C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 239/94 (2006.01) A61K 31/517 (2006.01) A61P 43/00 (2006.01)
Patent
CA 2666837
The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralising prosurvival Bcl-2 proteins: wherein A1, A2, B1, B2, B3, X, Z, R1, R2, R3 and t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.
L'invention concerne de manière générale des petites molécules qui imitent l'activité biologique de certains peptides et protéines, des compositions les contenant et leur utilisation. En particulier, l'invention concerne des composés de formule générale (I) qui imitent l'activité biologique de protéines uniquement BH3 et qui sont capables de se lier et de neutraliser des protéines pro-survie Bcl-2 : où A1, A2, B1, B2, B3, X, Z, R1, R2, R3 et t sont tels que décrits ici. L'invention concerne également des procédés de préparation des composés benzènesulfonamide qui imitent des parties de peptides et protéines, et l'utilisation de ces composés dans la régulation de la mort cellulaire et le traitement et/ou la prophylaxie de maladies et d'états associés à la dérégulation de la mort cellulaire.
Baell Jonathan Bayldon
Fairbrother Wayne J.
Flygare John A.
Koehler Michael F. T.
Lessene Guillaume Laurent
Genentech Inc.
Smart & Biggar
The Walter And Eliza Hall Institute Of Medical Research
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