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12 条记录 (耗时 0.021 秒)

    Antihistaminic imidazoles
    1.
    发明授权
    Antihistaminic imidazoles 失效
    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。

    Morpholine derivatives, pharmaceutical compositions and use
    2.
    发明授权
    Morpholine derivatives, pharmaceutical compositions and use 失效
    吗啉衍生物，药物组合物和用途

    公开(公告)号：US4923863A

    公开(公告)日：1990-05-08

    申请号：US362170

    申请日：1989-06-06

    申请人： David I. C. Scopes ,  David E. Bays

    发明人： David I. C. Scopes ,  David E. Bays

    IPC分类号： A61K31/535 ,  A61K31/5375 ,  A61P9/00 ,  A61P9/10 ,  A61P25/04 ,  C07D265/30 ,  C07D413/06

    CPC分类号： C07D265/30

    摘要： Compounds are disclosed of formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are C.sub.1-6 alkyl or C.sub.3-6 alkenyl; or --NR.sub.1 R.sub.2 forms a 5-membered (optionally containing an oxygen atom adjacent to the nitrogen) or a 6-membered ring, which ring optionally contains one unit of unsaturation and which is unsubstituted or substituted by hydroxy, oxo, optionally substituted methylidene, --COR.sub.3 (where R.sub.6 represents C.sub.1-6 alkyl, OR.sub.4 or --NHR.sub.4, and R.sub.4 represents hydrogen, C.sub.1-6 alkyl, aryl, ar(C.sub.1-6)alkyl) or .dbd.NOR.sub.5 (where R.sub.5 represents C.sub.1-6 alkyl);X represents a direct bond, --CH.sub.2 -- or --CH.sub.2 O--;Ar represents a substituted phenyl moiety;and physiologically acceptable salts thereof.The compounds are indicated as useful for the treatment of pain and cerebral ischaemia.Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.

    Spiropiperidine derivatives
    4.
    发明授权
    Spiropiperidine derivatives 失效
    螺哌啶衍生物

    公开(公告)号：US5114945A

    公开(公告)日：1992-05-19

    申请号：US315261

    申请日：1989-02-23

    申请人： Norman F. Hayes ,  David I. C. Scopes ,  Andrew B. McElroy ,  Ann G. Hayes ,  Clive A. Meerholz

    发明人： Norman F. Hayes ,  David I. C. Scopes ,  Andrew B. McElroy ,  Ann G. Hayes ,  Clive A. Meerholz

    IPC分类号： C07D211/26 ,  C07D211/42 ,  C07D211/46 ,  C07D211/56 ,  C07D211/62 ,  C07D211/70 ,  C07D211/74 ,  C07D491/10 ,  C07D491/113 ,  C07D495/10 ,  C07D513/10

    CPC分类号： C07D491/10 ,  C07D211/26 ,  C07D211/42 ,  C07D211/46 ,  C07D211/56 ,  C07D211/62 ,  C07D211/70 ,  C07D211/74 ,  C07D495/10 ,  C07D513/10

    摘要： Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents hydroxy, C.sub.1-6 alkyl, C.sub.1-6 hydroxyalkyl, C.sub.1-6 carboxyalkyl, phenyl, oxo, amino, carboxy, amido, --NR.sub.4 COR.sub.5 (where R.sub.4 and R.sub.5 both represent C.sub.1-6 alkyl), optionally substituted methylidene or, together with the carbon atom to which it is attached, R.sub.1 forms a 5 or 6-membered ring containing one or more heteroatoms;R.sub.2 and R.sub.3 are the same or different and are C.sub.1-6 alkyl or C.sub.3-6 alkenyl; or --NR.sub.2 R.sub.3 forms a 5-membered (optionally containing an oxygen atom adjacent to the nitrogen) or a 6-membered ring, which ring optionally contains one unit of unsaturation and which is unsubstituted or substituted by hydroxy, oxo, optionally substituted methylidene, --COR.sub.6 (where R.sub.6 represents C.sub.1-6 alkyl, OR, or --NHR, and R represents hydrogen, C.sub.1-6 alkyl, aryl, ar(C.sub.1-6)alkyl) or .dbd.NOR.sub.8 (where R.sub.8 represents C.sub.1-6 alkyl);X represents a direct bond, --CH.sub.2 -- or --CH.sub.2 0--;Ar represents a substituted phenyl moiety;and physiologically acceptable salts thereof.The compounds are indicated as useful for the treatment of pain and cerebral ischemia.Proccesses and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.

    摘要翻译： 公开了式（I）的化合物其中R 1表示羟基，C 1-6烷基，C 1-6羟基烷基，C 1-6羧基烷基，苯基，氧代，氨基，羧基，酰氨基，-NR 4 COR 5（其中R 4和 R5均表示C1-6烷基），任选取代的亚甲基，或与其连接的碳原子一起形成含有一个或多个杂原子的5或6元环; R2和R3相同或不同，为C1-6烷基或C3-6烯基; 或-NR 2 R 3形成5元（任选地含有与氮相邻的氧原子）或6元环，该环任选地含有一个不饱和单元，并且是未取代的或被羟基，氧代，任选取代的亚甲基取代的 - COR6（其中R6表示C1-6烷基，OR或-NHR，R表示氢，C1-6烷基，芳基，芳基（C1-6）烷基）或= NOR8（其中R8表示C1-6烷基）; X表示直接键，-CH 2 - 或-CH 2 O-; Ar表示取代的苯基部分; 及其生理上可接受的盐。 这些化合物被指示用于治疗疼痛和脑缺血。 还公开了其制备方法和中间体以及含有它们的药物组合物。

    Imidazopyridayine derivatives having antiviral activity
    9.
    发明授权
    Imidazopyridayine derivatives having antiviral activity 失效
    具有抗病毒活性的咪唑并噻吩衍生物

    公开(公告)号：US4690917A

    公开(公告)日：1987-09-01

    申请号：US800667

    申请日：1985-11-22

    申请人： David J. Knight ,  David I. C. Scopes ,  Richard Storer ,  Stuart Holman

    发明人： David J. Knight ,  David I. C. Scopes ,  Richard Storer ,  Stuart Holman

    IPC分类号： A61K31/50 ,  A61P31/12 ,  C07D487/04 ,  C07D519/00 ,  A61K31/70 ,  C07H3/02

    CPC分类号： C07D487/04 ,  Y02P20/55

    摘要： Compounds of the formula: ##STR1## wherein R.sub.1, R.sub.3 and R.sub.4 each independently represents a hydrogen atom or a protecting group;R.sub.2 represents a halogen atom or a group of formula --NR.sub.a R.sub.b (where R.sub.a and R.sub.b, which may be the same or different, each represents a hydrogen atom or an alkyl group; or R.sub.a and R.sub.b may be linked to form, together with the nitrogen atom to which they are attached, a heterocyclic ring which optionally contains a further heteroatom);and their physiological equivalents as well as salts thereof with acids, exhibit antiviral activity against RNA viruses such as Influenza and/or are intermeidates for the preparation of antivirally active compounds.

    摘要翻译： 下式的化合物：其中R 1，R 3和R 4各自独立地表示氢原子或保护基; R 2表示卤素原子或式-NR a R b的基团（其中R a和R b可以相同或不同，各自表示氢原子或烷基;或者R a和R b可以与 它们所连接的氮原子，任选地含有另外的杂原子的杂环）; 和它们的生理等同物以及其与酸的盐，表现出对RNA病毒如流感的抗病毒活性和/或是用于制备抗病毒活性化合物的中间体。