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1. 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。

2. 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。

3. 发明授权

US5240954A Medicaments 失效
标题翻译：药剂
公开(公告)号：US5240954A
公开(公告)日：1993-08-31
申请号：US804020
申请日：1991-12-09
申请人： Michael B. Tyers , Ian H. Coates , David C. Humber , George B. Ewan , James A. Bell
发明人： Michael B. Tyers , Ian H. Coates , David C. Humber , George B. Ewan , James A. Bell
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## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group; and one of the groups represented byR.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.2-6 alkenyl 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 alkyl group; and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage in radiological examination procedures.The invention also relates to a product containing a therapeutic agent liable to induce nausea and vomiting, e.g. a cytostatic agent such as a cyclophosphamide, an alkylating agent or a platinum complex, and a compound of the general formula (I) as a combined preparation for simultaneous separate or sequential use in therapy.
摘要翻译：本发明涉及通式（I）化合物其中R 1表示氢原子或C 1-10烷基，C 3-7环烷基，C 3-7环烷基 - （C 1-4）烷基 C 3-6烯基，C 3-10炔基，苯基或苯基-C 1-3烷基; 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 2-6烯基或苯基-C 1-3烷基，其它两个基团可以是相同或不同，表示氢原子或C 1-6烷基; 及其生理上可接受的盐和溶剂化物，用于缓解恶心和呕吐和/或促进胃排空和用于制造用于此目的的药物。促进胃排空可能是为了缓解与胃潴留相关的胃肠道疾病，或者在放射学检查程序中可能是有利的。本发明还涉及含有易诱发恶心和呕吐的治疗剂的产品，例如，细胞生长抑制剂如环磷酰胺，烷化剂或铂络合物，以及通式（I）的化合物作为用于在治疗中同时分开或顺次使用的组合制剂。

4. 发明授权

US4753789A Method for treating nausea and vomiting 失效
标题翻译：治疗恶心呕吐的方法
公开(公告)号：US4753789A
公开(公告)日：1988-06-28
申请号：US877805
申请日：1986-06-24
申请人： Michael B. Tyers , Ian H. Coates , David C. Humber , George B. Ewan , James A. Bell
发明人： Michael B. Tyers , Ian H. Coates , David C. Humber , George B. Ewan , James A. Bell
IPC分类号： C07D403/06 , A61K31/415 , A61P1/00 , A61P1/08
CPC分类号： A61K31/415 , Y10S514/872 , Y10S514/917 , Y10S514/922
摘要： The invention relates to the use of compounds of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycoalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group, and one of the groups represented byR.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.2-6 alkenyl 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 alkyl group;and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage of radiological examination procedures.The invention also relates to a product containing a therapeutic agent liable to induce nausea and vomiting, e.g. a cytostatic agent such as a cyclophosphamide, an alkylating agent or a platinum complex, and a compound of the general formula (I) as a combined preparation for simultaneous separate or sequential use in therapy.

5. 发明授权

US5578628A Medicaments for the treatment of nausea and vomiting 失效
标题翻译：用于治疗恶心和呕吐的药物
公开(公告)号：US5578628A
公开(公告)日：1996-11-26
申请号：US501974
申请日：1990-03-30
申请人： Michael B. Tyers , Ian H. Coates , David C. Humber , George B. Ewan , James A. Bell
发明人： Michael B. Tyers , Ian H. Coates , David C. Humber , George B. Ewan , James A. Bell
IPC分类号： A61K31/415 , A61K31/4178
CPC分类号： A61K31/4178 , A61K31/415 , Y10S514/966
摘要： The invention relates to the use of compounds of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.-7 cycloalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group; and one of the groups represented byR.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkynyl, C.sub.2-6 alkenyl 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 alkyl group; and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting.
摘要翻译：本发明涉及通式（I）的化合物其中R 1表示氢原子或C 1-10烷基，C 3-7环烷基，C 7环烷基 - （C 1-4）烷基 C 3-6烯基，C 3-10炔基，苯基或苯基-C 1-3烷基; 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环炔基，C 2-6烯基或苯基-C 1-3烷基，其它两个基团可以是相同或不同，表示氢原子或C 1-6烷基; 及其生理上可接受的盐和溶剂化物，用于缓解恶心和呕吐。

6. 发明授权

US4929632A Medicaments 失效
公开(公告)号：US4929632A
公开(公告)日：1990-05-29
申请号：US177042
申请日：1988-04-04
申请人： Michael B. Tyers , Ian H. Coates , David C. Humber , George B. Ewan , James A. Bell
发明人： Michael B. Tyers , Ian H. Coates , David C. Humber , George B. Ewan , James A. Bell
IPC分类号： C07D403/06 , A61K31/415 , A61P1/00 , A61P1/08
CPC分类号： A61K31/415 , Y10S514/872 , Y10S514/917 , Y10S514/922
摘要： The invention relates to the use of compounds of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group; and one of the groups represented byR.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.2-6 alkenyl 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 alkyl group; and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage in radiological examination procedures.The invention also relates to a product containing a therapeutic agent liable to induce nausea and vomiting, e.g. a cytostatic agent such as a cyclophosphamide, an alkylating agent or a platinum complex, and a compound of the general formula (I) as a combined preparation for simultaneous separate or sequential use in therapy.

7. 发明授权

US5198447A Medicaments 失效
标题翻译：药剂
公开(公告)号：US5198447A
公开(公告)日：1993-03-30
申请号：US734281
申请日：1991-07-16
申请人： Michael B. Tyers
发明人： Michael B. Tyers
IPC分类号： A61K31/435 , A61K31/46
CPC分类号： A61K31/435 , A61K31/46
摘要： The invention relates to the use of compounds which act as antagonists of 5-hydroxytryptamine (5-HT) at 5-HT.sub.3 receptors for the relief or prevention of a withdrawal syndrome resulting from addiction to a drug or substance of abuse and/or for the suppression of dependence on drugs or substances of abuse.
摘要翻译：本发明涉及作为5-羟色胺（5-HT）拮抗剂在5-HT 3受体上的化合物在缓解或预防由药物或滥用物质成瘾引起的戒断综合征和/或制止对毒品或滥用物质的依赖。

8. 发明授权

US4973594A Medicaments 失效
标题翻译：药剂
公开(公告)号：US4973594A
公开(公告)日：1990-11-27
申请号：US133896
申请日：1987-12-16
申请人： Michael B. Tyers
发明人： Michael B. Tyers
IPC分类号： C07D487/08 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/46 , A61K31/495 , A61K31/50 , A61K31/55 , A61P25/24 , A61P25/26 , C07D403/06 , C07D451/04 , C07D451/12 , C07D451/14 , C07D471/08
CPC分类号： A61K31/46 , A61K31/415 , A61K31/445 , A61K31/50 , A61K31/55
摘要： The invention relates to the use of compounds which act as antagonists of 5-hydroxytryptamine (5-HT) at 5-HT.sub.3 receptors for the treatment of depression.

9. 发明授权

US4835173A Method of medical treatment 失效
标题翻译：医疗方法
公开(公告)号：US4835173A
公开(公告)日：1989-05-30
申请号：US133887
申请日：1987-12-16
申请人： Michael B. Tyers
发明人： Michael B. Tyers
IPC分类号： A61K31/415 , A61P25/24 , A61P25/26 , C07D403/06
CPC分类号： A61K31/415
摘要： The invention relates to the use of 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carbazol-4-one and physiologically acceptable salts and solvates thereof in the treatment of depression.

10. 发明授权

US5298510A Medicaments 失效
标题翻译：药剂
公开(公告)号：US5298510A
公开(公告)日：1994-03-29
申请号：US1665
申请日：1993-01-07
申请人： Michael B. Tyers
发明人： Michael B. Tyers
IPC分类号： A61K31/42 , A61K31/435 , A61K31/46 , A61K45/00 , A61P43/00 , C07D403/06 , C07D451/04 , C07D451/12 , C07D451/14 , C07D455/00 , A61K31/44
CPC分类号： A61K31/46 , A61K31/435 , Y10S514/81
摘要： The invention relates to the use of compounds which act as antagonists of 5-hydroxytryptamine (5-HT) at 5-HT.sub.3 receptors for the relief or prevention of a withdrawal syndrome resulting from addiction to a drug or substance of abuse and/or for the suppression of dependence on drugs or substances of abuse.
摘要翻译：本发明涉及作为5-羟色胺（5-HT）拮抗剂在5-HT 3受体上的化合物在缓解或预防由药物或滥用物质成瘾引起的戒断综合征和/或制止对毒品或滥用物质的依赖。

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