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65 条记录 (耗时 0.035 秒)

    2-alkylidene hydroxycoumaranone derivatives
    2.
    发明授权
    2-alkylidene hydroxycoumaranone derivatives 失效
    2-亚烷基羟基香豆酮衍生物

    公开(公告)号：US06307051B1

    公开(公告)日：2001-10-23

    申请号：US09497220

    申请日：2000-01-31

    申请人： Walter-Gunar Friebe ,  Bernhard Koenig ,  Hans-Willi Krell ,  Sabine Woelle

    发明人： Walter-Gunar Friebe ,  Bernhard Koenig ,  Hans-Willi Krell ,  Sabine Woelle

    IPC分类号： A61K31445

    CPC分类号： C07D405/12 ,  C07D307/83 ,  C07D405/14

    摘要： New compounds of formula I wherein: R and R1 are independently selected from hydrogen, (C1-C6)alkyl, styryl and (C3-C6)cycloalkyl or, taken together with the carbon to which they are linked, form a (C3-C6)cycloalkyl group; A is selected from the following groups: —CH2C≡CCH2—, or —(CH2)q—NH—(CH2)q—, wherein q is an integer from 2 to 3 B is selected from T is selected from —CH2—C≡CH, —C≡CH, —(CH2)p—R3, —CH═CH—R3, —CH2—NHCO—R3, —(CH2)p—O—R3, —CH(NH2)—CH2R3, in which p is 0 or an integer from 1 to 4, R3 is a carbocyclic or heterocyclic ring as medicaments having antitumor and/or antimetastatic activities.

    摘要翻译： 新的式I化合物，其中R和R 1独立地选自氢，（C 1 -C 6）烷基，苯乙烯基和（C 3 -C 6）环烷基，或与它们所连接的碳一起形成（C 3 -C 6） 环烷基; A选自以下基团：-CH 2 C = CCH 2 - 或 - （CH 2）q -NH-（CH 2）q - ，其中q为2至3B的整数，选自T选自-CH 2 - C = CH，-C = CH， - （CH 2）p -R 3，-CH = CH-R 3，-CH 2 -NHCO-R 3， - （CH 2）p O-R 3，-CH（NH 2）-CH 2 R 3，其中p 为0或1至4的整数，R 3为作为具有抗肿瘤和/或抗转移活性的药物的碳环或杂环。

    Pyrazolo(3,4-d)pyrimidine compounds, compositions and method of use
    8.
    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。

    N.sup.6 -disubstituted purine derivatives, and pharmaceutical compositions containing them, useful for treating allergic diseases, bronchospastic and bronchoconstrictory conditions
    9.
    发明授权
    N.sup.6 -disubstituted purine derivatives, and pharmaceutical compositions containing them, useful for treating allergic diseases, bronchospastic and bronchoconstrictory conditions 失效
    N6-二取代嘌呤衍生物和含有它们的药物组合物，其可用于治疗过敏性疾病，支气管痉挛和支气管收缩条件

    公开(公告)号：US4853386A

    公开(公告)日：1989-08-01

    申请号：US897109

    申请日：1986-08-15

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

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

    IPC分类号： A61K31/52 ,  A61P11/08 ,  A61P37/08 ,  C07D473/00 ,  C07D473/16 ,  C07D473/34 ,  C07D473/40

    CPC分类号： C07D473/00 ,  C07D473/16 ,  C07D473/34

    摘要： The present invention provides N.sup.6 -disubstituted purine derivatives of the general formula: ##STR1## wherein R.sub.1 and R.sub.4 are the same or different and each represents a hydrogen or halogen atom or an --NR.sub.6 R.sub.7 group, R.sub.2 and R.sub.3 are the same or different and each represents a C.sub.1 -C.sub.6 alkyl radical, a C.sub.2 -C.sub.6 alkenyl radical, a C.sub.3 -C.sub.7 cycloalkyl radical, a phenalkyl radical containing up to 4 carbon atoms in the alkyl moiety, which can be straight-chained or branched, the phenyl moiety of which can be substituted one or more times by halogen, hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio or trifluoromethyl; a furylmethyl or furylethyl radical, a thiophenemethyl or thiopheneethyl radical, a pyridylmethyl or pyridylethyl radical optionally substituted by a C.sub.1 -C.sub.4 alkyl radical, an indanyl radical or a tetrahydronaphthyl radical, R.sub.5 is a hydrogen atom, a tetrahydrofuranyl or tetrahydropyranyl radical or a C.sub.1 -C.sub.10 radical which is optionally substituted one or more times by hydroxyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.2 -C.sub.6 carboxyalkanoyloxy, C.sub.2 -C.sub.6 hydroxyalkoxy, C.sub.3 -c.sub.6 dihydroxyalkoxy, carboxyl, cyano or 1H-tetrazol-5-yl radical, R.sub.6 and R.sub.7 are the same or different and each represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical or together represent a C.sub.2 -C.sub.5 alkylene radical optionally interrupted by oxygen, sulphur or an NR.sub.8 group and R.sub.8 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical; as well as the pharmacologically acceptable salts thereof.

    摘要翻译： 本发明提供以下通式的N6-二取代的嘌呤衍生物：其中R 1和R 4相同或不同，并且各自表示氢或卤素原子或-NR 6 R 7基团，R 2和R 3相同或不同， 各自表示C1-C6烷基，C2-C6链烯基，C3-C7环烷基，在烷基部分含有至多4个碳原子的苯烷基，其可以是直链或支链的，苯基 其部分可以被卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6烷硫基或三氟甲基取代一次或多次; 呋喃基甲基或呋喃乙基，噻吩甲基或噻吩乙基，任选被C 1 -C 4烷基，茚满基或四氢萘基取代的吡啶基甲基或吡啶基，R5是氢原子，四氢呋喃基或四氢吡喃基或C1- C 1 -C 6烷氧基，C 1 -C 6烷氧基羰基，C 2 -C 6羧基烷酰氧基，C 2 -C 6羟基烷氧基，C 3 -C 6二羟基烷氧基，羧基，氰基或1H-四唑-5-基 ，R6和R7相同或不同，各自表示氢原子或C1-C6烷基，或一起代表任选被氧，硫或NR8基中断的C2-C5亚烷基，R8是氢原子或C1 -C6烷基; 以及其药理学上可接受的盐。