Patent ID: 6180635
Filing Date: 2001-01-30
Classification: A61P,C07D

Abstract:
A compound of formula (I): ##STR111##wherein:R is --C(O)Ar.sup.1, --C(R.sup.4)(R.sup.5)Ar.sup.1, or Ar.sup.2 ;Ar.sup.1 is naphthyl, quinolyl, isoquinolyl, indolyl, benzofuranyl or benzothienyl, each of which can be optionally substituted by one or more substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, or Ar.sup.1 is phenyl optionally substituted by one or more substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, trifluoromethyl, amino, nitro, cyano, trifluoromethoxy, phenoxy, --CH.sub.2 N(R.sup.6).sub.2, --NHSO.sub.2 CF.sub.3, C.sub.1-4 alkylsulphonylamino, --NHC(O)R.sup.6a, CO.sub.2 R.sup.7 or --C(O)NR.sup.8 R.sup.8a ;R.sup.4 represents H or C.sub.1-4 alkyl;R.sup.5 represents H or OH;each R.sup.6 independently represents H or C.sub.1-4 alkyl;R.sup.6a represents H, C.sub.1-6 alkyl, aryl or arC.sub.1-4 alkyl, wherein the aryl group or aryl moiety in the aralkyl group is phenyl or pyridyl, each of which may be optionally substituted by one or more substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylcarbonylamino, halogen or trifluoromethyl;R.sup.7 represents H or C.sub.1-4 alkyl;R.sup.8 and R.sup.8a each independently represent H, C.sub.1-4 alkyl, phenyl or pyridyl;Ar.sup.2 is acenaphthenyl, indanyl, iminodihydrobenzofuranyl or fluorenyl, each of which can be optionally substituted by one or more substituents selected from OH, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, or trifluoromethyl;R.sup.1 and R.sup.2 are independently H, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, CH.sub.2 C.sub.3-5 cycloalkyl orC.sub.3-6 cycloalkyl;R.sup.3 represents H, X--R.sup.9 or X--Ar.sup.3 ;X represents S(O).sub.n, C(O)NR.sup.10, C(O)O, NH(CO)NR.sup.10, NH(CO)O or SO.sub.2 NR.sup.10 ;n is 0, 1 or 2;R.sup.9 represents a methyl group optionally substituted by one or more substituents selected from CN, CO.sub.2 H, C.sub.1-5 alkoxycarbonyl, 5-tetrazolyl, SO.sub.2 NH.sub.2 or C(O)NR.sup.11 R.sup.12, or R.sup.9 represents C.sub.2-6 alkyl or C.sub.3-6 alkenyl, each of which may be optionally substituted by one or more substituents selected from OH, CN, CO.sub.2 H, C.sub.1-5 alkoxy, C.sub.1-5 alkoxycarbonyl, 5-tetrazolyl, azide, phthalimido, SO.sub.2 NH.sub.2, C(O)NR.sup.11 R.sup.12, NR.sup.13 R.sup.14, NHC(O)R.sup.15 or NHSO.sub.2 R.sup.16 where R.sup.11, R.sup.12, R.sup.13 and R.sup.14 each independently represent H or C.sub.1-4 alkyl, R.sup.15 represents C.sub.1-4 alkyl, C.sub.1-4 alkoxy, di(C.sub.1-4 alkyl)amino, or alkoxyalkylene containing up to 6 carbon atoms, and R.sup.16 represents C.sub.1-4 alkyl or trifluoromethyl; or, additionally, in the case where X represents C(O)NR.sup.10, NH(CO)NR.sup.10 or SO.sub.2 NR.sup.10, R.sup.9 and R.sup.10 together with the nitrogen atom to which they are attached may form a 4- to 7-membered heterocyclic ring which may be optionally substituted by one or more OH groups;R.sup.10 represents H, C.sub.1-6 alkyl or is linked to R.sup.9 as defined above; andAr.sup.3 is phenyl, pyridyl or pyridine N-oxide, each of which may be optionally substituted by one or more substituents selected from OH, NO.sub.2, NH.sub.2, NHSO.sub.2 CF.sub.3, C.sub.1-4 alkoxy, bis-C.sub.1-4 alkanesulphonylamino, C.sub.1-4 alkylcarbonylamino or C.sub.1-4 alkoxycarbonylamino; or a pharmaceutically-acceptable salt or solvate thereof.