Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof

Patent metadata

Field	Value
Publication number	US-2022040159-A1
Application number	US-202117347700-A
Country	US
Kind code	A1
Filing date	Jun 15, 2021
Priority date	Nov 15, 2013
Publication date	Feb 10, 2022
Grant date	—

Abstract

Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino} acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.

First claim

1 .- 32 . (canceled)

33 . A crystalline Compound (I):

Which has an X-ray powder diffraction pattern comprising peaks at 8.6, 15.3, 22.7, and 28.1±0.2° 2θ.

34 . The crystalline Compound (I) of claim 33 , which has an X-ray powder diffraction pattern as shown in FIG. 11 .

35 . The crystalline Compound (I) of claim 33 , which has a DSC endotherm at about 176.2° C.

36 . The crystalline Compound (I) of claim 33 , wherein the crystalline Compound (I) comprises less than 10% by weight of any other crystalline Compound (I).

37 . The crystalline Compound (I) of claim 36 , wherein the crystalline Compound (I) comprises less than 5% by weight of any other crystalline Compound (I).

38 . The crystalline Compound (I) of claim 33 , wherein the crystalline Compound (I) comprises less than 10% by weight of amorphous Compound (I).

39 . The crystalline Compound (I) of claim 38 , wherein the crystalline Compound (I) comprises less than 5% by weight of amorphous Compound (I).

40 . The crystalline Compound (I) of claim 33 , wherein the crystalline Compound (I) comprises less than 100 ppm of a compound of Formula (II):

as determined by GC/MS.

41 . The crystalline Compound (I) of claim 40 , wherein the crystalline Compound (I) comprises less than 50 ppm of a compound of Formula (II) as determined by GC/MS.

42 . The crystalline Compound (I) of claim 33 , wherein the crystalline Compound (I) is at least 99.5% pure as measured by HPLC.

43 . A pharmaceutical composition comprising a crystalline Compound (I) of claim 33 .

44 . A method of treating anemia, comprising administering a pharmaceutical composition comprising an effective amount of a crystalline Compound (I) of claim 33 .

45 . A crystalline Compound (I):

which has an X-ray powder diffraction pattern comprising peaks at 7.2, 17.4, 22.3, 22.4, 22.4, 28.9, 33.7, and 33.8 ±0.2°2θ.

46 . The crystalline Compound (I) of claim 45 , which has an X-ray powder diffraction pattern as shown in FIG. 12 .

47 . The crystalline Compound (I) of claim 45 , wherein the crystalline Compound (I) comprises less than 10% by weight of any other crystalline Compound (I).

48 . The crystalline Compound (I) of claim 47 , wherein the crystalline Compound (I) comprises less than 5% by weight of any other crystalline Compound (I).

49 . The crystalline Compound (I) of claim 45 , wherein the crystalline Compound (I) comprises less than 10% by weight of amorphous Compound (I).

50 . The crystalline Compound (I) of claim 49 , wherein the crystalline Compound (I) comprises less than 5% by weight of amorphous Compound (I).

51 . The crystalline Compound (I) of claim 45 , wherein the crystalline Compound (I) comprises less than 100 ppm of a compound of Formula (II):

as determined by GC/MS.

52 . The crystalline Compound (I) of claim 51 , wherein the crystalline Compound (I) comprises less than 50 ppm of a compound of Formula (II) as determined by GC/MS.

53 . The crystalline Compound (I) of claim 45 , wherein the crystalline Compound (I) is at least 99.5% pure as measured by HPLC.

54 . A pharmaceutical composition comprising a crystalline Compound (I) of claim 45 .

55 . A method of treating anemia, comprising administering a pharmaceutical composition comprising an effective amount of a crystalline Compound (I) of claim 45 .

Assignees

• Akebia Therapeutics Inc

Inventors

• Copp James Densmore
• Newman Ann W
• Luong Anne

Classifications

• A61K31/4418

  having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine · CPC title

• A61P7/06

  Antianaemics · CPC title

• C07D213/81 Primary

  Amides; Imides · CPC title

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title

• A61P43/00

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