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公开(公告)号：US5360800A
公开(公告)日：1994-11-01
申请号：US741570
申请日：1991-08-07
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。
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公开(公告)号：US5183820A
公开(公告)日：1993-02-02
申请号：US691814
申请日：1991-04-26
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。
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公开(公告)号：US5008272A
公开(公告)日：1991-04-16
申请号：US393145
申请日：1989-08-14
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.
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公开(公告)号：US5229407A
公开(公告)日：1993-07-20
申请号：US911395
申请日：1992-07-10
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。
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公开(公告)号：US4994483A
公开(公告)日：1991-02-19
申请号：US443874
申请日：1989-11-30
IPC分类号： C07D209/14 , A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , A61P25/02 , A61P25/04 , A61P25/06 , C07C67/00 , C07C301/00 , C07C311/02 , C07C311/35 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/16 , C07D209/18 , C07D209/48
CPC分类号： C07D209/48 , C07C205/44 , C07C309/00 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/16 , C07D209/18 , Y10S514/93
摘要： Indole derivatives are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl; R.sub.2 is a hydrogen, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, phenyl, phen(C.sub.1-4)alkyl or C.sub.5-7 cycloalkyl; R.sub.3 and R.sub.4 are hydrogen, C.sub.1-3 alkyl or propenyl groups or together form an aralkylidene group; Alk is C.sub.2 -C.sub.3 alkylene chain and A is C.sub.2 -C.sub.5 alkylene chainand its physiologically acceptable salts and solvates.The compounds may be prepared, for example, by cyclization of a compound of general formula (II): ##STR2## where Q is the group NR.sub.3 R.sub.4 or a protected derivative thereof or a leaving group and R.sub.1 l, R.sub.2, R.sub.3, R.sub.4, A and Alk are as defined for formula (I).The compounds have a selective vosoconstrictor action and are useful in treating pain such as migraine. The compounds may be formulated as pharmaceutical compositions in conventional manner, preferably for oral administration.
摘要翻译： 公开了通式（I）的吲哚衍生物：其中R 1是氢，C 1-6烷基或C 3-6烯基; R 2是氢，C 1-3烷基，C 3-6烯基，苯基，苯基（C 1-4）烷基或C 5-7环烷基; R3和R4是氢，C1-3烷基或丙烯基或一起形成亚烷基; Alk是C2-C3亚烷基链，A是C2-C5亚烷基链及其生理上可接受的盐和溶剂合物。 化合物可以例如通过环化通式（II）的化合物来制备：其中Q是NR3R4基团或其保护的衍生物或离去基团，R1，R2，R3 ，R4，A和Alk如式（I）所定义。 该化合物具有选择性的血管收缩作用，并且可用于治疗疼痛如偏头痛。 化合物可以以常规方式配制成药物组合物，优选用于口服给药。
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公开(公告)号：US4870096A
公开(公告)日：1989-09-26
申请号：US940652
申请日：1986-12-11
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , A61P25/04 , C07D209/16
CPC分类号： C07D209/16
摘要： Indoles are disclosed of formula (I): ##STR1## wherein R.sub.1 represents R.sub.5 R.sub.6 NCOCH.sub.2 --, R.sub.5 CONH(CH.sub.2).sub.p --,R.sub.5 R.sub.6 NSO.sub.2 (CH.sub.2).sub.p -- or R.sub.7 SO.sub.2 NH(CH.sub.2).sub.p --, (where R.sub.5 and R.sub.6 each represents a hydrogen atom or a C.sub.1-3 alkyl group, R.sub.7 represents C.sub.1-3 alkyl and p is zero or one),R.sub.2 is hydrogen or C.sub.1-3 alkyl;R.sub.3 and R.sub.4 each represents hydrogen atom, C.sub.1-3 alkyl, or 2-propenyl;m is zero or an integer from 1 to 4; andn is an integer from 2 to 5; and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. They may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers of excipients for administration by any convenient route.Various methods for the preparation of the compounds (I) are disclosed.
摘要翻译： 公开了式（I）的吲哚：其中R1表示R5R6NCOCH2-，R5CONH（CH2）p-，R5R6NSO2（CH2）p-或R7SO2NH（CH2）p-，（其中R5和R6各自表示 氢原子或C 1-3烷基，R 7表示C 1-3烷基，p为0或1），R 2为氢或C 1-3烷基; R3和R4各自表示氢原子，C1-3烷基或2-丙烯基; m为0或1至4的整数; n为2〜5的整数。 和其生理上可接受的盐和溶剂合物（例如水合物）。 这些化合物具有有效和选择性的血管收缩剂活性，并被用于治疗偏头痛。 它们可以配制成具有药学上可接受的赋形剂载体的药物组合物，用于通过任何方便的途径给药。 公开了制备化合物（I）的各种方法。
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公开(公告)号：US5225407A
公开(公告)日：1993-07-06
申请号：US941951
申请日：1992-09-08
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。
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公开(公告)号：US5196534A
公开(公告)日：1993-03-23
申请号：US704099
申请日：1991-05-22
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.
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公开(公告)号：US5116984A
公开(公告)日：1992-05-26
申请号：US333967
申请日：1989-04-06
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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公开(公告)号：US5013733A
公开(公告)日：1991-05-07
申请号：US485532
申请日：1990-02-27
申请人： Ian H. Coates , Alexander W. Oxford , Peter C. North , Thomas Miller , Anthony D. Baxter , Kevin I. Hammond
发明人： Ian H. Coates , Alexander W. Oxford , Peter C. North , Thomas Miller , Anthony D. Baxter , Kevin I. Hammond
IPC分类号： C07D453/02 , A61K31/435 , A61P1/00 , A61P1/04 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/28 , A61P43/00 , C07D519/00
CPC分类号： C07D519/00
摘要： The invention provides lactam derivatives of the general formula (I) ##STR1## wherein 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.3, --COR.sup.3, --CONR.sup.3 R.sup.4 or --SO.sub.2 R.sup.3 (wherein R.sup.3 and R.sup.4, 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.3 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.3 or --SO.sub.2 R.sup.3);and R.sup.2 represents a group of formula (a), (b) or (c): ##STR2## wherein R.sup.5 represents a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl or phenylC.sub.1-3 alkyl group;n represents 2, 3 or 4;Q represents a hydrogen or a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenylC.sub.1-3 alkoxy or C.sub.1-6 alkyl group or a group --NH.sup.6 R.sup.7 or --CONR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl or C.sub.3-4 alkenyl group, or together with the nitrogen atom to which they are attached form a saturated 5 to 7 membered ring); 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.
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