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1. 发明授权

US5610154A Bicyclic carboxamides 失效
标题翻译：双环甲酰胺
公开(公告)号：US5610154A
公开(公告)日：1997-03-11
申请号：US448962
申请日：1995-05-24
申请人： Ian A. Cliffe , Howard L. Mansell , Terence J. Ward , James A. Nelson , Uresh S. Shah , Mira A. Kanzelberger
发明人： Ian A. Cliffe , Howard L. Mansell , Terence J. Ward , James A. Nelson , Uresh S. Shah , Mira A. Kanzelberger
IPC分类号： A61K31/495 , A61K31/55 , A61P9/12 , A61P25/18 , A61P25/20 , A61P43/00 , C07D209/44 , C07D209/52 , C07D223/14 , C07D295/185 , C07D403/12 , C07D451/02 , C07D295/16
CPC分类号： C07D295/185 , C07D209/52 , C07D223/14 , C07D451/02
摘要： Bicyclic carboxamides of formula I ##STR1## and the pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents, particularly 5-HT.sub.1A antagonists and may be used, for example, as anxiolytics. In the formulaX represents --CR.sup.2 .dbd.CR.sup.2 -- or --(CR.sup.2)q--;m represents 0,1 or 2; n represents 0,1 or 2; p represents 0,1,2 or 3 and q represents 0,1,2 or 3;A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups,R is a mono or bicyclic aryl or heteroaryl radical,R.sup.1 is an aryl or aryl(lower)alkyl radicaland each R.sup.2 is independently hydrogen or lower alkyl.
摘要翻译：式I的双环甲酰胺（I）和药学上可接受的酸加成盐是5-HT1A结合剂，特别是5-HT 1A拮抗剂，并且可以用于例如抗焦虑剂。式X表示-CR2 = CR2-或 - （CR2）q-; m表示0,1或2; n表示0,1或2; p表示0,1,2或3，q表示0,1,2或3; A是任选被一个或多个低级烷基取代的1或2个碳原子的亚烷基链，R是单或双环芳基或杂芳基，R 1是芳基或芳基（低级）烷基，每个R 2独立地是氢或低级烷基。

2. 发明授权

US06228880B1 4-amino-(ethylamino)-oxindole dopamine autoreceptor agonists 失效
标题翻译： 4-氨基 - （乙基氨基） - 氧吲哚多巴胺自身受体激动剂
公开(公告)号：US06228880B1
公开(公告)日：2001-05-08
申请号：US09287675
申请日：1999-04-07
申请人： James A. Nelson , Mira A. Kanzelberger , Richard E. Mewshaw
发明人： James A. Nelson , Mira A. Kanzelberger , Richard E. Mewshaw
IPC分类号： A61K31404
CPC分类号： C07D209/34
摘要： Compounds having dopaminegic activity are provided, having the formula: wherein R1 and R2 are each, independently, hydrogen, C1-10 alkyl, or (CH2)mR4, wherein R4 is phenyl or naphthyl which may be substituted by one or two substituents selected from the group consisting of C1-6 alkyl, halogen, C1-6 alkoxide and trifluoromethyl and m is 1 to 5; and R3 is hydrogen or C1-6 alkyl; or pharmaceutically acceptable salts thereof.
摘要翻译：提供了具有多巴胺活性的化合物，其具有下式：其中R 1和R 2各自独立地为氢，C 1-10烷基或（CH 2）m R 4，其中R 4为苯基或萘基，其可以被一个或两个选自由C 1-6烷基，卤素，C 1-6烷氧基和三氟甲基组成的组，m为1至5; 和R 3是氢或C 1-6烷基; 其药学上可接受的盐。

3. 发明授权

US5610164A (Thiophen-2-yl)-piperidin or tetrahydropyridin azabicyclocarboxamides 失效
标题翻译：（噻吩-2-基） - 哌啶或四氢吡啶氮杂双环羧酰胺
公开(公告)号：US5610164A
公开(公告)日：1997-03-11
申请号：US685132
申请日：1996-07-24
申请人： Reinhardt B. Baudy , James A. Nelson , Mira A. Kanzelberger
发明人： Reinhardt B. Baudy , James A. Nelson , Mira A. Kanzelberger
IPC分类号： C07D451/02 , A61K31/435
CPC分类号： C07D451/02
摘要： This invention provides compounds having the structure ##STR1## wherein R is hydrogen, alkyl, alkenyl, alkynyl, --COR.sup.2, phenyl, or phenylalkyl; the dotted line represents an optional double bond;R.sup.1 is hydrogen, --OH, OR.sup.3, or is absent if the optional double bond is present;R.sup.2 and R.sup.3 are each, independently, alkyl, alkenyl, alkynyl, phenyl, or phenylalkyl;R.sup.4 is hydrogen, --OR.sup.5, alkyl, alkenyl, alkynyl, --COR.sup.5, --CO.sub.2 R.sup.5, --CONR.sup.5 R.sup.6, perhaloalkyl, halogen, phenyl, or phenylalkyl;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, phenyl, or phenylalkyl; andn=0-2or a pharmaceutically acceptable salt thereof that are useful as antipsychotic, antidepressant and anxiolytic agents useful in the treatment and relief of the symptoms of these disease states.
摘要翻译：本发明提供了具有结构“IMAGE”的化合物，其中R是氢，烷基，烯基，炔基，-COR 2，苯基或苯基烷基; 虚线表示可选的双键; R1是氢，-OH，OR3，如果存在任选的双键，则不存在; R2和R3各自独立地为烷基，烯基，炔基，苯基或苯基烷基; R 4是氢，-OR 5，烷基，烯基，炔基，-COR 5，-CO 2 R 5，-CONR 5 R 6，全卤代烷基，卤素，苯基或苯基烷基; R 5和R 6各自独立地为氢，烷基，烯基，炔基，苯基或苯基烷基; 和n = 0-2或其药学上可接受的盐，其可用作抗精神病药，抗抑郁药和抗焦虑剂，其用于治疗和缓解这些疾病状态。

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