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    Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them
    1.
    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。

    Use of thiazole derivatives for preparing a medicine for protecting mitochondria
    5.
    发明授权
    Use of thiazole derivatives for preparing a medicine for protecting mitochondria 有权
    噻唑衍生物用于制备线粒体保护药物的应用

    公开(公告)号：US07345066B2

    公开(公告)日：2008-03-18

    申请号：US10483823

    申请日：2002-07-25

    申请人： Michel Auguet ,  Pierre-Etienne Chabrier de Lassauniere ,  Jeremiah Harnett

    发明人： Michel Auguet ,  Pierre-Etienne Chabrier de Lassauniere ,  Jeremiah Harnett

    IPC分类号： A01N43/78

    CPC分类号： A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/497 ,  A61K31/54 ,  Y10S514/838

    摘要： The invention concerns compounds of general formula (I), wherein: A represents one of the radicals in which R5 represents independently a hydrogen atom, or alkyl; R6, R7 and R8 independently represent a hydrogen atom, alkyl, cycloalkyl, hydroxy or alkoxy; R11 represents a hydrogen atom of alkyl; and R9, R10 and R12 independently represent a hydrogen atom, alkyl, hydroxy or alkoxy; B represents a hydrogen atom or alkyl; n represents an integer from 0 to 5; R1 and R2 independently represent a hydrogen atom, alkyl or cycloalkyl; R3 and R4 independently represent a hydrogen atom or an alkyl radical, or R3 and R4 together form with the nitrogen atom which bears them a heterocycle optionally substituted comprising in all 1 to 2 heteroatoms and 5 to 7 members. Said compounds can be used for preparing a medicine for protecting mitochondria, and in particular a medicine for preventing or treating cirrhosis.

    摘要翻译： 本发明涉及通式（I）的化合物，其中：A表示其中R 5独立地表示氢原子或烷基的基团之一; R 6，R 7和R 8独立地表示氢原子，烷基，环烷基，羟基或烷氧基; R 11表示烷基的氢原子; R 9，R 10和R 12独立地表示氢原子，烷基，羟基或烷氧基; B表示氢原子或烷基; n表示0〜5的整数， R 1和R 2独立地表示氢原子，烷基或环烷基; R 3和R 4独立地表示氢原子或烷基，或R 3和R 4共同 与带有它们的氮原子一起形成任选被取代的杂环，其包含所有1至2个杂原子和5至7个成员。 所述化合物可用于制备用于保护线粒体的药物，特别是用于预防或治疗肝硬化的药物。

    Lipoic acid derivatives, their preparation, and pharmaceutical compositions containing them
    8.
    发明授权
    Lipoic acid derivatives, their preparation, and pharmaceutical compositions containing them 失效
    硫辛酸衍生物，它们的制备和含有它们的药物组合物

    公开(公告)号：US06605637B1

    公开(公告)日：2003-08-12

    申请号：US09937823

    申请日：2001-09-27

    申请人： Jeremiah Harnett ,  Michel Auguet ,  Pierre-Etienne Chabrier de Lassauniere

    发明人： Jeremiah Harnett ,  Michel Auguet ,  Pierre-Etienne Chabrier de Lassauniere

    IPC分类号： A61K31385

    CPC分类号： C07D409/12 ,  C07C323/60 ,  C07D339/04

    摘要： The invention concerns novel lipoic acid derivatives, which have an inhibiting action with respect to NO-synthase enzymes producing nitrogen monoxide NO and/or are agents enabling the regeneration of antioxidants or entities trapping reactive oxygen species (ROS) and intervening in a more general manner in the redox status of thiol groups. The invention also concerns methods for preparing them, pharmaceutical compositions containing them and their use for therapeutic purposes, particularly their use as NO-synthase inhibitors and/or as agents acting more generally in the redox status of thiol groups.

    摘要翻译： 本发明涉及关于产生一氧化氮NO的NO合成酶具有抑制作用的新型硫辛酸衍生物和/或能够更有效地吸收抗氧化剂或捕获活性氧（ROS）的物质并以更一般的方式进行干预的试剂 在硫醇基团的氧化还原状态。 本发明还涉及制备它们的方法，含有它们的药物组合物及其用于治疗目的的用途，特别是其用作NO-合酶抑制剂和/或作为更一般地在硫醇基团的氧化还原状态中起作用的作用剂。