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    Azabicyclic compounds, process for their preparation and pharmaceutical compositions containing them
    51.
    发明公开
    Azabicyclic compounds, process for their preparation and pharmaceutical compositions containing them 失效
    化学化合物，其制备方法和含有它们的药物组合物

    公开(公告)号：EP0289170A3

    公开(公告)日：1990-04-25

    申请号：EP88303336.7

    申请日：1988-04-13

    申请人： BEECHAM GROUP PLC

    发明人： King, Francis David, c/o SmithKline Beecham

    IPC分类号： C07D519/00 ,  C07D471/08 ,  C07D453/06 ,  A61K31/435

    CPC分类号： C07D451/04 ,  C07D451/12 ,  C07D451/14 ,  C07D453/02

    摘要： Compounds of formula (I), or a pharmaceutically acceptable salt thereof:
        Y-CO-L-Z      (I)
    wherein
    L      is NH or O;
    Y      is a group of formula (a), (b) or (c):
    wherein
    R₁ and R₂, R₅ and R₆, R₉ and R₁₀,      are independently selected from hydrogen or halogen;
    X      is N or CR₃ wherein
    R₃      is hydrogen or C₁₋₆ alkoxy;
    R₄      is hydrogen, halogen, CF₃, C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ alkylthio, C₁₋₆ alkylsulphonyl, C₁₋₆ alkylsulphinyl, C₁₋₇ acyl, cyano, C₁₋₆ alkoxycarbonyl, C₁₋₇ acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C₁₋₆ alkyl, C₃₋₈ cycloalkyl, and C₃₋₈ cycloalkyl C₁₋₄ alkyl or disubstituted by C₄ or C₅ polymethylene; phenyl or phenyl C₁₋₄ alkyl group optionally substituted in the phenyl ring by one or two of halogen, C₁₋₆ alkoxy or C₁₋₆ alkyl groups;
        one of R₇ and R₈      is C₁₋₆ alkyl and the other is C₁₋₆ alkyl, phenyl or phenyl C₁₋₄ alkyl optionally substituted in either phenyl ring by one or two of C₁₋₆ alkyl, C₁₋₆ alkoxy or halogen; or
    R₇ and R₈      together are C₂₋₆ polymethylene or C₂₋₅ polymethylene interrupted by an -O- linkage;
    R₁₁      is hydrogen or C₁₋₆ alkoxy;
    R₁₂      is hydrogen, halogen, CF₃, C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ alkylthio, C₁₋₆ alkylsulphonyl, C₁₋₆ alkylsulphinyl, C₁₋₇ acyl, cyano, C₁₋₆ alkoxycarbonyl, C₁₋₇ acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C₁₋₆ alkyl, C₃₋₈ cycloalkyl, and C₃₋₈ cycloalkyl C₁₋₄ alkyl or disubstituted by C₄ or C₅ polymethylene; phenyl or phenyl C₁₋₄ alkyl optionally substituted in either phenyl ring by one or two of halogen, C₁₋₆ alkoxy or C₁₋₆ alkyl groups; Z      is a group of formula (d), (e) or (f):
    wherein
    n      is 2 or 3;
    p      is 1 or 2;
    q      is 1 to 3;
    r      is 1 to 3; and
    R₁₃ or R₁₄      is C₁₋₄ alkyl;
    having 5-HT₃ receptor antagonist activity, a process for their preparation and their use as pharmaceuticals.

    Benzopyran derivatives with antihypertensive activity
    53.
    发明公开
    Benzopyran derivatives with antihypertensive activity 失效
    Benzopyranderivate mit einer blutdrucksenkenden Wirkung。

    公开(公告)号：EP0359537A1

    公开(公告)日：1990-03-21

    申请号：EP89309272.6

    申请日：1989-09-12

    申请人： BEECHAM GROUP PLC

    发明人： Stemp, Geoffrey ,  Burrell, Gordon ,  Smith, David Glynn Beecham Pharmaceuticals

    IPC分类号： C07D311/68 ,  C07D405/04 ,  C07D491/04 ,  C07C247/14 ,  C07C255/59 ,  C07C279/16 ,  C07C335/14 ,  A61K31/44

    CPC分类号： C07D405/04 ,  C07C255/59 ,  C07C255/67 ,  C07C279/28 ,  C07C335/32 ,  C07C2602/08 ,  C07D311/68 ,  C07D491/04

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof:
    wherein
    a and b together form an -O- or -CH₂- linkage or a bond;
    either Y is N and R₂ is hydrogen; or
    Y is C-R₁
    wherein
    either one of R₁ and R₂ is hydrogen and the other is nitro, cyano, halo, CF₃, formyl, aldoxime, CF₃O, NO₂-CH=CH-, NC-CH=CH-; a group R x X- wherein R x is C₁₋₆ alkyl, aryl or heteroaryl either of which may be optionally substituted by one, two or three of C₁₋₄ alkyl, C₁₋₄ alkoxy, nitro, halo, CF₃ and cyano; and X is C=O, O.C=O, C=O.O, CHOH, SO, SO₂, O.SO, O.SO₂, CONH, O.CONH, C=S, O.C=S, C=S.O, CH.SH, SONH, SO₂NH, O.SONH, O.SO₂NH, CO-CH=CH, C=NHOH, C=NNH₂; or a group R y R z NZ- wherein R y and R z are independently hydrogen or C₁₋₆ alkyl and Z is C=O, SO or SO₂; or
    R₁ is a C₃₋₈ cycloalkyl group or a C₁₋₆ alkyl group optionally substituted by a group which is hydroxy, C₁₋₆ alkoxy, amino optionally substituted by one or two C₁₋₆ alkyl groups, C₁₋₇ alkanoylamino, C₃₋₈ cycloalkyloxy or C₃₋₈ cycloalkylamino; and R₂ is hydrogen; or
    one of R₁ and R₂ is nitro, cyano or C₁₋₃ alkylcarbonyl and the other is a different group selected from nitro, cyano, halo, C₁₋₃ alkylcarbonyl, methoxy or amino optionally substituted by one or two C₁₋₆ alkyl or by C₂₋₇ alkanoyl;
    either one of R₃ and R₄ is hydrogen or C₁₋₄ alkyl and the other is C₁₋₄ alkyl; or
    R₃ and R₄ together are C₂₋₅ polymethylene;
    either R₅ is hydrogen, hydroxy, C₁₋₆ alkoxy or C₁₋₇ acyloxy; and
    R₆ is hydrogen; or
    R₅ and R₆ together are a bond;
    either R₇ is hydrogen, C₁₋₆ alkyl, C₃₋₆ cycloalkyl, C₂₋₆ alkenyl or C₂₋₆ alkynyl; and
    R₈ is hydrogen or C₁₋₆ alkyl; or
    R₇ and R₈ together are C₂₋₄ polymethylene;
    R₉ is CN, NO₂, COR₁₀ or SO₂R₁₀ wherein R₁₀ is C₁₋₃ alkyl, NH₂, NH(C₁₋₃ alkyl), CF₃ or phenyl optionally substituted as defined for R x ; and
    the R₈N(NR₉)NHR₇ moiety is trans to the R₅ group when R₅ is hydroxy, C₁₋₆ alkoxy or C₁₋₇ acyloxy;
    having antihypertensive and/or bronchodilator activity, processes for their preparation and their use as pharmaceuticals.

    摘要翻译： 式（I）化合物及其药学上可接受的盐：其中a和b一起形成-O-或-CH 2 - 键或键; Y是N，R 2是氢; 或Y是C-R1，其中R1和R2中的任一个是氢，另一个是硝基，氰基，卤素，CF 3，甲酰基，醛肟，CF 3 O，NO 2 -CH = CH-，NC-CH = CH-; 基团RxX-，其中Rx是C 1-6烷基，芳基或杂芳基，其中任一个可以任选被C 1-4烷基，C 1-4烷氧基，硝基，卤素，CF 3和氰基中的一个，两个或三个取代; 并且X为C = O，OC = O，C = OO，CHOH，SO，SO2，O.SO，O.SO2，CONH，O.CONH，C = S，OC = S，C = SO，CH.SH ，SONH，SO2NH，O.SONH，O.SO2NH，CO-CH = CH，C = NHOH，C = NNH2; 或RyRzNZ-基团，其中R y和R z独立地为氢或C 1-6烷基，Z为C = O，SO或SO 2; 或R 1为任选被羟基，C 1-6烷氧基，任选被一个或两个C 1-6烷基取代的氨基，C 1-7烷酰基氨基，C 3-8烷基氨基， 8环烷氧基或C 3-8环烷基氨基; R2是氢; 或R 1和R 2中的一个是硝基，氰基或C 1-3烷基羰基，另一个是选自硝基，氰基，卤素，C 1-3烷基羰基，甲氧基或任选被一个或两个C 1-6烷基取代的氨基或不同的基团 C2-7烷酰基; R3和R4中的任一个是氢或C 1-4烷基，另一个是C 1-4烷基; 或R3和R4一起是C2-5聚亚甲基; R5是氢，羟基，C1-6烷氧基或C1-7酰氧基; R6为氢; 或R5和R6一起是键; R 7是氢，C 1-6烷基，C 3-6环烷基，C 2-6烯基或C 2-6炔基; R8是氢或C1-6烷基; 或R7和R8一起是C2-4聚亚甲基; R9是CN，NO2，COR10或SO2R10，其中R10是C1-3烷基，NH2，NH（C1-3烷基），CF3或如Rx所定义的任选取代的苯基; 当R 5为羟基，C 1-6烷氧基或C 1-7酰氧基时，R 8 N（NR 9）NHR 7部分为反式基团; 具有抗高血压和/或支气管扩张剂活性，其制备方法及其作为药物的用途。

    Skin treatment composition
    54.
    发明公开
    Skin treatment composition 无效
    皮肤治疗组合物

    公开(公告)号：EP0330496A3

    公开(公告)日：1990-02-28

    申请号：EP89301855.6

    申请日：1989-02-24

    申请人： BEECHAM GROUP PLC

    发明人： Batt, Margaret Dorothy

    IPC分类号： A61K7/48

    CPC分类号： A61Q19/004 ,  A61K8/585 ,  A61K8/671 ,  A61Q19/08

    摘要： A skin treatment composition comprising a topically acceptable base and an effective amount of at least one ester of retinol is useful in the treatment of photoaged human skin.

    摘要翻译： 包含局部可接受的碱和有效量的至少一种视黄醇酯的皮肤处理组合物可用于治疗光老化人皮肤。

    Use of imidazolinylaminoisoindolines and related compounds for the manufacture of a medicament for the treatment of hyperglycaemia.
    58.
    发明公开
    Use of imidazolinylaminoisoindolines and related compounds for the manufacture of a medicament for the treatment of hyperglycaemia. 失效
    咪唑啉基氨基异吲哚啉和相关化合物用于制造治疗高血糖的药物的用途。

    公开(公告)号：EP0254777A3

    公开(公告)日：1989-11-08

    申请号：EP86305248.6

    申请日：1986-07-07

    申请人： BEECHAM GROUP PLC

    发明人： Cawthorne, Michael Anthony Beecham Pharmaceuticals

    IPC分类号： A61K31/40 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  A61K31/435 ,  A61K31/47 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55

    CPC分类号： A61K31/425 ,  A61K31/40 ,  A61K31/415 ,  A61K31/42 ,  A61K31/435 ,  A61K31/47 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55

    摘要： A method for the treatment and/or prophylaxis of hyperglycaemia in human or non-human mammals which comprises administering to the mammal in need of such treatment and/or prophylaxis an effective non-toxic amount of:
    a compound of formula (I):
    or a pharmaceutically acceptable acid addition salt thereof, wherein
    each of R¹ and R², which may be the same or different, represents a hydrogen or halogen atom, or an alkyl or alkoxy group containing 1 to 4 carbon atoms,
    X represents an oxygen or sulphur atom, an imino group, an acylimino group containing 2 to 4 carbon atoms in the acyl group, or a methylene group, each of n and m, which may be the same or different, represents the number 1, 2 or 3, and p represents the number 2 or 3; with the proviso that when the moiety is present in formula (I), then either R¹ or R² must represent hydrogen; or
    a compound of formula (II):
    or a pharmaceutically acceptable acid addition salt thereof, wherein
    each of R³ and R⁴ may be either a hydrogen or halogen atom; or an alkyl or alkoxy group either of which groups may have from 1 to 4 carbon atoms; providing that either R³ or R⁴ must be hydrogen;
    R⁵ and R⁶ can be identical or different and either a hydrogen or an alkyl with 1 to 4 carbon atoms, and
    R⁷, R⁸, R⁹, and R¹⁰ can be identical or different and either hydrogen or an alkyl with 1 to 4 carbon atoms, or in which
    R⁷ and R⁸ together represent an ethylene group with the further proviso that when R⁷ and R⁸ represent an ethylene group then at least one of R⁵, R⁶, R⁹ and R¹⁰ represents an alkyl group with 1 to 4 carbon atoms; and compositions for use in such method.

    摘要翻译： 一种治疗和/或预防人或非人哺乳动物高血糖症的方法，包括对需要这种治疗和/或预防的哺乳动物施用有效无毒量的：式（I）化合物：或 其中R 1和R 2可以相同或不同，代表氢或卤素原子，或含有1-4个碳原子的烷基或烷氧基，X代表氧或硫原子 亚氨基，酰基中含有2至4个碳原子的酰基亚氨基或亚甲基，n和m各自可以相同或不同，代表数字1,2或3，并且p代表 数字2或3; 条件是当该部分存在于式（I）中时，则R 1或R 2必须代表氢; 或式（Ⅱ）化合物或其药学上可接受的酸加成盐，其中R 3和R 4各自可以是氢原子或卤素原子; 或者这些基团中的任一个可以具有1至4个碳原子的烷基或烷氧基; 条件是R 3或R 4必须是氢; R 5和R 6可以相同或不同，为氢或具有1至4个碳原子的烷基，R 7，R 8，R 8和R 10可以相同或不同，为氢或具有1至4个碳原子的烷基，或 其中R 9和R 9一起代表亚乙基，进一步的条件是当R 7和R 7代表亚乙基时，则R 5，R 6，R 7和R 10中至少一个代表具有1至4个碳原子的烷基; 和用于这种方法的组合物。