IP Library Granted Patent US 9,617,232
Granted Patent B2
US 9,617,232 · App. 14/784,187 · Granted Apr 11, 2017

Dicarboxylic acid compound

Inventors: Yoshikazu Uto (Tokyo, JP); Mikio Kato (Tokyo, JP); Hidenori Takahashi (Tokyo, JP); Yasuyuki Ogawa (Tokyo, JP); Osamu Iwamoto (Tokyo, JP); Hiroko Kono (Tokyo, JP); Kazumasa Aoki (Tokyo, JP)
Assignee: DAIICHI SANKYO COMPANY, LIMITED
C07D295/155C07C311/20C07D213/75C07D213/82C07D295/14C07C2101/02C07C2101/14
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Quick Facts
Patent No.
US 9,617,232
App. No.
14/784,187
Granted
Apr 11, 2017
Kind
B2
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].

Claims (42)

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.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 14, 2015
From: UTO, YOSHIKAZU; KATO, MIKIO; TAKAHASHI, HIDENORI; OGAWA, YASUYUKI; IWAMOTO, OSAMU; KONO, HIROKO; AOKI, KAZUMASA
To: DAIICHI SANKYO COMPANY, LIMITED
Reel/Frame 036787/0035 →
Priority Claims (1)
JP 2013-091090 · Apr 24, 2013 · national
Continuity (1)
Related Publication 20160046568A1 · Feb 18, 2016