IP Library Patent Application 12102554
Patent Application
App. No. 12/102,554

ANTAGONISTS OF PROSTAGLANDIN RECEPTORS EP2 AND/OR EP4 FOR THE TREATMENT OF DYSMENORRHEA AND MENORRHAGIA

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Patent No.
US None
App. No.
12/102,554
Abstract

A method of treating menorrhagia and/or dysmenorrhoea in a patient the method comprising administering to the patient an antagonist of a prostaglandin EP2 and/or EP4 receptor. Preferably the patient is a human female.

Claims (11)

1 . A method of therapeutically treating menorrhagia in a patient the method comprising administering to the patient an antagonist of a prostaglandin EP2 and/or EP4 receptor.

2 . A method according to claim 1 comprising administering an antagonist of a prostaglandin EP2 receptor.

3 . A method according to claim 1 comprising administering an antagonist of a prostaglandin EP4 receptor.

4 . A method according to claim 1 wherein the patient is premenopausal or perimenopausal.

5 . A method according to claim 1 wherein the patient is administered any one or more of AH6809 (whose chemical name is 6-isopropoxy-9-oxoxanthene-2-carboxylic acid), an omega-substituted phenyl-prostaglandin E derivative, AH23848B (whose chemical name is [1α(Z),2β5α]-(+/−)-7-[5-[[(1,1′-biphenyl)-4-yl]methoxy]-2-(4-morpholinyl)-3-oxo-cyclopentyl]-4-heptenoic acid), IFTSYLECL (SEQ ID NO: 1), IFASYECL (SEQ ID NO: 2), IFTSAECL (SEQ ID NO: 3), IFTSYEAL (SEQ ID NO: 4), ILASYECL (SEQ ID NO: 5), IFTSTDCL (SEQ ID NO: 6), XTSYEAL (where X is 4-biphenylalanine) (SEQ ID NO: 7), XTSYEAL (where X is_homophenylalanine) (SEQ ID NO: 8), a 5-thia-omega-substituted phenyl-prostaglandin E derivative, 5-butyl-2,4-dihydro-4-[[2′-[N-(3-chloro-2-thiophenecarbonyl)sulfamoyl]biphenyl-4-yl]methyl]-2-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-one potassium salt, 5-butyl-2,4-dihydro-4-[[2′-[N-(2-methyl-3-furoyl)sulfamoyl]biphenyl-4-yl]methyl]-2-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-one, 5-butyl-2,4-dihydro-4-[[2′-[N-(3-methyl-2-thiophenecarbonyl)sulfamoyl]biphenyl-4-yl]methyl]-2-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-one, 5-butyl-2,4-dihydro-4-[[2′-[N-(2-thiophenecarbonyl)sulfamoyl]biphenyl-4-yl]methyl]-2-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-one, and 5-butyl-2,4-dihydro-4-[[2′-[N-[2-(methypyrrole)carbonyl]sulfamoyl]biphenyl-4-yl]methyl]-2-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-one.

6 . A method according to claim 2 wherein the EP2 receptor antagonist is AH6809.

7 . A method according to claim 3 wherein the EP4 receptor antagonist is any one or more of AH23848B (whose chemical name is [1α(Z),2β5α]-(+/−)-7-[5-[[(1,1′-biphenyl)-4-yl]methoxy]-2-(4-morpholinyl)-3-oxo-cyclopentyl]-4-heptenoic acid), IFTSYLECL (SEQ ID NO: 1), IFASYECL (SEQ ID NO: 2), IFTSAECL (SEQ ID NO: 3), IFTSYEAL (SEQ ID NO: 4), ILASYECL (SEQ ID NO: 5), IFTSTDCL (SEQ ID NO: 6), XTSYEAL (where X is 4-biphenylalanine) (SEQ ID NO: 7), XTSYEAL (where X is homophenylalanine) (SEQ ID NO, 8), a 5-thia-omega-substituted phenyl-prostaglandin E derivative, 5-butyl-2,4-dihydro-4-[[2′-[N-(3-chloro-2-thiophenecarbonyl)sulfamoyl]biphenyl-4-yl]methyl]-2-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-one potassium salt, 5-butyl-2,4-dihydro-4-[[2′-[N-(2-methyl-3-furoyl)sulfamoyl]biphenyl-4-yl]methyl]-2-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-one, 5-butyl-2,4-dihydro-4-[[2′-[N-(3-methyl-2-thiophenecarbonyl)sulfamoyl]biphenyl-4-yl]methyl]-2-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-one, 5-butyl-2,4-dihydro-4-[[2′-[N-(2-thiophenecarbonyl)sulfamoyl]biphenyl-4-yl]methyl]-2-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-one, and 5-butyl-2,4-dihydro-4-[[2′-[[N-[2-(methypyrrole)carbonyl]sulfamoyl]biphenyl-4-yl]methyl]-2-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-one.

8 . A vaginal ring or a tampon or an intrauterine device comprising an EP2 and/or an EP4 receptor antagonist.

9 . A combination of any one or more of an EP2 and/or EP4 receptor antagonist and a further agent used to treat menorrhagia and/or dysmenorrhoea.

10 . A combination according to claim 9 wherein the further agent is tranexamic acid or mefenamic acid.

11 . A pharmaceutical composition comprising a combination according to claim 9 and a pharmaceutically acceptable carrier.

Assignments (1)
CHANGE OF ADDRESS Recorded Mar 21, 2011
From: MEDICAL RESEARCH COUNCIL
To: MEDICAL RESEARCH COUNCIL
Reel/Frame 025990/0240 →