Patent ID: 6500803
Filing Date: 2002-12-31
Classification: A61K,A61P,C07K

Abstract:
A compound of formula I, wherein:r is 0, 1, 2, or 3; s is 0, 1, 2, 3, or 4; t is 0, 1, or 2; R1 is selected from hydrogen, R11â€”COâ€”, and R12â€”SO2â€”; R11 is selected from (C1-C8)-alkyl, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C4)-alkyl-, Het-, Het-(C1-C4)-alkyl-, (C1-C8)-alkyloxy-, (C6-C14)-aryloxy-, (C6-C14)-aryl-(C1-C4)-alkyloxy-, amino, (C1-C8)-alkylamino-, (C6-C14)-arylamino-, and (C6-C14)-aryl-(C1-C4)-alkylamino-, where all these groups are unsubstituted or substituted by one or more identical or different R40 substituents or R11 is hydrogen; R12 is selected from (C1-C8)-alkyl, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C4)-alkyl- Het-, Het-(C1-C4)-alkyl-, di((C1-C8)-alkyl)amino-, and di((C6-C14)-aryl-(C1-C4)-alkyl)amino-, where all these groups are unsubstituted or substituted by one or more identical or different R40 substituents; R2 is hydrogen R21(R22)CHâ€”, R23â€”Het-(CH2)kâ€”, R23(R24)Nâ€”(CH2)mâ€”Dâ€”(CH2)nâ€”, or R25(R26)Nâ€”COâ€”(CH2)pâ€”Dâ€”(CH2)qâ€”, wherein D is a divalent â€”C(R31)(R32)â€” residue, a divalent (C6-C14)-arylene residue, or a divalent residue of an aromatic Het group containing 5 to 10 ring atoms of which 1, 2, 3, or 4 are identical or different ring heteroatoms selected from nitrogen, oxygen, and sulfur, and the numbers k, m, n, p, and q which are independent of each other and can be identical or different are 0, 1, 2, 3, 4, or 5, with the proviso that when D is â€”C(R31)(R32)â€”, the sum m+n cannot be 0 and the sum p+q cannot be 0; R21 and R22 which are independent of each other and can be identical or different are selected from hydrogen, (C1-C12)-alkyl, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C4)-alkyl-, Het-, and Het-(C1-C4)-alkyl-, where all these groups are unsubstituted or substituted by one or more identical or different substituents selected from R40, (C1-C8)-alkylamino-, di-((C1-C8)-alkyl)-amino-, (C6-C14)-aryl-(C1-C4)-alkylamino-, (C6-C14)-arylamino-, aminocarbonyl-, and aminocarbonyl-(C1-C8)-alkyl-, or R21 and R22 together with the carbon atom to which they are bonded form a saturated or unsaturated 3-membered to 8-membered carbocyclic ring which can be condensed to one or two ring systems which are heteroaromatic rings containing 5 to 10 ring atoms of which 1, 2, or 3 are identical or different heteroatoms selected from nitrogen, oxygen, and sulfur, and/or (C6-C10) carbocyclic aromatic rings, where the resulting R21(R22)CHâ€” group is unsubstituted or substituted by one or more identical or different substituents selected from R40, (C1-C8)-alkylamino-, di-((C1-C8)-alkyl)-amino-, (C6-C14)-aryl-(C1-C4)-alkylamino-, (C6-C14)-arylamino-, aminocarbonyl-, and aminocarbonyl-(C1-C8)-alkyl-; R23 is hydrogen, R27â€”SO2â€”, or R28â€”COâ€”; R24 is selected from hydrogen, (C1-C8)-alkyl, (C6-C14)-aryl, and (C6-C14)-aryl-(C1-C4)-alkyl-; R25 and R26 which are independent of each other and can be identical or different are selected from hydrogen, (C1-C8)-alkyl, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C4)-alkyl-, Het-, and Het-(C1-C4)-alkyl-, where all these groups are unsubstituted or substituted by one or more identical or different R40 substituents; R27 is selected from (C1-C8)-alkyl, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C4)-alkyl-, Het-, (C1-C4)-alkyl-, amino, (C1-C8)-alkylamino-, di-((C1-C8)-alkyl)amino-, (C6-C14)-arylamino-, and (C6-C14)-aryl-(C1-C4)-alkylamino-, where all these groups are unsubstituted or substituted by one or more identical or different R40 substituents; R28 is selected from R27, (C1-C8)-alkyloxy-, (C6-C14)-aryloxy-, and (C6-C14)-aryl-(C1-C4)-alkyloxy-, where all these groups are unsubstituted or substituted by one or more identical or different R40 substituents; R31 and R32 which are independent of each other and can be identical or different are selected from hydrogen, (C1-C12)-alkyl, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C4)-alkyl-, Het-, and Het-(C1-C4)-alkyl-, where all these groups are unsubstituted or substituted by one or more identical or different R40 substituents; R40 is selected from halogen, hydroxy, (C1-C8)-alkyloxy-, (C6-C14)-aryl-(C1-C8)-alkyloxy-, (C6-C14)-aryloxy-, (C1-C8)-alkyl, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C8)-alkyl-, (C1-C8)-alkylsulfonyl-, trifluoromethyl, acetylamino-, amino, amidino, guanidino, oxo, nitro, and cyano, where the R40 groups are independent of each other and can be identical or different; R91, R92, and R93 which are independent of each other and can be identical or different are selected from hydrogen, (C1-C8)-alkyl, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C4)-alkyl-, Het-, and Het-(C1-C4)-alkyl-; R94 is selected from (C1-C4)-alkyl, (C6-C14)-aryl, amino, nitro, halogen, trifluoromethyl, hydroxy, and (C1-C4)-alkyloxy-, where the R94 groups are independent of each other and can be identical or different; R95 is selected from amidino, guanidino, ((C1-C4)-alkyl)oxycarbonylamidino-, ((C1-C4)-alkyl)oxycarbonylguanidino-, and hydroxyamidino-; R96 is selected from hydrogen, R98â€”(C1-C8)-alkyl-, R98-(C6-C14)-aryl-, R98â€”(C6-C14)-aryl-(C1-C4)-alkyl-, R98â€”Het-, and R98â€”Het-(C1-C4)-alkyl-; R97 is selected from R99â€”(C1-C8)-alkyl-, R99â€”(C6-C14)-aryl-, R99â€”(C6-C14)-aryl-(C1-C4)-alkyl-, R99â€”Het-, and R99â€”Het-(C1-C4)-alkyl-; R98 and R99 which are independent of each other and can be identical or different are selected from hydroxycarbonyl-, (C1-C8)-alkyloxycarbonyl-, (C6-C14)- aryloxycarbonyl-, (C6-C14)-aryl-(C1-C4)-alkyloxycarbonyl-, aminocarbonyl-, (C1-C8)-alkylaminocarbonyl-, tetrazolyl, â€”P(O)(OH)2, â€”S(O)2OH, and â€”S(O)2NH2; Het is a saturated, partially unsaturated, or aromatic monocyclic or bicyclic heterocyclic ring system containing 3 to 10 ring atoms of which 1, 2, 3, or 4 are identical or different heteroatoms selected from nitrogen, oxygen, and sulfur; or a stereoisomer of formula I, or a salt of formula I, or mixtures of any of the foregoing.