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    Stimulating the differentiation of preadipocytic cells and therapies based thereon
    7.
    发明授权
    Stimulating the differentiation of preadipocytic cells and therapies based thereon 有权
    基于此，刺激前脂肪细胞的分化和疗法

    公开(公告)号：US06248791B1

    公开(公告)日：2001-06-19

    申请号：US09127734

    申请日：1998-08-03

    申请人： Gérard Ailhaud ,  Paul Grimaldi ,  Irina Safonova ,  Braham Shroot ,  Uwe Reichert

    发明人： Gérard Ailhaud ,  Paul Grimaldi ,  Irina Safonova ,  Braham Shroot ,  Uwe Reichert

    IPC分类号： A61K3107

    CPC分类号： A61K31/195 ,  A61K31/20 ,  A61K31/19 ,  A61K2300/00

    摘要： The differentiation of preadipocytic cells into adipocytic cells, in particular for correcting insulin-resistance disease states in mammalian organisms, notably in humans, for example type II diabetes and cardiovascular disorders such as hypertension and atherosclerosis, is stimulated by treating such preadipocytic cells, or a patient in need of such treatment, with an effective amount of (a) at least one ligand displaying affinity for the nuclear receptors for retinoic acid and/or isomers thereof, preferably at least one ligand displaying a specific affinity for the RAR receptors and even more preferably the RAR-&agr; receptor and (b) at least one fatty acid, e.g., a polyunsaturated fatty acid.

    摘要翻译： 前脂肪细胞分化为脂肪细胞，特别是用于校正哺乳动物生物体，特别是人类中的胰岛素抗性疾病状态，例如II型糖尿病和心血管疾病如高血压和动脉粥样硬化，通过治疗这种前脂肪细胞被刺激，或 需要这种治疗的患者，有效量的（a）至少一种对视黄酸和/或其异构体的核受体显示亲和力的配体，优选至少一种对RAR受体显示特异性亲和力的配体，甚至更多 优选RAR-α受体和（b）至少一种脂肪酸，例如多不饱和脂肪酸。

    Bi-aromatic esters, a process for their preparation and their use in human or veterinary medicine and in cosmetic compositions
    9.
    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。