Patent ID: 6545050
Filing Date: 2003-04-08
Classification: A61P,C07C,Y02P

Abstract:
A compound of the general formula (I)R1â€”Aâ€”Dâ€”Eâ€”Gâ€”Lâ€”R2â€ƒâ€ƒ(I) in whichR1 represents a radical of the formula â€ƒin which a represents a number 1 or 2, and where all of the phenyl ring systems listed above are optionally substituted, optionally geminally, by one or more identical or different substituents selected from the group consisting of: halogen, carboxyl, hydroxyl, phenyl, (C1-C6)-alkoxy, (C1-C6)-alkoxycarbonyl, (C1-C8)-alkyl, which for its part may be substituted by halogen, (C1-C6)-alkylsulphonyloxy, azide, amino, mono(C1-C6)-alkylamino, di(C1-C6)-alkylamino or hydroxyl, a group of the formula â€”(CO)bâ€”NR4R5, in which b represents a number 0 or 1, R4 and R5 are identical or different and independently of one another represent hydrogen, phenyl, (C1-C6)-acyl, cyclo(C4-C7)-acyl benzoyl or (C1-C6)-alkyl, which is optionally substituted by amino, mono(C1-C6)-alkylamino, di(C1-C6)-alkylamino, or R4 and R5 together with the nitrogen atom form a 5- or 6-membered saturated heterocycle which may optionally contain one or more further heteroatom(s) from the group consisting of S and O and/or one or more radical(s) of the formula â€”NR8, in which R8 represents hydrogen, (C1-C6)-alkyl or (C1-C6)-acyl, and a group of the formula â€”NR6â€”SO2â€”R7 in which R6 represents hydrogen, phenyl, (C1-C6)-alkyl or (C1-C6)-acyl, R7 represents phenyl or (C1-C6)-alkyl, Q represents a radical of the formula â€ƒin which c represents a number 1, 2, 3, 4, 5 or 6, R9 and R10 are identical or different and represent hydrogen or (C1-C6)-alkyl, T represents a radical of the formula â€”(CH2)dâ€”, in which d represents a number 1, 2, 3, 4, 5, 6, 7 or 8, or T represents a moiety of an amino acid radical of the formula â€ƒin which R13 and R14 are identical or different and represent hydrogen or methyl, or R13 represents hydrogen or methyl and R14 represents (C3-C8)-cycloalkyl or (C6-C10)-aryl or hydrogen, or (C1-C8)-alkyl, where the (C1-C6)-alkyl is optionally substituted by methlythio, hydroxyl, mercapto, guanidyl or by a group of the formula â€”NR15R16 or â€”NR17â€”OCâ€”, in which R15 and R16 independently of one another represent hydrogen, (C1-C8)-alkyl or phenyl and R17 represents hydroxyl, benzyloxy, (C1-C8)-alkoxy or the group â€”NR15R16 listed above, or the (C1-C8)-alkyl is optionally substituted by (C3-C6)cycloalkyl or phenyl, which for its part is substituted by hydroxyl, halogen or (C1-C6)-alkoxy or amino, or the (C1-C8)-alkyl is optionally substituted by imidazolyl or indolyl, in which the corresponding â€”NH functions are optionally protected by (C1-C6)-alkyl or by an amino protective group, R11 and R12 are identical or different and represent hydrogen, (C1-C6)-alkyl or a typical amino protective group, or R11 and R12 together with the nitrogen atom form a 5- to 6-membered saturated heterocycle, which may optionally contain a further heteroatom from the group consisting of S and O or a radical of the formula â€”NR18, in which R18 represents hydrogen, (C1-C6)-alkyl or phenyl, A and E are identical or different and represent a bond or represent (C1-C4)-alkylene, D represents an oxygen atom or represents a radical of the formula â€”S(O)eâ€” or â€”N(R19)â€”, in which e represents a number 0, 1 or 2, R19 represents hydrogen, (C1-C6)-alkyl or (C1-C6)-acyl, G represents doubly attached (C6-C10)-aryl or represents a doubly attached 5- to 7-membered aromatic heterocycle having up to 3 heteroatoms from the group consisting of S, N and O, which are optionally substituted by one or more identical or different substituents selected from the group consisting of: hydroxyl, trifluoromethyl, carboxyl, halogen, (C1-C6)-alkyl, hydroxy(C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxycarbonyl, and groups of the formulae â€”COâ€”Oâ€”(CH2)fâ€”NR20R21, â€”NR22â€”SO2R23, â€”(CH2)gâ€”(CO)hâ€”NR24R25 and â€”OR26, in which f represents a number 1, 2, 3 or 4, g and h are identical or different and represent a number 0 or 1, R20 and R21 have the meaning of R4 and R5 given above and are identical to or different from this meaning, R22 has the meaning of R6 given above and is identical to or different from this meaning, R23 has the meaning of R7 given above and is identical to or different from this meaning, R24 and R25 have the meaning of R4 and R5 given above and are identical to or different from this meaning, or independently of one another represent a radical of the formula â€”CH2)iâ€”NR27R28, â€ƒin which i represents a number 1, 2, 3 or 4, and R27 and R28 have the meaning of R4 and R5 given above and are identical to or different from this meaning, R26 represents (C6-C10)-aryl, L represents a radical of the formula â€”Oâ€”, â€”NHâ€”, where the left-hand side of the radicals is attached to G, and in which R29, R30, R31, R32, R33, R34, R35, R36 and R37 are identical or different and represent hydrogen or (C1-C4)-alkyl, or R29 represents a radical of the formula â€”SO2R2, R2 represents (C6-C10)-aryl or represents a 5- to 7-membered saturated or aromatic heterocycle having up to 3 heteroatoms from the group consisting of S, N and O, which are optionally substituted by one or more identical or different substituents selected from the group consisting of: halogen, trifluoromethyl, nitro, amino and (C1-C6)-alkyl, or represents the radical of the formula or morpholine, or represents C3-C8-cycloalkyl, or represents (C1-C12)-alkyl, (C2-C12)-alkenyl or (C2-C12)-alkinyl, which are optionally substituted by one or more identical or different substituents selected from the group consisting of: halogen, trifluoromethyl, hydroxyl, cyano, azido, (C1-C6)-alkoxy, (C1-C6)-perfluoroalkoxy, partially fluorinated (C1-C6)-alkoxy, a radical of the formula â€ƒin which R38 and R39 have the meaning of R4 and R5 given above and are identical to or different from this meaning, phenyl, optionally substituted by one or more identical or different substituents selected from the group consisting of: halogen, nitro, hydroxyl, (C1-C6)-alkyl, (C1-C6)-alkoxy and a group of the formula â€”NR40R41, in which R40 and R41 are identical or different and represent hydrogen or (C1-C6)-alkyl or (C1-C6)-acyl, and a 5- to 6-membered aromatic heterocycle having up to three heteroatoms from the group consisting of S, N and O, optionally substituted by one or more identical or different substituents selected from the group consisting of: halogen, nitro, hydroxyl, (C1-C6)-alkyl, (C1-C6)-alkoxy and a group of the formula â€”NR40R41, in which R40 and R41 are as defined above, or L and R2 together represent a radical of the formula and pharmaceutically acceptable salts thereof.