SUBSTITUTED BENZOPYRAZOLO[1,5-a][1,4]DIAZEPINES AS GABA POSITIVE ALLOSTERIC MODULATORS

Abstract: this disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof, or an n-oxide thereof) of formula (i), which are positive allosteric modulators of one or more gaba-a receptors, e.g., which are peripherally restricted, positive allosteric modulators of one or more gaba-a receptors; e.g., which are positive allosteric modulators of one or more gaba-a receptors and which selectively target the peripheral nervous system and organs of the body, and which do not substantially pass through the blood-brain barrier. said compounds are useful e.g., for the treatment of systemic diseases of the body, e.g., diseases in which modulation of one or more peripherally restricted gaba-a receptors is beneficial (e.g., diseases or disorders which are mediated by gaba-a neuronal activitye. this disclosure also features pharmaceutical compositions containing the chemical entities described herein as well as methods of using same for the treatment of systemic diseases of the body.

Inventor(s): Yifang Huang, Pankaj Jay Pasricha, James C. Barrow, Ingrid Buchler, Michael Poslusney

CPC Classification: C07D487/04 (Ortho-condensed systems)

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