Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof
The invention provides α-amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1′-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorphs thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as preterm labor at the early gestational stage by the administration of these substances to a patient in need of treatment.
1. A method of treating preterm labor in a human patient in need thereof, the method comprising providing to the patient a therapeutically effective amount of a compound represented by formula (II)
and wherein the patient is administered nifedipine or atosiban.
2. A method of delaying labor in a human patient in need thereof, the method comprising providing to the patient a therapeutically effective amount of a compound represented by formula (II)
and wherein the patient is administered nifedipine or atosiban.
3. The method of claim 1 , wherein the patient is administered atosiban.
4. The method of claim 1 , wherein the patient is administered nifedipine.
5. The method of claim 1 , wherein the patient is further administered a betamimetic, a magnesium salt, a nitric oxide donor, progesterone or a variant thereof, or a corticosteroid.
6. The method of claim 5 , wherein the patient is administered a betamimetic selected from the group consisting of terbutaline, ritodrine, hexoprenaline, albuterol, fenoterol, nylidrin, and orciprenaline.
7. The method of claim 5 , wherein the patient is administered magnesium sulfate.
8. The method of claim 5 , wherein the patient is administered nitroglycerine.
9. The method of claim 5 , wherein the patient is administered progesterone or 17-α-hydroxyprogesterone caproate.
10. The method of claim 5 , wherein the patient is administered a corticosteroid selected from the group consisting of betamethasone, dexamethasone, or hydrocortisone.
11. The method of claim 1 , wherein the patient is characterized by a gestational age of from about 24 weeks to about 34 weeks.
12. The method of claim 2 , wherein the patient is administered atosiban.
13. The method of claim 2 , wherein the patient is administered nifedipine.
14. The method of claim 2 , wherein the patient is further administered a betamimetic, a magnesium salt, a nitric oxide donor, progesterone or a variant thereof, or a corticosteroid.
15. The method of claim 14 , wherein the patient is administered a betamimetic selected from the group consisting of terbutaline, ritodrine, hexoprenaline, albuterol, fenoterol, nylidrin, and orciprenaline.
16. The method of claim 14 , wherein the patient is administered magnesium sulfate.
17. The method of claim 14 , wherein the patient is administered nitroglycerine.
18. The method of claim 14 , wherein the patient is administered progesterone or 17-α-hydroxyprogesterone caproate.
19. The method of claim 14 , wherein the patient is administered a corticosteroid selected from the group consisting of betamethasone, dexamethasone, or hydrocortisone.
20. The method of claim 2 , wherein the patient is characterized by a gestational age of from about 24 weeks to about 34 weeks.