Patent ID: 6630493
Filing Date: 2003-10-07
Classification: A61P,C07D

Abstract:
An amide of the general formula I and its tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the following meanings:R1 is selected from the group consisting of phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyrazyl, pyridazyl, imidazolyl, thiazole, quinazyl, isoquinolyl, quinazyl, quinoxalyl, thienyl, benzothienyl, benzofuranyl, furanyl, and indolyl, where the rings can be additionally substituted by up to 3 radicals R5, R2 is selected from the group consisting of chlorine, bromine, fluorine, C1-C6-alkyl, C1-C6-alkenyl, C1-C6-alkynyl, C1-C6-alkylphenyl, C1-C6-alkenylphenyl, C1-C6-alkynylphenyl, phenyl, NHCOâ€”C1-C4-alkyl, NHSO2â€”C1-C4-alkyl, â€”NHCOphenyl â€”NHCO-naphthyl, NO2, â€”Oâ€”C1-C4-alkyl and NH2, where the aromatic rings can additionally carry one or two radicals R5 and two radicals R2 together can also be a chain â€”CH&boxH;CHâ€”CH&boxH;CHâ€” and thus form a fused benzo ring, which can be substituted by one R5, R3 is â€”C1-C6-alkyl, which is branched or unbranched, and which can additionally carry an Sâ€”CH3 radical or a phenyl, cyclohexyl, cycloheptyl, cyclopentyl, indolyl, pyridyl or naphthyl ring which is substituted by at most two radicals R5, where R5 is selected from the group consisting of hydrogen, C1-C4-alkyl, which is branched or unbranched, â€”Oâ€”C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COOâ€”C1-C4-alkyl, â€”NHCOâ€”C1-C4-alkyl, â€”NHCO-phenyl, â€”NHSO2â€”C1-C4-alkyl, â€”NHSO2-phenyl, â€”SO2â€”C1-C4-alkyl, â€”(CH2)nâ€”NR12R13 and â€”SO2-phenyl, X is selected from the group consisting of a bond, â€”(CH2)mâ€”, â€”(CH2)mâ€”Oâ€”(CH2)oâ€”, â€”(CH2)o-Sâ€”(CH2)mâ€”, â€”(CH2)oâ€”SOâ€”(CH2)mâ€”, â€”(CH2)oâ€”SO2â€”(CH2)mâ€”, â€”CH&boxH;CHâ€”, â€”CbCâ€”, â€”COâ€”CH&boxH;CHâ€”, â€”(CH2)oâ€”COâ€”(CH2)mâ€”, â€”(CH2)mâ€”NHCOâ€”(CH2)oâ€”(CH2)mâ€”CONHâ€”(CH2)oâ€”, â€”(CH2)mâ€”NHSO2â€”(CH2)oâ€”, â€”NHâ€”COâ€”CH&boxH;CHâ€”, â€”(CH2)mâ€”SO2NHâ€”(CH2)oâ€”, â€”CH&boxH;CHâ€”CONHâ€” and and in the case of CH&boxH;CH double bonds can be either the E or the Z form and R1-X together are also Y is pyridine, and R4 is selected from the group consisting of hydrogen, COOR6, COâ€”Z, in which Z is NR7R8, R6 is hydrogen or C1-C6-alkyl, which is linear or branched, and which can be substituted by a phenyl ring which itself can additionally be substituted by one or two radicals R9, R7 is hydrogen or C1-C6-alkyl, which is branched and unbranched, R8 is hydrogen or C1-C6-alkyl, which is branched or unbranched which can additionally be substituted by a phenyl ring which can additionally carry a radical R9, and by R9 is selected from the group consisting of hydrogen, C1-C4-alkyl, which is branched or unbranched, â€”Oâ€”C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COOâ€”C1-C4-alkyl, â€”NHCOâ€”C1-C4-alkyl, â€”NHCO-phenyl, â€”NHSO2â€”C1-C4-alkyl, â€”NHSO2-phenyl, â€”SO2â€”C1-C4-alkyl and â€”SO2-phenyl, R10 is hydrogen or C1-C6-alkyl, which is linear or branched, and which can be substituted by a phenyl ring which itself can additionally be substituted by one or two radicals R9, R11 is hydrogen or C1-C6-alkyl, which is linear or branched, and which can be substituted by a phenyl ring which itself can additionally be substituted by one or two radicals R9, n is a number 0, 1 or 2, and m and o independently of one another are each a numeral 0, 1, 2, 3 or 4.