Pyrrolidine derivatives as oxytocin antagonists

Details Pyrrolidine derivatives as oxytocin antagonists Pyrrolidine derivatives as oxytocin antagonists

C - Chemistry, Metallurgy

07

D

C07D 207/22 (2006.01) A61K 31/40 (2006.01) A61K 31/4184 (2006.01) A61K 31/4245 (2006.01) A61K 31/5377 (2006.01) A61P 15/06 (2006.01) C07D 403/06 (2006.01) C07D 413/06 (2006.01)

Patent

CA 2515546

The present invention relates to novel pyrrolidine derivatives of Formula (I), its geometrical isomers, its optically active forms as enantiomers, diastercomers, 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; R2 is selected from the group comprising or 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 cycloallcyl, C1-C6-alkyI heterocycloalkyl, C1~C6 alkyl carboxy, acyl, C1-C6-alkyl acyl, C1-C6-alkyl acyloxy, C1-C6-alkyl alkoxy, alkoxycarbonyl, C1-C6-alkyI alkoxycarbonyl, aminocarbonyl, C1-C6-alkyl aminocarbonyl, C1-C6-alkyl acylarnino, 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, C1-C6-alkyl sulfonylamino.

La présente invention a trait à de nouveaux dérivés de pyrrolidine de formule (I), dans laquelle : R?1 ¿est choisi parmi le groupe comprenant ou constitué de H et alkyle en C¿1?-C¿6 ?; R?2¿ choisi parmi le groupe comprenant ou constitué de l'hydrogène, alkyle en C¿1?-C¿6?, alkyle aryle C¿1?-C¿6?, hétéroaryle, alkyle hétéroaryle en C¿1 ?-C¿6,?, alcényle en C¿2?-C¿6?, alcényle aryle en C¿2?-C¿6?, alcényle hétéroaryle en C¿2?-C¿6?, alcynyle en C¿2?-C¿6?, alcynyle aryle en C¿2?-C¿6?, alcynyle hétéroaryle en C¿2?-C¿6?, cycloalkyle en C¿3?-C¿8?, heterocycloalkyle, alkyle cycloalkyle en C¿1?-C¿6?, alkyIe hétérocycloalkyle en C¿1?C¿6?, alkyle carboxy en C¿1?-C¿6?, acyle, alkyle acyle en C¿1?-C¿6?, alkyle acyloxy en C¿1?-C¿6?, alkyle alcoxy en C¿1?-C¿6?, alcoxycarbonyle, alkyIe alcoxycarbonyle en C¿1?-C¿6?, aminocarbonyle, alkyle aminocarbonyle en C¿1?-C¿6?, alkyle acylamino en C¿1-?C¿6?, alkyle ureido en C¿1?-C¿6?, amino, alkyle amino en C¿1?-C¿6?, sulfonyloxy, alkyle sulfonyloxy en C¿1?C¿6?, sulfonyle, alkyle sulfonyle en C¿1?-C¿6?, sulfinyle, alkyle sulfinyle en C¿1?C¿6?, alkyle sulfanyle en C¿1?-C¿6?, alkyle sulfonylamino en C¿1?-C¿6?; leurs isomères géométriques, leurs formes optiquement actives sous forme d'énantiomères, de diastéréomères, des mélanges de ceux-ci et leurs formes racémiques, ainsi que des sels de ceux-ci.

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