Patent ID: 6329379
Filing Date: 2001-12-11
Classification: A61K,A61P,C07D,C07K,C12P

Abstract:
A racemate, diastereoisomer or optical isomer of a compound of formula (I): ##STR318##whereinB is H, a C.sub.6 or C.sub.10 aryl, C.sub.7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C.sub.1-6 alkyl; C.sub.1-6 alkoxy; C.sub.1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C.sub.1-6 alkyl; amido; or (lower alkyl)amide;or B is an acyl derivative of formula R.sub.4 --C(O)--; a carboxyl derivative of formula R.sub.4 --O--C(O)--; an amide derivative of formula R.sub.4 --N(R.sub.5)--C(O)--; a thioamide derivative of formula R.sub.4 --N(R.sub.5)--C(S)--; or a sulfonyl derivative of formula R.sub.4 --SO.sub.2 whereinR.sub.4 is(i) C.sub.1-10 alkyl optionally substituted with carboxyl, C.sub.1-6 alkanoyl, hydroxy, C.sub.1-6 alkoxy, amino optionally mono- or di-substituted with C.sub.1-6 alkyl, amido, or (lower alkyl) amide;(ii) C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkoxy, or C.sub.4-10 alkylcycloalkyl, all optionally substituted with hydroxy, carboxyl, (C.sub.1-6 alkoxy)carbonyl, amino optionally mono- or di-substituted with C.sub.1-6 alkyl, amido, or (lower alkyl) amide;(iii) amino optionally mono- or di-substituted with C.sub.1-6 alkyl; amido; or (lower alkyl)amide;(iv) C.sub.6 or C.sub.10 aryl or C.sub.7-16 aralkyl, all optionally substituted with C.sub.1-6 alkyl, hydroxy, amido, (lower alkyl)amide, or amino optionally mono- or di-substituted with C.sub.1-6 alkyl; or(v) Het or (lower alkyl)-Het, both optionally substituted with C.sub.1-6 alkyl, hydroxy, amido, (lower alkyl) amide, or amino optionally mono- or di-substituted with C.sub.1-6 alkyl;R.sub.5 is H or C.sub.1-6 alkyl; with the proviso that when B is a carboxyl derivative, an amide derivative or a thioamide derivative, R.sub.4 is not a cycloalkoxy;Y is H or C.sub.1-6 alkyl;R.sup.3 is C.sub.1-8 alkyl, C.sub.3-7 cycloalkyl, or C.sub.4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 thioalkyl, amido, (lower alkyl)amido, C.sub.6 or C.sub.10 aryl, or C.sub.7-16 aralkyl;R.sup.2 is CH.sub.2 --R.sub.20, NH--R.sub.20, O--R.sub.20 or S--R.sub.20, wherein R.sub.20 is pyrimidinyl, quinazolinyl, (lower alkyl)-pyrimidinyl or (lower alkyl)-quinazolinyl, each optionally mono-, di- or tri-substituted with R.sub.21,wherein each R.sub.21 is independently C.sub.1-6 alkyl; C.sub.1-6 alkoxy; lower thioalkyl; sulfonyl; NO.sub.2 ; OH; SH; halo; haloalkyl; amino optionally mono- or di-substituted with C.sub.1-6 alkyl, C.sub.6 or C.sub.10 aryl, C.sub.7-14 aralkyl, Het or (lower alkyl)-Het; amido optionally mono-substituted with C.sub.1-6 alkyl, C.sub.6 or C.sub.10 aryl, C.sub.7-14 aralkyl, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C.sub.6 or C.sub.10 aryl, C.sub.7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted with R.sub.22 ;wherein R.sub.22 is C.sub.1-6 alkyl; C.sub.3-7 cycloalkyl; C.sub.1-6 alkoxy; amino optionally mono- or di-substituted with C.sub.1-6 alkyl; sulfonyl; (lower alkyl)sulfonyl; NO.sub.2 ; OH; SH; halo; haloalky; carboxyl; amide; (lower alkyl)amide; or Het optionally substituted with C.sub.1-6 alkyl;R.sup.1 is H; C.sub.1-6 alkyl, C.sub.3-7 cycloalkly, or C.sub.2-6 alkynyl, all optionally substituted with halogen;or a pharmaceutically acceptable salt or ester thereof;wherein ""Het"" is defined as a five-membered saturatd or unsaturated, aromatic or non-aromatic, heterocycle containing from one to four heteroatoms selected from nitrogen, oxygen and sulfur, wherein said heterocycle is optionally fused to a benzene ring.