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18 条记录 (耗时 0.019 秒)

    Heterocyclic compounds
    11.
    发明授权
    Heterocyclic compounds 失效

    公开(公告)号：US5246932A

    公开(公告)日：1993-09-21

    申请号：US887211

    申请日：1992-05-21

    申请人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    发明人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    IPC分类号： A61K31/53 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07D487/04 ,  C07D519/00

    CPC分类号： C07D519/00

    摘要： A compound of the formula I ##STR1## wherein: A.sup.1 and A.sup.2 are each independently N or CT in which T is hydrogen or (1-4C)alkyl;R.sup.1 and R.sup.2 are each independently hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;X.sup.1 and X.sup.2 are each independently O, S or NH; andL is a (3-7C)cycloalkylene group or a (1-8C)alkylene chain optionally interrupted or extended by a group selected from phenylene, phenyleneoxy or oxyphenyleneoxy, the phenylene portion of said group being unsubstituted or substituted by one of halogen, hydroxy and (1-4C)alkoxy, provided that all heteroatoms in the group X.sup.1 --L--X.sup.2 are separated from one another by at least two carbon atoms; or a pharmaceutically acceptable salt thereof, processes for preparing the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

    2-furyl-triazalo [1,5-a]-[1,3,5]triazines and pyrazolo [2,3-a][1,3,5]triazines
    15.
    发明授权
    2-furyl-triazalo [1,5-a]-[1,3,5]triazines and pyrazolo [2,3-a][1,3,5]triazines 失效
    2-呋喃基 - 三氮杂[1,5-a] - [1,3,5]三嗪和吡唑并[2,3-a] [1,3,5]三嗪

    公开(公告)号：US5380714A

    公开(公告)日：1995-01-10

    申请号：US979549

    申请日：1992-11-20

    申请人： Geraint Jones ,  Roger James ,  Rodney B. Hargreaves

    发明人： Geraint Jones ,  Roger James ,  Rodney B. Hargreaves

    IPC分类号： A61K31/53 ,  A61P9/00 ,  A61P9/10 ,  A61P25/04 ,  A61P25/06 ,  C07D487/04 ,  A61K31/70 ,  C07H17/00

    CPC分类号： C07D487/04

    摘要： Compounds of the formula I: ##STR1## wherein: X is O, S or NH;n is O or an integer of from 1 to 3;R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 is CH.sub.2 R.sup.3, NHR.sup.4, SO.sub.2 NR.sup.5 YNR.sup.6 R.sup.7 or R.sup.8, in which R.sup.3 is hydroxy, (1-4C)alkoxy or (1-4C)alkylsulphonyl; R.sup.4 is (1-4C)alkylsulphonyl, (1-4C)haloalkylsulphonyl, formyl, carbamoyl or 2,6-dichloro-4-(2-(1,1-dimethylethyl)amino-1-hydroxyethyl)phenyl; R.sup.5 is hydrogen or (1-4C)alkyl; Y is CO or (1-6C)alkylene; R.sup.6 and R.sup.7 are independently (1-4C)alkyl, or R.sup.6 is hydrogen and R.sup.7 is (1-4C)alkyl, (1-4C)haloalkyl, phenyl(1-4C)alkyl or, when Y is (1-6C)alkylene, is (1-4C)alkylaminocarbonyl or (5-6C)cycloalkylaminocarbonyl; and R.sup.8 is a sugar residue of formula II in which R.sup.9 represents hydrogen, methyl or hydroxymethyl and m is 2 or 3;A is N or CT in which T is hydrogen or (1-4C)alkyl; or a pharmaceutically acceptable salt thereof, processes for their manufacture and pharmaceutical compounds containing them. The compounds are useful as adenosine antagonists.

    摘要翻译： 式I的化合物：其中：X是O，S或NH; n为0或1〜3的整数; R1是氢，（1-6C）烷基或（1-4C）烷酰基; R2是CH2R3，NHR4，SO2NR5YNR6R7或R8，其中R3是羟基，（1-4C）烷氧基或（1-4C）烷基磺酰基; R4是（1-4C）烷基磺酰基，（1-4C）卤代烷基磺酰基，甲酰基，氨基甲酰基或2,6-二氯-4-（2-（1,1-二甲基乙基）氨基-1-羟乙基）苯基; R5是氢或（1-4C）烷基; Y是CO或（1-6C）亚烷基; R6和R7独立地是（1-4C）烷基，或R6是氢，R7是（1-4C）烷基，（1-4C）卤代烷基，苯基（1-4C）烷基或当Y是（1-6C） （1-4C）烷基氨基羰基或（5-6C）环烷基氨基羰基; R8为式Ⅱ的糖残基，其中R9表示氢，甲基或羟甲基，m为2或3; A是N或CT，其中T是氢或（1-4C）烷基; 或其药学上可接受的盐，其制备方法和含有它们的药物化合物。 这些化合物可用作腺苷拮抗剂。

    1-Phenyl-2-aminoethanol derivatives
    17.
    发明授权
    1-Phenyl-2-aminoethanol derivatives 失效
    1-苯基-2-氨基乙醇衍生物

    公开(公告)号：US4323575A

    公开(公告)日：1982-04-06

    申请号：US147074

    申请日：1980-05-06

    申请人： Geraint Jones

    发明人： Geraint Jones

    IPC分类号： H01J31/20 ,  A61K31/16 ,  A61K31/165 ,  A61K31/195 ,  A61K31/22 ,  A61K31/325 ,  A61K31/40 ,  A61K31/445 ,  A61P29/00 ,  C07C237/10 ,  C07C237/20 ,  C07C237/22 ,  C07D205/04 ,  C07D207/16 ,  C07D211/60 ,  H01J29/02 ,  H01J29/07 ,  H01J29/86 ,  H01J31/12 ,  A61K31/395 ,  C07D211/62

    CPC分类号： C07D205/04 ,  C07D207/16 ,  C07D211/60

    摘要： The invention concerns compounds of the formula:- R.sup.1.CH(OH).CH.sub.2 NH.CR.sup.2 R.sup.3.A.sup.1. NH.CO.CHR.sup.4.A.sup.2.NR.sup.5. Q I wherein R.sup.1 is 3,4-bis[(3-8C)alkanoyloxy]-phenyl, 3,5- bis [(3-8C)alkanoyloxy]phenyl, 3-[(3-8C)alkanoyloxy]methyl-4-[(3-8C)alkanoyloxy]phenyl, 4-[(3-8C)alkanoyloxy]phenyl, 2-chlorophenyl or 3,5-dichloro-4-aminophenyl; R.sup.2 and R.sup.3 are independently hydrogen or (1-4C) alkyl; A.sup.1 is (1-4C) alklylene; A.sup.2 is a direct bond or (1-4C) alkylene; R.sup.4 is hydrogen, (1-6C)alkyl, phenyl-(1-4C)alkyl or halogenophenyl-(1-4 C)alkyl; and R.sup.5 is (1-6C)alkyl; or R.sup.4 and R.sup.5 together form (2-5C) alkylene; and Q is (3-12C) alkanoyl, [(3-6C)alkoxy]carbonyl, phenylacetyl, phenoxyacetyl, benzoyl or benzyloxycarbonyl, the phenyl rings of which may optionally bear a substitutent selected from halogeno, (1-4C)alkyl, (1-4C)alkoxy and trifuloromethyl; and the pharmaceutically acceptable acid-addition salts thereof; processes for their manufacture; and pharmaceutical compositions thereof.The compounds of formula I are topical anti-inflammatory agents. A representative compound is 1-[3,4-bis (pivaloyloxy)phenyl]-2-{2-[(N-phenylacetyl-proyly)amino]-1,1-dimethyl-ethylamino}ethanol.

    摘要翻译： 本发明涉及下式的化合物：-R1.CH（OH）.CH2NH.CR2R3.A1。 NH.CO.CHR4.A2.NR5。 QI其中R1是3,4-双[（3-8C）烷酰氧基] - 苯基，3,5-双[（3-8C）烷酰氧基]苯基，3 - [（3-8C）烷酰氧基]甲基-4- [ （3-8C）烷酰氧基]苯基，4 - [（3-8C）烷酰氧基]苯基，2-氯苯基或3,5-二氯-4-氨基苯基; R2和R3独立地是氢或（1-4C）烷基; A1为（1-4C）亚烷基; A2是直接键或（1-4C）亚烷基; R4是氢，（1-6C）烷基，苯基 - （1-4C）烷基或卤代苯基 - （1-4C）烷基; R5为（1-6C）烷基; 或R 4和R 5一起形成（2-5C）亚烷基; 和（3-12C）烷酰基，[（3-6C）烷氧基]羰基，苯乙酰基，苯氧基乙酰基，苯甲酰基或苄氧基羰基，其苯环可以任选地具有选自卤代，（1-4C）烷基，（1-4C） 1-4C）烷氧基和三氟甲基; 及其药学上可接受的酸加成盐; 制造过程; 及其药物组合物。 式I的化合物是局部抗炎剂。 代表性化合物是1- [3,4-双（新戊酰氧基）苯基] -2- {2 - [（N-苯基乙酰基）氨基] -1,1-二甲基 - 乙基氨基}乙醇。