Solid forms of 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one as TOR kinase inhibitors

Patent metadata

Field	Value
Publication number	US-9981971-B2
Application number	US-201615205114-A
Country	US
Kind code	B2
Filing date	Jul 8, 2016
Priority date	Apr 16, 2014
Publication date	May 29, 2018
Grant date	May 29, 2018

Abstract

Provided herein are formulations, processes, solid forms and methods of use relating to the Compound for formula 1:

having the name 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and tautomers thereof.

First claim

What is claimed is:

1. An amorphous form of the compound of formula (I):

or a tautomer thereof,
wherein the amorphous form has an X-ray powder diffraction pattern as shown in FIG. 28 .

2. The amorphous form of claim 1 , which has a differential scanning calorimetry thermogram comprising an endotherm between 160° C.±5° C. and 200° C.±5° C. with a maximum at 188.1° C.±5° C.

3. The amorphous form of claim 1 , which has a glass transition temperature at 120° C.±5° C.

4. The amorphous form of claim 1 , which is pure.

5. A method for modulating target of rapamycin kinase activity in a subject, comprising administering to a subject in need thereof an effective amount of the amorphous form of claim 1 .

6. The method of claim 5 , wherein the subject suffers from a condition, disorder or disease selected from the group consisting of an inflammatory condition, an immunological condition, a cardiovascular condition, a neurological disorder, a neurodegenerative disease, an age-related disease, diabetes and obesity.

Assignees

• Signal Pharm Llc

Inventors

• Boersen Nathan

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P37/02

  Immunomodulators · CPC title