Dicarboxylic acid compound

Patent metadata

Field	Value
Publication number	US-9617232-B2
Application number	US-201414784187-A
Country	US
Kind code	B2
Filing date	Apr 23, 2014
Priority date	Apr 24, 2013
Publication date	Apr 11, 2017
Grant date	Apr 11, 2017

Abstract

It is an object of the present invention to provide a medicament for preventing or treating hyperphosphatemia. Solution: A compound represented by a general formula (I) or a pharmacologically acceptable salt thereof. [In the formula, R 1 : a methyl group or the like, R 2 : a hydrogen atom or the like, R 3 : a hydrogen atom or the like, A: a cyclohexyl ring or the like, X: CH or the like, Y: CH or the like, Z: CH or the like, and n: 2 or the like].

First claim

The invention claimed is:

1. A compound of general formula (I) or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof:

wherein each substituent is as defined below:
R 1 : a C1-6 alkyl group, a C1-6 alkoxy C1-6 alkyl group, a C3-6 cycloalkyl group, or a C3-6 cycloalkyl C1-6 alkyl group,
R 2 : a hydrogen atom or a halogen group,
R 3 : a hydrogen atom, a halogen group, a halogeno C1-6 alkyl group, a halogeno C1-6 alkoxy group, a C2-5 saturated cyclic amino group, a C1-6 dialkylamino group, a C3-6 cycloalkyl C1-6 alkoxy group, or a C1-6 alkoxy group,
A: a C3-6 cycloalkyl ring,
X: CH or N,
Y: CH or N,
Z: CH or N, and
n: an integer selected from 1, 2, 3, and 4.

2. The compound or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof, according to claim 1 , wherein the compound of the general formula (I) is a compound of general formula (I′):

3. The compound or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof, according to claim 1 , wherein R 1 represents a methyl group, an ethyl group, a methoxyethyl group, a cyclopropyl group, or a cyclopropylmethyl group.

4. The compound or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof, according claim 1 , wherein R 2 represents a hydrogen atom, a chlorine atom, or a bromine atom.

5. The compound or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof, according claim 1 , wherein R 3 represents a hydrogen atom, a fluorine atom, a chlorine atom, a bromine atom, a trifluoromethyl group, a 2,2,2-trifluoroethoxy group, a pyrrolidin-1-yl group, a piperidin-1-yl group, a diethylamino group, a cyclopropylmethoxy group, or a methoxy group.

6. The compound or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof, according to claim 1 , wherein A represents a cyclohexane ring.

7. The compound or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof, according to claim 1 , wherein X, Y, and Z each represent CH.

8. The compound or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof, according to claim 1 , wherein n is 2.

9. The compound or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof, according to claim 1 , wherein:
R 1 is a methyl group, an ethyl group, a methoxyethyl group, a cyclopropyl group, or a cyclopropylmethyl group,
R 2 is a hydrogen atom, a chlorine atom, or a bromine atom,
R 3 is a hydrogen atom, a fluorine atom, a chlorine atom, a bromine atom, a trifluoromethyl group, a 2,2,2-trifluoroethoxy group, a pyrrolidin-1-yl group, a piperidin-1-yl group, a diethylamino group, a cyclopropylmethoxy group, or a methoxy group,
A is a cyclohexane ring,
X is CH or N,
Y is CH or N,
Z is CH or N, and
n is 2 or 3.

10. The compound according to claim 1 , wherein the compound is selected from the following compound group:

or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof.

11. The compound according to claim 1 , wherein the compound has the following formula:

or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof.

12. The compound according to claim 1 , wherein the compound has the following formula:

or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof.

13. The compound according to claim 1 , wherein the compound has the following formula:

or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof.

14. The compound according to claim 1 , wherein the compound has the following formula:

or a pharmacologically acceptable salt thereof, or a hydrate of the compound or pharmacologically acceptable salt thereof.

15. The pharmacologically acceptable salt of the compound according to claim 10 , which is a dipotassium salt or a hydrate thereof.

16. The pharmacologically acceptable salt of the compound according to claim 10 , which is a disodium salt or a hydrate thereof.

17. The pharmacologically acceptable salt according to claim 15 , which is a hydrate thereof.

18. A method for the prevention or treatment of hyperphosphatemia comprising administering to a patient a compound or pharmacologically acceptable salt thereof, or the hydrate of the compound or pharmacologically acceptable salt thereof, according to claim 1 .

19. A pharmaceutical composition comprising the compound or pharmacologically acceptable salt thereof, or the hydrate of the compound or pharmacologically acceptable salt thereof, according to claim 1 .

20. The pharmaceutical composition according to claim 19 , wherein administration to a patient of an effective amount of the pharmaceutical composition inhibits the uptake of phosphorus in the patient.

Assignees

• Daiichi Sankyo Co Ltd

Inventors

• Uto Yoshikazu
• Kato Mikio
• Takahashi Hidenori
• Ogawa Yasuyuki
• Iwamoto Osamu
• Kono Hiroko
• Aoki Kazumasa

Classifications

• A61P7/00

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

• A61P43/00

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

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P3/14

  for calcium homeostasis (vitamin D A61P3/02; parathyroid hormones A61P5/18; calcitonin A61P5/22; osteoporosis A61P19/10; bone metastasis A61P35/04) · CPC title

• A61P3/00

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