Patent ID: 6114380
Filing Date: 2000-09-05
Classification: C07C,C07D

Abstract:
A compound of Formula 1 ##STR72## and the stereoisomers, hydrates, isosteres and the pharmaceutically acceptable salts thereof whereinP.sub.1 is Q or B, whereinB is C.sub.1-6 alkylene ##STR73## wherein T is [(O).sub.b --W--R] and T' is [(O).sub.b' --W'--R'] or H, wherein each of W and W' are independentlyC.sub.1-6 alkylene or nothing and R and R' are each independently --CH.sub.2 CHO, hydroxy C.sub.1-6 alkyl,C.sub.1-6 alkoxy C.sub.1-6 alkyl, C.sub.1-6 alkyl, Q, ##STR74## or R.sub.7 ; provided that W is C.sub.2-6 alkylene when W is directly attached to a nitrogen atom in R, provided that W' is C.sub.2-6 alkylene when W' is directly attached to a nitrogen atom in R', provided that W or W' are each independently C.sub.1-6 alkylene when R or R' are each independently an aryl, and provided that B is other than p-hydroxybenzyl or p-alkoxybenzyl;Q is ##STR75## P.sub.2 is C.sub.1-6 alkyl, cyclopentyl, hydroxy C.sub.1-6 alkyl, phenyl, benzyl or 3-tetrahydrofuryl;R.sub.1 is benzyloxy, C.sub.1-6 alkoxy, C.sub.1-6 alkyl, phenyl, benzyl, phenethyl, fluorenylmethylenoxy, 2-isoquinolinyl, PDL, ##STR76## wherein PDL is --(CH.sub.2).sub.a -2-,3-, or 4-pyridyl, or p-substituted benzyloxy, wherein the substitution is with a nitro, OH, amino, C.sub.1-6 alkoxy, hydroxy C.sub.1-6 alkylene, or halogeno;R.sub.3 is C.sub.1-6 alkenyl, C.sub.1-6 alkoxy, hydroxy C.sub.1-6 alkyl, C.sub.1-6 alkyl, or OH,R.sub.4 is H, C.sub.1-6 alkyl, phenyl or benzyl,R.sub.5 is CH([(CH.sub.2).sub.d --O--CH.sub.2 ].sub.x --R.sub.8).sub.2, chiral branched-chain C.sub.1-6 alkylene ##STR77## or CH(Y)(Z) whereinY is C.sub.1-15 alkyl, hydroxy C.sub.1-15 alkyl or ##STR78## and Z is (CH.sub.2).sub.d --O--CHO,C.sub.1-6 alkylene-O-(CH.sub.2).sub.d -(O--CH.sub.2 --CH.sub.2).sub.e --O--C.sub.1-6 alkyl, ##STR79## provided that d'=2 when R.sub.7 is piperazinyl, substituted piperazinyl, piperidyl or morpholinyl, andwhereinV is OR.sub.4 or hydroxy C.sub.1-6 alkyl;R.sub.6 is H or C.sub.1-3 alkyl;R.sub.7 is piperazinyl, substituted piperazinyl, piperidyl, morpholinyl, pyridyl, pyrazinyl, pyrimidinyl or phenyl, wherein substituted piperazinyl is piperazinyl substituted on one nitrogen atom thereof with CHO, C(O)NHR.sub.4, C.sub.1-4 alkyl or CO.sub.2 R.sub.4 ;R.sub.8 is pyrimydyl, pyridyl, pyrazinyl or phenyl;a is zero, 1, 2 or 3;b and b' are each independently zero or 1;d and d' are each independently 1 or 2;e and e' are each independently zero, 1 or 2; andx is zero or one.