公开(公告)号：WO2016126570A1

公开(公告)日：2016-08-11

申请号：PCT/US2016/015881

申请日：2016-02-01

Applicant: MERCK SHARP & DOHME CORP. ,  ALI, Amjad ,  ZHOU, Gang ,  KUANG, Rongze ,  LIM, Yeon-Hee ,  LO, Michael Man-Chu ,  TING, Pauline, C. ,  BIJU, Purakkattle ,  RUIZ, Manuel de Lera ,  DEGRADO, Sylvia, J. ,  TUNG, Alexander, L. ,  HENDERSON, Timothy, J. ,  HONG, Liwu ,  KIM, Jae-Hun ,  KIM, David Won-Shik ,  LEE, Joe, F. ,  WU, Jie ,  WU, Heping ,  XIAO, Yushi ,  YU, Tao ,  ZHU, Xiaohong ,  MCCORMICK, Kevin, D. ,  TAGAT, Jayaram, R. ,  XIAO, Dong ,  KHAN, Tanweer ,  CAO, Jianhua ,  BERLIN, Michael ,  ZHANG, Yonglian

Inventor： ALI, Amjad ,  ZHOU, Gang ,  KUANG, Rongze ,  LIM, Yeon-Hee ,  LO, Michael Man-Chu ,  TING, Pauline, C. ,  BIJU, Purakkattle ,  RUIZ, Manuel de Lera ,  DEGRADO, Sylvia, J. ,  TUNG, Alexander, L. ,  HENDERSON, Timothy, J. ,  HONG, Liwu ,  KIM, Jae-Hun ,  KIM, David Won-Shik ,  LEE, Joe, F. ,  WU, Jie ,  WU, Heping ,  XIAO, Yushi ,  YU, Tao ,  ZHU, Xiaohong ,  MCCORMICK, Kevin, D. ,  TAGAT, Jayaram, R. ,  XIAO, Dong ,  KHAN, Tanweer ,  CAO, Jianhua ,  BERLIN, Michael ,  ZHANG, Yonglian

IPC: A61K31/517 ,  C07D239/84 ,  C07D403/12

CPC classification number: C07D239/84 ,  A61K31/517 ,  A61P25/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.

Abstract translation: 本发明涉及被认为可用作A2A受体拮抗剂的通式I化合物或其药学上可接受的盐。

公开(公告)号：WO2014101113A1

公开(公告)日：2014-07-03

申请号：PCT/CN2012/087851

申请日：2012-12-28

Applicant: MERCK SHARP & DOHME CORP. ,  ALI, Amjad ,  LO, Michael Man-Chu ,  LIM, Yeon-Hee ,  STAMFORD, Andrew ,  KUANG, Rongze ,  TEMPEST, Paul ,  YU, Younong ,  BERLIN, Michael ,  TING, Pauline ,  ZHOU, Gang ,  YU, Tao ,  BOYCE, Christopher ,  KELLY, Joseph Michael ,  TAGAT, Jayaram R. ,  ZHENG, Junying ,  HUANG, Xianhai ,  ZHOU, Wei ,  KIM, Jae-Hun ,  ZORN, Nicolas ,  XIAO, Dong ,  GALLO, Gioconda V. ,  WON, Walter ,  WU, Heping ,  ANAND, Rajan

Inventor： ALI, Amjad ,  LO, Michael Man-Chu ,  LIM, Yeon-Hee ,  STAMFORD, Andrew ,  KUANG, Rongze ,  TEMPEST, Paul ,  YU, Younong ,  BERLIN, Michael ,  TING, Pauline ,  ZHOU, Gang ,  YU, Tao ,  BOYCE, Christopher ,  KELLY, Joseph Michael ,  TAGAT, Jayaram R. ,  ZHENG, Junying ,  HUANG, Xianhai ,  ZHOU, Wei ,  KIM, Jae-Hun ,  ZORN, Nicolas ,  XIAO, Dong ,  GALLO, Gioconda V. ,  WON, Walter ,  WU, Heping ,  ANAND, Rajan

IPC: C07D487/04 ,  A61K31/4196 ,  A61K31/517 ,  A61K31/519 ,  A61P25/28

CPC classification number: C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

Abstract: Disclosed are compounds of Formula (A), as defined herein, which have binding activity for an A 2A -receptor and are believed to be useful for treatment or management of CNS diseases or conditions which can be treated or managed using compounds which have A 2A receptor antagonist activity.

Abstract translation: 公开了本文定义的式（A）化合物，其具有对A2A受体的结合活性，并被认为可用于治疗或治疗CNS疾病或病症，其可以使用具有A2A受体拮抗剂的化合物治疗或治疗 活动。

公开(公告)号：WO2012047772A3

公开(公告)日：2012-06-07

申请号：PCT/US2011054524

申请日：2011-10-03

Applicant: SCHERING CORP ,  TING PAULINE C ,  ASLANIAN ROBERT G ,  KUANG RONGZE ,  WU HEPING ,  ZHOU GANG

Inventor： TING PAULINE C ,  ASLANIAN ROBERT G ,  KUANG RONGZE ,  WU HEPING ,  ZHOU GANG

IPC: A01N43/50

CPC classification number: C07D401/04 ,  C07D401/14

Abstract: Described herein are compounds of formula (I). The compounds of formula (I) act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

Abstract translation: 本文描述的是式（I）的化合物。 式（I）化合物作为DGAT1抑制剂，可用于预防，治疗或作为高脂血症，糖尿病和肥胖症的补救剂。

公开(公告)号：WO2010059606A3

公开(公告)日：2010-09-16

申请号：PCT/US2009064747

申请日：2009-11-17

Applicant: SCHERING CORP ,  TING PAULINE C ,  ASLANIAN ROBERT G ,  CAPLEN MARY ANN ,  CAO JIANHUA ,  KIM DAVID WON-SHIK ,  KIM HYUNJIN ,  KUANG RONGZE ,  LEE JOE F ,  SCHWERDT JOHN H ,  WU HEPING ,  ZHOU GANG ,  ZORN NICOLAS

Inventor： TING PAULINE C ,  ASLANIAN ROBERT G ,  CAPLEN MARY ANN ,  CAO JIANHUA ,  KIM DAVID WON-SHIK ,  KIM HYUNJIN ,  KUANG RONGZE ,  LEE JOE F ,  SCHWERDT JOHN H ,  WU HEPING ,  ZHOU GANG ,  ZORN NICOLAS

IPC: C07D401/12 ,  A61K31/422 ,  A61K31/427 ,  A61K31/506 ,  A61P3/00 ,  A61P9/00 ,  C07D401/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

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

Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below.

Abstract translation: 本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物以及该化合物用于治疗或预防心血管疾病，代谢障碍，肥胖或肥胖相关障碍的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 本发明的说明性化合物如下所示。

公开(公告)号：WO2008115385A3

公开(公告)日：2009-01-08

申请号：PCT/US2008003292

申请日：2008-03-12

Applicant: SCHERING CORP ,  BLACK TODD A ,  MCNICHOLAS PAUL M ,  WALKER SCOTT S ,  XU YIMING ,  TING PAULINE C

Inventor： BLACK TODD A ,  MCNICHOLAS PAUL M ,  WALKER SCOTT S ,  XU YIMING ,  TING PAULINE C

IPC: A61K31/501 ,  A01N43/60 ,  A61P31/10

CPC classification number: A61K31/501 ,  A01N43/58 ,  A01N43/60

Abstract: There is disclosed a method for treating or preventing fungal infections comprising the administration of at least one glucan synthase inhibitor of a formula as described above in the specification or a pharmaceutically acceptable salt thereof; also claimed are methods of preparing pharmaceutical compositions comprising a compound as described above in the specification and a carrier, method of treating or preventing fungal infections comprising administration of combinations of glucan synthase inhibitor of a formula as described above in the specification and other antifungal agents, and method of treating or preventing fungal infections comprising administration of pharmaceutical compositions prepared according to a method described above in the specification, and a method of preparing a kit in a single package of the above described pharmaceutical composition and other antifungal agents.

Abstract translation: 公开了一种用于治疗或预防真菌感染的方法，其包括施用至少一种如说明书中所述的式的葡聚糖合成酶抑制剂或其药学上可接受的盐; 还要求的是制备药物组合物的方法，所述药物组合物包含上述说明书中所述的化合物和载体，治疗或预防真菌感染的方法，包括施用上述说明书中所述的式的葡聚糖合成酶抑制剂和其它抗真菌剂的组合， 以及治疗或预防真菌感染的方法，包括施用根据说明书中所述的方法制备的药物组合物，以及在上述药物组合物和其它抗真菌剂的单一包装中制备试剂盒的方法。

公开(公告)号：WO2008115385A2

公开(公告)日：2008-09-25

申请号：PCT/US2008/003292

申请日：2008-03-12

Applicant: SCHERING CORPORATION ,  BLACK, Todd, A. ,  MCNICHOLAS, Paul, M. ,  WALKER, Scott, S. ,  XU, Yiming ,  TING, Pauline, C.

Inventor： BLACK, Todd, A. ,  MCNICHOLAS, Paul, M. ,  WALKER, Scott, S. ,  XU, Yiming ,  TING, Pauline, C.

IPC: A61K31/501 ,  A61P31/10 ,  A01N43/60

CPC classification number: A61K31/501 ,  A01N43/58 ,  A01N43/60

Abstract: There is disclosed a method for treating or preventing fungal infections comprising the administration of at least one glucan synthase inhibitor of a formula as described above in the specification or a pharmaceutically acceptable salt thereof; also claimed are methods of preparing pharmaceutical compositions comprising a compound as described above in the specification and a carrier, method of treating or preventing fungal infections comprising administration of combinations of glucan synthase inhibitor of a formula as described above in the specification and other antifungal agents, and method of treating or preventing fungal infections comprising administration of pharmaceutical compositions prepared according to a method described above in the specification, and a method of preparing a kit in a single package of the above described pharmaceutical composition and other antifungal agents.

Abstract translation: 公开了一种用于治疗或预防真菌感染的方法，其包括施用至少一种如说明书中所述的式的葡聚糖合成酶抑制剂或其药学上可接受的盐; 还要求的是制备药物组合物的方法，所述药物组合物包含上述说明书中所述的化合物和载体，治疗或预防真菌感染的方法，包括施用上述说明书中所述的式的葡聚糖合成酶抑制剂和其它抗真菌剂的组合， 以及治疗或预防真菌感染的方法，包括施用根据说明书中所述的方法制备的药物组合物，以及在上述药物组合物和其它抗真菌剂的单一包装中制备试剂盒的方法。

公开(公告)号：WO2019118313A1

公开(公告)日：2019-06-20

申请号：PCT/US2018/064649

申请日：2018-12-10

Applicant: MERCK SHARP & DOHME CORP. ,  ALI, Amjad ,  LIM, Yeon-Hee ,  GALLO-ETIENNE, Gioconda, V. ,  KELLY, Joseph, Michael ,  BERLIN, Michael ,  TING, Pauline ,  TAGAT, Jayaram, R. ,  XIAO, Dong ,  KUANG, Rongze ,  WU, Heping ,  WANG, Hongwu

Inventor： ALI, Amjad ,  LIM, Yeon-Hee ,  GALLO-ETIENNE, Gioconda, V. ,  KELLY, Joseph, Michael ,  BERLIN, Michael ,  TING, Pauline ,  TAGAT, Jayaram, R. ,  XIAO, Dong ,  KUANG, Rongze ,  WU, Heping ,  WANG, Hongwu

IPC: A61K31/4188 ,  A61K31/505 ,  A61K31/519 ,  C07D247/00 ,  C07D247/02 ,  C07D255/00

Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof: wherein: "Z" and R1 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

公开(公告)号：WO2014105666A1

公开(公告)日：2014-07-03

申请号：PCT/US2013/076781

申请日：2013-12-20

Applicant: MERCK SHARP & DOHME CORP. ,  ALI, Amjad ,  LO, Michael Man-Chu ,  LIM, Yeon-Hee ,  STAMFORD, Andrew ,  KUANG, Rongze ,  TEMPEST, Paul ,  YU, Younong ,  HUANG, Xianhai ,  HENDERSON, Timothy, J. ,  KIM, Jae-Hun ,  BOYCE, Christopher ,  TING, Pauline ,  ZHENG, Junying ,  METZGER, Edward ,  ZORN, Nicolas ,  XIAO, Dong ,  GALLO, Gioconda, V. ,  WON, Walter ,  WU, Heping

Inventor： ALI, Amjad ,  LO, Michael Man-Chu ,  LIM, Yeon-Hee ,  STAMFORD, Andrew ,  KUANG, Rongze ,  TEMPEST, Paul ,  YU, Younong ,  HUANG, Xianhai ,  HENDERSON, Timothy, J. ,  KIM, Jae-Hun ,  BOYCE, Christopher ,  TING, Pauline ,  ZHENG, Junying ,  METZGER, Edward ,  ZORN, Nicolas ,  XIAO, Dong ,  GALLO, Gioconda, V. ,  WON, Walter ,  WU, Heping

IPC: A61K31/4985 ,  A61K31/519 ,  C07D487/04 ,  A61P25/16

CPC classification number: C07D519/00 ,  C07D487/04

Abstract: Disclosed are compounds of Formula Gl (structurally represented): where "RG3" "Rd1" to "Rd4", "n", "m", "p", "W", "X", "Y", and "Z" are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

Abstract translation: 公开了式（式III）化合物：其中“RG3”“Rd1”至“Rd4”，“n”，“m”，“p”，“W”，“X”，“Y” “在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

公开(公告)号：WO2014105664A1

公开(公告)日：2014-07-03

申请号：PCT/US2013/076775

申请日：2013-12-20

Applicant: MERCK SHARP & DOHME CORP. ,  ALI, Amjad ,  LO, Michael Man-Chu ,  LIM, Yeon-Hee ,  STAMFORD, Andrew ,  KUANG, Rongze ,  TEMPEST, Paul ,  YU, Younong ,  BERLIN, Michael ,  TING, Pauline ,  ZHOU, Gang ,  YU, Tao ,  BOYCE, Christopher ,  KELLY, Joseph Michael ,  TAGAT, Jayaram, R. ,  ZHENG, Junying ,  HUANG, Xianhai ,  ZHOU, Wei ,  KIM, Jae-Hun ,  ZORN, Nicolas ,  XIAO, Dong ,  GALLO, Gioconda, V. ,  WON, Walter ,  WU, Heping ,  ANAND, Rajan

Inventor： ALI, Amjad ,  LO, Michael Man-Chu ,  LIM, Yeon-Hee ,  STAMFORD, Andrew ,  KUANG, Rongze ,  TEMPEST, Paul ,  YU, Younong ,  BERLIN, Michael ,  TING, Pauline ,  ZHOU, Gang ,  YU, Tao ,  BOYCE, Christopher ,  KELLY, Joseph Michael ,  TAGAT, Jayaram, R. ,  ZHENG, Junying ,  HUANG, Xianhai ,  ZHOU, Wei ,  KIM, Jae-Hun ,  ZORN, Nicolas ,  XIAO, Dong ,  GALLO, Gioconda, V. ,  WON, Walter ,  WU, Heping ,  ANAND, Rajan

IPC: A61K31/4985 ,  A61K31/519

CPC classification number: C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

Abstract: Disclosed are compounds of Formula A: (structurally represented) where "RG1", "RG2a", "RG4", "RG5", "MG1", "n" and "m" are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

Abstract translation: 公开了式A化合物（结构上表示），其中“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

公开(公告)号：WO2011031628A1

公开(公告)日：2011-03-17

申请号：PCT/US2010/047765

申请日：2010-09-03

Applicant: SCHERING CORPORATION ,  TING, Pauline, C. ,  LEE, Joe, F. ,  ASLANIAN, Robert, G.

Inventor： TING, Pauline, C. ,  LEE, Joe, F. ,  ASLANIAN, Robert, G.

IPC: A01N57/00 ,  C07C403/00

CPC classification number: C07D405/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (DGAT) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below:

Abstract translation: 本发明涉及作为二酰基甘油酰基转移酶（DGAT）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖或肥胖相关病症，糖尿病， 血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 本发明的说明性化合物如下所示：