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41. 发明授权

US6121307A N-aryloxyethyl-indoly-alkylamines for the treatment of depression 失效
标题翻译：用于治疗抑郁症的N-芳氧基乙基 - 吲哚烷基胺
公开(公告)号：US6121307A
公开(公告)日：2000-09-19
申请号：US287831
申请日：1999-04-07
申请人： Richard E. Mewshaw , Dahui Zhou
发明人： Richard E. Mewshaw , Dahui Zhou
IPC分类号： C07D209/14 , C07D401/12 , C07D405/12 , A61K31/4015 , A61K31/404 , C07D209/02 , C07D209/04 , C07D405/02
CPC分类号： C07D401/12 , C07D209/14 , C07D405/12
摘要： Compounds useful for alleviating symptoms of depression are provided which have the following formula: wherein:R.sub.1 is hydrogen, lower alkyl or aryl;R.sub.2 is hydrogen, lower alkyl, phenyl or substituted phenyl;X and Y are each, independently, hydrogen, lower alkyl, lower alkoxy, or halogen, or together combine with the carbon atoms to which they are attached to complete a pyranyl, dihydrofuranyl, furanyl, or dioxanyl, group;Z is hydrogen, halogen or lower alkoxy; with the proviso that when X, Y or Z represent lower alkoxy, they are not present at the ortho position;W is hydrogen, halogen, lower alkyl, cyano or a trifluoromethyl group; andn is 2-5; orpharmaceutically acceptable salts thereof.
摘要翻译：提供了可用于缓解抑郁症状的化合物，其具有下式：其中：R1是氢，低级烷基或芳基; R2是氢，低级烷基，苯基或取代的苯基; X和Y各自独立地为氢，低级烷基，低级烷氧基或卤素，或与它们所连接的碳原子一起结合形成吡喃基，二氢呋喃基，呋喃基或二恶烷基; Z是氢，卤素或低级烷氧基; 条件是当X，Y或Z表示低级烷氧基时，它们不存在于邻位; W是氢，卤素，低级烷基，氰基或三氟甲基; n为2-5; 或其药学上可接受的盐。

42. 发明授权

US5756521A Chroman-2-ylmethylamino derivatives 失效
标题翻译：色满-2-基甲基氨基衍生物
公开(公告)号：US5756521A
公开(公告)日：1998-05-26
申请号：US816585
申请日：1997-03-13
申请人： Richard E. Mewshaw
发明人： Richard E. Mewshaw
IPC分类号： C07D405/12 , A61K31/44 , C07D401/04 , C07D405/00
CPC分类号： C07D405/12
摘要： Compounds of the formula: ##STR1## in which n is one of the integers 1, 2, 3 or 4, or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs.
摘要翻译： n为整数1,2,3或4之一的其中之一的化合物或其药学上可接受的盐，可用于治疗精神分裂症，帕金森病， Tourette综合征，酒精成瘾，可卡因成瘾和类似药物成瘾。

43. 发明授权

US5670667A Chroman-2-ylmethylamino derivatives 失效
标题翻译：色满-2-基甲基氨基衍生物
公开(公告)号：US5670667A
公开(公告)日：1997-09-23
申请号：US630794
申请日：1996-04-10
申请人： Richard E. Mewshaw
发明人： Richard E. Mewshaw
IPC分类号： C07D311/58 , C07D311/04
CPC分类号： C07D311/58
摘要： Compounds of the formula: ##STR1## in which Z is hydrogen or a halogen; n is one of the integers 1, 2, 3, or 4; m is one of the integers 0 or 1; R is a substituted or unsubstituted aryl group in which the substituents are, independently, one or two members selected from the group consisting of alkyl, hydroxy, halo or amino groups; R.sup.2 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.
摘要翻译：下式的化合物：其中Z是氢或卤素; n是整数1,2,3或4之一; m是整数0或1之一; R是取代或未取代的芳基，其中取代基独立地是选自烷基，羟基，卤素或氨基的一个或两个成员; R2是氢或烷基; 或其药学上可接受的盐是多巴胺合成和释放的抑制剂，其可用于治疗精神分裂症，帕金森病，图雷特综合征，酒精成瘾，可卡因成瘾和对药物成瘾。

44. 发明授权

US5663194A Chroman-2-ylmethylamino derivatives 失效
标题翻译：色满-2-基甲基氨基衍生物
公开(公告)号：US5663194A
公开(公告)日：1997-09-02
申请号：US684521
申请日：1996-07-19
申请人： Richard E. Mewshaw
发明人： Richard E. Mewshaw
IPC分类号： C07D307/58 , A61K31/35 , C07D311/58
CPC分类号： C07D307/58
摘要： Described herein are compounds of the formula: ##STR1## in which n is 1, 2 or 3; m is 0 or 1; and R is a substituted or unsubstituted phenyl group in which the substitutents are, independently, one or two members selected from the group consisting of alkyl, hydroxy, halo or amino groups or R is alkyl of 1 to 6 carbon atoms or hydroxyalkyl of 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are inhibitors of dopamine synthesis and release, and are useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.
摘要翻译：本文描述的是下式的化合物：其中n是1,2或3; m为0或1; 并且R是取代或未取代的苯基，其中取代基独立地是选自烷基，羟基，卤素或氨基的一个或两个成员，或者R是1至6个碳原子的烷基或1至 6个碳原子; 或其药学上可接受的盐，其是多巴胺合成和释放的抑制剂，并且可用于治疗精神分裂症，帕金森氏病，图雷特氏综合征，酒精成瘾，可卡因成瘾和对肛门药物的成瘾。

45. 发明授权

US5391571A 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：US5391571A
公开(公告)日：1995-02-21
申请号：US62026
申请日：1993-05-13
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 , A61K31/325 , C07C271/02
CPC分类号： C07D295/205 , C07C271/40 , C07C2101/14 , C07C2103/93
摘要： The compounds of the formula: ##STR1## in which R.sup.1 is alkyl of 4 or more carbon atoms, cycloalkyl, 1-adamantyl, 2-adamantyl, 3-noradamantyl, 3-methyl-1-adamantyl, 1-fluorenyl, 9-fluorenyl, cycloalkylalkyl, phenyl, substituted phenyl, alkyl, alkoxy, halo, nitro, cyano or trifluoromethyl, phenylalkyl or substituted phenylalkyl, where the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl; R.sup.2 is hydrogen, alkyl or R.sup.1 taken with R.sup.2 and the nitrogen atom to which they are attached form a heterocyclic moiety of the formula: ##STR2## wherein ##STR3## in which 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, R5 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; useful as inhibitors of cholesterol ester hydrolase.
摘要翻译：下式的化合物：其中R1是4个或更多个碳原子的烷基，环烷基，1-金刚烷基，2-金刚烷基，3-降金刚烷基，3-甲基-1-金刚烷基，1-芴基，9-芴基烷基，烷氧基，卤素，硝基，氰基或三氟甲基，苯基烷基或取代的苯基烷基，其中苯环上的取代基是烷基，烷氧基，卤素，硝基，氰基，三氟甲基或苯基; R 2是氢，烷基或R 1与R 2取代，并且与它们相连的氮原子形成下式的杂环部分：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。

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