Crystalline form of (1R,2R)-2-[4-(3-methyl-1H-pyrazol-5-yl)benzoyl]-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-A]pyrazin-3-yl)cyclohexanecarboxamide

Patent metadata

Field	Value
Publication number	US-10689387-B2
Application number	US-201716345016-A
Country	US
Kind code	B2
Filing date	Oct 27, 2017
Priority date	Oct 28, 2016
Publication date	Jun 23, 2020
Grant date	Jun 23, 2020

Abstract

A crystalline form of (1R,2R)-2-[4-(3-Methyl-1H-pyrazol-5-yl)benzoyl]-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-3-yl)cyclohexanecarboxamide, pharmaceutical compositions containing it and its use in the prevention or treatment of cardiovascular diseases.

First claim

The invention claimed is:

1. A crystalline form of (1R,2R)-2-[4-(3-methyl-1H-pyrazol-5-yl)benzoyl]-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-3-yl)cyclohexanecarboxamide:

2. A crystalline form according to claim 1 , characterised in that it has that has an X-ray powder diffraction pattern with at least one specific peak at 2θ about =9.7, 10.6, 15.8, 16.7, 17.3, 18.7, 19.5, 21.3, 23.3 and/or 24.8° when measured using CuKα radiation.

3. A crystalline form according to claim 1 , characterised in that it has an X-ray powder diffraction pattern with at least one specific peak at 2θ about =9.7, 15.8, 17.3, 19.5 and/or 24.8° when measured using CuKα radiation.

4. A crystalline form according to claim 1 , characterised in that it has an X-ray powder diffraction pattern with specific peaks at 2θ about =9.7, 15.8, 17.3, 19.5 and 24.8° when measured using CuKα radiation.

5. A crystalline form according to claim 1 , characterised in that it has an X-ray powder diffraction pattern with specific peaks at 2θ about =9.7, 10.6, 15.8, 16.7, 17.3, 18.7, 19.5, 21.3, 23.3 and 24.8° when measured using CuKα radiation.

6. A crystalline form according to claim 1 , characterised in that it has an X-ray powder diffraction pattern substantially as shown in FIG. 1 , when measured using CuKα radiation.

7. A pharmaceutical composition comprising a crystalline form as claimed in claim 1 and a pharmaceutically acceptable adjuvant, diluent or carrier.

8. A method of treating acute coronary syndrome comprising administering a crystalline form according to claim 1 to a patient in need thereof.

Assignees

• Astrazeneca Ab

Inventors

• Pettersen Anna Matilda Angelica

Classifications

• C07D487/04 Primary

  Ortho-condensed systems · CPC title

• C07D403/14

  containing three or more hetero rings · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61K31/4985 Primary

  Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems · CPC title

• A61K31/4155

  non condensed and containing further heterocyclic rings · CPC title