Patent ID: 6177466
Filing Date: 2001-01-23
Classification: C07C,C07D

Abstract:
A compound of the formula (Ib): ##STR749##wherein R.sup.1 is hydrogen, or C1-4 alkyl;R.sup.2 is (1) hydrogen, (2) C1-8 alkyl, (3) phenyl, or (4) C1-4 alkyl substituted by phenyl, --OCOR.sup.16, in which R.sup.16 is C1-4 alkyl; or --CONR.sup.17 R.sup.18, in which R.sup.17 and R.sup.18 each, independently, is hydrogen or C1-4 alkyl;E is (1) --CONR.sup.3 --, in which R.sup.3 is hydrogen, C1-4 allyl, phenyl, C1-4 alkyl substituted by phenyl;(2) --NR.sup.3 CO--, in which R.sup.3 is the same meaning as hereinbefore defined;(3) --CO--O--,(4) --O--CO--,(5) --NR.sup.3 --CO--NR.sup.3 --, in which R.sup.3 is the same meaning as hereinbefore defined;(6) --CO--CH.sub.2 --,(7) --CO--,(8) --O--CO--NR.sup.3 --, in which R.sup.3 is the same meaning as hereinbefore defined;(9) --NR.sup.3 --CO--O--, in which R.sup.3 is the same meaning as hereinbefore defined;(10) --O--CO--O--,(11) --CS--NR.sup.3 --, in which R.sup.3 is the same meaning as hereinbefore defined;(12) --NR.sup.3 --CS--, in which R.sup.3 is the same meaning as hereinbefore defined;(13) --NR.sup.3 --CS--NR.sup.3 --, in which R.sup.3 is the same meaning as hereinbefore defined;(14) --O--CS--NR.sup.3 --, in which R.sup.3 is the same meaning as hereinbefore defined;(15) --NR.sup.3 --CS--O--, in which R.sup.3 is the same meaning as hereinbefore defined;(16) --CS--O--,(17) --O--CS--,(18) --O--CS--O--A is (1) hydrogen, (2) C1-8 alkyl, (3) C3-7 cycloalkyl, or (4) Ar, in which Ar is carbocyclic aryl or heterocyclic aryl, and these ring may be substituted by 1-3 of C1-15 alkyl, C1-15 alkoxy, halogen, nitro, cyano, guanidino, amidino, hydroxy, benzyloxy, --NR.sup.9 R.sup.10, in which R.sup.9 and R.sup.10 each, independently, is hydrogen or C1-4 alkyl; --COOR.sup.11, in which R.sup.11 is hydrogen or C1-4 alkyl;trifluoromethyl, phenyl or heterocyclic ring;J is (1) bond, (2) C2-4 alkylene, (3) C2-4 alkenylene, or (4) ##STR750##in which R.sup.4 and R.sup.5 each, independently, is (i) hydrogen, (ii) C 1-4 alkyl, (iii) C 1-4 alkoxy, R.sup.4 and R5, taken together with the carbon to which they are attached, is C3-7 cycloalkyl,G is ##STR751##in which R.sup.6 and R.sup.7 each, independently, is (i) hydrogen or (ii) C1-8 alkyl substituted bycarbocyclic aryl and the carbocyclic aryl may be substituted by 1-3 of C1-15 alkyl C1-15 alkoxy, halogen, nitro, cyano, guanidino, amidino, hydroxy, benzyloxy, NR.sup.9 R.sup.10, and R.sup.6 and R.sup.7 do not represent hydrogen at the same time;and non-toxic salts thereof;with the proviso that:1) a compound in which E is --O--CO--NR.sup.3 --, --O--CO--O--, --O--CS--NR.sup.3 -- or --O--CS--O--, J is bond and A is hydrogen, is excluded;2) when E is --CONR.sup.3 --, J is bond, A is Ar and Ar is carbocyclic aryl, then this ring may be substituted by one of C1-15 allyl, C1-15 alkoxy, halogen, nitro, cyano, guanidino, amidino, hydroxy, benzyloxy, --NR.sup.9 R.sup.10 ; and3) when E is --CO--O--, then J is bond and A is hydrogen atom, C3-7 cycloalkyl or Ar.