Patent ID: 6340679
Filing Date: 2002-01-22
Classification: A61P,C07D

Abstract:
A compound of the formula I in whichR1 is (C1-C20)-alkyl, (C3-C16)-cycloalkyl, (C3-C16)-cycloalkyl-(C1-C6)-alkyl-, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C6)-alkyl-, (C5-C14)-heteroaryl or (C5-C14)-heteroaryl-(C1-C6)-alkyl-, where the alkyl residue, the cycloalkyl residue, the aryl residue and the heteroaryl residue each is unsubstituted or is substituted by one, two or three identical or different residues R3, and where in the alkyl residue and the cycloalkyl residue one, two or three CH2 groups can be replaced by identical or different groups selected from the series consisting of O, S and NR4; R2 is hydroxy, amino, (C1-C6)-alkoxy, (C1-C6)-alkyl-COâ€”Oâ€”(C1-C4)-alkoxy-, (C3-C16)-cycloalkyloxy, (C3-C16)-cycloalkyl-COâ€”Oâ€”(C1-C4)-alkoxy- or (C6-C14)-aryl-COâ€”Oâ€”(C1-C4)-alkoxy-, where the alkoxy residue, the alkyl residue, the aryl residue and the cycloalkyl residue each is unsubstituted or is substituted by one, two or three identical or different residues from the group consisting of hydroxy, halogen, oxo, CN, (C1-C4)-alkyl-COâ€”, (C1-C4)-alkyl-COâ€”NHâ€”, H2Nâ€”COâ€”, (C1-C4)-alkyl-NHâ€”COâ€”, COOH, â€”COâ€”Oâ€”(C1-C4)-alkyl, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkyl-S(O)2â€”, â€”NR7R7â€² and â€”N+R7R7â€²R7â€³ Qâˆ’, where R7, R7â€² and R7â€³ independently of one another are hydrogen, (C1-C6)-alkyl, (C5-C14)-aryl or (C5-C14)-aryl-(C1-C6)-alkyl- and Qâˆ’ is a physiologically tolerable anion, or R2 is an amino acid residue which is bonded to the CO group carrying the group R2 through an amino group; R3 is (C1-C8)-alkyl, (C3-C12)-cycloalkyl, (C1-C8)-alkoxy, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C4)-alkyl-, halogen, trifluoromethyl, cyano, hydroxy, oxo, nitro, amino, (C1-C4)-alkyl-S(O)2â€”, â€”NHâ€”(C1-C4)-alkyl, â€”N((C1-C4)-alkyl)2, â€”NHâ€”COâ€”(C1-C4)-alkyl, â€”COâ€”(C1-C4)-alkyl, â€”COâ€”NH2, â€”COâ€”NHâ€”(C1-C4)-alkyl, â€”COOH or â€”COâ€”Oâ€”(C1-C4)-alkyl; R4 is hydrogen or (C1-C8)-alkyl; Ar is a 6-membered monocyclic aromatic ring system containing 0, 1, 2, 3, or 4 ring nitrogen atoms which is unsubstituted or substituted with one or more identical or different residues R3; X is CH2, O, NR4 or S; n is zero, one or two; in all its stereoisomeric forms and mixtures thereof in all ratios, and its physiologically tolerable salts.