Macrolides

Details Macrolides Macrolides

C - Chemistry, Metallurgy

07

K

C07K 5/062 (2006.01) A61K 38/05 (2006.01) C07D 309/10 (2006.01) C07D 309/30 (2006.01) C07D 491/10 (2006.01) C07D 491/107 (2006.01) C07D 519/00 (2006.01) C07F 7/08 (2006.01) C07K 5/06 (2006.01) C12N 1/20 (2006.01) C12N 1/21 (2006.01) C12P 21/02 (2006.01) G01N 33/53 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2224715

A novel class of macrolides in which i) positions 2 to 6 inclusive of the macrocyclic ring are provided by a piperidazinyl carboxylic acid residue; and/or ii) positions 7 to 9 inclusive of the macrocyclic ring are provided by an aromatic .alpha.-amino acid residue; and/or iii) positions 10 to 12 inclusive of the macrocyclic ring are provided by an aliphatic .alpha.-amino acid residue, preferably comprising two, or especially all three of the characteristic structural features i), ii) and iii), more especially a compound of formula (IX) is provided having immunosuppressant and anti- inflammatory properties and protected and ring-open forms thereof.

L'invention concerne une nouvelle classe de macrolides dans lesquelles i) les positions 2 à 6 de l'anneau macrocyclique sont occupées par un résidu d'acide carboxylique de piperidazinyl; et/ou ii) les positions 7 à 9 de l'anneau macrocyclique sont occupées par un résidu d'acide .alpha.-amino aromatique; et/ou iii) les positions 10 à 12 de l'anneau macrocyclique sont occupées par un résidu d'acide .alpha.-amino aliphatique, comprenant de préférence deux, ou plus particulièrement les trois caractéristiques structurelles i), ii) et iii), plus spécialement un composé de la formule (IX) ayant des propriétés d'immunosuppression et anti-inflammation, ainsi que leurs formes protégées et à cycles ouverts.

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