IP Library › Granted Patent US 9,688,674
Granted Patent B2
US 9,688,674 · App. 14/547,247 · Granted Jun 27, 2017

Selective EP4 receptor antagonistic substance for treatment of cancer

Inventors: Yukinori Take (Aichi, JP); Shinichi Koizumi (Aichi, JP); Takako Okumura (Aichi, JP); Kazuhiko Nonomura (Aichi, JP)
Assignee: AskAt Inc.
C07D471/04A61K31/192A61K31/437A61K31/44A61K31/4412A61K45/06C07C235/60C07D213/82
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Quick Facts
Patent No.
US 9,688,674
App. No.
14/547,247
Granted
Jun 27, 2017
Kind
B2
Abstract

This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.

Claims (14)

1. A method for the treatment of colon cancer or breast cancer in which COX-2/PGE2 is expressed, which comprises administering an effective amount of a compound selected from the group consisting of:

3-[2-(4-{2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl}phenyl)ethyl]-1-[(4-methylbenzene)sulfonyl]urea;

4-((1S)-1-{[5-chloro-2-(4-fluorophenoxy)benzoyl]amino}ethyl)benzoic acid; and

4-[(1S)-1-({[5-chloro-2-(3-fluorophenoxy)pyridin-3-yl]carbonyl}amino)ethyl]-benzoic acid, or a pharmaceutically acceptable salt thereof to a human or an animal.

2. A method for reducing colon cancer tissues or breast cancer tissues in which COX-2/PGE2 is expressed, which comprises contacting the cancer tissues with a compound selected from the group consisting of:

3-[2-(4-{2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl}phenyl)ethyl]-1-[(4-methylbenzene)sulfonyl]urea;

4-((1S)-1-{5-chloro-2-(4-fluorophenoxy)benzoyl]amino}ethyl)benzoic acid; and

4-[(1S)-1-({[5-chloro-2-(3-fluorophenoxy)pyridin-3-yl]carbonyl}amino)ethyl]-benzoic acid, or a pharmaceutically acceptable salt thereof.

3. The method according to claim 1 , further comprising combining the compound of 3-[2-(4-{2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl}phenyl)ethyl]-1-(4-methylbenzene)sulfonyl]urea,

4-((1 S)-1-{[5-chloro-2-(4-fluorophenoxy)benzoyl]amino}ethyl)benzoic acid, or

4-[(1 S)-1-({[5-chloro-2-(3-fluorophenoxy)pyridin-3-yl]carbonyl}amino)ethyl]-benzoic acid, or the pharmaceutically acceptable salt thereof, with at least one additional active agent.

4. The method according to claim 3 , wherein the additional active agent is at least one selected from the group consisting of a steroidal or nonsteroidal antiandrogen agent, an antiestrogen agent, a chemotherapeutic agent, a GnRH antagonistic peptide, an alpha-reductase inhibitor, an alpha-receptor inhibitor, an aromatase inhibitor, a 17beta-hydroxysteroid dehydrogenase inhibitor, an adrenal androgen production inhibitor, a kinase inhibitor, a drug for hormone therapy, and a drug inhibiting cell growth factor or its receptor.

5. The method according to claim 1 , wherein the cancer further expresses an EP4 receptor.

6. The method according to claim 2 , wherein the cancer tissues further express an EP4 receptor.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 4, 2017
From: RAQUALIA PHARMA INC.
To: ASKAT INC.
Reel/Frame 041845/0751 →
Priority Claims (2)
JP 2009-104568 · Apr 22, 2009 · national
JP 2010-015445 · Jan 27, 2010 · national
Continuity (2)
Continuation 13265216
Related Publication 20150111920A1 · Apr 23, 2015