Patent ID: 6451781
Filing Date: 2002-09-17
Classification: A61P,C07J

Abstract:
A compound of the formula I in which:T1 and T2 independently of one another are or hydrogen, where T1 and T2 cannot simultaneously be hydrogen; Z is A is a bond, (C1-C4)-alkyl, or (C0-C4)-alkyl-X; X is â€”Oâ€”, â€”COâ€”, â€”CH[OH]â€”, â€”CH[OCH3]â€”, â€”SO(0-2)â€”, â€”NHâ€”, or â€”N(CH3)â€”; D is phenylene which is not substituted or is substituted by 1-3 substituents selected from the group consisting of F, Cl, â€”CF3, (C1-C4)-alkyl, hydroxyl, methoxy, â€”NH2, NHCH3, N(CH3)2, CH3SO2â€” and H2NO2Sâ€”; R(A), R(B), R(C), R(D), R(E), R(F) independently of one another are hydrogen, F, Cl, Br, I, CN, OH, OR(6), NR(7)R(8), (C1-C8)-alkyl, Oâ€”(C1-C12)-alkyl, or (C3-C8)-cycloalkyl, it being possible in the alkyl radicals for one, a number or all hydrogens to be replaced by fluorine; R(6) is (C3-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl or benzyl, it being possible for the phenyl nucleus to be up to trisubstituted by F, Cl, CF3, methyl, methoxy, and/or NR(9)R(10); R(9), R(10) independently of one another are H, (C1-C4)-alkyl or (C1-C4)-perfluoroalkyl; R(7) and R(8) independently of one another are (C1-C4)-alkyl, (C3-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl or benzyl, it being possible for the phenyl nucleus to be up to trisubstituted by F, Cl, CF3, methyl, methoxy, and/or NR(9)R(10); or R(7) and R(8) together form a chain of 4 or 5 methylene groups, of which one CH2 group can be replaced by oxygen, sulfur, NH, Nâ€”CH3 or N-benzyl; s is zero or 1, x is zero, 1 or 2; y is zero, 1 or 2; R(1), R(2), R(3) independently of one another are hydrogen, F, Cl, Br, I, CN, â€”(C&boxH;O)â€”N&boxH;C(NH2)2, â€”SO(0-1)â€”(C1-C8)-alkyl, Oâ€”(C0-C4)-alkylphenyl, â€”(C0-C4)-alkylphenyl, it being possible for the phenyl nucleus to be up to trisubstituted by F, Cl, CF3, methyl, methoxy, and/or â€”(C0-C4)-alkyl-NR(21)R(22); (C1-C8)-alkyl, Oâ€”(C1-C12)-alkyl, or (C3-C8)-cycloalkyl, it being possible in the alkyl radicals for one, a number or all hydrogens to be replaced by fluorine; R(21), R(22) independently of one another are H or (C1-C4)-alkyl; L is (C1-C15)-alkyl, it being possible for one or more (CH2) groups to be replaced by â€”CH&boxH;CHâ€”, â€”Câ‰¡Câ€”, â€”Oâ€”, â€”NR(47)-, â€”NR(48)-, â€”COâ€”, and/or â€”SO2â€”; R(47) is hydrogen, (C1-C8)-alkyl, R(48)-COâ€”, phenyl, or benzyl; R(48) is hydrogen, (C1-C8)-alkyl, phenyl, or (CH2)-phenyl, it being possible for the phenyl nucleus to be up to trisubstituted by F, Cl, CF3, methyl, and/or methoxy; R(40) to R(45) independently of one another are H, â€”O R(50), â€”S R(50), NH R(50), â€”N R(50)2, â€”Oâ€”(CO)â€” R(50), â€”Sâ€”(CO)â€” R(50), â€”NHâ€”(CO)â€” R(50), â€”Oâ€”POâ€”(O R(50))-O R(50), â€”Oâ€”(SO2)â€”O R(50), â€”R(50), a bond to L; or R(40) and R(41), R(42) and R(43), R(44) and R(45) in each case together are the oxygen of a carbonyl group; just one of the radicals always having the meaning of a bond to L; R(50) is hydrogen, (C1-C4)-alkyl, phenyl, or (CH2)-phenyl, it being possible for the phenyl nucleus to be up to trisubstituted by F, Cl, CF3, methyl, and/or methoxy; K is â€”OR(51), â€”NH(R51), â€”N(R51)2, â€”HNâ€”CH2â€”CH2â€”CO2H, â€”HNâ€”CH2â€”CH2â€”SO3H, â€”N(CH3)CH2CO2H, â€”HNâ€”CH(R46)CO2H, or â€”OKa, Ka being a cation; R(46) is hydrogen, C1-C4-alkyl, benzyl, â€”CH2â€”OH, H3CSCH2CH2â€”, HO2CCH2â€”, or HO2CCH2CH2â€”; R(51) is H, (C1-C4)-alkyl, phenyl, or (CH2)-phenyl, it being possible for the phenyl radical to be up to trisubstituted by F, Cl, CF3, methyl, and/or methoxy; or a pharmaceutically tolerable salt or physiologically functional derivative thereof.