 11 , carboxybenzyl claim 11 , benzyl or amino.13. The method according to wherein the step of deprotecting the piperazine ring comprises N-methylation with methyl iodide.14. The method according to wherein ...

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Номер записи: 55
28-04-2016 дата публикации

Process for the manufacture of n-acylbiphenyl alanine

Номер: US20160115118A1
Автор: Desong Shi, Fengfeng Tao, Guoliang Zhu, Junhui Wei
Принадлежит: Individual

The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.

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Номер записи: 56
28-04-2016 дата публикации

alpha-SUBSTITUTED GLYCINAMIDE DERIVATIVE

Номер: US20160115119A1
Автор: Hirasawa Hideaki, Kawamura Naohiro, KOBAYASHI Junichi
Принадлежит: KISSEI PHARMACEUTICAL CO., LTD.

The present invention is to provide a novel α-substituted glycinamide derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof. 2. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein X is CH; and n is 1.4. The compound according to or a pharmaceutically acceptable salt thereof claim 3 , wherein Y is —CRR—.7. The compound according to or a pharmaceutically acceptable salt thereof claim 6 , wherein Ais a group selected from the group consisting of the following d1) and e):{'sub': 1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '7-10, 'd1) phenyl, wherein the ring is unsubstituted or substituted with 1 to 2 substituents independently selected from the group consisting of the following: a halogen atom, hydroxy, Calkyl, Calkoxy, hydroxy-Calkoxy, halo-Calkyl, halo-Calkoxy, cyano, amino, nitro, carboxy, (Calkyl)carbonylamino, (Calkyl)carbonyloxy, (Calkyl)carbonyl and (Caralkyloxy)carbonyl, and'}{'sub': 1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '7-10', '1-6', '1-6', '2-6', '1-6, 'e) heterocycle, wherein the ring is unsubstituted or substituted with 1 to 2 substituents independently selected from the group consisting of the following: a halogen atom, hydroxy, Calkyl, Calkoxy, halo-Calkyl, halo-Calkoxy, cyano, mono(di)Calkylamino, Calkylsulfanyl, amino, (Caralkyloxy)carbonyl, hydroxy-Calkyl, hydroxy-Calkoxy, Calkenyl, morpholino and (Calkyl)carbonyl.'}8. The compound according to or a pharmaceutically acceptable salt thereof claim 7 , wherein Ais a group selected from the group consisting of the following a2) claim 7 , b1) and c1):{'sub': 1-6', '1-6', '1-6, 'a2) phenyl, wherein the ring is unsubstituted or substituted with 1 to 2 substituents independently selected from the group consisting of the following: a halogen atom, hydroxy, hydroxy-Calkyl, cyano, amino, mono(di)Calkylamino and Calkoxy,'}b1) thiazolyl, and{'sub': 1-6', '1-6, 'c1) a group ...

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Номер записи: 57
27-04-2017 дата публикации

NOVEL EFFECTIVE ANTIVIRAL COMPOUNDS AND METHODS USING SAME

Номер: US20170114060A1
Автор: FREEDMAN Bruce D., HARTY Ronald N., Reitz Allen B., Wrobel Jay E.
Принадлежит:

The present invention includes compounds that are useful in preventing or treating viral infections caused by an enveloped RNA virus, such as viral infections caused by a Filovirus, arenavirus, rhabdovirus, paramyxovirus, orthomyxovirus and/or retrovirus. The present invention further includes compositions comprising such compounds, and methods of treating a viral infection in a subject using such compounds. 1. A method of treating or preventing a viral infection in a subject in need thereof , the method comprising administering to subject an effective amount of at least one inhibitor of a channel selected from the group consisting of calcium-release activated calcium (CRAC) channel and transient receptor potential mucolipin I (TRPML1) channel , whereby the viral infection is treated or prevented in the subject.2. The method of claim 1 , wherein administration of the inhibitor blocks claim 1 , inhibits or interferes with viral spread or viral trafficking within the subject or to another subject.3. The method of claim 1 , wherein administration of the inhibitor blocks claim 1 , inhibits or interferes with viral budding within the subject.4. The method of claim 1 , wherein administration of the inhibitor blocks claim 1 , inhibits or interferes with virus dissemination within the subject or to another subject.5. The method of claim 1 , wherein administration of the inhibitor blocks claim 1 , inhibits or interferes with viral disease progression in the subject or viral disease transmission within the subject or to another subject.6. The method of claim 1 , wherein the virus is selected from the group consisting of a filovirus claim 1 , arenavirus claim 1 , rhabdovirus claim 1 , paramyxovirus claim 1 , retrovirus claim 1 , orthomyxovirus claim 1 , and any combinations thereof.7. The method of claim 6 , wherein the virus is selected from the group consisting of Influenza A claim 6 , Influenza B claim 6 , Influenza C claim 6 , Junin claim 6 , Ebola claim 6 , Marburg claim ...

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Номер записи: 58
13-05-2021 дата публикации

PRODUCTION METHOD OF ORGANIC COMPOUND

Номер: US20210139390A1
Автор: FUKUBAYASHI Yumeto, Nakai Makoto, YANAKA Ayumi
Принадлежит: UNITIKA LTD.

The present invention provides a production method of an organic compound, in which a reaction is performed between functional groups without using any solvents. The present invention relates to a production method of an organic compound, in which a reaction is performed between functional groups by using a mechanochemical effect. 138-. (canceled)39. A production method of an organic compound , wherein a reaction is performed between functional groups by using , a mechanochemicai effect , and wherein the organic compound is a high-molecular compound containing a repeating unit and the high-molecular compound is a polyamic acid-based compound , a polyimide-based compound , or a polyamide-imide-based compound.40. The production method of an organic compound of claim 39 , wherein the reaction is performed in a presence of a terminal blocking agent.41. The production method of an organic compound of claim 39 , wherein the polyamic acid-based compound claim 39 , the polyimide-based compound claim 39 , or a mixture thereof is produced as the organic compound by performing a reaction of a tetracarboxylic dianhydride component with a diamine component or a diisocyanate component claim 39 , as the reaction.42. The production method of an organic compound of claim 41 , wherein the components are used in an amount such that one component has a molar amount of 0.8 to 11 times that of the other component.43. The production method of an organic compound of claim 39 , Wherein the polyaniide-imide-based compound is produced as the organic compound by performing a reaction of a tricarboxylic acid anhydride component or its acid halide component with a diamine component or a diisocyanate component claim 39 , as the reaction.44. The production method of an organic compound of claim 43 , wherein the components are used in an amount such that one component has a molar amount of 0.8 to L2 times that of the other component.45. A production method of an organic compound claim 43 , wherein ...

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Номер записи: 59
13-05-2021 дата публикации

PROSTAGLANDIN ANALOGS AND USES THEREOF

Номер: US20210139435A1
Автор: Han Cheolkyu, Kang Hongjun, Kim Moonhwan, Seo Jeongbeob, Sreekanth Rajan, Yoo Jun Yeob, Yoon Cheolhwan, YOON Ho Sup
Принадлежит:

The present invention relates to pharmaceutical composition for the prevention or treatment of a disease, disorder, or condition associated with Nurr1, including, as an active ingredient, a prostaglandin analog or a pharmaceutically acceptable salt thereof, wherein the compound has excellent effects in inducing Nurr1, and thus, can be useful as a pharmaceutical composition for the prevention or treatment of a disease, disorder, or condition associated with Nurr1, in particular, cancer, autoimmune disease such as rheumatoid arthritis, schizophrenia, manic depression and neurodegenerative disease such as Alzheimers disease or Parkinson's disease. 2. The prostaglandin analog claim 1 , or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , solvate claim 1 , polymorph claim 1 , ester claim 1 , tautomer claim 1 , or prodrug thereof according to claim 1 ,{'sub': a', 'a', 'b, 'wherein X is —(C1-C8) alkyl or —(C1-C8) alkenyl which is optionally substituted with one or more substituents selected from the group consisting of hydroxyl, —(C1-C6) alkoxy, —C(═O)OR, —C(═O)NRR,'}{'sub': a', '2', 'c', 'c', 'c', '3, 'where Ris H, (C1-C8) alkyl, (C6-C9) aryl, (C6-C9) aryloxy, —NH(C6-C9)aryl, 5- to 12-membered heteroaryl having one or more heteroatom selected from the group consisting of N, O and S, said (C1-C8) alkyl, (C6-C9) aryl, 5- to 12-membered heteroaryl may be optionally substituted with halo, hydroxyl, cyano, nitro, amino, substituted amino, (C1-C6)acyl, —ONO, (C1-C8) alkoxy, (C1-C8)alkyl, substituted (C1-C8)alkyl, (C1-C8)haloalkyl, (C3-C7)cycloalkyl, (C1-C8)alkylcarboxy, —NHC(═O)R, or —C(═O)R, where Ris (C1-C8) alkyl or (C6-C9) aryl which may be optionally substituted with one or more substituents of halo, CF, (C1-C6)acyl, amino, substituted amino, cyano, nitro, (C1-C8)alkyl, substituted (C1-C8)alkyl, (C1-C8)haloalkyl, (C1-C8)alkoxy, (C1-C3)acyloxy, and (C6-C9)aryloxy 5- to 12-membered heterocycloalkyl having one or more heteroatoms selected from the group ...

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Номер записи: 60
05-05-2016 дата публикации

COMPOSITIONS INCLUDING 6-AMINOHEXANOIC ACID DERIVATIVES AS HDAC INHIBITORS

Номер: US20160122290A1
Автор: Hopper Allen, Peet Norton P., Rusche James R.
Принадлежит:

This invention relates to compounds of Formula (I) wherein Cy, L, Y, R, L, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions. 2. The compound according to claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein Cyis selected from Cheterocycloalkyl claim 1 , which is substituted with n independently selected Rgroups.3. The compound according to claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein Cyis selected from Caryl claim 1 , which is substituted with n independently selected Rgroups.4. The compound according to claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein Cyis selected from Cheteroaryl claim 1 , which is substituted with n independently selected Rgroups.5. The compound according to claim 4 , or pharmaceutically acceptable salt thereof claim 4 , wherein Cyis indolyl or indazolyl claim 4 , each of which is substituted with n independently selected Rgroups.6. The compound according to claim 4 , or pharmaceutically acceptable salt thereof claim 4 , wherein Cyis indazolyl claim 4 , which is substituted with n independently selected Rgroups.7. The compound or salt of claim 6 , wherein n is 0.8. The compound or salt of claim 6 , wherein n is an integer selected from 1 and 2 claim 6 , and each occurrence of Ris independently selected from Calkyl and Calkoxy claim 6 , wherein said Calkyl and Calkoxy are each optionally substituted by 1 claim 6 , 2 claim 6 , or 3 independently selected R groups.9. The compound according to claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein Cyis selected from phenyl and Cheteroaryl claim 1 , each of which is optionally substituted with n independently selected Rgroups.10. The compound according to claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein Cyis phenyl claim 1 , which is optionally substituted with n independently selected Rgroups.11. The compound according to claim 1 , ...

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Номер записи: 61
12-05-2016 дата публикации

CYCLOPROPANEAMINE COMPOUND

Номер: US20160130215A1
Автор: CARY Douglas Robert, Hara Ryujiro, Imamura Shinichi, Kajii Shigeo, MATSUDA Satoru, Tominari Yusuke, TOMITA Daisuke, Tomita Naoki, Tsuchida Ken
Принадлежит:

The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like. The present invention relates to a compound represented by the formula 2. The compound according to claim 1 , whereinA is{'sub': '3-8', '(1) a Ccycloalkyl group optionally having substituent(s),'}{'sub': '6-14', '(2) a Caryl group optionally having substituent(s),'}{'sub': 6-14', '1-6, '(3) a Caryl Calkyl group optionally having substituent(s),'}{'sub': 6-14', '1-6', '6-14, '(4) a Caryl Calkyl Caryl group optionally having substituent(s),'}(5) a 4- to 11-membered heterocyclic group containing, as a ring-constituting atom besides carbon atom, 1 to 3 hetero atoms selected from a nitrogen atom, a sulfur atom and an oxygen atom, and optionally having substituent(s), or{'sub': '10-14', '(6) a Ccyclic hydrocarbon group optionally having substituent(s);'}{'sub': '1-6', 'R is a hydrogen atom or a Calkyl group optionally having substituent(s); or'}A and R are optionally bonded to each other to form a 4- to 10-membered heterocycle optionally having substituent(s), or a salt thereof.3. The compound according to claim 1 , wherein{'sup': '1', 'sub': '1-6', 'Qis a hydrogen atom or a Calkyl group, and'}{'sup': 2', '3', '4, 'Q, Qand Qare each a hydrogen atom,'}or a salt thereof.4. The compound according to claim 1 , wherein{'sub': '1-6', 'X is a hydrogen atom or an optionally substituted Calkyl group;'}{'sup': 1', '2', '3, 'Y, Yand Yare each independently'}(1) a hydrogen atom,{'sub': '1-20', '(2) a Calkyl group optionally having substituent(s),'}{'sub': '3-8', '(3) a Ccycloalkyl group optionally having substituent(s),'}{'sub': '6-14', '(4) a Caryl group optionally having substituent(s),'}{'sub': 6-14', '1-6, '(5) a Caryl Calkyl group optionally having substituent(s),'}(6) a 5- to 7-membered monocyclic aromatic heterocyclic group containing, as a ring- ...

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Номер записи: 62
10-05-2018 дата публикации

SYNTHESIS OF NON-CYCLIC AMIDE AND THIOAMIDE BASED IONIC LIQUIDS

Номер: US20180127352A1
Автор: Bhattacharyya Alakananda, Broderick Erin M., Buchbinder Avram M.
Принадлежит:

Non-cyclic amide or thioamide based ionic liquids and methods of making them are disclosed. The non-cyclic amide or thioamide based ionic liquid comprises a cation and an anion and has the formula: 2. The ionic liquid of wherein the anion is a carboxylate claim 1 , a nitrate claim 1 , a phosphate claim 1 , a phosphinate claim 1 , a phosphonate claim 1 , an imide claim 1 , a cyanate claim 1 , a borate claim 1 , a sulfate claim 1 , a sulfonate claim 1 , an acetate claim 1 , a halide claim 1 , a halometallate claim 1 , and combinations thereof.3. The ionic liquid of wherein the anion is the halide and wherein the halide is bromide claim 1 , chloride claim 1 , iodide claim 1 , fluoride claim 1 , or combinations thereof.4. The ionic liquid of wherein the anion is the halometallate claim 1 , wherein the metal in the halometallate comprises Sn claim 1 , Al claim 1 , Zn claim 1 , Mn claim 1 , Fe claim 1 , Ga claim 1 , Cu claim 1 , Ni claim 1 , Co claim 1 , In claim 1 , or combinations thereof claim 1 , and wherein the halide in the halometallate comprises bromide claim 1 , chloride claim 1 , iodide claim 1 , fluoride claim 1 , or combinations thereof claim 1 , and wherein the halometallate optionally includes an —OH group.5. The ionic liquid of wherein the anion is the halometallate claim 1 , and wherein the halometallate comprises AlCl claim 1 , AlCl claim 1 , AlCl claim 1 , AlClBr claim 1 , AlClBr claim 1 , AlClBr claim 1 , AlBr claim 1 , AlBr claim 1 , AlBr claim 1 , GaCl claim 1 , GaCl claim 1 , GaCl claim 1 , GaClBr claim 1 , GaClBr claim 1 , GaClBr claim 1 , CuCl claim 1 , CuCl claim 1 , CuCl claim 1 , ZnCl claim 1 , FeCl claim 1 , FeCl claim 1 , FeCl claim 1 , InCl claim 1 , InCl claim 1 , InCl claim 1 , or combinations thereof.6. The ionic liquid of wherein the cation comprises N claim 1 ,N-dimethylacetamidium claim 1 , acetamidium claim 1 , carbonyl diamidium claim 1 , thioamidium claim 1 , N-methylthioacetamidium claim 1 , N claim 1 ,N-dimethylthioacetamidium ...

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Номер записи: 63
01-09-2022 дата публикации

DUAL MODULATOR OF MGLUR5 AND 5-HT2A RECEPTOR, AND USE THEREOF

Номер: US20220274939A1
Автор: BAE Mi Seon, Choi Dae Kyu, Choi Jin, HEO Hyun Jin, KIM Hyo Jin, LEE Geon Ho, LEE Han Mi, LEE Yong Seok, PARK Jin Sun, Shim Mi Yon
Принадлежит:

Disclosed are a dual modulator of mGluR5 and 5-HT2AR (5-HT2A receptor), and use thereof. More specifically, disclosed are a compound which acts as modulator of mGluR5 and an antagonist of 5-HT2AR at the same time, and use thereof as therapeutic agent for pain. 2. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein{'sub': 1', '2', '4', '7, 'Xand Xtogether with carbon atom to which they are attached form C-Ccycloalkyl or 4- to 6-membered heterocycloalkyl;'}{'sub': '3', 'Xis CH or N;'}{'sub': 1', '1', '8, 'Ris hydroxy, halo or C-Calkyl;'}{'sub': 2', '1', '8', '1', '5', '1', '5', '1', '5', '1', '5', '3', '6', '1', '5', '3', '6', '1', '5', '1', '5', '1', '5', '1', '5', '1', '8', '1', '8', '1', '8', '1', '8', '1', '5', '1', '5', '1', '5, 'Ris hydroxy, halo, C-Calkyl, C-Calkoxy, 4- to 6-membered heterocycloalkyl, hydroxy-C-Calkyl, halo-C-Calkyl, C-Calkylamino, C-Ccycloalkyl-C-Calkyl, C-Ccycloalkylamino, halo-C-Calkylamino, C-Calkylaminocarbonyl, C-Calkoxycarbonyl-C-Calkyl, carboxy-C-Calkyl, aminocarbonyl-C-Calkyl, hydroxyaminocarbonyl-C-Calkyl, C-Calkylaminocarbonyl-C-Calkyl, di(C-Calkyl)aminocarbonyl-C-Calkyl or pyridyl;'}{'sub': 3', '1', '8, 'Ris deuterium, fluoro or C-Calkyl;'}{'sub': 4', '5', '1', '5, 'Rand Rare each independently halo or C-Calkyl;'}m is an integer of 0 to 2;n is 0 or 1; andl, p and q are each independently an integer of 0 to 2;wherein the heterocycloalkyl has 1 to 3 heteroatoms selected from the group consisting of N and O.3. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the 4- to 7-membered aliphatic ring is cyclobutane claim 1 , cyclopentane claim 1 , cyclohexane or cycloheptane.4. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the 4- to 6-membered heteroaliphatic ring is oxetane claim 1 , tetrahydrofuran claim 1 , tetrahydropyran claim 1 , dioxane or piperidine.5. The compound or pharmaceutically acceptable salt thereof according ...

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Номер записи: 64
18-05-2017 дата публикации

6-AMINO-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL OR 3-AMINOCHROMAN-7-YL DERIVATIVES

Номер: US20170137416A1
Автор: Cecere Giuseppe, Galley Guido, Goergler Annick, Norcross Roger, Pflieger Philippe, Schmid Philipp, Tirla Alina
Принадлежит: Hoffmann-La Roche Inc.

The present invention relates to compounds TAAR receptor antagonists of formula I wherein X, R, L, Ar and Rare as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I. 2. The compound according to wherein L is —C(O)NH—.3. The compound according to claim 2 , said compound selected from the group consisting of:N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-(trifluoromethyl)isonicotinamide;N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-4-bromo-5-cyclopropyl-1H-pyrazole-3-carboxamide;N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-6-methyl-2-(trifluoromethyl)-pyrimidine-4-carboxamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-6-methyl-2-(trifluoromethyl)-pyrimidine-4-carboxamide;N-(3-aminochroman-7-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;N-(3-aminochroman-7-yl)-6-methyl-2-(trifluoromethyl)pyrimidine-4-carboxamide;(R)—N-(3-aminochroman-7-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(S)—N-(3-aminochroman-7-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(R)—N-(3-aminochroman-7-yl)-6-methyl-2-(trifluoromethyl)pyrimidine-4-carboxamide;(S)—N-(3-aminochroman-7-yl)-6-methyl-2-(trifluoromethyl)pyrimidine-4-carboxamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-4-chlorobenzamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-chlorobenzamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-methylisonicotinamide;(S)-2-acetamido-N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)isonicotinamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-ethoxyisonicotinamide;(S ...

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Номер записи: 65
10-06-2021 дата публикации

1,4-DISUBSTITUTED IMIDAZOLE DERIVATIVE

Номер: US20210171440A1
Автор: Ban Hitoshi, Hasegawa Futoshi, Hashizume Miki, Kusagi Manabu, Tojo Shingo
Принадлежит:

The present invention provides a 1,4-disubstituted imidazole derivative of formula (1′) wherein ring Qis optionally-substituted Caryl group, etc.; Rand Rare independently hydrogen atom, etc.; Wis optionally-substituted Calkylene group; Wis —NRC(O)— wherein Ris hydrogen atom or Calkyl group, etc.; ring Qis 5- to 10-membered heteroaryl group, etc.; Wis optionally-substituted Calkylene group, etc.; n is 1, 2, 3, 4, or 5; Ris independently halogen atom, optionally-substituted Calkyl group, etc.; Ris hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent. 141-. (canceled)52. A method of treating a cancer claim 42 , administering a therapeutically effective amount of the compound of formula (1-7) claim 42 , or a pharmaceutically acceptable salt thereof claim 42 , to a patient in need thereof claim 42 , the compound of formula (1-7) is prepared by the process according to .53. A method of treating a cancer in a patient in need thereof claim 42 , comprising administering to the patient a therapeutically effective amount of a compound of formula (1-7) claim 42 , or a pharmaceutically acceptable salt thereof claim 42 , in combination with an additional anti-cancer agent selected from the group consisting of an anti-cancerous alkylating agent claim 42 , an anti-cancerous antimetabolite claim 42 , an anti-cancerous antibiotic claim 42 , a plant-based anti-cancer agent claim 42 , an anti-cancerous platinum coordination compound claim 42 , an anti-cancerous camptothecin derivative claim 42 , an anti-cancerous tyrosine kinase inhibitor claim 42 , a serine-threonine kinase claim 42 , a phospholipid kinase claim 42 , a monoclonal antibody claim 42 , an interferon claim 42 , a biological response modifier claim 42 , a hormone preparation claim 42 , an immune checkpoint inhibitor claim 42 , an epigenetics-related molecule inhibitor ...

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Номер записи: 66
25-05-2017 дата публикации

METHODS OF LOWERING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9)

Номер: US20170144972A1
Автор: Jirousek Michael R., Milne Jill C., Vu Chi B.
Принадлежит:

The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases. 120-. (canceled)2298-. (canceled)103. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.104. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.105. A method for treating a metabolic disease in a subject in need thereof claim 21 , the method comprising administering an effective amount of a compound of to the subject.106. The method of claim 105 , wherein the metabolic disease is selected from hypertriglyceridemia claim 105 , severe hypertriglyceridemia claim 105 , hypercholesterolemia claim 105 , familial hypercholesterolemia claim 105 , elevated cholesterol caused by a genetic condition claim 105 , fatty liver disease claim 105 , nonalcoholic fatty liver disease (NFLD) claim 105 , nonalcoholic steatohepatitis (NASH) claim 105 , dyslipidemia claim 105 , mixed dyslipidemia claim 105 , Type I hyperlipoproteinemia claim 105 , Type V hyperlipoproteinemia claim 105 , atherosclerosis claim 105 , coronary heart disease claim 105 , Type 2 diabetes claim 105 , diabetic nephropathy claim 105 , diabetic neuropathy claim 105 , diabetic retinopathy claim 105 , metabolic syndrome claim 105 , or cardiovascular disease.107. The method of claim 105 , wherein the metabolic disease is hypertriglyceridemia.108. The method of claim 105 , wherein the metabolic disease is hypercholesterolemia.109. A method for treating a metabolic disease by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) by administering to a patient in need thereof an effective amount of a ...

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Номер записи: 67
14-08-2014 дата публикации

Cyclopropaneamine compound

Номер: US20140228405A1
Автор: Daisuke Tomita, Douglas Robert CARY, Ken Tsuchida, Naoki Tomita, Ryujiro HARA, Satoru Matsuda, Shigeo KAJII, Shinichi Imamura
Принадлежит: Takeda Pharmaceutical Co Ltd

The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like. The present invention relates to a compound represented by the formula wherein A is a hydrocarbon group or heterocyclic group optionally having substituent(s); R is H, a hydrocarbon group or heterocyclic group optionally having substituent(s); A and R are optionally bonded to each other to form a ring optionally having substituent(s); Q 1 , Q 2 , Q 3 and Q 4 are each a hydrogen atom or a substituent; Q 1 and Q 2 , and Q 3 and Q 4 , are each optionally bonded to each other to form a ring optionally having substituent(s); X is H, an acyclic hydrocarbon group or saturated cyclic group optionally having substituent(s); Y 1 , Y 2 and Y 3 are each H, a hydrocarbon group or heterocyclic group optionally having substituent(s); X and Y 1 , and Y 1 and Y 2 , are each optionally bonded to each other to form a ring optionally having substituent(s); and Z 1 , Z 2 and Z 3 are each H or a substituent, or a salt thereof.

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Номер записи: 68
16-05-2019 дата публикации

PROTEASOME INHIBITORS

Номер: US20190144470A1
Автор: Danca Mihaela Diana, Olhava Edward J.
Принадлежит:

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The method of claim 1 , wherein Zand Zare each hydroxy.3. The method of claim 1 , wherein Zand Ztogether form a moiety derived from a boronic acid complexing agent.6. The method of claim 1 , wherein the compound of formula (I) is selected from:[(1R)-1-({[(2,3-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(5-chloro-2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,5-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,5-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-bromobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chloro-5-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,4-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,5-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,4-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chloro-4-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,3-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,4-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-chloro-2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1 ...

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Номер записи: 69
17-06-2021 дата публикации

Method for Producing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclo-propylpropanoic Acid and the Crystalline Form Thereof for Use as a Pharmaceutical Ingredient

Номер: US20210179541A1
Автор: FEY Peter, Kusel Julia, Lovis Kai, Olenik Britta, Rubenbauer Philipp, SPINDLER Felix
Принадлежит: BAYER PHARMA AKTIENGESELLSCHAFT

The present invention relates to a novel and improved process for preparing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid of the formula (I), to the compound of the formula (I) in crystalline form and to their use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular, cardiopulmonary and cardiorenal disorders. 6. The process according to claim 5 , further comprising purifying the compound of the formula (II-Ch) in a first step by crystallization from a mixture of water and methanol in a ratio of from 1:1 to 1:5 and in a second step by crystallization from a mixture of water and ethanol in a ratio of from 1:1 to 1:10. The present invention relates to a novel and improved process for preparing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid of the formula (I)in particular of the compound of formula (I) in crystalline modification 1 (I-1), and to its use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular, cardiopulmonary and cardiorenal disorders.In the context of this invention, (I-A) refers to the compound of the formula (I) in amorphous form; the crystalline modification 1 is referred to as (I-1). Without further differentiation, the compound of the formula (I) is present in one or more modifications or as a solvate.The compound of the formula (I) and the compound of the formula (I) in crystalline modification 1 (I-1) act as activators of soluble guanylate cyclase and can be employed as agents for the prophylaxis and/or treatment of cardiovascular disorders and in particular renal disorders, for example for the treatment of chronic kidney disease (CKD).The compound of the formula (I) in amorphous form (I-A) and its preparation process are described in the patent application WO 2012/139888. ...

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Номер записи: 70
31-05-2018 дата публикации

CHARGE-TRANSPORTING VARNISH, AND ORGANIC ELECTROLUMINESCENT ELEMENT

Номер: US20180151805A1
Автор: ENDO Toshiyuki, NAKAZAWA Taichi
Принадлежит: NISSAN CHEMICAL INDUSTRIES, LTD.

Provided are: a charge-transporting varnish that contains a charge-transporting substance comprising an oligoaniline derivative represented by formula (1), a charge transporting substance that does not contain fluorine atoms, and an organic solvent; and an organic electroluminescent element including a thin film obtained from the varnish. 2. The charge-transporting varnish of claim 1 , wherein letter A is a fluoroalkyl group having 1 to 20 carbon atoms which may be substituted with a cyano group claim 1 , chlorine atom claim 1 , bromine atom claim 1 , iodine atom claim 1 , nitro group or fluoroalkoxy group having 1 to 20 carbon atoms; a fluoroaryl group having 6 to 20 carbon atoms which may be substituted with a cyano group claim 1 , chlorine atom claim 1 , bromine atom claim 1 , iodine atom claim 1 , nitro group claim 1 , alkyl group having 1 to 20 carbon atoms claim 1 , fluoroalkyl group having 1 to 20 carbon atoms or fluoroalkoxy group having 1 to 20 carbon atoms; or an aryl group having 6 to 20 carbon atoms is substituted with a fluoroalkyl group having 1 to 20 carbon atoms claim 1 , fluorocycloalkyl group having 3 to 20 carbon atoms claim 1 , fluorobicycloalkyl group having 4 to 20 carbon atoms claim 1 , fluoroalkenyl group having 2 to 20 carbon atoms or fluoroalkynyl group having 2 to 20 carbon atoms claim 1 , and may be substituted with a cyano group claim 1 , halogen atom claim 1 , or fluoroalkoxy group having 1 to 20 carbon atoms.3. The charge-transporting varnish of claim 2 , wherein letter A is a phenyl group which is substituted with at least 3 fluorine atoms claim 2 , and may be substituted with a cyano group claim 2 , chlorine atom claim 2 , bromine atom claim 2 , iodine atom claim 2 , nitro group claim 2 , alkyl group having 1 to 20 carbon atoms claim 2 , fluoroalkyl group having 1 to 20 carbon atoms or fluoroalkoxy group having 1 to 20 carbon atoms; or a phenyl group which is substituted with a fluorocycloalkyl group having 3 to 20 carbon atoms claim ...

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Номер записи: 71
23-05-2019 дата публикации

BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

Номер: US20190152997A1
Автор: Elliott Eric L., Ferdous Abu J., Kaufman Michael J., Komar-Lay Sonja A., Maccubbin Quentin J., Mazaik Debra L., Nguyen Phuong M., Palaniappan Valthlanathan, Skwierczynski Raymond D., Truong Nobel T., Varga Csnad M., Zawaneh Peter N.
Принадлежит:

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 131.-. (canceled)33. A pharmaceutical composition comprising a compound of claim 32 , or pharmaceutically acceptable salt thereof claim 32 , and a pharmaceutically acceptable carrier.34. The pharmaceutical composition of claim 33 , wherein the compound is present in an amount of about 0.2% to about 12% by weight as a percentage of total weight.35. The pharmaceutical composition of claim 33 , wherein the compound of formula (II) is present in an amount of about 0.2% to about 3% by weight as a percentage of total weight.36. The pharmaceutical composition of claim 33 , wherein the pharmaceutical composition optionally comprising a buffer.37. The pharmaceutical composition of claim 33 , wherein the pharmaceutical composition optionally comprising sodium citrate claim 33 , or citric acid claim 33 , or mixtures thereof.38. The pharmaceutical composition of claim 33 , wherein the compound is formed in situ from the corresponding boronic acid.40. The pharmaceutical composition of claim 39 , further comprising the boronic acid of formula (VIII-15).41. The pharmaceutical composition of any one of - claim 39 , wherein the pH of the pharmaceutical composition is between about pH 4.7 and pH 6.1.42. The pharmaceutical composition of claim 41 , wherein the pH is adjustable using an inorganic acid or organic acid.43. The pharmaceutical composition of claim 33 , wherein the composition is manufactured by a granulating claim 33 , mixing claim 33 , dissolving claim 33 , encapsulating claim 33 , lyophilizing claim 33 , or emulsifying process.44. The pharmaceutical composition of claim 43 , wherein the composition is manufactured by a lyophilizing process.45. The pharmaceutical composition of any one of - claim 43 , wherein the ...

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Номер записи: 72
24-06-2021 дата публикации

COMPOUNDS AND METHODS FOR HEMATOPOIETIC REGENERATION

Номер: US20210188763A1
Автор: Chute John P., DIERS Emelyne, Gim Hyo Jin, Jung Michael E., Roos Martina
Принадлежит:

The invention relates to compounds that promote hematopoietic regeneration. The invention further relates to methods of promoting hematopoietic regeneration using the novel compounds of the invention. 2. (canceled)3. (canceled)4. The compound of claim 1 , wherein Ais phenyl.5. The compound of claim 1 , wherein Q and T are both CH or Q and T are both N.6. (canceled)7. The compound of claim 1 , wherein the compound is represented by formula II.8. The compound of claim 7 , wherein the alkene stereochemistry is in the E configuration.9. (canceled)12. The compound of claim 7 , wherein Ais aryl claim 7 , heteroaryl claim 7 , cycloalkyl or heterocyclyl.1316-. (canceled)17. The compound of claim 7 , wherein Ris hydrogen.18. The compound of claim 1 , wherein the compound is represented by formula III.19. The compound of claim 18 , wherein Ais aryl.20. (canceled)21. The compound of claim 18 , wherein L is —N(R)C(═X)— or —C(═X)N(R)—.22. (canceled)23. The compound of claim 18 , wherein Ris hydrogen.24. The compound of claim 18 , wherein the alkene stereochemistry is in the Z configuration.25. The compound of claim 1 , wherein X is oxygen.26. The compound of claim 1 , wherein B is aryl.2729-. (canceled)31. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable excipient.32. A method of inhibiting PTPσ in a cell claim 1 , comprising contacting the cell with a compound of .33. A method of promoting the self-renewal or regeneration of hematopoietic stem cells comprising administering to a subject in need thereof a compound of .3439-. (canceled) This application claims the benefit of U.S. Provisional Application No. 62/592,303, filed Nov. 29, 2017, the contents of which are fully incorporated by reference herein.This invention was made with Government support under AI067769, awarded by the National Institutes of Health. The Government has certain rights in the invention.Hematopoietic stem cells (HSCs) possess the unique capability to ...

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Номер записи: 73
16-06-2016 дата публикации

DI(HETERO)ARYLAMIDES AND SULFONAMIDES, METHODS FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF

Номер: US20160168132A1
Автор: AYMAMI BOFARULL Juan, BARRIL ALONSO Xavier, GARCÍA COLLAZO Ana Maria, LAVILLA GRIFOLS Rodolfo, MARTINELL PEDEMONTE Marc, Revés Vilaplana Marc
Принадлежит: Minoryx Therapeutics S.L.

The present invention refers to compounds of formula (I): as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of conditions associated with the alteration of the activity of β-galactosidase, specially galactosidase beta-1 or GLB1, including GM1 gangliosidoses and Morquio syndrome, type B. 2. A compound for use according to wherein G is a group —C(═O)—.3. A compound for use according to anyone of and wherein Ris selected from chloro claim 1 , bromo and —CF.4. A compound for use according to anyone of to wherein Ris selected from hydrogen claim 1 , halogen claim 1 , —ORa and —Calkyl optionally substituted with 1 claim 1 , 2 or 3 groups independently selected from halogen claim 1 , hydroxy claim 1 , —Calkyl claim 1 , —N(Rb) claim 1 , methoxy claim 1 , -haloCalkyl claim 1 , -dihaloCalkyl claim 1 , -trihaloCalkyl claim 1 , halomethoxy claim 1 , dihalomethoxy claim 1 , and trihalomethoxy.5. A compound for use according to anyone of to wherein Ra and Rb are independently selected from —Calkyl claim 1 , —Ccycloalkyl claim 1 , —Caryl claim 1 , —Cheteroaryl claim 1 , and —Cheterocyclyl; said alkyl claim 1 , cycloalkyl claim 1 , aryl claim 1 , heteroaryl claim 1 , or heterocyclyl groups optionally being substituted with 1 claim 1 , 2 or 3 groups independently selected from halogen claim 1 , hydroxy claim 1 , amine claim 1 , —Calkyl claim 1 , —CN claim 1 , methoxy claim 1 , substituted aryl claim 1 , substituted heteroaryl claim 1 , -haloCalkyl claim 1 , -dihaloCalkyl claim 1 , -trihaloCalkyl claim 1 , halomethoxy claim 1 , dihalomethoxy and trihalomethoxy.6. A compound for use according to anyone of to wherein Rc and Rd are independently selected from —Calkyl claim 1 , —Caryl claim 1 , and —Cheterocyclyl; said alkyl claim 1 , cycloalkyl claim 1 , aryl or heterocyclyl groups optionally being substituted with 1 claim 1 , 2 or 3 groups independently selected from halogen claim 1 , ...

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Номер записи: 74
29-09-2022 дата публикации

SMALL MOLECULE INHIBITORS OF A PROTEIN COMPLEX

Номер: US20220304958A1
Автор: Ballatore Carlo, FRANCISCO Karol Rogelle Karagdag, Gingras Alexandre, GINSBERG, Mark, Sklar Larry
Принадлежит:

Compositions and methods for treating thrombosis, inflammation, and atherosclerosis by administration of a compound that binds to KRIT1 to inhibit binding with HEG1. 1. A method of treating a disease in a subject by reducing thrombosis , atherosclerosis , or inflammation comprising administering to a subject in need an effective amount of a Siritol compound or salt thereof that binds to KRIT1 FERM domain to inhibit binding with HEG1.2. The method of claim 1 , wherein the disease is rheumatoid arthritis claim 1 , gout claim 1 , spondyloarthritis claim 1 , vasculitis claim 1 , adult respiratory distress syndrome claim 1 , post-perfusion injury claim 1 , glomerulonephritis claim 1 , cytokine storm claim 1 , myocardial infarction claim 1 , stroke claim 1 , deep vein thrombosis claim 1 , pulmonary embolus claim 1 , thrombotic thrombocytopenic purpura claim 1 , COVID-19 claim 1 , coronary artery disease claim 1 , carotid atherosclerosis claim 1 , cerebrovascular disease claim 1 , vascular dementia claim 1 , or aortic aneurysm.4. The method of claim 3 , wherein the compound is selected from the group consisting of HKi1 claim 3 , HKi2 claim 3 , HKi5 claim 3 , BL-0549 claim 3 , BL-0558 claim 3 , BL-0552 claim 3 , BL-0628 claim 3 , BL-0661 claim 3 , BL-0666 claim 3 , BL-0670 claim 3 , BL-0691 claim 3 , BL-0693 claim 3 , BL-0700 claim 3 , BL-702 claim 3 , BL-0736 claim 3 , BL-0737 claim 3 , BL-0738 claim 3 , BL-0739 claim 3 , BL-0740 claim 3 , BL-0742 claim 3 , BL-0743 claim 3 , BL-0744 claim 3 , BL-0745 claim 3 , BL-0788 claim 3 , BL-0794 claim 3 , BL-0817 claim 3 , BL-0818 claim 3 , and BL-0819.5. The method of claim 3 , wherein the Sirtinol derivative comprises an aldehyde moiety.6. The method of claim 1 , wherein the administering upregulates endothelial nitric oxide synthase claim 1 , thrombomodulin 1 claim 1 , vascular endothelial growth factor A claim 1 , Thrombospondin 1 claim 1 , Monocyte chemoattractant protein claim 1 , or C-X-C chemokine receptor type 4.7. The ...

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Номер записи: 75
25-06-2015 дата публикации

SECONDARY AMINES AS THERAPEUTIC AGENTS

Номер: US20150175567A1
Автор: Ngo Vinh X., Old David W.
Принадлежит:

Compounds such as those represented by Formulas 1-6 can be used in topical liquids, creams, or other dosage forms such as solids, for reducing intraocular pressure, treating glaucoma, growing hair, or other medical uses. 2. The compound of claim 1 , wherein a is 1.3. The compound of claim 1 , wherein a is 2.4. The compound of claim 1 , wherein Ris H.5. The compound of claim 1 , wherein Ris H.6. The compound of claim 1 , wherein Ris H.7. The compound of claim 1 , wherein W is CH.8. The compound of claim 1 , wherein W is O.9. The compound of claim 1 , wherein X is NR.10. The compound of claim 9 , wherein Ris H.11. The compound of claim 9 , wherein Ris Calkyl claim 9 , or COCH.12. The compound of claim 1 , wherein X is O.13. The compound of claim 1 , wherein L is -A-OCH—.14. The compound of claim 1 , wherein A is interphenylene.15. The compound of claim 1 , wherein Q is COR.16. The compound of claim 1 , wherein Q is CHOH.17. The compound of claim 1 , wherein B is 3-fluorophenyl.19. An ophthalmic liquid comprising a compound according to .20. A solid dosage form comprising a compound according to .21. An ophthalmic liquid comprising a compound according to .22. A solid dosage form comprising a compound according to .23. A method of reducing intraocular pressure comprising administering a compound according to to a mammal in need thereof.24. A method or growing hair comprising administering a compound according to to a mammal in which hair growth is desirable. This application claims priority to and the benefit of U.S. Provisional Patent Application No. 61/919,557, filed Dec. 20, 2013, the disclosure of which is hereby incorporated by reference in its entirety.Ocular hypotensive agents are useful in the treatment of a number of various ocular hypertensive conditions, such as post-surgical and post-laser trabeculectomy ocular hypertensive episodes, glaucoma, and as pre-surgical adjuncts.Glaucoma is a disease of the eye characterized by increased intraocular pressure. On ...

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Номер записи: 76
01-07-2021 дата публикации

BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

Номер: US20210198289A1
Автор: Elliott Eric L., Ferdous Abu J., Kaufman Michael J., Komar-Lay Sonja A., Mazaik Debra L., Mccubbin Quentin J., Nguyen Phuong M., Palaniappan Vaithianathan, Skwierczynski Raymond D., Truong Nobel T., Varga Csanad M., Zawaneh Peter N.
Принадлежит:

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The process of claim 1 , wherein the reaction of step (1) or step (3) or both is conducted in the presence of a peptide coupling reagent.3. The process of claim 2 , wherein the peptide coupling reagent is selected from the group consisting of a carbodiimide reagent claim 2 , phosphonium reagent claim 2 , and uronium reagent.4. The process of claim 3 , wherein the peptide coupling reagent is selected from one or more of the group consisting of dicyclohexylcarbodiimide (DCC) claim 3 , 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC) claim 3 , benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) claim 3 , and Of 1H-benzotriazol-1-yl-N claim 3 ,N claim 3 ,N′ claim 3 ,N′-tetramethyluronium tetrafluoroborate (TBTU).5. The process of claim 1 , further comprising converting the carboxylic acid moiety of compound (ii) to an activated ester or acid halide prior to the reaction of step (1).6. The process of claim 5 , wherein said activated ester or acid halide is an O-(N-hydroxysuccinnimide) ester.7. The process of claim 1 , wherein the reaction of step (3) is conducted in the presence of a solvent.8. The process of claim 7 , wherein the solvent is tetrahydrofuran.9. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an aqueous mineral acid.10. The process of claim 9 , wherein the mineral acid is hydrochloric acid.11. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an organic boronic acid acceptor.12. The process of claim 11 , wherein the organic boronic acid acceptor is i-BuB(OH).13. The process of claim 1 , wherein the reaction of step (5) is conducted in the presence of a solvent selected from the group consisting ...

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Номер записи: 77
21-06-2018 дата публикации

PPAR AGONISTS

Номер: US20180170857A1
Автор: Baiga Thomas J., BOCK Mark G., Downes Michael, Embler Emi Kanakubo, Evans Ronald M., Fan Weiwei, Keana John F.W., Kluge Authur F., Noel Joseph P., Patane Mike A.
Принадлежит:

Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases). 3. The compound of claim 1 , wherein ring B is selected from phenyl claim 1 , pyridine claim 1 , thiophene claim 1 , thiazole claim 1 , pyrazole claim 1 , oxazole claim 1 , isoxazole claim 1 , benzo[b]furan claim 1 , indazole claim 1 , piperidine claim 1 , cyclohexane claim 1 , piperidin-2-one claim 1 , piperazine-2 claim 1 ,5-dione or quinazolin-4(3H)-one.6. The compound of claim 1 , wherein Ris selected from alkyl claim 1 , heteroalkyl claim 1 , cycloalkyl claim 1 , heterocycloalkyl claim 1 , aryl or heteroaryl.7. The method of claim 1 , wherein L claim 1 , Land Lare each independently selected from a bond or alkylene.8. The compound of claim 1 , wherein LRis isopropyl claim 1 , cyclopropyl claim 1 , cyclopentyl claim 1 , sec-butyl claim 1 , benzyl claim 1 , morpholinopropyl claim 1 , or (2-pyridinyl)ethyl.9. The compound of claim 1 , wherein each Rindependently is Cl claim 1 , F claim 1 , I claim 1 , Br claim 1 , cyano claim 1 , NO claim 1 , or OH.10. The compound of claim 1 , wherein each Rindependently is halogen claim 1 , alkyloxy claim 1 , haloalkyloxy claim 1 , cycloalkyloxy claim 1 , haloalkyl claim 1 , alkyl claim 1 , amino claim 1 , heterocyclic claim 1 , aryl claim 1 , cycloaliphatic or heteroaryl.11. The compound of claim 1 , wherein n is from 2 to 4 claim 1 , and two adjacent Rgroups form a fused ring system with ring B.13. The compound of claim 1 , wherein n is 1 and Ris furan-2-yl or furan-3-yl.15. The compound of claim 1 , wherein Lis Clinear or branched alkylene.16. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of .17. A method claim 1 , comprising contacting a PPARδ protein with an effective amount of one or more compounds of ...

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Номер записи: 78
08-07-2021 дата публикации

PROTEASOME INHIBITORS

Номер: US20210206784A1
Автор: Danca Mihaela Diana, Olhava Edward J.
Принадлежит:

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The method of claim 1 , wherein Zand Zare each hydroxy.3. The method of claim 1 , wherein Zand Ztogether form a moiety derived from a boronic acid complexing agent.6. The method of claim 1 , wherein the compound of formula (I) is selected from:[(1R)-1-({[(2,3-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(5-chloro-2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,5-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,5-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-bromobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chloro-5-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,4-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,5-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,4-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chloro-4-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,3-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,4-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-chloro-2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1 ...

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Номер записи: 79
04-06-2020 дата публикации

DUAL MODULATORS OF FARNESOID X RECEPTOR AND SOLUBLE EPOXIDE HYDROLASE

Номер: US20200172473A1
Автор: Helmstaedter Moritz, Merk Daniel, Proschak Ewgenij, Schmidt Jurema, SCHUBERT-ZSILAVECZ Manfred
Принадлежит:

The present invention pertains to novel dual modulators of farnesoid X receptor (FXR) and soluble epoxide hydrolase (sEH). The modulators of the invention were designed to provide compounds which harbor a dual activity as agonists of FXR and inhibitors (antagonists) of sEH. The invention also provides methods for treating subjects suffering from diseases associated with FXR and sEH, such as metabolic disorders, in particular non-alcoholic fatty liver or nonalcoholic steatohepatitis (NASH). 2. The compound according to claim 1 , wherein Ris C-Calkyl claim 1 , preferably a branched alky claim 1 , more preferably —C(CH) claim 1 , preferably Ris H claim 1 , —OH or —OMe claim 1 , and preferably Ris H claim 1 , —OH or —OMe.3. The compound according to claim 1 , wherein Ris a mono or polysubstituted aryl.7. The compound according to claim 1 , which is a farnesoid X receptor (FXR) agonist and a soluble epoxide hydrolase (sEH) inhibitor.8. The compound according to claim 1 , for use in the treatment of a disease.9. The compound for use according to claim 8 , wherein the disease is a disorder associated with FXR and sEH.10. The compound for use according to claim 8 , wherein the disease is a metabolic disorder claim 8 , preferably a metabolic disorder caused by or associated with a high-fat diet.11. The compound for use according to claim 8 , wherein the disease is a liver disease claim 8 , such as non-alcoholic fatty liver disease or non-alcoholic steatohepatitis (NASH).12. A method for producing a compound according to any .13. A pharmaceutical composition comprising a compound according to claim 1 , together with a pharmaceutical acceptable carrier and/or excipient.14. A method for concomitant modulation of FXR and sEH claim 1 , the method comprising the step of administering to a subject a compound according to .15. The method according to claim 14 , wherein the subject is suffering from a disease claim 14 , preferably a metabolic disease.16. The method according to claim ...

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Номер записи: 80
18-09-2014 дата публикации

NOVEL SOLID FORMS OF TACEDINALINE

Номер: US20140275268A1
Автор: Holson Edward, Stahly G. Patrick, Wagner Florence F.
Принадлежит: THE BROAD INSTITUTE, INC.

Novel solid forms of tacedinaline (4-(acetylamino)-N-(2-aminophenyl)benzamide), including crystalline tacedinaline Form B, a novel crystalline tacedinaline TFA salt, and amorphous tacedinaline, are disclosed. Pharmaceutical compositions comprising crystalline tacedinaline Form B, the novel crystalline tacedinaline TFA salt, and/or amorphous tacedinaline, and methods of treating various conditions by administering those novel solid forms, are also disclosed. 1. A solid form of crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form B (tacedinaline Form B) , crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide TFA salt , or amorphous 4-(acetylamino)-N-(2-aminophenyl)benzamide.2. A pharmaceutical composition comprising at least one of the solid forms of 4-(acetylamino)-N-(2-aminophenyl)benzamide of .3. A pharmaceutical formulation comprising at least one of the solid forms of 4-acetylamino)-N-(2-aminophenyl)benzamide of and a pharmaceutically acceptable carrier.4. The pharmaceutical formulation of or claim 1 , wherein the solid form is a solid unit dosage form.5. A pharmaceutical formulation comprising at least one of the solid forms of 4-(acetylamino)-N-(2-aminophenyl)benzamide of claim 1 , wherein the solid form has improved thermal stability relative to tacedinaline Form C.6. A pharmaceutical formulation comprising at least one of the solid forms of 4-(acetylamino)-N-(2-aminophenyl)benzamide of claim 1 , wherein the solid form does not contain methanol.7. A pharmaceutical formulation comprising at least one of the solid forms of 4-(acetylamino)-N-(2-aminophenyl)benzamide of claim 1 , wherein the solid form is more soluble than tacedinaline Form A or tacedinaline Form D.8. A method of preparing a solid form of 4-(acetylamino)-N-(2-aminophenyl)benzamide claim 1 , comprising preparing any of crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form B claim 1 , crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide TFA salt claim 1 , or amorphous 4-(acetylamino ...

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Номер записи: 81
22-07-2021 дата публикации

Compounds and Methods for Inhibiting CPY26 Enzymes

Номер: US20210220326A1
Автор: Board Johnathan, Cameron Donald Andrew, Maheta Ashishkumar Jayantilal, Petkovich Martin, Rantanen Toni Kristian, Singh Suneel, Snieckus Victor
Принадлежит:

Compounds described herein are inhibitors of retinoic acid inducible P450 (CYP26) enzymes, and are useful for treating diseases that are responsive to retinoids. Certain compounds have retinoid activity, are resistant to CYP26-mediated catabolism, and are used for treating diseases that are responsive to retinoids. 2. The method of claim 1 , wherein the disease or condition is a skin disease.3. The method of claim 2 , wherein the skin disease is actinic keratosis claim 2 , arsenic keratosis claim 2 , inflammatory and non-inflammatory acne claim 2 , psoriasis claim 2 , ichthyosis and other keratinization claim 2 , hyperproliferative disorders of the skin claim 2 , eczema claim 2 , atopic dermatitis claim 2 , Darriers disease claim 2 , lichen planus claim 2 , glucocorticoid damage claim 2 , or steroid atrophy.4. The method of or claim 2 , wherein the compound is applied as a topical antimicrobial claim 2 , a skin anti pigmentation agent claim 2 , to treat and reverse the effects of age and photo damage to the skin.5. The method of or claim 2 , wherein the method of treating a disease or condition in a mammal claim 2 , further comprises preventing cancerous or precancerous conditions.6. The method of claim 1 , wherein the condition is premalignant or malignant hyperprolifertive diseases claim 1 , cancer of the breast claim 1 , skin claim 1 , prostate claim 1 , cervix claim 1 , uterus claim 1 , colon claim 1 , bladder claim 1 , esophagus claim 1 , stomach claim 1 , lung claim 1 , larynx claim 1 , oral cavity claim 1 , blood claim 1 , lymphatic system claim 1 , metaplasias claim 1 , dysplasias claim 1 , neoplasias claim 1 , leukoplasias claim 1 , or papillomas of the mucous membranes claim 1 , or Kaposi's sarcoma.7. The method of claim 1 , wherein the compound is useful to treat diseases of the eye comprising prolieferative vitreoretinopathy (PVR) claim 1 , retinal detachment claim 1 , dry eye claim 1 , corneopathies.8. The method of claim 2 , wherein the compound is ...

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Номер записи: 82
22-07-2021 дата публикации

ARYL HYDROCARBON RECEPTOR ANTAGONISTS AND METHODS OF USE

Номер: US20210220408A1
Автор: Boitano Anthony, Cooke Michael, GONCALVES Kevin A., HOBAN Megan
Принадлежит:

The disclosure relates to aryl hydrocarbon receptor antagonists as well as methods of modulating aryl hydrocarbon receptor activity and expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies, such as cancer, by administration of these aryl hydrocarbon receptor antagonists. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells. The disclosure further relates to pharmaceutical compositions comprising the compounds and methods of treating or preventing a disease in which aryl hydrocarbon receptor plays a role. 2. The compound of claim 1 , wherein b is 1 and c is 0.3. The compound of any one of the preceding claims claim 1 , wherein A is an optionally substituted monocyclic ring selected from the group consisting of benzene claim 1 , pyridine claim 1 , thiazole claim 1 , piperazine claim 1 , pyrimidine claim 1 , 1 claim 1 ,2 claim 1 ,3-triazole claim 1 , pyrazole claim 1 , furan claim 1 , isoxazole claim 1 , 4H-pyridazine claim 1 , thiophene claim 1 , oxazole claim 1 , and 2H-pyridine.4. The compound of any one of the preceding claims claim 1 , wherein A is an optionally substituted bicyclic ring selected from the group consisting of benzo[d][1 claim 1 ,2 claim 1 ,3]triazole claim 1 , thieno[2 claim 1 ,3-b]pyridine claim 1 , imidazo[1 claim 1 ,2-a]pyridine claim 1 , quinolone claim 1 , pyrido[1 claim 1 ,2-a]pyrimidine claim 1 , 6 claim 1 ,7-dihydro-5H-thiazolo[4 claim 1 ,5-b]pyridine claim 1 , benzo[d]imidazole claim 1 , isoindoline claim 1 , benzo[d]isothiazole claim 1 , benzo[d]thiazole claim 1 , benzo[b]thiophene claim 1 , indoline claim 1 , and [1 claim 1 ,2 claim 1 ,4]triazolo[1 claim 1 ...

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Номер записи: 83
11-06-2020 дата публикации

BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

Номер: US20200181176A1
Автор: Elliott Eric L., Ferdous Abu J., Kaufman Michael J., Komar-Lay Sonja A., Mazaik Debra L., Mccubbin Quentin J., Nguyen Phuong M., Palaniappan Vaithianathan, Skwierczynski Raymond D., Truong Nobel T., Varga Csanad M., Zawaneh Peter N.
Принадлежит:

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The process of claim 1 , wherein the reaction of step (1) or step (3) or both is conducted in the presence of a peptide coupling reagent.3. The process of claim 2 , wherein the peptide coupling reagent is selected from the group consisting of a carbodiimide reagent claim 2 , phosphonium reagent claim 2 , and uronium reagent.4. The process of claim 3 , wherein the peptide coupling reagent is selected from one or more of the group consisting of dicyclohexylcarbodiimide (DCC) claim 3 , 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC) claim 3 , benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) claim 3 , and O-(1H-benzotriazol-1-yl)-N claim 3 ,N′ claim 3 ,N′-tetramethyluronium tetrafluoroborate (TBTU).5. The process of claim 1 , further comprising converting the carboxylic acid moiety of compound (ii) to an activated ester or acid halide prior to the reaction of step (1).6. The process of claim 5 , wherein said activated ester or acid halide is an O—(N-hydroxysuccinnimide) ester.7. The process of claim 1 , wherein the reaction of step (3) is conducted in the presence of a solvent.8. The process of claim 7 , wherein the solvent is tetrahydrofuran.9. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an aqueous mineral acid.10. The process of claim 9 , wherein the mineral acid is hydrochloric acid.11. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an organic boronic acid acceptor.12. The process of claim 11 , wherein the organic boronic acid acceptor is i-BuB(OH).13. The process of claim 1 , wherein the reaction of step (5) is conducted in the presence of a solvent selected from the group consisting of ethyl ...

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Номер записи: 84
25-09-2014 дата публикации

Aromatic Amide Compound

Номер: US20140288221A1
Автор: Gray Steven D., Nair Kamlesh P.
Принадлежит:

An aromatic amide compound having the following general formula (I) is provided: 2. The compound of claim 1 , wherein m is 0.4. The compound of claim 3 , wherein Gand Qare hydrogen.5. The compound of claim 4 , wherein Gand Qare hydrogen and Gand Qselected from C(O)NH-phenyl or NHC(O)-phenyl.6. The compound of claim 4 , wherein Gand Qare hydrogen and Gand Qare selected from C(O)NH-phenyl or NHC(O)-phenyl.8. The compound of claim 7 , wherein Y claim 7 , Gand Qare hydrogen.9. The compound of claim 8 , wherein Y claim 8 , G claim 8 , and Qare hydrogen and Y claim 8 , Gand Qare selected from C(O)NH-phenyl or NHC(O)-phenyl.10. The compound of claim 8 , wherein Y claim 8 , Gand Qare hydrogen and Y claim 8 , Gand Qare selected from C(O)NH-phenyl or NHC(O)-phenyl.12. The compound of claim 1 , wherein the compound is N1 claim 1 ,N3-bis(4-benzamidophenyl)benzene-1 claim 1 ,3-dicarboxamide or N1 claim 1 ,N3-bis(3-benzamidophenyl)benzene-1 claim 1 ,3-dicarboxamide.13. The compound of claim 1 , wherein the compound is N1 claim 1 ,N3 claim 1 ,N5-tris(4-benzamidophenyl)benzene-1 claim 1 ,3 claim 1 ,5-tricarboxamide.14. A polymer composition comprising the compound of and a polymer.15. The polymer composition of claim 14 , wherein the polymer is a thermotropic liquid crystalline polymer.16. The polymer composition of claim 15 , wherein the polymer is a wholly aromatic liquid crystalline polymer.18. The method of claim 17 , wherein the aromatic acyl chloride is benzoyl chloride.19. The method of claim 17 , wherein the amine-substituted phenyl is 1 claim 17 ,3-phenyldiamine or 1 claim 17 ,4-phenyldiamine.20. The method of claim 17 , wherein the precursor is an aminophenyl substituted benzamide.21. The method of claim 17 , wherein the precursor is reacted with isophthaloyl chloride.22. The method of claim 17 , wherein the precursor is reacted with trimesoyl chloride. The present application claims priority to U.S. provisional applications serial nos. 61/528,445, filed on Aug. 29,2011, ...

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Номер записи: 85
18-06-2020 дата публикации

COMPOUNDS AND METHODS FOR INDUCING CHONDROGENESIS

Номер: US20200188407A1
Автор: CHATTERJEE Arnab K., PAYETTE Joshua, Schultz Peter G., YANG Baiyuan, YOON Hongchul, ZHU Shoutian
Принадлежит:

Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes. 1119.-. (canceled)121. The method of claim 120 , wherein B is NHC(O)R.122. The method of claim 120 , wherein each Rand Ris independently optionally substituted alkyl.123. The method of claim 120 , wherein Rand Rtogether with the N to which they are attached make a ring.124. The method of claim 120 , wherein Ris optionally substituted phenyl.125. The method of claim 120 , wherein the phenyl of Ris monosubstituted or disubstituted.126. The method of claim 125 , wherein substitution on the phenyl of Ris independently selected from F claim 125 , Cl claim 125 , COH claim 125 , CN claim 125 , OCH claim 125 , C(O)CH claim 125 , CF claim 125 , CH claim 125 , CHOH claim 125 , CHCHOH claim 125 , and CHCHCHOH.129. The method of claim 128 , wherein X is O or NH and A is CH—CRR—C(O)R.130. The method of claim 128 , X is NRand A is C(O) or CH.131. The method of claim 128 , wherein Ris phenyl and the phenyl of Ris monosubstituted or disubstituted.132. The method of claim 131 , wherein substitution on the phenyl is independently selected from F claim 131 , Cl claim 131 , COH claim 131 , CN claim 131 , OCH claim 131 , C(O)CH claim 131 , CF claim 131 , CH claim 131 , CHOH claim 131 , CHCHOH claim 131 , and CHCHCHOH.133. The method of claim 128 , wherein n is 0 or 1.134. The method of claim 133 , wherein Ris independently selected from Cl claim 133 , F claim 133 , CHOH claim 133 , CHNH claim 133 , OCH claim 133 , OCF claim 133 , OCHF claim 133 , CN claim 133 , NO claim 133 , COH claim 133 , and COCH.137. A pharmaceutical composition comprising a compound of claim 136 , or a pharmaceutically acceptable salt claim 136 , solvate claim 136 , polymorph claim 136 , prodrug claim 136 , ester claim 136 , metabolite claim 136 , N-oxide claim 136 , stereoisomer claim 136 , or isomer thereof claim 136 , and a pharmaceutically acceptable ...

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Номер записи: 86
18-06-2020 дата публикации

PPAR AGONISTS

Номер: US20200190019A1
Автор: Baiga Thomas J., BOCK Mark G., Downes Michael, Embler Emi Kanakubo, Evans Ronald M., Fan Weiwei, Keana John F.W., Kluge Authur F., Noel Joseph P., Patane Mike A.
Принадлежит:

Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases). 3. The compound of claim 1 , wherein ring B is selected from phenyl claim 1 , pyridine claim 1 , thiophene claim 1 , thiazole claim 1 , pyrazole claim 1 , oxazole claim 1 , isoxazole claim 1 , benzo[b]furan claim 1 , indazole claim 1 , piperidine claim 1 , cyclohexane claim 1 , piperidin-2-one claim 1 , piperazine-2 claim 1 ,5-dione or quinazolin-4(3H)-one.6. The compound of claim 1 , wherein Ris selected from alkyl claim 1 , heteroalkyl claim 1 , cycloalkyl claim 1 , heterocycloalkyl claim 1 , aryl or heteroaryl.7. The compound of claim 1 , wherein L claim 1 , Land Lare each independently selected from a bond or alkylene.8. The compound of claim 1 , wherein LRis isopropyl claim 1 , cyclopropyl claim 1 , cyclopentyl claim 1 , sec-butyl claim 1 , benzyl claim 1 , morpholinopropyl claim 1 , or (2-pyridinyl)ethyl.9. The compound of claim 1 , wherein each Rindependently is Cl claim 1 , F claim 1 , I claim 1 , Br claim 1 , cyano claim 1 , NO claim 1 , or OH.10. The compound of claim 1 , wherein each Rindependently is halogen claim 1 , alkyloxy claim 1 , haloalkyloxy claim 1 , cycloalkyloxy claim 1 , haloalkyl claim 1 , alkyl claim 1 , amino claim 1 , heterocyclic claim 1 , aryl claim 1 , cycloaliphatic or heteroaryl.11. The compound of claim 1 , wherein n is from 2 to 4 claim 1 , and two adjacent Rgroups form a fused ring system with ring B.13. The compound of claim 1 , wherein n is 1 and Ris furan-2-yl or furan-3-yl.15. The compound of claim 1 , wherein Lis Clinear or branched alkylene.16. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of . This application is a divisional of U.S. patent application Ser. No. 15/897,796, filed on Feb. 15, 2018, which ...

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Номер записи: 87
18-06-2020 дата публикации

PROTEASOME INHIBITORS

Номер: US20200190118A1
Автор: Danca Mihaela Diana, Olhava Edward J.
Принадлежит:

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The method of claim 1 , wherein Zand Zare each hydroxy.3. The method of claim 1 , wherein Zand Ztogether form a moiety derived from a boronic acid complexing agent.6. The method of claim 1 , wherein the compound of formula (I) is selected from:[(1R)-1-({[(2,3-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(5-chloro-2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,5-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,5-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-bromobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chloro-5-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,4-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,5-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3,4-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(3-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chloro-4-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,3-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(2,4-difluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-chloro-2-fluorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1-({[(4-chlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]boronic acid;[(1R)-1 ...

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Номер записи: 88
19-07-2018 дата публикации

NOVEL COMPOUND HAVING BLT INHIBITORY ACTIVITY AND COMPOSITION, FOR PREVENTING OR TREATING INFLAMMATORY DISEASES, COMPRISING SAME AS ACTIVE INGREDIENT

Номер: US20180201573A1
Автор: CHOI YongSeok, GOO Ja-Il, HAN Hyo-Kyung, Kim Jae-Hong, KWON Jinsun, LEE Kyeong, WEI Jun Dong
Принадлежит:

The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases. 2. The compound of claim 1 , wherein the compound represented by Formula 1 is selected from the group consisting of the following compounds:tert-butyl 4-(4-(3-(N-phenylpentaneamido)prop-1-ynyl)benzoyl)piperazine-1-carboxylate; N-phenyl-N-(3-(4-(piperazine-1-carbonyl)phenyl)prop-2-ynyl)pentaneamide; N-(3-(4-(4-methylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide; N-(3-(4-(4-ethylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide; N-(3-(4-(4-isopropylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide; N-(3-(4-(4-(2-hydroxyethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide; N-(3-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide; N-(3-(4-(4-cyclohexylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide; N-(3-(4-(4-(cyclohexylmethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide; N-(3-(4-(4-isobutylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide; N-phenyl-N-(3-(4-(4-(prop-2-ynyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)pentaneamide; N-(3-(4-(4-cyanopiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide; tert-butyl 4-(4-(3-(N-(3-fluorophenyl)pentaneamido)prop-1-ynyl)benzoyl)piperazine-1-carboxylate; N-(3-fluorophenyl)-N-(3-(4-(piperazine-1-carbonyl)phenyl)prop-2- ...

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Номер записи: 89
26-07-2018 дата публикации

BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

Номер: US20180208609A1
Автор: Elliott Eric L., Ferdous Abu J., Kaufman Michael J., Komar-Lay Sonja A., Mazaik Debra L., Mccubbin Quentin J., Nguyen Phuong M., Palaniappan Vaithianathan, Skwierczynski Raymond D., Truong Nobel T., Varga Csanad M., Zawaneh Peter N.
Принадлежит:

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The process of claim 1 , wherein the reaction of step (1) or step (3) or both is conducted in the presence of a peptide coupling reagent.3. The process of claim 2 , wherein the peptide coupling reagent is selected from the group consisting of a carbodiimide reagent claim 2 , phosphonium reagent claim 2 , and uronium reagent.4. The process of claim 3 , wherein the peptide coupling reagent is selected from one or more of the group consisting of dicyclohexylcarbodiimide (DCC) claim 3 , 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC) claim 3 , benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) claim 3 , and O-(1H-benzotriazol-1-yl)-N claim 3 ,N claim 3 ,N′ claim 3 ,N′-tetramethyluronium tetrafluoroborate (TBTU).5. The process of claim 1 , further comprising converting the carboxylic acid moiety of compound (ii) to an activated ester or acid halide prior to the reaction of step (1).6. The process of claim 5 , wherein said activated ester or acid halide is an O—(N-hydroxysuccinnimide) ester.7. The process of claim 1 , wherein the reaction of step (3) is conducted in the presence of a solvent.8. The process of claim 7 , wherein the solvent is tetrahydrofuran.9. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an aqueous mineral acid.10. The process of claim 9 , wherein the mineral acid is hydrochloric acid.11. The process of claim 1 , wherein the reaction of step (4) is conducted in the presence of an organic boronic acid acceptor.12. The process of claim 11 , wherein the organic boronic acid acceptor is i-BuB(OH).13. The process of claim 1 , wherein the reaction of step (5) is conducted in the presence of a solvent selected from the group consisting ...

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Номер записи: 90
09-10-2014 дата публикации

Compounds for Modulating Integrin CD11B/CD18

Номер: US20140303026A1
Автор: M. Amin Arnaout, Vineet Gupta
Принадлежит: General Hospital Corp

The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.

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Номер записи: 91
05-08-2021 дата публикации

VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF

Номер: US20210238192A1
Автор: Adler Marc, Buckman Brad Owen, Emayan Kumaraswamy, IBRAHIM PRABHA, Yuan Shendong
Принадлежит:

Disclosed herein are small molecule Vascular Adhesion Protein-1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof. 3. The compound of claim 2 , wherein Ais selected from the group consisting of —O— claim 2 , —NH— claim 2 , and —S—.4. The compound of claim 2 , wherein Ris selected from the group consisting of —NHCONHPr claim 2 , —NHCONEt claim 2 , —N(Me)CONHEt claim 2 , —NHCOOEt claim 2 , —NHCOEt claim 2 , and —NHCONHEt.7. The compound of claim 6 , wherein X is ═N— and Y is —NH—.8. The compound of claim 6 , wherein X is ═N— and Y is —S—.10. The compound of claim 9 , wherein Z is selected from the group consisting of —O— claim 9 , —NH claim 9 , —NCOCH claim 9 , and —OC(O)NH—.13. The compound of claim 12 , wherein Ais selected from the group consisting of —NHSOMe claim 12 , and —NHSOPh.16. The compound of claim 15 , wherein Ris selected from the group consisting of H claim 15 , —C(O)NRR claim 15 , —NRCOOR claim 15 , —NRCONRR claim 15 , and —O(CO)NRR claim 15 , and —SONRR.18. The compound of claim 17 , wherein Ris selected from the group consisting of H claim 17 , —COMe claim 17 , —COPh claim 17 , —CHPh claim 17 , phenyl claim 17 , and cyclohexyl.19. The compound of claim 17 , wherein Ris —CONHBu.20. The compound of claim 1 , wherein Ais selected from the group consisting of —S— claim 1 , —S(═O)— claim 1 , —SO— claim 1 , —O— claim 1 , —C(═S)— claim 1 , —C(═O)— claim 1 , —NR— claim 1 , —C(O)NR— claim 1 , —S(CH)— claim 1 , —O(CH)— claim 1 , —NR(CH)— claim 1 , —OC(O)NR— claim 1 , —NHC(O)NH— —NHC(S)NH— claim 1 , —NHC(S)O— claim 1 , —NHC(S)— claim 1 , and —NRSO—.22. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any one of - and a pharmaceutically acceptable excipient.23. A method of treating fibrotic disease or a secondary disease state or condition thereof claim 1 , comprising administering to a subject in need thereof claim 1 , a compound according to any one of -.24. The method of ...

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Номер записи: 92
25-06-2020 дата публикации

BROAD SPECTRUM GPCR BINDING AGENTS

Номер: US20200200765A1
Автор: Boursier Michelle, Kirkland Thomas, Levin Sergiy, Ohana Rachel Friedman, Wood Keith
Принадлежит:

Provided herein are broad-spectrum G-Protein coupled receptor (GPCR) binding agents, detectable/isolatable compounds comprising such binding agents (e.g., broad-spectrum GPCR binding agents linked to a functional element and/or solid surface), and methods of use thereof for the detection/isolation of GPCRs. 211-. (canceled)12. The composition of claim 1 , wherein the solid surface is selected from a sedimental particle claim 1 , a membrane claim 1 , glass claim 1 , a tube claim 1 , a well claim 1 , a self-assembled monolayer claim 1 , a surface plasmon resonance chip claim 1 , or a solid support with an electron conducting surface.13. The composition of claim 12 , wherein the sedimental particle is a magnetic particle.14. The composition of claim 1 , wherein the functional element is selected from a detectable element claim 1 , an affinity element claim 1 , and a capture element.15. The composition of claim 14 , wherein the detectable element comprises a fluorophore claim 14 , chromophore claim 14 , radionuclide claim 14 , electron opaque molecule claim 14 , a MM contrast agent claim 14 , SPECT contrast agent claim 14 , or mass tag.16. The composition of claim 1 , wherein the broad-spectrum GPCR binding agent is attached to the functional element or solid surface directly.17. The composition of claim 1 , wherein the broad-spectrum GPCR binding agent is attached to the functional element or solid surface via a linker.18. The composition of claim 17 , wherein the linker comprises [(CH)O] claim 17 , wherein n is 1-20.19. The composition of claim 17 , wherein the linker is attached to the broad-spectrum GPCR binding agent and/or the functional element by an amide bond.2130-. (canceled)31. The composition of claim 20 , wherein X is a fluorophore.32. The composition of claim 1 , comprising a non-natural abundance of one or more stable heavy isotopes.33. A method of detecting or quantifying GPCRs in a sample claim 1 , comprising contacting the sample with a composition of ...

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Номер записи: 93
13-08-2015 дата публикации

NOVEL HYDROXAMIC ACID DERIVATIVE

Номер: US20150225335A1
Автор: KAWAGUCHI Yasuko, KOTSUBO Hironori, OKA Yusuke, SHOJI Muneo, SUGA Yoichiro, TAKAHASHI Masato, Takashima Hajime, TSURUTA Risa, UNEUCHI Fumito, Urabe Hiroki, YABUUCHI Tetsuya
Принадлежит:

Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof: 3. The compound or the pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Ris a hydrogen atom or a Calkyl group (the Calkyl group may be substituted with the same or different 1 to 3 halogen atoms).4. The compound or the pharmaceutically acceptable salt thereof claim 3 , according to claim 3 , wherein Ris a Calkyl group (the Calkyl group may be substituted with the same or different 1 to 3 halogen atoms).5. The compound or the pharmaceutically acceptable salt thereof claim 4 , according to claim 4 , wherein Ris a methyl group.6. The compound or the pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Ris a hydrogen atom.7. The compound or the pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Ris a methyl group.8. The compound or the pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein{'sup': '3', 'Ris a hydrogen atom, and'}{'sup': 4', '45', '46', '47', '48, 'sub': 1-6', '1-6', '1-6', '3-8', '1-6', '1-6', '2-8', '1-6', '3-8', '1-6', '1-6, 'Ris a Calkyl group (the Calkyl group may be substituted with a phenyl group or a monocyclic aromatic heterocyclic group (the phenyl group and the monocyclic aromatic heterocyclic group may be substituted with 1 to 3 substituents which are the same or different and are selected from “a halogen atom, a Calkyl group, a Ccycloalkyl group, a Chaloalkyl group, a Chydroxyalkyl group, a Calkoxyalkyl group, a hydroxy group, a Calkoxy group, a Ccycloalkoxy group, an amino group, a Calkylamino group, a di(Calkyl)amino group, —N(R)COR, —CON(R)(R)″)).'}9. The ...

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Номер записи: 94
16-10-2014 дата публикации

Polymeric Compounds And Methods Of Making And Using The Same

Номер: US20140308317A1
Автор: Costanzo Michael J., FAN XIAODONG, Liu Dahui, Xu Yongjiang
Принадлежит: CELLCEUTIX CORPORATION

The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a infection; killing or inhibiting the growth of a species; inhibiting the growth of a species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative. 28-. (canceled)1018-. (canceled)2023-. (canceled)2542-. (canceled)4448-. (canceled)5057-. (canceled)5971-. (canceled)7385-. (canceled)87105-. (canceled)107117-. (canceled)119125-. (canceled)127136-. (canceled)138149-. (canceled)151160-. (canceled)162173-. (canceled)175196-. (canceled)198218-. (canceled)220232-. (canceled)234244-. (canceled)246257-. (canceled)258. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.259263-. (canceled)264. A method of inhibiting the growth of a microbe comprising contacting the microbe with a compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , of .265. A method of treating a mammal having a microbial infection comprising administering to the mammal in need thereof an anti-microbial effective amount of a compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , of .266271-. (canceled)272. A method of treating malaria in a mammal comprising administering to the mammal in need thereof a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.273. (canceled)274Plasmodium. A method of killing or inhibiting the growth of a species comprising contacting the species with an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.275MycobacteriumMycobacterium. A method of inhibiting the growth of a species ...

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Номер записи: 95
10-08-2017 дата публикации

Ppar agonists and methods of use thereof

Номер: US20170226154A1
Автор: Michael Downes, Ronald M. Evans
Принадлежит: SALK INSTITUTE FOR BIOLOGICAL STUDIES

Provided herein are deuterated compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).

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Номер записи: 96
30-10-2014 дата публикации

Gasoline fuel composition for improved performance in fuel injected engines

Номер: US20140318486A1
Автор: Scott D. Schwab, Xinggao Fang
Принадлежит: Afton Chemical Corp

A fuel soluble additive for a gasoline engine, a method for improving performance of fuel injectors and a method for cleaning fuel injectors for a gasoline engine. The fuel soluble additive includes a quaternary ammonium salt derived from an amido amine containing at least one tertiary amino group and an epoxide, in the presence of a proton donor selected from a carboxylic acid and an alkyl phenol. The amido amine is made in a reaction medium that is substantially devoid of an acylating agent.

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Номер записи: 97
09-07-2020 дата публикации

PPAR AGONISTS AND METHODS OF USE THEREOF

Номер: US20200216490A1
Автор: Downes Michael, Evans Ronald M.
Принадлежит: The Salk Institute for Biological Studies

Provided herein are deuterated compounds and compositions useful in increasing PPARδ activity. The compounds have a formula 3. The compound of claim 1 , wherein ring B is phenyl.5. The compound of claim 1 , wherein p is 1.6. The compound of claim 5 , wherein each of Rand Ris independently H or D.7. The compound of claim 1 , wherein Z is COH.8. The compound of claim 1 , wherein at least one of Lor Rcomprises at least one deuterium.9. The compound of wherein X is O.11. The compound of claim 1 , wherein n is 1 and Ris heteroaryl.12. The compound of claim 1 , wherein Ris furan-2-yl or furan-3-yl.14. The compound of claim 13 , wherein at least one of Lor Rcomprises at least one deuterium.15. The compound of claim 13 , wherein Lis —CHD- or -CD-.16. The compound of claim 15 , wherein Lis —CHD-.18. The compound of claim 13 , wherein n is 1 and Ris heteroaryl.19. The compound of claim 13 , wherein Ris furan-2-yl or furan-3-yl.20. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound according to . This application is a continuation of U.S. patent application Ser. No. 16/022,578, filed on Jun. 28, 2018, which is a divisional of U.S. application Ser. No. 15/482,385, filed on Apr. 7, 2017, which is a continuation of International Application No. PCT/US2015/053674, filed on Oct. 2, 2015, which claims the benefit of the earlier filing date of U.S. Provisional Application No. 62/061,547, filed on Oct. 8, 2014, the contents of which are incorporated herein by reference in its entirety.This invention was made with government support under DK057978-32 awarded by the National Institutes of Health. The government has certain rights in the invention.This application concerns agonists of peroxisome proliferator-activated receptors (PPAR), particularly PPAR delta (PPARδ), and methods for their use, such as to treat or prevent one or more PPARδ-related diseases.Skeletal muscle is a mechanically and energetically active organ, supporting vital ...

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Номер записи: 98
16-08-2018 дата публикации

1,4-disubstituted imidazole derivative

Номер: US20180230085A1
Автор: Futoshi Hasegawa, Hitoshi Ban, Manabu Watanabe, Miki HASHIZUME, Shingo Tojo
Принадлежит: Sumitomo Dainippon Pharma Co Ltd

The present invention provides a 1,4-disubstituted imidazole derivative of formula (1′) wherein ring Q 1 is optionally-substituted C 6-10 aryl group, etc.; R 1 and R 2 are independently hydrogen atom, etc.; W 1 is optionally-substituted C 1-4 alkylene group; W 2 is —NR 3a C(O)— wherein R 3a is hydrogen atom or C 1-6 alkyl group, etc.; ring Q 2 is 5- to 10-membered heteroaryl group, etc.; W 3 is optionally-substituted C 1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R 4 is independently halogen atom, optionally-substituted C 1-6 alkyl group, etc.; R 5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.

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Номер записи: 99
08-09-2016 дата публикации

ANTIMICROBIAL COMPOUNDS

Номер: US20160257642A1
Автор: Agerberth Birgitta, Gudmundsson Gudmundur, Miraglia Erica, Nylen Frank, Ottoson Hakan, Stromberg Roger
Принадлежит: AKTHELIA PHARMACEUTICALS

The invention provides compounds for use in treating microbial infection in an animal. Example compounds include Pyridin-3-ylmethyl (4-((2-aminophenyl)-carbamoyl)benzyl)carbamate (“Entinostat”). The compounds can act via induction of the innate antimicrobial peptide defense system, and stimulation of autophagy. 2. A compound according to claim 1 , wherein Aand A claim 1 , together with the atoms to which they are bound claim 1 , form an optionally substituted phenyl claim 1 , naphthalene or heteroaryl group.3. A compound according to or claim 1 , wherein Aand A claim 1 , together with the atoms to which they are bound claim 1 , form a phenyl group.4. A compound according to or claim 1 , wherein Aand A claim 1 , together with the atoms to which they are bound claim 1 , form a naphthalene group.5. A compound according to or claim 1 , wherein Aand A claim 1 , together with the atoms to which they are bound claim 1 , form a heteroaryl group.6. A compound according to any one of to claim 1 , wherein Ris H.7. A compound according to any one of to claim 1 , wherein n is 0.8. A compound according to any one of to claim 1 , wherein Q is Q1.9. A compound according to claim 8 , wherein Bis —X—R.10. A compound according to or claim 8 , wherein B claim 8 , B claim 8 , Band Bare all H.11. A compound according to any one of to claim 8 , wherein L is selected from —(CH)— claim 8 , —C(═O)— claim 8 , —NH—C(═O)— claim 8 , and —NR—C(═O)—.12. A compound according to claim 11 , wherein L is —C(═O)—.13. A compound according to any one of to claim 11 , wherein L is —NH—C(═O)—(CH)—C(═O)—.14. A compound according to any one of to claim 11 , wherein X is a covalent bond.15. A compound according to any one of to claim 11 , wherein X is Calkylene.16. A compound according to claim 15 , wherein X is independently: —CH— claim 15 , —CHCH— claim 15 , —CHCHCH— claim 15 , —CH(CH)— claim 15 , —CH(CH)CH— claim 15 , —CHCH(CH)— claim 15 , or —CH(CHCH)—.17. A compound according to claim 15 , wherein X is — ...

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Номер записи: 100