Piperidinyl camphorsulfonyl oxytocin antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 401/12 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) A61K 31/675 (2006.01) C07D 221/20 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01) C07F 9/576 (2006.01)

Patent

CA 2174650

Spirocyclic compounds of formula (I), where m is an integer from zero to one; Y is CH or CH2; and X is C=O, CH2, PO2H, PO2Z, where Z is C1-10 alkyl, SO2, CONH, or SO2NH. Such compounds are useful as oxytocin and vasopressin receptor antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery, timing of parturition, uterine hyperactivity, endometriosis, hypertension, congestive heart failure, hyponatremia and cognitive disorders. Also disclosed are pharmaceutical compositions containing these compounds, methods of their use and methods of their preparation.

L'invention concerne des composés spirocycliques de formule (I) dans laquelle m est un entier de zéro à un; Y représente CH ou CH¿2?; et X représente C=O, CH¿2?, PO¿2?H, PO¿2?Z, Z représentant alkyle C¿1-10?, SO¿2?, COHN ou SO¿2?NH. Ces composés sont utiles en tant qu'antagonistes du récepteur de la vasopressine et de l'oxytocine utile dans le traitement du travail prématuré, de la dysménorrhée ainsi que pour stopper le travail préparatoire à l'accouchement par césarienne, déclencher la parturition, traiter l'hyperactivité utérine, l'endométriose, l'hypertension, l'insuffisance cardiaque congestive, l'hyponatrémie et les troubles cognitifs. L'invention porte également sur des compositions pharmaceutiques contenant ces composés, ainsi que leurs procédés d'utilisation et de préparation.

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