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    Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them
    9.
    发明授权
    Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them 失效
    2-（亚氨基甲基）氨基 - 苯基的衍生物，它们的制备，它们作为药物的用途以及含有它们的药物组合物

    公开(公告)号：US06809088B2

    公开(公告)日：2004-10-26

    申请号：US10191950

    申请日：2002-07-09

    申请人： Pierre Etienne Chabrier de Lassauniere ,  Serge Auvin ,  Dennis Bigg ,  Michel Auguet ,  Jeremiah Harnett

    发明人： Pierre Etienne Chabrier de Lassauniere ,  Serge Auvin ,  Dennis Bigg ,  Michel Auguet ,  Jeremiah Harnett

    IPC分类号： A61K3133

    CPC分类号： C07D333/34 ,  C07D333/38 ,  C07D409/12 ,  C07D417/12

    摘要： The invention relates to new derivatives of 2-(iminomethyl)amino-phenyl which are NO synthase inhibitors and can trap reactive oxygen species. These compounds can notably be used for the treatment of stroke, of neurodegenerative diseases and of ischemic or hemorragic cardiac or cerebral infarctions. These compounds include: N-{4-[({[4-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3-thiazol-2-yl]methyl}amino)methyl]phenyl}thiophene-2-carboximidamide; N-{3-[({[4-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3-thiazol-2-yl]methyl}amino)methyl]phenyl}thiophene-2-carboximidamide; N-(4-{[{[4-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3-thiazol-2-yl]methyl}(methyl)amino]methyl}phenyl)thiophene-2-carboximidamide; N-[3-({[3-(3,5-di-tert-butyl-4-hydroxyphenyl)propyl]amino}methyl)phenyl]thiophene-2-carboximidamide; N-(3-{[(3,5-di-tert-butyl-4-hydroxybenzyl)amino]methyl}phenyl)thiophene-2-carboximidamide; N-[3-({[2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethyl]amino}methyl)phenyl]thiophene-2-carboximidamide; N-[3-({[3-(4-hydroxy-3,5-diisopropylphenyl)propyl]amino}methyl)phenyl]thiophene-2-carboximidamide; N-(3-{[(4-hydroxy-3,5-diisopropylbenzyl)amino]methyl}phenyl) thiophene-2-carboximidamide; N-[3-({[2-(4-hydroxy-3,5-diisopropylphenyl)ethyl]amino}methyl)phenyl]thiophene-2-carboximidamide; N-2-(3,5-di-tert-butyl-4-hydroxybenzoyl)-N-1-(4-{[imino(thien-2-yl)methyl]amino}phenyl)-L-leucinamide; and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及作为NO合酶抑制剂的2-（亚氨基甲基）氨基 - 苯基的新衍生物，并可捕获活性氧。 这些化合物可以显着地用于治疗中风，神经变性疾病和缺血性或血液性心脏病或脑梗塞。这些化合物包括：N- {4 - [（{[4-（3,5-二叔丁基 -4-羟基苯基）-1,3-噻唑-2-基]甲基}氨基）甲基]苯基}噻吩-2-甲脒; N- {3 - [（{[4-（3,5-二 - 丁基-4-羟基苯基）-1,3-噻唑-2-基]甲基}氨基）甲基]苯基}噻吩-2-甲脒; N-（4 - {[{[4-（3,5-二叔丁基 （3-（3,5-二叔丁基-4-羟基苯基）-1,3-噻唑-2-基]甲基}（甲基）氨基]甲基}苯基）噻吩-2-甲脒; N-〔3 - 二 - 叔丁基-4-羟基苯基）丙基]氨基}甲基）苯基]噻吩-2-甲脒; N-（3 - {[（3,5-二叔丁基-4-羟基苄基）氨基]甲基} 苯基）噻吩-2-甲脒; N- [3 - （{[2-（3,5-二叔丁基-4-羟基苯基）乙基]氨基}甲基）苯基]噻吩-2-甲脒; N- [ 3 - （{[3-（4-羟基-3,5-二异丙基苯基）丙基]氨基}甲基）苯基]噻吩-2-甲脒; N-（3 - {[（4-羟基-3,5-二异丙基苄基） 氨基]甲基}苯基）硫代 2- [3 - （{[2-（4-羟基-3,5-二异丙基苯基）乙基]氨基}甲基）苯基]噻吩-2-亚甲代酰胺; N-2- 二 - 叔丁基-4-羟基苯甲酰基）-N-1-（4 - {[亚氨基（噻吩-2-基）甲基]氨基}苯基）-L-亮氨酰胺;及其药学上可接受的盐。