Patent ID: 6218547
Filing Date: 2001-04-17
Classification: A61P,C07D

Abstract:
A chemical compound represented by the formula (I): ##STR20##in which formula (I),x is 0, 1, 2 or 3;R.sup.1 represents a C.sub.3-8 -cycloalkyl group, a phenyl group, or a 5- or 6-membered monocyclic heterocyclic group, which groups are unsubstituted or substituted one or more times with substituents selected from the group consisting of C.sub.1-8 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.3-7 -cycloalkyl-C.sub.1-8 -alkyl, alkoxy, halogen, trifluoromethyl, cyano, NH.sub.2, NH(C.sub.1-8 -alkyl), N(C.sub.1-8 -alkyl).sub.2, and nitro;or R.sup.1 represents a cyano group, or a group of the formula --C.sub.1-8 -alkyl-CO.sub.2 R.sup.2, C.sub.2-6 -alkenyl-CO.sub.2 R.sup.2, --CO--R.sup.2, --CO.sub.2 (CH.sub.2).sub.m R.sup.2, or --C(R.sup.3).dbd.N--OR.sup.2, in which formulasm is 0, 1, 2 or 3;R.sup.2 and R.sup.3 independently represents hydrogen, C.sub.1-8 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.2-6 -alkenyl, C.sub.2-6 -alkynyl, phenyl, benzyl, or a 5- or 6-membered heterocyclic group, which heterocyclic group is unsubstituted or substituted one or more times with substituents selected from the group consisting of C.sub.1-8 -alkyl, C.sub.3-7 -cycloalkyl, hydroxy, alkoxy, halogen, trifluoromethyl, cyano, NH.sub.2, NH(C.sub.1-8 -alkyl), N(C.sub.1-8 -alkyl).sub.2, and nitro;or R.sup.2 and R.sup.3 independently represent a group of the formula --(CH.sub.2).sub.q --NR.sup.4 R.sup.5, --(CH.sub.2).sub.q --CON(R.sup.4 R.sup.5), --(CH.sub.2).sub.q --CO.sub.2 R.sup.4, or --C.sub.1-8 -alkyl-CO.sub.2 R.sup.4, in which formulasR.sup.4 and R.sup.5 independently represent hydrogen, C.sub.1-8 -alkyl, or C.sub.3-7 -cycloalkyl; andq is 0, 1, 2 or 3;R.sup.11 represents a group of the formula --CO.sub.2 --R.sup.9, whereinR.sup.9 represents C.sub.1-8 -alkyl, or C.sub.3-7 -cycloalkyl, which alkyl groups are unsubstituted or substituted with a 5- or 6-membered heterocyclic group, which heterocyclic group is unsubstituted or substituted one or more times with substituents selected from the group consisting of C.sub.1-8 -alkyl, C.sub.3-7 -cycloalkyl, hydroxy, alkoxy, halogen, trifluoromethyl, cyano, NH.sub.2, NH(C.sub.1-8 -alkyl), N(C.sub.1-8 -alkyl).sub.2, and nitro;or R.sup.9 is a 5- or 6-membered heterocyclic group, which heterocyclic group is unsubstituted or substituted one or more times with substituents selected from the group consisting of C.sub.1-8 -alkyl, C.sub.3-7 -cycloalkyl, hydroxy, alkoxy, halogen, trifluoromethyl, cyano, NH.sub.2, NH(C.sub.1-8 -alkyl), N(C.sub.1-8 -alkyl).sub.2, and nitro;or R.sup.9 represent a group of the -alkyl-N(R.sup.10 R.sup.12), in which formulaR.sup.10 and R.sup.12 independently represent hydrogen or C.sub.1-8 -alkyl, C.sub.3-7 -cycloalkyl;or R.sup.11 represents a group of formula (II): ##STR21##in which formula (II),n is 0, 1, 2, or 3;R' and R"" together with the N atom to which they are attached form a 5- or 6-membered heterocyclic ring, which heterocyclic ring has as a ring member, one or more members selected from the group consisting of one oxygen atom, one additional nitrogen atom and one --CH.dbd.CH-- chain;which heterocyclic ring is unsubstituted or substituted one or more times with a group of the formula --(CH.sub.2).sub.p X, whereinp is 0, 1, 2 or 3;X represents hydrogen, hydroxy, C.sub.1-8 -alkyl, C.sub.3-7 -cycloalky, or C.sub.2-6 -alkenyl, which alkyl, cycloalkyl or alkenyl groups are unsubstituted or substituted one or more times with a group of the formula --CO.sub.2 R.sup.6 ;or X represents a group of the formula --CO--R.sup.6, --CO.sub.2 --R.sup.6, --CON--R.sup.6 R.sup.7, or --COO--R.sup.6 --NR.sup.7 R.sup.8, in which formulasR.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen or C.sub.1-8 -alkyl, C.sub.3-7 -cycloalkyl;or R.sup.11 represents a group of the formula (III): ##STR22##in which formula (III),n is 0, 1, 2 or 3;R' is hydrogen, C.sub.1-8 -alkyl or C.sub.3-7 -cycloalkyl;R'"" and R"""" together with the atoms to which they are attached form a 5- or 6-membered heterocyclic ring, which heterocyclic ring has as a ring member, one or more members selected from the group consisting of one oxygen atom, one additional nitrogen atom, and one --CH.dbd.CH-- chain;and in which formula the heterocyclic ring formed by R'"" and R"""" is unsubstituted or substituted one ore more times with the group of the formula --(CH.sub.2).sub.p X, whereinp is 0, 1, 2 or 3;X represents hydrogen, hydroxy, C.sub.1-8 -alkyl, C.sub.3-7 -cycloalkyl, or C.sub.2-6 -alkenyl, which alkyl, cycloalkyl or alkenyl groups are unsubstituted or substituted one or more times with a group of the formula --CO.sub.2 R.sup.6 ;or X represents a group of the formula --CO--R.sup.6, --CO.sub.2 --R.sup.6, --CON--R.sup.6 R.sup.7, or --COO--R.sup.6 --NR.sup.7 R.sup.8, in which formulasR.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen or C.sub.1-8 -alkyl, C.sub.3-7 -cycloalkyl;or a pharmaceutically acceptable salt thereof or an oxide thereof;provided, however, that R.sup.11 is not 1-imidazolyl, 3-pyridyl, oxadiazolyl or morpholinyl.