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    • 5. 发明授权
    • Azabicycloheptanes
    • 氮杂双环庚烷
    • US4138403A
    • 1979-02-06
    • US708343
    • 1976-07-26
    • Thomas T. HowarthAllan G. BrownDavid F. CorbettRoger J. Ponsford
    • Thomas T. HowarthAllan G. BrownDavid F. CorbettRoger J. Ponsford
    • A61K31/42A61P31/04C07D205/08C07D205/09C07D263/16C07D503/00C07F7/18C07D498/04
    • C07D263/16C07D205/08C07D205/09C07D503/00C07F7/1852
    • Compounds of the formula ##STR1## and salts and esters thereof wherein R.sub.1 is hydrogen, alkyl of 1 to 4 carbon atoms, phenyl, alkenyl of 2 to 4 carbon atoms, alkynyl of 2 to 4 carbon atoms, acyl of 1 to 4 carbon atoms, a carboxylic acid group or ester thereof of 1 to 7 carbon atoms, or alkyl of 1 to 4 carbon atoms substituted by 1 or 2 halogen atoms, hydroxyl, substituted hydroxyl, amino, protected amino, substituted thio of 1 to 7 carbon atoms, substituted sulphinyl of 1 to 7 carbon atoms, substituted sulphonyl of 1 to 7 carbon atoms, or by a carboxylic acid group or ester thereof of 1 to 7 carbon atoms;R.sub.2 is hydrogen or alkyl of 1 to 4 carbon atoms, or is joined to R.sub.1 to form a cycloalkyl group of 3 to 6 carbon atoms;R.sub.3 is hydrogen, chlorine or bromine; andR.sub.4 is hydrogen, halogen, azido or amino; provided that when R.sub.4 is azido, R.sub.3 is hydrogen and R.sub.1 is methyl,R.sub.2 is not methyl, and that when R.sub.2 R.sub.3 and R.sub.4 are hydrogen andR.sub.1 is hydroxyethyl or an acyl derivative thereof, the compound does not have the (2R, 3S, 5R) stereochemistry; inhibit certain .beta.-lactamate enzymes and are useful in antiseptic and disinfectant solutions.
    • 式(I)的化合物及其盐和酯,其中R 1是氢,1至4个碳原子的烷基,苯基,2至4个碳原子的烯基,2至4个碳原子的炔基,1至 4个碳原子,1至7个碳原子的羧酸基团或其酯,或被1或2个卤素原子取代的1至4个碳原子的烷基,羟基,取代的羟基,氨基,保护的氨基,取代的硫代1至7个 碳原子,1至7个碳原子的取代亚磺酰基,1至7个碳原子的取代磺酰基,或其1至7个碳原子的羧酸基或其酯; R2是氢或1〜4个碳原子的烷基,或者与R1连接,形成3〜6个碳原子的环烷基; R3是氢,氯或溴; R4是氢,卤素,叠氮基或氨基; 条件是当R 4是叠氮基时,R 3是氢,R 1是甲基,R 2不是甲基,当R 2 + L,R 3和R 4是氢并且R 1是羟乙基或其酰基衍生物时,该化合物不具有 ,3S,5R)立体化学; 抑制某些β-乳酸酶,并且可用于消毒和消毒溶液。