IP Library Granted Patent US 9,073,963
Granted Patent B2
US 9,073,963 · App. 12/423,975 · Granted Jul 7, 2015

Peptides and peptidomimetics useful for inhibiting the activity of prostaglandin F

Inventors: Krishna Peri (Saint-Laurent, CA); Felix Polyak (Montréal, CA); William Lubell (Montreal, CA); Eryk Thouin (Montréal, CA); Sylvain Chemtob (Montreal, CA)
Assignees: Universite De Montreal; Theratechnologies, Inc.
C07K7/06A61K38/00
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Quick Facts
Patent No.
US 9,073,963
App. No.
12/423,975
Granted
Jul 7, 2015
Kind
B2
Abstract

The invention relates to compositions which are useful for inhibiting prostaglandin F 2α receptor. The compositions include, but are not limited to, linear peptides, peptide analogs, and peptidomimetics. Methods of using the compositions of the invention to treat preterm labor and dysmenorrhea are disclosed.

Claims (16)

1. A peptidomimetic compound selected from the group consisting of:

(3S,6S,9S)-2-Oxo-3-phenylacetamido-1-azabicyclo[4.3.0]nonane-9-carboxyl-L-argininyl-(3′S)-3′-amino-4′-phenylbutanoic acid;

(3S,6S,9S)-2-Oxo-3-phenylacetamido-1-azabicyclo[4.3.0]nonane-9-carboxyl-L-citrulinyl-(3′S)-3′-amino-4′-phenylbutanoic acid;

(3S,6S,9S)-2-Oxo-3-phenylacetamido-1-azabicyclo[4.3.0]nonane-9-carboxyl-(3-pyridyl)-L-alaninyl-(3′S)-3′-amino-4′-phenylbutanoic acid;

(3S,6S,9S)-2-Oxo-3-phenylacetamido-1-azabicyclo[4.3.0]nonane-9-carboxyl-(4-pyridyl)-L-alaninyl-(3′S)-3′-amino-4′-phenylbutanoic acid; and

pharmaceutically acceptable salts thereof.

2. A compound in accordance with claim 1 wherein the peptidomimetic comprises (3S,6S,9S)-2-Oxo-3-phenylacetamido-1-azabicyclo[4.3.0]nonane-9-carboxyl-L-argininyl-(3′S)-3′-amino-4′-phenylbutanoic acid.

3. A compound in accordance with claim 1 wherein the peptidomimetic comprises (3S,6S,9S)-2-Oxo-3-phenylacetamido-1-azabicyclo[4.3.0]nonane-9-carboxyl-L-citrulinyl-(3′S)-3′-amino-4′-phenylbutanoic acid.

4. A compound in accordance with claim 1 wherein the peptidomimetic comprises (3S,6S,9S)-2-Oxo-3-phenylacetamido-1-azabicyclo[4.3.0]nonane-9-carboxyl-(3-pyridyl)-L-alaninyl-(3′S)-3′-amino-4′-phenylbutanoic acid.

5. A compound in accordance with claim 1 wherein the peptidomimetic comprises (3S,6S,9S)-2-Oxo-3-phenylacetamido-1-azabicyclo[4.3.0]nonane-9-carboxyl-(4-pyridyl)-L-alaninyl-(3′S)-3′-amino-4′-phenylbutanoic acid.

6. A pharmaceutical composition comprising a therapeutically effective amount of at least one compound of claim 1 in association with a pharmaceutically acceptable carrier.

7. A method of inhibiting Prostaglandin F (FP) receptor function in an individual in need thereof, the method comprising administering to such an individual an inhibitory amount of the pharmaceutical composition of claim 6 .

8. The method of claim 7 wherein said receptor is from a mammal.

9. The method of claim 8 wherein said mammal is a human.

10. A method of treating preterm labor comprising administering to an individual the pharmaceutical composition of claim 6 .

11. A method of treating dysmenorrhea comprising administering to an individual the pharmaceutical composition of claim 6 .

Priority Claims (1)
WO PCT/CA03/000903 · Jun 11, 2003 · international
Continuity (2)
Continuation 10517687 · Dec 10, 2004
Related Publication 20120172318A1 · Jul 5, 2012