IP Library Granted Patent US 8,901,155
Granted Patent B2
US 8,901,155 · App. 13/680,465 · Granted Dec 2, 2014

Method for treating a TRPV1-mediated disease

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Quick Facts
Patent No.
US 8,901,155
App. No.
13/680,465
Granted
Dec 2, 2014
Kind
B2
Abstract

A method for treating a TRPV1-mediated disease by administering to a patient a therapeutically effective amount of a compound or a salt thereof having the following formula [I]: wherein A represents a lower alkylene group or a lower alkenylene group; R 1 represents a hydrogen atom, an unsubstituted or substituted alkyl group or an unsubstituted or substituted alkenyl group; and R 2 and R 3 are the same or different and represent a hydrogen atom, an unsubstituted lower alkyl group or a lower alkyl group substituted by a monocyclic cycloalkyl group, a polycyclic cycloalkyl group or an aryl group.

Claims (31)

1. A method for treating a TRPV1-mediated disease, comprising administering to a patient a therapeutically effective amount of a compound, or a salt thereof, represented by the following formula [I]:

wherein A represents a lower alkylene group or a lower alkenylene group; R 1 represents a hydrogen atom, an unsubstituted or substituted alkyl group or an unsubstituted or substituted alkenyl group; and R 2 and R 3 are the same or different and represent a hydrogen atom, an unsubstituted lower alkyl group or a lower alkyl group substituted by a monocyclic cycloalkyl group, a polycyclic cycloalkyl group or an aryl group, wherein the TRPV1-mediated disease is selected from the group consisting of pain, an overactive bladder and a gastrointestinal dysfunction.

2. The method according to claim 1 , wherein

A is a lower alkylene group or a lower alkenylene group;

R 1 is an unsubstituted or substituted lower alkyl group; and

R 2 is a hydrogen atom, and

R 3 is a lower alkyl group substituted by a monocyclic cycloalkyl group, a polycyclic cycloalkyl group or an aryl group; or

R 3 is a hydrogen atom, and R 2 is a lower alkyl group substituted by a monocyclic cycloalkyl group, a polycyclic cycloalkyl group or an aryl group.

3. The method according to claim 1 , wherein

A represents a lower alkylene group;

R 1 represents an unsubstituted or substituted alkyl group;

R 2 represents an unsubstituted lower alkyl group or a lower alkyl group which is substituted by a monocyclic cycloalkyl group, a polycyclic cycloalkyl group or an aryl group; and

R 3 is a hydrogen atom.

4. The method according to claim 2 , wherein

A is a lower alkylene group;

R 1 is an unsubstituted or substituted lower alkyl group;

R 2 is a lower alkyl group substituted by a monocyclic cycloalkyl group or a polycyclic cycloalkyl group; and

R 3 is a hydrogen atom.

5. The method according to claim 4 , wherein A is a trimethylene group or a methyltrimethylene group; R 1 is a straight lower alkyl group which may have a substituent; R 2 is an adamantylethyl group or an adamantylpropyl group; and R 3 is a hydrogen atom.

6. The method according to claim 1 , wherein A is a lower alkylene group, R 1 is an unsubstituted alkyl group or a substituted alkyl group, R 2 is an unsubstituted lower alkyl group or a lower alkyl group substituted with a substituent selected from the group consisting of a monocyclic cycloalkyl group, a polycyclic cycloalkyl group and an aryl group.

7. The method according to claim 1 , wherein the compound is selected from the group consisting of:

1-[2-(1-adamantyl)ethyl]-1-pentyl-3-[3-(4-pyridyl)propyl]urea,

1-[2-(1-adamantyl)ethyl]-3-[3-(4-pyridyl)propyl]-1-(3,3,3-trifluoropropyl)urea,

1-[3-(1-adamantyl)propyl]-1-propyl-3-[3-(4-pyridyl)propyl]urea,

1-[2-(1-adamantyl)ethyl]-3-[1-methyl-3-(4-pyridyl)propyl]-1-pentylurea,

1-[2-(1-adamantyl)ethyl]-3-[2-methyl-3-(4-pyridyl)propyl]-1-pentylurea and

(+)-1-[2-(1-adamantyl)ethyl]-3-[2-methyl-3-(4-pyridyl)propyl]-1-pentylurea.

8. The method according to claim 1 , wherein the compound is 1-[2-(1-adamantyl)ethyl]-1-pentyl-3-[3-(4-pyridyl)propyl]urea.

9. The method according to claim 1 , wherein the TRPV1-mediated disease is pain.

10. The method according to claim 1 , wherein the TRPV1-mediated disease is an overactive bladder.

11. The method according to claim 1 , wherein the TRPV1-mediated disease is a gastrointestinal dysfunction.

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE INCORRECT PATENT NUMBER 7122598 PREVIOUSLY RECORDED ON REEL 037834 FRAME 0513. ASSIGNOR(S) HEREBY CONFIRMS THE PATENT NUMBER SHOULD BE 7112598. Recorded Apr 12, 2016
From: SANTEN PHARMACEUTICAL CO.,LTD.
To: AYUMI PHARMACEUTICAL CORPORATION
Reel/Frame 038408/0987 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 26, 2016
From: SANTEN PHARMACEUTICAL CO.,LTD.
To: AYUMI PHARMACEUTICAL CORPORATION
Reel/Frame 037834/0513 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 19, 2012
From: OKI, KENJI; TSUJI, FUMIO; SETOGUCHI, CHIKAKO; SEKI, IWAO; MURAI, MASAAKI; SASANO, MINORU
To: SANTEN PHARMACEUTICAL CO., LTD.
Reel/Frame 029320/0561 →