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111. 发明申请

WO2021019245A1 BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR EphA2 审中-公开
公开(公告)号：WO2021019245A1
公开(公告)日：2021-02-04
申请号：PCT/GB2020/051829
申请日：2020-07-30
申请人： BICYCLETX LIMITED
发明人： MCDONNELL, Kevin , UPADHYAYA, Punit , LAHDENRANTA, Johanna , MUDD, Gemma
IPC分类号： A61P35/00 , A61K47/50 , A61K38/12 , C07K7/54
摘要： The present invention relates to polypeptides which are covalently bound to non-aromatic molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of the Eph receptor tyrosine kinase A2 (EphA2). The invention also relates to pharmaceutical compositions comprising said peptide ligands and to the use of said peptide ligands in preventing, suppressing or treating a disease or disorder characterised by overexpression of EphA2 in diseased tissue (such as a tumour).

112. 发明申请

WO2020148525A1 BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR CAIX 审中-公开
公开(公告)号：WO2020148525A1
公开(公告)日：2020-07-23
申请号：PCT/GB2020/050069
申请日：2020-01-15
申请人： BICYCLETX LIMITED
发明人： BALDASSARRE, Leonardo , CHEN, Liuhong , LANI, Rachid , STACE, Catherine , TEUFEL, Daniel , WALKER, Edward
IPC分类号： C07K7/64 , A61P27/02 , A61P27/06 , C12N9/88 , A61P35/00 , A61K38/00 , A61K38/10 , A61K38/12 , A61K47/62
摘要： The present invention relates to polypeptides which are covalently bound to non-aromatic molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of carbonic anhydrase IX (CAIX). The invention also includes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups, to pharmaceutical compositions comprising said peptide ligands and drug conjugates and to the use of said peptide ligands and drug conjugates in preventing, suppressing or treating a disease or disorder mediated by CAIX.

113. 发明申请

WO2019243329A1 PEPTIDE LIGANDS FOR BINDING TO INTEGRIN ανβ3 审中-公开
公开(公告)号：WO2019243329A1
公开(公告)日：2019-12-26
申请号：PCT/EP2019/066010
申请日：2019-06-18
申请人： BICYCLETX LIMITED
发明人： TEUFEL, Daniel , MUDD, Gemma , PAVAN, Silvia
IPC分类号： C07K7/08 , A61K47/64 , A61P35/00
摘要： A peptide ligand specific for integrin ανβ3 comprising a polypeptide comprising three residues selected from cysteine, L-2,3 -diaminopropionic acid (Dap), N-beta-alkyl-L-2,3- diaminopropionic acid (N-AlkDap) and N-beta-haloalkyl-L-2,3-diaminopropionic acid (N- HAlkDap), with the proviso that at least one of said three residues is selected from Dap, N- AlkDap or N-HAlkDap, the said three residues being separated by at least two loop sequences, and a molecular scaffold, the peptide being linked to the scaffold by covalent alkylamino linkages with the Dap or N-AlkDap or N-HAlkDap residues of the polypeptide and by thioether linkages with the cysteine residues of the polypeptide when the said three residues include cysteine, such that two polypeptide loops are formed on the molecular scaffold. Also provided are drug conjugates comprising the peptide ligands conjugated to one or more effector groups and pharmaceutical compositions comprising the conjugates.

114. 发明申请

WO2018115204A1 PEPTIDE LIGANDS FOR BINDING TO MT1-MMP 审中-公开
公开(公告)号：WO2018115204A1
公开(公告)日：2018-06-28
申请号：PCT/EP2017/083954
申请日：2017-12-20
申请人： BICYCLETX LIMITED
发明人： TEUFEL, Daniel , MUDD, Gemma , PAVAN, Silvia
IPC分类号： C07K7/08 , A61K51/04 , A61K51/08 , A61K47/64
摘要： A peptide ligand specific for MT1 -MMP comprising a polypeptide comprising two diaminopropionic acid (Dap) or N-alkyldiaminopropionic acid (N-AlkDap) residues, and a third residue selected from cysteine, Dap or N-AlkDap, separated by at least two loop sequences, and a molecular scaffold, the peptide being linked to the scaffold by covalent alkylamino linkages with the Dap or N-AlkDap residues of the polypeptide and by covalent thioether linkages with the cysteine when the third residue is cysteine, such that two polypeptide loops are formed on the molecular scaffold, wherein the peptide ligand comprises an amino acid sequence of formula (II): -A 1 -X 1 -U/O 2 -X 3 -X 4 -G 5 -A 2 -E 6 -D 7 -F 8 -Y 9 -X 10 -X 11 -A 3 - (SEQ ID NO: 1) (II) or a pharmaceutically acceptable salt thereof; wherein: A 1 , A 2 , and A 3 are independently cysteine, L-2,3-diaminopropionic acid (Dap), N-beta-alkyl-L-2,3- diaminopropionic acid (N-AlkDap), or N-beta-haloalkyl-L-2,3-diaminopropionic acid (N- HAlkDap), provided that at least one of A 1 , A 2 , and A 3 is Dap, N-AlkDap or N-HAlkDap; X represents any amino acid residue; U represents a polar, uncharged amino acid residue selected from N, C, Q, M, S and T; and O represents a non-polar aliphatic amino acid residue selected from G, A, I, L, P and V.

115. 发明申请

WO2023084236A1 NOVEL USE 审中-公开
公开(公告)号：WO2023084236A1
公开(公告)日：2023-05-19
申请号：PCT/GB2022/052867
申请日：2022-11-11
申请人： BICYCLETX LIMITED
发明人： BESWICK, Paul , CHEN, Liuhong , DEMYDCHUK, Yuliya , HARMAN, Maximilian , KEEN, Nicholas , SKYNNER, Michael , VAN RIETSCHOTEN, Katerine
IPC分类号： A61P1/00 , A61K38/00 , A61P1/04 , A61P29/00 , C07K7/08
摘要： The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of ACE2. The invention also includes pharmaceutical compositions comprising said polypeptides and to the use of said polypeptides in suppressing or treating a disease or disorder mediated by ACE2, such as infection of COVID-19 or for providing prophylaxis to a subject at risk of infection of COVID-19.

116. 发明申请

WO2023031623A2 SYNTHESIS OF BICYCLE TOXIN CONJUGATES, AND INTERMEDIATES THEREOF 审中-公开
公开(公告)号：WO2023031623A2
公开(公告)日：2023-03-09
申请号：PCT/GB2022/052249
申请日：2022-09-02
申请人： BICYCLETX LIMITED
发明人： WITTY, David , LIMB, Darren , MIN, Byoung Joon , HE, Liwen , SANDERS, William J. , NNANABU, Ernest Obinna
IPC分类号： A61K47/64 , C07K5/02 , C07K5/0205
摘要： The present invention relates to Bicycle toxin conjugates, methods for preparation, and methods of use for treating cancer.

117. 发明申请

WO2022101633A1 BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR TRANSFERRIN RECEPTOR 1 (TfR1) 审中-公开
公开(公告)号：WO2022101633A1
公开(公告)日：2022-05-19
申请号：PCT/GB2021/052927
申请日：2021-11-12
申请人： BICYCLETX LIMITED
发明人： GOWANS, Ellen , MUDD, Gemma , RIGBY, Michael , SETH, Punit , SKYNNER, Michael , STANWAY, Steven , URBONAS, Liudvikas , VAN RIETSCHOTEN, Katerine
IPC分类号： C07K7/08 , A61K47/64 , C12N15/10
摘要： The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which bind to TfR1. The invention also relates to multimeric binding complexes which comprise at least two of said bicyclic peptide ligands. The invention also includes pharmaceutical compositions comprising said peptide ligands and multimeric binding complexes and the use of said peptide ligands, and multimeric binding complexes and pharmaceutical compositions in preventing, suppressing or treating a disease or disorder through TfR1 mediated delivery of a therapeutic agent.

118. 发明申请

WO2022029420A1 PEPTIDE-BASED LINKERS 审中-公开
公开(公告)号：WO2022029420A1
公开(公告)日：2022-02-10
申请号：PCT/GB2021/052001
申请日：2021-08-03
申请人： BICYCLETX LIMITED
发明人： MUDD, Gemma , MCDONNELL, Kevin , BESWICK, Paul
IPC分类号： C07K5/062 , C07K5/065 , C07K5/093 , A61K47/65
摘要： The invention relates to novel linkers which comprise two or three basic, acidic or hydrophobic natural or non-natural amino acids. The invention also relates to drug conjugates comprising said linkers, to pharmaceutical compositions comprising said drug conjugates and to the use of said drug conjugates in preventing, suppressing or treating cancer.

119. 发明申请

WO2021234391A1 BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR NECTIN-4 AND USES THEREOF 审中-公开
公开(公告)号：WO2021234391A1
公开(公告)日：2021-11-25
申请号：PCT/GB2021/051220
申请日：2021-05-20
申请人： BICYCLETX LIMITED
发明人： DICKSON, Amy Katherine , LIMB, Darren , MAHNKE, Lisa , RIGBY, Michael , WEST, Terrence Allen , WITTY, David
IPC分类号： A61K47/64 , A61K47/65 , A61K9/00 , A61K9/19 , A61K39/395 , A61K47/18 , A61K47/26 , A61P35/00
摘要： The present invention relates to a Bicycle toxin conjugate BT8009, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof, and uses thereof. In one embodiment, the pharmaceutical composition comprises BT8009, histidine, sucrose and Polysorbate 20. In another embodiment, the pharmaceutical composition is for use in treating an advanced solid tumor malignancy associated with Nectin-4-expression in a patient, preferably in combination with Nivolumab.

120. 发明申请

WO2021171028A1 ANTI-INFECTIVE BICYCLIC PEPTIDE CONJUGATES 审中-公开
公开(公告)号：WO2021171028A1
公开(公告)日：2021-09-02
申请号：PCT/GB2021/050490
申请日：2021-02-26
申请人： BICYCLETX LIMITED
发明人： BALMFORTH, Matthew , BESWICK, Paul , DAWSON, Mike , DODS, Rachel , ROWLAND, Catherine , SKYNNER, Michael , RIETSCHOTEN, Katerine Van , WAGSTAFF, James
IPC分类号： A61K47/54 , A61K47/64 , A61P31/00 , C07K7/64
摘要： The present invention relates to a polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the bicyclic peptides of the invention are conjugated to a carrier peptide in order to greatly enhance the bacterial cell killing activity. More particularly, the invention describes peptides which are high affinity binders of penicillin-binding proteins (PBPs), such as PBP3 and PBP3a. The invention also includes pharmaceutical compositions comprising said conjugates and to the use of said conjugates in suppressing or treating a disease or disorder mediated by bacterial infection or for providing prophylaxis to a subject at risk of infection.

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