Merck Sharp + Dohme Corp.

Rexahn Pharmaceuticals, Inc.

Cerecor, Inc.

Avalo Therapeutics, Inc.

Cardioxyl Pharmaceuticals, Inc.

Reza Mazhari

Young Bok Lee

Deog Joong Kim

Blake Paterson

James Vornov

Todd D Nelson

Djelila Mezaache

Rachel M Garner

Daniel Edward Emrich

Godefridus J Peters

Dzjemma Sarkisjan

Blake M Paterson

The disclosed subject matter provides certain polymorphic forms of Compound (I) as well as pharmaceutical compositions comprising Compound (I) or such polymorphic forms, and methods of using or making such compounds and pharmaceutical compositions. It has now been discovered that Compound (I) can exist in multiple crystalline forms (polymorphs). One particular crystalline form, Form II, has been found to be more thermodynamically stable and, thus, likely more suitable for bulk preparation and handling than other polymorphic forms. Efficient and economic methods have been developed to prepare Compound (I) and Form II in high purity on a large scale. In animal studies, Form II has demonstrated safety and efficacy in treating depressive disorders and, when micronized, improved absorption compared to non-micronized Form II.

Compounds, compositions and methods

The disclosed subject matter provides certain polymorphic forms of Compound (I) as well as pharmaceutical compositions comprising Compound (I) or such polymorphic forms, and methods of using or making such compounds and pharmaceutical compositions. It has now been discovered that Compound (I) can exist in multiple crystalline forms (polymorphs). One particular crystalline form, Form II, has been found to be more thermodynamically stable and, thus, likely more suitable for bulk preparation and handling than other polymorphic forms. Efficient and economic methods have been developed to prepare Compound (I) and Form II in high purity on a large scale. In animal studies, Form II has demonstrated safety and efficacy in treating depressive disorders and, when micronized, improved absorption compared to non-micronized Form II. 

The disclosed subject matter provides methods using and kits comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

Quinoxalinyl-piperazinamide methods of use

The disclosed subject matter provides methods using and kits comprising a compound of formula (I) or a hydrate, a solvate, or a pharmaceutically acceptable salt thereof. The disclosed subject matter further provides a method of treating one or more symptoms of cancer comprising administering to a subject in need thereof a compound of formula (I) and a process for preparing such.

Fluorocyclopentenylcytosine methods of use

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Towson, MD, United States of America

Reza Mazhari