发明名称 ARYL OR HETEROARYL AMIDES OF TETRAHYDRONAPHTALENE, CHROMAN, THIOCHROMAN AND 1,2,3,4-TETRAHYDROQUINOLINE CARBOXYLIC ACIDS HAVING RETINOID-LIKE BIOLOGICAL ACTIVITY
摘要 Carbo- and hetero- bicyclo carboxamidoaryl carboxylic acid derivatives and their amino carbonylaryl analogues of formula (I) and their salts are new. X = O, S, NH, 1-6C alkylimino, or (C(R1)2)n; R1, R2 = H, or 1-6C alkyl; R3 = H, 1-6C alkyl, or F; m, n, p, r = 0-2; provided that, when Z = O, then p+r is not 0; q = 0-4; Y = phenyl, naphthyl, pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, imidazolyl, or pyrazolyl (all optionally substituted by 1 or 2 R2); W = halo, 1-6C alkyl, fluoroalkyl, alkylsulphinyl, alkylsulphonyl, fluoroalkyl sulphonyl, nitro, azido, hydroxy, 1-10C alkoxy, methoxymethyl, tetrazolyl, cyano, 1-7C alkylcarbonyl, COOR8, or phenyl (optionally substituted by W other than phenyl or substituted phenyl); L = C(=Z)NH or NHC(=Z); Z = O or S; A = 1-5C straight chain or 3-6C branched chain alkylene, 3-6C cycloalkylene, or 2-6C alkenylene, alkadienylene, alkynylene, alkadiynylene or is absent; B = COOH, COOR8, CONR9R10, CH2OR11, CH(OR12)2, CHOR13O, COR7, CR7(OR12)2, or CR7OR13O; R7 = 1-5C alkyl, cycloalkyl, or alkenyl; R8 = 1-10C alkyl, trimethylsilyl 1-10C alkyl, 5-10C cycloalkyl, phenyl, or (1-6C alkyl)phenyl; R9, R10 = H, 1-10C alkyl, 5-10C cycloalkyl, phenyl, or (1-6C alkyl)phenyl; R11 = 1-6C alkyl, phenyl, or (1-6C alkyl)phenyl; R12 = 1-6C alkyl; and R13 = 2-5C alkylene.
申请公布号 HU9902536(A2) 申请公布日期 1999.12.28
申请号 HU19990002536 申请日期 1996.11.18
申请人 Allergan 发明人 CHANDRARATNA, ROSHANTHA A.;DUONG, TIEN T.;TENG, MIN
分类号 A61K31/16;C07C233/81;C07C235/66;C07D215/48;C07D311/58;C07D335/06 主分类号 A61K31/16
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