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1. 发明申请

WO2018039094A1 PYRIDINE-1-OXIDE DERIVATIVES AND THEIR USE AS FACTOR XIA INHIBITORS 审中-公开
标题翻译：吡啶-1-氧化物衍生物及其作为因子XIA抑制剂的用途
公开(公告)号：WO2018039094A1
公开(公告)日：2018-03-01
申请号：PCT/US2017/047718
申请日：2017-08-21
申请人： MERCK SHARP & DOHME CORP. , SHEN, Dong-Ming , KUANG, Rongze , KUMAR, Puneet , DUFFY, Joseph, L. , ZHU, Cheng , ALI, Amjad , YANG, Meng , DEBENHAM, John, S.
发明人： SHEN, Dong-Ming , KUANG, Rongze , KUMAR, Puneet , DUFFY, Joseph, L. , ZHU, Cheng , ALI, Amjad , YANG, Meng , DEBENHAM, John, S.
IPC分类号： C07D213/89 , A61K31/4425 , A61P7/02
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。

2. 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.

3. 发明申请

WO2008066803A2 SUBSTITUTED PIPERIZINES FOR THE TREATMENT OF PAIN 审中-公开
标题翻译：用于治疗疼痛的替代管
公开(公告)号：WO2008066803A2
公开(公告)日：2008-06-05
申请号：PCT/US2007/024430
申请日：2007-11-26
申请人： MERCK & CO, INC. , ABBADIE, Catherine , CHAKRAVARTY, Prasun, K. , DUFFY, Joseph, L.
发明人： ABBADIE, Catherine , CHAKRAVARTY, Prasun, K. , DUFFY, Joseph, L.
IPC分类号： A61K31/495 , A61P29/00
CPC分类号： A61K31/495
摘要： The present invention is directed to the use of substituted piperizine compounds represented by Formula I, for the treatment of pain, including acute pain, chronic pain, cancer pain, visceral pain, inflammatory pain, neuropathic pain, post-herpetic neuralgia, diabetic neuropathy, trigeminal neuralgia, migraine, and fibromyalgia.
摘要翻译：本发明涉及式I代表的取代哌嗪化合物用于治疗疼痛的用途，包括急性疼痛，慢性疼痛，癌症疼痛，内脏痛，炎性疼痛，神经性疼痛，疱疹后神经痛，糖尿病性神经病变，三叉神经痛，偏头痛和纤维肌痛。

4. 发明申请

WO2012024183A1 SPIROXAZOLIDINONE COMPOUNDS 审中-公开
标题翻译： SPIROXAZOLIDINONE化合物
公开(公告)号：WO2012024183A1
公开(公告)日：2012-02-23
申请号：PCT/US2011/047590
申请日：2011-08-12
申请人： MERCK SHARP & DOHME CORP. , DUFFY, Joseph, L. , BAO, Jianming , ONDEYKA, Debra, L. , TYAGARAJAN, Sriram , SHAO, Patrick , YE, Feng , KATIPALLY, Revathi , ZWICKER, Aaron , SHERER, Edward, C. , PLOTKIN, Michael A. , MONINGKA, Remond , HUSSIAN, Zahid , WOOD, Harold B. , UJJAINWALLA, Feroze , ROMERO, Anthony , FINKE, Paul , ZANG, Yi , LIU, Weiguo
发明人： DUFFY, Joseph, L. , BAO, Jianming , ONDEYKA, Debra, L. , TYAGARAJAN, Sriram , SHAO, Patrick , YE, Feng , KATIPALLY, Revathi , ZWICKER, Aaron , SHERER, Edward, C. , PLOTKIN, Michael A. , MONINGKA, Remond , HUSSIAN, Zahid , WOOD, Harold B. , UJJAINWALLA, Feroze , ROMERO, Anthony , FINKE, Paul , ZANG, Yi , LIU, Weiguo
IPC分类号： A01N43/76 , A61K31/42
CPC分类号： C07D498/10 , C07D519/00
摘要： Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
摘要翻译：结构式（I）的取代的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，可用于治疗，控制或预防对SSTR5的拮抗作用有响应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍，肥胖症，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。

5. 发明申请

WO2010129729A1 SUBSTITUTED SPIROCYCLIC AMINES USEFUL AS ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译：取代的螺环化合物作为抗真菌剂有用
公开(公告)号：WO2010129729A1
公开(公告)日：2010-11-11
申请号：PCT/US2010/033808
申请日：2010-05-06
申请人： MERCK SHARP & DOHME CORP. , ASTER, Susan, D. , DUFFY, Joseph, L. , LIANG, Gui-Bai , SHAO, Patrick , YE, Feng
发明人： ASTER, Susan, D. , DUFFY, Joseph, L. , LIANG, Gui-Bai , SHAO, Patrick , YE, Feng
IPC分类号： C07D471/10 , A61K31/435 , A61P3/10
CPC分类号： C07D471/10
摘要： Substituted spirocyclic amines of structural formula I are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
摘要翻译：结构式I的取代的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，可用于治疗，控制或预防对SSTR5的拮抗作用有反应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍，肥胖，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。

6. 发明申请

WO2004069162A2 3-AMINO-4-PHENYLBUTANOIC ACID DERIVATIVES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 审中-公开
公开(公告)号：WO2004069162A2
公开(公告)日：2004-08-19
申请号：PCT/US2004/002309
申请日：2004-01-27
申请人： MERCK & CO., INC. , ASHTON, Wallace, T. , CALDWELL, Charles, G. , DUFFY, Joseph, L. , MATHVINK, Robert, J. , WANG, Liping , WEBER, Ann, E.
发明人： ASHTON, Wallace, T. , CALDWELL, Charles, G. , DUFFY, Joseph, L. , MATHVINK, Robert, J. , WANG, Liping , WEBER, Ann, E.
IPC分类号： A61K
CPC分类号： C07D471/04 , C07D217/06 , C07D217/26
摘要： The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.

7. 发明申请

WO2003082817A2 BETA-AMINO HETEROCYCLIC DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 审中-公开
标题翻译： BETA-AMINO杂环二肽磷酸二酯酶抑制剂，用于治疗或预防糖尿病
公开(公告)号：WO2003082817A2
公开(公告)日：2003-10-09
申请号：PCT/US2003/008723
申请日：2003-03-21
申请人： MERCK & CO., INC. , BROCKUNIER, Linda, L. , DUFFY, Joseph, L. , KIM, Dooseop , PARMEE, Emma, R. , WEBER, Ann, E.
发明人： BROCKUNIER, Linda, L. , DUFFY, Joseph, L. , KIM, Dooseop , PARMEE, Emma, R. , WEBER, Ann, E.
IPC分类号： C07D211/36
CPC分类号： C07D487/04
摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防其中二肽基肽酶涉及-IV酶，如糖尿病，特别是2型糖尿病。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二肽基肽酶-IV酶的疾病中的用途。

8. 发明申请

WO2017165256A1 ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS 审中-公开
标题翻译：烟碱乙酰胆碱受体的变构调节剂
公开(公告)号：WO2017165256A1
公开(公告)日：2017-09-28
申请号：PCT/US2017/023127
申请日：2017-03-20
申请人： MERCK SHARP & DOHME CORP. , CROWLEY, Brendan, M. , CAMPBELL, Brian, T. , DUFFY, Joseph, L. , GRESHOCK, Thomas, J. , GUIADEEN, Deodial, G. , HARVEY, Andrew John , HUFF, Belinda, C. , LEAVITT, Kenneth, J. , RADA, Vanessa, L. , SANDERS, John, M. , SHIPE, William, D. , SUEN, Linda, M. , BELL, Ian, M.
发明人： CROWLEY, Brendan, M. , CAMPBELL, Brian, T. , DUFFY, Joseph, L. , GRESHOCK, Thomas, J. , GUIADEEN, Deodial, G. , HARVEY, Andrew John , HUFF, Belinda, C. , LEAVITT, Kenneth, J. , RADA, Vanessa, L. , SANDERS, John, M. , SHIPE, William, D. , SUEN, Linda, M. , BELL, Ian, M.
IPC分类号： C07D231/12 , C07D233/64 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D249/06 , C07D249/08 , C07D261/08 , C07D263/32 , C07D271/06 , C07D495/04 , C07D277/26 , C07D285/08 , C07D285/12
摘要： The present disclosure relates to compounds of formula (I) that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
摘要翻译：本发明涉及可用作α7nAChR调节剂的式（I）化合物，包含此类化合物的组合物，以及此类化合物用于预防，治疗或改善疾病，特别是疾病的中枢神经系统，例如阿尔茨海默病，帕金森病和精神分裂症中的认知障碍，以及L-DOPA诱导的运动障碍和炎症。

9. 发明申请

WO2015164308A1 FACTOR XIa INHIBITORS 审中-公开
标题翻译：因子XIA抑制剂
公开(公告)号：WO2015164308A1
公开(公告)日：2015-10-29
申请号：PCT/US2015/026774
申请日：2015-04-21
申请人： MERCK SHARP & DOHME CORP. , 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
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.
摘要翻译：本发明提供式（I）的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，高凝状态或纤维变化的方法。该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。

10. 发明申请

WO2010036589A1 SUBSTITUTED ARYL SULFONE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译：取代的ARYL SULFONE衍生物作为钙通道阻断剂
公开(公告)号：WO2010036589A1
公开(公告)日：2010-04-01
申请号：PCT/US2009/057617
申请日：2009-09-21
申请人： MERCK SHARP & DOHME CORP. , CHAKRAVARTY, Prasun, K. , DUFFY, Joseph, L. , SHAO, Pengcheng Patrick
发明人： CHAKRAVARTY, Prasun, K. , DUFFY, Joseph, L. , SHAO, Pengcheng Patrick
IPC分类号： C07C315/00
CPC分类号： C07D215/06
摘要： A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
摘要翻译：一系列由式I表示的取代的芳基砜衍生物或其药学上可接受的盐。药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。治疗与钙通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，尿失禁，瘙痒，过敏性皮炎，癫痫，糖尿病性神经病，肠易激综合征综合征，抑郁症，焦虑症，多发性硬化症，睡眠障碍，双相性精神障碍和中风，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。

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