发明名称 TERTIARY AMINE
摘要 Tertiary amines of formula (I) and their acid addition salts are new: A1 = alkyl or alkenyl; A2 = cycloalkyl, cycloalkylalkyl or alkyl or alkenyl which is optionally substituted by R1, CONH2 or CN. If A1 = alkyl, then A2 can also be OH; A3, A4 = H or alkyl or A1 together with A2 or A3 forms an alkylene, alkenylene or alkadienylene group with up to 5C atoms which is optionally substituted by R1 and where one or two of these C atoms may be replaced by one or two N atoms(s) or N-alkyl group(s); R1 = OH, oxo, O- or S-alkyl or dialkylamino, which is bound via a saturated C atom. The C atom to which R1 is attached (or an unsaturated C atom elsewhere in A1, A2, A1-A2 or A1-A3) may be attached to N(A1, A2); when p = 1, L = phenylene, cycloalkylene-alkylene or 1-11C alkylene or alkenylene (which is bound to M directly or via O, NH or N(alkyl or alkanoyl)); when p = 0, L and T = 6-11C alkenylene or alkadienylene; M = thienylene or pyridylene, or 1,4-phenylene (which is optionally substituted by one or more alkyl, halo, N(R2, R21), CONH2, CN, NO2, CF3, OH, O- or S-alkyl, 1,2,4-triazol-1-yl or tetrazol-1-yl) or a group of formula M<1>; q = 0 or 1; R2, R21 = H, alkyl, alkenyl, alkanoyl or SO2-alkyl; T = CO, CH(R3), C(R4, R5) or C=NOR6, when M = M1 and q = 0, T can also be SO2; R3 = OH, F, alkoxy or alkanoyloxy; R4 = OH and R5 = alkyl, alkenyl, alkynyl, cycloalkyl or CF3, or R4+R5 = CH2, CH2O or CH2CH2; R6 = H, alkyl or alkenyl; Q = cycloalkyl, C(R7, R8), phenyl (which is optionally substituted by one or more alkyl, halo, N(R9, R10), CONH2, CN, NO2, CF3, 1,2,4-triazol-1-yl or tetrazol-1-yl groups), or 6-13C linear alkyl, alkenyl, alkadienyl or alka-trienyl with 0-3 CH3 substituents and which can also be substituted by OH and/or N(R9, R10); R7, R8 = 5-11C alkyl, alkenyl or alkadienyl; R9, R10 = H, alkyl, alkenyl or alkanoyl. A number of provisos are given in the claims: (a) when T = CO or CHOH; L = phenylene or alkylene/alkenylene bound to M via O or N-alkyl; M = 1,4-phenylene or 1,4-phenylene monosubstituted by alkoxy, halo, CN, NO2 or CF3 and Q = substituted phenyl, alkenyl, alkyl or OH-alkyl, then A2 is not alkyl or alkenyl and A1 cannot form alkylene with A2; (b) when A1 and A2 together form alkylene or R1-alkylene, A2 = hydroxyalkyl or A1 and A2 are each alkyl, then M is not pyridylene; (c) when T = C(OH, R51), where R51 = alkyl, alkenyl, alkynyl or cycloalkyl; M = optionally substituted 1,4-phenylene and L = alkylenoxy, L has at least 5C atoms between its two free valencies and contains up to 11C atoms.
申请公布号 JPH09221458(A) 申请公布日期 1997.08.26
申请号 JP19960326948 申请日期 1996.12.06
申请人 F HOFFMANN LA ROCHE AG 发明人 YOHANESU AEBI;HENRIETSUTA DEEMUROU;ZAAKU ANBAA;SHINEEZU JIYORIDON;HANSU RENGUSUFUERUTO;ORIBUIE MOORANDO;JIERAARU SHIYUMATSUDO;YUUFUA JI
分类号 C07D249/08;A61K31/135;A61K31/15;A61K31/165;A61K31/275;A61K31/35;A61K31/351;A61K31/38;A61K31/381;A61K31/40;A61K31/44;A61K31/4402;A61K31/4418;A61K31/445;A61P3/06;A61P9/00;A61P31/04;A61P31/10;C07C211/08;C07C211/15;C07C211/16;C07C217/20;C07C217/46;C07C217/52;C07C217/76;C07C225/22;C07C235/78;C07C235/84;C07C237/06;C07C255/56;C07C255/58;C07C311/04;C07C317/16;C07C323/10;C07C323/22;C07C323/25;C07D207/08;C07D211/46;C07D211/58;C07D213/64;C07D233/60;C07D257/04;C07D309/12;C07D333/20;C07D333/22;(IPC1-7):C07C211/08 主分类号 C07D249/08
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