Patent ID: 6743790
Filing Date: 2004-06-01
Classification: A61P,C07C,C07D

Abstract:
A compound of the formula I, wherein m is 0, 1, 2, 3, or 4; n is 0, 1, 2, or 3; A is halogen; X is sulfur or oxygen; R1 is chosen from hydrogen, hydroxy, (C1-C12)-alkoxycarbonyl-,(C6-C14)- aryl-(C1-C4)-alkoxycarbonyl-, and (C6-C14)-aryloxycarbonyl-, wherein each of the aryl groups is unsubstituted or substituted by at least one identical or different substituent chosen from (C1-C12)-alkyl, halogen and (C1-C12)-alkoxy; R2 is chosen from hydrogen, (C1-C12)-alkyl, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C4)-alkyl-, R20-(C6-C12)-alkyl-, R20-(C1-C14)-aryl-, and R20-(C6-C14)-aryl-(C1-C4)-alkyl-, wherein R20 is chosen from hydroxycarbonyl-, aminocarbonyl-, (C1-C12)-alkoxycarbonyl-, and (C6-C14)-aryl-(C1-C4)-alkoxycarbonyl-; R3 is chosen from hydrogen, cyano, hydroxy, and (C1-C12)-alkyl; R4 is chosen from (C1-C12)-alkyl, (C6-C14),-aryl, (C8-C14-aryl-(C1-C4)-alkyl-, Het, and Het-(C1-C4)-alkyl-, wherein the alkyl, aryl and Het groups are unsubstituted or substituted by at least one identical or different substituent R10; R5 is chosen from hydrogen, (C1-C12)-alkyl, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C4)-alkyl-, Het, Het-(C1-C4)-alkyl-, (C6-C14)-aryl-(C1-C4)-alkyl-aminocarbonyl-, and Het-(C1-C4)-alkyl-aminocarbonyl-, wherein the alkyl, aryl and Het groups are unsubstituted or substituted by at least one identical or different substituent R10; orR4 and R5 together with the carbon atom to which they are bonded form a saturated or unsaturated 3-membered to 8-membered ring which is a carbocyclic ring or a heterocyclic ring containing 1, 2 or 3 identical or different ring heteroatoms chosen from nitrogen, oxygen and sulfur, and which is optionally condensed to one or two saturated or unsaturated carbocyclic ring systems or heterocyclic ring systems containing 5 to 10 ring atoms of which 1, 2 or 3 are identical or different ring heteroatoms chosen from nitrogen, oxygen and sulfur, wherein the resulting R4(R5)C group is unsubstituted or substituted by at least one identical or different substituent R10; R6 is chosen from hydrogen, hydroxy, (C1-C8)-alkoxy, and (C6-C14)-aryl-(C1-C4)-alkoxy-; R10 is chosen from (C1-C12)-alkyl, (C6-C14)-aryl-(C1-C4)-alkyl-, (C1-C8)-alkoxy, (C1-C4)-alkoxy-(C2-C4)-alkoxy-, (C6-C14)-aryl-(C1-C4)-alkoxy-, (C6-C14)-aryloxy-, Het-oxy-, Het-(C1-C4)-alkoxy-, (C6-C14)-aryl, Het, Het-(C1-C4,-alkyl-, trifluoromethoxy, trifluoromethyl, halogen, oxo, hydroxy, amino, (C1-C12)-alkylcarbonylamino-, aminocarbonylamino-, (C6-C14)-arylcarbonylamino-, Het-carbonylamino-, (C6-C14)-aryl-(C1-C4)-alkylcarbonylamino-, Het-(C1-C4)-alkylcarbonylamino-, (C1-C8)-alkylcarbonyl-, (C6-C14)-arylcarbonyl-, (C1-C8)-alkylaminocarbonyl-, (C6-C14)-arylaminocarbonyl-, (C6-C14-aryl-(C1-C4)-alkylaminocarbonyl-, Het-aminocarbonyl-, Het-(C1-C4)-alkylaminocarbonyl-, aminocarbonyl-, (C1-C8)-alkoxycarbonyl-, hydroxycarbonyl-, cyano, nitro, amidino, acetimino, tri-((C1-C4)-alkyl)ammonio-, (C1-C8)-alkylamino-, di-((C1-C8)-alkyl)amino-, hydroxycarbonylmethoxy-, (C1-C8)-alkylsulfonyl-, (C6-C14)-arylsulfonyl-, (C1-C8)-alkylaminosulfonyl-, (C6-C14)-arylaminosulfonyl-, (C6-C14)-aryl-(C1-C4)-alkylaminosulfonyl-, Het-aminosulfonyl, Het-(C1-C4)-alkylaminosulfonyl-, (C1-C8)-alkylsulfonylamino-, (C6-C14)-arylsulfonylamino-, (C6-C14)-aryl-(C1-C4)-alkylsulfonylamino-, Het-sulfonylamino-, and Het-(C1-C4)-alkylsulfonylamino-, wherein (C1-C12)-alkylcarbonylamino- representing R10 is unsubstituted or substituted in the alkyl group by a substituent chosen from amino, hydroxy and (C1-C4)-alkoxy, and wherein (C1-C12)-alkyl and (C1-C8)-alkoxy representing R10 are unsubstituted or substituted by at least one identical or different substituent chosen from (C1-C8)-alkoxycarbonyl-, hydroxycarbonyl- and aminocarbonyl-, wherein each of the aryl groups and Het group in a group R10 is unsubstituted or substituted by at least one identical or different substituent chosen from halogen, nitro, oxo, hydroxy, (C1-C8)-alkyl, (C1-C8)-alkoxy, (C1-C4)-alkoxy-(C2-C4)-alkoxy-, (C6-C14)-aryloxy-, (C6-C14-aryl-(C1-C4)-alkoxy-, Het-oxy-, Het-(C1-C4)-alkoxy-, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C4)-alkyl-, Het, Het-(C1-C4)-alkyl-, trifluoromethyl, cyano, trifluoromethoxy, (C1-C8)-alkylsulfonyl-, (C1-C8)-alkoxycarbonyl-, hydroxycarbonyl-, aminocarbonyl-, amino, (C1-C8)-alkylamino-, di-((C1-C8)-alkyl)amino-, (C1-C8)-alkylcarbonylamino-, (C6-C14)-aryl-(C1-C4)-alkylcarbonylamino-, (C6-C14)-arylcarbonylamino-, Het-carbonylamino-, Het-(C1-C4)-alkylcarbonylamino-, and (C1-C8)-alkylcarbonyl-, wherein (C1-C8)-alkyl and (C1-C8)-alkoxy representing a substituent on an aryl group or Het group in a group R10 are unsubstituted or substituted by at least one identical or different substituent chosen from (C1-C8)-alkoxycarbonyl-, hydroxycarbonyl- and aminocarbonyl-, with the proviso that, when a substituent R10 is bonded to an alkyl group, it cannot be (C1-C8)-alkoxycarbonyl-, hydroxycarbonyl-, aminocarbonyl-, (C1-C8)-alkylaminocarbonyl-, or (C1-C8)-alkylaminosulfonyl-, and that, when a substituent R10 is bonded to an alkyl group, it cannot be (C1-C8)-alkyl which is substituted by at least one identical or different substituent chosen from (C1-C8)-alkoxycarbonyl-, hydroxycarbonyl- and aminocarbonyl-; Het is a residue of a saturated or unsaturated monocyclic or bicyclic, 3-membered to 10-membered heterocyclic ring system containing 1, 2 or 3 identical or different ring heteroatoms chosen from nitrogen, oxygen and sulfur; or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.