Collagen receptor i-domain binding modulators

Details Collagen receptor i-domain binding modulators Collagen receptor i-domain binding modulators

C - Chemistry, Metallurgy

07

K

C07K 14/705 (2006.01) A61K 31/18 (2006.01) A61K 31/65 (2006.01) C07C 49/798 (2006.01) C07C 317/32 (2006.01) C40B 30/02 (2006.01) G01N 33/68 (2006.01) G06F 19/00 (2006.01)

Patent

CA 2622616

The present invention relates to a refined and detailed molecular model of the .alpha.2.beta.1 integrin l-domain, especially the MIDAS and to the use of such a model for designing novel integrin modulators, especially .alpha.2.beta.1 integrin modulators. The present invention further relates to novel .alpha.2.beta.1 I- domain modulators, which are of therapeutic potential. The present invention further relates to specific families of small molecule modulators interacting with collagen receptors, tetracyclic polyketides and sulfonamides. The present invention further relates to the use of such modulators for the manufacture of medicaments for thrombosis, inflammation and/or cancer.

La présent invention concerne un modèle moléculaire perfectionné et détaillé du domaine l de l~intégrine .alpha.2.beta.1, en particulier le MIDAS, ainsi que l~utilisation d'un tel modèle pour la conception de nouveaux modulateurs de l~intégrine, en particulier les modulateurs de l~intégrine .alpha.2.beta.1. Cette invention concerne également de nouveaux modulateurs du domaine I de .alpha.2.beta.1 qui présentent un potentiel thérapeutique. Cette invention concerne également des familles spécifiques de modulateurs de petites molécules qui interagissent avec les récepteurs du collagène, les polykétides tétracycliques et les sulfamides. L~invention concerne également l~utilisation de ces modulateurs en vue de fabriquer des médicaments pour la thrombose, l~inflammation et/ou le cancer.

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