公开(公告)号：US5807868A

公开(公告)日：1998-09-15

申请号：US564156

申请日：1995-12-21

申请人： Bruce Jeremy Sargent ,  David Norman Johnston ,  Andrew Philip Austin Crew

发明人： Bruce Jeremy Sargent ,  David Norman Johnston ,  Andrew Philip Austin Crew

IPC分类号： C07D217/14 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61P21/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07D217/04 ,  C07D401/08 ,  C07D405/08 ,  C07D409/08

CPC分类号： C07D401/08 ,  C07D217/04 ,  C07D405/08 ,  C07D409/08

摘要： Tetrahydroisoquinoline compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof, in which: R.sub.1 represents one or more substituents selected from H, halo, hydroxy, alkyl (optionally substituted by hydroxy), alkoxy, alkylthio, alkylsulphinyl, alkyl-sulphonyl, nitro, cyano, polyhaloalkyl, polyhaloalkoxy, phenyl (optionally substituted by one or more of halo, alkyl or alkoxy), or R.sub.1 is optionally alkylated carbamoyl; R.sub.2 represents a saturated or unsaturated aliphatic group optionally substituted by hydroxy or alkoxy; E represents an alkylene chain optionally substituted by one or more alkyl groups; and G represents (a) optionally substituted saturated or unsaturated alicyclic group containing 3 to 8 carbon atoms, or (b) optionally substituted saturated or unsaturated aliphatic chain containing 1 to 12 carbon atoms, or (c) optionally substituted 5 or 6 membered heterocyclic ring containing one or more N or O atoms or SO.sub.n groups in which n is 0, 1 or 2; and O-acylated derivatives thereof which provide lipophilic esters have utility in analgesia or in the treatment of psychoses (e.g. schizophrenia), Parkinson's disease, Lesch-Nyan syndrome, attention deficit disorder or cognitive impairment or in the relief of drug dependence or tardive dyskinesia.

摘要翻译： PCT No.PCT / EP94 / 01926 Sec。 371 1995年12月21日第 102（e）日期1995年12月21日PCT提交1994年6月10日PCT公布。 公开号WO95 / 00489 日期1995年1月5日式Ⅰ的四氢异喹啉化合物及其药学上可接受的盐，其中：R1表示一个或多个选自H，卤素，羟基，烷基（任选被羟基取代），烷氧基，烷硫基，烷基亚磺酰基 ，烷基磺酰基，硝基，氰基，多卤代烷基，多卤代烷氧基，苯基（任选被卤素，烷基或烷氧基中的一个或多个取代），或R 1任选被烷基化的氨基甲酰基; R2表示任选被羟基或烷氧基取代的饱和或不饱和脂族基; E表示任选被一个或多个烷基取代的亚烷基链; G表示（a）含有3〜8个碳原子的任选取代的饱和或不饱和脂环基，或（b）任选取代的含有1至12个碳原子的饱和或不饱和脂族链，或（c）任选取代的5或6元杂环 含有一个或多个N或O原子或其中n为0,1或2的SO n基团; 提供亲脂性酯的O-酰化衍生物可用于镇痛或治疗精神病（例如精神分裂症），帕金森病，莱斯奈恩综合症，注意力缺陷障碍或认知障碍或缓解药物依赖或迟发性运动障碍。

公开(公告)号：US5804586A

公开(公告)日：1998-09-08

申请号：US826012

申请日：1997-03-27

申请人： Bruce Jeremy Sargent ,  David Norman Johnston ,  Andrew Philip Austin Crew

发明人： Bruce Jeremy Sargent ,  David Norman Johnston ,  Andrew Philip Austin Crew

IPC分类号： C07D217/14 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61P21/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07D217/04 ,  C07D401/08 ,  C07D405/08 ,  C07D409/08

CPC分类号： C07D401/08 ,  C07D217/04 ,  C07D405/08 ,  C07D409/08

摘要： Tetrahydroisoquinoline compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof, in which: R.sub.1 represents one or more substituents selected from H, halo, hydroxy, alkyl (optionally substituted by hydroxy), alkoxy, alkylthio, alkylsulphinyl, alkyl-sulphonyl, nitro, cyano, polyhaloalkyl, polyhaloalkoxy, phenyl (optionally substituted by one or more of halo, alkyl or alkoxy), or R.sub.1 is optionally alkylated carbamoyl; R.sub.2 represents a saturated or unsaturated aliphatic group optionally substituted by hydroxy or alkoxy; E represents an alkylene chain optionally substituted by one or more alkyl groups; and G represents (a) optionally substituted saturated or unsaturated alicyclic group containing 3 to 8 carbon atoms, or (b) optionally substituted saturated or unsaturated aliphatic chain containing 1 to 12 carbon atoms, or (c) optionally substituted 5 or 6 membered heterocyclic ring containing one or more N or O atoms or SO.sub.n groups in which n is 0, 1 or 2; and O-acylated derivatives thereof which provide lipophilic esters have utility in analgesia or in the treatment of psychoses (e.g. schizophrenia), Parkinson's disease, Lesch-Nyan syndrome, attention deficit disorder or cognitive impairment or in the relief of drug dependence or tardive dyskinesia.

摘要翻译： 式I的四氢异喹啉化合物及其药学上可接受的盐，其中：R 1表示一个或多个选自H，卤素，羟基，烷基（任选被羟基取代），烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基， 硝基，氰基，多卤代烷基，多卤代烷氧基，苯基（任选被卤素，烷基或烷氧基中的一个或多个取代），或R 1任选被烷基化的氨基甲酰基; R2表示任选被羟基或烷氧基取代的饱和或不饱和脂族基; E表示任选被一个或多个烷基取代的亚烷基链; G表示（a）含有3〜8个碳原子的任选取代的饱和或不饱和脂环基，或（b）任选取代的含有1至12个碳原子的饱和或不饱和脂族链，或（c）任选取代的5或6元杂环 含有一个或多个N或O原子或其中n为0,1或2的SO n基团; 提供亲脂性酯的O-酰化衍生物可用于镇痛或治疗精神病（例如精神分裂症），帕金森病，莱斯奈恩综合症，注意力缺陷障碍或认知障碍或缓解药物依赖或迟发性运动障碍。