Patent ID: 6207669
Filing Date: 2001-03-27
Classification: A61P,C07C,C07D

Abstract:
A compound of formula (I): ##STR26##or a salt or solvent thereof;wherein X is N;Y is a group W(CH.sub.2), (CH.sub.2)W, or W, in which W is O, S(O).sub.m wherein m is 0, 1 or 2, or NR.sup.a wherein R.sup.a is hydrogen or a C.sub.1-8 alkyl group;R.sup.1 is selected from the group consisting a phenyl, furan, thiophene, pyridine, pyrimidine, pyrazine, pyrrole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, triazole, tetrazole and imidazole ring or a hydrogenated derivative of the aforementioned, the ring being substituted:either (a) by one or more groups selected from dioxolanyl, hydroxy- C.sub.1-4 alkyl C.sub.1-4 alkylamino-C.sub.1-4 alkyl or di(C.sub.1-4 alkyl)-amino- C.sub.1-4 alkyl;or (b) by one or more groups independently selected from M.sup.1 -M.sup.2 -M.sup.3 -M.sup.4, M.sup.1 -M.sup.5 or M.sup.1 -M.sup.2 -M.sup.3' -M.sup.6whereinM.sup.1 represents a C.sub.1-4 alkyl group, wherein optionally a CH.sub.2 group is replaced by a CO group;M.sup.2 represents NR.sup.12 or CR.sup.12 and R.sup.13 each independently represent H or C.sub.1-4 alkyl;M.sup.3 represents a C.sub.1-4 alkyl group;M.sup.3 represents a C.sub.1-4 alkyl group or is absent;M.sup.4 represents CN, NR.sup.12 S(O).sub.m R.sup.13, S(O).sub.m NR.sup.14 R.sup.1, CONR.sup.14 R.sup.15, S(O).sub.m R.sup.13 or CO.sub.2 R.sup.13, in which R.sup.12, R.sup.13 and m are as hereinbefore defined and R.sup.14 and R.sup.15 each independently represent H or C.sub.1-4 alkyl, or R.sup.14 and R.sup.15 together with the nitrogen atom to which they are attached represent a 5-or 6-membered ring optionally containing 1 or 2 additional heteroatoms selected from N, O or S(O).sub.m in which ring any nitrogen atom present may optionally be substituted with a C.sub.1-4 alkyl group;M.sup.5 represents the group NR.sup.14 R.sup.15 or the group ##STR27##in which t represents 2 to 4 and R.sup.16 represents OH, OC.sub.1-4 alkyl or NR.sup.14 R.sup.15 ; andM.sup.6 represents a C.sub.3-6 cycloalkyl group, the group NR.sup.14 R.sup.15 or a 5- or 6membered heterocyclic ring system containing 1 to 4 heteroatoms selected from N, O or S;and R.sup.1 is optionally further substituted by one or two halogeno, C.sub.1-4 alkyl or C.sub.1-4 alkoxy groups;R.sup.2 represents hydrogen;each R.sup.5 is independently selected from the group consisting hydrogen, hydroxy, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylamino, di-[C.sub.1-4 alkylamino, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, C.sub.1-4 alkylcarbamoyl, di-carbamoyl, carbamyl, C.sub.1-4 alkoxycarbonyl, cyano, nitro and trifluoromethyl, and n is 1, 2 or 3;R.sup.3 is a group ZR.sup.4 wherein Z is joined to R.sup.4 through a (CH.sub.2)p group in which p is 0, 1 or 2 and Z is oxygen, dicarbonyl, OCH.sub.2, CH(CN), S(O).sub.m or NR.sup.b, wherein R.sup.b is hydrogen or C.sub.1-4 alkyl; and R.sup.4 is an optionally substituted phenyl, dioxolanyl, thienyl, cyclohexyl or pyridyl group;wherein any optional substituent on R.sup.4 is either (a) selected from the group consisting CH.sub.2).sub.q S(O).sub.m C.sub.1-4 alkyl, (CH.sub.2).sub.q S(O).sub.m -C.sub.3-6 cycloalkyl, (CH.sub.2).sub.q SO.sub.2 NR.sup.8 R.sup.9, (CH.sub.2).sub.q CO.sub.2 R.sup.8, (CH.sub.2).sub.q OR.sup.8, (CH.sub.2).sub.q CONR.sup.8 R.sup.9, (CH.sub.2).sub.q NR.sup.8 COR.sup.9, (CH.sub.2).sub.q COR.sup.8, (CH.sub.2).sub.q R.sup.8, NRSSO.sub.2 R.sup.9 and S(O).sub.m R.sup.8 ; wherein q is an integer from 0 to 4 inclusive and m is as defined above; and wherein R.sup.8 and R.sup.9 are independently selected from the group consisting hydrogen, Ci- alkyl, C.sub.3-5 cycloalkyl, aryl, a 5-or 6-membered saturated or unsaturated heterocyclic ring which may be the same ordifferent and which contains one or more heteroatoms which are selected from N, O or S(O).sub.m, with the proviso that the heterocyclic ring does not contain two adjacent O or S(O).sub.m atoms; or (b) is selected from the group consisting halogen, trifluoromethyl, trifluoromethoxy, nitro and cyano; ##STR28##andrepresents ##STR29##