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    • 3. 发明授权
    • Melanocortin receptor ligands
    • 黑皮质素受体配体
    • US07132539B2
    • 2006-11-07
    • US10689022
    • 2003-10-20
    • Frank Hallock EbetinoXinrong TianWieslaw Adam MazurAnny-Odile Colson
    • Frank Hallock EbetinoXinrong TianWieslaw Adam MazurAnny-Odile Colson
    • C07D403/12C07D241/04A61K31/495A61K31/496
    • C07D401/12C07D241/04C07D241/08C07D403/12
    • The present invention relates to compounds which comprise a nitrogen-containing ring scaffold substituted by an R1 alkyl units selected from the group consisting of C1–C12 linear or branched alkyl, C3–C8 cyclic alkyl, C2–C12 linear or branched alkenyl, or haloalkyl, for example, the 2-keto-3-alkylpiperazines having the formula: wherein R is selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, and 4-chlorophenyl; R1 is selected from the group consisting of methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, sec-butyl, tert-butyl, cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl, benzyl, allyl, 1-methylallyl, 2-methylallyl, but-2-enyl, and propargyll; R7a is selected from the group consisting of hydrogen, —CO2H, —CONH2, —CONHCH3, and —CON(CH3)2; R8 is benzyl, substituted benzyl, or naphthalen-2-ylmethyl.
    • 本发明涉及包含由选自C 1 -C 12烷基的R 1烷基单元取代的含氮环支架的化合物, 直链或支链烷基,C 3 -C 8环烷基,C 2 -C 12直链状 或支链烯基或卤代烷基,例如具有下式的2-酮-3-烷基哌嗪:其中R选自苯基,3-氟苯基,4-氟苯基,3,5-二氟苯基和4-氟苯基, 氯苯基; R 1选自甲基,乙基,丙基,异丙基,丁基,异丁基,仲丁基,叔丁基,环丙基,环丙基甲基,环戊基,环戊基甲基,环己基, 环己基甲基,苄基,烯丙基,1-甲基烯丙基,2-甲基烯丙基,丁-2-烯基和炔丙基; R 7a选自氢,-CO 2 H,-CONH 2,-CONHCH 3,/ SUB >和-CON(CH 3 3)2。 R 8是苄基,取代的苄基或萘-2-基甲基。