US 8,044,047 B2 · 5-substituted benzoxazines

Abstract

The present invention is concerned with 5-substituted benzoxazine derivatives of formula (I) wherein X, R1 and R2 are as described herein, as well as their manufacture, pharmaceutical compositions containing them. Compounds of the present invention are 5-HT5A receptor antagonists, and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.

Claims15

Dependent claims

A compound of formula (I)

wherein:
X is a bond, —NH—, —NH—S(O)2—, or —NH—C(O)—CH2—;
R1 is halo, C1-7-alkyl, —NRaRb, cyano, nitro, or is phenyl or 3- to 8-membered cycloalkyl, each of which is optionally substituted by one or more halo;
R2 is cycloalkyl or a 5- or 6-membered heterocycloalkyl, each optionally with phenyl or a 5- or 6-membered heteroaryl, wherein the phenyl or 5- or 6-membered heteroaryl each is optionally and independently substituted with one or more halo, C1-7-alkyl and/or C1-7-alkoxy;
Ra and Rb is each independently hydrogen or C1-7-alkyl;
or a pharmaceutically acceptable salt thereof.

3 more elements

Dependencies are inferred from the claim text.

5-substituted benzoxazines

Life of this patent

5-substituted benzoxazines

Life of this patent

Abstract

Claims15