| 摘要 |
<p>Dihydropyridines of formula (I) and their salts are new (R1 = H or 1-6C alkyl; R3, R5 = (CH2)x-(CHR34)yR35; x = 0-7; y = 0-1; R34 = H, 1-6C alkyl or up to 8C cycloalkyl; R35 = H, 1-6C alkyl opt. substd. by 1-6C alkoxy, 1-6C alkanoyl, or OH, a 4-6 membered O, N or S(O)n contg. heterocyclic ring opt. substd. C t; or cycloalkyl or cycloalkenyl contg. up to 8C and the cycloalkyl may be bridged, substd. by 1-6C alkyl or fused to a phenyl ring; or CH=CHR13 or 1-6C alkylamino in which the alkyl gp(s). are opt. substd.-eny; or when x is a whole number 1-7, R35 = CN, OSO2R33 or (II) or (III) R13 = up to 8C cycloalkyl; R11, R12 = 1-6C alkyl or phenyl; R33 = 1-6C alkyl or (1-6C alkyl)-phenyl; R2, R6 = CN, CHO or 1-6C alkyl opt. interrupted by O and opt. substd. by halogen, OH, COOH or a 1-6C alkyl esteral te, by 1-6C beta-ketoester gp., by a 2-amino-6-hydroxy-pyridmidin-4-yl gp. or NR14R16; R14,R15 = halogen, 1-6C alkyl, C(=NCN)S-1-6C alkyl or (IV) or together form a chain CR16 = N-CR17=CR18, CH2CH2N(R19)CH2CH2 or -CO(o-phenylene)CO-; RR19 = H, 1-6C alkyl opt. substd. by phenyl wc s opt- subat. b le; CONR20R21 or a 5-membered unsatd. ring contg. N and opt. also S; R20, R21 = H or 1-6C alkyl; R4 = phenyl carrying 3 or 4 substits. or is an unsatd. 5-membered heterocyclic gp. contg. a single heteroatom selected from O, S or N, R4 being substd. by CF3, XR22, NO2, halogen, CN, 1-6C alkyl, formyl, dioxalanyl, N(R23)COR24, CONR25R26 or amino which is opt. substd. by phenylsulphonyl or trifluoroacetyl and R4 carries a substit. on the atom adjacent to the atom through which R4 is connected to the remainder of the molecule; R22 = phenyl or 1-6C alkyl opt. substd. by halogen; x = O or S(O)n n = 0, 1 or 2; R23, R24, R25 = H or 1-6C alkyl; provided that (i) when R1 = H or Me, R2 = CH2F, R3 = Me and R5 = 1-methylethyl or cyclopentyl then R4 is not 2-(trifluoromethyl)-3-chloro-6 fluorophenyl, (ii) when R1 = H, R2 = CH2F, R3 = Me and R5 = 1-methylethyl then R4 i.</p> |
