Patent ID: 6121283
Filing Date: 2000-09-19
Classification: A61P,C07D

Abstract:
A compound of the formula ##STR70## or the stereoisomers, pharmaceutically acceptable salts and hydrates thereof, wherein G is selected from:(a) a phenyl or heterocyclic ring wherein said heterocyclic ring contains a total of from 3 to 14 ring atoms, wherein said heterocyclic ring incorporates a total of from 1 to 4 ring heteroatoms selected independently from oxygen, nitrogen, and sulfur, wherein the individual rings of said heterocyclic ring may be independently saturated, partially saturated or aromatic, and wherein each of said phenyl or heterocyclic rings may have optionally from 1 to 4 substituents selected independently from halogen, hydroxy, cyano, nitro, oxo, thioxo, aminosulfonyl, phenyl, phenoxy, phenylthio, benzyl, benzoyl, benzyloxy, (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.4)perfluoroalkyl, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.4)perfluoroalkoxy, (C.sub.1 -C.sub.10)alkoxycarbonyl, (C.sub.1 -C.sub.10)alkylthio, (C.sub.1 -C.sub.10)alkylamino, di(C.sub.1 -C.sub.10)alkylamino, (C.sub.1 -C.sub.10)alkylaminocarbonyl, di(C.sub.1 -C.sub.10)alkylaminocarbonyl, (C.sub.1 -C.sub.10)acyl, (C.sub.1 -C.sub.10)perfluoroacyl, (C.sub.1 -C.sub.10)acyloxy, (C.sub.1 -C.sub.6)acylamino and (C.sub.1 -C.sub.6)perfluoroacylamino;(b) --CH.sub.2 CN, ##STR71## (d) (C.sub.2 -C.sub.12)alkyl or (C.sub.2 -C.sub.12)perfluoroalkyl wherein each of said (C.sub.2 -C.sub.12)alkyl and (C.sub.2 -C.sub.12)perfluoroalkyl is substituted optionally with from 1-3 substituents selected independently from:(1) phenyl, halogen, nitro, cyano, hydroxy, --NR.sup.1 R.sup.2, --OCOR.sup.3, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)perfluoroalkoxy, (C.sub.1 -C.sub.4)thioalkoxy or (C.sub.1 -C.sub.4)perfluorothioalkoxy,where R.sup.1 and R.sup.2 in the definition of --NR.sup.1 R.sup.2 are each selected independently from hydrogen, formyl, phenyl, benzyl, benzoyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.3 -C.sub.8)cycloalkenyl, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)perfluoroalkyl, (C.sub.1 -C.sub.10)alkoxycarbonyl, (C.sub.1 -C.sub.6)acyl, (C.sub.1 -C.sub.6)perfluoroacyl, aminocarbonyl, (C.sub.1 -C.sub.10)alkylaminocarbonyl, di(C.sub.1 -C.sub.10)alkylaminocarbonyl, aminosulfonyl, (C.sub.1 -C.sub.4)alkylaminosulfonyl, di(C.sub.1 -C.sub.4)alkylaminosulfonyl, (C.sub.1 -C.sub.4)perfluoroalkylaminosulfonyl, (C.sub.1 -C.sub.4)perfluoroalkylaminosulfonyl, (C.sub.1 -C.sub.4)alkylsulfonyl, and(C.sub.1 -C.sub.4)perfluoroalkylsulfonyl,or where R.sup.1 and R.sup.2, taken together with the nitrogen atom to which they are attached, form a saturated, partially-saturated or aromatic heterocyclic ring, wherein said heterocyclic ring contains a total of from 3 to 14 ring atoms and incorporates optionally an additional 1 to 4 ring heteroatoms selected independently from oxygen, nitrogen and sulfur, wherein said heterocyclic ring may have optionally from 1 to 4 substituents selected independently from halogen, hydroxy, cyano, nitro, oxo, thioxo, aminosulfonyl, phenyl, phenoxy, phenylthio, benzyl, benzoyl, benzyloxy, (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.4)perfluoroalkyl, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.4)perfluoroalkoxy, (C.sub.1 -C.sub.10)alkoxycarbonyl, (C.sub.1 -C.sub.10)alkylthio, (C.sub.1 -C.sub.10)alkylamino, di(C.sub.1 -C.sub.10)alkylamino, (C.sub.1 -C.sub.10)alkylaminocarbonyl, di(C.sub.1 -C.sub.10)alkylaminocarbonyl, (C.sub.1 -C.sub.10)acyl, (C.sub.1 -C.sub.10)perfluoroacyl, (C.sub.1 -C.sub.10)acylamino, and (C.sub.1 -C.sub.10)acyloxy,where R.sup.3 in the definition of --OCOR.sup.3 is selected from --NR.sup.1 R.sup.2, phenyl, (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.4)perfluoroalkyl, (C.sub.1 -C.sub.6)alkoxy and (C.sub.1 -C.sub.6)perfluoroalkoxy,(2) (C.sub.3 -C.sub.8)cycloalkyl or (C.sub.3 -C.sub.8)cycloalkenyl wherein each of said (C.sub.3 -C.sub.8)cycloalkyl and (C.sub.3 -C.sub.8)cycloalkenyl may have optionally from 1 to 4 substituents selected independently from halogen, hydroxy, cyano, nitro, oxo, thioxo, aminosulfonyl, phenyl, phenoxy, phenylthio, benzyl, benzoyl, benzyloxy, (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.4)perfluoroalkyl, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.4)perfluoroalkoxy, (C.sub.1 -C.sub.10)alkoxycarbonyl, (C.sub.1 -C.sub.10)alkylthio, (C.sub.1 -C.sub.10)alkylamino, di(C.sub.1 -C.sub.10)alkylamino, (C.sub.1 -C.sub.10)alkylaminocarbonyl, di(C.sub.1 -C.sub.10)alkylaminocarbonyl, (C.sub.1 -C.sub.10)acyl, (C.sub.1 -C.sub.10)perfluoroacyl, (C.sub.1 -C.sub.10)acylamino, (C.sub.1 -C.sub.10)perfluoroacylamino, (C.sub.1 -C.sub.10)acyloxy, and(3) a saturated, partially-saturated or aromatic heterocyclic ring containing a total of from 3 to 14 ring atoms, wherein said heterocyclic ring incorporates a total of from 1 to 4 ring heteroatoms selected independently from oxygen, nitrogen and sulfur, wherein said heterocyclic ring may have optionally from 1 to 4 substituents selected independently from halogen, hydroxy, cyano, nitro, oxo, thioxo, aminosulfonyl, phenyl, phenoxy, phenylthio, benzyl, benzoyl, benzyloxy, (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.4)perfluoroalkyl, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.4)perfluoroalkoxy, (C.sub.1 -C.sub.10)alkoxycarbonyl, (C.sub.1 -C.sub.10)alkylthio, (C.sub.1 -C.sub.10)alkylamino, di(C.sub.1 -C.sub.10)alkylamino, (C.sub.1 -C.sub.10)alkylaminocarbonyl, di(C.sub.1 -C.sub.10)alkylaminocarbonyl, (C.sub.1 -C.sub.10)acyl, (C.sub.1 -C.sub.10)perfluoroacyl, (C.sub.1 -C.sub.10)acylamino, (C.sub.1 -C.sub.10)perfluoroacylamino, (C.sub.1 -C.sub.10)acyloxy,provided that (C.sub.2 -C.sub.12)alkyl does not include unsubstituted allyl;(e) (C.sub.3 -C.sub.8)cycloalkyl or (C.sub.3 -C.sub.8)cycloalkenyl wherein each of said (C.sub.3 -C.sub.8)cycloalkyl and (C.sub.3 -C.sub.8)cycloalkenyl may have optionally from 1 to 4 substituents selected independently from halogen, hydroxy, cyano, nitro, oxo, thioxo, aminosulfonyl, phenyl, phenoxy, phenylthio, benzyl, benzoyl, benzyloxy, (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.4)perfluoroalkyl, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.4)perfluoroalkoxy, (C.sub.1 -C.sub.10)alkoxycarbonyl, (C.sub.1 -C.sub.10)alkylthio, (C.sub.1 -C.sub.10)alkylamino, di(C.sub.1 -C.sub.10)alkylamino, (C.sub.1 -C.sub.10)alkylaminocarbonyl, di(C.sub.1 -C.sub.10)alkylaminocarbonyl, (C.sub.1 -C.sub.10)acyl, (C.sub.1 -C.sub.10)perfluoroacyl, (C.sub.1 -C.sub.10)acylamino, (C.sub.1 -C.sub.10)perfluoroacylamino, (C.sub.1 -C.sub.10)acyloxy; and(f) --(CH.sub.2).sub.n COR.sup.4 where R.sup.4 in the definition of --(CH.sub.2).sub.n COR.sup.4 is selected from hydroxy, phenyl, --NR.sup.1 R.sup.2, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)perfluoroalkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)perfluoroalkoxy, (C.sub.3 -C.sub.8)cycloalkyl, and (C.sub.3 -C.sub.8)cycloalkenyl,where n is an integer from 1 to 4.