C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 307/16 (2006.01) A61K 31/17 (2006.01) A61K 31/34 (2006.01) A61K 31/38 (2006.01) A61K 31/44 (2006.01) C07C 317/22 (2006.01) C07D 307/12 (2006.01) C07D 333/24 (2006.01) C07D 405/00 (2006.01) C07D 405/04 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01)
Patent
CA 2180123
2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothlophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.
L'invention porte sur des 2,5 diaryl-tétrahydrofuranes, des 2,5 diaryl-tétrahydrothiophènes et des 1,3 diaryl-cyclopentanes qui réduisent la chémiotaxie et les explosions respiratoires conduisant à la formation de radicaux oxygène nuisibles des leucocytes polymorphonucléaires lors d'une réponse à caractère inflammatoire ou immunitaire. Ces composés agissent biologiquement soit simplement comme antagonistes des récepteurs PAF en inhibant l'enzyme "5-lipogénase", soit doublement comme antagonistes des récepteurs PAF et comme inhibiteurs de l'enzyme "5-lipogénase". L'invention porte également sur une méthode de traitement des troubles dus au PAF et aux leucotriènes consistant à administrer au patient une dose efficace d'un ou de plusieurs des composés ci-dessus ou leurs sels pharmacocompatibles placés facultativement dans un excipient pharmacocompatible.
Biftu Tesfaye
Cai Xiong
Grewal Gurmit
Hussoin Sajjat
Shen T. Y.
Bereskin & Parr
Cytomed Inc.
Millennium Pharmaceuticals Inc.
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