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    Antivirally active heterocyclic azahexane derivatives
    7.
    发明授权
    Antivirally active heterocyclic azahexane derivatives 失效
    抗病毒活性杂环氮杂己烷衍生物

    公开(公告)号：US6110946A

    公开(公告)日：2000-08-29

    申请号：US108481

    申请日：1998-07-01

    Applicant: Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    Inventor： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    IPC: C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D213/42 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20 ,  A01K31/44 ,  C07C241/00 ,  C07C261/00 ,  C07D277/04 ,  C07D401/00

    CPC classification number: C07D213/42 ,  C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20

    Abstract: There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

    Abstract translation: 描述式I *的化合物，其中R 1是低级烷氧基羰基，R 2是仲或叔低级烷基或低级烷硫基 - 低级烷基，R 3是未被取代或被一个或多个低级烷氧基取代的苯基或C 4 -C 8环烷基， R4是通过环碳原子连接的不饱和杂环基在4-位上被取代的苯基或环己基，具有5-8个环原子，含有1-4个选自氮，氧，硫，亚硫酰基的杂原子 （-SO-）和磺酰基（-SO 2 - ），并且未被取代或被低级烷基或苯基 - 低级烷基取代，R 5与R 2独立地具有R2中所提及的含义之一，R 6独立地为R 1， 低级烷氧基羰基或其盐，条件是存在至少一个成盐基团。 这些化合物是逆转录病毒天冬氨酸蛋白酶的抑制剂，可以用于例如艾滋病的治疗。 它们具有出色的药效学性质。

    Method of using 1-arylheteroarylalkyl substituted-1H-1,2,4-triazole compounds for treatment of a glaucoma disorder
    8.
    发明授权
    Method of using 1-arylheteroarylalkyl substituted-1H-1,2,4-triazole compounds for treatment of a glaucoma disorder 失效
    使用1-芳基杂芳基烷基取代的1H-1,2,4-三唑化合物治疗青光眼病症的方法

    公开(公告)号：US5563139A

    公开(公告)日：1996-10-08

    申请号：US76019

    申请日：1993-06-14

    Applicant: David B. Reitz

    Inventor： David B. Reitz

    IPC: A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D521/00 ,  A61K31/535 ,  C07D401/04 ,  C07D413/04 ,  A01K31/44

    CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14

    Abstract: Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein A is selected from ##STR2## wherein m is one; wherein R.sup.1 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R.sup.2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neo-pentyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl, 1,1-dimethoxypropyl, 1,1-dimethoxypentyl, halo, difluoromethyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluoro-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and butylthio; wherein each of R.sup.3, R.sup.4, R.sup.6 through R.sup.11 is hydrido and R.sup.5 is selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR3## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl.

    Abstract translation: 特别感兴趣的化合物是下式的血管紧张素II拮抗剂：其中A选自 其中m为1; 其中R 1选自乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，4-甲基丁基，正戊基，新戊基，苄基，环己基，环己基甲基，2-丁烯基， ，2-丁炔基，3-丁炔基和2-羟基丁基; 其中R2选自乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，4-甲基丁基，叔丁基，正戊基，新戊基，1-氧代乙基，1-氧代丙基，1-氧代丁基 ，1-氧代戊基，1,1-二甲氧基丙基，1,1-二甲氧基戊基，卤代，二氟甲基，1-氧代-2-苯基乙基，1-氧代-2-环己基乙基，1,1-二氟-2-苯基乙基，1,1 2-氟-2-环己基乙基，2-环己基乙基，1,1-二氟-3-环己基丙基，1,1-二甲氧基丁基，1,1-二氟乙基，1,1-二氟丙基，1,1-二氟丁基，1,1-二氟戊基 苄基，2-苯基乙基，1,1-二氟-3-苯基丙基，环己基甲基，环己酰基，1-丁烯基，2-丁烯基，3-丁烯基，1-丁炔基，2-丁炔基，3-丁炔基，丙硫基和丁硫基; 其中R 3，R 4，R 6至R 11各自为氢，R 5选自COOH，SH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，OH，NR 42和NHNR 43; + RE，其中R 42和R 43各自独立地选自氯， 氰基，硝基，三氟甲基，甲氧基羰基和三氟甲基磺酰基。

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