Combinatorial hydroxypropylamine library

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/25 (2006.01) C07B 61/00 (2006.01) C07C 237/22 (2006.01) C07C 237/24 (2006.01) C07C 237/42 (2006.01) C07D 211/62 (2006.01) G01N 33/543 (2006.01)

Patent

CA 2243568

A combinatorial library is disclosed which is represented by formula (I) or (I') wherein: (A) is a solid support; T'-L- is an identifier residue; and -L'- II' is a ligand/linker residue. This library contains hydroxypropylamines of the formula (II): -Aa1-Aa2-(CH2Ar1)-CH2CHOH-CH2XR1 wherein: Aa1 and Aa2 is each an amino acid joined to each other through an amide bond; Ar1 is an aromatic ring system; -CH2Ar1 is attached to N on Aa2; and R1 is H, C1-20 alkyl, alkenyl, alkynyl, aryl, heteroaryl, aryl or heteroaryl fused to a 3- or 4-membered moiety to form a non-aromatic second ring, or substituted C1-20 alkyl, alkenyl, or alkynyl.

L'invention porte sur une bibliothèque combinatoire représentée par la formule (I) ou la formule (I') dans lesquelles: (A) est un support solide; T'-L- est un résidu identificateur; et -L'-II' est un résidu ligand/segment de liaison. Cette bibliothèque comprend des hydroxypropylamines de formule (II) -Aa?1¿-Aa?2¿-(CH¿2?Ar?1¿)-CH¿2?CHOH-CH¿2?XR?1¿ dans laquelle Aa?1¿ et Aa?2¿ sont tous deux un acide aminé lié à l'autre par l'intermédiaire d'une liaison amide; Ar?1¿ est un système de cycles aromatiques; -CH¿2?Ar?1¿ est lié à N sur Aa?2¿; et R?1¿ est H, alkyle C¿1-20?, alcényle, alcynyle, aryle, hétéroaryle, ou hétéroaryle fusionné à une fraction à trois ou quatre éléments pour former un second cycle non aromatique, ou un alkyle C¿1-20?, un alcényle, ou un alcynyle, substitués.

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