Patent ID: 6015904
Filing Date: 2000-01-18
Classification: A61K,C07B,C07D,C07K

Abstract:
A stable hydrazone having the formula:R.sup.44 (C.dbd.O).sub.s (R.sup.45)N--N.dbd.CR.sup.80 R.sup.81wherein:s is 0 or 1;R.sup.44 is selected from the group:aryl substituted with 1 R.sup.59 ;and heterocycle substituted with 1 R.sup.59 ;R.sup.45 is selected from the group:hydrogen and C.sub.1 -C.sub.6 alkyl,R.sup.59 is a chemically reactive moiety selected from the group:alkyl substituted with halogen;acid anhydride;acid halide;active ester;isothiocyanate;maleimide;R.sup.80 and R.sup.81 are independently selected from the group:H;C.sub.1 -C.sub.10 alkyl;--CN;--CO.sub.2 R.sup.85 ;--C(.dbd.O)R.sup.85 ;--C(.dbd.O)N(R.sup.85).sub.2 ;C.sub.2 -C.sub.10 1-alkene substituted with 0-3 R.sup.84 ;C.sub.2 -C.sub.10 1-alkyne substituted with 0-3 R.sup.84 ;aryl substituted with 0-3 R.sup.84 ;unsaturated heterocycle substituted with 0-3 R.sup.84 ; andunsaturated carbocycle substituted with 0-3 R.sup.84 ;provided that when one of R.sup.80 and R.sup.81 is H or alkyl, then the other is not H or alkyl;or, alternatively, R.sup.80 and R.sup.81, may be taken together with the shown divalent carbon radical to form: ##STR17## wherein: R.sup.82 and R.sup.83 are independently selected at each occurrence from the group:H;R.sup.84 ;C.sub.1 -C.sub.10 alkyl substituted with 0-3 R.sup.84 ;C.sub.2 -C.sub.10 alkenyl substituted with 0-3 R.sup.84 ;C.sub.2 -C.sub.10 alkynyl substituted with 0-3 R.sup.84 ;aryl substituted with 0-3 R.sup.84 ;heterocycle substituted with 0-3 R.sup.84 ; andcarbocycle substituted with 0-3 R.sup.84 ;or, alternatively,R.sup.82, R.sup.83 may be taken together to form a fused aromatic or heterocyclic ring; anda and b indicate the positions of optional double bonds;n is 0 or 1,R.sup.84 is independently selected at each occurrence from the group: .dbd.O, F, Cl, Br, I, --CF.sub.3, --CN, --CO.sub.2 R.sup.85, --C(.dbd.O)R.sup.85, --C(.dbd.O)N(R.sup.85).sub.2, --CH.sub.2 OR.sup.85, --OC(.dbd.O)R.sup.85, --OC(.dbd.O)OR.sup.85a, --OR.sup.85, --OC(.dbd.O)N(R.sup.85).sub.2, --NR.sup.85 C(.dbd.O)R.sup.85, --NR.sup.86 C(.dbd.O)OR.sup.85a, --NR.sup.85 C(.dbd.O)N(R.sup.85).sub.2, --SO.sub.3 Na, --NR.sup.86 SO.sub.2 N(R.sup.85 ).sub.2, --NR.sup.86 SO.sub.2 R.sup.85a, --SO.sub.3 H, --SO.sub.2 R.sup.85a, --SR.sup.85, --S(.dbd.O)R.sup.85a, --SO.sub.2 N(R.sup.85).sub.2, --N(R.sup.85).sub.2, N(R.sup.85).sub.3.sup.+, --NHC(.dbd.NH)NHR.sup.85, --C(.dbd.NH)NHR.sup.85, .dbd.NOR.sup.85, --C(.dbd.O)NHOR.sup.85, --OCH.sub.2 CO.sub.2 H, 2-(1-morpholino)ethoxy;R.sup.85, R.sup.85a, and R.sup.86 are independently selected at each occurrence from the group: hydrogen, C.sub.1 -C.sub.6 alkyl.