| 摘要 |
Acylguanidine derivatives (I) in all possible isomeric forms and their mixtures, their salts and promedicaments, are new. Acylguanidine derivatives of formula (I) in all possible isomeric forms and their mixtures, their salts and promedicaments, are new. R1, R2 = H, 1-6C alkyl optionally substituted by R3; or R1 + R2 = form a bivalent saturated or unsaturated 2-9C alkylene group, such as -(CH2)p- (optionally substituted by one or more halogen, 1-6C alkyl or alkoxy, 6-14C aryl, arylalkyl, 5-14C heteroaryl, heteroarylalkyl, 3-12C cycloalkyl, cycloalkylalkyl, or oxo groups), optionally condensed through carbon atoms to a carbocycle or 5-7 membered heterocycle with 1 or 2 N atoms, that may be saturated or unsaturated and may be substituted by one or two groups R3; R3 = 1-8C alkyl or alkoxy, 5-14C aryl, aryl alkyl, halogen, trifluoromethyl, OH, NO2, NH2, mono- or di-(1-4C alkyl)-amino, NHC(O)(1-4C alkyl) or C(O)-(1-4C alkyl); p = 2 - 9; R4 = H, (1-6C alkyl)-C(O)O-(1-4C alkyl), or 1-6C alkyl optionally substituted by OH, 1-4C alkoxy, SO2-(1-4C alkyl), NR9R9', or N<+>R9R9'R9''Q<->, or a group of formula (i) - (vi); dotted line = linking bonds; Q = an anion; R5 = H, C(O)R6, C(O)OR6, SO2R6, SO2NHR6, SO2NHC(O)R6, SO2NHC(O)OR6, C(O)NH2 or C(O)NHR6; R6 = 1-8C alkyl, 6-14C aryl, aryl alkyl, 5-14C heteroaryl, heteroaryl alkyl, 3-20C mono-, di, or tricyclic cycloalkyl, or cycloalkyl alkyl, aryl and heteroaryl groups being optionally substituted by 1-3 groups R3; R7 = H, 1-6C alkyl-O-CO-, OH, 1-6C alkyl-O-CO-, or NO2; R8 = H, halogen, 1-6C alkyloxy; R9, R9' and R9 = H, 1-6C alkyl, 5-14C aryl, or aryl alkyl; R12 = H or 1-6C alkyl; m = 0, 1, 2, or 3; n = 1, 2, or 3 such that the acylguanidine group is para or meta to the oxygen. An Independent claim is also provided for the preparation of (I)
|
