Peptor Limited

Yeda Research and Develpment & Co. Ltd

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

Steba Biotech S.a.

Other

Develogen Israel Ltd.

Tookad IP Sarl

Doron Eren

Chaim Gilon

Alon Seri-Levy

Dan Muller

Irina Zeltser

Gal Bitan

Avigdor Scherz

Yoram Salomon

Alexander Brandis

Yoseph Salitra

Tamar Yechezkel

Natalia Koudinova

Efrat Rubinstein

Karin Neimann

Avraham Cohen

Nitsa Mazor

Gal Gitan

Conjugates of porphyrin, chlorophyll and bacteriochlorophyll photosensitizers with RGD-containing peptides or RGD peptidomimetics are provided that are useful for photodynamic therapy (PDT), particularly vascular-targeted PDT (VTP), of tumors and nonneoplastic vascular diseases such as age-related macular degeneration, and for diagnosis of tumors by different techniques.

Conjugates of RGD peptides and (bacterio)chlorophyll photosensitizers

A fed-batch fermentation method is for production of bacteriochlorophyll a (Bchla) from. The growth medium contains an inorganic nitrogen compound as a nitrogen source. During fermentation, the growth medium is supplemented with a succinate carbon source, an inorganic compound nitrogen source and a phosphorous source from external reservoirs connected to the fermenter vessel. After completion of the fermentation, Bchla is recovered from the separated cells.

Method for producing bacteriochlorophyll a

Conjugates of RGD peptides and porphyrin or (bacterio)chlorophyll photosynthesizers and their uses

The invention provides RGD-containing cyclic peptidomimetics; conjugates of said peptidomimetics and a moiety of a payload selected from fluorescent probes, photosensitizers, chelating agents, or cytotoxic agents; and pharmaceutical compositions comprising these conjugates. The conjugates of the invention are useful both for diagnostic purposes and treatment of various diseases, disorders and conditions. More specifically, conjugates comprising fluorescent probes can be used for diagnostic purposes, e.g., visualization of organs and tissues, and diagnosis of tumors; conjugates comprising photosensitizers can be used for photodynamic therapy of both tumors and nonneoplastic tissues; conjugates comprising chelating agents can be used in radioimaging or radiotherapy; and conjugates comprising cytotoxic agents can be used for targeted chemotherapy.

RGD-containing peptidomimetics and uses thereof

The invention provides RGD-containing cyclic peptidomimetics; conjugates of said peptidomimetics and a moiety of a payload selected from fluorescent probes, photosensitizers, chelating agents, or cytotoxic agents; and pharmaceutical compositions comprising these conjugates. The conjugates of the invention are useful both for diagnostic purposes and treatment of various diseases, disorders and conditions. More specifically, conjugates comprising fluorescent probes can be used for diagnostic purposes, e.g., visualization of organs and tissues, and diagnosis of tumors; conjugates comprising photosensitizers can be used for photodynamic therapy of both tumors and nonneoplastic tissues; conjugates comprising chelating agents can be used in radio imaging or radiotherapy; and conjugates comprising cytotoxic agents can be used for in targeted chemotherapy.

The invention provides cationic tetracyclic and pentacyclic bacteriochlorophyll derivatives (Bchls) containing at least one positively charged group and/or at least one basic group that is converted to a positively charged group under physiological conditions, preferably Bchls having an onium group derived from a N-containing aliphatic or heterocyclic radical such as ammonium, guanidinium, imidazolium, pyridinium, and the like or a phosphonium, arsonium, oxonium, sulfonium, selenonium, telluronium, stibonium, or bismuthonium group, or a basic group that is converted to such onium groups under physiological conditions, said groups being bound to one or more of the positions 17&#x3c;3&#x3e;, 13&#x3c;3&#x3e; and 3&#x3c;2&#x3e; of the Bchl molecule by ester or amide bond. The Bchls are useful for photodynamic therapy and diagnosis.

Catatonic bacteriochlorophyll derivatives

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 disclosed are N(&#x3c9;-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N(&#x3c9;-functionalized) amino acids are incorporated into a peptide sequence, 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 specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

Conformationally constrained backbone cyclized peptide analogs

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 disclosed are N (&ohgr;-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N (&ohgr;-functionalized) amino acids are incorporated into a peptide sequence, 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 specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

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 disclosed are N,(&ohgr;-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N,(&ohgr;-functionalized) amino acids are incorporated into a peptide sequence, 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 specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

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 disclosed are N.sup..alpha. (.omega.-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N.sup..alpha. (.omega.-functionalized) amino acids are incorporated into a peptide sequence, 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 backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

Growing community of inventors

Rehovot, Israel

Doron Eren