Patent ID: 6242601
Filing Date: 2001-06-05
Classification: A61P,C07D

Abstract:
A compound of formula: ##STR10##whereinR.sup.1 is pyridyl, pyridyl substituted with halogen, lower alkyl, hydroxy-lower alkyl or lower alkenyl, pyrrolyl, pyrrolyl substituted with halogen, lower alkyl, hydroxy-lower alkyl or lower alkenyl, imidazolyl, imidazolyl substituted with halogen, lower alkyl, hydroxy-lower alkyl or lower alkenyl, thiazolyl, thiazolyl substituted with halogen, lower alkyl, hydroxy-lower alkyl or lower alkenyl, thiazolinyl, thiazolinyl substituted with halogen, lower alkyl, hydroxy-lower alkyl or lower alkenyl, oxazolyl, or oxazolyl substituted with halogen, lower alkyl, hydroxy-lower alkyl or lower alkenyl;R.sup.2 is (i) R.sup.21, (ii) --Y--R.sup.22, (iii) heterocyclyl selected from the group consisting of pyrimidinyl, imidazolyl, oxadiazolyl, oxazolyl and thiazolyl, or (iv) heterocyclyl selected from the group consisting of pyrimidinyl, imidazolyl, oxadiazolyl, oxazolyl and thiazolyl, which is mono-, di- or tri-substituted, independently, with hydroxy, lower alkenyl, amino, lower alkanoylamino, lower alkoxycarbonylamino, lower alkyl or hydroxy-lower alkyl;R.sup.21 is cyano, hydroxy-lower alkyl, carboxy, --C(O)NR.sup.a R.sup.b, --(CH.sub.2).sub.1-4 NHR.sup.c, --(CH.sub.2).sub.1-4 NHC(O)NH(CH.sub.2).sub.0-3 CH.sub.3, amidino, hydroxyamidino, lower alkoxycarbonyl or hydroxy-lower alkoxycarbonyl;R.sup.22 is hydrogen, lower alkanoyl, carboxy-lower alkyl, lower alkoxycarbonyl, lower alkoxycarbonyl-lower alkyl, carbamoyl-lower alkyl, di-lower alkylcarbamoyl-lower alkyl, allyl, lower alkyl or hydroxy-lower alkyl;R.sup.a is hydrogen, lower alkyl, or lower alkyl substituted with hydroxy or lower alkoxy;R.sup.b is hydrogen or lower alkyl;R.sup.c is hydrogen, acetyl or lower alkylsulfonyl;X is --CH-- or --N--; andY is --O--, --NH--;or a pharmaceutically acceptable salt or ester thereof.