Solid forms of an ASK1 inhibitor

Patent metadata

Field	Value
Publication number	US-10946004-B2
Application number	US-201916530205-A
Country	US
Kind code	B2
Filing date	Aug 2, 2019
Priority date	Dec 23, 2014
Publication date	Mar 16, 2021
Grant date	Mar 16, 2021

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

We claim:

1. A method of treating chronic kidney disease in a patient in need thereof comprising administering a therapeutically effective amount of crystalline 5-4-cyclopropyl-1 H-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.

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 claim 2 , wherein the additional therapeutic agent is a compound of formula:

or a salt thereof.

5. A method of treating diabetic kidney disease in a patient in need thereof comprising administering a therapeutically effective amount of crystalline 5-4-cyclopropyl-1 H-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.

6. The method of claim 5 , further comprising administering another therapeutic agent.

7. The method of claim 6 , wherein the additional therapeutic agent is filgotinib.

8. The method of claim 6 , wherein the additional therapeutic agent is a compound of formula:

or a salt thereof.

Assignees

• Gilead Sciences Inc

Inventors

• Andres Mark
• Burke Chan Brenda J
• Carra Ernest A
• Chiu Anna
• Lapina Olga Viktorovna
• Lathrop Stephen P
• Notte Gregory
• Smolenskaya Valeriya N
• Yu Lok Him

Classifications

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title

• C07D401/14 Primary

  containing three or more hetero rings · CPC title

• A61P19/02

  for joint disorders, e.g. arthritis, arthrosis · CPC title

• A61K31/422

  not condensed and containing further heterocyclic rings · CPC title