Patent ID: 6011045
Filing Date: 2000-01-04
Classification: A61P,C07D

Abstract:
A compound of formula 1,A--B--D--E--F--G (1)in which:A=A.sub.1 or A.sub.2, whereA.sub.1 =R.sup.2 R.sup.3 N--C(.dbd.NR.sup.2)NR.sup.2 C(O)--, R.sup.2 R.sup.3 N--C(.dbd.NR.sup.2)NR.sup.2 C(S)--, R.sup.2 R.sup.3 N--C(.dbd.NR.sup.2)NR.sup.2 --S(O).sub.n --, ##STR90## and A.sub.2 = ##STR91## where, in A.sub.1 or A.sub.2 ##STR92## is a 5-membered to 10-membered monocyclic or polycyclic, aromatic or nonaromatic ring system which contains the grouping ##STR93## and, in addition, can contain from 1 to 4 heteroatoms selected from the group consisting of N, O and S, and, optionally, can be substituted, once or more than once, by R.sup.12, R.sup.13, R.sup.14 or R.sup.15 ;B is a direct linkage, (C.sub.1 -C.sub.8)-alkanediyl, --CR.sup.2 .dbd.CR.sup.3 --, (C.sub.5 -C.sub.10)-arylene, (C.sub.3 -C.sub.8)-cycloalkylene, or --C.tbd.C--, which can in each case be substituted, once or twice, by (C.sub.1 -C.sub.8)-alkyl;D is a direct linkage, (C.sub.1 -C.sub.8)-alkanediyl, (C.sub.5 -C.sub.10)-arylene, --O--, --NR.sup.2 --, --CO--NR.sup.2 --, --NR.sup.2 --CO--, --NR.sup.2 --C(O)--NR.sup.2 --, --NR.sup.2 --C(S)--NR.sup.2 --, --OC(O)--, --C(O)O--, --CO--, --CS--, --S(O)--, --S(O).sub.2 --, --S(O).sub.2 --NR.sup.2 --, --S(O)--NR.sup.2 --, --NR.sup.2 --S(O)--, --NR.sup.2 --S(O).sub.2 --, --S--, --CR.sup.2 .dbd.CR.sup.3 --, --C.tbd.C--, --NR.sup.2 --N.dbd.CR.sup.2 --, --N.dbd.CR.sup.2, --R.sup.2 C.dbd.N--, --CH(OH)--, which can in each case be substituted, once or twice, by (C.sub.1 -C.sub.8)--alkyl, --CR.sup.2 .dbd.CR.sup.2 -- or (C.sub.5 -C.sub.6)-aryl, where, if B is a direct linkage, D can also be a direct linkage or a radical as defined under D, which radical is substituted once or twice, as described under D, and is linked to B by way of one of these substituents;E is ##STR94## where (R.sub.2).sub.p is bonded to one or more carbon atoms of the 6-membered ring and is, independently of each other, a radical selected from the group consisting of hydrogen, alkyl, halogen-substituted alkyl, hydroxyalkyl, alkenyl, alknyl, cycloalkyl, aryl, aryloxy, aralkyl, hydroxyl, alkoxy, aralkoxy, carbamyl, amino, substituted amino, acyl, cyano, halogen, nitro and sulfo;R is (C.sub.1 -C.sub.4)-alkylp is an integer from 1 to 3,F is defined like D; andG is ##STR95## where R.sup.2 and R.sup.3 are, independently of each other, hydrogen, (C.sub.1 -C.sub.10)-alkyl, which is optionally substituted, once or more than once, by fluorine, (C.sub.3 -C.sub.12)-cycloalkyl, (C.sub.3 -C.sub.12)-cycloalkyl-(C.sub.1 -C.sub.8)-alkyl, (C.sub.5 -C.sub.14)-aryl, (C.sub.5 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkyl, R.sup.8 OC(O)R.sup.9, R.sup.8 R.sup.8 NC(O)R.sup.9 or R.sup.8 C(O)R.sup.9 ;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are, independently of each other, hydrogen, fluorine, OH, (C.sub.1 -C.sub.8)-alkyl, (C.sub.3 -C.sub.14)-cycloalkyl, (C.sub.3 -C.sub.14)-cycloalkyl-(C.sub.1 -C.sub.8)-alkyl, or R.sup.8 OR.sup.9, R.sup.8 SR.sup.9, R.sup.8 CO.sub.2 R.sup.9, R.sup.8 --(C.sub.5 -C.sub.14)-aryl-R.sup.9, R.sup.8 N(R.sup.2)R.sup.9, R.sup.8 R.sup.8 NR.sup.9, R.sup.8 N(R.sup.2)C(O)OR.sup.9, R.sup.8 S(O).sub.n N(R.sup.2)R.sup.9, R.sup.8 OC(O)N(R.sup.2)R.sup.9, R.sup.8 C(O)N(R.sup.2)R.sup.9, R.sup.8 N(R.sup.2)C(O)N(R.sup.2)R.sup.9, R.sup.8 N(R.sup.2)S(O).sub.n N(R.sup.2)R.sup.9, R.sup.8 S(O).sub.n R.sup.9, R.sup.8 SC(O)N(R.sup.2)R.sup.9, R.sup.8 C(O)R.sup.9, R.sup.8 N (R.sup.2)C(O)R.sup.9 or R.sup.8 N(R.sup.2)S(O).sub.n R.sup.9 ;R.sup.8 is hydrogen, (C.sub.1 -C.sub.8)-alkyl, (C.sub.3 -C.sub.14)-cycloalkyl, (C.sub.3 -C.sub.14)-cycloalkyl-(C.sub.1 -C.sub.8)-alkyl, (C.sub.5 -C.sub.14)-aryl or (C.sub.5 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkyl, where the alkyl radicals can be substituted, once or more than once, by fluorine;R.sup.9 is a direct linkage or (C.sub.1 -C.sub.8)-alkanediyl;R.sup.10 is C(O)R.sup.11, C(S)R.sup.11, S(O)R.sub.n R.sup.11, P(O)(R.sup.11).sub.n or a four-membered to eight-membered, saturated or unsaturated heterocycle which contains 1, 2, 3 or 4 heteroatoms selected from the group consisting of N, O and S;R.sup.11 is OH, (C.sub.1 -C.sub.8)-alkoxy, (C.sub.5 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkoxy, (C.sub.5 -C.sub.14)-aryloxy, (C.sub.1 -C.sub.8)-alkylcarbonyloxy-(C.sub.1 -C.sub.4)-alkoxy, (C.sub.5 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkylcarbonyloxy-(C.sub.1 -C.sub.6)-alkoxy, NH.sub.2, mono- or di-((C.sub.1 -C.sub.8)-alkyl)-amino, (C.sub.5 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkylamino, (C.sub.1 -C.sub.8)-dialkylaminocarbonylmethyloxy, (C.sub.5 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-dialkylaminocarbonylmethyloxy or (C.sub.5 -C.sub.14)-arylamino or the radical of an L-amino acid or D-amino acid;R.sup.12, R.sup.13, R.sup.14 and R.sup.15 are, independently of each other, hydrogen, (C.sub.1 -C.sub.10)-alkyl which is optionally substituted once or more than once by fluorine, (C.sub.3 -C.sub.12)-cycloalkyl, (C.sub.3 -C.sub.12)-cycloalkyl-(C.sub.1 -C.sub.8)-alkyl, (C.sub.5 -C.sub.14)-aryl, (C.sub.5 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkyl, H.sub.2 N, R.sup.8 ONR.sup.9, R.sup.8 OR.sup.9, R.sup.8 OC(O)R.sup.9, R.sup.8 R.sup.8 NR.sup.9, R.sup.8 -(C.sub.5 -C.sub.14)-aryl-R.sup.9, HO--(C.sub.1 -C.sub.8)-alkyl-N(R.sup.2)R.sup.9, R.sup.8 N(R.sup.2)C(O)R.sup.9, R.sup.8 C(O)N(R.sup.2)R.sup.9, R.sup.8 C(O)R.sup.9, R.sup.2 R.sup.3 N--C(.dbd.NR.sup.2)--NR.sup.2, R.sup.2 R.sup.3 N--C(.dbd.NR.sup.2), .dbd.O, or .dbd.S;where two adjacent substituents from R.sup.12, R.sup.13, R.sup.14, and R.sup.15 can also together be --OCH.sub.2 O--, --OCH.sub.2 CH.sub.2 O-- or --OC(CH.sub.3)O--;n is 1 or 2;p and q are, independently of each other, 0 or 1;in all its stereoisomeric forms and mixtures thereof in all proportions, and its physiologically tolerated salts.