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：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：EP2908824A4

公开(公告)日：2016-03-09

申请号：EP13846341

申请日：2013-10-14

申请人： MERCK SHARP & DOHME

发明人： GILBERT ERIC J ,  CUMMING JARED N ,  STAMFORD ANDREW W ,  YU YOUNONG ,  SCOTT JACK D ,  ISERLOH ULRICH ,  WANG LINGYAN ,  CALDWELL JOHN P

IPC分类号： C07D417/14 ,  A61K31/549 ,  A61P25/16 ,  A61P25/28 ,  C07D417/10 ,  C07D495/04

CPC分类号： C07D417/14 ,  A61K31/549 ,  A61K45/06 ,  C07D417/10 ,  C07D495/04

摘要： In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 6-membered ring, and each of the remaining variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.

摘要翻译： 在其许多实施方案中，本发明提供了某些亚氨基噻嗪二氧化物化合物，包括式（I）：（I）的化合物及其互变异构体和立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中中环 在本文中作为“环B”）是三环取代基是任选取代的6元环，并且式中所示的各个残基如本文所定义。 本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括阿尔茨海默氏病。

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：EP3220910A4

公开(公告)日：2018-04-25

申请号：EP15861650

申请日：2015-11-13

申请人： MERCK SHARP & DOHME

发明人： KUANG RONGZE ,  TING PAULINE ,  ALI AMJAD ,  WU HEPING ,  BERLIN MICHAEL ,  STAMFORD ANDREW ,  WANG HONGWU ,  ZHOU GANG ,  KIM DAVID ,  DENG QIAOLIN ,  LIM YEON-HEE ,  YU YOUNONG

IPC分类号： A61K31/497 ,  C07D241/26 ,  C07D413/04

CPC分类号： C07D241/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

摘要： Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein "R1", "RA-1", "R2", "R3", and "Het" are defined herein above, 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：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：EP2627178A4

公开(公告)日：2014-08-20

申请号：EP11833150

申请日：2011-10-06

申请人： MERCK SHARP & DOHME

发明人： PALANI ANANDAN ,  ASLANIAN ROBERT G ,  BOYCE CHRISTOPHER W ,  MAZZOLA ROBERT D JR ,  MCKITTRICK BRIAN A ,  MCCORMICK KEVIN D ,  QIN JUN ,  TANG HAIQUN ,  XIAO DONG ,  YU YOUNONG ,  CALDWELL JOHN P ,  KELLEY ELIZABETH HELEN ,  ZHANG HONGJUN ,  SILIPHAIVANH PHIENG ,  MACCOSS RACHEL N ,  METHOT JOEY L ,  GAUUAN JOLICIA POLIVINA ,  JIANG QIN ,  LEYHANE ANDREW J ,  BIJU PURAKKATTLE JOHNY ,  DONG LI ,  HUANG XIANHAI ,  SHAO NING ,  ZHOU WEI ,  DHONDI PAWAN K ,  RAO ASHWIN U

IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04

CPC分类号： C07D239/91 ,  A61K31/517 ,  A61K31/5395 ,  A61K31/55 ,  A61K45/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/10 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D471/04 ,  C07D498/10

摘要： This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.

摘要翻译： 本申请提供式I化合物或其药学上可接受的盐，其中各个变量在本文中定义，以及制备这些化合物的方法，包含其的药物组合物及其用于治疗与CRTH2相关的疾病状态 受体。

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：EP2945632A4

公开(公告)日：2016-09-14

申请号：EP13866588

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 ,  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 ,  DENG QIAOLIN

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

CPC分类号： C07D519/00 ,  C07D487/04

摘要： 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.

摘要翻译： 公开了式（式1）化合物：其中“RG3”“Rd1”〜“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。