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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

WO2006002117A1 LACTAM TACHYKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译： LACTAM TACHYKININ受体拮抗剂
公开(公告)号：WO2006002117A1
公开(公告)日：2006-01-05
申请号：PCT/US2005/021840
申请日：2005-06-17
申请人： MERCK & CO., INC. , FINKE, Paul, E. , MEURER, Laura, C. , MILLS, Sander, G.
发明人： FINKE, Paul, E. , MEURER, Laura, C. , MILLS, Sander, G.
IPC分类号： C07D207/26
CPC分类号： C07D207/27 , C07D207/273
摘要： The present invention is directed to certain lactam compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
摘要翻译：本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些内酰胺化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂和使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。

3. 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。

4. 发明申请

WO2009058237A1 ANTIDIABETIC TRICYCLIC COMPOUNDS 审中-公开
标题翻译：抗菌三环化合物
公开(公告)号：WO2009058237A1
公开(公告)日：2009-05-07
申请号：PCT/US2008/012181
申请日：2008-10-27
申请人： MERCK & CO., INC. , LIANG, Gui-bai , LIAO, Xibin , LIU, Weiguo , FINKE, Paul, E. , KIM, Dooseop , YANG, Lihu , LIN, Songnian
发明人： LIANG, Gui-bai , LIAO, Xibin , LIU, Weiguo , FINKE, Paul, E. , KIM, Dooseop , YANG, Lihu , LIN, Songnian
IPC分类号： C07D265/38
CPC分类号： C07D305/06 , C07B2200/07 , C07C62/34 , C07C2603/12 , C07D471/04
摘要： Tricyclic compounds containing a cyclopropanecarboxylic acid fused to a bicyclic ring, including pharmaceutically acceptable salts, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes, 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：包含与双环稠合的环丙烷羧酸的三环化合物（包括药学上可接受的盐）是G蛋白偶联受体40（GPR40）的激动剂，可用作治疗性化合物，特别是用于治疗2型糖尿病，以及通常与该疾病有关，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。

5. 发明申请

WO2009035541A1 METHOD OF TREATING INHERITED SEVERE NEUTROPENIA 审中-公开
标题翻译：治疗非常严重的中耳炎的方法
公开(公告)号：WO2009035541A1
公开(公告)日：2009-03-19
申请号：PCT/US2008/010430
申请日：2008-09-05
申请人： MERCK & CO., INC. , UNIVERSITY OF WASHINGTON , DALE, David, C. , FINKE, Paul, E. , MUMFORD, Richard, A. , APRIKYAN, Andranik Andrew
发明人： DALE, David, C. , FINKE, Paul, E. , MUMFORD, Richard, A. , APRIKYAN, Andranik Andrew
IPC分类号： A01N43/62
CPC分类号： A61K31/4965 , A61K31/36
摘要： The invention is directed to a method of treating severe neutropenia, and in particular, cyclic neutropenia (CN) or severe congenital neutropenia (SCN), in a patient in need of such treatment comprising: administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及在需要这种治疗的患者中治疗严重中性粒细胞减少症，特别是循环中性粒细胞减少症（CN）或严重先天性中性粒细胞减少症（SCN）的方法，其包括：施用治疗有效量的式 I）或其药学上可接受的盐。

6. 发明申请

WO2003007887A2 SUBSTITUTED IMIDAZOLES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：取代的咪唑作为大麻素受体调节剂
公开(公告)号：WO2003007887A2
公开(公告)日：2003-01-30
申请号：PCT/US2002/023230
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： A61K
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：本发明化合物作为大麻素-1（CB1）受体的拮抗剂和/或反向激动剂的用途，特别是在治疗，预防和抑制由大麻素-1（CB1）介导的疾病）受体。本发明涉及这些新型化合物选择性拮抗大麻素-1（CB1）受体的用途。因此，本发明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，包括多发性硬化症和格林 - 巴利综合征的神经炎症和病毒性脑炎，脑炎的炎性后遗症的精神药物血管意外，头部创伤，焦虑症，压力，癫痫，帕金森病和精神分裂症。这些化合物还可用于治疗物质滥用障碍，特别是阿片类药物，酒精和尼古丁。该化合物还可用于治疗与过量食物摄入和与之相关的并发症相关的肥胖症或进食障碍。结构式（I）的新化合物也被要求保护。

7. 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。

8. 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。

9. 发明申请

WO2013039802A1 INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL 审中-公开
标题翻译：肾脏外部药物通道的抑制剂
公开(公告)号：WO2013039802A1
公开(公告)日：2013-03-21
申请号：PCT/US2012/054354
申请日：2012-09-10
申请人： MERCK SHARP & DOHME CORP. , WALSH, Shawn , PASTERNAK, Alexander , CATO, Brian , FINKE, Paul, E. , FRIE, Jessica , FU, Qinghong , KIM, Dooseop , PIO, Barbara , SHAHRIPOUR, Aurash , SHI, Zhi-Cai , TANG, Haifeng
发明人： WALSH, Shawn , PASTERNAK, Alexander , CATO, Brian , FINKE, Paul, E. , FRIE, Jessica , FU, Qinghong , KIM, Dooseop , PIO, Barbara , SHAHRIPOUR, Aurash , SHI, Zhi-Cai , TANG, Haifeng
IPC分类号： A61K31/497
CPC分类号： C07D401/10 , C07D211/28 , C07D211/48 , C07D211/62 , C07D403/10 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/14 , C07D471/08 , C07D487/04
摘要： This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
摘要翻译：本发明涉及具有结构式I的化合物及其药学上可接受的盐，它们是肾外
膜（ROMK）通道（Kir1.1）的抑制剂。式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水保持引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。

10. 发明申请

WO1993000332A1 SUBSTITUTED AZETIDINONES AS ANTI-INFLAMMATORY AND ANTIDEGENERATIVE AGENTS 审中-公开
标题翻译：替代亚硫酸钠作为抗炎和抗感染药物
公开(公告)号：WO1993000332A1
公开(公告)日：1993-01-07
申请号：PCT/US1992004993
申请日：1992-06-15
申请人： MERCK & CO., INC.
发明人： MERCK & CO., INC. , FINKE, Paul, E. , KISSINGER, Amy, L. , MACCOSS, Malcolm , SHAH, Shrenik, K. , DOHERTY, James, B. , HAGMANN, William, K. , DAVIES, Philip , HUMES, John, L. , LUEDKE, Edward, S. , MUMFORD, Richard, A.
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：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代谢剂的通式（I）的新的取代的氮杂环丁酮被描述。

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