A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/44 (2006.01) A61K 31/395 (2006.01) A61K 31/455 (2006.01) A61K 31/5375 (2006.01) A61P 13/08 (2006.01)
Patent
CA 2444395
The invention relates to the use of an NK-1 receptor antagonist for the treatment or prevention of benign prostatic hyperplasia (BPH). The preferred NK-1 receptor antagonists are compounds of the general formula (I) wherein the meanings of R, R1, R2, R2', R3, R4 are explained in the specification and the pharmaceutically acceptable acid addition salts and the prodrugs thereof. Preferred compounds are 2-(3,5-bis-trifluoromethyl-phenyl)-N-methyl-N-(6- morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide,3-(3,5-bis- trifluoromethyl-phenyl)-N-methyl-N-[6-(4-methyl-piperazin-1-yl)-4-o-tolyl- pyridin-3-yl]-isobutyramide,2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo- 1.lambda.6-thiomorpholin-4-yl)-4-o-tolyl-pyridin-3-yl]-N-methyl-isobutyramide and 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1.lambda.6- thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl- isobutyramide. The invention also relates to pharmaceutical composition comprising one or more such NK-1 receptor antagonists and a pharmaceutically acceptable excipient for the treatment and/or prevention of benign prostatic hyperplasia.
La présente invention concerne l'utilisation d'un antagoniste du récepteur de NK-1 pour le traitement ou la prévention de l'hyperplasie bénigne de la prostate. Les antagonistes préférés de récepteur de NK-1 sont des composés de formule générale (I), dans laquelle R, R?1¿, R?2¿, R?2'¿, R?3¿, R?4¿ sont tels que définis dans la description et les sels d'addition à des acides pharmaceutiquement acceptables et des prodrogues de ceux-ci. Les composé préférés sont 2-(3,5-bis-trifluorométhyl-phényl)-N-méthyl-N-6(-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide, 2-(3,5-bis-trifluorométhyl-phényl)-N-méthyl-N-[6-(4-méthyl pipérazin-1-yl)-4-o-tolyl-pyridin-3-yl]-isobutyramide, 2-(3,5-bis-trifluorométhyl-phényl)-N-[6-1,1-dioxo-1.lambda.?6¿ -thiomorphin-4-yl)-4-o-tolyl-pyridin-3-yl)-N-méthyl-isobutyramide et 2-(3,5-bis-trifluorométhyl-phényl)-N-[6--1,1-dioxo-1.lambda.?6¿-thiomorpholin-4-yl)-4-(4-fluoro-2-méthyl-phényl)-pyridin-3-yl]-N-méthyl-isobutyramide. L'invention concerne également une composition pharmaceutique comprenant un ou des tels antagonistes du récepteur de NK-1 et un excipient pharmaceutiquement acceptable pour le traitement et/ou la prévention de l'hyperplasie bénigne de la prostate.
Buser Susanne
Ford Anthony P. D. W.
Hoffmann Torsten
Lenz Barbara
Sleight Andrew John
Borden Ladner Gervais Llp
F. Hoffmann-La Roche Ag
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