Method of drug design

C - Chemistry – Metallurgy – 40 – B

Patent

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Details

C40B 30/04 (2006.01) A61K 31/7052 (2006.01) A61P 5/02 (2006.01) C07B 61/00 (2006.01) C07D 309/10 (2006.01) C07D 309/14 (2006.01) C07H 7/00 (2006.01) C07H 7/02 (2006.01) C07H 15/00 (2006.01) C07H 15/04 (2006.01) C07H 15/12 (2006.01) C07H 15/18 (2006.01) C07H 15/26 (2006.01) C07K 14/655 (2006.01) C40B 20/06 (2006.01) C40B 40/12 (2006.01) C40B 50/08 (2006.01) C40B 50/14 (2006.01) G01N 33/53 (2006.01)

Patent

CA 2619457

The invention provides a method of identifying biologically active compounds comprising: (a) designing a first library of compounds of formula (1) to scan molecular diversity wherein each compound of the library has at least two pharmacophoric groups R1 to R5 as defined below and wherein compound of the library has same number of pharmacophoric groups; (b) assaying the first library of compounds in one or more biological assay(s); and (c) designing a second library wherein each compound of the second library contains one or more additional pharmacophoric group with respect to the first library; such that the/each component of the first and second library is a compound of formula (1).

La présente invention concerne une méthode d'identification de composés biologiquement actifs qui comprend : (a) la conception d'une première bibliothèque de composés de formule (1) pour balayer la diversité moléculaire, chaque composé de la bibliothèque portant au moins deux groupements pharmacophores R1 à R5 comme défini ci-dessous, et chaque composé de la bibliothèque ayant le même nombre de groupements pharmacophores ; (b) l'évaluation de la première bibliothèque de composés dans un ou plusieurs tests biologiques ; et (c) la conception d'une seconde bibliothèque, chaque composé de la seconde bibliothèque contenant un ou plusieurs groupements pharmacophores supplémentaires par rapport à la première bibliothèque ; de sorte que le/chaque composant de la première et de la seconde bibliothèque soit un composé de formule (1).

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