Tocolytic oxytocin receptor antagonists

Details Tocolytic oxytocin receptor antagonists Tocolytic oxytocin receptor antagonists

C - Chemistry, Metallurgy

07

D

C07D 413/14 (2006.01) A61K 31/47 (2006.01) A61K 31/535 (2006.01) C07D 401/14 (2006.01) C07D 413/04 (2006.01)

Patent

CA 2210138

Compounds of formula (I) wherein X is selected from CH2 or O; provided that when R1 and R3 are both simultaneously hydrogen then (a) R8 is C1-5 alkyl or halogen, and R2 is C1-5 alkoxy, or (b) R4 is (II); and the pharmaceutically acceptable salts thereof. Such compounds are useful in mammals as oxytocin receptor antagonists for the treatment of preterm labor, dysmenorrhea and stopping labor prior to cesarean delivery.

L'invention concerne des composés de la formule (I) dans laquelle X est choisi entre CH¿2? et O, à condition que lorsque R?1¿ et R?3¿ représentent l'un et l'autre simultanément hydrogène, alors (a) R?8¿ représente alkyle C¿1-5? ou halogène, et R?2¿ représente alcoxy C¿1-5?, ou (b) R?4¿ représente (II); ainsi que leurs sels pharmaceutiquement acceptables. Ces composés sont utiles chez les mammifères en tant qu'antagonistes des récepteurs de l'oxytocine, dans le traitement du travail avant terme, de la dysménorrhée et de l'arrêt du travail avant l'accouchement par césarienne.

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