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    • 1. 发明授权
    • Benzimidazole-derived compounds, method for preparing the same, and
therapeutical and cosmetic uses thereof
    • 衍生自苯并咪唑的化合物,其制备方法及其治疗和美容用途
    • US5446059A
    • 1995-08-29
    • US142464
    • 1994-01-10
    • Jean-Philippe RocherDaniel Cavey
    • Jean-Philippe RocherDaniel Cavey
    • A61K8/49A61K8/00A61K8/11A61K31/415A61K31/4184A61P29/00A61P37/08A61Q17/00A61Q19/00A61Q19/10C07D235/12C07D235/18C07F9/6506
    • C07F9/65068A61K8/4946A61Q19/00C07D235/18
    • Benzimidazole derivatives having general formula (I), wherein R.sub.1 and R.sub.2 are a hydrogen atom, a lower alkyl radical, an OR.sub.4 radical, a lower fluoroalkyl radical or a halogen atom; R.sub.3 is a hydrogen atom, a lower alkyl radical, a halogen, a hydroxyl or a lower alkoxy radical having 1-6 carbon atoms; R.sub.4 is a hydrogen atom, a lower alkyl radical, a benzyl radical or a (II) radical, PO.sub.3 H, SO.sub.3 H or an aminoacid residue; R.sub.7 is a lower alkyl radical, a lower alkoxy radical having 1-6 carbon atoms, a --(CH.sub.2).sub.n --COOH radical where n=1-6, or the radical (III), where r' and r" are a hydrogen atom or a lower alkyl radical, or form, together with the nitrogen atom, a 5 or 6-membered heterocyclic ring optionally interrupted by a heteroatom; R.sub.5 and R.sub.6 are different and represent the OR.sub.8 radical or a mono or polycyclic cycloalkyl radical having 5-12 carbon atoms bound to the phenyl core by a tertiary carbon; R.sub.8 is a hydrogen atom, a lower alkyl radical, an acyl radical having 2-7 carbon atoms, a benzyl radical optionally substituted by one or more halogen atoms, or a benzoyl radical; and salts of said compounds obtained by adding a pharmaceutically acceptable acid or base. Said compounds may be used therapeutically, in particular in relation to inflammatory and/or immunoallergic conditions, and cosmetically to provide body and hair care.
    • PCT No.PCT / FR92 / 00482 Sec。 371日期1994年1月10日 102(e)日期1994年1月10日PCT提交1992年5月29日PCT公布。 WO92 / 21663 PCT出版物 1992年12月10日授权。具有通式(I)的苯并咪唑衍生物,其中R1和R2为氢原子,低级烷基,OR4基,低级氟代烷基或卤素原子。 R3是氢原子,低级烷基,卤素,羟基或具有1-6个碳原子的低级烷氧基; R4是氢原子,低级烷基,苄基或(Ⅱ)基,PO3H,SO3H或氨基酸残基; R7是低级烷基,具有1-6个碳原子的低级烷氧基,其中n = 1-6的 - (CH2)n-COOH基团或基团(III),其中r'和r“是 氢原子或低级烷基,或与氮原子一起形成任选被杂原子间隔的5或6元杂环; R5和R6不同,代表OR8基团或具有5-12个碳原子的单或多环环烷基,其通过叔碳与苯基键合; R8是氢原子,低级烷基,具有2-7个碳原子的酰基,任选被一个或多个卤素原子取代的苄基或苯甲酰基; 和通过加入药学上可接受的酸或碱获得的所述化合物的盐。 所述化合物可以在治疗上,特别是关于炎性和/或免疫过敏性病症,以及美容方面用于提供身体和头发护理。