专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

31. 发明授权

US5512565A Cholesterol ester hydrolase inhibitors 失效
标题翻译：胆固醇酯水解酶抑制剂
公开(公告)号：US5512565A
公开(公告)日：1996-04-30
申请号：US413559
申请日：1995-03-30
申请人： Richard E. Mewshaw , Thomas J. Commons , Donald P. Strike
发明人： Richard E. Mewshaw , Thomas J. Commons , Donald P. Strike
IPC分类号： C07C271/40 , C07D295/205 , A61K31/54 , C07D279/12
CPC分类号： C07D295/205 , C07C271/40 , C07C2101/14 , C07C2103/93
摘要： The compounds of the formula: ##STR1## in which ##STR2## where R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.9 is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R.sup.10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is --NR.sup.9 -- or R.sup.7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; are useful as inhibitors of cholesterol ester hydrolase.
摘要翻译：其中R7是氢，烷基，羟基，烷酰氧基，羟基烷基，羟基羰基，烷氧基羰基，苯基或取代的苯基，其中取代基是烷基，烷氧基，卤素，硝基，氰基，卤代烷基，全卤代烷基或二烷基氨基烷基; R8是氢或烷基或R7和R8一起是聚亚甲基; R9是氢，烷基，苯基或取代的苯基，其中取代基是烷基，烷氧基，卤素，硝基，氰基或全卤代烷基; R10为氢，烷基或偕二烷基; n是整数0,1或2之一; 并且R 3，R 4，R 5和R 6独立地为氢，烷基，烷氧基，卤素，硝基，氰基或全卤代烷基，烷氧基羰基或羟基羰基。当X是-NR9-或R7是氨基烷基时，其药学上可接受的盐; 可用作胆固醇酯水解酶的抑制剂。

32. 发明授权

US5190940A Cholesterol ester hydrolase inhibitors 失效
标题翻译：胆固醇酯水解酶抑制剂
公开(公告)号：US5190940A
公开(公告)日：1993-03-02
申请号：US796500
申请日：1991-11-22
申请人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
发明人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
IPC分类号： C07C271/44 , C07C271/56 , C07D211/16 , C07D295/205
CPC分类号： C07D295/205 , C07C271/44 , C07C271/56 , C07D211/16
摘要： The compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl; R.sup.2 is alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkylphenylalkyl; or R.sup.1 and R.sup.2 taken together complete a heterocyclic moiety of the formula: ##STR2## in which X is ##STR3## where R.sup.3,R.sup.4 and R.sup.5 are, independently hydrogen, alkyl, phenyl or substituted phenyl, in which the substituents are halogeno, alkoxy or trifluoromethyl; R.sup.6 is hydrogen, alkyl or gemdialkyl and n is one of the integers 0, 1 or 2, are cholesterol ester hydrolase inhibitors useful in the treatment of high serum cholesterol levels and associated disease states in the mammal such as coronary heart disease, atherosclerosis, familial hypercholesterolemia, hyperlipemia, and the like.
摘要翻译：下式的化合物：其中R 1是氢或烷基; R2是烷基，环烷基，环烷基烷基，苯基烷基或烷基苯基烷基; 或者R 1和R 2一起形成下式的杂环部分：其中X是，其中R 3，R 4和R 5独立地是氢，烷基，苯基或取代的苯基，其中取代基是卤代，烷氧基或三氟甲基; R6是氢，烷基或偕二烷基，n是整数0,1或2之一，是用于治疗哺乳动物高血清胆固醇水平和相关疾病状态的胆固醇酯水解酶抑制剂，例如冠心病，动脉粥样硬化，家族性高胆固醇血症，高脂血症等。

33. 发明授权

US5112859A Biphenyl amide cholesterol ester hydrolase inhibitors 失效
标题翻译：联苯酰胆固醇酯水解酶抑制剂
公开(公告)号：US5112859A
公开(公告)日：1992-05-12
申请号：US582687
申请日：1990-09-14
申请人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
发明人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
IPC分类号： C07C271/44 , C07C271/56 , C07D211/16 , C07D295/205
CPC分类号： C07D295/205 , C07C271/44 , C07C271/56 , C07D211/16
摘要： The compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl; R.sup.2 is alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkylphenylalkyl; or R.sup.1 and R.sup.2 taken together complete a heterocyclic moiety of the formula: ##STR2## in which X is ##STR3## NR.sup.5,--O-- or --S--; where R.sup.3, R.sup.4 and R.sup.5 are, independently hydrogen, alkyl, phenyl or substituted phenyl, in which the substituents are halogeno, alkoxy or trifluoromethyl; R.sup.6 is hydrogen, alkyl of gemdialkyl and n is one of the integers 0, 1 or 2, are cholesterol ester hydrolase inhibitors useful in the treatment of high serum cholesterol levels and associated disease states in the mammal such as coronary heart disease, atherosclerosis, familial hypercholesterolemia, hyperlipemia, and the like.
摘要翻译：下式的化合物：其中R 1是氢或烷基; R2是烷基，环烷基，环烷基烷基，苯基烷基或烷基苯基烷基; 或者R 1和R 2一起形成下式的杂环部分：其中X是NR 5，-O-或-S-; 其中R3，R4和R5独立地是氢，烷基，苯基或取代的苯基，其中取代基是卤代，烷氧基或三氟甲基; R6是氢，gemdialkyl烷基，n是整数0,1或2之一，是胆固醇酯水解酶抑制剂，可用于治疗哺乳动物高血清胆固醇水平和相关疾病状态，如冠心病，动脉粥样硬化，家族性高胆固醇血症，高脂血症等。

34. 发明授权

US4812583A Substituted acyloxyalkylphenylethylene inhibitors of 3-hydroxy-3-methylglutaryl-coa reductase 失效
标题翻译： 3-羟基-3-甲基戊二酰基 - 还原酶的取代的酰氧基烷基苯基乙烯抑制剂
公开(公告)号：US4812583A
公开(公告)日：1989-03-14
申请号：US095800
申请日：1987-09-11
申请人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
发明人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
IPC分类号： C07C45/41 , C07C57/76 , C07D309/30
CPC分类号： C07D309/30 , C07C45/41 , C07C57/76
摘要： Compounds of the formula: ##STR1## where M is hydrogen or alkyl; R.sup.2 and R.sup.3 are, independently, alkyl; R.sup.4 is hydrogen, alkyl, phenyl or substituted phenyl, trifluoromethyl; and R.sup.5 is alkyl, phenyl or substituted phenyl, alkoxy, or trifluoromethyl; or a pharmaceutically acceptable salt thereof, are hypocholesteremic agents.
摘要翻译：下式的化合物：其中M是氢或烷基; R2和R3独立地是烷基; R4是氢，烷基，苯基或取代的苯基，三氟甲基; R 5为烷基，苯基或取代的苯基，烷氧基或三氟甲基; 或其药学上可接受的盐是hypocholesteremic试剂。

35. 发明授权

US06903110B2 Antidepressant azaheterocyclylmethyl derivatives of 7,8-dihydro-6H-5-oxa-1-aza-phenanthrene 失效
标题翻译： 7,8-二氢-6H-5-氧杂-1-氮杂菲的抗抑郁药氮杂环甲基衍生物
公开(公告)号：US06903110B2
公开(公告)日：2005-06-07
申请号：US10201862
申请日：2002-07-24
申请人： Rulin Zhao , Megan Tran , Gary P. Stack , Richard E. Mewshaw
发明人： Rulin Zhao , Megan Tran , Gary P. Stack , Richard E. Mewshaw
IPC分类号： A61K31/4741 , A61K31/4745 , A61P25/24 , C07D491/02 , C07D491/04 , A61K31/44
CPC分类号： C07D491/04
摘要： Compounds of the formula useful for the treatment of such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder (including trichotillomania), social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addition, sexual dysfunction (including premature ejaculation), and related illnesses.
摘要翻译：可用于治疗抑郁症（包括但不限于重度抑郁障碍，儿童抑郁症和抑郁症），焦虑症，恐慌症，创伤后应激障碍，经前期焦虑症（也称为经前期综合征）的化合物，注意力缺陷障碍（伴有和不伴有多动症），强迫症（包括拔毛病），社会焦虑症，广泛性焦虑症，肥胖症，进食障碍如神经性厌食症，神经性贪食症，血管舒缩性潮红，可卡因和酒精增加，性功能障碍早泄）和相关疾病。

36. 发明授权

US06743796B2 Piperazinyl-isatins 失效
标题翻译：哌嗪基异丁酯
公开(公告)号：US06743796B2
公开(公告)日：2004-06-01
申请号：US10139695
申请日：2002-05-03
申请人： Lynne P. Greenblatt , Ivo Jirkovsky , Richard E. Mewshaw
发明人： Lynne P. Greenblatt , Ivo Jirkovsky , Richard E. Mewshaw
IPC分类号： A61K31496
CPC分类号： C07D295/073 , C07D209/38 , C07D295/135 , C07D295/155
摘要： This invention provides compounds of formula VI wherein Y is hydrogen, methyl, methoxy, methylthio or trifluoromethyl; R is hydrogen, C1-3alkyl or (CH2)nAr; n is 0, 1 or 2; and Ar is phenyl or methoxyphenyl, or a pharmaceutically acceptable salt thereof. These compounds are selective dopamine autoreceptor agonists useful in treating disease states involving hyperactivity of dopamine systems. The invention also comprises intermediate compounds, compositions and methods related to the compounds of formula VI.
摘要翻译：本发明提供式VI化合物，其中Y是氢，甲基，甲氧基，甲硫基或三氟甲基; R是氢，C1-3烷基或（CH2）nAr; n是0,1或2; 和Ar是苯基或甲氧基苯基，或其药学上可接受的盐。这些化合物是可用于治疗涉及多巴胺系统多动症的疾病状态的选择性多巴胺自身受体激动剂。本发明还包括与式VI化合物相关的中间体化合物，组合物和方法。

37. 发明授权

US06610712B2 Aryloxy piperidinyl derivatives for the treatment of depression 失效
标题翻译：芳氧基哌啶衍生物用于治疗抑郁症
公开(公告)号：US06610712B2
公开(公告)日：2003-08-26
申请号：US10000642
申请日：2001-11-15
申请人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
发明人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
IPC分类号： C07D40104
CPC分类号： C07D401/06 , C07D405/14
摘要： This invention provides compounds useful in treating serotonin-related central nervous system disorders, including anxiety, generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, sleep disorders, sexual dysfunction, alcohol and drug addiction, Alzheimer's disease, Parkinson's disease, obesity and migraine, the compounds having the general formula: wherein: R1 and R2 may each be H or an alkyl or alkoxy group; or R1 and R2 may be concatenated to form a bicyclic ring system with the phenyl ring to which they are bound; X is selected from hydrogen, halogen, cyano, C1-C6 alkoxy; Z is (CH2)n or carbonyl; n is 0, 1 or 2; the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了可用于治疗血清素相关的中枢神经系统疾病的化合物，包括焦虑，广泛性焦虑症，恐慌症，强迫症，睡眠障碍，性功能障碍，酒精和药物成瘾，阿尔茨海默病，帕金森病，肥胖症和偏头痛具有以下通式的化合物：其中：R 1和R 2可以各自为H或烷基或烷氧基; 或者R 1和R 2可以连接形成与它们所结合的苯环的双环系统; X选自氢，卤素，氰基，C 1 -C 6烷氧基; Z是（CH 2）n或羰基; n为0,1或2; 虚线表示可选的双键; 或其药学上可接受的盐。

38. 发明授权

US06337326B1 N-aryl-(homopiperazinyl)-cyclohexyl amines 失效
标题翻译： N-芳基 - （高哌嗪基） - 环己胺
公开(公告)号：US06337326B1
公开(公告)日：2002-01-08
申请号：US09706640
申请日：2000-11-06
申请人： Adam M. Gilbert , Richard E. Mewshaw
发明人： Adam M. Gilbert , Richard E. Mewshaw
IPC分类号： C07D40308
CPC分类号： C07D401/14 , C07D403/08
摘要： This invention provides novel compounds and methods and compositions using them in the treatment of central nervous system disorders, including depression and anxiety, the compounds having the formula: wherein Ar is an aryl group of 4 to 10 carbon atoms or a heteraryl group of 4 to 10 carbon atoms; R1 and R2 are independently selected from hydrogen, straight chain alkyl of 1 to 12 carbon atoms, branched alkyls of 3 to 10 carbon atoms or cycloalkyl of 3 to 10 carbon atoms; R3 is H, straight chain, branched or cyclic alkyl, halogen, alkoxy, haloalkyl, OH, nitro, nitrile, amino, CN, carboxy, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl and alkylaminocarbonyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供新颖的化合物及其组合物，其用于治疗中枢神经系统疾病（包括抑郁和焦虑），具有下式的化合物：其中Ar为4-10个碳原子的芳基或4至 10个碳原子; R 1和R 2独立地选自氢，1至12个碳原子的直链烷基，3至10个碳原子的支链烷基或3至10个碳原子的环烷基; R 3是H，直链，支链或环状烷基，卤素，烷氧基，卤代烷基，OH，硝基，腈，氨基，CN，羧基，烷氧基羰基，烷基羰基，氨基羰基和烷基氨基羰基; 或其药学上可接受的盐。

39. 发明授权

US06313114B1 3,4-Dihydro-2H-benzo[1,4]oxazinyl-methyl)-[3-(1H-indol-3yl)-alkyl]- amines 失效
标题翻译： 3,4-二氢-2H-苯并[1,4]恶嗪基 - 甲基） - [3-（1H-吲哚基） - 烷基] - 胺
公开(公告)号：US06313114B1
公开(公告)日：2001-11-06
申请号：US09475940
申请日：1999-12-30
申请人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
发明人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
IPC分类号： C07D41312
CPC分类号： C07D413/12
摘要： Compounds are provided which have the following formula: wherein: R is hydrogen, alkyl of 1 to 6 carbon atoms, phenyl, or substituted phenyl; X and Y are each, independently, hydrogen, halogen, cyano, or alkoxy of 1 to 6 carbon atoms; and m is 1 to 5; or a pharmaceutically acceptable salt thereof.
摘要翻译：提供具有下式的化合物：其中：R是氢，1至6个碳原子的烷基，苯基或取代的苯基; X和Y各自独立地是氢，卤素，氰基或1-6个碳的烷氧基原子 andm是1到5; 或其药学上可接受的盐。

40. 发明授权

US06245780B1 Tetrahydroisoquinolinyl-indole derivatives for the treatment of depression 失效
标题翻译：用于治疗抑郁症的四氢异喹啉基 - 吲哚衍生物
公开(公告)号：US06245780B1
公开(公告)日：2001-06-12
申请号：US09551137
申请日：2000-04-17
申请人： Richard E. Mewshaw , Kristin L. Meagher
发明人： Richard E. Mewshaw , Kristin L. Meagher
IPC分类号： A01N4342
CPC分类号： C07D401/06 , C07D401/08
摘要： Compounds are provided which have the formula: wherein: R1, R2, R3, and R4 are, independently, hydrogen, halogen, alkoxy, or carboxamide; R5 is hydrogen, halogen, CF3, CN, carbamide or alkoxy; and X is (CH2)n or a 4-6 membered carbocyclic ring, wherein n is an integer of 2 to 4; or pharmaceutically acceptable salts thereof.
摘要翻译：提供具有下式的化合物：其中：R 1，R 2，R 3和R 4独立地是氢，卤素，烷氧基或羧酰胺; R 5是氢，卤素，CF 3，CN，和X是（CH 2）n或4-6元碳环，其中n是2至4的整数;或其药学上可接受的盐。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式