Solid forms of an ASK1 inhibitor

Patent metadata

Field	Value
Publication number	US-9907790-B2
Application number	US-201715481365-A
Country	US
Kind code	B2
Filing date	Apr 6, 2017
Priority date	Dec 23, 2014
Publication date	Mar 6, 2018
Grant date	Mar 6, 2018

Abstract

Crystalline forms of 5-(4-cyclopropyl-1H-imidazol-1-yl)-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-2-fluoro-4-methylbenzamide (Compound I) were prepared and characterized in the solid state:

Also provided are processes of manufacture and methods of using the crystalline forms.

First claim

I claim:

1. A method of treating a disease mediated, at least in part, by ASK1 in a patient in need thereof comprising administering a therapeutically effective amount of crystalline 5-(4-cyclopropyl-1H-imidazol-1-yl)-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-2-fluoro-4-methylbenzamide (Compound I Form I) characterized by an X-ray powder diffractogram comprising the following peaks: 16.7, 21.3, and 22.8° 2θ±0.2° 2θ, as determined on a diffractometer using Cu-Kα radiation at a wavelength of 1.5406 Å, wherein the disease is diabetes, diabetic nephropathy, kidney disease, kidney fibrosis, lung fibrosis, idiopathic pulmonary fibrosis (IPF), liver fibrosis, pulmonary hypertension, nonalcoholic steatohepatitis, liver disease, alcoholic liver disease, alcoholic hepatitis, an inflammatory condition, an autoimmune disease, a proliferative disease, a transplantation rejection, a disease involving impairment of cartilage turnover, a congenital cartilage malformation, or a disease associated with hypersecretion of IL6.

2. The method of claim 1 , further comprising administering another therapeutic agent.

3. The method of claim 2 , wherein the additional therapeutic agent is filgotinib.

4. The method of 2 , wherein the additional therapeutic agent is a compound of formula:

or a salt thereof.

5. The method of claim 1 , wherein the disease is an inflammatory condition.

6. The method of claim 1 , wherein the disease is Crohn's disease.

7. The method of claim 1 , wherein the disease is rheumatoid arthritis.

8. The method of claim 1 , wherein the disease is inflammatory bowel disease.

9. The method of claim 1 , wherein the disease is non-alcoholic steatohepatitis.

10. The method of claim 1 , wherein the disease is alcoholic steatohepatitis.

Assignees

• Gilead Sciences Inc

Inventors

• Notte Gregory

Classifications

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P43/00

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