Crystalline forms of a prolyl hydroxylase inhibitor

Patent metadata

Field	Value
Publication number	US-9115085-B2
Application number	US-201313942443-A
Country	US
Kind code	B2
Filing date	Jul 15, 2013
Priority date	Jul 16, 2012
Publication date	Aug 25, 2015
Grant date	Aug 25, 2015

Abstract

The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.

First claim

What is claimed is:

1. A pharmaceutical composition comprising crystalline [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid (Compound A Form A) characterized by an X-ray powder diffractogram comprising the following peaks: 8.5, 16.2, and 27.4° 2θ±0.2° 2θ, and a pharmaceutically acceptable excipient, wherein at least about 85% of Compound A is in Form A.

2. The pharmaceutical composition of claim 1 , wherein at least about 90% of Compound A is in Form A.

3. The pharmaceutical composition of claim 1 , wherein at least about 95% of Compound A is in Form A.

4. The pharmaceutical composition of claim 1 , wherein at least about 99% of Compound A is in Form A.

5. The pharmaceutical composition of claim 1 , wherein at least about 99.5% of Compound A is in Form A.

6. The pharmaceutical composition of claim 1 , wherein at least about 99.9% of Compound A is in Form A.

7. The pharmaceutical composition of claim 1 , wherein at least about 99.99% of Compound A is in Form A.

8. The pharmaceutical composition of claim 1 , wherein the diffractogram further comprises peaks at 12.8, 21.6, and 22.9° 2θ±0.2° 2θ.

9. The pharmaceutical composition of claim 1 , wherein the diffractogram is substantially as shown in FIG. 1 .

10. The pharmaceutical composition of claim 1 , wherein the Compound A Form A is characterized by a differential scanning calorimetry (DSC) curve that comprises an endotherm at about 223° C.

11. The pharmaceutical composition of claim 10 , wherein the DSC curve is substantially as shown in FIG. 2 .

Assignees

• Fibrogen Inc

Inventors

• Witschi Claudia
• Park Jung Min
• Thompson Michael D
• Martinelli Michael John
• Yeowell David A
• Arend Michael P

Classifications

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P7/06

  Antianaemics · CPC title

• A61P9/04

  Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure · 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