摘要 |
Cpds. of formula e.g. (I), (II), (VII) and (XII) are new: (I) = (A; X1 = R1); (II) = (A; X1 = a gp. of formula (i)); (VII) = (C; either K = CR3 and L = CH or K = CHR3 and L = CH2); (XII) = (C; K = CR3R21 and L = C=X); R1 = heteroaryl opt. substd. by 1-4C alkyl, F, Cl, Br, NO2, CO2H, CO2R2, CHO, CN, CF3, CH2OH or COMe, and is attached through C or N atom; R2 = H, 1-4C alkyl or perfluoroalkyl, aryl, heteroaryl or opt. substd. allyl, arylmethyl, alkynyl or alkenyl; R3 = H, 1-4C alkyl or perfluoroalkyl, hydroxymethyl, aryl, heteroaryl or opt. substd. allyl, arylmethyl, alkynyl or alkenyl; R4-R6, R11-R15 = H, F, Cl, Br, I, NO2, CO2H, CO2R2, CN, CF3, CH2OH, 1-4C alkyl or perfluoroalkyl, OR2, SR2, S(O)R2, SO2R2, SO3H, S(NR2R7)R2, S(O)(NR2R7)R2, NR2R7, aryl, heteroaryl or opt. substd. allyl, arylmethyl, alkynyl or alkenyl; R7 = H, 1-4C alkyl or perfluoroalkyl, aryl, heteroaryl, opt. substd. allyl or arylmethyl, OR8 or NHR8; R8 = H, 1-6C alkyl or perfluoroalkyl, aryl, heteroaryl, opt. substd. allyl or arylmethyl, SO2R2 or S(O)R2; R9, R10 = H, 1-6C alkyl or perfluoroalkyl, aryl, heteroaryl or opt. substd. allyl, arylmethyl, alkynyl or alkenyl; or R9 + R10 = 3-7 membered ring opt. substd. by H, F, OR2 or NR2R7; X = CH2, O, S or NR7; R20 = 1-6C alkyl or opt. substd. allyl, arylmethyl, alkenyl, aryl or heteroaryl; R21 = H, 1-4C alkyl or opt. substd. allyl, arylmethyl, aryl or heteroaryl; with provisos. |
申请人 |
Ligand Pharmaceuticals Incorporated |
发明人 |
DAVIS, ROBERT J.;EDWARDS, JAMES E.;FARMER, LUC J.;GOLDMAN, MARK E.;HAMANN, LAWRENCE G.;JONES, TODD K.;POOLEY, CHARLOTTE L.F.;TEGLEY, CHRISTOPHER M.;WEST, SARAH J.;WINN, DAVID T.;ZHI, LIN |