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1. 发明申请

WO2014022528A1 ANTIDIABETIC TRICYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2014022528A1
公开(公告)日：2014-02-06
申请号：PCT/US2013/052961
申请日：2013-07-31
申请人： MERCK SHARP & DOHME CORP. , HAGMANN, William, K. , NARGUND, Ravi, P. , BLIZZARD, Timothy, A. , JOSIEN, Hubert , BIJU, Purakkattle , PLUMMER, Christopher, W. , DANG, Qun , LI, Bing , LIN, Linus, S. , CUI, Mingxiang , HU, Bin , HAO, Jinglai , CHEN, Zhengxia
发明人： HAGMANN, William, K. , NARGUND, Ravi, P. , BLIZZARD, Timothy, A. , JOSIEN, Hubert , BIJU, Purakkattle , PLUMMER, Christopher, W. , DANG, Qun , LI, Bing , LIN, Linus, S. , CUI, Mingxiang , HU, Bin , HAO, Jinglai , CHEN, Zhengxia
IPC分类号： C07D401/14 , C07D221/16 , C07D401/12 , C07F9/40 , A61K31/435 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07F9/582 , A61K31/435 , A61K31/4412 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D221/16 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/14 , C07D417/12
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, 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.

2. 发明申请

WO2013096093A1 COMPOUNDS AS DGAT-1 INHIBITORS 审中-公开
标题翻译：化合物作为DGAT-1抑制剂
公开(公告)号：WO2013096093A1
公开(公告)日：2013-06-27
申请号：PCT/US2012/069616
申请日：2012-12-14
申请人： MERCK SHARP & DOHME CORP. , DEVITA, Robert, J. , HE, Shuwen , LIU, Jian , CERNAK, Timothy, A. , KRIKORIAN, Arto, D. , YANG, Ginger XuQiang , WU, Zhicai , YU, Yang , SHEN, Dong-Ming , LAI, Zhong , HONG, Qingmei , NARGUND, Ravi, P.
发明人： DEVITA, Robert, J. , HE, Shuwen , LIU, Jian , CERNAK, Timothy, A. , KRIKORIAN, Arto, D. , YANG, Ginger XuQiang , WU, Zhicai , YU, Yang , SHEN, Dong-Ming , LAI, Zhong , HONG, Qingmei , NARGUND, Ravi, P.
IPC分类号： A61K31/44
CPC分类号： C07D401/14 , C07D249/08 , C07D401/04 , C07D401/10 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D493/04
摘要： Described herein are compounds of formula I. The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
摘要翻译：本文描述的是式I化合物。式I化合物作为DGAT1抑制剂，可用于预防，治疗或作为高脂血症，糖尿病和肥胖症的补救剂。

3. 发明申请

WO2010065432A1 NITROOXY DERIVATIVES AS ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： NITROOXY衍生物作为血管紧张素II受体拮抗剂
公开(公告)号：WO2010065432A1
公开(公告)日：2010-06-10
申请号：PCT/US2009/066041
申请日：2009-11-30
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael Man-Chu , NARGUND, Ravi, P.
发明人： ALI, Amjad , LO, Michael Man-Chu , NARGUND, Ravi, P.
IPC分类号： C07D235/08 , C07D257/04 , C07D403/10 , C07D409/06 , A61K31/164 , A61K31/4178 , A61K31/4184
CPC分类号： C07D403/10 , C07D235/08 , C07D257/04 , C07D409/06
摘要： A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is Y is selected from the group consisting of R1 is selected from the group consisting of -O-C 1-6 alkyl, -O-aryl, -O-heteroaryl, -O-C 3-8 cycloalkyl, -C 1-6 alkyl, -aryl, -heteroaryl, and -C 3-8 cycloalkyl; R 2 and R 3 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是Y选自由R 1选自-OC 1-6烷基，-O-芳基，-O-杂芳基，-OC 3-8环烷基，-C 1-6烷基， - 芳基， - 杂芳基和-C 3-8环烷基; R2和R3独立地选自氢和C 1-4烷基，或其药学上可接受的盐或水合物，其可用于治疗高血压。

4. 发明申请

WO2008076246A3 NITRODERIVATIVES AS ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2008076246A3
公开(公告)日：2009-01-15
申请号：PCT/US2007025232
申请日：2007-12-11
申请人： MERCK & CO INC , NICOX SA , SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARGUND RAVI P , ALI AMJAD , FRANKLIN CHRIS , ALMIRANTE NICOLETTA , STORONI LAURA , STEFANINI SILVIA
发明人： SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARGUND RAVI P , ALI AMJAD , FRANKLIN CHRIS , ALMIRANTE NICOLETTA , STORONI LAURA , STEFANINI SILVIA
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (Formula I), wherein R is an angiotensin receptor antagonist active group, Y is -Y1-Y2-Y3-Y4-Y5.; Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and -0C(0)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is -(CH2) 1-2-(X)0-1-(CH2)0-1- or is absent; X is -O- or -CR3R4-; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构（式I）的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是-Y1-Y2-Y3-Y4-Y5。 Y1是C（R1R2）; R 1选自氢和C 1-4烷基; R 2选自氢，C 1-4烷基和-C（O）C 1-4烷基; Y2是O或CH2; Y 3是C（O）或CH 2; Y4是O或CH2; Y 5是 - （CH 2）1-2 - （X）0-1 - （CH 2）0-1-或不存在; X是-O-或-CR 3 R 4 - ; 并且R 3和R 4独立地选自氢和C 1 -C 4烷基; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

5. 发明申请

WO2008076245A3 NITRODERIVATIVES AS ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2008076245A3
公开(公告)日：2008-09-12
申请号：PCT/US2007025231
申请日：2007-12-11
申请人： MERCK & CO INC , SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARGUND RAVI P , ALI AMJAD
发明人： SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARGUND RAVI P , ALI AMJAD
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (Formula I), wherein Y is -Y 1 -Y 2 -Y 3 -Y 4 -Y 5 -; Y 1 is C(O) or C(R 1 R 2 ); Y 2 is O, C(O), P(O)(OH) or CH 2 , provided that when Y 1 is C(O), Y 2 is not C(O); R 1 is selected from the group consisting of hydrogen and C 1-4 alkyl; R 2 is selected from the group consisting of hydrogen, C 1-4 alkyl, and -OC(O)C 1-4 alkyl; Y 3 is O, C(O) or CH 2 , provided that when Y 2 is C(O), then Y 3 is not C(O), and further provided that when Y 2 is O, then Y 3 is not O; Y 4 is O or CH 2 or is absent, provided that when Y 3 is O, then Y 4 is not O; Y5 is -(CH 2 ) 1-2 -(X) 0- l -(CH 2 ) 0-l - or is absent; X is -O- or -CR 3 R 4 -; and R 3 and R 4 are independently selected from the group consisting of hydrogen and C 1 -C 4 alkyl; or a pharmaceutically acceptable salt thereof, which is useful for treating hypertension.
摘要翻译：具有结构（式I）的化合物，其中Y为-Y 1 -Y 2 -Y 3 -Y 4 - / SUP> -Y ^{5 - ; Y 1是C（O）或C（R 1 R 2）2）。 Y 2是O，C（O），P（O）（OH）或CH 2，条件是当Y 1是C（ O），Y 2不是C（O）; R 1选自氢和C 1-4烷基; R 2选自氢，C 1-4烷基和-OC（O）C 1-4烷基; Y 3是O，C（O）或CH 2，条件是当Y 2是C（O）时，则Y 3不是C（O），并且进一步地，当Y 2为O时，Y 3不为O; Y 4是O或CH 2或不存在，条件是当Y 3为O时，则Y 4为O，不是O Y 5是 - （CH 2）2 - （X）0-1 - （CH 2）2 - 0-1 - 或不存在; X是-O-或-CR 3 R 4 - 。和R 3和R 4独立地选自氢和C 1 -C 4烷基 ; 或其药学上可接受的盐，其可用于治疗高血压。}

6. 发明申请

WO2008073311A3 SUBSTITUTED DIAZEPINE SULFONAMIDES AS BOMBESIN RECEPTOR SUBTYPE-3 MODULATORS 审中-公开
公开(公告)号：WO2008073311A3
公开(公告)日：2008-06-19
申请号：PCT/US2007/025104
申请日：2007-12-07
申请人： MERCK & CO., INC. , BAKER, Robert, K. , CHANG, Linda, L. , CHIODA, Marc , CHOBANIAN, Harry, R. , GAO, Ying-Duo , GUO, Yan , LIN, Linus, S. , LIU, Ping , NARGUND, Ravi, P. , RUPPRECHT, Kathleen, M. , MIAO, Shouwu
发明人： BAKER, Robert, K. , CHANG, Linda, L. , CHIODA, Marc , CHOBANIAN, Harry, R. , GAO, Ying-Duo , GUO, Yan , LIN, Linus, S. , LIU, Ping , NARGUND, Ravi, P. , RUPPRECHT, Kathleen, M. , MIAO, Shouwu
IPC分类号： C07D471/04 , C07D471/14 , A61K31/551 , A61P31/04
摘要： Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.

7. 发明申请

WO2006019787A2 ACYLATED PIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR AGONISTS 审中-公开
标题翻译：作为MELANOCORTIN-4受体激动剂的酰基哌啶衍生物
公开(公告)号：WO2006019787A2
公开(公告)日：2006-02-23
申请号：PCT/US2005/024806
申请日：2005-07-13
申请人： MERCK & CO., INC. , BARAKAT, Khaled, J. , GUO, Liangqin , LIU, Jian , NARGUND, Ravi, P. , SEBHAT, Iyassu, K. , YE, Zhixiong
发明人： BARAKAT, Khaled, J. , GUO, Liangqin , LIU, Jian , NARGUND, Ravi, P. , SEBHAT, Iyassu, K. , YE, Zhixiong
IPC分类号： A61K31/454 , A61K31/445
CPC分类号： C07D211/62 , C07D401/06 , C07D401/14
摘要： Certain novel N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
摘要翻译：某些新的N-酰化哌啶衍生物是人类黑皮质素受体的激动剂，特别是人黑皮质素-4受体（MC-4R）的选择性激动剂。因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。

8. 发明申请

WO2004087159A1 BICYCLIC PIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR AGONISTS 审中-公开
标题翻译：双酚A衍生物作为MELANOCORTIN-4受体激动剂
公开(公告)号：WO2004087159A1
公开(公告)日：2004-10-14
申请号：PCT/US2004/008711
申请日：2004-03-22
申请人： MERCK & CO., INC. , NARGUND, Ravi, P. , YE, Zhixiong , GUO, Liangqin
发明人： NARGUND, Ravi, P. , YE, Zhixiong , GUO, Liangqin
IPC分类号： A61K31/46
CPC分类号： C07D451/02
摘要： Certain novel bicyclic N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
摘要翻译：某些新型双环N-酰化哌啶衍生物是人类黑皮质素受体的激动剂，特别是人黑皮质素-4受体（MC-4R）的选择性激动剂。因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。

9. 发明申请

WO2004024720A1 PIPERAZINE UREA DERIVATIVES AS MELANOCORTIN-4 RECEPTOR AGONISTS 审中-公开
标题翻译：作为梅毒素-4受体激动剂的哌嗪尿酸衍生物
公开(公告)号：WO2004024720A1
公开(公告)日：2004-03-25
申请号：PCT/US2003/027892
申请日：2003-09-05
申请人： MERCK & CO., INC. , BAKSHI, Raman Kumar , NARGUND, Ravi, P. , PALUCKI, Brenda, L. , PARK, Min, K. , YE, Zhixiong
发明人： BAKSHI, Raman Kumar , NARGUND, Ravi, P. , PALUCKI, Brenda, L. , PARK, Min, K. , YE, Zhixiong
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D211/18 , C07D211/22 , C07D211/62 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08
摘要： Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity and diabetes.
摘要翻译：某些新型哌嗪脲衍生物是人类黑皮质素-4受体（MC-4R）的激动剂，特别是MC-4R的受体亚型选择性激动剂。它们可用于治疗，控制或预防对MC-4R活化反应的疾病和病症，例如肥胖症和糖尿病。

10. 发明申请

WO2015051052A3 GLUCOSE-RESPONSIVE INSULIN CONJUGATES 审中-公开
标题翻译：葡萄糖反应性胰岛素结合
公开(公告)号：WO2015051052A3
公开(公告)日：2015-07-02
申请号：PCT/US2014058714
申请日：2014-10-02
申请人： MERCK SHARP & DOHME , LIN SONGNIAN , YAN LIN , KEKEC AHMET , ZHU YUPING , HUNTER DAVID N , HUO PEI , FENG DANQING , NARGUND RAVI P , MOYES CHRISTOPHER R , ZHAO ZHIQIANG , PIPIK BRENDA , PISSARNITSKI DMITRI , DUFFY JOSEPH L , GUIDRY ERIN N
发明人： LIN SONGNIAN , YAN LIN , KEKEC AHMET , ZHU YUPING , HUNTER DAVID N , HUO PEI , FENG DANQING , NARGUND RAVI P , MOYES CHRISTOPHER R , ZHAO ZHIQIANG , PIPIK BRENDA , PISSARNITSKI DMITRI , DUFFY JOSEPH L , GUIDRY ERIN N
IPC分类号： A61K47/48 , A61P3/10
CPC分类号： A61K47/4823 , A61K38/28 , A61K47/48092 , A61K47/549 , A61K47/61 , C07K14/62
摘要： Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.
摘要翻译：胰岛素缀合物包含共价连接到具有两个臂的至少一个双齿连接体的胰岛素分子，每个臂独立地连接到包含糖的配体，并且其中至少一个连接体的配体是岩藻糖。胰岛素缀合物显示药代动力学（PK）和/或药效学（PD）谱，其对糖类如葡萄糖或α-甲基甘露糖的全身浓度有反应，即使在不存在外源多价的情况下施用于有需要的受试者时糖结合分子如Con A.

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