N-(4-{ 2-[4-aryl-piperazin-1-yl]ethyl} cyclohexyl)-acetamide derivatives for the treatment of neuropsychiatric disorders

• Main Authors: ROBERT, PHILIPPE, DANVY, DENIS, LECOMTE, JEANNE-MARIE, CAPET, MARC, LIGNEAU, XAVIER, SCHWARTZ, JEANARLES, LEVOIN, NICOLAS, BERREBI-BERTRAND, ISABELLE, CALMELS, THIERRY
• Format: Patent
• Language: English
• Published: 25.11.2011
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Disclosed are N-(4-{ 2-[4-aryl-piperazin-1-yl]ethyl} cyclohexyl)-acetamide derivatives as represented by the general formula (I), wherein Z is -NH-CH<, and NR1R2 is a 4-aryl-piperazine moiety; and wherein the remaining substituents are as defined herein. Of particular importance are the compounds N-(4-{ 2-[4-(3-cyanophenyl)piperazin-1-yl]ethyl} cyclohexyl)-2-methoxyacetamide, N-(4-{ 2-[4-(3,5-bistrifluoromethylphenyl)piperazin-1-yl]ethyl} cyclohexyl)-2-cyanoacetamide, 2-cyano-N-(4-{ 2-[4-(3-methanesulfonylphenyl)piperazin-1-yl]ethyl} cyclohexyl)acetamide, 2-cyano-N-[4-(2-{ 4-[3-(1-hydroxypropyl)phenyl]piperazin-1-yl} ethyl)cyclohexyl]acetamide, N-(4-{ 2-[4-(3-cyanophenyl)piperazin-1-yl]ethyl} cyclohexyl)-4,4,4-trifluorobutanamide and N-(4-{ 2-[4-(3-cyanophenyl)piperazin-1-yl]ethyl} cyclohexyl)-3-methoxypropanamide. Further disclosed is pharmaceutical composition which comprises a therapeutically effective amount of at least one compound as defined above and a pharmaceutically acceptable vehicle or excipient for the treatment of illnesses involving the dopamine D3 receptor and particularly for the treatment of neuropsyachiatric illness selected from Parkinson's disease, schizophrenia, dementia, psychosis or psychotic states, depression, mania, anxiety, dyskinesias, equilibration disorders and Gilles de la Tourette's disease.