Patent ID: 6127402
Filing Date: 2000-10-03
Classification: A61P,C07D

Abstract:
A compound selected from the group of compounds represented by formula I: ##STR75## where: R.sub.1 and R.sub.5 together are --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 --;R.sub.3 and R.sub.4 are independently H, halo, alkyl, alkyloxy, or alkylthio;R.sub.10 is a group represented by formula (A), (B) or (C): ##STR76## where: X is O or S;R.sub.12 and R.sub.16 are independently H, halo, alkyl, alkyloxy, alkylthio, cyano, or hydroxy;R.sub.13 and R.sub.15 are independently H, halo, alkyl, alkyloxy, or alkylthio; andR.sub.14 is H, halo, alkyl, haloalkyl, amino, alkylamino, dialkylamino, alkyloxy, hydroxy, alkylthio, alkenyl, alkynyl, cyano, --SO.sub.2 R.sub.17 where R.sub.17 is alkyl, or --SO.sub.2 NR.sub.18 R.sub.19 where R.sub.18 and R.sub.19 are independently H or alkyl;provided that at least two of R.sub.12, R.sub.13, R.sub.14, R.sub.15 and R.sub.16 are H, and that if only two of R.sub.12, R.sub.13, R.sub.14, R.sub.15, and R.sub.16 are H, the non-hydrogen substituents are not all adjacent; orR.sub.12, R.sub.15, and R.sub.16 are H and R.sub.13 and R.sub.14 together are --OCH.sub.2 O--;R.sub.20 is a group represented by formula (U), (V) or (W): ##STR77## where: R.sub.22 is H, halo, alkyl, cyano, trifluoromethyl, hydroxy, alkyloxy, or --CO.sub.2 R.sub.27 where R.sub.27 is H or alkyl;one of R.sub.23, R.sub.24, and R.sub.25 is R.sub.30 ; andeither all the remaining R.sub.23, R.sub.24, R.sub.25, and R.sub.26 are H; or one of the remaining R.sub.23, R.sub.24, R.sub.25, and R.sub.26 is halo, alkyl, cyano, trifluoromethyl, hydroxy, or alkyloxy; andR.sub.30 is --OH*, --NHH*, --NH*CHO, --NH*C(X)R.sub.31, --NH*SO.sub.2 R.sub.31, --NH*C(X)NR.sub.32 R.sub.33, or --NH*SO.sub.2 NR.sub.32 R.sub.34,where:H* is hydrogen, optionally replaced by an in vivo hydrolyzable protecting group;R.sub.31 is alkyl, haloalkyl, hydroxyalkyl, alkenyl, benzyl, aryl, cycloamino, --CH.sub.2 SO.sub.2 Me, or --(CH.sub.2).sub.n R.sub.35, where n is an integer from 2 to 5 and R.sub.35 is alkylamino, dialkylamino, cycloamino, alkyloxy, acyloxy, or --CO.sub.2 R.sub.27 ;R.sub.32 is H, alkyl, or --(CH.sub.2).sub.n OR.sub.27 ;R.sub.33 is H, alkyl, haloalkyl, aryl, hydroxyalkyl, tetrahydrofuran-2-ylmethyl, --CH.sub.2 CO.sub.2 R.sub.27, or --(CH.sub.2).sub.n R.sub.35 ; andR.sub.34 is H, alkyl, acetyl, hydroxyalkyl, or --(CH.sub.2).sub.n R.sub.35 ;and their pharmaceutically acceptable salts.