公开(公告)号：EP3283464A1

公开(公告)日：2018-02-21

申请号：EP16780505.0

申请日：2016-04-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： MERTZ, Eric ,  EDMONDSON, Scott D. ,  SO, Sung-Sau ,  SUN, Wanying ,  LIU, Weiguo ,  NEELAMKAVIL, Santhosh F. ,  GAO, Ying-Duo ,  HRUZA, Alan ,  ZANG, Yi ,  ALI, Amjad ,  MAL, Rudrajit ,  HE, Jiafang ,  KUANG, Rongze ,  WU, Heping ,  OGAWA, Anthony K. ,  NOLTING, Andrew F.

IPC: C07D233/68 ,  A61K31/426 ,  A61K31/4178 ,  A61P9/00 ,  C07D241/00

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

Abstract: 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：EP2720544B1

公开(公告)日：2016-12-21

申请号：EP12800485.0

申请日：2012-06-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： MILLER, Michael ,  STAMFORD, Andrew ,  BASU, Kallol ,  WOOD, Harold, B. ,  DEMONG, Duane ,  SUN, Wanying ,  GARFUNKLE, Joie ,  MOYES, Christopher ,  HU, Zhiyong ,  LIU, Ping ,  EDMONDSON, Scott, D. ,  DAI, Xing ,  DUBOIS, Byron, Gabriel

IPC: A01N43/40 ,  A61K31/445 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D211/22 ,  C07D211/24 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04

CPC classification number: C07D211/24 ,  C07D211/22 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

公开(公告)号：EP3368036A1

公开(公告)日：2018-09-05

申请号：EP16860556.6

申请日：2016-10-24

Applicant: Merck Sharp & Dohme Corp.

Inventor： XU, Jiayi ,  ALI, Amjad ,  ZHOU, Wei ,  GAO, Ying-Duo ,  EDMONDSON, Scott, D. ,  MERTZ, Eric ,  NEELAMKAVIL, Santhosh, F. ,  LIU, Weiguo ,  SUN, Wanying ,  SHEN, Dong-Ming ,  HARPER, Bart ,  ZHU, Cheng ,  BARA, Thomas ,  LIM, Yeon-Hee ,  YANG, Meng

IPC: A61K31/44 ,  A61K31/4418 ,  A61K31/4427 ,  C07D213/02 ,  C07D213/04 ,  C07D401/06

CPC classification number: C07D401/14 ,  A61K45/06 ,  A61P7/02 ,  C07D401/04 ,  C07D413/14 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D513/08

Abstract: 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：EP2693882B1

公开(公告)日：2017-06-28

申请号：EP12767881.1

申请日：2012-04-05

Applicant: Merck Sharp & Dohme Corp.

Inventor： EDMONDSON, Scott ,  GUO, Zhiqiang ,  GEISS, William, B. ,  WOOD, Harold, B. ,  STAMFORD, Andrew, W. ,  MILLER, Michael, W. ,  DEMONG, Duane, E. ,  MORRIELLO, Gregori, J. ,  ANAND, Rajan ,  COLANDREA, Vincent, J. ,  MACALA, Megan ,  MALETIC, Milana ,  ZHU, Cheng ,  ZHU, Yuping ,  SUN, Wanying ,  ZHAO, Kake ,  HUANG, Yong ,  HARRIS, Joel, M. ,  CHANG, Lehua ,  KAR, Nam Fung ,  HU, Zhiyong ,  WANG, Liping ,  WANG, Bowei ,  LIU, Ping ,  SZEWCZYK, Jason, W.

IPC: C07D211/22 ,  C07D401/12 ,  C07D405/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/506 ,  A61P5/50

CPC classification number: C07D513/04 ,  A61K9/4858 ,  C07D211/22 ,  C07D401/12 ,  C07D405/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

公开(公告)号：EP3148542A1

公开(公告)日：2017-04-05

申请号：EP15800524.9

申请日：2015-05-22

Applicant: Merck Sharp & Dohme Corp.

Inventor： LIU, Weiguo ,  EDMONDSON, Scott D. ,  GUO, Zhuyan ,  MERTZ, Eric ,  OGAWA, Anthony K. ,  SO, Sung-Sau ,  SUN, Wanying ,  BROCKUNIER, Linda L. ,  ALI, Amjad ,  KUANG, Rongze ,  WU, Heping

IPC: A61K31/44 ,  A61K31/4192 ,  A61K31/167

CPC classification number: C07D417/10 ,  C07D213/89 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/10

Abstract: The present invention provides a compound of Formula I(The chemical formula should be inserted here.) 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.

Abstract translation: 本发明提供了式I化合物（化学式应插入此处）和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维化改变的方法。 这些化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。

公开(公告)号：EP2720544A1

公开(公告)日：2014-04-23

申请号：EP12800485.0

申请日：2012-06-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： MILLER, Michael ,  STAMFORD, Andrew ,  BASU, Kallol ,  WOOD, Harold, B. ,  DEMONG, Duane ,  SUN, Wanying ,  GARFUNKLE, Joie ,  MOYES, Christopher ,  HU, Zhiyong ,  LIU, Ping ,  EDMONDSON, Scott, D. ,  DAI, Xing ,  DUBOIS, Byron, Gabriel

IPC: A01N43/40 ,  A61K31/445

CPC classification number: C07D211/24 ,  C07D211/22 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.

Abstract translation: 公开的式I的取代环丙基化合物及其药学上可接受的盐公开用于治疗或预防2型糖尿病和类似病症。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 药物组合物和治疗方法也包括在内。

公开(公告)号：EP2632269A1

公开(公告)日：2013-09-04

申请号：EP11836937.0

申请日：2011-10-25

Applicant: Merck Sharp & Dohme Corp.

Inventor： LU, Zhijian ,  CHEN, Yi-Heng ,  SMITH, Cameron ,  LI, Hong ,  THOMPSON, Christopher, F. ,  SWEIS, Ramzi ,  SINCLAIR, Peter ,  KALLASHI, Florida ,  HUNT, Julianne ,  ADAMSON, Samantha, E. ,  DONG, Guizhen ,  ONDEYKA, Debra, L. ,  QIAN, Xiaoxia ,  SUN, Wanying ,  VACHAL, Petr ,  ZHAO, Kake

IPC: A01N43/76 ,  A61K31/42

CPC classification number: C07D491/08 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14 ,  A61K2300/00

Abstract: CCompounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, A
3 is a substitiuted phenyl group or indanyl group.Formula (I).

公开(公告)号：EP1943224B1

公开(公告)日：2011-07-27

申请号：EP06849833.6

申请日：2006-09-29

Applicant: Merck Sharp & Dohme Corp.

Inventor： GREENLEE, Mark, L. ,  MENG, Dongfang ,  PARKER, Dann, L., Jr. ,  SUN, Wanying ,  WILDONGER, Kenneth, J. ,  WILKENING, Robert, R.

IPC: C07D231/00 ,  A61K31/416 ,  A61K31/4192 ,  C07D249/16

CPC classification number: C07D249/16 ,  C07D231/54 ,  C07D235/02 ,  C07D405/04 ,  C07D413/04

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.

公开(公告)号：EP3978472A1

公开(公告)日：2022-04-06

申请号：EP21204101.6

申请日：2016-12-12

Applicant: MERCK SHARP & DOHME CORP.

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 ,  C07F9/6558 ,  C07C53/18

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 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：EP3226689B1

公开(公告)日：2020-01-15

申请号：EP15866163.7

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： FISCHER, Christian ,  BOGEN, Stephane, L. ,  CHILDERS, Matthew, L. ,  LLINAS, Francesc Xavier Fradera ,  ELLIS, J. Michael ,  ESPOSITE, Sara ,  HOFFMAN, Dawn, M. ,  HUANG, Chunhui ,  KATTAR, Solomon ,  KIM, Alexander, J. ,  LAMPE, John, W. ,  MACHACEK, Michelle, R. ,  MCMASTERS, Daniel, R. ,  PARKER, Dann, L., Jr. ,  REUTERSHAN, Michael ,  SCIAMMETTA, Nunzio ,  SHAO, Pengcheng, P. ,  SLOMAN, David, L. ,  SUN, Wanying ,  UJJAINWALLA, Feroze ,  WU, Zhicai

IPC: A61K31/551 ,  A61P35/00 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00