Appeal No. 94-4265
Application 08/035,915
4
R represents a C -C alkyl group;
1 6
a non-aromatic heterocyclic group having from 4 to 8 ring carbon atoms and having one or
two ring nitrogen atoms and optionally containing an oxygen atom, a sulphur atom, a sulphinyl group,
a sulphonyl group or a carbonyl group, and optionally having one or more substituents attached to
the carbon atoms or to any nitrogen atom, selected from the group consisting of (1) substituents for
attachment to the ring carbon atoms selected from the group consisting of C -C alkyl groups,
1 6
cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl groups, C -C alkoxyalkyl groups,
2 8
methoxycarbonylmethyl, ethoxycarbonylmethyl, t-butoxycarbonylmethyl, benzyloxycarbonylethyl,
methoxycarbonylpropyl groups, C -C cyanoalkyl groups, C -C haloalkyl groups, C -C alkoxy2 7 1 6 1 6
groups, halogen atoms, C -C aliphatic acyloxy groups, C -C aliphatic acylamino groups, cyano1 6 1 6
group, azido group, carboxy group, C -C alkoxycarbonyl groups, carbamoyl group, C -C alkylthio16
2 7 1 6
groups, C -C alkylsulphinyl groups, C -C alkylsulphonyl groups, nitro group; and (2) substituents1 6 1 6
for attachment to said ring nitrogen atom(s) selected from the group consisting of C -C alkyl groups,
1 6
C -C alkenyl groups, C -C alkynyl groups, C -C cycloalkyl groups, cyclopropylmethyl, cyclo-2 6 2 6 3 8
butylmethyl, cyclopentylmethyl, cyclohexylmethyl, cycloheptylmethyl, 2-cyclopentylethyl, 2-cyclo-
hexylethyl, 3-cyclopentylpropyl, 2-cyclopentylpropyl, 3-cyclohexylpropyl, 2-cyclohexylpropyl, 4-
cyclopentylbutyl, 3-cyclohexylbutyl, phenyl, naphthyl groups, benzyl, phenethyl, 3-phenylpropyl, C -
1
C aliphatic acyl groups, cyclopropanecarbonyl, cyclobutanecarbonyl, cyclopentanecarbonyl,
6
cyclohexanecarbonyl, cyclopropylacetyl, cyclobutylacetyl, cyclopentylacetyl, cyclohexylacetyl, 3-
cyclopentylpropionyl, 3-cyclohexylpropionyl, 4-cyclopentylbutyryl, 4-cyclohexylbutyryl benzoyl, l-
,
naphthoyl, 2-naphthoyl groups, phenylacetyl, l-naphthylacetyl, 3-phenylpropionyl, hydratropoyl,
cinnamoyl, phenylpropioloyl, furoyl, thenoyl, nicotinoyl, isonicotinoyl, 4-thiazolecarbonyl, 5-
pyrimidinecarbonyl, 2-pyrazinecarbonyl, 2-thienylacetyl, 3-(2-thienyl)propionyl, 4-thiazolylacetyl, 2-
pyridylacetyl, 4-pyridylacetyl, 5-pyrimidinylacetyl, 1-aziridinylacetyl, 1-azetidinylacetyl, 3-
azetidinylacetyl, l-pyrrolidinylacetyl, 2-pyrrolidinylacetyl, 3-pyrrolidinylacetyl, 3-(2-pyrrolidinyl)-
propionyl, piperidinoacetyl, 2-piperidinylacetyl, 4-piperidinylacetyl, morpholinoacetyl, l-aziridine-
carbonyl, 1-azetidinecarbonyl, 3-azetidinecarbonyl, 1-pyrrolidinecarbonyl, 2-pyrrolidinecarbonyl, 3-
pyrrolidinecarbonyl, 1-piperidinecarbonyl 2-piperidinecarbonyl, 4-piperidinecarbonyl, 4-
morpholinecarbonyl, phenacyl group, sulpho group, C -C alkoxysulphonyl groups, C -C1 6 1 6
alkylsulphonyl groups, C -C alkenylsulphonyl groups, C -C alkynylsulphonyl groups, cyclo-2 6 2 6
propylsulphonyl, cyclobutylsulphonyl, cyclopentylsulphonyl, cyclohexylsulphonyl, cyclopropyl-
methylsulphonyl, cyclobutylmethylsulphonyl, cyclopentylmethylsulphonyl, cyclohexylmethyl-
sulphonyl, 2-cyclopentylethylsulphonyl, 2-cyclohexylethylsulphonyl, 3-cyclopentylpropyl-sulphonyl,
2-cyclopentylpropylsulphonyl, phenylsulphonyl, l-naphthylsulphonyl, 2-naphthyl-sulphonyl,
benzylsulphonyl, phenethylsulphonyl, 3-phenylpropylsulphonyl, 2-phenylpropyl-sulphonyl, 2-
thienylsulphonyl, 4-thiazolylsulphonyl, 2-pyridylsulphonyl, 4-pyridyl-sulphonyl, 2-
thienylmethylsulphonyl, 3-(2-thienyl)propylsulphonyl, 4-thiazolylmethylsulphonyl, 2-pyridyl-
methylsulphonyl, 4-pyridylmethylsulphonyl group, groups of the formula
-13-
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Last modified: November 3, 2007