Patent ID: 6306849
Filing Date: 2001-10-23
Classification: A61P,C07D

Abstract:
A compound defined by the general formula (I): ##STR13##wherein:one R.sup.1 or R.sup.2 is selected from CO(CH.sub.2).sub.j R.sup.4, CH(OH)(CH.sub.2).sub.b R.sup.4A, (CH.sub.2).sub.k R.sup.7, C.ident.C(CH.sub.2).sub.n R.sup.13, HC.dbd.CH(CH.sub.2).sub.m R.sup.12, HC.dbd.CH(CO.sub.2 R.sup.33).sub.2, CO(CH.sub.2).sub.j SR.sup.27, CH.sub.2 OR.sup.44, CH.sub.2 CHR.sup.31 CO.sub.2 R.sup.32, and CHO;the other R.sup.1 or R.sup.2 is selected from hydrogen, lower alkyl, halogen, nitro, NR.sup.14 R.sup.15, CH.sub.2 SR.sup.37, CO(CH.sub.2).sub.q R.sup.16, CH(OH)(CH.sub.2).sub.e R.sup.38, (CH.sub.2).sub.r R.sup.17, HC.dbd.CH(CH.sub.2).sub.t R.sup.18, C.ident.C(CH.sub.2).sub.u R.sup.19, CO(CH.sub.2).sub.q SR.sup.37, CHO, CH(SR.sup.34).sub.2, CH.sub.2 CHR.sup.39 CO.sub.2 R.sup.40, and CH.sub.2 OR.sup.36 ;R.sup.4 and R.sup.16 are selected from halogen, OR.sup.29, and NR.sup.5 R.sup.6 ;R.sup.4A and R.sup.38 are selected from hydrogen, halogen and NR.sup.5 R.sup.6 ;R.sup.5 and R.sup.6 are selected from hydrogen, lower alkyl, and phenyl; or R.sup.5 and R.sup.6 are combined with a nitrogen atom to form piperidine, morpholine, tetrahydropyrrole or piperazine;R.sup.7 and R.sup.17 are selected from halogen, phenyl, pyridyl, piperidinyl, morpholinyl, imidazolyl, OC(.dbd.O)H, OR.sup.9, NR.sup.10 R.sup.11, CO.sub.2 R.sup.8, N.sub.3, and SR.sup.27 ;R.sup.8 is selected from hydrogen, lower alkyl, phenyl, and pyridyl;R.sup.9 is selected from hydrogen, pyridylcarbonyl, and lower alkyl;R.sup.10 and R.sup.11 are selected from hydrogen, lower alkyl, hydroxyalkyl, phenyl, benzyl, methoxybenzyl, lower alkyloxycarbonyl, and lower alkylaminocarbonyl; or R.sup.10 and R.sup.11 combine together to form piperidine, morpholine, tetrahydropyrrole or piperazine;R.sup.12 and R.sup.18 are selected from hydrogen, lower alkyl, phenyl, pyridyl, imidazolyl, CO.sub.2 R.sup.8, and NR.sup.10 R.sup.11 ;R.sup.13 and R.sup.19 are selected from hydrogen, lower alkyl, NR.sup.10 R.sup.11, and OR.sup.9 ;R.sup.14 and R.sup.15 are independently selected from hydrogen, lower alkyl, and lower alkylaminocarbonyl;R.sup.27 and R.sup.37 are selected from hydrogen, lower alkyl, hydroxyalkyl, phenyl, hydroxyphenyl, pyridyl, pyrimidine, thiazolinyl, benzothiazolyl, alkyltetrazole, benzimidazole, (CH.sub.2).sub.2 NMe.sub.2, and (CH.sub.2).sub.a CO.sub.2 R.sup.28 ;R.sup.28, R.sup.29, R.sup.32, R.sup.33, and R.sup.40 are selected from hydrogen and lower alkyl;R.sup.31 and R.sup.39 are selected from hydrogen and CO.sub.2 R.sup.33 ;R.sup.34 is lower alkyl;R.sup.36 is selected from hydrogen, (CH.sub.2).sub.2 NMe.sub.2, methoxymethyl, ethoxymethyl, methoxyethyl, and ti-lower alkylsilyl in which the three lower alkyl groups are the same or different;R.sup.44 is selected from hydrogen, (CH.sub.2).sub.2 NMe.sub.2, methoxymethyl, ethoxymethyl, and methoxyethyl;a, b, and e are each 1 or 2;k and r are each 2, 3 or 4;m, n, t, and u are each 0 or 1;j and q are each 1, 2, 3, or 4;R.sup.3 is selected from hydrogen, acetyl, and lower alkyl;X is selected from hydrogen, hydroxymethyl, lower alkoxycarbonyl, and CONR.sup.20 R.sup.21 ;R.sup.20 and R.sup.21 are independently selected from hydrogen and lower alkyl;Y is selected from hydroxy, lower alkoxy, aralkyloxy, and acyloxy; andeach W.sup.1 and W.sup.2 is hydrogen or together represent oxygen.