公开(公告)号：WO2017095760A1

公开(公告)日：2017-06-08

申请号：PCT/US2016/063893

申请日：2016-11-29

申请人： MERCK SHARP & DOHME CORP. ,  OGAWA, Anthony, K. ,  BROCKUNIER, Linda, L. ,  TATA, James ,  PARKER, Dann, L., Jr. ,  WANG, Ming

发明人： OGAWA, Anthony, K. ,  BROCKUNIER, Linda, L. ,  TATA, James ,  PARKER, Dann, L., Jr. ,  WANG, Ming

IPC分类号： C07D213/00 ,  A61K31/44

CPC分类号： C07D409/14 ,  C07D401/10 ,  C07D401/14

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.

摘要翻译： 本发明提供了式I化合物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：WO2015089809A1

公开(公告)日：2015-06-25

申请号：PCT/CN2013/090014

申请日：2013-12-19

申请人： MERCK SHARP & DOHME CORP. ,  HAGMANN, William K. ,  LI, Bing ,  SZEWCZYK, Jason W. ,  WANG, Bowei ,  PARKER, Dann ,  BLIZZARD, Timothy ,  JOSIEN, Hubert ,  BIJU, Purakkattle ,  CHOBANIAN, Harry ,  GUDE, Candido ,  NARGUND, Ravi P. ,  PIO, Barbara ,  DANG, Qun ,  LIN, Linus S. ,  HU, Bin ,  CUI, Mingxiang ,  CHEN, Zhengxia ,  DAI, Meibi ,  ZHANG, Zaihong ,  LV, Ying ,  TIAN, Lili

发明人： HAGMANN, William K. ,  LI, Bing ,  SZEWCZYK, Jason W. ,  WANG, Bowei ,  PARKER, Dann ,  BLIZZARD, Timothy ,  JOSIEN, Hubert ,  BIJU, Purakkattle ,  CHOBANIAN, Harry ,  GUDE, Candido ,  NARGUND, Ravi P. ,  PIO, Barbara ,  DANG, Qun ,  LIN, Linus S. ,  HU, Bin ,  CUI, Mingxiang ,  CHEN, Zhengxia ,  DAI, Meibi ,  ZHANG, Zaihong ,  LV, Ying ,  TIAN, Lili

IPC分类号： C07D213/30 ,  C07D401/04 ,  C07D409/04 ,  C07D487/04 ,  C07D405/12 ,  C07D405/14 ,  C07D401/12 ,  C07D401/14 ,  C07D493/04 ,  C07D451/02 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/4427 ,  A61K31/44

CPC分类号： C07D493/04 ,  A61K31/437 ,  A61K31/438 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/46 ,  A61K31/505 ,  A61K31/506 ,  A61K45/06 ,  C07D213/64 ,  C07D213/74 ,  C07D221/20 ,  C07D239/34 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/04 ,  C07D451/06 ,  C07D471/04

摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

摘要翻译： 本发明涉及由式I表示的化合物及其药学上可接受的盐。 式I化合物是G蛋白偶联受体40（GPR40）的激动剂，可用于治疗，预防和抑制由G蛋白偶联受体40介导的疾病。本发明的化合物可能是有用的 在治疗2型糖尿病以及通常与该疾病有关的病症，包括肥胖症和脂质疾病，例如混合型或糖尿病性血脂异常，高脂血症，高胆固醇血症和高甘油三酯血症。

公开(公告)号：WO2010019206A1

公开(公告)日：2010-02-18

申请号：PCT/US2009/004569

申请日：2009-08-10

申请人： MERCK SHARP & DOHME CORP. ,  SCYNEXIS, INC. ,  GREENLEE, Mark, L. ,  WILKENING, Robert ,  APGAR, James ,  SPERBECK, Donald ,  WILDONGER, Kenneth, James ,  MENG, Dongfang ,  PARKER, Dann, L., Jr. ,  MAMAI, Ahmed

发明人： GREENLEE, Mark, L. ,  WILKENING, Robert ,  APGAR, James ,  SPERBECK, Donald ,  WILDONGER, Kenneth, James ,  MENG, Dongfang ,  PARKER, Dann, L., Jr. ,  MAMAI, Ahmed

IPC分类号： A01N43/64 ,  A61K31/21 ,  A61K31/41

CPC分类号： A61K31/21 ,  A61K31/41 ,  C07D405/04

摘要： Novel derivatives of enfumafungin are disclosed herein, along with' their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and method of using such compounds as antifungal agents and/or inhibitors of (l,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

摘要翻译： 本文公开了enfumafungin的新型衍生物以及“其药学上可接受的盐，水合物和前药”。 还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这种化合物作为（1,3）-β-D-葡聚糖合酶的抗真菌剂和/或抑制剂的方法。 所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。

公开(公告)号：WO2003015761A1

公开(公告)日：2003-02-27

申请号：PCT/US2002/025377

申请日：2002-08-09

申请人： MERCK & CO., INC. ,  MENG, Dongfang ,  PARKER, Dann, LeRoy, Jr. ,  RATCLIFFE, Ronald, W. ,  WILKENING, Robert, R.

发明人： MENG, Dongfang ,  PARKER, Dann, LeRoy, Jr. ,  RATCLIFFE, Ronald, W. ,  WILKENING, Robert, R.

IPC分类号： A61K31/135

CPC分类号： C07D295/088 ,  A61K31/135 ,  C07B2200/07 ,  C07C225/22 ,  C07C255/47 ,  C07C255/58 ,  C07C2603/18 ,  C07C2603/86 ,  C07D307/46

摘要： 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, and cancer, in particular of the breast, uterus and prostate.

摘要翻译： 本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。 本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特氏病，牙周病 ，软骨变性，子宫内膜异位症，子宫肌瘤病，热潮红症，低密度脂蛋白胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育不良，血管平滑肌细胞增殖，肥胖症，失禁和癌症 的乳房，子宫和前列腺。

公开(公告)号：WO2016191334A1

公开(公告)日：2016-12-01

申请号：PCT/US2016/033692

申请日：2016-05-23

申请人： MERCK SHARP & DOHME CORP. ,  GARFUNKLE, Joie ,  ORNOSKI, Olga ,  PARKER, Dann, L., Jr. ,  RAGHAVAN, Subharekha ,  XU, Libo

发明人： GARFUNKLE, Joie ,  ORNOSKI, Olga ,  PARKER, Dann, L., Jr. ,  RAGHAVAN, Subharekha ,  XU, Libo

IPC分类号： C07D487/04 ,  A61K31/519

CPC分类号： A61K31/519 ,  A61K45/06 ,  A61P9/08 ,  C07D519/00

摘要： A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate ("cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or pharmaceutically acceptable salt thereofs, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or pharmaceutically acceptable salts thereof.

摘要翻译： 式I化合物或其药学上可接受的盐能够调节身体产生环鸟苷酸（“cGMP”），并且通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。 本发明还涉及用于制备式I化合物或其药学上可接受的盐的方法，用于治疗和预防上述疾病和用于制备用于此目的的药物，以及包含式I化合物或 其药学上可接受的盐。

公开(公告)号：WO2016133793A1

公开(公告)日：2016-08-25

申请号：PCT/US2016/017652

申请日：2016-02-12

申请人： MERCK SHARP & DOHME CORP. ,  MENG, Dongfang ,  LI, Hong ,  YANG, Meng ,  RUIZ, Manuel de Lera ,  DEWNANI, Sunita, V. ,  JIAN, Tianying ,  PARKER, Dann, L., Jr. ,  ZHANG, Ting ,  CAMPEAU, Louis-Charles ,  HARPER, Bart ,  WOOD, Harold, B. ,  XU, Jiayi ,  BERGER, Richard ,  WU, Jane Yang ,  ORR, Robert, K. ,  WALSH, Shawn, P.

发明人： MENG, Dongfang ,  LI, Hong ,  YANG, Meng ,  RUIZ, Manuel de Lera ,  DEWNANI, Sunita, V. ,  JIAN, Tianying ,  PARKER, Dann, L., Jr. ,  ZHANG, Ting ,  CAMPEAU, Louis-Charles ,  HARPER, Bart ,  WOOD, Harold, B. ,  XU, Jiayi ,  BERGER, Richard ,  WU, Jane Yang ,  ORR, Robert, K. ,  WALSH, Shawn, P.

IPC分类号： A61K31/33 ,  A61K31/41 ,  A61K31/395 ,  A61K31/4164 ,  A61K31/4184

CPC分类号： C07D471/04 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/14 ,  C07D498/04 ,  C07D513/04

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 unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.

摘要翻译： 本发明提供式I化合物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不稳定型心绞痛，难治性心绞痛，心肌梗死，短暂性脑缺血发作，心房颤动，血栓性中风，栓塞性中风的方法 ，深静脉血栓形成，弥散性血管内凝血，眼纤维蛋白增多，以及再通血管再狭窄或再狭窄。 该化合物是选择性因子IXa抑制剂。

公开(公告)号：WO2016089797A1

公开(公告)日：2016-06-09

申请号：PCT/US2015/063061

申请日：2015-12-01

申请人： MERCK SHARP & DOHME CORP. ,  FISCHER, Christian ,  BOGEN, Stephane, L. ,  CHILDERS, Matthew, L. ,  LLINAS, Francesc Xavier Fradera ,  ELLIS, J. Michael ,  ESPOSITE, Sara ,  HONG, Qingmei ,  HUANG, Chunhui ,  KIM, Alexander, J. ,  LAMPE, John, W. ,  MACHACEK, Michelle, R. ,  MCMASTERS, Daniel, R. ,  OTTE, Ryan, D. ,  PARKER, Dann, L., Jr. ,  REUTERSHAN, Michael ,  SCIAMMETTA, Nunzio ,  SHAO, Pengcheng, P. ,  SLOMAN, David, L. ,  UJJAINWALLA, Feroze ,  WHITE, Catherine ,  WU, Zhicai ,  YU, Yang ,  ZHAO, Kake ,  GIBEAU, Craig ,  BIFTU, Tesfaye ,  BIJU, Purakkattle ,  CHEN, Lei ,  CLOSE, Joshua ,  FULLER, Peter, H. ,  HUANG, Xianhai ,  PARK, Min, K. ,  SIMOV, Vladimir ,  WITTER, David, J. ,  ZHANG, Hongjun

发明人： FISCHER, Christian ,  BOGEN, Stephane, L. ,  CHILDERS, Matthew, L. ,  LLINAS, Francesc Xavier Fradera ,  ELLIS, J. Michael ,  ESPOSITE, Sara ,  HONG, Qingmei ,  HUANG, Chunhui ,  KIM, Alexander, J. ,  LAMPE, John, W. ,  MACHACEK, Michelle, R. ,  MCMASTERS, Daniel, R. ,  OTTE, Ryan, D. ,  PARKER, Dann, L., Jr. ,  REUTERSHAN, Michael ,  SCIAMMETTA, Nunzio ,  SHAO, Pengcheng, P. ,  SLOMAN, David, L. ,  UJJAINWALLA, Feroze ,  WHITE, Catherine ,  WU, Zhicai ,  ZHAO, Kake ,  GIBEAU, Craig ,  BIFTU, Tesfaye ,  BIJU, Purakkattle ,  CHEN, Lei ,  CLOSE, Joshua ,  FULLER, Peter, H. ,  HUANG, Xianhai ,  PARK, Min, K. ,  SIMOV, Vladimir ,  WITTER, David, J. ,  ZHANG, Hongjun

IPC分类号： A01N43/00

CPC分类号： C07D498/08 ,  A01N43/00 ,  C07D471/04 ,  C07D471/08 ,  C07D498/04 ,  C07D498/10

摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein 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.

摘要翻译： 本发明涉及作为一种或多种突变体IDH酶的抑制剂的式（I）的三环化合物：（I）。 本发明还涉及本文所述的三环化合物在潜在的治疗或预防涉及一种或多种突变体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这种癌症的潜在预防或治疗中的用途。

公开(公告)号：WO2015187470A1

公开(公告)日：2015-12-10

申请号：PCT/US2015/033084

申请日：2015-05-29

申请人： MERCK SHARP & DOHME CORP. ,  CAMPBELL, Brian, T. ,  DONG, Guizhen ,  GARFUNKLE, Joie ,  KIM, Alexander ,  ORNOSKI, Olga ,  PARKER, Dann, L., Jr. ,  RAGHAVAN, Subharekha ,  XU, Libo ,  YANG, Zhiqiang

发明人： CAMPBELL, Brian, T. ,  DONG, Guizhen ,  GARFUNKLE, Joie ,  KIM, Alexander ,  ORNOSKI, Olga ,  PARKER, Dann, L., Jr. ,  RAGHAVAN, Subharekha ,  XU, Libo ,  YANG, Zhiqiang

IPC分类号： C07D487/04

CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06

摘要： A compound of Formula II or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate ("cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula II, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula II or a pharmaceutically acceptable salt thereof.

摘要翻译： 式II化合物或其药学上可接受的盐能够调节身体产生环鸟嘌呤一磷酸（“cGMP”），并且通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。 本发明还涉及用于制备式II化合物或其药学上可接受的盐的方法，用于治疗和预防上述疾病和用于制备用于该目的的药物以及包含式II化合物的药物制剂 或其药学上可接受的盐。

公开(公告)号：WO2015148350A3

公开(公告)日：2015-11-26

申请号：PCT/US2015021944

申请日：2015-03-23

申请人： MERCK SHARP & DOHME ,  MITCHELL HELEN ,  FRALEY MARK E ,  COOKE ANDREW J ,  STUMP CRAIG A ,  ZHANG XU-FANG ,  MCCOMAS CASEY C ,  SCHIRRIPA KATHY ,  MCWHERTER MELODY ,  LIU PING ,  PARKER DANN ,  LI CHUN SING ,  MAO QINGHUA

发明人： MITCHELL HELEN ,  FRALEY MARK E ,  COOKE ANDREW J ,  STUMP CRAIG A ,  ZHANG XU-FANG ,  MCCOMAS CASEY C ,  SCHIRRIPA KATHY ,  MCWHERTER MELODY ,  LIU PING ,  PARKER DANN ,  LI CHUN SING ,  MAO QINGHUA

IPC分类号： A61K31/166

CPC分类号： C07D487/04 ,  C07D231/40 ,  C07D277/46 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

摘要翻译： 本发明涉及作为原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂的式（I）（式（I））的取代的五元杂芳基苯甲酰胺化合物，因此可用于治疗疼痛，炎症，癌症 ，再狭窄，动脉粥样硬化，牛皮癣，血栓形成，疾病，障碍，损伤或与神经生长因子（NGF）受体TrkA的异常活动相关的疾病或病症相关的异常髓鞘或脱髓鞘的功能障碍。

公开(公告)号：WO2015148350A2

公开(公告)日：2015-10-01

申请号：PCT/US2015/021944

申请日：2015-03-23

申请人： MERCK SHARP & DOHME CORP. ,  MITCHELL, Helen ,  FRALEY, Mark, E. ,  COOKE, Andrew, J. ,  STUMP, Craig, A. ,  ZHANG, Xu-Fang ,  MCCOMAS, Casey, C. ,  SCHIRRIPA, Kathy ,  MCWHERTER, Melody ,  LIU, Ping ,  PARKER, Dann ,  LI, Chun Sing ,  MAO, Qinghua

发明人： MITCHELL, Helen ,  FRALEY, Mark, E. ,  COOKE, Andrew, J. ,  STUMP, Craig, A. ,  ZHANG, Xu-Fang ,  MCCOMAS, Casey, C. ,  SCHIRRIPA, Kathy ,  MCWHERTER, Melody ,  LIU, Ping ,  PARKER, Dann ,  LI, Chun Sing ,  MAO, Qinghua

IPC分类号： A61K31/501 ,  A61K31/4439

CPC分类号： C07D487/04 ,  C07D231/40 ,  C07D277/46 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

摘要翻译： 本发明涉及作为原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂的式（I）（式（I））的取代的五元杂芳基苯甲酰胺化合物，因此可用于 治疗与神经生长因子（NGF）受体TrkA的异常活性有关的疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成，疾病，病症，损伤或与dysmyelination或脱髓鞘相关的功能障碍或疾病或病症。