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US 7,115,754 B2Granted
Pyrrolidine derivatives as oxytocin antagonists
AssigneeApplied Research Systems ARS Holding N.V.
InventorsCatherine Jorand-Lebrun, Jerome Dorbais, Anna Quattropani, Matthias Schwarz, Delphine Valognes
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Abstract
The present invention relates to novel pyrrolidine derivative of formula (I), its geometrical isomers, its optically active forms as enantiomers, diastereomers, mixtures of these and its racemate forms, as well as salts thereof, wherein R1 is selected from the group comprising or consisting of H and C1–C6-alkyl, for the prevention and/or treatment of preterm labor, premature birth or dysmenorrhea
Claims11
A pyrrolidine derivative of Formula I:
- a geometrical isomer thereof, an optically active form thereof, an enantiomer thereof, a diastereomer thereof, one or more mixtures thereof, a racemate form thereof, or a salt thereof, wherein:
- R1 is selected from the group consisting of H and C1–C6-alkyl;
- R2 is selected from the group consisting of hydrogen, C1–C6-alkyl, C1–C6-alkyl aryl, heteroaryl, C1–C6-alkyl heteroaryl, C2–C6-alkenyl, C2–C6-alkenyl aryl, C2–C6-alkenyl heteroaryl, C2–C6-alkynyl, C2–C6-alkynyl aryl, C2–C6-alkynyl heteroaryl, C3–C8-cycloalkyl, heterocycloalkyl, C1–C6-alkyl cycloalkyl, C1–C6-alkyl heterocycloalkyl, C1–C6-alkyl carboxy, acyl, C1–C6-alkyl acyl, C1–C6-alkyl acyloxy, C1–C6-alkyl alkoxy, alkoxycarbonyl, C1–C6-alkyl alkoxycarbonyl, aminocarbonyl, C1–C6-alkyl aminocarbonyl, C1–C6-alkyl acylamino, C1–C6-alkyl ureido, amino, C1–C6-alkyl amino, sulfonyloxy, C1–C6-alkyl sulfonyloxy, sulfonyl, C1–C6-alkyl sulfonyl, sulfinyl, C1–C6-alkyl sulfinyl, C1–C6-alkyl sulfanyl, and C1–C6-alkyl sulfonylamino;
- R3 is selected from the group consisting of aryl and heteroaryl;
- X is selected from the group consisting of O and NR4;
- R4 is selected from the group consisting of H, C1–C6-alkyl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl, aryl and heteroaryl;
- wherein
- R2 and R4 can form together with the N atom to which they are linked to, a 5–8 membered saturated or unsaturated heterocycloalkyl ring;
- and
- n is an integer from 1 to 3.
7 more elements
Dependencies are inferred from the claim text.