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65 条记录 (耗时 0.025 秒)

    Heterocyclic oxypropanolamine compounds and pharmaceutical compositions
    6.
    发明授权
    Heterocyclic oxypropanolamine compounds and pharmaceutical compositions 失效

    公开(公告)号：US4346093A

    公开(公告)日：1982-08-24

    申请号：US117190

    申请日：1980-01-31

    申请人： Walter-Gunar Friebe ,  Helmut Michel ,  Carl H. Ross ,  Fritz Wiedemann ,  Wolfgang Bartsch ,  Karl Dietmann

    发明人： Walter-Gunar Friebe ,  Helmut Michel ,  Carl H. Ross ,  Fritz Wiedemann ,  Wolfgang Bartsch ,  Karl Dietmann

    IPC分类号： C07D251/72 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61P9/00 ,  A61P9/08 ,  A61P9/12 ,  A61P25/02 ,  C07D209/04 ,  C07D209/08 ,  C07D209/42 ,  C07D209/43 ,  C07D231/56 ,  C07D233/00 ,  C07D235/02 ,  C07D235/06 ,  C07D235/26 ,  C07D235/28 ,  C07D249/08 ,  C07D249/18 ,  C07D401/12 ,  C07D405/12 ,  A61K31/41

    CPC分类号： C07D209/08 ,  C07D209/42 ,  C07D235/26 ,  C07D249/18 ,  Y10S514/929

    摘要： The present invention provides heterocyclic oxypropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl, aralkyl or lower alkanoyl radical, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen atoms or lower alkyl, hydroxyalkyl, alkoxycarbonyl or alkanoyloxyalkyl radicals or together represent an alkylene radical, R.sub.4 is a hydrogen atom or a lower alkanoyl radical or an aroyl radical, R.sub.5 is a hydrogen atom or a lower alkyl radical or an aralkyl radical, R.sub.6 is a hydrogen atom or a lower alkyl radical, R.sub.7 is a hydrogen atom, a hydroxyl group or a lower alkyl radical, Z is a valency bond, a methylene radical or an oxygen or sulphur atom, Ar is a carbocyclic aryl radical or a pyridyl radical, R.sub.8, R.sub.9 and R.sub.10, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, lower alkyl radicals, lower alkenyl radicals, lower alkoxy radicals, aralkoxy radicals, allyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or lower alkanoylamino radicals or R.sub.8 and R.sub.9 together represent a lower alkylenedioxy radical or R.sub.7 and R.sub.8 together represent a --CH.sub.2 --O-- radical and A is --X.sub.1 --Y.sub.1, in which X.sub.1 is a methylene or --NR.sub.11 -- radical, R.sub.11 being a hydrogen atom or a lower alkyl radical, and Y.sub.1 is a methylene radical or .dbd.C.dbd.Q, Q being an oxygen or sulphur atom; or A is --X.sub.2 .dbd.Y.sub.2 --, in which X.sub.2 and Y.sub.2, which can be the same or different and signify nitrogen atoms or .dbd.C(R.sub.12)-- groups, R.sub.12 being a hydrogen atom or a lower alkyl or an alkoxycarbonyl radical, and when --X.sub.2 .dbd.Y.sub.2 -- represents a --CH.dbd.N-- group and R.sub.1 is an alkyl or aralkyl radical, because of the ability of indazole to tautomerise, this can also be localized on the nitrogen atom represented by Y.sub.2, with the proviso that Y.sub.1 or Y.sub.2 is joined to .dbd.N--R.sub.1 in general formula (I), and, when Q is an oxygen atom or --X.sub.2 .dbd.Y.sub.2 -- represents --CR.sub.12 .dbd.CR.sub.12 -- and Z is a valency bond or when --X.sub.1 --Y.sub.1 -- represents ##STR2## and Z is an oxygen atom or a valency bond, either the two symbols R.sub.2 and R.sub.3 do not simultaneously represent hydrogen atoms or R.sub.7 and R.sub.8 together must form a --CH.sub.2 --O-- radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.Furthermore, the present invention is concerned with the use of these compounds for the treatment of cardiac and circulatory diseases.

    Anti-allergy bicyclic phenol ethers
    7.
    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

    申请人： Walter-Gunar Friebe ,  Wolfgang Kampe ,  Androniki Roesch nee Apostolides ,  Wolfgang Schaumann

    发明人： Walter-Gunar Friebe ,  Wolfgang Kampe ,  Androniki Roesch nee Apostolides ,  Wolfgang Schaumann

    IPC分类号： A61K31/443 ,  A61K31/445 ,  A61P37/08 ,  C07D307/83 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

    CPC分类号： C07D401/12 ,  C07D307/83 ,  C07D405/12

    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
    10.
    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

    申请人： Walter-Gunar Friebe ,  Wolfgang Kampe ,  Otto-Henning Wilhelms

    发明人： Walter-Gunar Friebe ,  Wolfgang Kampe ,  Otto-Henning Wilhelms

    IPC分类号： A61K31/505 ,  A61K31/519 ,  A61P11/08 ,  A61P11/16 ,  A61P29/00 ,  A61P37/08 ,  C07D487/04

    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。