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59 条记录 (耗时 0.037 秒)

    Viral polymerase inhibitors
    51.
    发明授权
    Viral polymerase inhibitors 有权

    公开(公告)号：US06479508B1

    公开(公告)日：2002-11-12

    申请号：US09995099

    申请日：2001-11-27

    申请人： Pierre Louis Beaulieu ,  Gulrez Fazal ,  James Gillard ,  George Kukolj ,  Volkhard Austel

    发明人： Pierre Louis Beaulieu ,  Gulrez Fazal ,  James Gillard ,  George Kukolj ,  Volkhard Austel

    IPC分类号： A61K31437

    CPC分类号： C07D401/04 ,  C07D235/18 ,  C07D403/12 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D417/14 ,  C07D471/04 ,  Y10S514/894

    摘要： A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl , cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-3)alkyl, (C6-10)bicycloalkyl, adamantyl, phenyl, and pyridyl, all of which is optionally substituted with from 1 to 4 substituents; R3 is selected from H, (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-6)alkyl, (C6-10)aryl (C6-10)aryl(C1-6)alkyl, (C2-6)alkenyl, (C3-6)cycloalkyl(C2-6)alkenyl, (C6-10)aryl(C2-6)alkenyl, N{(C1-6) alkyl}2, NHCOO(C1-6)alkyl(C6-10)aryl, NHCO(C6-10)aryl, (C1-6)alkyl-5- or 10-atom heterocycle, having 1 to 4 heteroatoms selected from O, N and S, and 5- or 10-atom heterocycle having 1 to 4 heteroatoms selected from O, N and S; wherein said alkyl, cycloalkyl, aryl, alkenyl and heterocycle are all optionally substituted with from 1 to 4 substituents; n is zero or 1; or a detectable derivative or salt thereof. The compounds of the invention may be used as inhibitors of hepatitis C virus replication. The invention further provides a method for treating or preventing hepatitis C virus infection.

    Benzotriazolyl-4,5-dihydro-3(2H)-pyridazinones
    53.
    发明授权
    Benzotriazolyl-4,5-dihydro-3(2H)-pyridazinones 失效
    苯并三唑基-4,5-二氢-3（2H） - 哒嗪酮

    公开(公告)号：US4699909A

    公开(公告)日：1987-10-13

    申请号：US889814

    申请日：1986-07-24

    申请人： Norbert Hauel ,  Volkhard Austel ,  Joachim Heider ,  Manfred Reiffen ,  Willi Diederen ,  Walter Haarman

    发明人： Norbert Hauel ,  Volkhard Austel ,  Joachim Heider ,  Manfred Reiffen ,  Willi Diederen ,  Walter Haarman

    IPC分类号： C07D237/04 ,  C07D249/18 ,  C07D401/14 ,  C07D403/04 ,  C07D403/02 ,  A61K31/50

    CPC分类号： C07D401/14 ,  C07D237/04 ,  C07D249/18 ,  C07D403/04

    摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; alkyl of 1 to 7 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; monosubstituted alkyl of 1 to 3 carbon atoms, where the substituent is pyridyl, methypyridyl, phenyl, mono-, di- or trisubstituted phenyl, where the substituents on the phenyl ring, which may be identical to or different from each other, are selected from the group consisting of one amino, one dimethylamino, one to two hydroxyls, one to three methoxys and one to three halogens; .omega.-monosubstituted alkyl of 2 to 4 carbon atoms, where the substituent is hydroxyl or di(alkyl of 1 to 3 carbon atoms)amino; phenyl; monohalo-phenyl; unsubstituted or monosubstituted straight or branched alkanoyl of 1 to 6 carbon atoms, where the substituent is phenyl, methoxyphenyl or cycloalkyl of 3 to 7 carbon atoms; or unsubstituted or monosubstituted phenylsulfonyl, where the substituent is methyl or methoxy; andR.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics, hypotensives and antithrombotics.

    摘要翻译： 其中R 1是氢的式IMAMA的化合物; 1至7个碳原子的烷基; 3至7个碳原子的环烷基; 取代基为吡啶基，甲基吡啶基，苯基，单 - ，二 - 或三取代苯基的单取代烷基，其中苯环上的取代基可以相同或不同，选自 由一个氨基，一个二甲基氨基，一至两个羟基，一至三个甲氧基和一至三个卤素组成的组; 2至4个碳原子的ω-单取代的烷基，其中取代基是羟基或二（1至3个碳原子的烷基）氨基; 苯基; 单卤代苯基; 未取代的或单取代的1至6个碳原子的直链或支链烷酰基，其中取代基是苯基，甲氧基苯基或3-7个碳原子的环烷基; 或未取代或单取代的苯基磺酰基，其中取代基是甲基或甲氧基; 并且R 2是氢或1至3个碳原子的烷基; 和无毒的，药学上可接受的酸加成盐。 化合物及其盐可用作强心剂，低血糖剂和抗血栓药物。

    2-(Alkoxy-phenyl)-imidazo(4,5-b)pyridines and salts thereof
    55.
    发明授权
    2-(Alkoxy-phenyl)-imidazo(4,5-b)pyridines and salts thereof 失效
    2-（烷氧基 - 苯基） - 咪唑并（4,5-b）吡啶及其盐

    公开(公告)号：US4327100A

    公开(公告)日：1982-04-27

    申请号：US163970

    申请日：1980-06-30

    申请人： Volkhard Austel ,  Manfred Reiffen ,  Joachim Heider ,  Willi Diederen

    发明人： Volkhard Austel ,  Manfred Reiffen ,  Joachim Heider ,  Willi Diederen

    IPC分类号： A61K31/435 ,  A61P9/04 ,  A61P9/12 ,  C07D471/04 ,  A61K31/44

    CPC分类号： C07D471/04

    摘要： Compounds of the formula ##STR1## wherein R.sub.1 is alkoxy of 1 to 3 carbon atoms; andR.sub.2 is (aralkylsulfinyl of 7 to 9 carbon atoms)-(alkoxy of 2 to 3 carbon atoms); or (unsubstituted, mono-, di- or trisubstituted phenyl-sulfinyl)-(alkoxy of 2 to 3 carbon atoms), where the substituents are attached to the phenyl moiety and are nitro, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or halogen;their 3H-tautomers; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds are useful as hypertensives and cardiotonics.

    摘要翻译： 其中R 1为1至3个碳原子的烷氧基的式IMA化合物; R2为（碳原子数7〜9的芳烷基亚磺酰基） - （碳原子数2〜3的烷氧基）。 或（未取代的，单 - ，二 - 或三取代的苯基 - 亚磺酰基） - （2至3个碳原子的烷氧基），其中取代基连接到苯基部分并且是硝基，1至3个碳原子的烷基， 3个碳原子或卤素; 他们的3H-互变异构体; 和无毒的，药学上可接受的酸加成盐。 这些化合物可用作高血压和强心剂。

    8-Phenyl-purines and pharmaceutical compositions containing same
    56.
    发明授权
    8-Phenyl-purines and pharmaceutical compositions containing same 失效
    8-苯基嘌呤和含有它们的药物组合物

    公开(公告)号：US4299834A

    公开(公告)日：1981-11-10

    申请号：US166709

    申请日：1980-07-08

    申请人： Volkhard Austel ,  Eberhard Kutter ,  Joachim Heider ,  Willi Diederen

    发明人： Volkhard Austel ,  Eberhard Kutter ,  Joachim Heider ,  Willi Diederen

    IPC分类号： A61K31/52 ,  A61P9/04 ,  C07D239/48 ,  C07D473/00

    CPC分类号： C07D239/48 ,  C07D473/00

    摘要： This invention is directed to 8-phenyl-purines of general formula ##STR1## wherein R.sub.1 is a hydrogen or halogen atom; an alkoxy group optionally substituted by alkylmercapto, alkylsulfinyl or alkylsulfonyl group; or an alkylmercapto, alkylsulfinyl or alkylsulfonyl group, whereby each alkyl moiety may contain from 1 to 3 carbon atoms, andR.sub.2 is an alkoxy group with from 1 to 3 carbon atoms, and their physiologically compatible acid addition salts. The compounds exhibit valuable pharmacological properties, particularly positive inotropic activity.

    摘要翻译： 本发明涉及通式为“IMAGE”的8-苯基嘌呤，其中R 1是氢或卤素原子; 任选被烷基巯基，烷基亚磺酰基或烷基磺酰基取代的烷氧基; 或烷基巯基，烷基亚磺酰基或烷基磺酰基，其中每个烷基部分可以含有1至3个碳原子，并且R 2是具有1至3个碳原子的烷氧基，以及它们的生理上相容的酸加成盐。 该化合物显示出有价值的药理学性质，特别是正性肌力活性。