Heterocyclic amides as inhibitors of factor xa

Details Heterocyclic amides as inhibitors of factor xa Heterocyclic amides as inhibitors of factor xa

C - Chemistry, Metallurgy

07

D

C07D 211/62 (2006.01) A61K 31/445 (2006.01) C07D 401/06 (2006.01) C07D 405/04 (2006.01) C07D 409/04 (2006.01)

Patent

CA 2356214

This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt thereof) wherein: Q1 is phenyl or 2-naphthalenyl either of which may bear one or more halo, trifluoromethyl, methoxy or methyl substituents; L1 is a direct bond, methylene, ethylene or ethen-1, 2-diyl; and Q2 is Q2A, Q2B, or Q2C in which Q2A (showing the CO to which it is attached) is of formula (a) in which each of m and n independently is 0 or 1; Q2B is 1- piperazinyl which bears at the 4-position the group R; Q2C is 3,4- didehydropiperidin-4-yl which bears at the 1-position the group R; pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

La présente invention concerne un composé (ou un sel acceptable du point de vue pharmaceutique dudit composé) représenté par la formule (I) dans laquelle Q?1¿ est phényle ou 2-naphthalényle, l'un ou l'autre pouvant comporter un ou plusieurs substituants halogéno, trifluorométhyle, méthoxy ou méthyle; L?1¿ est une liaison directe, méthylène, éthylène ou éthèn-1,2-diyle; et Q?2¿ est Q?2A¿, Q?2B¿, ou Q?2C¿, Q?2A¿ (représenté avec le CO auquel il est lié) étant de formule (a) dans laquelle m et n sont indépendamment égaux à 0 ou 1; Q?2B¿ étant 1-pipérazinyle qui porte le groupe R en position 4; et Q?2C¿ étant 3,4-didéshydropipéridine-4-yle qui porte le groupe R en position 1. L'invention concerne également des compositions pharmaceutiques dudit composé et son utilisation comme inhibiteur du facteur Xa, ainsi que son procédé de préparation et les intermédiaires utilisés à cet effet.

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