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    • 2. 发明授权
    • Bi-aromatic esters, a process for their preparation and their use in
human or veterinary medicine and in cosmetic compositions
    • 双芳族酯,其制备方法及其在人或兽医学和化妆品组合物中的应用
    • US5468897A
    • 1995-11-21
    • US237991
    • 1994-05-04
    • Braham ShrootJean-Michel BernardonWilliam R. Pilgrim
    • Braham ShrootJean-Michel BernardonWilliam R. Pilgrim
    • A61K31/235A61K8/00A61K8/30A61K8/33A61K8/37A61K8/40A61K8/41A61K8/42A61K8/46A61K8/49A61P11/00A61P17/00A61P27/02A61P29/00A61P35/00A61Q5/00A61Q19/00C07C67/14C07C69/00C07C69/76C07C69/773C07C69/78C07C69/88C07C69/94C07C309/42C07C309/58C07C311/29C07C317/22C07C317/44C07C323/62C07C321/00
    • C07C323/62C07C69/94C07C2103/74
    • Bi-aromatic esters have the formula ##STR1## wherein R.sub.1 represents H, OH, --CH.sub.3, --CH.sub.2 OH, --CH(OH)CH.sub.3, --COOR.sub.9, ##STR2## or SO.sub.2 R.sub.10 ; R.sub.9 represents H, C.sub.1 -C.sub.6 alkyl or mono or polyhydroxyalkyl; R.sub.10 represents OH, C.sub.1 -C.sub.6 alkyl or ##STR3## r' and r" represent H, C.sub.1 -C.sub.6 alkyl, aryl, aralkyl, mono or polyhydroxyalkyl, or r' and r" taken together form a heterocycle; R.sub.2 represents H, C.sub.1 -C.sub.6 alkyl, OR.sub.9, F or --CF.sub.3 ; R.sub.3, R.sub.4 and R.sub.5 represent H, F, OH, --CH.sub.3, --OCH.sub.3, --CF.sub.3, --COOH or --CH.sub.2 OH; R.sub.6 and R.sub.8 represent H, .alpha.-substituted C.sub.3 -C.sub.15 alkyl, .alpha., .alpha.'-disubstituted C.sub.4 -C.sub.12 alkyl, C.sub.3 -C.sub.12 cycloalkyl, C.sub.5 -C.sub.12 mono or polycyclic cycloalkyl whose linking carbon is trisubstituted, --SR.sub.11, --SO.sub.2 R.sub.11 or --SOR.sub.11 ; R.sub.11 represents C.sub.1 -C.sub.6 alkyl or cycloalkyl; R.sub.6 and R.sub.8 cannot simultaneously represent H; R.sub.7 represents H, C.sub.1 -C.sub.6 alkyl, alkenyl, alkenyloxy, OR.sub.12 or SR.sub.13 ; R.sub.12 represents H, C.sub.1 -C.sub.6 alkyl or alkenyl; R.sub.3 represents H, C1-C.sub.6 alkyl or aralkyl; with the proviso that when R.sub.1 represents ##STR4## and R.sub.2 represents H then: (i) either R.sub.3 and R.sub.4 are other than H or --CH.sub.3, (ii) or R.sub.7 is other than OR.sub.12 and R.sub.6 or R.sub.8 is cycloalkyl having more than 7 carbon atoms, (iii) or R.sub.7 is OR.sub.12 but R.sub.6 and R.sub.8 are other than H, (iv) or R.sub.7 is OR.sub.12 but R.sub.5 is other than H.The bi-aromatic esters are employed in human and veterinary medicine and in cosmetic compositions.
    • 双芳族酯具有式(I)其中R 1表示H,OH,-CH 3,-CH 2 OH,-CH(OH)CH 3,-COOR 9,或SO 2 R 10; R9表示H,C1-C6烷基或单或多羟基烷基; R 10表示OH,C 1 -C 6烷基或R 3',R“表示H,C 1 -C 6烷基,芳基,芳烷基,单或多羟基烷基,或r'和r”一起形成杂环; R 2表示H,C 1 -C 6烷基,OR 9,F或-CF 3; R3,R4和R5表示H,F,OH,-CH3,-OCH3,-CF3,-COOH或-CH2OH; R 6和R 8表示H,α-取代的C 3 -C 15烷基,α,α'-二取代的C 4 -C 12烷基,C 3 -C 12环烷基,连接碳是三取代的C 5 -C 12单环或多环环烷基,-SR 11,-SO 2 R 11或 - SOR11; R11表示C1-C6烷基或环烷基; R6和R8不能同时代表H; R7表示H,C1-C6烷基,烯基,烯氧基,OR12或SR13; R12表示H,C1-C6烷基或烯基; R3表示H,C1-C6烷基或芳烷基; 条件是当R1表示且R2表示H时:(i)R3和R4不是H或-CH3,(ii)或R7不是OR12,R6或R8是大于7的环烷基 碳原子,(iii)或R7是OR12,但R6和R8不是H,(iv)或R7是OR12,但R5不是H.双芳族酯用于人类和兽医学和化妆品组合物中。
    • 3. 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。