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1.发明公开
公开(公告)号：EP0920446A1
公开(公告)日：1999-06-09
申请号：EP97932978.0
申请日：1997-07-30
发明人： HORNIK, Vered , SERI-LEVY, Alon , GELLERMAN, Gary , GILON, Chaim
CPC分类号： C07K1/047 , A61K38/00 , C07K14/001 , C07K14/655 , C07K14/6555 , G01R31/318541 , Y02P20/55
摘要： 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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公开(公告)号：EP0804468A1
公开(公告)日：1997-11-05
申请号：EP95919592.0
申请日：1995-06-08
发明人： GILON, Chaim , EREN, Doron , ZELTSER, Irina , SERI-LEVY, Alon , BITAN, Gal , MULLER, Dan
CPC分类号： C07K14/001 , A61K38/00 , C07C271/22 , C07K7/02 , C07K7/18 , C07K7/56 , C07K14/6555 , G01R31/318541 , Y02P20/55
摘要： 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/(φ-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these Nα(φ-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.
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3.发明授权
公开(公告)号：EP0920446B1
公开(公告)日：2007-06-06
申请号：EP97932978.6
申请日：1997-07-30
申请人： DeveloGen Israel Ltd. , Yissum Research Development Company of the Hebrew University of Jerusalem
发明人： HORNIK, Vered , SERI-LEVY, Alon , GELLERMAN, Gary , GILON, Chaim
IPC分类号： A61K38/04 , C07K14/655 , A61P5/02
CPC分类号： C07K1/047 , A61K38/00 , C07K14/001 , C07K14/655 , C07K14/6555 , G01R31/318541 , Y02P20/55
摘要： 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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4.发明授权
公开(公告)号：EP0804468B1
公开(公告)日：2007-04-25
申请号：EP95919592.6
申请日：1995-06-08
申请人： DeveloGen Israel Ltd. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
发明人： GILON, Chaim , EREN, Doron , ZELTSER, Irina , SERI-LEVY, Alon , BITAN, Gal , MULLER, Dan
IPC分类号： C07K7/02 , C07K14/655 , C07K7/18 , C07C271/22
CPC分类号： C07K14/001 , A61K38/00 , C07C271/22 , C07K7/02 , C07K7/18 , C07K7/56 , C07K14/6555 , G01R31/318541 , Y02P20/55
摘要： 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 /( omega -functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N ( 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.
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