Modulators of proteins with phosphotyrosine recognition units

Details Modulators of proteins with phosphotyrosine recognition units Modulators of proteins with phosphotyrosine recognition units

C - Chemistry, Metallurgy

07

D

C07D 233/70 (2006.01) A61K 31/21 (2006.01) A61K 31/235 (2006.01) A61K 31/4164 (2006.01) A61K 31/695 (2006.01) A61P 43/00 (2006.01) C07C 59/52 (2006.01) C07C 59/84 (2006.01) C07C 69/44 (2006.01) C07C 235/12 (2006.01) C07C 327/10 (2006.01) C07D 233/60 (2006.01) C07D 233/64 (2006.01) C07D 241/42 (2006.01) C07D 263/32 (2006.01) C07D 277/24 (2006.01) C07D 401/04 (2006.01) C07D 471/04 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2275610

The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1) Y-X- C(R')=C(R")COOR''', to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. R' and R'' are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R''' is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or .alpha. wherein (*) indicates a potential point of attachment to X.

La présente invention concerne de nouveaux composés modulant la protéine tyrosine phosphatase et correspondant à la structure générale illustrée dans la formule (A1) Y-X-C(R')=C(R'')COOR''', des procédés de préparation de ces composés et des compositions contenant ces composés. L'invention se rapporte en outre à l'utilisation de ces composés dans le traitement de troubles chez l'être humain et chez l'animal, dans la purification de protéines ou de glycoprotéines, et dans des diagnostics. L'invention se rapporte enfin à la modulation de l'activité de molécules possédant des unités de reconnaissance de la phosphotyrosine, y compris les protéines tyrosine phosphatases (PTPases) et les protéines possédant des domaines Src-homologie-2, dans des systèmes in vitro, des micro-organismes et des cellules eucaryotes, ainsi que chez des animaux et des êtres humains dans leur ensemble. R' et R'' sont choisis indépendamment l'un de l'autre dans le groupe comprenant un hydrogène, un halo, cyano, nitro, trihalométhyle, alkyle, arylalkyle. R''' est choisi dans le groupe comprenant un hydrogène, un alkyle, alkyle substitué, aryle, arylalkyle. X est un aryle. Y est choisi entre un hydrogène ou .alpha. où (*) indique un point éventuel de rattachement à X.

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