Patent ID: 6740647
Filing Date: 2004-05-25
Classification: A61K,A61P,C07K

Abstract:
A compound of the formula IAâ€”Bâ€”Dâ€”Eâ€”Fâ€ƒâ€ƒI in which A, B, D, E and F have the following meanings:A: â€ƒwhere m is 0, 1 or 2,n is0, 1 or 2, R1 is HOOCâ€”, C1-6-alkyl-OOCâ€”, aryl-C0-4-alkyl-OOC or â€”OH, R2 is Hâ€”, C1-4-alkyl- or R1â€”(CH2)mâ€” and R3 is Hâ€” or C1-4-alkyl-, B: â€ƒwhere R4 is Hâ€”, C1-4-alkyl- or R1â€”(CH2)mâ€”(where R1 and m have the abovementioned meanings), p is 0 or 1, R5 is Hâ€” or C1-4-alkyl-, R6 is Hâ€”, C1-8-alkyl-, 2-thienyl-, 3-thienyl-, 3-indolyl-, 4-imidazolyl-, 2-pyridyl-, 3-pyridyl-, 4-pyridyl-, phenyl- which may carry up to three identical or different radicals selected from the group of C1-4-alkyl-, CF3â€”, C1-4-alkoxy-, HOâ€”, BnOâ€”, Fâ€” and Clâ€”, C3-8-cycloalkyl- which may carry up to four identical or different C1-4-alkyl- radicals and/or where one or two Câ€”C single bonds in the ring can be replaced by a C&boxH;C double bond and/or a phenyl ring can be fused on, C7-C12-bicycloalkyl- or C10-tricycloalkyl- or R4 and R6 together are an ethylene or propylene group, R7 is H, C1-8-alkyl-, phenyl- which may carry up to three identical or different radicals from the group of C1-4-alkyl-, CF3â€”, C1-4-alkoxy-, Fâ€” and Clâ€”, or C3-8-cycloalkyl- which may carry up to four identical or different C,4-alkyl radicals, and R8 is H or C1-4-alkyl, D: where R20 is H, C1-4-alkyl, Bnor BnO(CO)â€” and where the following applies:if D is II, III or XI, then E has the following meaning: wherea) in the event that X=S, O, NH or NR12, Y is â€”CR13&boxH;, â€”CH&boxH; and Z is â€”CR&boxH;or Y is â€”CR3&boxH; and Z is â€”CH&boxH;or b) in the event that X=NR12, Y is â€”CH&boxH; and Z is â€”CH&boxH;or c) in the event that X=S, O or NH, Y is â€”CR15&boxH; and Z is â€”N&boxH;or Y is â€”N&boxH; and Z is â€”CR15 &boxH;or d) in the event that X=â€”NR12â€”, Y is â€”N&boxH; and Z is â€”CR16&boxH;, â€”N&boxH;or Y is â€”CR16&boxH; and Z is â€”N&boxH;and R9 is Hâ€” or C1-3-alkyl-, R10 is Hâ€” or C1-4-alkyl-, R11 is Hâ€” or C1-4-alkyl-, R12 is CH3â€” or C2H5â€”, R13 is Clâ€”, CF3â€” or C1-4-alkyl-, R14 is Clâ€”, CF3â€” or C1-4-alkyl-, R15 is CF3â€” or C1-4-alkyl-, R16 is Hâ€”, CF3â€” or C1-4-alkyl- and R20 is as above, or, if D is IV, VI, VII, VIII, IX or X, then E has the following meaning: whereX is O, S or â€”NR17â€”and Y is â€”N&boxH; and Z is â€”CR16&boxH; or â€”N&boxH;or Y is â€”CR16&boxH; and Z is â€”N&boxH;or Y is â€”CR18&boxH; and Z is â€”CR19&boxH;and R9, R10, R11, R16 and R20 are as above, R17 is H, CH3â€” or C2H5â€”, R18 is Hâ€”, Clâ€”, CF3â€” or C1-4-alkyl-, R19 is Hâ€”, Clâ€”, CF3â€” or C1-4-alkyl-, orif D is II, III, IV, VI, VII, VIII, IX, X or XI, E has the following meanings: wherea) in the event that X=S, Y is â€”CR18&boxH; and Z is â€‰CR19&boxH;or Y is â€”CR16&boxH; and Z is â€”N&boxH;or b) in the event that X=O or â€”NR12â€”, Y is â€”N&boxH;, â€”CR16&boxH; and Z is â€”N&boxH;, â€”CR18&boxH;and R9, R10, R11, R12, R16, R18, R19 and R20 have the abovementioned meanings, F: or a salt thereof with a physiologically acceptable acid.