Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof
AssigneeMerck Serono SA
InventorsPatrick Naxos PAGE, Matthias SCHWARZ, Catherine JORAND-LEBRUN, Anna QUATTROPANI, Vincent POMEL
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Abstract
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 polymorph s thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as pre-term labor at the early gestational stage by the administration of these substances to a patient in need of treatment.
Claims26
A compound represented by formula (III).
A method of synthesizing a compound represented by formula (III),
- said method comprising reacting a precursor represented by formula (IV)
- with a precursor represented by formula (V)
- to form an amino ester, wherein X is a protecting group, and wherein said method further comprises reacting said amino ester with a reagent capable of deprotecting said amino ester.
A method of making a compound represented by formula (III) in a crystalline state,
- said method comprising mixing a compound represented by formula (I)
- with aqueous hydrochloric acid.
A method of treating preterm labor in a human subject, said method comprising administering to said human subject a therapeutically effective amount of a compound of formula (III).
Dependencies are inferred from the claim text.