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    Bi-aromatic esters, a process for their preparation and their use in human or veterinary medicine and in cosmetic compositions
    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 失效
    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

    公开(公告)号：US5468897A

    公开(公告)日：1995-11-21

    申请号：US237991

    申请日：1994-05-04

    申请人： Braham Shroot ,  Jean-Michel Bernardon ,  William R. Pilgrim

    发明人： Braham Shroot ,  Jean-Michel Bernardon ,  William R. Pilgrim

    IPC分类号： A61K31/235 ,  A61K8/00 ,  A61K8/30 ,  A61K8/33 ,  A61K8/37 ,  A61K8/40 ,  A61K8/41 ,  A61K8/42 ,  A61K8/46 ,  A61K8/49 ,  A61P11/00 ,  A61P17/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61Q5/00 ,  A61Q19/00 ,  C07C67/14 ,  C07C69/00 ,  C07C69/76 ,  C07C69/773 ,  C07C69/78 ,  C07C69/88 ,  C07C69/94 ,  C07C309/42 ,  C07C309/58 ,  C07C311/29 ,  C07C317/22 ,  C07C317/44 ,  C07C323/62 ,  C07C321/00

    CPC分类号： C07C323/62 ,  C07C69/94 ,  C07C2103/74

    摘要： 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.

    摘要翻译： 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。

    Benzimidazole-derived compounds, method for preparing the same, and therapeutical and cosmetic uses thereof
    3.
    发明授权
    Benzimidazole-derived compounds, method for preparing the same, and therapeutical and cosmetic uses thereof 失效
    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

    公开(公告)号：US5446059A

    公开(公告)日：1995-08-29

    申请号：US142464

    申请日：1994-01-10

    申请人： Jean-Philippe Rocher ,  Daniel Cavey

    发明人： Jean-Philippe Rocher ,  Daniel Cavey

    IPC分类号： A61K8/49 ,  A61K8/00 ,  A61K8/11 ,  A61K31/415 ,  A61K31/4184 ,  A61P29/00 ,  A61P37/08 ,  A61Q17/00 ,  A61Q19/00 ,  A61Q19/10 ,  C07D235/12 ,  C07D235/18 ,  C07F9/6506

    CPC分类号： C07F9/65068 ,  A61K8/4946 ,  A61Q19/00 ,  C07D235/18

    摘要： 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.

    摘要翻译： 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。