(Oxo-pyrazolo[1,5a]pyrimidin-2-yl)alkyl-carboxamides
AssigneeNeurogen Corporation
InventorsGuiying Li, John Peterson, Pamela Albaugh
Life of this patent
Estimating the term…
Abstract
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof where the variables R1, R2, A, R4, R5, R6, R6′, n, and W are defined herein. These compounds bind to the benzodiazepine site of GABAA receptors are provided and, therefore can be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals.
Claims66
A method for the treatment of anxiety, depression, a sleep disorder selected from primary insomnia, circadian rhythm sleep disorder, dyssomnia NOS, parasomnias including nightmare disorder, sleep terror disorder, sleep disorders secondary to depression, anxiety and/or other mental disorders and substance-induced sleep disorder, or attention deficit disorder, comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of Formula I where Formula I is
- or a pharmaceutically acceptable salt thereof, wherein
- n is 1, 2, or 3;
- R1 and R2 are independently chosen from hydrogen, halogen, hydroxy, amino, mono- and di(C1–C6)alkyl amino, halo(C1–C6)alkyl, halo(C1–C6)alkoxy, C1–C6 alkyl and C1–C6 alkoxy;
- or
- R1 and R2 together with the atoms with which they are attached form a partially saturated or unsaturated carbocyclic ring of from 3 to 8 carbon atoms, wherein the ring is optionally substituted by up to 5 substituents independently chosen from halogen, hydroxy, amino, mono- and di(C1–C6)alkyl amino, halo(C1–C6)alkyl, halo(C1–C6)alkoxy, C1–C6 alkyl and C1–C6 alkoxy;
- R3, R4 and R5 are independently chosen from hydrogen;
- C1–C6 acyl;
- and C1–C6 alkyl;
- wherein each C1–C6 acyl and C1–C6 alkyl is optionally substituted with up to three substituents independently chosen from halogen, hydroxy, halo(C1–C2)alkyl, halo(C1–C2)alkoxy, methoxy, ethoxy, C3–C7 cycloalkyl, phenyl, pyridyl, and pyrimidyl, wherein each of phenyl, pyridyl, and pyrimidyl is optionally substituted with up to three groups independently selected from halogen, C1–C6 alkyl, C1–C6 alkoxy, hydroxy and amino;
- R6 and R6′ are independently selected at each occurrence from hydrogen and C1–C6 alkyl;
- W is aryl or heteroaryl, each of which is optionally substituted with up to 5 groups independently selected from hydrogen, halogen, hydroxy, amino, mono- or di(C1–C6)alkyl amino, halo(C1–C6)alkyl, halo(C1–C6)alkoxy, C1–C6 alkyl, and C1–C6 alkoxy.
Dependencies are inferred from the claim text.