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59 条记录 (耗时 0.032 秒)

    Benzazepine derivatives
    33.
    发明授权
    Benzazepine derivatives 失效
    苯扎西平衍生物

    公开(公告)号：US4604389A

    公开(公告)日：1986-08-05

    申请号：US732204

    申请日：1985-05-08

    申请人： Manfred Reiffen ,  Klaus Noll ,  Joachim Heider ,  Volkhard Austel ,  Norbert Hauel ,  Walter Kobinger ,  Christian Lillie

    发明人： Manfred Reiffen ,  Klaus Noll ,  Joachim Heider ,  Volkhard Austel ,  Norbert Hauel ,  Walter Kobinger ,  Christian Lillie

    IPC分类号： A61K31/55 ,  A61P9/06 ,  C07C59/64 ,  C07D223/16 ,  C07D233/16 ,  C07D243/04 ,  C07D405/12 ,  C07D491/04 ,  C07D491/056 ,  C07D521/00

    CPC分类号： C07D223/16 ,  C07C59/64 ,  C07D243/04 ,  C07D405/12 ,  C07D491/04

    摘要： This invention relates to benzazepine derivatives of formula I ##STR1## wherein A is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;R.sub.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.3 alkyl, amino, C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3 dialkylamino, acylamino, hydroxy, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy;R.sub.2 is hydrogen, chlorine, bromine, hydroxy, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy or, together with R.sub.1, can be C.sub.1 -C.sub.3 alkylenedioxy;R.sub.3 is hydrogen, chlorine, bromine or C.sub.1 -C.sub.3 alkoxy;R.sub.4 is hydrogen, benzyl, C.sub.1 -C.sub.3 alkyl or C.sub.3 -C.sub.5 alkenyl;R.sub.5 is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy;R.sub.6 is hydrogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy or, together with R.sub.5, can be a C.sub.1 -C.sub.2 alkylenedioxy;X is an imino, optionally substituted by a benzyl or C.sub.1 -C.sub.3 alkyl, or is oxygen, sulphur, sulphinyl or sulphonyl;Y is an imino, optionally substituted by a benzyl or C.sub.1 -C.sub.3 alkyl, or is methylene or carbonyl;m and n are each independently 2, 3 or 4; and nontoxic, pharmaceutically acceptable addition salts thereof. These compounds have valuable pharmacological properties, particularly the effect of lowering heart rate and reducing the O.sub.2 requirement of the heart.

    摘要翻译： 本发明涉及式I的苯并氮杂衍生物，其中A是-CH 2 CH 2 - 或-CH = CH-; R1是氢，氯，溴，C1-C3烷基，氨基，C1-C3烷基氨基，C1-C3二烷基氨基，酰氨基，羟基，C1-C3烷氧基或苯基C1-C3烷氧基; R2是氢，氯，溴，羟基，C1-C3烷基，C1-C3烷氧基或苯基C1-C3烷氧基，或与R1一起可以是C1-C3亚烷基二氧基; R3是氢，氯，溴或C1-C3烷氧基; R4是氢，苄基，C1-C3烷基或C3-C5烯基; R5是氢，卤素，C1-C3烷基或C1-C3烷氧基; R 6是氢，C 1 -C 3烷基或C 1 -C 3烷氧基，或与R 5一起可以是C 1 -C 2亚烷基二氧基; X是任选被苄基或C 1 -C 3烷基取代的亚氨基，或是氧，硫，亚磺酰基或磺酰基; Y是任选被苄基或C 1 -C 3烷基取代的亚氨基，或亚甲基或羰基; m和n各自独立地为2,3或4; 和无毒的药学上可接受的加成盐。 这些化合物具有有价值的药理学特性，特别是降低心率并降低心脏O2需求的作用。

    Aminotetralin derivatives
    34.
    发明授权
    Aminotetralin derivatives 失效
    氨基四氢萘衍生物

    公开(公告)号：US4584293A

    公开(公告)日：1986-04-22

    申请号：US732199

    申请日：1985-05-08

    申请人： Manfred Reiffen ,  Joachim Heider ,  Volkhard Austel ,  Norbert Hauel ,  Walter Kobinger ,  Christian Lillie

    发明人： Manfred Reiffen ,  Joachim Heider ,  Volkhard Austel ,  Norbert Hauel ,  Walter Kobinger ,  Christian Lillie

    IPC分类号： A61K31/55 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C45/00 ,  C07C45/51 ,  C07C49/755 ,  C07C57/58 ,  C07C59/64 ,  C07C205/56 ,  C07D223/16 ,  C07D243/04 ,  C07D491/056 ,  C07D521/00

    CPC分类号： C07D223/16 ,  C07C205/56 ,  C07C45/00 ,  C07C45/513 ,  C07C49/755 ,  C07C57/58 ,  C07C59/64 ,  C07D231/12 ,  C07D233/56 ,  C07D243/04 ,  C07D249/08

    摘要： This invention related to new aminotetralin derivatives of formula I ##STR1## wherein ##STR2## B is methylene or, when A is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --NH--CO-- or --CH.sub.2 --CO--, B can also be carbonyl or thiocarbonyl;E is a C.sub.2 -C.sub.4 straight-chain alkylene, optionally substituted by a C.sub.1 -C.sub.3 alkyl, or is 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene;R.sub.1 is hydrogen, fluorine, chlorine, bromine, trifluoromethyl, nitro, amino, C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3 dialkylamino, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylthio, hydroxy, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy;R.sub.2 is hydrogen, chlorine, bromine, hydroxy, C.sub.1 -C.sub.3 alkoxy phenyl C.sub.1 -C.sub.3 alkoxy, or C.sub.1 -C.sub.3 alkyl or, together with R.sub.1, can be a C.sub.1 -C.sub.2 alkylenedioxy;R.sub.3 and R.sub.4 are each independently selected from hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.3 alkoxy, nitro, amino, C.sub.1 -C.sub.3 alkylamino, or C.sub.1 -C.sub.3 dialkylamino, or together can be methylenedioxy; andR.sub.5 is hydrogen, C.sub.3 -C.sub.5 alkenyl, C.sub.1 -C.sub.3 alkyl, or phenyl C.sub.1 -C.sub.3 alkyl, and nontoxic, pharmaceutically acceptable addition salts thereof which have valuable pharmacological properties, particularly a long-lasting heart rate lowering effect and the effect of reducing the O.sub.2 requirement of the heart.

    摘要翻译： 本发明涉及新的式I的氨基蝶呤衍生物，其中B是亚甲基，或当A是-CH 2 -CH 2 - 时，-CH = CH-，-NH-CO-或-CH 2 -CO-，B也可以是羰基或硫代羰基; E是任选被C 1 -C 3烷基取代的C 2 -C 4直链亚烷基，或是2-羟基 - 正丙烯，2-羟基 - 正丁烯或3-羟基 - 正丁烯; R1是氢，氟，氯，溴，三氟甲基，硝基，氨基，C1-C3烷基氨基，C1-C3二烷基氨基，C1-C3烷基，C1-C3烷硫基，羟基，C1-C3烷氧基或苯基C1-C3烷氧基; R2是氢，氯，溴，羟基，C1-C3烷氧基苯基C1-C3烷氧基或C1-C3烷基，或与R1一起可以是C1-C2亚烷基二氧基; R 3和R 4各自独立地选自氢，氟，氯，溴，C 1 -C 3烷基，羟基，C 1 -C 3烷氧基，硝基，氨基，C 1 -C 3烷基氨基或C 1 -C 3二烷基氨基，或一起可以是亚甲二氧基; 并且R 5是氢，C 3 -C 5烯基，C 1 -C 3烷基或苯基C 1 -C 3烷基，以及其无毒的药学上可接受的加成盐，其具有有价值的药理学性质，特别是持久的心率降低效果和降低 心脏的O2要求。

    Viral polymerase inhibitors
    37.
    发明授权
    Viral polymerase inhibitors 有权

    公开(公告)号：US07439258B2

    公开(公告)日：2008-10-21

    申请号：US10851710

    申请日：2004-05-21

    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： A61K31/4439 ,  C07D401/04

    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
    40.
    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：US4616018A

    公开(公告)日：1986-10-07

    申请号：US749580

    申请日：1985-06-27

    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： A61K31/50 ,  A61K31/501 ,  A61P7/02 ,  A61P9/12 ,  C07D237/04 ,  C07D249/18 ,  C07D401/14 ,  C07D403/04 ,  C07D403/02

    CPC分类号： C07D401/14 ,  C07D237/04 ,  C07D249/18 ,  C07D403/04 ,  Y10S514/822

    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, methylpyridyl, 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; and,R.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; 其中取代基是吡啶基，甲基吡啶基，苯基，单 - ，二 - 或三取代的苯基，其中可以相同或不同的苯环上的取代基选自 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; R2为氢或1〜3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。