PYRROLE DERIVATIVES AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISORDERS SUCH AS ALZHEIMER'S AND PARKINSON'S DISEASE

• Main Authors: NAVNATH POPAT KARCHE, NEELIMA SINHA, VENKATA P. PALLE, GOURHARI JANA, RAJENDER KUMAR KAMBOJ, AJAY RAMCHANDRA TILEKAR
• Format: Patent
• Language: English; Spanish
• Published: 06.12.2013
• 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 is a compound of formula (I) wherein 'a' and R1-R5 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the α7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereofs, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like. Se describe un compuesto de la fórmula (I) en donde 'a' y R1-R5 son como se describen en el presente, como un modulador de receptores de acetilcolina nicotínica particularmente el subtipo a7, en un sujeto en la necesidad del mismo, así como los análogos, profármacos, análogos de manera isotópica sustituidos, metabolitos, sales farmacéuticamente aceptables, polimorfos, solvatos, isómeros, clatratos y co-cristales de los mismos, para uso ya sea solos o en combinaciones con otros medicamentos adecuados y composiciones farmacéuticas que contienen dichos compuestos y análogos. También se describen procesos de preparación de los compuestos y los usos deseados de los mismos en terapia, particularmente en el profilaxis y terapia de desórdenes como enfermedad Alzheimer, daño cognitivo medio, demencia senil y similares.