Patent ID: 6410531
Filing Date: 2002-06-25
Classification: A61K,A61P,C07D,C07K,C12P

Abstract:
The racemates, diastereoisomers or optical isomers of a compound of formula (I): whereinB is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4â€”C(O)â€”; a carboxyl derivative of formula R4â€”Oâ€”C(O)â€”; an amide derivative of formula R4â€”N(R5)â€”C(O)â€”; a thioamide derivative of formula R4â€”N(R5)â€”C(S)â€”; or a sulfonyl derivative of formula R4â€”SO2 wherein R4 is (i) C1-10 alkyl optionally substituted with carboxyl, C1-6 alkanoyl, hydroxy, C1-6 alkoxy, amino optionally mono-or di-substituted with C1-6 alkyl, amido, or (lower alkyl) amide; (ii) C3-7 cycloalkyl, C3-7 cycloalkoxy, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, carboxyl, (C1-6 alkoxy)carbonyl, amino optionally mono-or di-substituted with C1-6 alkyl, amido, or (lower alkyl) amide; (iii) amino optionally mono- or di-substituted with C1-6 alkyl; amido; or (lower alkyl)amide; (iv) C6 or C10 aryl or C7-16 aralkyl, all optionally substituted with C1-6 alkyl, hydroxy, amido, (lower alkyl)amide, or amino optionally mono-or di-substituted with C1-6 alkyl; or (v) Het or (lower alkyl)-Het, both optionally substituted with C1-6 alkyl, hydroxy, amido, (lower alkyl) amide, or amino optionally mono-or di-substituted with C1-6 alkyl; R5 is H or C1-6 alkyl; with the proviso that when B is a carboxyl derivative, an amide derivative or a thioamide derivative, R4 is not a cycloalkoxy; Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2â€”R20, NHâ€”R20, Oâ€”R20 or Sâ€”R20, wherein R20 is pyridinyl, quinolyl, (lower alkyl)-pyridinyl or (lower alkyl)-quinolyl, each optionally mono-, di- or tri-substituted with R21, wherein each R21 is independently C1-6 alkyl; C1-6 alkoxy; lower thioalkyl; sulfonyl; NO2; OH; SH; halo; haloalkyl; amino optionally mono-or di-substituted with C1-6 alkyl, C6 or C10 aryl, C7-14 aralkyl, Het or (lower alkyl)-Het; amido optionally mono-substituted with C1-6 alkyl, C6 or C10 aryl, C7-14 aralkyl, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6 or C10 aryl, C7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted with R22; wherein R22 is C1-6 alkyl; C3-7 cycloalkyl; C1-6 alkoxy; amino optionally mono- or di-substituted with C1-6 alkyl; sulfonyl; (lower alkyl)sulfonyl; NO2; OH; SH; halo; haloalkyl; carboxyl; amide; (lower alkyl)amide; or Het optionally substituted with C1-6 alkyl; R1 is H; C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, or C2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof;wherein at least one â€œHetâ€  group is present in the compound of formula (I) and â€œHetâ€  is defined as a six- or seven-membered saturated or unsaturated aromatic or heterocycle containing from one to four heteroatoms selected from nitrogen, oxygen and sulfur, wherein said heterocycle is optionally fused to a benzene ring.