公开(公告)号：WO2019070492A1

公开(公告)日：2019-04-11

申请号：PCT/US2018/053039

申请日：2018-09-27

Applicant: MERCK SHARP & DOHME CORP. ,  BIFTU, Tesfaye ,  HUANG, Xianhai ,  LIU, Weiguo ,  PAN, Weidong ,  PARK, Min ,  PASTERNAK, Alexander ,  SUN, Wanying ,  TANG, Haifeng ,  ZANG, Yi

Inventor： BIFTU, Tesfaye ,  HUANG, Xianhai ,  LIU, Weiguo ,  PAN, Weidong ,  PARK, Min ,  PASTERNAK, Alexander ,  SUN, Wanying ,  TANG, Haifeng ,  ZANG, Yi

IPC: A61K31/427 ,  A61K31/433 ,  A61K31/4439

Abstract: The present invention relates to monobactam compounds of Formula (I) and pharmaceutically acceptable salts thereof. The present invention also relates to compositions which comprise a monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.

公开(公告)号：WO2017106064A1

公开(公告)日：2017-06-22

申请号：PCT/US2016/066064

申请日：2016-12-12

Applicant: MERCK SHARP & DOHME CORP. ,  TANG, Haifeng ,  LIU, Weiguo ,  DING, Fa-Xiang ,  SUN, Wanying ,  ZANG, Yi ,  PAN, Weidong ,  OGAWA, Anthony ,  BROCKUNIER, Linda ,  HUANG, Xianhai ,  WANG, Hongwu ,  MAL, Rudrajit ,  BIFTU, Tesfaye ,  PARK, Min ,  GUO, Yan ,  JIANG, Jinlong ,  CHEN, Helen ,  PLUMMER, Christopher, W.

Inventor： TANG, Haifeng ,  LIU, Weiguo ,  DING, Fa-Xiang ,  SUN, Wanying ,  ZANG, Yi ,  PAN, Weidong ,  OGAWA, Anthony ,  BROCKUNIER, Linda ,  HUANG, Xianhai ,  WANG, Hongwu ,  MAL, Rudrajit ,  BIFTU, Tesfaye ,  PARK, Min ,  GUO, Yan ,  JIANG, Jinlong ,  CHEN, Helen ,  PLUMMER, Christopher, W.

IPC: C07D205/08 ,  A61K31/397 ,  A61P31/04

CPC classification number: A61K31/397 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A 1 , Q, A 2 , M, W, R X and R z are as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt therof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.

Abstract translation: 本发明涉及式I的联芳基单环内酰胺化合物及其药学上可接受的盐，其中X，Y，Z，A 1，Q，A 2 M，W，R X和R Z如本文所定义。 本发明还涉及包含本发明的联芳单胞菌素化合物或其药学上可接受的盐和药学上可接受的载体的组合物。 本发明还涉及治疗细菌感染的方法，其包括向患者单独或与治​​疗有效量的第二种β-内酰胺抗生素联合给药治疗有效量的本发明化合物。

公开(公告)号：WO2017074914A1

公开(公告)日：2017-05-04

申请号：PCT/US2016/058614

申请日：2016-10-25

Applicant: MERCK SHARP & DOHME CORP. ,  WITTER, David, J. ,  BIFTU, Tesfaye ,  BIJU, Purakkattle ,  BOGEN, Stephane, L. ,  HONG, Qingmei ,  HUANG, Chunhui ,  HUANG, Xianhai ,  LI, Bing ,  PARK, Min, K. ,  SLOMAN, David, L.

Inventor： WITTER, David, J. ,  BIFTU, Tesfaye ,  BIJU, Purakkattle ,  BOGEN, Stephane, L. ,  HONG, Qingmei ,  HUANG, Chunhui ,  HUANG, Xianhai ,  LI, Bing ,  PARK, Min, K. ,  SLOMAN, David, L.

IPC: C07D487/04 ,  C07D487/12

CPC classification number: C07D519/00 ,  C07D471/04

Abstract: The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

Abstract translation: 本发明涉及作为一种或多种突变IDH酶抑制剂的式（I），（Ia）或（Ib）的三环化合物。 本发明还涉及这些三环化合物在潜在治疗或预防其中涉及一种或多种突变IDH酶的癌症中的用途。 本发明还涉及包含这些化合物的组合物。 本发明还涉及这些组合物在潜在预防或治疗这些癌症中的用途。

公开(公告)号：WO2016100051A1

公开(公告)日：2016-06-23

申请号：PCT/US2015/064861

申请日：2015-12-10

Applicant: MERCK SHARP & DOHME CORP. ,  MSD R&D (CHINA) CO., LTD. ,  SILIPHAIVANH, Phieng ,  SLOMAN, David, L. ,  WITTER, David ,  MANSOOR, Umar Faruk ,  KOZLOWSKI, Joseph ,  LIU, Ziping ,  FU, Jianmin ,  WAN, Zhilong ,  LIU, Wei ,  QIAN, Yimin ,  HUANG, Xianhai

Inventor： SILIPHAIVANH, Phieng ,  SLOMAN, David, L. ,  WITTER, David ,  MANSOOR, Umar Faruk ,  KOZLOWSKI, Joseph ,  LIU, Ziping ,  FU, Jianmin ,  WAN, Zhilong ,  LIU, Wei ,  QIAN, Yimin ,  HUANG, Xianhai

IPC: C07D471/04

CPC classification number: C07D498/18 ,  A61K31/437 ,  A61K31/444 ,  C07D471/18 ,  C07D471/22

Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of Formula (I). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).

Abstract translation: 本发明提供了作为ERK2抑制剂的式（I）化合物或其药学上可接受的盐，酯和前药。 本发明还提供了一种在需要这种治疗的患者中抑制ERK2的方法，包括向所述患者施用有效量的至少一种式（I）的化合物。 本发明还提供了在需要这种治疗的患者中治疗癌症的方法，所述方法包括向所述患者施用有效量的至少一种式（I）的化合物。

公开(公告)号：WO2016095088A1

公开(公告)日：2016-06-23

申请号：PCT/CN2014/093858

申请日：2014-12-15

Applicant: MERCK SHARP & DOHME CORP. ,  SILIPHAIVANH, Phieng ,  SLOMAN, David L. ,  WITTER, David ,  MANSOOR, Umar Faruk ,  KOZLOWSKI, Joseph ,  LIU, Ziping ,  FU, Jianmin ,  WAN, Zhilong ,  LIU, Wei ,  QIAN, Yimin ,  HUANG, Xianhai

Inventor： SILIPHAIVANH, Phieng ,  SLOMAN, David L. ,  WITTER, David ,  MANSOOR, Umar Faruk ,  KOZLOWSKI, Joseph ,  LIU, Ziping ,  FU, Jianmin ,  WAN, Zhilong ,  LIU, Wei ,  QIAN, Yimin ,  HUANG, Xianhai

IPC: C07D471/14 ,  C07D498/14 ,  A61K31/437 ,  A61K31/444 ,  A61P35/00

CPC classification number: C07D498/18 ,  A61K31/437 ,  A61K31/444 ,  C07D471/18 ,  C07D471/22

Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors.

Abstract translation: 本发明提供了作为ERK2抑制剂的式（I）化合物或其药学上可接受的盐，酯和前药。

公开(公告)号：WO2015161016A1

公开(公告)日：2015-10-22

申请号：PCT/US2015/026076

申请日：2015-04-16

Applicant: MERCK SHARP & DOHME CORP. ,  CROWLEY, Brendan ,  FRALEY, Mark ,  BURGEY, Chris ,  MITCHELL, Helen ,  BIFTU, Tesfaye ,  NAIR, Anilkumar ,  WANG, Cheng ,  HUANG, Xianhai ,  PARK, Min, K. ,  CAI, Jiaqiang ,  LIU, Qingsheng

Inventor： CROWLEY, Brendan ,  FRALEY, Mark ,  BURGEY, Chris ,  MITCHELL, Helen ,  BIFTU, Tesfaye ,  NAIR, Anilkumar ,  WANG, Cheng ,  HUANG, Xianhai ,  PARK, Min, K. ,  CAI, Jiaqiang ,  LIU, Qingsheng

IPC: C07D213/02 ,  C07D221/00 ,  C07D239/06

CPC classification number: C07D417/14 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

Abstract: The present invention is directed to bicyclic compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的双环化合物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

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：WO2013063214A1

公开(公告)日：2013-05-02

申请号：PCT/US2012/061836

申请日：2012-10-25

Applicant: MERCK SHARP & DOHME CORP. ,  LIM, Jongwon ,  KELLEY, Elizabeth Helen ,  METHOT, Joey, L. ,  ZHOU, Hua ,  PETROCCHI, Alessia ,  MANSOOR, Umar Faruk ,  FISCHER, Christian ,  O'BOYLE, Brendan, M. ,  GUERIN, David Joseph ,  BIENSTOCK, Corey, E. ,  BOYCE, Christopher, W. ,  DANIELS, Matthew, H. ,  FALCONE, Danielle ,  FERGUSON, Ronald, D., II ,  FEVRIER, Salem ,  HUANG, Xianhai ,  LIPFORD, Kathryn Ann ,  SLOMAN, David, L. ,  WILSON, Kevin ,  ZHOU, Wei ,  WITTER, David ,  MALETIC, Milana, M. ,  SILIPHAIVANH, Phieng

Inventor： LIM, Jongwon ,  KELLEY, Elizabeth Helen ,  METHOT, Joey, L. ,  ZHOU, Hua ,  PETROCCHI, Alessia ,  MANSOOR, Umar Faruk ,  FISCHER, Christian ,  O'BOYLE, Brendan, M. ,  GUERIN, David Joseph ,  BIENSTOCK, Corey, E. ,  BOYCE, Christopher, W. ,  DANIELS, Matthew, H. ,  FALCONE, Danielle ,  FERGUSON, Ronald, D., II ,  FEVRIER, Salem ,  HUANG, Xianhai ,  LIPFORD, Kathryn Ann ,  SLOMAN, David, L. ,  WILSON, Kevin ,  ZHOU, Wei ,  WITTER, David ,  MALETIC, Milana, M. ,  SILIPHAIVANH, Phieng

IPC: A61K9/66

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D519/00

Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).

Abstract translation: 公开了式（1）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1）的化合物治疗癌症的方法。

公开(公告)号：WO2010054078A1

公开(公告)日：2010-05-14

申请号：PCT/US2009/063396

申请日：2009-11-05

Applicant: SCHERING CORPORATION ,  ZHU, Zhaoning ,  GREENLEE, William, J. ,  COLE, David, James ,  PISSARNITSKI, Dmitri, A. ,  GALLO, Gioconda, V. ,  LI, Hongmei ,  JOSIEN, Hubert, B. ,  QIN, Jun ,  KNUTSON, Chad, E. ,  MANDAL, Mihirbaran ,  VICAREL, Monica, L. ,  RAJAGOPALAN, Murali ,  DHONDI, Pawan, Kumar ,  XU, Ruo ,  SUN, Zhong-Yue ,  BARA, Thomas, A. ,  HUANG, Xianhai ,  ZHU, Xiaohong ,  ZHAO, Zhiqiang ,  CLADER, John, W. ,  PALANI, Anandan ,  ASBEROM, Theodros ,  MCCRACKEN, Troy ,  BENNETT, Chad, E.

Inventor： ZHU, Zhaoning ,  GREENLEE, William, J. ,  COLE, David, James ,  PISSARNITSKI, Dmitri, A. ,  GALLO, Gioconda, V. ,  LI, Hongmei ,  JOSIEN, Hubert, B. ,  QIN, Jun ,  KNUTSON, Chad, E. ,  MANDAL, Mihirbaran ,  VICAREL, Monica, L. ,  RAJAGOPALAN, Murali ,  DHONDI, Pawan, Kumar ,  XU, Ruo ,  SUN, Zhong-Yue ,  BARA, Thomas, A. ,  HUANG, Xianhai ,  ZHU, Xiaohong ,  ZHAO, Zhiqiang ,  CLADER, John, W. ,  PALANI, Anandan ,  ASBEROM, Theodros ,  MCCRACKEN, Troy ,  BENNETT, Chad, E.

IPC: C07D413/10 ,  C07D471/04 ,  C07D498/04 ,  C07D498/20 ,  A61K31/4245 ,  A61K31/4162 ,  A61P25/28

CPC classification number: C07D471/04 ,  C07D413/10 ,  C07D498/04 ,  C07D498/20 ,  C07F7/0812

Abstract: In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了作为γ-分泌酶的调节剂的新型杂环化合物，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法， 使用这种化合物或药物组合物预防，抑制或改善与中枢神经系统相关的一种或多种疾病。

公开(公告)号：WO2010009212A1

公开(公告)日：2010-01-21

申请号：PCT/US2009/050664

申请日：2009-07-15

Applicant: SCHERING CORPORATION ,  TENDOLKAR, Amol ,  PALANI, Anandan ,  HUANG, Xianhai ,  ASLANIAN, Robert, G.

Inventor： TENDOLKAR, Amol ,  PALANI, Anandan ,  HUANG, Xianhai ,  ASLANIAN, Robert, G.

IPC: C07D213/80 ,  C07D213/83 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052 ,  A61K31/455 ,  A61K31/5415 ,  A61P3/06 ,  A61P3/10

CPC classification number: C07D213/80 ,  C07D213/83 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052

Abstract: The present invention provides compounds of the Formula I: (I) wherein R' represents a recoverable residue of a non-steroidal anti-inflammatory drug (NSAID); and G represents a hydrolysable or metabolizable linker group; and salts, solvates, esters and prodrugs thereof, as well as pharmaceutical compositions containing them, and methods of using them to treat metabolic syndrome, dyslipidemia, cardiovascular diseases, disorders of the peripheral and central nervous system, hematological diseases, cancer, inflammation, respiratory diseases, gastroenterological diseases, diabetes, and non-alcoholic fatty liver diseases.

Abstract translation: 本发明提供式I化合物：（I）其中R'表示非甾体抗炎药（NSAID）的可回收残基; G代表可水解或可代谢的连接基团; 以及其盐，溶剂合物，酯和前药，以及含有它们的药物组合物，以及使用它们治疗代谢综合征，血脂异常，心血管疾病，外周和中枢神经系统疾病，血液疾病，癌症，炎症，呼吸 疾病，胃肠疾病，糖尿病和非酒精性脂肪性肝病。