Compositions for modulating a kinase cascade and methods of use thereof

US10323001B2 · kind B2 · utility

Assignee

• Athenex, Inc. · US

Inventors

• David G. Hangauer, Jr. · East Amherst, US
• Debasis Patra · Manlius, US
• Jeremy A. Cody · Clifton Springs, US
• Grant J. Palmer · Clifton Park, US
• Paul K. Isbester · New York, US
• Jonathon S. Salsbury · Madison, US

Key dates

• Filing date: Dec 21, 2016
• Grant date: Jun 18, 2019
• Expiry date: Dec 21, 2036

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/13
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl) pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.