CONFORMATIONALLY CONSTRAINED BACKBONE CYCLIZED PEPTIDE ANALOG
申请人:PEPTOR LTD
公开号:EP0804468A1
公开(公告)日:1997-11-05
METHOD OF MAKING AN OMEGA-FUNCTIONALIZED AMINO ACID DERIVATIVE
申请人:DeveloGen Israel Ltd.
公开号:EP0804468B1
公开(公告)日:2007-04-25
[EN] CONFORMATIONALLY CONSTRAINED BACKBONE CYCLIZED PEPTIDE ANALOG<br/>[FR] ANALOGUES PEPTIDIQUES CYCLISES PAR LE SQUELETTE, A CONFORMATION RESTREINTE
申请人:PEPTOR LTD.
公开号:WO1995033765A1
公开(公告)日:1995-12-14
(EN) 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$g(a)/($g(v)-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N$g(a)($g(v)-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.(FR) On obtient de nouveaux analogues peptidiques cyclisés par le squelette à l'aide de groupes de pontage, fixés par les azotes alpha des dérivés d'acides aminés afin de former de nouvelles liaisons non peptidiques. Les nouveaux motifs de constitution décrits sont des acides aminés N$g(a)($g(v)-fonctionnalisés) structurés pour renfermer un espaceur et un groupe fonctionnel. Un ou plusieurs de ces acides aminés N$g(a)($g(v)-fonctionnalisés) sont incorporés dans une séquence peptidique, de préférence lors de la synthèse peptidique en phase solide. Les groupes fonctionnels, terminaux, réactifs sont protégés par des groupes inhibants, spécifiques qui peuvent être sélectivement retirés pour effectuer des cyclisations soit squelette/squelette, soit squelette/chaîne latérale. Les antagonistes de la bradykinine cyclisés par le squelette et ayant une activité biologique sont un exemple illustrant l'invention. D'autres modes de réalisation de l'invention sont des analogues de la somatostatine présentant une ou deux structures cycliques comprenant la cyclisation du squelette.
[EN] CONFORMATIONALLY CONSTRAINED BACKBONE CYCLIZED PEPTIDE ANALOGS<br/>[FR] ANALOGUES PEPTIDIQUES CYCLISES POSSEDANT UN SQUELETTE A CONFORMATION CONTRAINTE
申请人:GILON CHAIM
公开号:WO2004074316A1
公开(公告)日:2004-09-02
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 Nα (ω-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these Nα (ω-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 selectivley 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.