| abstract |
Amidines (I) are new. <??>Amidines (I) of formula (I') and their salts are new. <??>A = phenyl, benzhydryl or a group of formula A1 - A9; <??>R1-R3 = halo, OH, SR6, 1-6C alkyl, 2-6C alkenyl, 1-6C alkoxy or NR6R7; <??>R4 = H or 1-6C alkyl; <??>R5 = OH, SR6, 1-6C alkyl or 1-6C alkoxy, but may not be SR6 nor alkoxy in A4; <??>R6 = H, 1-6C alkyl or 1-6C alkoxy; <??>R7 and R8 = H, OH, 1-6C alkyl or -CO-R9 but may not be alkyl nor COR9 in A5; <??>R9 = H, OH, 1-6C alkyl or 1-6C alkoxy, but may not be H, OH nor alkoxy in A1; <??>R10 and R11 = H or OH; <??>B' = 1-6C alkyl, 5-6 membered carbocyclic or heterocyclic aryl (heterocycle having 1-4 O, N, or S atoms, aryl optionally substituted by 1-6C alkyl, 1-6C alkoxy or 2-6C alkenyl) or NR13R14; <??>R13 and R14 = H or 1-6C alkyl; or <??>NR13R14 = 5 or 6 membered non-aromatic heterocycle comprising CH2, NH, O or S; <??>X = -(CH2)m-, -O-(CH2)m-, -S-(CH2)m-, -NR15-(CH2)m-, -CO-NR15-, -O-(CH2)m-CO-, -S-(CH2)m-CO-, -NR15-(CH2)m-CO- or -(CH2)m-C(OH)(CH3)-CO-; <??>Y' = -(CH2)n- or -(CH2)r-Q-(CH2)s-; <??>Q = piperazine, homopiperazine, 2-methyl piperazine, 2,5-dimethyl piperazine, piperidine, 1,2,3,6-tetrahydropiperidine, pyrrolidine, azetidine or a saturated 3-7C chain; <??>T = -(CH2)p-O-(CH2)q-, -(CH2)p-S-(CH2)q-, -(CH2)p-NR16-(CH2)q-, -(CH2)p-CO-NR16-(CH2)q-, or -CO-(CH2)p-NR16-(CH2)q-; <??>R12, R13, R14, R15, and R16 = H or 1-6C alkyl; <??>m, n, p, q, r, and s = 0-6;and <??>provided that when A = A6, then Y' is piperidine, and when A = A4, then Y' is -(CH2)r-Q-(CH2)s in which Q is a saturated 3-7 membered ring. |