Fused bicyclic pyrimidine derivatives
AssigneeKyorin Pharmaceutical Co., Ltd.
InventorsShigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru Izawa
Life of this patent
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Abstract
A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following general formula (1): wherein the rings A and B are each a benzene ring having 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring; R is a hydrogen atom, a C1 to C6 alkyl group, a C1 to C6 alkylcarbonyl group, or a C1 to C6 alkylsulfonyl group; m is 1 or 2; and n is 2 or 3.
Claims12
A compound of formula (1), or a salt thereof:
- wherein the rings A and B are each a benzene ring, which may have 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring selected from the group consisting of
- each independently selected from the group consisting of a halogen atom, a C1 to C6 alkyl group, which may be substituted with a halogen atom, and a C1 to C6 alkoxyl group;
- the ring C is a 5- to 7-membered nitrogen-containing ring, which may contain, aside from the nitrogen atom, 1 to 3 heteroatoms selected from the group consisting of a nitrogen atom, a sulfur atom, and an oxygen atom;
- the ring C may further contain a substituent (a substituent selected from the group consisting of a C1 to C6 alkyl group, a hydroxyl group, a C1 to C6 alkoxyl group, a formyl group, a C1 to C6 alkylcarbonyl group, a C1 to C6 alkoxycarbonyl group, a carbamoyl group, a mono- or di-substituted C1 to C6 alkylcarbamoyl group, a C1 to C6 alkylsulfonyl group, an amino group, a mono- or di-substituted C1 to C6 alkylamino group, a C1 to C6 alkylcarbonylamino group, a C1 to C6 alkoxycarbonylamino group, a C1 to C6 alkylsulfonylamino group, an oxo group, a 6-membered aromatic heterocyclic group, and a substituent represented by the following formula:
- wherein the ring D is a 3- to 7-membered nonaromatic heterocyclic ring, which may contain, aside from the nitrogen atom, 1 to 3 heteroatoms selected from the group consisting of a nitrogen atom, a sulfur atom, and an oxygen atom and may further contain 1 or 2 oxo-substituted carbon atoms);
- R is a hydrogen atom, a C1 to C6 alkyl group, a C1 to C6 alkylcarbonyl group, or a C1 to C6 alkylsulfonyl group;
- m is 1 or 2;
- and
- n is 2 or 3.
Dependencies are inferred from the claim text.