公开(公告)号：EP2734529A4

公开(公告)日：2015-06-03

申请号：EP12814549

申请日：2012-07-19

申请人： MERCK SHARP & DOHME ,  MERCK SHARP & DOHME

发明人： DE MAN ADRIANUS P A ,  STERRENBURG JAN-GERARD ,  RAAIJMAKERS HANS C A ,  KAPTEIN ALLARD ,  OUBRIE ARTHUR ,  REWINKEL JOHANNES B M ,  JANS CHRISTIAAN G J M ,  WIJKMANS JACOBUS C H M ,  BARF TJEERD A ,  COOPER ALAN B ,  KIM RONALD M ,  BOGA SOBHANA BABU ,  ZHU HUGH Y ,  GAO XIAOLEI ,  YAO XIN ,  ANAND RAJAN ,  WU HAO ,  LIU SHILAN ,  YANG CHUNDAO ,  ALHASSAN ABDUL-BASIT ,  WANG JAMES ,  YU YOUNONG ,  LIU JIAN ,  VACCARO HENRY M

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P19/08 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P37/00 ,  C07D519/00

CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D513/04 ,  C07D519/00

摘要： The present invention provides 6-5 membered fused pyridine ring compounds according to Formula I or pharmaceutically acceptable salts thereof. or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.

公开(公告)号：EP3082809A4

公开(公告)日：2017-08-09

申请号：EP14870699

申请日：2014-12-16

申请人： MERCK SHARP & DOHME

发明人： LIU JIAN ,  KIM RONALD M ,  KOZLOWSKI JOSEPH ,  KRIKORIAN ARTO D ,  ANAND RAJAN

IPC分类号： A61K31/437 ,  A61K31/4375 ,  A61K31/4545 ,  A61K45/06 ,  A61P3/10 ,  A61P19/02 ,  C07D471/04 ,  C07D519/00

CPC分类号： C07D471/04 ,  A61K31/4375 ,  A61K31/4545 ,  A61K45/06 ,  C07D519/00

摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.

摘要翻译： 本发明提供根据式I的布鲁顿酪氨酸激酶（Btk）抑制剂化合物或其药学上可接受的盐式I或其药学上可接受的盐或包含这些化合物的药物组合物，并涉及它们在治疗中的用途。 具体而言，本发明涉及Btk抑制剂化合物在治疗Btk介导的病症中的用途。

公开(公告)号：EP2938344A4

公开(公告)日：2016-06-08

申请号：EP13867977

申请日：2013-12-20

申请人： MERCK SHARP & DOHME

发明人： 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 ,  DENG QIAOLIN

IPC分类号： A61K31/519 ,  A61P25/00 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

摘要： 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.

公开(公告)号：EP2677869A4

公开(公告)日：2015-04-08

申请号：EP12749051

申请日：2012-02-23

申请人： MERCK SHARP & DOHME

发明人： ANAND RAJAN ,  APGAR JAMES M ,  BIFTU TESFAYE ,  CHEN PING ,  CHU LIN ,  COLANDREA VINCENT J ,  DONG GUIZHEN ,  DROPINSKI JAMES F ,  FENG DANQING ,  HICKS JACQUELINE D ,  JIANG JINLONG ,  KIM ALEXANDER J ,  LEAVITT KENNETH J ,  LI BING ,  QIAN XIAOXIA ,  SEBHAT IYASSU ,  WEI LAN ,  WILKENING ROBERT R ,  WU ZHICAI

IPC分类号： A01N43/58

CPC分类号： A61K31/5377 ,  A61K31/351 ,  A61K31/366 ,  A61K31/397 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/519 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

公开(公告)号：EP2938344B1

公开(公告)日：2017-06-21

申请号：EP13867977

申请日：2013-12-20

申请人： MERCK SHARP & DOHME

发明人： 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 ,  DENG QIAOLIN

IPC分类号： A61K31/519 ,  A61P25/00 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

摘要： 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.

摘要翻译： 公开了式A化合物:(结构表示）其中本文定义了“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”，其中化合物是A2A受体的拮抗剂。 本文还公开了本文所述化合物作为A2a受体的拮抗剂在潜在治疗或预防其中涉及A 2A受体的神经病症和疾病中的用途。 本文还公开了包含这些化合物的药物组合物以及这些药物组合物的用途。

公开(公告)号：EP2970119A4

公开(公告)日：2016-10-26

申请号：EP14763846

申请日：2014-03-10

申请人： MERCK SHARP & DOHME

发明人： ACTON JOHN J III ,  ANAND RAJAN ,  ARASAPPAN ASHOK ,  DANG QUN ,  SEBHAT IYASSU ,  PU ZHIFA ,  SUZUKI TAKAO

IPC分类号： C07D209/12 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4353 ,  A61K31/495 ,  A61K31/5365 ,  A61P3/10 ,  C07D209/30 ,  C07D403/10 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D471/04 ,  A61K31/366 ,  A61K31/397 ,  A61K31/404 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/541 ,  C07D209/08 ,  C07D209/12 ,  C07D209/18 ,  C07D209/30 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D413/04 ,  C07D413/10 ,  C07D493/04 ,  C07D519/00 ,  A61K2300/00

摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

公开(公告)号：EP3134408A4

公开(公告)日：2018-01-03

申请号：EP15783339

申请日：2015-04-21

申请人： MERCK SHARP & DOHME

发明人： LIM YEON-HEE ,  GUO ZHUYAN ,  ALI AMJAD ,  EDMONDSON SCOTT D ,  LIU WEIGUO ,  GALLO-ETIENNE GIOCONDA V ,  WU HEPING ,  GAO YING-DUO ,  STAMFORD ANDREW M ,  YU YOUNONG ,  KEVIN NANCY J ,  ANAND RAJAN ,  SHA DEYOU ,  NEELAMKAVIL SANTHOSH F ,  HUSSAIN ZAHID ,  KUMAR PUNEET ,  MONINGKA REMOND ,  DUFFY JOSEPH L ,  XU JIAYI ,  JIANG YU ,  SONE HIROKI ,  CHAKRABARTI ANJAN

IPC分类号： C07D471/10 ,  A61K31/438 ,  C07D498/20

CPC分类号： C07D498/20 ,  C07D471/10 ,  C07D487/10 ,  C07D498/10 ,  C07F9/6561

摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

公开(公告)号：EP3240542A4

公开(公告)日：2018-07-04

申请号：EP15875967

申请日：2015-12-17

申请人： MERCK SHARP & DOHME

发明人： LIU JIAN ,  KOZLOWSKI JOSEPH A ,  ALHASSAN ABDUL-BASIT ,  ANAND RAJAN ,  BOGA SOBHANA BABU ,  GUIADEEN DEODIALSINGH ,  YU WENSHENG ,  YU YOUNONG ,  WU HAO ,  YANG CHUNDAO

IPC分类号： A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  C07D487/04

CPC分类号： A61K31/4985 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K45/06 ,  A61K2300/00 ,  C07D519/00 ,  C07K16/2887

摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.

公开(公告)号：EP2948458A4

公开(公告)日：2016-07-27

申请号：EP14743619

申请日：2014-01-22

申请人： MERCK SHARP & DOHME

发明人： WU HAO ,  KIM RONALD M ,  LIU JIAN ,  GAO XIAOLEI ,  BOGA SOBHANA BABU ,  GUIADEEN DEODIALSINGH ,  KOZLOWSKI JOSEPH ,  YU WENSHENG ,  ANAND RAJAN ,  YU YOUNONG ,  SELYUTIN OLEG B ,  GAO YING-DUO ,  LIU SHILAN ,  YANG CHUNDAO ,  WANG HONGJIAN

IPC分类号： C07D519/00 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/5383 ,  A61P19/02 ,  A61P29/00 ,  A61P37/00 ,  C07D487/04

CPC分类号： C07D491/048 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/5383 ,  A61K45/06 ,  C07D455/02 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00

摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.

公开(公告)号：EP2744788A4

公开(公告)日：2015-04-15

申请号：EP12825316

申请日：2012-08-13

申请人： MERCK SHARP & DOHME

发明人： ANAND RAJAN ,  COLANDREA VINCENT J ,  REITER MAUD ,  VACHAL PETR ,  ZWICKER AARON ,  WILSON JONATHAN E ,  ZHANG FENGQI ,  ZHAO KAKE

IPC分类号： C07D243/00 ,  A61K31/498 ,  C07D487/00 ,  C07D498/00

CPC分类号： C07D409/06 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D241/42 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06