Conformationally constrained backbone cyclized somatostatin...

A - Human Necessities – 61 – K

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A61K 38/04 (2006.01) A61K 38/12 (2006.01) C07K 7/50 (2006.01) C07K 7/64 (2006.01) C07K 14/655 (2006.01) G01R 31/3185 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2335488

Novel peptides which are conformationally constrained backbone cyclized somatostatin analogs, having somatostatin receptor sub-type selectivity are disclosed. These patterns of receptor subtype selectivity provide compounds having improved therapeutic utility. Methods for synthesizing the somatostatin analogs and for screening of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs, and methods of using such compositions are disclosed.

L'invention concerne de nouveaux peptides qui sont des analogues de la somatostatine cyclisés par squelette à contrainte de conformation et qui présentent une sélectivité de sous-type de récepteur de la somatostatine. Ces motifs de sélectivité de sous-type de récepteur fournissent des composés présentant une utilité thérapeutique améliorée. L'invention concerne également des méthodes de synthèse des analogues de la somatostatine ainsi que des méthodes de criblage de ces analogues de la somatostatine. L'invention concerne également des compositions pharmaceutiques comprenant ces analogues de la somatostatine ainsi que des procédés d'utilisation de ces compositions.

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