IP Library Granted Patent US 6,956,057
Granted Patent B2
US 6,956,057 · App. 10/672,499 · Granted Oct 18, 2005

EP4 agonists as agents for lowering intraocular pressure

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Quick Facts
Patent No.
US 6,956,057
App. No.
10/672,499
Granted
Oct 18, 2005
Kind
B2
Abstract

The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound which is a EP 4 agonist.

Claims (23)

1. A method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma a therapeutically effective amount of a compound which is an EP 4 agonist, having an ocular activity.

2. The method of claim 1 wherein said compound is represented by the general formula I;

wherein hatched lines represent the α configuration, a triangle represents the β configuration, a wavy line represents either the α configuration or the β configuration end a dotted line represents the presence or absence of a double bond;

A and B are independently selected from the group consisting of O, S and CH 2 , provided that at least one of A or B is S;

D represents a covalent bond or CH 2 , O, S or NH;

X is CO 2 R, CONR 2 , CH 2 OR, P(O)(OR) 2 , CONRSO 2 R, SONR 2 or

Y is O, OH, OCOR 2 , halogen or cyano;

Z is CH 2 or a covalent bond;

R is H or R 2 ;

R 1 is H, R 2 , phenyl, or COR 2 ;

R 2 is C 1 -C 5 lower alkyl or alkenyl;

R 3 is benzothienyl, benzofuranyl, naphthyl, or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C 1 -C 5 alkyl, halogen, CF 3 , CN, NO 2 , NR 2 , CO 2 R and OR and R 4 hydrogen or C 1 -C 5 lower alkyl.

3. The method according to claim 2 wherein said compound is represented by the general formula II;

4. The method according to claim 3 wherein said compound is represented by the general formula III;

5. The method of claim 2 wherein Z represents a covalent bond.

6. The method of claim 2 wherein D represents a covalent bond or is CH 2 .

7. The method of claim 2 wherein X is CO 2 R.

8. The method of claim 7 wherein R is selected from the group consisting of H, methyl, i-propyl, and n-propenyl.

9. The method of claim 2 wherein R is H, or n-propenyl.

10. The method of claim 2 wherein R 1 is H.

11. The method of claim 2 wherein D is CH 2 .

12. The method of claim 11 wherein R 3 is benzo[b]thienyl, 3-chlorobenzo[b]thienyl or naphthyl.

13. The method of claim 1 wherein said compound is GR 50209X.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 27, 2004
From: WOODWARD, DAVID F.; KRAUSS, ACHIM H.; BURK, ROBERT M.; HOLOABASKI, MARK; POSNER, MARI F.
To: ALLEGAN, INC.
Reel/Frame 015371/0057 →