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1. 发明授权

US5221687A Medicaments 失效
标题翻译：药剂
公开(公告)号：US5221687A
公开(公告)日：1993-06-22
申请号：US934307
申请日：1992-08-25
申请人： Ian H. Coates , Alexander W. Oxford , Peter C. North , Michael B. Tyers
发明人： Ian H. Coates , Alexander W. Oxford , Peter C. North , Michael B. Tyers
IPC分类号： A61K31/00 , A61K31/445 , A61K31/55
CPC分类号： A61K31/00 , A61K31/445 , A61K31/55
摘要： The invention relates to the use of compounds of formula (I) ##STR1## wherein Im represents an imidazolyl group of formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 (wherein R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenylC.sub.1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.5 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.5 or --SO.sub.2 R.sup.5);one of the groups represented by R.sup.2, R.sup.3 and R4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;and n represents 2 or 3,and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the treatment of depression.
摘要翻译：本发明涉及式（I）化合物其中Im表示下式的咪唑基，R1表示氢原子或选自C 1-6烷基，C 3-6烯基， C 3-10炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，苯基C 1-3烷基，苯基甲氧基甲基，苯氧基乙基，苯氧基甲基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5（其中R 5和R 6可以相同或不同各自表示氢原子，C 1-6烷基或C 3-7环烷基，或苯基或苯基C 1-4烷基，其中苯基任选被一个或多个C 1-4烷基，C 1-4烷氧基或羟基或卤素原子，条件是当R 1表示-CO 2 R 5或-SO 2 R 5基团时，R 5不表示氢原子）; 由R 2，R 3和R 4表示的基团之一是氢原子或C 1-6烷基，C 3-7环烷基，C 3-6烯基，苯基或苯基C 1-3烷基，其它两个基团可以相同或不同，代表氢原子或C1-6烷基; 和n表示2或3，以及其生理上可接受的盐和溶剂合物，用于制备用于治疗抑郁症的药物。

2. 发明授权

US5229407A Medicaments 失效
标题翻译：药剂
公开(公告)号：US5229407A
公开(公告)日：1993-07-20
申请号：US911395
申请日：1992-07-10
申请人： Ian H. Coates , Alexander W. Oxford , Peter C. North , Michael B. Tyers
发明人： Ian H. Coates , Alexander W. Oxford , Peter C. North , Michael B. Tyers
IPC分类号： A61K31/00 , A61K31/445 , A61K31/55
CPC分类号： A61K31/445 , A61K31/00 , A61K31/55
摘要： The invention relates to the use of compounds of formula (I) ##STR1## wherein Im represents an imidazolyl group of formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 (wherein R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenylC.sub.1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.5 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.5 or --SO.sub.2 R.sup.5);one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;and n represents 2 or 3,and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the treatment of a cognitive disorder.
摘要翻译：本发明涉及式（I）化合物其中Im表示下式的咪唑基，R1表示氢原子或选自C 1-6烷基，C 3-6烯基， C 3-10炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，苯基C 1-3烷基，苯基甲氧基甲基，苯氧基乙基，苯氧基甲基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5（其中R 5和R 6可以相同或不同各自表示氢原子，C 1-6烷基或C 3-7环烷基，或苯基或苯基C 1-4烷基，其中苯基任选被一个或多个C 1-4烷基，C 1-4烷氧基或羟基或卤素原子，条件是当R 1表示-CO 2 R 5或-SO 2 R 5基团时，R 5不表示氢原子）; 由R 2，R 3和R 4表示的基团之一是氢原子或C 1-6烷基，C 3-7环烷基，C 3-6烯基，苯基或苯基C 1-3烷基，其它两个基团可以相同或不同，代表氢原子或C1-6烷基; 和n表示2或3，以及其生理上可接受的盐和溶剂合物，用于制备用于治疗认知障碍的药物。

3. 发明授权

US5276050A Medicaments 失效
标题翻译：药剂
公开(公告)号：US5276050A
公开(公告)日：1994-01-04
申请号：US908329
申请日：1992-07-06
申请人： Steven J. Cooper , Ian H. Coates , Alexander W. Oxford , Peter C. North
发明人： Steven J. Cooper , Ian H. Coates , Alexander W. Oxford , Peter C. North
IPC分类号： A61K31/415
CPC分类号： A61K31/415
摘要： The invention relates to the use of compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, in which Im represents an imidazolyl group of formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 (wherein R.sup.5 and R.sup.6, which may be the same or different each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenylC.sub.1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.5 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.5 or --SO.sub.2 R.sup.5);one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;and n represents 2 or 3,for the treatment of a condition involving excessive eating, for example bulimia.
摘要翻译：本发明涉及通式（I）化合物（Ⅰ）及其生理上可接受的盐和溶剂化物，其中Im表示下式的咪唑基：其中R1表示氢原子或选自C 1-6烷基，C 3-6烯基，C 3-10炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，苯基C 1-3烷基，苯基甲氧基甲基，苯氧基乙基，苯氧基甲基，-CO 2 R 5，-COR 5，-CONR 5 R 6或 -SO 2 R 5（其中R 5和R 6可以相同或不同，各自表示氢原子，C 1-6烷基或C 3-7环烷基或苯基或苯基C 1-4烷基，其中苯基任选被一个或更多C 1-4烷基，C 1-4烷氧基或羟基或卤素原子，条件是当R 1表示-CO 2 R 5或-SO 2 R 5基团时，R 5不表示氢原子）; 由R 2，R 3和R 4表示的基团之一是氢原子或C 1-6烷基，C 3-7环烷基，C 3-6烯基，苯基或苯基C 1-3烷基，其它两个基团可以相同或不同的是氢原子或C1-6烷基; n表示2或3，用于治疗涉及过度饮食的病症，例如贪食症。

4. 发明授权

US4997831A Lactam derivatives 失效
公开(公告)号：US4997831A
公开(公告)日：1991-03-05
申请号：US401249
申请日：1989-08-31
申请人： David E. Bays , Ian H. Coates , Alexander W. Oxford , Peter C. North
发明人： David E. Bays , Ian H. Coates , Alexander W. Oxford , Peter C. North
IPC分类号： A61K31/415 , A61K31/435 , A61K31/495 , A61K31/535 , A61K31/55 , A61P1/00 , A61P1/04 , A61P1/08 , A61P3/06 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D471/16 , C07D487/16 , C07D495/16 , C07D498/16 , C07D513/16 , C07D471/04 , A61K31/475
CPC分类号： C07D471/16 , C07D487/16 , C07D498/16
摘要： The invention provides lactam derivatives of the general formula (I) ##STR1## wherein n represents 2 or 3; Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl- group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, wherein m represents 2, 3 or 4; or Y represents a group --X(CH.sub.2).sub.p --, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.3 receptors and are useful, for example in the treatment of psychotic disorders, anxiety and nausea and vomiting.

5. 发明授权

US5360800A Tetrahydro-1H-pyrido[4,3-b]indol-1-one derivatives 失效
标题翻译：四氢-1H-吡啶并[4,3-b]吲哚-1-酮衍生物
公开(公告)号：US5360800A
公开(公告)日：1994-11-01
申请号：US741570
申请日：1991-08-07
申请人： Ian H. Coates , Peter C. North , Alexander W. Oxford
发明人： Ian H. Coates , Peter C. North , Alexander W. Oxford
IPC分类号： C07D471/04 , C07D487/04 , C07D401/06 , A61K31/44 , A61K31/55
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to tricyclic lactams of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenyl C.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl or phenoxymethyl,one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkhyl group;n represents 2 or 3; and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.
摘要翻译：本发明涉及通式（I）的三环内酰胺（I）其中Im表示下式的咪唑基，R1表示氢原子或选自C1-6烷基，C3-6烯基，C3-10炔基，C3-7环烷基，C3-7环烷基C1-4烷基，苯基，苯基C1-3烷基，苯基甲氧基甲基，苯氧基乙基或苯氧基甲基，由R2，R3和R4表示的基团之一是氢原子或C1-6烷基，C3 7-环烷基，C 3-6烯基，苯基或苯基C 1-3烷基，其它可以相同或不同的两个基团表示氢原子或C1-6烷基; n表示2或3; 及其生理上可接受的盐和溶剂合物。这些化合物是5-HT在5-HT 3受体上的作用的有效和选择性拮抗剂，可用于治疗精神病，焦虑和恶心和呕吐。

6. 发明授权

US5183820A Lactam derivatives 失效
标题翻译：内酰胺衍生物
公开(公告)号：US5183820A
公开(公告)日：1993-02-02
申请号：US691814
申请日：1991-04-26
申请人： Ian H. Coates , Alexander W. Oxford , Peter C. North , Barry J. Price
发明人： Ian H. Coates , Alexander W. Oxford , Peter C. North , Barry J. Price
IPC分类号： C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention provides potent and selective antagonists of 5-HT at 5-HT.sub.3 receptors which are tricyclic lactams of the formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Y represents the group CH.dbd.CH or (CH.sub.2).sub.n, wherein n represents 2 or 3;Q represents a halogen atom, or a group selected from hydroxy, C.sub.1-4 alkoxy, phenylC.sub.1-3 alkoxy, C.sub.1-6 alkyl, cyano, phenyl which may be unsubstituted or substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, --NR.sup.7 R.sup.8, --CONR.sup.7 R.sup.8 , --(CH.sub.2).sub.p CONR.sup.7 R.sup.8, --(CH.sub.2).sub.q NR.sup.9 R.sup.10 or --(CH.sub.2).sub.2 CO.sub.2 R.sup.11 ;Q' represents a hydrogen or a fluorine atom;and physiologically acceptable salts and solvates thereof.
摘要翻译：本发明提供5-HT受体的有效和选择性拮抗剂，其为作为式（I）的三环内酰胺的5-HT 3受体，其中Im表示下式的咪唑基：其中R1表示氢原子或选自C 1-6烷基，C 3-6烯基，C 3-10炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，苯基C 1-3烷基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5中的基团; 由R 2，R 3和R 4表示的基团之一是氢原子或C 1-6烷基，C 3-7环烷基，C 3-6烯基，苯基或苯基C 1-3烷基，其它两个基团可以相同或不同表示氢原子或C 1-6烷基; Y表示基团CH = CH或（CH 2）n，其中n表示2或3; Q表示卤原子，或选自羟基，C 1-4烷氧基，苯基C 1-3烷氧基，C 1-6烷基，氰基，可未被取代或被一个或多个C 1-4烷基，C 1-4烷氧基或羟基或卤素取代的苯基的基团原子，-NR 7 R 8，-CONR 7 R 8， - （CH 2）p CONR 7 R 8， - （CH 2）q NR 9 R 10或 - （CH 2）2 CO 2 R 11; Q'表示氢或氟原子; 及其生理上可接受的盐和溶剂合物。

7. 发明授权

US5008272A Lactam derivatives 失效
标题翻译：内酰胺衍生物
公开(公告)号：US5008272A
公开(公告)日：1991-04-16
申请号：US393145
申请日：1989-08-14
申请人： Ian H. Coates , Alexander W. Oxford , Peter C. North
发明人： Ian H. Coates , Alexander W. Oxford , Peter C. North
IPC分类号： C07D233/64 , A61K31/435 , A61P1/00 , A61P1/04 , A61P3/06 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/24 , A61P25/26 , A61P43/00 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention provides potent and selective antagonists of 5-HT and 5-HT.sub.3 receptors which are tricyclic lactams of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;one of the group represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;and physiologically acceptable salts and solvates thereof.

8. 发明授权

US5225407A 5-HT.sub.3 receptor antagonists for the treatment of autism 失效
标题翻译： 5-HT3受体拮抗剂治疗自闭症
公开(公告)号：US5225407A
公开(公告)日：1993-07-06
申请号：US941951
申请日：1992-09-08
申请人： Nigel R. Oakley , Ian H. Coates , Peter C. North , Alexander W. Oxford
发明人： Nigel R. Oakley , Ian H. Coates , Peter C. North , Alexander W. Oxford
IPC分类号： A61K31/00 , A61K31/44 , A61K31/445 , A61K31/46 , A61K31/55
CPC分类号： A61K31/55 , A61K31/00 , A61K31/44 , A61K31/445 , A61K31/46
摘要： The invention relates to the use of a compound which acts as an antagonist of 5-HT at 5-HT.sub.3 receptors in the treatment of autism or another disorder originating in childhood in which there is mental retardation.
摘要翻译：本发明涉及在5-HT 3受体中作为5-HT拮抗剂的化合物在治疗自闭症或其中存在精神发育迟滞的儿童期的另一种病症中的用途。

9. 发明授权

US5196534A Process for the preparation of lactam derivatives 失效
标题翻译：制备LACTAM衍生物的方法
公开(公告)号：US5196534A
公开(公告)日：1993-03-23
申请号：US704099
申请日：1991-05-22
申请人： John W. F. Whitehead , Keith Mills , Ian H. Coates , Alexander W. Oxford , Peter C. North
发明人： John W. F. Whitehead , Keith Mills , Ian H. Coates , Alexander W. Oxford , Peter C. North
IPC分类号： C07B61/00 , C07D211/86 , C07D471/04
CPC分类号： C07D471/04 , C07D211/86
摘要： The invention relates to a process for the preparation of a compound of formula (I) ##STR1## wherein R represent a hydrogen atom or a methyl or ethyl group, which comprises cyclising a compound of formul (IV) ##STR2## Where R represents a hydrogen atom, the compound of formula (IV) may optionally be alkylated to produce a compound in whcich R is methyl or ethyl.The compound of formula (I) is useful as an intermediate in the preparation of 2,3,4,5-tetrahydro-2-[(imidazol-4(or 5)-yl)methyl]-1H-pyrido[4,3-b]indol-1-ones having 5-HT.sub.3 antagonist activity.

10. 发明授权

US5116984A Imidazole derivatives 失效
公开(公告)号：US5116984A
公开(公告)日：1992-05-26
申请号：US333967
申请日：1989-04-06
申请人： Peter C. North , Alexander W. Oxford , Ian H. Coates
发明人： Peter C. North , Alexander W. Oxford , Ian H. Coates
IPC分类号： A61K31/415 , A61P25/00 , C07D233/54 , C07D233/64 , C07D401/06 , C07D403/06
CPC分类号： C07D233/64 , C07D401/06 , C07D403/06
摘要： The invention relates to imidazole derivatives of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of formula: ##STR2## A represents the group CH or a nitrogen atom; R.sup.1 and R.sup.2, which may be the same or different, and may be attached to either the same or different fused rings of the naphthalene moiety, each represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 alkyl or C.sub.1-4 alkylthio group, and one of R.sup.1 and R.sup.2 may also represent a group --NR.sup.3 R.sup.4 (wherein R.sup.3 and R.sup.4, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl group, or together with the nitrogen atom to which they are attached form a saturated 5 to 7 membered ring);n represents 1, 2 or 3;R.sup.5, R.sup.6, R.sup.7, are as defined in the specification; and physiologically acceptable salts and solvates thereof.

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