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1. 发明申请

WO2003082191A3 SUBSTITUTED 2,3-DIPHENYL PYRIDINES 审中-公开
公开(公告)号：WO2003082191A3
公开(公告)日：2003-10-09
申请号：PCT/US2003/009005
申请日：2003-03-24
申请人： MERCK & CO., INC. , FINKE, Paul, E. , MEURER, Laura, C. , DEBENHAM, John, S. , TOUPENCE, Richard, B. , WALSH, Thomas, F.
发明人： FINKE, Paul, E. , MEURER, Laura, C. , DEBENHAM, John, S. , TOUPENCE, Richard, B. , WALSH, Thomas, F.
IPC分类号： C07D401/02
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

2. 发明申请

WO1996010568A1 SUBSTITUTED ARYL PIPERAZINES AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的ARYL PIPERAZINES作为神经营养因子拮抗剂
公开(公告)号：WO1996010568A1
公开(公告)日：1996-04-11
申请号：PCT/US1995012341
申请日：1995-09-26
申请人： MERCK & CO., INC. , CHIANG, Yuan-Ching, P. , FINKE, Paul, E. , MacCOSS, Malcolm , MEURER, Laura, C. , MILLER, Daniel, J. , MILLS, Sander, G. , ROBICHAUD, Albert, J. , SHAH, Shrenik, K.
发明人： MERCK & CO., INC.
IPC分类号： C07D295/15
CPC分类号： C07D213/64 , C07D213/65 , C07D213/74 , C07D231/12 , C07D233/56 , C07D241/20 , C07D249/08 , C07D257/04 , C07D295/125 , C07D471/04 , C07D473/18 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Disclosed are substituted aryl piperazines of Formula (I) which are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis. In particular compounds of Formula (I) are shown to be neurokinin antagonists.
摘要翻译：公开了式（I）的取代的芳基哌嗪，其是可用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐的速激肽受体拮抗剂。特别地，式（I）的化合物显示为神经激肽拮抗剂。

3. 发明申请

WO2016022446A1 [5,6]-FUSED BICYCLIC ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译： [5,6] - 双金属抗生素化合物
公开(公告)号：WO2016022446A1
公开(公告)日：2016-02-11
申请号：PCT/US2015/043352
申请日：2015-08-03
申请人： MERCK SHARP & DOHME CORP. , CHEN, Helen, Y. , DEMONG, Duane , FINKE, Paul, E. , PLUMMER, Christopher, W.
发明人： CHEN, Helen, Y. , DEMONG, Duane , FINKE, Paul, E. , PLUMMER, Christopher, W.
IPC分类号： A61K31/343 , A61K31/443 , C07D307/79
CPC分类号： C07D405/04 , A61K31/343 , A61K31/443 , A61K45/06 , C07D307/80 , C07D405/10 , A61K2300/00
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.
摘要翻译：结构式（I）的新型化合物及其药学上可接受的盐是G蛋白偶联受体40（GPR40）的激动剂，可用于治疗，预防和抑制G蛋白偶联受体受体40.本发明的化合物可用于治疗2型糖尿病，以及通常与该疾病相关的病症，包括肥胖症和脂质疾病，例如混合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。

4. 发明申请

WO2009045419A1 NOVEL AZETIDINONES USEFUL AS INHIBITORS OF ELASTASE 审中-公开
标题翻译：新AZETIDINONES有用的ELASTASE的抑制剂
公开(公告)号：WO2009045419A1
公开(公告)日：2009-04-09
申请号：PCT/US2008/011343
申请日：2008-10-01
申请人： MERCK & CO., INC. , DOHERTY, James, B. , FINKE, Paul, E. , MUMFORD, Richard, A. , TREONZE, Kelly, M.
发明人： DOHERTY, James, B. , FINKE, Paul, E. , MUMFORD, Richard, A. , TREONZE, Kelly, M.
IPC分类号： A01N43/00 , A61K31/397 , C07D205/00
CPC分类号： C07D205/08
摘要： The invention is directed to novel azetidinones selected from 2-(S)-[4-(((2-(Dimethylamino)ethyl)ethylamino)carbonyl)phenoxy]-3,3-diethyl-N-[1-(R)-(4-(trifluoromethoxy)phenyl)butyl]-4-oxo-1-azetidin ecarboxamide, 2-(S)-[4-(((2-(Dimethylamino)ethyl)ethylamino)carbonyl)phenoxy]-3,3-diethyl-N-[1-(R)-(4-(trifluoromethyl)phenyl)butyl]-4-oxo-1-azetidinecarboxamide, and analogs thereof, and pharmaceutically acceptable salts thereof, and their use in the treatment of diseases associated with an excess of elastase, including emphysema, bronchial inflammation, chronic bronchitis, cystic fibrosis, acute respiratory distress syndrome, rheumatoid arthritis, osteoarthritis; glomerulonephritis, spondylitis, lupus, psoriasis, atherosclerosis, sepsis, septicemia, shock, myocardial infarction, reperfusion injury, and periodontitis.
摘要翻译：本发明涉及选自2-（S） - [4 - （（（2-（二甲基氨基）乙基）乙基氨基）羰基）苯氧基] -3,3-二乙基-N- [1-（R） - （4-（三氟甲氧基）苯基）丁基] -4-氧代-1-氮杂环丁烷甲酰胺，2-（S） - [4 - （（（2-（二甲基氨基）乙基）乙基氨基）羰基）苯氧基] 二乙基-N- [1-（R） - （4-（三氟甲基）苯基）丁基] -4-氧代-1-氮杂环丁烷甲酰胺及其类似物及其药学上可接受的盐，以及它们在治疗与弹性蛋白酶过多，包括肺气肿，支气管炎，慢性支气管炎，囊性纤维化，急性呼吸窘迫综合征，类风湿性关节炎，骨关节炎; 肾小球性肾炎，脊椎炎，狼疮，牛皮癣，动脉粥样硬化，败血症，败血病，休克，心肌梗塞，再灌注损伤和牙周炎。

5. 发明申请

WO03082191A2 SUBSTITUTED 2,3-DIPHENYL PYRIDINES 审中-公开
标题翻译：取代2,3-二苯基吡啶
公开(公告)号：WO03082191A2
公开(公告)日：2003-10-09
申请号：PCT/US0309005
申请日：2003-03-24
申请人： MERCK & CO INC , FINKE PAUL E , MEURER LAURA C , DEBENHAM JOHN S , TOUPENCE RICHARD B , WALSH THOMAS F
发明人： FINKE PAUL E , MEURER LAURA C , DEBENHAM JOHN S , TOUPENCE RICHARD B , WALSH THOMAS F
IPC分类号： C07D213/64 , A61K31/44 , A61K31/4418 , A61K31/4439 , A61K31/4545 , A61K31/455 , A61K31/496 , A61K31/5377 , A61K45/00 , A61K47/02 , A61K47/10 , A61K47/26 , A61K47/34 , A61P1/04 , A61P1/10 , A61P1/16 , A61P3/04 , A61P9/00 , A61P11/06 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P29/00 , A61P43/00 , C07D213/56 , C07D213/65 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/86 , C07D213/87 , C07D401/12 , A61K
CPC分类号： C07D213/79 , C04B35/632 , C07D213/65 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/86 , C07D213/87 , C07D401/12
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

6. 发明申请

WO03007887A3 SUBSTITUTED IMIDAZOLES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：取代的咪唑烷作为CANNABINOID受体调节剂
公开(公告)号：WO03007887A3
公开(公告)日：2003-04-17
申请号：PCT/US0223230
申请日：2002-07-16
申请人： MERCK & CO INC , FINKE PAUL E , MILLS SANDER G , PLUMMER CHRISTOPHER W , SHAH SHRENIK K , TRUONG QUANG T
发明人： FINKE PAUL E , MILLS SANDER G , PLUMMER CHRISTOPHER W , SHAH SHRENIK K , TRUONG QUANG T
IPC分类号： A61P21/04 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/30 , C07D233/90 , C07D405/12 , C08K5/34 , A61K31/415
CPC分类号： C07D405/12 , C07D233/90
摘要： The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1)receptor particularly in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB1) receptor. The invention is concerned with the use of these novel compounds to selectively antagonize the Cannabinoid-1 (CB1) receptor. As such, compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith. Novel compounds of structural formula (I) are also claimed.
摘要翻译：使用本发明的化合物作为大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，特别是用于治疗，预防和抑制由大麻素-1（CB1）受体介导的疾病。本发明涉及这些新化合物选择性拮抗大麻素-1（CB1）受体的用途。因此，本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症的精神药物。血管意外和头部创伤，焦虑障碍，压力，癫痫，帕金森病和精神分裂症。这些化合物也可用于治疗药物滥用障碍，特别是鸦片剂，酒精和尼古丁。所述化合物还可用于治疗与过量食物摄入和与其相关的并发症相关的肥胖或进食障碍。还要求新的结构式（I）化合物。

7. 发明申请

WO1994013636A1 NEW SUBSTITUTED AZETIDINONES AS ANTI-INFLAMMATORY AND ANTIDEGENERATIVE AGENTS 审中-公开
标题翻译：新的取代的氮杂环丁酮用作抗炎剂和抗变性
公开(公告)号：WO1994013636A1
公开(公告)日：1994-06-23
申请号：PCT/US1993012229
申请日：1993-12-15
申请人： MERCK & CO., INC. , DAVIES, Philip , DOHERTY, James, B. , FINKE, Paul, E. , HUMES, John, L. , HAGMANN, William, K. , KISSINGER, Amy, L. , LUEDKE, Edward, A. , MACCOSS, Malcolm , MUMFORD, Richard, A. , SHAH, Shrenik, K.
发明人： MERCK & CO., INC.
IPC分类号： C07D205/08
CPC分类号： C07D405/12 , C07D205/08
摘要： New substituted azetidinones of general formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described.
摘要翻译：这已被证明有效的弹性蛋白酶抑制剂和通式（I）的新的取代的氮杂环丁酮是有用的，因此作为抗炎剂和antidégénératifs。

8. 发明申请

WO1994010143A1 NEW SUBSTITUTED AZETIDINONES AS ANTI-INFLAMMATORY AND ANTIDEGENERATIVE AGENTS 审中-公开
标题翻译：新的替代AZETIDINONES作为抗炎和抗感染药物
公开(公告)号：WO1994010143A1
公开(公告)日：1994-05-11
申请号：PCT/US1993010269
申请日：1993-10-26
申请人： MERCK & CO., INC. , DOHERTY, James, B. , DORN, Conrad, P. , DURETTE, Philippe, L. , FINKE, Paul, E. , MacCOSS, Malcolm , MILLS, Sander, G. , SHAH, Shrenik, K. , SAHOO, Soumya, P. , POLO, Scott, A. , HAGMANN, William, K.
发明人： MERCK & CO., INC.
IPC分类号： C07D205/08
CPC分类号： C07D401/12 , C07D205/08 , C07D403/12 , C07D405/12
摘要： New substituted azetidinones of general formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described.
摘要翻译：已经发现已经被发现是有效的弹性蛋白酶抑制剂，从而有用的抗炎和抗再生剂的通式（I）的新取代的氮杂环丁酮被描述。

9. 发明申请

WO1994007839A1 PROCESS OF MAKING CHIRAL 2-ARYL-1,4-BUTANEDIAMINE DERIVATIVES 审中-公开
标题翻译：制备2-ARYL-1,4-BUTANEDIAMINE衍生物的方法
公开(公告)号：WO1994007839A1
公开(公告)日：1994-04-14
申请号：PCT/US1993008934
申请日：1993-09-21
申请人： MERCK & CO., INC. , FINKE, Paul, E. , HALE, Jeffrey, J. , MACCOSS, Malcolm , MILLS, Sander, G.
发明人： MERCK & CO., INC.
IPC分类号： C07C63/36
CPC分类号： C07D263/26 , C07C51/347 , C07C231/12 , C07C233/11 , C07C233/66 , C07C233/76 , C07D211/58 , C07C57/60 , C07C57/30
摘要： Disclosed herein is a process of making chiral 2-aryl-1,4-butanediamine derivatives useful as neurokinin-A antagonists of formula (7).
摘要翻译：本文公开了制备可用作式（7）的神经激肽A拮抗剂的手性2-芳基-1,4-丁二胺衍生物的方法。

10. 发明申请

WO2011146324A1 SPIRO ISOXAZOLINE COMPOUNDS AS SSTR5 ANTAGONISTS 审中-公开
标题翻译： SPIRO ISOXAZOLINE化合物作为SSTR5拮抗剂
公开(公告)号：WO2011146324A1
公开(公告)日：2011-11-24
申请号：PCT/US2011/036367
申请日：2011-05-13
申请人： MERCK SHARP & DOHME CORP. , DUFFY, Joseph, L. , BAO, Jianming , ONDEYKA, Debra, L. , TYAGARAJAN, Sriram , SHAO, Patrick , YE, Feng , KATIPALLY, Revathi , FINKE, Paul, E. , ZANG, Yi , PLOTKIN, Michael, A. , ROMERO, F. Anthony , MONINGKA, Remond , HUSSAIN, Zahid
发明人： DUFFY, Joseph, L. , BAO, Jianming , ONDEYKA, Debra, L. , TYAGARAJAN, Sriram , SHAO, Patrick , YE, Feng , KATIPALLY, Revathi , FINKE, Paul, E. , ZANG, Yi , PLOTKIN, Michael, A. , ROMERO, F. Anthony , MONINGKA, Remond , HUSSAIN, Zahid
IPC分类号： A01N43/40 , A01N43/42 , A61K31/44
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。

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