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公开(公告)号：US06967196B1
公开(公告)日：2005-11-22
申请号：US09890927
申请日：2000-02-22
申请人： David W. Smith , Benito Munoz , Kumar Srinivasan , Carl P. Bergstrom , Prasad V. Chaturvedula , Milind S. Deshpande , Daniel J. Keavy , Wai Yu Lau , Michael F. Parker , Charles P. Sloan , Owen B. Wallace , Henry Hui Wang
发明人： David W. Smith , Benito Munoz , Kumar Srinivasan , Carl P. Bergstrom , Prasad V. Chaturvedula , Milind S. Deshpande , Daniel J. Keavy , Wai Yu Lau , Michael F. Parker , Charles P. Sloan , Owen B. Wallace , Henry Hui Wang
IPC分类号： A61K31/40 , A61K31/407 , A61K31/47 , A61K31/4965 , A61K31/54 , A61P25/00 , C07C311/21 , C07C323/41
CPC分类号： C07D285/06 , C07C311/21 , C07C323/41 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/20 , C07D207/48 , C07D211/22 , C07D211/24 , C07D211/46 , C07D211/70 , C07D213/30 , C07D213/76 , C07D217/04 , C07D233/61 , C07D277/06 , C07D277/46 , C07D295/088 , C07D295/12 , C07D295/205 , C07D311/20 , C07D333/48 , C07D491/10
摘要： In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the sulfur atom and nitrogen atom of the sulfonamide group include substituted or unsubstituted hydrocarbyl moieties, substituted or unsubstituted heterocycle moieties, polycyclic moieties, halogen, alkoxy, ether, ester, amide, sulfonyl, sulfonamidyl, sulfide, carbamate, and the like. Invention compounds are capable of a wide variety of uses. For example sulfonamide compounds can act to modulate production of amyloid β protein and are useful in the prevention or treatment of a variety of diseases. Pharmaceutical compositions containing invention compounds are also provided. Such compositions have wide utility for the prevention or treatment of a variety of diseases.
摘要翻译： 根据本发明，提供了一类新型的磺酰胺化合物。 本发明的化合物含有核心磺酰胺基团。 连接到磺酰胺基团的硫原子和氮原子的可变部分包括取代或未取代的烃基部分，取代或未取代的杂环部分，多环部分，卤素，烷氧基，醚，酯，酰胺，磺酰基，磺酰胺基，硫醚，氨基甲酸酯，和 喜欢。 本发明化合物能够具有多种用途。 例如，磺酰胺化合物可以起到调节淀粉样蛋白β蛋白的产生的作用，并且可用于预防或治疗各种疾病。 还提供含有本发明化合物的药物组合物。 这样的组合物可广泛用于预防或治疗各种疾病。
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2.发明授权
公开(公告)号：US5472966A
公开(公告)日：1995-12-05
申请号：US412625
申请日：1995-03-29
申请人： Charles P. Sloan , David W. Smith
发明人： Charles P. Sloan , David W. Smith
IPC分类号： C07D211/14 , A61K31/4427 , A61K31/445 , A61K31/451 , A61K31/495 , A61K31/505 , A61P25/24 , A61P25/26 , C07D211/22 , C07D211/70 , C07D401/12
CPC分类号： C07D401/12 , C07D211/70
摘要： Certain aminoalkyl derivatives of naphthyl-piperidines and tetrahydro-pyridines of Formula (I) are useful antidepressant agents. ##STR1## The symbol (Aryl) denotes phenyl, naphthyl, pyridinyl, pyrimidinyl and pyrazinyl ring systems with n being an integer of 2-4.
摘要翻译： 式（I）的萘基哌啶和四氢吡啶的某些氨基烷基衍生物是有用的抗抑郁剂。 （I）符号（芳基）表示n为2-4的整数的苯基，萘基，吡啶基，嘧啶基和吡嗪基环体系。
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3.发明授权5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of .beta.-amyloid protein production 失效5-氨基-6-环己基-4-羟基 - 己酰胺衍生物作为β-淀粉样蛋白生产的抑制剂
公开(公告)号：US5703129A
公开(公告)日：1997-12-30
申请号：US723488
申请日：1996-09-30
IPC分类号： C07C237/14 , C07C323/41 , C07D307/33 , A61K31/17
CPC分类号： C07D307/33 , C07C237/14 , C07C323/41 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要： A series of 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives of Formula I have been synthesized. ##STR1## As inhibitors of the production of .beta.-amyloid protein from .beta.-amyloid precursor protein, these compounds are expected to be effective in treating patients suffering from or susceptible to conditions or disorders linked to brain accumulation of .beta.-amyloid protein; e.g., Alzheimer's Disease and Down's Syndrome.
摘要翻译： 已经合成了一系列式I的5-氨基-6-环己基-4-羟基 - 己酰胺衍生物。 （I）作为从β-淀粉样蛋白前体蛋白生产β-淀粉样蛋白的抑制剂，预期这些化合物可有效治疗患有或易于与β-淀粉样蛋白的脑积聚相关的病症或障碍的患者 ; 例如阿尔茨海默病和唐氏综合症。
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公开(公告)号：US5668151A
公开(公告)日：1997-09-16
申请号：US639968
申请日：1996-05-08
IPC分类号： A61K31/445 , A61K31/451 , A61K31/455 , A61P3/04 , A61P9/12 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D211/90 , C07D413/12 , C07D413/14 , C07D211/86
CPC分类号： C07D413/12 , C07D211/90
摘要： A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of piperidine and tetrahydropyridine derivatives of 4-phenyl-1,4-dihydropyridines of Formula I. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
摘要翻译： 已经合成了一系列NPY的非肽能拮抗剂，其由式I的4-苯基-1,4-二氢吡啶的哌啶和四氢吡啶衍生物组成。作为NPY诱导的摄食行为的拮抗剂，这些 预期化合物可用作促进减肥和治疗进食障碍的有效厌氧剂。
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5.发明授权
公开(公告)号：US5468767A
公开(公告)日：1995-11-21
申请号：US178073
申请日：1994-01-06
IPC分类号： C07D209/14 , C07D401/12 , C07D405/12 , A61K31/40 , C07D405/00
CPC分类号： C07D401/12 , C07D209/14 , C07D405/12
摘要： Certain 3-amino-cycloalkanyl and cycloalkenyl derivatives of 5-cyano-substituted indoles of Formula I are useful antidepressant agents. ##STR1## The substituent R.sup.1 is hydrogen or C.sub.1-4 alkyl and R.sup.2 is C.sub.1-4 alkyl or --(CH.sub.2).sub.p --Ar with Ar being a phenyl, pyridinyl, pyrimidinyl or 1,4-benzodioxan-2-yl moiety. The symbol m is zero or 1, n is 1 to 3 and p is zero or 1 to 4.
摘要翻译： 式I的5-氰基取代的吲哚的某些3-氨基 - 环烷基和环烯基衍生物是有用的抗抑郁剂。 取代基R 1是氢或C 1-4烷基，R 2是C 1-4烷基或 - （CH 2）p-Ar，Ar是苯基，吡啶基，嘧啶基或1,4-苯并二恶烷-2-基部分。 符号m为零或1，n为1至3，p为零或1至4。
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公开(公告)号：US5635503A
公开(公告)日：1997-06-03
申请号：US482355
申请日：1995-06-07
申请人： Graham S. Poindexter , Marc Bruce , Graham Johnson , Michael Kozlowski , Karen LeBoulluec , Ivo Monkovic , Ramakrishna Seethala , Charles P. Sloan
发明人： Graham S. Poindexter , Marc Bruce , Graham Johnson , Michael Kozlowski , Karen LeBoulluec , Ivo Monkovic , Ramakrishna Seethala , Charles P. Sloan
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/451 , A61K31/455 , A61K31/495 , A61K31/55 , A61P3/04 , A61P9/12 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D211/90 , C07D401/12 , C07D413/04 , C07D413/14 , A61K31/435
CPC分类号： C07D413/04 , C07D211/90
摘要： A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of piperazine and homopiperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
摘要翻译： 已经合成了一系列NPY的非肽能拮抗剂，其由式（I）的4-苯基-1,4-二氢吡啶的哌嗪和高哌嗪衍生物组成。 （I）作为NPY诱导的摄食行为的拮抗剂，预期这些化合物可用作促进减肥和治疗饮食失调的有效厌氧剂。
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公开(公告)号：US5583149A
公开(公告)日：1996-12-10
申请号：US517525
申请日：1995-08-21
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/505 , A61P25/04 , A61P25/06 , C07D209/14 , C07D401/12 , C07D403/12 , C07D401/10
CPC分类号： C07D401/12 , C07D209/14
摘要： A series of novel serotonergic indolyl derivatives of cycloalkanyl- and cycloalkenyl-amines of Formula I are intended for use in the alleviation of vascular headaches. ##STR1##
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公开(公告)号：US07049314B2
公开(公告)日：2006-05-23
申请号：US10662745
申请日：2003-09-15
申请人： Dalton King , Jeffrey A. Deskus , John E. Macor , Ronald J. Mattson , Zhaoxing Meng , Charles P. Sloan
发明人： Dalton King , Jeffrey A. Deskus , John E. Macor , Ronald J. Mattson , Zhaoxing Meng , Charles P. Sloan
IPC分类号： A61K31/535 , A61K31/445 , A61K31/40 , C07D413/06 , C07D209/04
CPC分类号： C07D209/30 , C07D209/42 , C07D403/08
摘要： The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.
摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐或溶剂合物和药学上可接受的制剂，其包含用于治疗早泄，抑郁，注意力缺陷多动障碍，强迫症，创伤后应激障碍 和物质滥用障碍。
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9.发明授权
公开(公告)号：US5607961A
公开(公告)日：1997-03-04
申请号：US517999
申请日：1995-08-22
IPC分类号： C07D209/14 , C07D401/12 , C07D405/12 , A61K31/405
CPC分类号： C07D401/12 , C07D209/14 , C07D405/12
摘要： Certain 3-amino-cycloalkanyl and cycloalkenyl derivatives of 5-cyano-substituted indoles of Formula I are useful antidepressant agents. ##STR1## The substituent R.sup.1 is hydrogen or C.sub.1-4 alkyl and R.sup.2 is C.sub.1-4 alkyl or --(CH.sub.2).sub.p --Ar with Ar being a phenyl, pyridinyl, pyrimidinyl or 1,4-benzodioxan-2-yl moiety. The symbol m is zero or 1, n is 1 to 3 and p is zero or 1 to 4.
摘要翻译： 式I的5-氰基取代的吲哚的某些3-氨基 - 环烷基和环烯基衍生物是有用的抗抑郁剂。 取代基R 1是氢或C 1-4烷基，R 2是C 1-4烷基或 - （CH 2）p-Ar，Ar是苯基，吡啶基，嘧啶基或1,4-苯并二恶烷-2-基部分。 符号m为零或1，n为1至3，p为零或1至4。
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公开(公告)号：US5468768A
公开(公告)日：1995-11-21
申请号：US178079
申请日：1994-01-06
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/505 , A61P25/04 , A61P25/06 , C07D209/14 , C07D401/12 , C07D403/12 , C07D209/08
CPC分类号： C07D401/12 , C07D209/14
摘要： A series of novel serotonergic indolyl derivatives of cycloalkanyl- and cycloalkenyl-amines of Formula I are intended for use in the alleviation of vascular headaches. ##STR1##
摘要翻译： 式I的环烷基 - 和环烯基 - 胺的一系列新型5-羟色胺能吲哚衍生物旨在用于缓解血管性头痛。
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