Patent ID: 6191282
Filing Date: 2001-02-20
Classification: A61K,A61P,C07D,C07K

Abstract:
5-Membered ring heterocycle of the formula I, ##STR12##in whichW represents R.sup.1 -A--C (R.sup.13) or R.sup.1 -A--C.dbd.C;Y represents a carbonyl group, a thiocarbonyl group or a methylene group;Z represents N (R.sup.0), oxygen, sulphur or a methylene group;A denotes a (C.sub.1 -C.sub.6)-alkylene, (C.sub.3 -C.sub.7)-cycloalkylene, phenylene, phenylene-(C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkylene-phenyl or phenylene-(C.sub.2 -C.sub.6)-alkenyl divalent radical, or a divalent radical of a 5-membered or 6-membered saturated or unsaturated ring containing 0, 1 or 2 nitrogen atoms and substituted by 0, 1, or 2 (C.sub.1 -C.sub.6)-alkyl or doubly bonded oxygen or sulphur;B denotes a (C.sub.1 -C.sub.6)-alkylene, (C.sub.2 -C.sub.6)-alkenylene, phenylene, phenylene-(C.sub.1 -C.sub.3)-alkyl or (C.sub.1 -C.sub.3)-alkylene-phenyl divalent radical;D represents C(R.sup.2) (R.sup.3), N(R.sup.3) or CH.dbd.C(R.sup.3);E denotes tetrazolyl, (R.sup.8 O).sub.2 P(O), HOS (O).sub.2, R9NHS (O).sub.2 or R.sup.10 CO;R and R.sup.0 denote, independently of each other, hydrogen, (C.sub.1 -C.sub.8) alkyl, (C.sub.3 -C.sub.8) alkyl, (C.sub.3 -C.sub.8)-cycloalkyl, substituted or unsubstituted (C.sub.6 -C.sub.14)-aryl, or (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkyl which is substituted or unsubstituted in the aryl radical;R.sup.1 represents X--NH--C (.dbd.NH)--(CH.sub.2).sub.p or X.sup.1 -NH-(CH.sup.2).sub.p, where p is an integer from 0 to 3;X denotes hydrogen, (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub.6) alkylcarbonyl, (C.sub.1 -C.sub.6) -alkoxycarbonyl, C.sub.1 -C.sub.18)-alkylcarbonyloxy-(C.sub.1 -C.sub.6)-alkoxycarbonyl, substituted or unsubstituted (C.sub.6 -C.sub.14)-arylcarbonyl, substituted or unsubstituted (C.sub.6 -C.sub.14)-aryloxycarbonyl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.6)-alkoxycarbonyl which is unsubstituted or substituted in the aryl radical (R.sup.8 O).sub.2 P(O), cyano, hydroxyl, (C.sub.1 -C.sub.6)-alkoxy, (C.sub.5 -C.sub.14)-aryl-(C.sub.1 -C.sub.6)-alkoxy which is substituted or unsubstituted in the aryl radical, or amino;X.sup.1 has one of the meanings of X or denotes R'-NH--C (.dbd.N--R""), where R' and R"", independently of each other, have the meanings of X;R.sup.2 denotes hydrogen, (C.sub.1 -C.sub.8)-alkyl, substituted or unsubstituted (C.sub.6 -C.sub.14)-aryl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkyl which is substituted or unsubstituted in the aryl radical, (C.sub.3 -C.sub.8)-alkyl which is substituted or unsubstituted in the aryl radical, or (C.sub.3 -C.sub.8)-cycloalkyl;R.sup.3 denotes COOR.sup.15, CON (CH.sub.3)R.sup.15 or CONHUR.sup.15 ;R.sup.8 denotes hydrogen, (C.sub.1 -C.sub.18)-alkyl, substituted or unsubstituted (C.sub.6 -C.sub.14)-aryl or (C.sub.6 -C.sub.14)-aryl-(C.sub.1 C.sub.8)-alkyl which is unsubstituted or substituted in the aryl radical;R.sup.9 denotes hydrogen, aminocarbonyl, (C.sub.1 -C.sub.18)-alkylaminocarbonyl, (C.sub.3 -C.sub.8)-cycloalkylaminocarbonyl, substituted or unsubstituted (C.sub.6 -C.sub.14)-arylaminocarbonyl, (C.sub.1 -C.sub.18)-alkyl, substituted or unsubstituted (C.sub.6 -C.sub.14)-aryl, or (C.sub.3 -C.sub.8)-cycloalkyl;R.sup.10 denotes hydroxyl, (C.sub.1 -C.sub.18)-alkoxy, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkoxy which is unsubstituted or substituted in the aryl radical, substituted or unsubstituted (C.sub.6 -C.sub.14)-aryloxy, amino or mono- or di-((C.sub.1 -C.sub.18)-alkyl)-amino;R.sup.13 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkyl which is substituted or unsubstituted in the aryl radical, or (C.sub.3 -C.sub.8)-cycloalkyl;R.sup.15 represents R.sup.16 -(C.sub.1 -C.sub.6)-alkyl or represents R.sup.16 ;R.sup.16 represents 6- to 24-membered bicyclic or tricyclic radical which is saturated or partially unsaturated and which contains form zero to four identical or different heteroatoms from the group nitrogen, oxygen and sulphur, and which is unsubstituted or substituted by one or more identical or different sustituents from the group (C.sub.1 -C.sub.4)-alkyl and oxo;b, c, d, and f, independently of each other, represent 0 or 1, but cannot all simultaneously be 0;e, g, and h, independently of each other, represent integers from 0 to 6;where, however, when at the same time, W represents R.sup.1 -A--CH or R.sup.1 -A--CH.dbd.C, D represents N (R.sup.3) and c, d, and f represent 0, R.sup.3 cannot when represents COOR.sup.a where R.sup.a represents methyl which is substituted by a 9-fluorenyl radical, or the physiologically tolerated salts thereof.