公开(公告)号：WO2010077861A1

公开(公告)日：2010-07-08

申请号：PCT/US2009/068048

申请日：2009-12-15

Applicant: VIA PHARMACEUTICALS, INC ,  BOLIN, David, R. ,  CHEUNG, Adrian, Wai-Hing ,  FIROOZNIA, Fariborz ,  MARCOPULOUS, Nicholas ,  QIAN, Yimin

Inventor： BOLIN, David, R. ,  CHEUNG, Adrian, Wai-Hing ,  FIROOZNIA, Fariborz ,  MARCOPULOUS, Nicholas ,  QIAN, Yimin

IPC: A01N43/54 ,  A01N57/00 ,  A61K31/4965

CPC classification number: C07D413/12 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14

Abstract: Provided herein are amides containing at least a four ring structure, which are inhibitors of diacylglycerol acyltransferase and are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

Abstract translation: 本文提供了含有至少四环结构的酰胺，其是二酰基甘油酰基转移酶的抑制剂，并且可用于治疗疾病，例如肥胖症，II型糖尿病和代谢综合征。

公开(公告)号：WO2013124335A1

公开(公告)日：2013-08-29

申请号：PCT/EP2013/053409

申请日：2013-02-21

Applicant: F. HOFFMANN-LA ROCHE AG ,  CHEUNG, Adrian Wai-Hing ,  SCHOENFELD, Ryan Craig ,  YUN, Weiya ,  ZHAO, Shu-Hai

Inventor： CHEUNG, Adrian Wai-Hing ,  SCHOENFELD, Ryan Craig ,  YUN, Weiya ,  ZHAO, Shu-Hai

IPC: C07D207/16 ,  C07D211/60 ,  C07D401/12 ,  C07D413/04 ,  A61K31/401 ,  A61K31/422 ,  A61K31/423 ,  A61K31/4709 ,  A61K31/4468 ,  A61P31/12

CPC classification number: C07D413/04 ,  C07D207/16 ,  C07D211/60 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12

Abstract: The present invention provides compounds of formula I, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Abstract translation: 本发明提供式I化合物，治疗丙型肝炎病毒（HCV）感染的组合物和方法。 还公开了含有这些化合物的药物组合物和使用这些化合物治疗HCV感染的方法。

公开(公告)号：WO2009037222A1

公开(公告)日：2009-03-26

申请号：PCT/EP2008/062234

申请日：2008-09-15

Applicant: F. HOFFMANN-LA ROCHE AG ,  BOLIN, David Robert ,  CAI, Jianping ,  CHEUNG, Adrian Wai-Hing ,  GOODNOW JR., Robert Alan ,  HAMILTON, Matthew Michael ,  LI, Shiming ,  MCDERMOTT, Lee Apostle ,  YUN, Weiya

Inventor： BOLIN, David Robert ,  CAI, Jianping ,  CHEUNG, Adrian Wai-Hing ,  GOODNOW JR., Robert Alan ,  HAMILTON, Matthew Michael ,  LI, Shiming ,  MCDERMOTT, Lee Apostle ,  YUN, Weiya

IPC: C07D401/14 ,  C07D403/12 ,  C07D407/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61K31/437 ,  A61K31/416 ,  A61K31/404 ,  A61P3/00

CPC classification number: C07D413/12 ,  C07D401/14 ,  C07D403/12 ,  C07D407/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: Provided herein are compounds of the formula (I), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

Abstract translation: 本文提供式（I）化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗疾病，例如肥胖症，II型糖尿病和代谢综合征。

公开(公告)号：WO2007134958A1

公开(公告)日：2007-11-29

申请号：PCT/EP2007/054416

申请日：2007-05-08

Applicant: F. HOFFMANN-LA ROCHE AG ,  BRINKMAN, John A. ,  CHEUNG, Adrian Wai-Hing ,  FIROOZNIA, Fariborz ,  GUERTIN, Kevin Richard ,  MARCOPULOS, Nicholas ,  QI, Lida ,  RACHA, Jagdish Kumar ,  SARABU, Ramakanth ,  TAN, Jenny ,  TILLEY, Jefferson Wright

Inventor： BRINKMAN, John A. ,  CHEUNG, Adrian Wai-Hing ,  FIROOZNIA, Fariborz ,  GUERTIN, Kevin Richard ,  MARCOPULOS, Nicholas ,  QI, Lida ,  RACHA, Jagdish Kumar ,  SARABU, Ramakanth ,  TAN, Jenny ,  TILLEY, Jefferson Wright

IPC: C07D513/04 ,  C07D521/00 ,  A61K31/519 ,  A61K31/437 ,  A61P3/10

CPC classification number: C07D513/04 ,  C07D521/00

Abstract: There are presented compounds of the formula (I) wherein R 1 , R 2 , R 3 and R 4 are as defined in the description and claims, or a pharmaceutically acceptable salt thereof, which are active adenosine A2B receptor antagonists and useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.

Abstract translation: 提出了式（I）的化合物，其中R 1，R 2，R 3和R 4， 是描述和权利要求中所定义的，或其药学上可接受的盐，其是活性腺苷A2B受体拮抗剂，可用于治疗糖尿病，糖尿病性视网膜病，哮喘和腹泻。

公开(公告)号：WO2006050843A1

公开(公告)日：2006-05-18

申请号：PCT/EP2005/011682

申请日：2005-11-02

Applicant: F. HOFFMANN-LA ROCHE AG ,  BERTHEL, Steven, Joseph ,  CHEUNG, Adrian, Wai-Hing ,  THAKKAR, Kshitij, Chhabilbhai ,  YUN, Weiya

Inventor： BERTHEL, Steven, Joseph ,  CHEUNG, Adrian, Wai-Hing ,  THAKKAR, Kshitij, Chhabilbhai ,  YUN, Weiya

IPC: C07D239/42 ,  A61K31/517

CPC classification number: C07D401/12 ,  C07D239/95 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D405/12 ,  C07D409/04 ,  C07D413/04

Abstract: The present invention is concerned with compounds of formula (1), wherein R 1 , R 2 and X are as defined in the description and claims. The compounds of the present invention are PTP-1B inhibitors and can be used as medicaments.

Abstract translation: 本发明涉及式（1）的化合物，其中R 1，R 2和X如说明书和权利要求中所定义。 本发明的化合物是PTP-1B抑制剂，可用作药物。

公开(公告)号：WO2012136684A1

公开(公告)日：2012-10-11

申请号：PCT/EP2012/056122

申请日：2012-04-04

Applicant: F. HOFFMANN-LA ROCHE AG ,  CHEUNG, Adrian Wai-Hing ,  GUERTIN, Kevin Richard ,  HAYNES, Nancy-Ellen ,  MERTZ, Eric ,  QI, Lida ,  QIAN, Yimin ,  SCOTT, Nathan Robert

Inventor： CHEUNG, Adrian Wai-Hing ,  GUERTIN, Kevin Richard ,  HAYNES, Nancy-Ellen ,  MERTZ, Eric ,  QI, Lida ,  QIAN, Yimin ,  SCOTT, Nathan Robert

IPC: C07D215/48 ,  C07D401/04 ,  C07D413/04 ,  C07D471/04

CPC classification number: C07D215/233 ,  C07D215/48 ,  C07D401/04 ,  C07D401/06 ,  C07D413/04 ,  C07D471/04

Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula (I): wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.

Abstract translation: 本发明涉及JNK抑制剂和用于抑制JNK和治疗JNK介导的病症的相应方法，制剂和组合物。 本申请公开了如下式（I）所述的JNK抑制剂：其中变量如本文所定义。 本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。 公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂，以及本文公开的化合物，以及制备所述化合物的方法和相应的组合物。

公开(公告)号：WO2010056506A1

公开(公告)日：2010-05-20

申请号：PCT/US2009/062154

申请日：2009-10-27

Applicant: VIA PHARMACEUTICALS, INC. ,  BOLIN, David, R. ,  CHEUNG, Adrian, Wai-hing ,  HAMILTON, Matthew, Michael ,  MARCOPULOUS, Nicholas ,  McDERMOTT, Lee, Apostle ,  QIAN, Yimin

Inventor： BOLIN, David, R. ,  CHEUNG, Adrian, Wai-hing ,  HAMILTON, Matthew, Michael ,  MARCOPULOUS, Nicholas ,  McDERMOTT, Lee, Apostle ,  QIAN, Yimin

IPC: C12Q1/48

CPC classification number: C07D401/04 ,  C07D213/75 ,  C07D213/82 ,  C07D277/46 ,  C07D277/82 ,  C07D295/155 ,  C07D295/185 ,  C07D295/205 ,  C07D333/54 ,  C07D401/12

Abstract: Provided herein are compounds of the formula (I): were Rl is phenyl, R2 is hyrogen, halogen or lower alkyl,X is carbon on nitrogen, and R3 is isoquinoline, -amino, or a-4- to 6-membered heterocycloalkyl ring and pharmaceutically acceptable salts thereof, which are active as DGAT inhibitors and therefore find uses in treatment of diseases associated with abnormal metabolism of triglicerides, such as, for example, obesity, type Il diabetes mellitus and metabolic syndrome.

Abstract translation: 本文提供了式（I）的化合物：R1是苯基，R2是氢，卤素或低级烷基，X是氮上的碳，R3是异喹啉， - 氨基或a-4-至6-元杂环烷基环 其药学上可接受的盐，其作为DGAT抑制剂是有活性的，因此可用于治疗与三联嘧啶的异常代谢相关的疾病，例如肥胖症，II型糖尿病和代谢综合征。

公开(公告)号：WO2007009911A1

公开(公告)日：2007-01-25

申请号：PCT/EP2006/064091

申请日：2006-07-11

Applicant: F. HOFFMANN-LA ROCHE AG ,  BERTHEL, Steven, Joseph ,  CHEUNG, Adrian, Wai-Hing ,  KIM, Kyungjin ,  LI, Shiming ,  THAKKAR, Kshitij, Chhabilbhai ,  YUN, Weiya

Inventor： BERTHEL, Steven, Joseph ,  CHEUNG, Adrian, Wai-Hing ,  KIM, Kyungjin ,  LI, Shiming ,  THAKKAR, Kshitij, Chhabilbhai ,  YUN, Weiya

IPC: C07D471/04 ,  A61P3/00 ,  A61K31/519

CPC classification number: C07D471/04

Abstract: The present invention is concerned with compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 and X are as described in the description and claims. The compounds are inhibitors of PTP1B. Accordingly, the compounds can be used for treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.

Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4，R 4， SUP>和X如说明书和权利要求中所述。 这些化合物是PTP1B的抑制剂。 因此，该化合物可用于治疗或预防PTP-1B介导的疾病，包括糖尿病，肥胖症和糖尿病相关疾病。

公开(公告)号：WO2013007676A1

公开(公告)日：2013-01-17

申请号：PCT/EP2012/063366

申请日：2012-07-09

Applicant: F. HOFFMANN-LA ROCHE AG ,  BILOTTA, Joseph Anthony ,  CHEUNG, Adrian Wai-Hing ,  FIROOZNIA, Fariborz ,  GUERTIN, Kevin Richard ,  HAYDEN, Stuart ,  HAYNES, Nancy-Ellen ,  LUKACS-LESBURG, Christine M. ,  MARCOPULOS, Nicholas ,  MERTZ, Eric ,  QI, Lida ,  QIAN, Yimin ,  SO, Sung-Sau ,  TAN, Jenny ,  THAKKAR, Kshitij Chhabilbhai

Inventor： BILOTTA, Joseph Anthony ,  CHEUNG, Adrian Wai-Hing ,  FIROOZNIA, Fariborz ,  GUERTIN, Kevin Richard ,  HAYDEN, Stuart ,  HAYNES, Nancy-Ellen ,  LUKACS-LESBURG, Christine M. ,  MARCOPULOS, Nicholas ,  MERTZ, Eric ,  QI, Lida ,  QIAN, Yimin ,  SO, Sung-Sau ,  TAN, Jenny ,  THAKKAR, Kshitij Chhabilbhai

IPC: C07D215/48 ,  C07D401/12 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D215/233 ,  A61K31/4709 ,  A61P3/10 ,  A61P19/00 ,  A61P35/00 ,  A61P25/00

CPC classification number: C07D215/48 ,  C07D215/233 ,  C07D401/12 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula (I): wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.

Abstract translation: 本发明涉及JNK抑制剂和用于抑制JNK和治疗JNK介导的病症的相应方法，制剂和组合物。 本申请公开了如下式（I）所述的JNK抑制剂：其中变量如本文所定义。 本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。 公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂，以及本文公开的化合物，以及制备所述化合物的方法和相应的组合物。

公开(公告)号：WO2008141976A1

公开(公告)日：2008-11-27

申请号：PCT/EP2008/055843

申请日：2008-05-13

Applicant: F. HOFFMANN-LA ROCHE AG ,  BOLIN, David Robert ,  CHEUNG, Adrian Wai-Hing ,  FIROOZNIA, Fariborz ,  HAMILTON, Matthew Michael ,  MCDERMOTT, Lee Apostle ,  QIAN, Yimin ,  TAN, Jenny ,  YUN, Weiya

Inventor： BOLIN, David Robert ,  CHEUNG, Adrian Wai-Hing ,  FIROOZNIA, Fariborz ,  HAMILTON, Matthew Michael ,  MCDERMOTT, Lee Apostle ,  QIAN, Yimin ,  TAN, Jenny ,  YUN, Weiya

IPC: C07D231/14 ,  C07D263/34 ,  C07D277/56 ,  C07D307/68 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4427

CPC classification number: C07D263/34 ,  C07D231/14 ,  C07D277/56 ,  C07D307/68 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

Abstract translation: 本文提供式（I）化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗疾病，例如肥胖症，II型糖尿病和代谢综合征。