C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 207/12 (2006.01) A61K 31/40 (2006.01) A61K 31/44 (2006.01) A61K 31/695 (2006.01) C07D 213/54 (2006.01) C07D 295/13 (2006.01) C07D 307/79 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) C07D 409/12 (2006.01) C07D 409/14 (2006.01) C07F 7/10 (2006.01)
Patent
CA 2213815
A compound of formula (I) and its pharmaceutically acceptable salt, wherein A is hydrogen, hydroxy or OY, wherein Y is a hydroxy protecting group; Ar is phenyl optionally substituted with one or more substituents selected from halo, hydroxy, C1-C4 alkyl, C1-C4 alkoxy, CF3, C1-C4 alkoxy-C1-C4 alkyloxy, and carboxy-C1-C4 alkyloxy; X is phenyl, naphthyl, biphenyl, indanyl, benzofuranyl, benzothiophenyl, 1-tetralone-6-yl, C1-C4 alkylenedioxy, pyridyl, furyl and thienyl, these groups optionally being substituted with up to three substituents selected from halo, C1-C4 alkyl, C1-C4 alkoxy, hydroxy, NO2, CF3 and SO2CH3; and R is hydrogen, C1-C4 alkyl or a hydroxy protecting group. These compounds and pharmaceutical compositions containing them are useful as analgesic, anti-inflammatory, diuretic, anesthetic or neuroprotective agents, or an agent for stroke or treatment of functional bowel diseases such as abdominal pain, for the treatment of a mammalian subject, especially a human subject. Further, the present invention provides processes for producing the hydroxamic compounds of formula (I) and their intermediate compounds of formula (II).
Composé de la formule (I) et son sel pharmaceutiquement acceptable. Dans cette formule, A est hydrogène, hydroxy ou OY, Y étant un groupe hydroxy inhibant; Ar est phényle, facultativement substitué par un ou plusieurs substituants choisis entre halo, hydroxy, C¿1-4? alkyle, C¿1-4? alcoxy, CF¿3?, C¿1-4? alcoxy-C¿1-4? alkyloxy, et carboxy C¿1-4? alkyloxy; X est phényle, naphtyle, biphényle, indanyle, benzofuranyle, benzothiophényle, 1-tétralone-6-yle, C¿1?-C¿4? alkylène dioxy, pyridyle, furyle et thiényle, ces groupes pouvant être facultativement substitués par jusqu'à trois substituants choisis entre halo, C¿1?-C¿4? alkyle, C¿1?-C¿4? alcoxy, hydroxy, NO¿2?, CF¿3? et SO¿2?CH¿3?; et R est hydrogène, C¿1?-C¿4? alkyle ou un groupe hydroxy protecteur. Ces composés et les compositions pharmaceutiques qui les renferment se révèlent utiles comme agents analgésiques, anti-inflammatoires, diurétiques, anesthésiants ou neuroprotecteurs, ou comme agent de traitement des perturbations intestinales fonctionnelles telles que les douleurs abdominales, pour le traitement d'un mammifère, notamment d'un être humain. L'invention porte également sur des procédés d'obtention de composés hydroxamiques de la formule (I) et sur leurs composés intermédiaires de la formule (II).
Pfizer Inc.
Smart & Biggar
LandOfFree
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