N-(iminomethyl)amines derivatives, their preparation, their use as medicines and compositions containing them
    4.
    发明授权
    N-(iminomethyl)amines derivatives, their preparation, their use as medicines and compositions containing them 失效
    N-(亚氨基甲基)胺衍生物,它们的制备,它们作为药物和含有它们的组合物的用途

    公开(公告)号:US06482822B1

    公开(公告)日:2002-11-19

    申请号:US09787466

    申请日:2001-03-16

    IPC分类号: A61K315415

    CPC分类号: C07D333/38

    摘要: The invention concerns novel N-(iminomethyl)amine derivatives comprising in their skeleton the aminophenylamine, oxodiphenylamine, carbazole, phenazine, phenoxazine or oxodiphenyl motif, their use as medicines and pharmaceutical compositions containing them. The invention concerns in particular the following compounds: -4-{[2-thienyl(imino)methyl]amino}-N-[2-(phenylamino)phenyl]-benzenebutanamide; -4-{[2-thienyl(imino)methyl]amino}-N-[4-(phenylamino)phenyl]-benzenebutanamide; -N-′[4-(10H-phenothiazin-2-yloxy)phenyl]-2-thiophenecarboximidamide; -4-(4-{[amino(2-thienyl)methylidene]amino}phenyl)-N-(10H-phenothiazin-3-ylH)butanamide; -3-[(3-{[amino(2-thienyl)methylidene]amino}-benzyl)amino]-N-(4-anilinophenyl)propanamide; -N′-(4-{2-[(10H-phenothiazin-3-ylmethyl)amino]ethyl}phenyl-2-thiophene carboximidamide.

    摘要翻译: 本发明涉及在其骨架中包含氨基苯基胺,氧代二苯胺,咔唑,吩嗪,吩恶嗪或氧代二苯基基团的新型N-(亚氨基甲基)胺衍生物,它们作为药物和含有它们的药物组合物的用途。 本发明特别涉及以下化合物:-4 - {[2-噻吩基(亚氨基)甲基]氨基} -N- [2-(苯基氨基)苯基] - 苯丁酰胺; -4 - {[2-噻吩基(亚氨基)甲基]氨基} -N- [4-(苯基氨基)苯基] - 苯丁酰胺; -N - [4-(10H-吩噻嗪-2-基氧基)苯基] -2-噻吩甲酰胺; -4-(4 - {[氨基(2-噻吩基)亚甲基]氨基}苯基)-N-(10H-吩噻嗪-3-基)丁酰胺; -3 - [(3 - {[氨基(2-噻吩基)亚甲基]氨基} - 苄基)氨基] -N-(4-苯胺基苯基)丙酰胺; -N' - (4- {2 - [(10H-吩噻嗪-3-基甲基)氨基]乙基}苯基-2-噻吩甲脒。

    Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them
    6.
    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

    IPC分类号: A61K3133

    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。

    Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them
    7.
    发明授权
    Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them 有权
    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:US07553976B2

    公开(公告)日:2009-06-30

    申请号:US12009742

    申请日:2008-01-22

    IPC分类号: C07D277/28

    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 of 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-2carboximidamide; N-(4-{[{[4-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3-thiazol-2-yl]methyl}(methyl)amino]methyl}phenyl)thiophene-2carboximidamide; N-[3-(}[3-(3,5-di-tert-butyl-4-hydroxyphenyl)propyl]amino}methyl) phenyl]thiophene-2carboximidamide; 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]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-(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,神经变性疾病和脑梗死的缺血性或血液性脑损伤。 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-甲酰胺; N-(4 - {[{[4-(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卡泊酰胺; N- [3 - ({[3-(3,5-二叔丁基-4-羟基苯基)丙基]氨基}甲基)苯基]噻吩-2-甲酰胺; 噻唑-2-甲酰胺; 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]苯基)噻吩-2-甲脒; N- [3 - ({[2-(4-羟基-3,5-二异丙基苯基)乙基]氨基}甲基)苯基]噻吩-2-甲脒; N-2-(3,5-二叔丁基-4-羟基苯甲酰基)-N-1(4-(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。