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11. 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.

12. 发明授权

US4985422A Lactam derivatives 失效
公开(公告)号：US4985422A
公开(公告)日：1991-01-15
申请号：US343359
申请日：1989-04-26
申请人： Peter C. North , Alexander W. Oxford , Ian H. Coates , Paul J. Beswick
发明人： Peter C. North , Alexander W. Oxford , Ian H. Coates , Paul J. Beswick
IPC分类号： A61K31/435 , A61K31/55 , A61P43/00 , C07D491/04 , C07D491/048 , C07D495/04
CPC分类号： C07D491/04 , C07D495/04
摘要： Compounds which are potent and selective antagonists of the effect of 5-HT.sub.3 receptors and are useful in the treatment of psychotic disorders, anxiety, and nausea and vomiting, of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula (a), (b) or (c): ##STR2## 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 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;n represents 1 or 2;Q represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenyl C.sub.1-3 alkoxy or C.sub.1-6 alkyl group, or a group --NR.sup.4 R.sup.5 or --CONR.sup.4 R.sup.5 ; andX represents an oxygen or a sulphur atom, and, when Im represents an imidazolyl group of formula (c), X may also represent the group NR.sup.6, where R.sup.6 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 cycloalkyl, C.sub.1-4 alkyl, phenyl, phenyl C.sub.1-3 alkyl, --CO.sub.2 R.sup.7, --COR.sup.7, --CONR.sup.7 R.sup.8 or --SO.sub.2 R.sup.7 ; and physiologically acceptable salts or solvates thereof.

13. 发明授权

US5066660A Indole derivatives 失效
标题翻译： INDOLE DORIVATIVES
公开(公告)号：US5066660A
公开(公告)日：1991-11-19
申请号：US570513
申请日：1990-08-21
申请人： Alexander W. Oxford , Ian H. Coates , Darko Butina
发明人： Alexander W. Oxford , Ian H. Coates , Darko Butina
IPC分类号： A61K31/4427 , A61K31/445 , A61P25/04 , A61P25/06 , C07D401/04
CPC分类号： C07D401/04
摘要： Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents H or C.sub.1-6 alkyl;R.sub.2 represents H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phen(C.sub.1-3)alkyl in which the phenyl ring is optionally substituted by halogen, C.sub.1-4 alkoxy, hydroxy or C.sub.1-3 alkyl;R.sub.3 represents H, C.sub.1-3 alkyl, --CO.sub.2 R.sub.5, --COR.sub.5, --COCO.sub.2 R.sub.5 or --CONHR.sub.5 whereR.sub.5 represents H, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkenyl, aryl or ar(C.sub.1-4)alkyl in which the aryl group is optionally substituted by halogen, C.sub.1-4 alkoxy, C.sub.1-4 alkyl or hydroxy) (provided that where R.sub.3 represents --CO.sub.2 R.sub.5, R.sub.5 is other than H);R.sub.4 represents H, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, phenyl or phen (C.sub.1-3)alkyl;A-B represents CH--CH.sub.2 --or C.dbd.CH--D represents --CO-- or --SO.sub.2 --n represents 0, 1-5;provided that when D represents --SO.sub.2, n is 2, R.sub.3 represents H and R.sub.4 represents H or C.sub.1-3 alkyl, R.sub.2 is other than H or C.sub.1-6 alkyl; and pharmaceutically acceptable salts and solvates (for example hydrates) thereof.The compounds are indicated as useful for the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.

14. 发明授权

US4739072A Process for preparing tetrahydrocarbazolones 失效
标题翻译：四氢咔唑酮的制备方法
公开(公告)号：US4739072A
公开(公告)日：1988-04-19
申请号：US888254
申请日：1986-07-23
申请人： Alexander W. Oxford , Colin D. Eldred , Ian H. Coates , James A. Bell , David C. Humber , George B. Ewan
发明人： Alexander W. Oxford , Colin D. Eldred , Ian H. Coates , James A. Bell , David C. Humber , George B. Ewan
IPC分类号： C07D403/06 , A61K31/415 , C07C221/00 , C07C225/14 , C07D233/60 , C07D233/61 , C07D521/00 , C07D403/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention relates to a process for the preparation of a compound of 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 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.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, represent a hydrogen atom or a C.sub.1-6 alkyl group;or a salt or protected derivative thereof, by cyclization of a compound of general formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, or a salt or a protected derivative thereof.The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.
摘要翻译：本发明涉及一种制备通式（I）化合物的方法，其中R1表示氢原子或C1-10烷基，C3-7环烷基，C3-7环烷基 - （C1- 4）烷基，C 3-6烯基，C 3-10炔基，苯基或苯基 - （C 1-3）烷基，并且由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，其它可以相同或不同的两个基团表示氢原子或C 1-6烷基; 或其盐或被保护的衍生物，通过使通式（II）化合物（II）其中R 1，R 2，R 3和R 4如上所定义的化合物或其盐或其保护的衍生物环化。式（I）化合物是“神经元”5-羟色胺受体的有效和选择性拮抗剂。

15. 发明授权

US4140713A Phenylethanolamine therapeutic agents 失效
标题翻译：苯乙醇胺治疗剂
公开(公告)号：US4140713A
公开(公告)日：1979-02-20
申请号：US873765
申请日：1978-01-31
申请人： Alexander W. Oxford , Ian H. Coates
发明人： Alexander W. Oxford , Ian H. Coates
IPC分类号： A61K31/165 , A61P25/02 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/06 , C07C231/12 , C07C237/30 , C07C301/00 , C07C303/40 , C07C311/08 , C07C313/00 , C07D295/112 , C07D295/135 , C07C91/06 , C07C143/78 , C07C143/80
CPC分类号： C07D295/112 , C07D295/135
摘要： Compounds of the general formula: ##STR1## and non-toxic physiologically acceptable salts thereof, in which R.sub.1 is a halogen atom or a group NR.sub.2 R.sub.3 ;R.sub.2 and R.sub.3, which may be the same or different, are hydrogen or (C.sub.1 -C.sub.6) straight or branched chain alkyl or R.sub.2 and R.sub.3 may, together with the nitrogen atom, form a 5 or 6 membered heterocyclic ring which may contain a further hetero atom selected from O, N or S; or R.sub.2 may be hydrogen and R.sub.3 may by group R.sub.4 CO or R.sub.4 SO.sub.2 where R.sub.4 is hydrogen or alkyl (C.sub.1-4);R.sub.5 is hydrogen or one or more halogen atoms or hydroxy or alkoxy (C.sub.1-4) groups; andX is CH.sub.2, O or a group NR.sub.6 where R.sub.6 is hydrogen or alkyl (C.sub.1-4). These compounds block .beta.-adrenoreceptors.
摘要翻译：其中R 1为卤素原子或NR 2 R 3基团的通式为：其无毒生理学上可接受的盐; R2和R3可以相同或不同，是氢或（C1-C6）直链或支链烷基或R2和R3可以与氮原子一起形成5或6元杂环，其可以含有另外选自O，N或S的杂原子; 或R 2可以是氢，R 3可以通过R4CO或R4SO2，其中R4是氢或烷基（C1-4）; R5是氢或一个或多个卤素原子或羟基或烷氧基（C1-4）基团; 并且X是CH 2，O或NR 6，其中R 6是氢或烷基（C 1-4）。这些化合物阻断β-肾上腺素受体。

16. 发明授权

US4939144A Tricyclic ketone derivatives as 5-HT antagonists 失效
标题翻译：三环酮衍生物作为5-HT拮抗剂
公开(公告)号：US4939144A
公开(公告)日：1990-07-03
申请号：US260680
申请日：1988-10-21
申请人： Ian H. Coates , David C. Humber , James A. Bell , George B. Ewan , Alexander W. Oxford , William L. Mitchell
发明人： Ian H. Coates , David C. Humber , James A. Bell , George B. Ewan , Alexander W. Oxford , William L. Mitchell
IPC分类号： A61K31/415 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , C07D403/06 , C07D405/06 , C07D409/06 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D403/06 , C07D405/06 , C07D409/06
摘要： The invention relates to ketones of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## 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 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;n represents 1, 2 or 3;Q represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenyl C.sub.1-3 alkoxy or C.sub.1-6 alkyl group, or a group --NR.sup.4 R.sup.5 or --CONR.sup.4 R.sup.5, (wherein R.sup.4 and R.sup.5, 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 X represents an oxygen or a sulphur atom, or, when Im represents an imidazolyl group of formula (c) and n represents 1 or 3, X may also represent the group NR.sup.6, wherein R.sup.6 represents a hydrogen atom or a group selected from C.sub.1-10 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, phenyl C.sub.1-3 alkyl, --CO.sub.2 R.sup.7, --COR.sup.7, --CONR.sup.7 R.sup.8 or --SO.sub.2 R.sup.7 (wherein R.sup.7 and R.sup.8, 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 phenyl C.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.7 does not represent a hydrogen atom when R.sup.6 represents a group --CO.sub.2 R.sup.7); and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT and 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.

17. 发明授权

US4994483A 5-substituted-3-aminoalkyl indole derivatives for migraine 失效
标题翻译：用于偏头痛的5-取代-3-氨基烷基吲哚衍生物
公开(公告)号：US4994483A
公开(公告)日：1991-02-19
申请号：US443874
申请日：1989-11-30
申请人： Alexander W. Oxford , Brian Evans , Michael D. Dowle , Ian H. Coates
发明人： Alexander W. Oxford , Brian Evans , Michael D. Dowle , Ian H. Coates
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。

18. 发明授权

US4870096A 5-substituted 3-aninoalkyl indoles 失效
标题翻译： 5-取代的3-苯基烷基吲哚
公开(公告)号：US4870096A
公开(公告)日：1989-09-26
申请号：US940652
申请日：1986-12-11
申请人： Alexander W. Oxford , Ian H. Coates , David E. Bays , Colin F. Webb
发明人： Alexander W. Oxford , Ian H. Coates , David E. Bays , Colin F. Webb
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。

19. 发明授权

US4855314A Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US4855314A
公开(公告)日：1989-08-08
申请号：US1469
申请日：1987-01-08
申请人： Alexander W. Oxford , Ian H. Coates , David E. Bays , Colin F. Webb , Michael D. Dowle , Keith Mills , Colin D. Eldred
发明人： Alexander W. Oxford , Ian H. Coates , David E. Bays , Colin F. Webb , Michael D. Dowle , Keith Mills , Colin D. Eldred
IPC分类号： C07D209/14 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61P9/00 , A61P25/04 , C07D209/16
CPC分类号： C07D209/16
摘要： Compounds are disclosed of formula (I): ##STR1## wherein R.sub.1 is halogen, a C.sub.1-3 alkoxy, R.sub.6 R.sub.7 NCO(CH.sub.2).sub.p --, R.sub.6 CONH(CH.sub.2).sub.p --, R.sub.6 R.sub.7 NSO.sub.2 (CH.sub.2).sub.p --, or R.sub.8 SO.sub.2 NH(CH.sub.2).sub.p -- (where R.sub.6 and R.sub.7 each represents hydrogen or C.sub.1-3 alkyl, R.sub.8 represents C.sub.1-3 alkyl and p is zero or 1);R.sub.2 represents hydrogen or C.sub.1-3 alkyl; R.sub.3 represents hydrogen or C.sub.1-3 alkyl;R.sub.4 and R.sub.5 each represents hydrogen, C.sub.1-3 alkyl or 2-propenyl;A represents --CO-- or --SO.sub.2 --;n represents an integer from 2 to 5; and m represents zero or an integer from 1 to 4; 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. The compounds may be formulated as pharmaceutical compositions with physiologically acceptable carriers or excipients for administration by any convenient route. Various methods for the preparation of the compounds (I) are disclosed.

20. 发明授权

US4316907A Heterocyclic compounds, processes for their preparation and their use 失效
标题翻译：杂环化合物，其制备方法及其用途
公开(公告)号：US4316907A
公开(公告)日：1982-02-23
申请号：US163568
申请日：1980-06-27
申请人： Alexander W. Oxford , John Bradshaw , Ian H. Coates
发明人： Alexander W. Oxford , John Bradshaw , Ian H. Coates
IPC分类号： A61K31/38 , A61K31/381 , A61P9/12 , A61P25/02 , C07D333/38 , C07D333/24
CPC分类号： C07D333/38 , Y10S514/913
摘要： Thiophene carboxamides are described of general formula I ##STR1## in which the amide function is in the 2- or 3-position on the thiophene ring, R.sub.1 to R.sub.5 inclusive are hydrogen atoms or lower alkyl groups, X is --CH.sub.2 --, --O-- or --NR.sub.6 -- where R.sub.6 is hydrogen or a lower alkyl group, n is a number from 0 to 3 and Ar is an optionally substituted phenyl groupand their physiologically acceptable salts.The compounds have been found to lower blood pressure in animals and to exhibit a blocking action at .beta.-adrenoreceptors and their use is indicated for the treatment of cardiovascular disorders such as hypertension and angina. Some of the compounds also exhibit a blocking action on .alpha.-adrenoreceptors and their use is indicated for the treatment of hypertention.
摘要翻译：噻吩甲酰胺描述为通式I ，其中酰胺官能团位于噻吩环上的2-或3-位，R 1至R 5包括氢原子或低级烷基，X为-CH 2 - ， - O - 或-NR 6 - ，其中R 6是氢或低级烷基，n是0-3的数，Ar是任选取代的苯基及其生理上可接受的盐。已经发现这些化合物降低动物血压并在β-肾上腺素受体上表现出阻断作用，并且它们用于治疗心血管疾病如高血压和心绞痛。一些化合物还对α-肾上腺素受体表现出阻断作用，并且其用途用于治疗高血压。

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