US 2010/0063092 A1 · 3-CYANO-4-(4-PHENYL-PIPERIDIN-1-YL)-PYRIDIN-2-ONE DERIVATIVES

Abstract

The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

Claims31

Dependent claims

A compound of formula (I″)

including any stereochemically isomeric form thereof, wherein
R1 is C4-6 alkyl, or C1-3 alkyl substituted with C3-7 cycloalkyl;
R2 is hydrogen;
hydroxyl;
fluoro;
C1-4 alkyl substituted with hydroxyl;
C1-4 alkyl substituted with fluoro;
or C1-4alkyloxy substituted with fluoro;
R3 is hydrogen or halo;
provided that if R3 is halo, then R2 is hydroxyl;
or a pharmaceutically acceptable salt thereof or a solvate thereof.

8 more elements

The method of claim 40, wherein the central nervous system disorder is (1) an anxiety disorder selected from the group consisting of agoraphobia, generalized anxiety disorder (GAD), obsessive-compulsive disorder (OCD), panic disorder, posttraumatic stress disorder (PTSD), social phobia and other phobias;

(2) a psychotic disorder selected from the group consisting of schizophrenia, delusional disorder, schizoaffective disorder, schizophreniform disorder and substance-induced psychotic disorder;
(3) a personality disorder selected from the group consisting of obsessive-compulsive personality disorder and schizoid, schizotypal disorder;
(4) a substance-related disorder selected from the group consisting of alcohol abuse, alcohol dependence, alcohol withdrawal, alcohol withdrawal delirium, alcohol-induced psychotic disorder, amphetamine dependence, amphetamine withdrawal, cocaine dependence, cocaine withdrawal, nicotine dependence, nicotine withdrawal, opioid dependence and opioid withdrawal;
(5) an eating disorder selected from the group consisting of anorexia nervosa and bulimia nervosa;
(6) a mood disorder selected from the group consisting of bipolar disorders (I & II), cyclothymic disorder, depression, dysthymic disorder, major depressive disorder and substance-induced mood disorder;
(7) a migraine;
(8) epilepsy or a convulsive disorder selected from the group consisting of generalized nonconvulsive epilepsy, generalized convulsive epilepsy, petit mal status epilepticus, grand mal status epilepticus, partial epilepsy with or without impairment of consciousness, infantile spasms, epilepsy partialis continua, and other forms of epilepsy;
(9) a childhood disorder selected from the group consisting of attention-deficit/hyperactivity disorder;
and (10) a cognitive disorder selected from the group consisting of delirium, substance-induced persisting delirium, dementia, dementia due to HIV disease, dementia due to Huntington's disease, dementia due to Parkinson's disease, dementia of the Alzheimer's type, substance-induced persisting dementia and mild cognitive impairment.

6 more elements

Dependencies are inferred from the claim text.

3-cyano-4-(4-phenyl-piperidin-1-yl)-pyridin-2-one derivatives

Life of this patent

3-cyano-4-(4-phenyl-piperidin-1-yl)-pyridin-2-one derivatives

Life of this patent

Abstract

Claims31