| 摘要 |
Medicaments contg. alpha-amino-3,5-di-t-butyl-4-hydroxybenzyl- phosphorus cpds. of formula (I) or their salts or stereoisomers are new: R1, R2 = H, 1-12C alkyl*, 1-12C alkyl (substd. by one or more of (a) phenyl*; (b) phenyl substd. by 1-3 halo, 1-3C alkyl, 1-3C alkoxy, methylenedioxy, NO2, NH2, amidino, guanidino, OH, 2-7C alkoxycarbonyl and/or CN; (c) 5- or 6-membered monocyclic satd. heterocyclyl; (d) amino opt. mono- or disubstd. by 1-3C alkyl; and (e) 2-4C alkoxycarbonyl; tetrahydronaphthyl; phenyl*; phenyl substd. by 1-3 f 1-4C alkyl, 1-4C haloalkyl, halo*, NO2, SO2NH2, amidino, guanidino, 1-3C alkoxy, methylenedioxy, OH, COOH, CN, 2-4C alkoxycarbonyl, CH=CHCOOR (R = H or 1-3C alkyl), NH2 and/or NHQ(Q = a gp. of formula (I) minus NR1R2); naphthyl*; naphthyl substd. by one or more of the above phenyl substits.; heteroaryl opt. substd. by one or more of phenyl, benzyl and the above phenyl substits.; or NR1R2 = a 4-7-membered ring* or a 5- 7-membered ring in which a C atom is replaced by O, N, NPh or NQ; X, Y = H, 1-6C alkyl, 1-6C alkoxy, 3-6C alkenyloxy, OPh or OH. Also claimed are : (A) cpds. (I) where the asterisked definitions are omitted; (B) cpds. (I) where R1 = phenyl or mono-, di- or trihalophenyl, R2 = H and X and Y are as above but not alkoxy. |
