Patent ID: 6423712
Filing Date: 2002-07-23
Classification: A61K,A61P,C07K,Y02A

Abstract:
A compound of the formula I, in whichW is R1â€”Aâ€”C(R13); Z is oxygen or sulfur; A is a direct bond or (C1-C2)-alkylene; B is a divalent radical selected from the group consisting of (C1-C6)-alkylene, (C2-C6)-alkenylene, phenylene, phenylene-(C1-C3)-alkyl, (C1-C3)-alkenylphenyl, where the divalent (C1-C6)-alkylene radical is unsubstituted or substituted by a radical selected from the group consisting of (C1-C8)-alkyl, (C2-C8)-alkenyl, (C2-C8)-alkynyl, (C3-C10)-cycloalkyl, (C3-C10)-cycloalkyl-(C1-C6)-alkyl, unsubstituted or substituted (C6-C14)-aryl, (C6-C14)-aryl-(C1-C6)-alkyl unsubstituted or substituted in the aryl radical, unsubstituted or substituted heteroaryl, and heteroaryl-(C1-C6)-alkyl unsubstituted or substituted in the heteroaryl radical; E is tetrazolyl, (R8O)2P(O), HOS(O)2, R9NHS(O)2 or R10CO; R is hydrogen, (C1-C8)-alkyl, (C3-C12)-cycloalkyl, (C3-C12)-cycloalkyl-(C1-C8)-alkyl, unsubstituted or substituted (C6-C14)-aryl, (C6-C14)-aryl-(C1-C8)-alkyl unsubstituted or substituted in the aryl radical, unsubstituted or substituted heteroaryl, or heteroaryl-(C1-C8)-alkyl unsubstituted or substituted in the heteroaryl radical; R0 is (C3-C12)-cycloalkyl, (C3-C12)-cycloalkyl-(C1-C8)-alkyl, (C6-C12)-bicycloalkyl, (C6-C12)-bicycloalkyl-(C1-C8)-alkyl, (C6-C12)-tricycloalkyl, (C6-C12)-tricycloalkyl-(C1-C8)-alkyl, unsubstituted or substituted (C6-C14)-aryl, C6-C14-aryl-(C1-C8)-alkyl unsubstituted or substituted in the aryl radical, unsubstituted or substituted heteroaryl, heteroaryl-(C1-C8)-alkyl unsubstituted or substituted in the heteroaryl radical, Hâ€”CO, (C1-C8)-alkyl-CO, (C3-C12)-cycloalkyl-CO, (C3-C12)-cycloalkyl-(C1-C8)-alkyl-CO, (C6-C12)-bicycloalkyl-CO, (C6-C12)-bicycloalkyl-(C1-C8)-alkyl-CO, (C6-C12)-tricycloalkyl-CO, (C6-C12)-tricycloalkyl-(C1-C8)-alkyl-CO, unsubstituted or substituted (C6-C14)-aryl-CO, (C6-C14)-aryl-(C1-C8)-alkyl-CO unsubstituted or substituted in the aryl radical, unsubstituted or substituted heteroaryl-CO, heteroaryl-(C1-C8)-alkyl-CO unsubstituted or substituted in the heteroaryl radical, (C1-C8)-alkyl-S(O)n, (C3-C12)-cycloalkyl-S(O)n, (C3-C12)-cycloalkyl-(C1-C8)-alkyl-S(O)n, (C6-C12)-bicycloalkyl-S(O)n, (C6-C12)-bicycloalkyl- (C1-C8)-alkyl-S(O)n, (C6-C12)-tricycloalkyl-S(O)n, (C6-C12)-tricycloalkyl-(C1-C8)-alkyl-S(O)n, unsubstituted or substituted (C6-C14)-aryl-S(O)n, (C6-C14)-aryl-(C1-C8)-alkyl-S(O)n unsubstituted or substituted in the aryl radical, unsubstituted or substituted heteroaryl-S(O)n or heteroaryl-(C1-C8)-alkyl-S(O)n unsubstituted or substituted in the heteroaryl radical, where n is 1 or 2; R1 is an unsubstituted or substituted radical selected from the group consisting of phenyl, furyl, thienyl, pyrrolyl, imidazolyl, and pyridyl, where each of these radicals is or is not benzo-fused; R2 is hydrogen, (C1-C8)-alkyl, unsubstituted or substituted (C6-C14)-aryl, (C6-C14)-aryl-(C1-C8)-alkyl unsubstituted or substituted in the aryl radical or (C3-C8)-cycloalkyl; R3 is hydrogen, (C1-C8)-alkyl, unsubstituted or substituted (C6-C14)-aryl, (C6-C14)-aryl-(C1-C8)-alkyl unsubstituted or substituted in the aryl radical, unsubstituted or substituted heteroaryl, heteroaryl-(C1-C8)-alkyl unsubstituted or substituted in the heteroaryl radical, (C3-C8)-cycloalkyl, (C3-C8)-cycloalkyl-(C1-C8)-alkyl, (C6-C12)-bicycloalkyl, (C6-C12)-bicycloalkyl-(C1-C8)-alkyl, (C6-C12)-tricycloalkyl, (C6-C12)-tricycloalkyl-(C1-C8)-alkyl, (C2-C8)-alkenyl, (C2-C8)-alkynyl or R11NH; R8 is hydrogen, (C1-C18)-alkyl, unsubstituted or substituted (C6-C14)-aryl or (C6-C14)-aryl-(C1-C8)-alkyl which is unsubstituted or substituted in the aryl radical; R9 is hydrogen, aminocarbonyl, (C1-C18)-alkylaminocarbonyl, (C3-C8)-cycloalkylaminocarbonyl, unsubstituted or substituted (C6-C14)-arylaminocarbonyl, (C1-C18)-alkyl, unsubstituted or substituted (C6-C14)-aryl or (C3-C8)-cycloalkyl; R10 is hydroxyl, (C1-C18)-alkoxy, (C6-C14)-aryl-(C1-C8)-alkoxy which is unsubstituted or substituted in the aryl radical, unsubstituted or substituted (C6-C14)-aryloxy, (C1-C8)-alkylcarbonyloxy-(C1-C6)-alkoxy, (C6-C14)-arylcarbonyloxy-(C1-C6)-alkoxy, amino or mono- or di((C1-C18)-alkyl)-amino; R11 is hydrogen, R12a, R12aâ€”CO, Hâ€”CO, R12aâ€”Oâ€”CO, R12bâ€”CO, R12bâ€”CS, R12aâ€”S(O)2 or R12bâ€”S(O)2; R12a is (C1-C18)-alkyl, (C2-C8)-alkenyl, (C2-C8)-alkynyl, (C3-C12)-cycloalkyl, (C3-C12)-cycloalkyl-(C1-C8)-alkyl, unsubstituted or substituted (C6-C14)-aryl, (C6-C14)-aryl-(C1-C8)-alkyl unsubstituted or substituted in the aryl radical, unsubstituted or substituted heteroaryl, heteroaryl-(C1-C8)-alkyl unsubstituted or substituted in the heteroaryl radical, or the radical R15; R12b is amino, di-((C1-C18)-alkyl)-amino, or R12aâ€”NH; R13 is (C1-C6)-alkyl, unsubstituted or substituted (C6-C14)-aryl, (C6-C14)-aryl-(C1-C6)-alkyl unsubstituted or substituted in the aryl radical, (C3-C8)-cycloalkyl, or (C3-C8)-cyclo-(C1-C6)-alkyl; R15 is R16-(C1-C6)-alkyl or R16; R16 is a 6-membered to 24-membered bicyclic or tricyclic radical which is saturated or partially unsaturated and which contains none or one, two, three, or four identical or different additional heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur and which is unsubstitueted or substitueted by one or more identical or different substituents selected from the group consisting of (C1-C4)-alkyl and oxo; and e and h independently of one another are 0 or 1; in any of its steroisomeric forms or mixtures thereof in any ratio, or a physiologically tolerable salt of the compound.