CERTAIN ALKYLENE DIAMINE-SUBSTITUTED PYRAZOLO/1,5-A/1,5- PYRIMIDINES AND PYRAZOLO/1,5-A/-1,3,5-TRIAZINES

• Main Authors: GRIFFITH, DAVID ANDREW, TRAN, JENNIFER, GIANGIORDANO, MARK, BLUM, CHARLES, DE, LOMBAERT STEPHANE, CARPINO, PHILIP ALBERT, DARROW, JAMES W
• Format: Patent
• Language: English
• Published: 03.09.2004
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PHYSICS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; TESTING

Odredjeni alkilen diamin supstituisani pirazolo[1.5-a]-1,5-pirimidini i pirazolo[1,5-a]-1,3,5-triazini. Otkrivena su jedinjenja formule: (I), u kojima R1, R2, R3, R4, R5, R6, i X su definisani u njima. Ova jedinjenja su selektivni modulatori NPY1 receptora. Ova jedinjenja su korisna u tretmanu brojnih CNS poremećaja, metaboličkih poremećaja, i periferalnih poremećaja, naročito poremećaja ishrane i hipertenzije. Metodi tretmana ovakvih poremećaja kao i pakovanih farmaceutskih kompozicija se takodje daju. Jedinjenja pronalaska su takodje korisna kao probe za lokalizaciju NPY1 receptora i kao standardi u ispitivanjima NPY1 receptor vezivanja. Metode uptorebe jedinjenja u proučavanjima receptor lokalizacije su data. Disclosed are compounds of the formula: where R , R , R , R , R , R , and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.