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new ligands as inhibitors of the rar receptors, processes for their manufacture and their use in human medicine and in cosmetics

机译:rar受体抑制剂的新配体,其制备方法及其在人用药物和化妆品中的用途

摘要

Biaryl compounds (I), their salts, bases or optical isomers are new. Biaryl compounds of formula (I), their salts, bases or optical isomers are new. R1 = -CH=CH-R6, -C-triple bond-C-R6 or 2-naphthyl substituted by C(O)R5; R2 and R3 = H, 1-6C alkyl (preferably T), -OR7 or -NR8R9; R2 + R3 = 6-membered ring optionally substituted by 1-3C alkyl; R4 = aryl (preferably phenyl (optionally substituted by at least one 1-6C alkyl, alkoxy, mono- or di-alkylamino or halo) or heterocyclyl (preferably pyridine, morpholine, piperidine, piperazine or tetrahydropyridine (all optionally N-substituted by alkyl or 1-4C alkylcarbamate)); X = -CR10R11, -C(O) or C=NOR12; R5 = OH, alkoxy (preferably T1), 1-6C alkyl (preferably T), or mono- or di-alkylamino; R6 = phenyl (substituted by R14 and C(O)R13) or pyridyl(substituted by C(O)R13); R7 = benzyl (optionally substituted by 1-6C alkyl (preferably T)), H, 1-6C alkyl (preferably T), halogen (preferably F, Cl or Br), dialkylamino or alkoxy (preferably T1); R8 and R9 = H, 1-6C alkyl (preferably T) or benzyl; R10 = H or OH; R11 and R12 = H or 1-6C alkyl (preferably T); R13 = OH, alkoxy (preferably T1), monoalkylamino or dialkylamino; R14 = H, OH or amino; T = methyl, ethyl, propyl, isopropyl, butyl, tert-butyl, pentyl or hexyl; T1 = methoxy, ethoxy, propyloxy, isopropyloxy, butyloxy, tert-butyloxy, pentyloxy or hexyloxy.
机译:联芳基化合物(I),其盐,碱或旋光异构体是新的。式(I)的联芳基化合物,其盐,碱或光学异构体是新的。 R1 = -CH = CH-R6,-C-三键-C-R6或2-萘基被C(O)R5取代; R2和R3 = H,1-6C烷基(优选T),-OR7或-NR8R9; R 2 + R 3 =任选被1-3C烷基取代的6元环; R4 =芳基(优选苯基(任选地被至少一个1-6C烷基,烷氧基,单或二烷基氨基或卤素取代)或杂环基(优选吡啶,吗啉,哌啶,哌嗪或四氢吡啶(所有任选地被烷基N-取代) X = -CR10R11,-C(O)或C = NOR12; R5 = OH,烷氧基(优选T1),1-6C烷基(优选T),或单或二烷基氨基;或R6 =苯基(被R14和C(O)R13取代)或吡啶基(被C(O)R13取代); R7 =苄基(可选被1-6C烷基(优选T)取代),H,1-6C烷基(优选T),卤素(优选F,Cl或Br),二烷基氨基或烷氧基(优选T1); R8和R9 = H,1-6C烷基(优选T)或苄基; R10 = H或OH; R11和R12 = H或1-6C烷基(优选T); R13 = OH,烷氧基(优选T1),单烷基氨基或二烷基氨基; R14 = H,OH或氨基; T =甲基,乙基,丙基,异丙基,丁基,叔丁基,戊基或己基; T1 =甲氧基,乙氧基,丙氧基,异丙基戊氧基,丁氧基,叔丁氧基,戊氧基或己氧基。

著录项

  • 公开/公告号DE60336312D1

    专利类型

  • 公开/公告日2011-04-21

    原文格式PDF

  • 申请/专利权人 GALDERMA RESEARCH & DEVELOPMENT;

    申请/专利号DE20036036312T

  • 发明设计人 BIADATTI THIBAUD;COLLETTE PASCAL;

    申请日2003-05-27

  • 分类号C07C65/36;A61K31/19;A61K31/195;A61K31/455;A61P3/04;A61P3/06;A61P3/10;A61P9;A61P17;A61P19/02;A61P27/02;A61P35;A61P37;C07C65/17;C07C65/19;C07C65/26;C07C65/28;C07C65/40;

  • 国家 DE

  • 入库时间 2022-08-21 17:46:10

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