Patent ID: 6476059
Filing Date: 2002-11-05
Classification: A61P,C07D,Y10S

Abstract:
A method for the treatment of obesity comprising administering to a patient in need thereof an obesity treating effective amount of a pharmaceutical composition comprising a compound of formula I in whichY is a direct linkage, CH2 or CH2â€”CH2; X is CH2, O, NH, NR6 or S; R1, R1â€² are independently H, F, Cl, Br, I, CF3, CN, NO2, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, Oâ€”(C1-C6)-alkyl (wherein one, more than one or all hydrogen(s) in the alkyl, alkenyl and alkynyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, Oâ€”CH2â€”Ph, NH2, NHâ€”COâ€”CH3 or N(COOCH2Ph)2), SO2â€”NH2, SO2NH(C1-C6)-alkyl, SO2N((C1-C6)-alkyl)2, Sâ€”(C1-C6)-alkyl, Sâ€”(CH2)n-phenyl, SOâ€”(C1-C6)-alkyl, SOâ€”(CH2)n-phenyl, SO2â€”(C1-C6)-alkyl, SO2â€”(CH2)n-phenyl (wherein n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, OH, CF3, NO2, CN, OCF3, Oâ€”(C1-C6)-alkyl, (C1-C6)-alkyl or NH2), NH2, NHâ€”(C1-C6)-alkyl, N((C1-C6)-alkyl)2, NH(C1-C7)-acyl, phenyl, biphenylyl, Oâ€”(CH2)n-phenyl (wherein n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl or thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, Oâ€”(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2â€”CH3, COOH, COOâ€”(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl); R2 is NH2, NHR3 or NR4R5, wherein R3 is (C1-C6)alkyl, CN, CHO, COâ€”NH2, CH&boxH;NH, C(S)â€”NH2, C(&boxH;NH)â€”NH-phenyl (wherein the phenyl ring may be optionally substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, Oâ€”(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2â€”CH3, COOH, COOâ€”(C1-C6)-alkyl or CONH2), phenyl or CH2-phenyl (wherein the phenyl ring may be optionally substituted up to 3 times by F, Cl, Br, I, OH, NO2, CN, OCF3, Oâ€”(C2-C6)-alkyl, (C2-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2â€”CH3, COOH, COOâ€”(C1-C6)-alkyl or CONH2), biphenylyl, 1- or 2-naphthyl, 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl, 5-tetrazolyl (wherein the biphenylyl, naphthyl, pyridyl, furanyl or thienyl rings may be optionally substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, Oâ€”(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2â€”CH3, COOH, COOâ€”(C1-C6)-alkyl or CONH2), CH2-phenyl, CH2-2-pyridyl or CH2-4-pyridyl (wherein the phenyl or pyridyl ring may be optionally substituted once or twice by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, Oâ€”(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2â€”CH3, COOH, COOâ€”(C1-C6)-alkyl or CONH2); R4 is (C1-C6)-alkyl, (C3-C6)-cycloalkyl, (C2-C6)-alkenyl, (C3-C6)-alkynyl, phenyl or CH2-phenyl (wherein the phenyl ring may be optionally substituted once or twice by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, Oâ€”(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2â€”CH3, COOH, COOâ€”(C1-C6)-alkyl or CONH2); R5 is H, (C1-C6)-alkyl, (C3-C6)-cycloalkyl, (C2-C6)-alkenyl, (C3-C6)-alkynyl, phenyl or CH2-phenyl (wherein the phenyl ring may be optionally substituted once or twice by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, Oâ€”(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2â€”CH3, COOH, COOâ€”(C1-C6)-alkyl or CONH2), or R4 and R5 together form one of the groups CH2â€”CH2â€”CH2â€”CH2â€”CH2, CH2â€”CH2â€”N(CH3)â€”CH2â€”CH2, CH2â€”CH2â€”N(CH2-phenyl)-CH2â€”CH2, CH2â€”CH2â€”Oâ€”CH2â€”CH2 or CH2â€”CH2â€”CH2â€”CH2; and R6 is (C1-C6)alkyl, acyl, (C&boxH;O)â€”(C1-C6)alkyl, (C&boxH;O)â€”(C3-C6)-cycloalkyl, phenyl, naphthyl, pyridyl, â€”SO2-phenyl, or SO2-naphthyl; and their physiologically tolerated salts.