Patent ID: 6194581
Filing Date: 2001-02-27
Classification: C07D,C07F

Abstract:
A compound having the structure: ##STR13##wherein:A is a 1, 2, 3, 4, 5 or 6 atom bridging species linking C.sup.3 of the pyridine ring with N.sup..alpha.,wherein A is selected from a straight chain or branched chain alkylene moiety having up to six atoms in the backbone thereof, or a substituted alkylene moiety, a straight chain or branched chain alkenylene moiety having up to six atoms in the backbone thereof, or a substituted alkenylene moiety, an alkynylene moiety having up to six atoms in the backbone thereof, or a substituted alkynylene moiety, provided that N.sup..alpha. is not conjugated with an alkenyl or alkynyl moiety;B is a 1, 2, 3 or 4 atom bridging species linking N.sup..alpha. with Z,wherein B is selected from a straight chain or branched chain alkylene moiety having up to four atoms in the backbone thereof, or a substituted alkylene moiety, a straight chain or branched chain alkenylene moiety having up to four atoms in the backbone thereof, or a substituted alkenylene moiety, an alkynylene moiety having up to four atoms in the backbone thereof, or a substituted alkynylene moiety, --O--, --C(O)--, --C(S)--, --N.sup.b (R.sup.b)--, --S--, --S(O)-- and/or --S(O).sub.2 -- containing alkylene moiety, wherein R.sup.b is hydrogen or a lower alkyl moiety; provided, however, that any heteroatom contained in B is separated from N.sup..alpha. by at least 2 carbon atoms, and further provided that when B is a --C(O)-- or --C(S)-- containing alkylene moiety, at least one methylene unit intervenes between the --C(O)-- or --C(S)-- moiety and N.sup..alpha., and further provided that N.sup..alpha. is not conjugated with an alkenyl or alkynyl moiety;Z is hydrogen, furanyl, imidazolyl, 3,4-benzopyrrolidine, or phenyl;R.sup..alpha. is selected from hydrogen or lower alkyl; andR.sup.2, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, or lower alkyl;provided, however, that the following compounds are excluded from the definition of Formula I: compounds wherein A is --CH.dbd.CH--(CH.sub.2).sub.1-5 --CH.sub.2 --, B is alkyl, Z is H or absent, R.sup..alpha. is H, and each of R.sup.2, R.sup.4, R.sup.5 and R.sup.6 are independently alkyl or halo; compounds wherein A is --(CH.sub.2).sub.1-5 --, B and R.sup..alpha. combine to form a B, R.sup..alpha., N.sup..alpha. ring such that B and R.sup..alpha. together are C.sub.4 R.sub.8 or C.sub.5 R.sub.10, wherein R is hydrogen or alkyl, and Z is absent; compounds wherein A is --CH.sub.2 --, B is --CH.sub.2 --CH(CH.sub.3)--CH-R, wherein R is para-tertiarybutylphenyl, Z is absent, R.sup..alpha. is CH.sub.3 or butyl, and each of R.sup.2, R.sup.4, R.sup.5 and R.sup.6 are hydrogen; compounds wherein A is --CH.sub.2 --(CHR).sub.n, wherein R is H or alkyl and n=0 or 1, B is --(CH.sub.2).sub.n --CHR--CH(X)--, wherein R is H, methyl or ethyl, X is phenyl or substituted aryl (substitution selected from halogen, alkyl or alkoxy), and n=0 or 1, Z is phenyl or substituted aryl (substitution selected from halogen, alkyl or alkoxy), R.sup..alpha. is H or alkyl, and each of R.sup.2, R.sup.4, R.sup.5 and R.sup.6 are selected from hydrogen, alkyl or alkenyl; compounds wherein A is --CH(CH.sub.3)--, B is --CH.sub.2 --, --CH.sub.2 --C.sub.6 H.sub.4 -- or --CH.sub.2 --C.sub.10 H.sub.6 --, Z is hydrogen, --C.sub.6 H.sub.5, or --C.sub.10 H.sub.7, R.sup..alpha. is CH.sub.3, and each of R.sup.2, R.sup.4, R.sup.5 and R.sup.6 are hydrogen; compounds wherein A is --CH(CH.sub.3)--, B is --CH.sub.2 --, Z is hydrogen, R.sup..alpha. is hydrogen, and each of R.sup.2, R.sup.4, R.sup.5 and R.sup.6 are hydrogen; compounds wherein A is --CH(CH.sub.3)--, B is --CH.sub.2 --CH.sub.2 --[2,3-(OR).sub.2 C.sub.6 H.sub.3 ], wherein R is methyl or benzyl, and R.sup..alpha. is hydrogen, or B and R.sup..alpha. combine to form a B, R.sup..alpha., N.sup..alpha. ring such that B and R.sup..alpha. together are --C(.dbd.CH.sub.2)--[1,2-(3,4(OR).sub.2 benzo)]--CH.sub.2 CH.sub.2 --, wherein R is methyl or benzyl, Z in all instances is absent, and each of R.sup.2, R.sup.4, R.sup.5 and R.sup.6 are hydrogen; as well as compounds wherein A is --CH(CH.sub.3)-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --, B is --CH.sub.2 --CH.sub.2 --CH(C.sub.6 H.sub.5)-- or --CH(CH.sub.3)--C.sub.6 H.sub.5, Z is phenyl or absent, R.sup..alpha. is hydrogen, and each of R.sup.2, R.sup.4, R.sup.5 and R.sup.6 are hydrogen.