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41. 发明授权

US5270333A Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US5270333A
公开(公告)日：1993-12-14
申请号：US745896
申请日：1991-08-16
申请人： David E. Bays , Alexander W. Oxford
发明人： David E. Bays , Alexander W. Oxford
IPC分类号： C07D209/14 , C07D209/16 , A61K31/40
CPC分类号： C07D209/14 , C07D209/16
摘要： Compounds are disclosed of general formula: ##STR1## wherein R.sup.1 is H, C.sub.1-6 alkyl or C.sub.3-6 alkenyl; R.sup.2 is H, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, aryl, ar(C.sub.1-4)-alkylene, or C.sub.5-7 cycloalkyl;R.sup.3 is H or C.sub.1-3 alkyl;R.sup.4 and R.sup.5 each represents H, C.sub.1-3 alkyl or 2-propenyl, or R.sup.4 and R.sup.5 together form an aralkylidene group;R.sup.6 represents --CO.sub.2 R.sup.7, COR.sup.7, --COCO.sub.2 R.sup.7, or --CONHR.sup.7, whereR.sup.7 represents H, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkenyl, aryl or ar(C.sub.1-4)alkylene (with the provisos that (a) R.sup.7 does not represent H or benzyl when R.sup.6 is --CO.sub.2 R.sup.7 and (b) R.sup.7 does not represent alkenyl when R.sup.6 is --CONHR.sup.7); and Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C.sub.1-3 alkyl group, 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.
摘要翻译：公开了以下通式的化合物：其中R 1是H，C 1-6烷基或C 3-6烯基; R 2是H，C 1-3烷基，C 3-6烯基，芳基，芳（C 1-4） - 亚烷基或C 5-7环烷基; R3是H或C1-3烷基; R4和R5各自表示H，C1-3烷基或2-丙烯基，或R4和R5一起形成亚烷基; R 6表示-CO 2 R 7，COR 7，-COCO 2 R 7或-CONHR 7，其中R 7表示H，C 1-4烷基，C 3-7环烷基，C 2-4烯基，芳基或芳（C 1-4）亚烷基（条件是（a ）当R 6为-CO 2 R 7时，R 7不表示H或苄基，（b）当R 6为-CONHR 7时，R 7不表示烯基）; 并且Alk表示可以是未被取代的或被不多于两个C 1-3烷基取代的含有两个或三个碳原子的亚烷基链，以及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。这些化合物可以配制成具有生理上可接受的载体或赋形剂的药物组合物，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。

42. 发明授权

US4997841A Indole derivatives 失效
公开(公告)号：US4997841A
公开(公告)日：1991-03-05
申请号：US231274
申请日：1988-08-12
申请人： Alexander W. Oxford , Darko Sutina , Martin R. Owen
发明人： Alexander W. Oxford , Darko Sutina , Martin R. Owen
IPC分类号： A61K31/4427 , A61K31/445 , A61P9/00 , A61P25/04 , A61P25/06 , A61P43/00 , 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 or C.sub.1-6 alkyl;R.sub.3 represents H;R.sub.4 represents H or C.sub.1-3 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.

43. 发明授权

US4324792A Antihistaminic imidazoles 失效
标题翻译：抗组胺咪唑
公开(公告)号：US4324792A
公开(公告)日：1982-04-13
申请号：US193846
申请日：1980-10-03
申请人： John Bradshaw , Alexander W. Oxford , David I. C. Scopes
发明人： John Bradshaw , Alexander W. Oxford , David I. C. Scopes
IPC分类号： A61K31/415 , A61P43/00 , C07D231/12 , C07D233/54 , C07D233/64 , C07D403/06 , A61K31/445
CPC分类号： C07D233/64 , C07C255/00
摘要： The present invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and bioprecursors thereof in which ##STR2## represents either ##STR3## R.sup.1 represents hydrogen, halogen, C.sub.1-4 alkoxy, hydroxy, alkyl, R.sup.4 CH(OH)--, cyano or R.sup.5 CONH--, R.sup.2 and R.sup.3, which may be the same or different, each represents a straight or branched chain alkyl group or alkenyl group or R.sup.2 and R.sup.3 may, together with the nitrogen atom to which they are attached, form a saturated heterocyclic ring containing from 5 to 7 members which may optionally contain an oxygen atom; R.sup.4 represents hydrogen or alkyl; and R.sup.5 represents hydrogen, alkyl or C.sub.1-4 alkoxy. The compounds have been shown to exhibit H.sub.1 -antagonist activity in standard pharmacological tests.
摘要翻译：本发明提供了通式（I）的化合物及其生理学上可接受的盐和生物前体，其中R 1表示氢，卤素，C 1-4烷氧基，羟基，烷基，R 4 CH （OH） - ，氰基或R 5 CONH - ，R 2和R 3可以相同或不同，表示直链或支链烷基或烯基，或者R 2和R 3可以与它们所连接的氮原子一起形成含有5至7个可任意含有氧原子的饱和杂环; R4表示氢或烷基; R5代表氢，烷基或C1-4烷氧基。化合物已被证明在标准药理学试验中显示出H1拮抗剂活性。

44. 发明授权

US4278673A Pharmacologically active compounds 失效
标题翻译：药理活性化合物
公开(公告)号：US4278673A
公开(公告)日：1981-07-14
申请号：US72098
申请日：1979-09-04
申请人： David Hartley , Alexander W. Oxford
发明人： David Hartley , Alexander W. Oxford
IPC分类号： A61K31/53 , A61P11/08 , C07D253/06 , C07D253/07 , C07D487/04 , A61K31/415
CPC分类号： C07D253/06 , C07D253/07 , C07D487/04
摘要： There are provided compounds of the general formula (I): ##STR1## and physiologically acceptable salts thereof in which Z represents a group ##STR2## wherein R.sub.2 represents a hydrogen atom or a straight or branched chain alkyl radical, or Z can additionally represent a group ##STR3## and R.sub.1, R.sub.3 and R.sub.4, which may be the same or different, each represent a hydrogen atom, a cycloalkyl group, an aryl group which may optionally be substituted by one or more hydroxy, alkoxy, or halogen radicals, or a straight or branched alkyl or alkenyl group, which alkyl or alkenyl group may be substituted with an aryl group, which aryl group may optionally be substituted by one or more hydroxy, alkoxy or halogen radicals. The compounds possess spasmolytic and cAMP phosphodiesterase inhibitory activity.
摘要翻译：提供通式（I）的化合物：其中Z表示基团，其中R2表示氢原子或直链或支链烷基，或Z可另外表示基团＆lt; IMAGE＆gt;和可以相同或不同的R 1，R 3和R 4各自表示氢原子，环烷基，可任意被一个或多个羟基，烷氧基或卤素基团取代的芳基，或直链或支链的烷基或链烯基，该烷基或烯基可以被芳基取代，该芳基可任选地被一个或多个羟基，烷氧基或卤素基团取代。该化合物具有解痉和cAMP磷酸二酯酶抑制活性。

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