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    • 5. 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。