Patent ID: 6194441
Filing Date: 2001-02-27
Classification: A61P,C07D

Abstract:
A compound of the formula (I): ##STR12##wherein:R.sup.1 is chloro, fluoro, (1-4C)alkanesulfonyloxy, azido, or of the formula --NHC(.dbd.O)R.sup.a wherein R.sup.a is hydrogen, (1-4C)alkoxy, chloromethyl, dichloromethyl, cyanomethyl, methoxymethyl, acetylmethyl or (1-4C)alkyl;R.sup.2 and R.sup.3 are independently hydrogen or fluoro;R.sup.4 is hydrogen, (1-4C)alkyl, halo or trifluoromethyl;R.sup.5 and R.sup.6 are independently selected from hydrogen, (1-4C)alkyl, halo, trifluoromethyl, an acetylene of the formula -.tbd.-H or -.tbd.-(1-4C)alkyl, and a group of the formula (IA) ##STR13##wherein Z is hydrogen or (1-4C)alkyl; X and Y are independently selected from hydrogen, (1-4C)alkyl, halo, cyano, nitro, --S(O).sub.n (1-4C)alkyl (wherein n is 0, 1 or 2), aminosulfonyl, (1-4C)alkylaminosulfonyl, di-(1-4C)alkylaminosulfonyl, trifluoromethyl, pentafluoroethyl, (1-4C)alkanoyl, carbamoyl, N-(1-4C)alkylcarbamoyl, and N,N-di-(1-4C)alkylcarbamoyl; or one of X and Y is selected from the above list and the other is selected from phenyl, phenylcarbonyl, --S(O).sub.n -phenyl (wherein n is 0, 1 or 2), N-(phenyl)carbamoyl, phenylaminosulfonyl, heteroaryl, heteroarylcarbonyl, --S(O).sub.n -heteroaryl (wherein n is 0, 1 or 2), N-(heteroaryl)carbamoyl and heteroarylaminosulfonyl; wherein any phenyl group above may be optionally substituted by up to three substituents independently selected from (1-4C)alkyl, cyano, trifluoromethyl, nitro, halo and (1-4C)alkylsulfonyl; wherein any heteroaryl group in X and Y may be optionally substituted on an available carbon atom by (1-4C)alkyl, and optionally substituted on a suitable nitrogen atom by oxo (to form an N-oxide); provided that X, Y and Z do not define a (2-4C)alkenyl group and provided that at least one of R.sup.5 and R.sup.6 is a group of the formula (IA) or an acetylene of the formula -.tbd.-H or -.tbd.-(1-4C)alkyl;or a pharmaceutically acceptable salt thereof.