1,3-bis-(substituted-phenyl)-2-propen-1-ones and their use...

Details 1,3-bis-(substituted-phenyl)-2-propen-1-ones and their use... 1,3-bis-(substituted-phenyl)-2-propen-1-ones and their use...

C - Chemistry, Metallurgy

07

D

C07D 333/56 (2006.01) A61K 31/09 (2006.01) A61K 31/12 (2006.01) A61K 31/381 (2006.01) A61K 31/4184 (2006.01) A61K 31/423 (2006.01) A61K 31/498 (2006.01) A61K 31/517 (2006.01) A61P 3/10 (2006.01) A61P 9/10 (2006.01) A61P 11/06 (2006.01) A61P 17/06 (2006.01) A61P 19/02 (2006.01) C07C 49/577 (2006.01) C07C 49/796 (2006.01) C07C 49/813 (2006.01) C07C 49/835 (2006.01) C07C 49/84 (2006.01) C07C 49/86 (2006.01) C07C 59/70 (2006.01) C07C 205/45 (2006.01) C07D 309/06 (2006.01) C07D 317/44 (2006.01) C07D 333/16 (2006

Patent

CA 2413878

It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post- angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.

Cette invention repose sur la découverte selon laquelle certains 1,3-bis-(phényl substitué)-2-propène-1-ones, notamment les composés de la formule (I), inhibent l'expression de VCAM-1, et par conséquent, peuvent être utilisés pour traiter un patient atteint d'un trouble véhiculé par VCAM-1. Les exemples des troubles inflammatoires véhiculés par VCAM-1, sont, entre autres, l'arthrite, l'asthme, la dermatite, la fibrose cystique, le rejet d'organe solide chronique ou tardif consécutif à la transplantation, la sclérose en plaques, le lupus érythémateux disséminé, les maladies entériques inflammatoires, le diabète auto-immun, la rétinopathie diabétique, la rhinite, les lésions résultant d'une ischémie/reperfusion, la resténose consécutive à une angioplastie, la bronchopneumopathie chronique obstructive (BPCO), la glomérulonéphrite, la maladie de Graves, les allergies gastro-intestinales, la conjonctivite, l'athérosclérose, les troubles de l'artère coronaire, l'angine et la maladie des petites artères.

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