Anti-allergy bicyclic phenol ethers
    6.
    发明授权
    Anti-allergy bicyclic phenol ethers 失效
    抗过敏双酚酚醚

    公开(公告)号:US4486442A

    公开(公告)日:1984-12-04

    申请号:US469856

    申请日:1983-02-25

    摘要: The present invention provides bicyclic phenol ethers of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,R.sub.2 is a hydrogen atom or an acyl radical,X is an oxygen or sulphur atom or an --NH-- group;Y is a --CO--CHR.sub.3 -- group or a ##STR2## group; R.sub.3 is a hydrogen atom, a lower alkyl radical which can be optionally substituted by an aryl radical, or a cycloalkyl radical containing 3 to 7 carbon atoms; andR.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms, lower alkyl radicals, lower alkyl radicals, alkenyl radicals containing 2 to 16 carbon atoms, which can be optionally substituted by an aryl radical, or an aryl radical; orR.sub.4 and R.sub.5, together with the carbon atom to which they are attached, form a cycloalkyl ring containing 3 to 7 carbon atoms; and thesalts thereof with pharmacologically acceptable acids.The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.

    摘要翻译: 本发明提供以下通式的双环酚醚:其中R 1为氢原子或低级烷基,R 2为氢原子或酰基,X为氧或硫原子或 - NH-基团; Y是-CO-CHR3-基团或基团; R3是氢原子,可任意被芳基取代的低级烷基或含有3至7个碳原子的环烷基; 和可以相同或不同的R 4和R 5是氢原子,低级烷基,低级烷基,含有2至16个碳原子的烯基,其可任选被芳基或芳基取代; 或R 4和R 5与它们所连接的碳原子一起形成含有3至7个碳原子的环烷基环; 其盐与药理学上可接受的酸。 本发明还提供了制备这些化合物的方法,以及含有它们的药物组合物。

    Pyrazolo(3,4-d)pyrimidine compounds, compositions and method of use
    9.
    发明授权
    Pyrazolo(3,4-d)pyrimidine compounds, compositions and method of use 失效
    吡唑并(3,4-d)嘧啶化合物,组合物和使用方法

    公开(公告)号:US4904666A

    公开(公告)日:1990-02-27

    申请号:US181729

    申请日:1988-04-14

    CPC分类号: C07D487/04

    摘要: The present invention provides pyrazolo[3,4-d]-pyrimidines of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 to C.sub.6 -alkyl radical, a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aryl radical, R.sub.2 is a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aralkyl or hetaralkyl radical with 1 to 6 carbon atoms in the alkyl moiety and substituted, if desired, one or more times by halogen, C.sub.1 to C.sub.6 -alkyl, hydroxyl, C.sub.1 to C.sub.6 -alkoxy, C.sub.1 to C.sub.3 -haloalkyl, C.sub.3 to C.sub.7 -alkoxy carbonyl, aminocarbonyl, C.sub.2 to C.sub.7 -alkylaminocarbonyl, C.sub.3 to C.sub.13 -dialkylaminocarbonyl, cyano or C.sub.1 to C.sub.6 -alkylthio and R.sub.3 is a hydrogen atom or a C.sub.2 to C.sub.6 -alkyl radical substituted, if desired, one or more times by hydroxyl or is a tetrahydrofuranyl or tetrahydropyranyl radical, with the proviso that R.sub.2 cannot be an unsubstituted benzyl radical when R.sub.1 is a methyl radical, and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

    摘要翻译: 本发明提供通式如下的吡唑并[3,4-d] - 嘧啶:其中R 1为C 1至C 6 - 烷基,C 2至C 6链烯基,C 3至C 7环烷基 基团或芳基,R 2是C 2至C 6 - 烯基,C 3至C 7 - 环烷基或在烷基部分具有1至6个碳原子的芳烷基或杂烷基,如果需要, 卤素,C1至C6烷基,羟基,C1至C6烷氧基,C1至C3-卤代烷基,C3至C7-烷氧基羰基,氨基羰基,C2至C7-烷基氨基羰基,C3至C13-二烷基氨基羰基,氰基或C1至C6-烷硫基 并且R 3是氢原子或C 2至C 6烷基如果需要,被羟基取代一次或多次,或者是四氢呋喃基或四氢吡喃基,条件是当R 1是甲基时,R 2不能是未被取代的苄基 ,以及其与无机和有机酸的生理上可接受的盐。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。

    Pyridine compounds which have useful pharmaceutical activity
    10.
    发明授权
    Pyridine compounds which have useful pharmaceutical activity 失效
    具有有用药物活性的吡啶化合物

    公开(公告)号:US5399575A

    公开(公告)日:1995-03-21

    申请号:US66058

    申请日:1993-06-14

    摘要: Compounds of the formula I ##STR1## in which A signifies an alkylene radical with 1 to 3 carbon atoms or a group --CH.dbd.CH--, B an oxygen atom or a valency bond, m a whole number from 0 to 5, n the number 0 or 1, X a valency bond, an oxygen atom or a sulphur atom, Y a valency bond or a phenylene radical substituted, if desired, one or more times by C.sub.1 - to C.sub.6 -alkyl, C.sub.1 - to C.sub.6 -alkoxy, halogen, hydroxyl or aminocarbonyl, Z hydrogen, halogen, C.sub.1 - to C.sub.6 -alkyl or cyano and R a group CN, COOH, COOC.sub.1 - to C.sub.6 -alkyl, CONH-tetrazolyl, CON(OH)(C.sub.1 -C.sub.6 -alkyl) or 5-(1H)-tetrazolyl, as well as, for the case that Y represents a phenylene radical, also hydrogen, with the exception of the compound 4-[2-(4)-pyridinovinyl]-carboxymethoxybenzene, their physiologically compatible salts and processes for their preparation, as well as medicaments containing these compounds for the treatment of allergic diseases.

    摘要翻译: PCT No.PCT / EP91 / 02249 Sec。 371日期:1993年6月14日 102(e)日期1993年6月14日PCT 1991年11月28日PCT PCT。 第WO92 / 09598号公报 日期:1992年6月11日。式I的化合物(I)其中A表示具有1至3个碳原子的亚烷基或基团-CH = CH-,B为氧原子或价键, 0至5的整数,n为0或1,X为价键,氧原子或硫原子,Y为化合键或亚苯基,如果需要,可以被C 1 -C 6 - 烷基,C 1至C 6 - 烷氧基,卤素,羟基或氨基羰基,Z氢,卤素,C 1至C 6 - 烷基或氰基,R a基团CN,COOH,COOC 1 -C 6烷基,CONH-四唑基,CON )(C 1 -C 6 - 烷基)或5-(1H) - 四唑基,以及对于Y代表亚苯基的情况,也是氢,除了化合物4- [2-(4) - 吡啶基乙烯基 ] - 羧甲氧基苯,它们的生理上相容的盐及其制备方法,以及含有这些化合物用于治疗过敏性疾病的药物。