Salt of dicarboxylic acid compound

Patent metadata

Field	Value
Publication number	US-10053437-B2
Application number	US-201515511974-A
Country	US
Kind code	B2
Filing date	Sep 18, 2015
Priority date	Sep 26, 2014
Publication date	Aug 21, 2018
Grant date	Aug 21, 2018

Abstract

It is an object of the present invention to provide a medicament for preventing or treating hyperphosphatemia. The solution is crystals, or hydrate thereof, of a salt of a compound represented by formula (I).

First claim

The invention claimed is:

1. Crystals of a salt, or hydrate thereof, of a compound of formula (I):

wherein the crystals are α crystals, β crystals, γ crystals, or δ crystals.

2. The crystals of a salt, or hydrate thereof, of a compound according to claim 1 , wherein the salt is a disodium salt.

3. The crystals of a salt, or hydrate thereof, of a compound according to claim 1 , wherein the hydrate is a trihydrate.

4. Crystals of a disodium salt trihydrate of the compound of formula (I):

wherein the crystals are α crystals.

5. The crystals according to claim 4 , wherein the crystals are α crystals, and wherein, in powder X-ray diffractometry using Cu as a radiation source, 2θ(°) shows peaks at around 5.72, around 10.10, around 10.96, around 11.98, around 13.34, around 15.02, around 17.26, around 20.26, around 21.66, and around 22.36.

6. The crystals or hydrates thereof according to claim 2 , wherein the crystals are β crystals, and wherein, in powder X-ray diffractometry using Cu as a radiation source, 2θ(°) shows peaks at around 5.82, around 9.78, around 11.18, around 12.26, around 12.86, around 15.38, around 16.34, around 18.34, around 19.68, and around 22.54.

7. The crystals or hydrates thereof according to claim 2 , wherein the crystals are γ crystals, and wherein, in powder X-ray diffractometry using Cu as a radiation source, 2θ(°) shows peaks at around 5.80, around 9.86, around 12.12, around 12.86, around 15.04, around 16.30, around 18.28, around 19.90, around 20.52, and around 22.58.

8. The crystals or hydrates thereof according to claim 2 , wherein the crystals are δ crystals, and wherein, in powder X-ray diffractometry using Cu as a radiation source, 2θ(°) shows a single characteristic peak only at around 6.04.

9. A pharmaceutical composition comprising the crystals or hydrates thereof according to claim 1 .

10. The pharmaceutical composition according to claim 9 , wherein the composition inhibits phosphorus uptake.

11. A method of treating hyperphosphatemia in a subject comprising, administering to a subject in need thereof the pharmaceutical composition according to claim 9 .

12. A method of treating hyperphosphatemia in a subject comprising, administering to a subject in need thereof the crystals according to claim 1 .

13. A method for preventing or treating hyperphosphatemia, comprising administering to a subject an effective amount of the crystals or hydrates thereof according to claim 1 .

Assignees

• Daiichi Sankyo Co Ltd

Inventors

• Yokoyama Mizuka
• Ueda Yasusi
• Fukatsu Daisuke
• Aki Yuichi

Classifications

• A61P43/00

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

• A61P7/00

  Drugs for disorders of the blood or the extracellular fluid · CPC title

• A61P3/12

  for electrolyte homeostasis · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title