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1.发明授权
公开(公告)号：EP1043974B1
公开(公告)日：2002-04-03
申请号：EP98966710.0
申请日：1998-12-28
申请人： Cellpep S.A.
CPC分类号： A61K9/127 , A61K38/162
摘要： The incorporation of multiple branch peptide constructions having activity against HIV (such as those described in WO 95/07929 and WO 98/29443) into liposomes of sufficient size for white blood cell internalisation (e.g. greater than 150 nm and preferably approximately 250 to 400 nm) has been shown to increase the activity of those MBPCs manifold. The liposomes and pharmaceutical compositions containing them are claimed.
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公开(公告)号：EP1315747B1
公开(公告)日：2006-03-29
申请号：EP01980332.9
申请日：2001-09-03
申请人： Cellpep S.A.
IPC分类号： C07K14/435 , A61K38/17 , A01N63/02
CPC分类号： C07K14/43522 , A61K38/00
摘要： Derivatives of Maurotoxin (MTX) in which the native disulfide bridge pattern (Cys3-Cys24, Cys9-Cys29, Cys19, Cys31-Cys34) has been disrupted are useful for the treatment of pathologies associated with dysfunctioning and/or activation of Ca -activated and/or voltage-gated K channel subtypes, such as IKCa1 or Kv1.2. One preferred group of derivatives is that in which one or more of the Cys residues have been replaced with
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公开(公告)号：EP1315747A2
公开(公告)日：2003-06-04
申请号：EP01980332.9
申请日：2001-09-03
申请人： Cellpep S.A.
IPC分类号： C07K14/435 , A61K38/17 , A01N63/02
CPC分类号： C07K14/43522 , A61K38/00
摘要： Derivatives of Maurotoxin (MTX) in which the native disulfide bridge pattern (Cys3-Cys24, Cys9-Cys29, Cys19, Cys31-Cys34) has been disrupted are useful for the treatment of pathologies associated with dysfunctioning and/or activation of Ca2+-activated and/or voltage-gated K+ channel subtypes, such as IKCa1 or Kv1.2. One preferred group of derivatives is that in which one or more of the Cys residues have been replaced with ?-aminobutyrate (Abu) residues, thus breaking one or more of the four disulphide bridges. Within this group, the preferred derivative is that in which the Cys residues at position 9, 19, 29 and 34 have been replaced with a ?-aminobutyrate residues. However, the derivative in which the Cys residues at positions 19 and 34 have been replaced with (Abu) residues is excluded Another preferred group of derivatives is that in which one or two of the amino acidresidues of maurotoxin have been replaced by different amino acid residues resulting in the disulfide bridge pattern being changed to Cys3-Cys24, Cys9-Cys29, Cys13-Cys31, Cys19-Cys34. Within this group, the preferred compounds are that which the Arg residue at position 14 has been replaced by a Gln residue, that in which the Lys residue at position 15 has been replaced by a Gln residue, that in which the Arg residue at position 14 and Lys residue at position 15 have both been replaced by Gln residues, those in which neither of the residues at positions 32 and 33 is a Gly or Pro residue, and that in which the Gly residue at position 33 has been replaced by an Ala residue. Pi1 and HsTx1 derivatives with disrupted native disulfide bridge patterns are similarly useful.
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公开(公告)号：EP0950063B1
公开(公告)日：2003-03-26
申请号：EP97953934.3
申请日：1997-12-30
申请人： Cellpep S.A.
CPC分类号： C07K14/005 , A61K38/00 , C12N2740/16122
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公开(公告)号：EP1758930A2
公开(公告)日：2007-03-07
申请号：EP05758794.1
申请日：2005-06-27
申请人： Cellpep S.A.
IPC分类号： C07K14/435
CPC分类号： C07K14/43522
摘要： OsK1 is a 38-residue peptide with 3 disulphide bridges and is found in the venom of the scorpion Orthochirus scrobiculosus. It is potently active on voltage-gated K+ channels Kv1.1, Kvl.2 and Kvl.3, and moderately active on the type 1 intermediate-conductance Cat2+-activated channel Kca3.1. Derivatives of OsK1, particularly involving truncation or point mutations, have been developed to enhance the activity against and selectivity for the Kvl.3 channel. This renders the derivatives likely candidates for the treatment of autoimmune diseases, including multiple sclerosis. Such use may be alone or in combination therapy with maurotoxin, another scorpion toxin.
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公开(公告)号：EP1263783B1
公开(公告)日：2007-01-17
申请号：EP01936061.9
申请日：2001-03-05
申请人： Cellpep S.A.
IPC分类号： C07K14/435
CPC分类号： C07K14/43522 , A61K38/00
摘要： Maurocalcine, a novel toxin isolated from the venom of the Tunisian chactidae scorpion Scorpio maurus palmatus, has the amino acid sequence GDCLPHLKLCKENKDCCSKKCKRRGTNIEKRCR (SEQ. ID. No. 1). It potently and reversibly modifies channel gating behaviour of type 1 ryanodine receptor (RyR1) by inducing prominent subconductance behavior. Maurocalcine and its bioactive structural analogues - preferably those containing the KKCKRR motif corresponding to part of the II-III loop of the alpha1S subunit of the voltage-dependent skeletal muscle calcium channel dihydropyridine receptor - appear to possess a therapeutic potential, notably as candidate immuno-suppressive drugs, and for the treatment of pathologies in humans that may involve a dysfunction of calcium channels.
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7.发明公开MODIFIED ANTIVIRAL PEPTIDES WITH INCREASED ACTIVITY AND CELL MEMBRANE AFFINITY 审中-公开改进的抗病毒肽具有提高活性和细胞膜亲和力
公开(公告)号：EP1635866A2
公开(公告)日：2006-03-22
申请号：EP04739320.2
申请日：2004-05-20
申请人： Cellpep S.A.
IPC分类号： A61K39/21
CPC分类号： C07K14/005 , A61K38/00 , A61K39/00 , C07K5/0806 , C07K5/1008 , C07K5/1019 , C07K7/02 , C07K2319/00 , C12N2740/16122
摘要： The activity and cell membrane affinity of certain antiviral multiple branch peptide constructions, including those known from WO 95/07929, WO 98/29443 and WO 03/95479, can be improved by bonding to the C-end of the peptide a terminator which is either (a) an ω-amino-fatty acid having from 4 to 10 carbon atoms and from 0 to 2 carbon-carbon double bonds or (b) a peptidic cell membrane penetrating agent. The improvement is so marked that in some cases the number of branches can be reduced, sometimes to a single branch, and/or that the branches may be shortened. The preferred ω-amino-fatty acids are Ϝ-aminobutyric acid, δ-aminovaleric acid and ϵ-aminocaproic acid. The peptidic cell membrane penetrating agent is suitably a TAT-derived peptide, penetratin® or Kpam.
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公开(公告)号：EP1628997A2
公开(公告)日：2006-03-01
申请号：EP04762984.5
申请日：2004-05-28
申请人： Cellpep S.A.
发明人： SABATIER, Jean-Marc , FAJLOUN, Ziad
IPC分类号： C07K1/113
CPC分类号： C07K1/1133
摘要： The folding/oxidation of a reduced peptide or partially reduced peptide to form a disulphide bridged peptide is effected by dissolving it in an oxidizing organic solvent, alone or in admixture with water, adding an aqueous alkaline buffer to the solution, and recovering the resultant disulphide bridged peptide. The preferred oxidizing organic solvent is dimethylsulphoxide, which is desirably used as a 10 to 50% aqueous solution. The addition of the aqueous alkaline buffer, which is preferably a 0.2 M Tris-HCI buffer, is preferably added during a period of from 5 to 90 minutes after dissolution of the reduced peptide in the oxidizing organic solvent. The method allows reduced peptides which are insoluble in alkaline conditions to be oxidized and allows reduced peptides which may form stable but inactive oxidized species if treated with dimethylsulphoxide alone to be fully oxidized.
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9.发明公开MULTIPLE BRANCH PEPTIDE CONSTRUCTIONS COMPRISING FROM 2 TO 16 BRANCHES OF THE PEPTIDE RQGYS OR FROM 8 TO 16 BRANCHES OF THE PEPTIDE RQGY PROVIDING FROM THE HIV GP41 GLYCOPROTEIN 有权多分支肽构建与肽RQGYS的2至16个分支或RQGY肽的8至16个分支来自HIV GP41糖蛋白
公开(公告)号：EP1497323A1
公开(公告)日：2005-01-19
申请号：EP03749859.9
申请日：2003-04-22
申请人： Cellpep S.A.
CPC分类号： C07K14/005 , A61K9/127 , A61K38/162 , C12N2740/16122
摘要： Multiple branch peptide constructions formed from peptides derived from the envelope transmembrane glycoprotein gp41 of HIV, and including from 2 to 16 branches of the peptide RQGYS or from 8 to 16 branches of the peptide RQGY, show increased receptor affinity and prevent cell-to-cell fusion. They have a direct virostatic effect. These MBPCs are able to neutralize in vitro the different steps of virus envelope/cell membrane fusion, and infected cell membrane/uninfected cell membrane fusion of several strains of HIV-1 and HIV-2. These results open a potential use in treatment of HIV infection.
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公开(公告)号：EP1263783A2
公开(公告)日：2002-12-11
申请号：EP01936061.9
申请日：2001-03-05
申请人： Cellpep S.A.
IPC分类号： C07K14/435
CPC分类号： C07K14/43522 , A61K38/00
摘要： Maurocalcine, a novel toxin isolated from the venom of the Tunisian chactidae scorpion Scorpio maurus palmatus, has the amino acid sequence GDCLPHLKLCKENKDCCSKKCKRRGTNIEKRCR (SEQ. ID. No. 1). It potently and reversibly modifies channel gating behaviour of type 1 ryanodine receptor (RyR1) by inducing prominent subconductance behavior. Maurocalcine and its bioactive structural analogues - preferably those containing the KKCKRR motif corresponding to part of the II-III loop of the alpha1S subunit of the voltage-dependent skeletal muscle calcium channel dihydropyridine receptor - appear to possess a therapeutic potential, notably as candidate immuno-suppressive drugs, and for the treatment of pathologies in humans that may involve a dysfunction of calcium channels.
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