Peptor Limited

Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.

Develogen Israel Ltd.

Vered Hornik

Gary Gellerman

Chaim Gilon

Michel M Afargan

Alon Seri-Levy

Eran Hadas

Mich El M Afargan

Mich El Afargan

Methods of use of pharmaceutical compositions and novel peptides which are conformationally constrained backbone cyclized somatostatin analogs, having somatostatin receptor subtype selectivity, are disclosed. These patterns or 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 are disclosed.

Conformationally constrained backbone cyclized somatostatin analogs

Novel peptides which are conformationally constrained backbone cyclized somatostatin analogs, having somatostatin receptor subtype selectivity are disclosed. These patterns or 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.

Novel peptides which are conformationally constrained backbone cyclized antagonists of IL-6, are disclosed. Methods for synthesizing the IL-6 antagonists are also disclosed. Furthermore, pharmaceutical compositions comprising IL-6 antagonists, and methods of using such compositions are disclosed.

Conformationally constrained backbone cyclized interleukin-6 antagonists

Novel backbone-cyclized BPI peptide analogs and methods of making the same by the use of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units used in the synthesis of these backbone-cyclized peptide analogs are N -functionalized amino acids constructed to include a spacer and a terminal functional group. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. A plurality of these N&agr;&ohgr;-functionalized amino acids are incorporated into a library of peptide sequences, preferably during solid phase peptide synthesis.

Backbone-cyclized BPI peptidomimetics

Novel peptides which are conformationally constrained backbone cyclized somatostatin analogs. Methods for synthesizing the somatostatin analogs and for producing libraries of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs, and methods of using such compositions are disclosed.

Libraries of novel backbone-cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units used in the synthesis of these backbone-cyclized peptide analogs are N(((-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N(((-functionalized) amino acids are incorporated into a library of peptide sequences, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by libraries of backbone-cyclized bradykinin analogs, somatostatin analogs, BPI analogs and Substance P analogs having biological activity. Further embodiments of the invention are Interleukin-6 receptor derived peptides having ring structures involving backbone cyclization.

Libraries of backbone-cyclized peptidomimetics

Novel peptide analogs are disclosed. The novel peptides are conformationally constrained backbone cyclized somatostatin analogs. Methods for synthesizing the somatostatin analogs and for producing libraries of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs, and methods of using such compositions in the treatment of endocrine disorders, neoplasms and metabolic disorders are also disclosed.

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Rehovot, Israel

Vered Hornik