PAINKILLING ASSOCIATION COMPRISING A DIHYDROIMIDAZOPYRAZINE DERIVATIVE
    1.
    发明申请
    PAINKILLING ASSOCIATION COMPRISING A DIHYDROIMIDAZOPYRAZINE DERIVATIVE 审中-公开
    包含二氢咪唑并吡啶衍生物的结合协会

    公开(公告)号:US20090270400A1

    公开(公告)日:2009-10-29

    申请号:US11722070

    申请日:2005-12-16

    IPC分类号: A61K31/495

    摘要: The invention relates to a product comprising (1R)-1-[(({2R)-2-amino-3-[(8S)-8-(cyclohexylmethyl) -2-phenyl-5,6-dihydroimidazo [1,2-a]pyrazin-7(8H)-yl]-3-oxopropyl}dithio)methyl]-2-[(8S)-8-(cyclohexylmethyl) -2-phenyl-5,6-dihydrolmidazo[1,2-a]pyrazin-7(8H)-yl]-2-oxoethylamine in association with an analgesic agent selected from morphine, the similar or a morphine derivative, sodium channel inhibitors, non-steroidal antiflammatory agents (AINS), glutamatergic system inhibitors, tricycle antidepressants and gabaergic derivatives for simultaneous therapeutic use which is separated or out over the time for pain treatment or prevention.

    摘要翻译: 本发明涉及包含(1R)-1 - [(((2R)-2-氨基-3 - [(8S)-8-(环己基甲基)-2-苯基-5,6-二氢咪唑并[1,2 -a]吡嗪-7(8H) - 基] -3-氧代丙基}二硫基)甲基] -2 - [(8S)-8-(环己基甲基)-2-苯基-5,6-二氢咪唑并[1,2-a ]吡嗪-7(8H) - 基] -2-氧代乙胺与选自吗啡,类似或吗啡衍生物,钠通道抑制剂,非甾体抗炎剂(AINS),谷氨酸能系统抑制剂,三轮车抗抑郁药 和用于同时治疗的gabaergic衍生物,其用于疼痛治疗或预防的时间分离或排出。

    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

    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。

    Thiazole Derivatives for Treating Restless Legs Syndrome
    10.
    发明申请
    Thiazole Derivatives for Treating Restless Legs Syndrome 审中-公开
    噻唑衍生物治疗不宁腿综合征

    公开(公告)号:US20080194657A1

    公开(公告)日:2008-08-14

    申请号:US11995089

    申请日:2006-07-07

    IPC分类号: A61K31/426 A61P25/00

    摘要: The invention relates to the use of derivatives of thiazoles having general formula (I) for the preparation of a medicament for the treatment or prevention of restless legs syndrome, also known as Ekbom syndrome. The invention also relates to a combination of thiazole derivatives having general formula (I) and at least one compound selected from among neuroleptics or products that act on the dopaminergic system for the treatment or prevention of restless legs syndrome, also known as Ekbom syndrome.

    摘要翻译: 本发明涉及具有通式(I)的噻唑衍生物在制备用于治疗或预防不宁腿综合征(也称为Ekbom综合征)的药物中的用途。 本发明还涉及具有通式(I)的噻唑衍生物和选自神经安定药或作用于多巴胺能系统用于治疗或预防不宁腿综合征(也称为Ekbom综合征)的产品中的至少一种化合物。