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1. 发明申请

WO2023034870A2 COMPOUNDS AND METHODS FOR REDUCING DMPK EXPRESSION 审中-公开
公开(公告)号：WO2023034870A2
公开(公告)日：2023-03-09
申请号：PCT/US2022/075772
申请日：2022-08-31
申请人： IONIS PHARMACEUTICALS, INC.
发明人： RIGO, Frank , DWYER, Chrissa, A.
IPC分类号： C12N15/113 , A61K47/06 , A61K47/26 , A61K47/68 , A61K31/7088 , A61K47/549 , A61K47/6807 , A61K47/6849 , C12N15/1137 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/3231 , C12N2310/3341 , C12N2310/341 , C12N2310/345 , C12N2310/346 , C12N2310/351
摘要： Provided are oligomeric compounds, methods, and pharmaceutical compositions for DMPK the amount or activity of DMPK RNA in a cell or animal, and in certain instances reducing the amount of DMPK protein in a cell or animal. Such oligomeric compounds, methods, and pharmaceutical compositions are useful to treat type 1 myotonic dystrophy.

2. 发明申请

WO2022231730A2 SYNTHETIC STRATEGY TO POLYMERIZE PROTEIN INTO MOLECULARLY DEFINED POLYMERS 审中-公开
公开(公告)号：WO2022231730A2
公开(公告)日：2022-11-03
申请号：PCT/US2022/021359
申请日：2022-03-22
申请人： NORTHWESTERN UNIVERSITY
发明人： MIRKIN, Chad, A. , WINEGAR, Peter, H. , FIGG, Charles, A.
IPC分类号： B82Y40/00 , C07K19/00 , C12N15/11 , A61K47/6807 , A61K47/6849 , C07K16/00 , C07K16/2803 , C07K16/2818 , C07K2317/31 , C07K2317/76 , C07K2317/92
摘要： Methods for forming a sequence encoded oligomer includes oligomerizing first and second antibody-oligonucleotide conjugates through hybridization using at least one template oligo nucleotide. The first antibody-oligonucleotide conjugate comprises an oligonucleotide strand comprising a first sequence and a second sequence joined by an alkyne. The second antibody- oligonucleotide conjugate comprises an oligonucleotide strand comprising a third sequence and a fourth sequence joined by an alkyne. The at least one template oligonucleotide strand comprises at least two template sequences, one of the t two template sequences being complementary to one of the first and second sequences of the first antibody-oligonucleotide conjugate and the other being complementary to one of the third and fourth sequences of the second antibody-oligonucleotide conjugate, such that the at least one template oligonucleotide strand hybridizes to a portion of the oligonucleotide strand of the first-antibody-oligonucleotide conjugate and to a portion of the oligonucleotide strand of the second-antibody.

3. 发明申请

WO2022032188A1 METHODS FOR THE SYNTHESIS OF PROTEIN-DRUG CONJUGATES 审中-公开
公开(公告)号：WO2022032188A1
公开(公告)日：2022-02-10
申请号：PCT/US2021/045096
申请日：2021-08-06
申请人： CIDARA THERAPEUTICS, INC.
发明人： BORCHARDT, Allen , HUGHES, Robert, Michael
IPC分类号： A61K47/68 , A61K47/64 , A61P31/16 , A61K47/643 , A61K47/6807
摘要： The present invention relates to methods for the synthesis of conjugates useful for the treatment of viral infections, e.g., conjugates containing inhibitors of viral neuraminidase (e.g., zanamivir or an analog thereof) linked to an Fc domain monomer.

4. 发明申请

WO2021261996A2 HYDRAZONE-BASED SAPONIN DERIVATIVES 审中-公开
公开(公告)号：WO2021261996A2
公开(公告)日：2021-12-30
申请号：PCT/NL2021/050392
申请日：2021-06-22
申请人： SAPREME TECHNOLOGIES B.V.
发明人： POSTEL, Ruben , HERMANS, Guy
IPC分类号： A61K47/54 , A61K47/68 , A61P35/00 , A61K47/549 , A61K47/6807 , A61K47/6849
摘要： The invention relates to a saponin derivative The invention also relates to a first pharmaceutical composition comprising the saponin derivative of the invention. In addition, the invention relates to a pharmaceutical combination comprising the first pharmaceutical composition of the invention and a second pharmaceutical composition comprising for example an ADC or AOC. The invention also relates to the first pharmaceutical composition or the pharmaceutical combination of the invention, for use as a medicament, or use in the treatment or prophylaxis of a cancer or an auto-immune disease. Furthermore, the invention relates to an in vitro or ex vivo method for transferring a molecule from outside a cell to inside said cell, comprising contacting said cell with the molecule and with a saponin derivative of the invention. The invention also relates to a saponin conjugate comprising a cell-surface molecule binding-molecule, capable of binding to a target cell, covalently bound to the saponin. The invention also relates to a pharmaceutical combination comprising a pharmaceutical composition comprising the saponin conjugate of the invention and a second pharmaceutical composition comprising an active pharmaceutical ingredient, or to a pharmaceutical composition comprising the saponin conjugate of the invention and an active pharmaceutical ingredient. In addition, the invention relates to said pharmaceutical combination of the invention or said pharmaceutical composition of the invention, for use as a medicament, or for use in the treatment or the prophylaxis of a cancer or an auto-immune disease.

5. 发明申请

WO2023278897A1 COMPOSITIONS AND METHODS FOR TREATING CANCERS 审中-公开
公开(公告)号：WO2023278897A1
公开(公告)日：2023-01-05
申请号：PCT/US2022/036143
申请日：2022-07-05
申请人： YALE UNIVERSITY , GENNAO BIO, INC. , BOMMIREDDYVENKATA, Venugopalareddy , ESCOBAR-HOYOS, Luisa
发明人： QUIJANO, Elias , GLAZER, Peter , TURNER, Bruce, C. , LUDWIG, Dale
IPC分类号： A61K47/68 , A61P35/00 , C07K16/44 , C12N15/87 , A61K47/6807 , A61K47/6835 , A61K47/6877 , A61K48/0008 , C07K2317/77
摘要： Compositions and methods are provided for treating cancer by administering a complex formed between a therapeutic polynucleotide and a 3E10 antibody or variant thereof, or antigen- binding fragment thereof. In some instances, the complexes are stabilized through a molar ratio of 3E10 antibody or variant thereof, or antigen-binding fragment thereof to therapeutic polynucleotide of at least about 2: 1.

6. 发明申请

WO2021260061A2 SAPONIN DERIVATIVES FOR USE IN MEDICINE 审中-公开
公开(公告)号：WO2021260061A2
公开(公告)日：2021-12-30
申请号：PCT/EP2021/067239
申请日：2021-06-23
申请人： SAPREME TECHNOLOGIES B.V. , CHARITÉ - UNIVERSITÄTSMEDIZIN BERLIN
发明人： POSTEL, Ruben , HERMANS, Guy , FUCHS, Hendrik
IPC分类号： A61K47/54 , A61P43/00 , A61K47/68 , A61K47/549 , A61K47/6807
摘要： The invention relates to a Quillaja saponaria saponin derivative based on a saponin comprising a triterpene aglycone and a first saccharide chain and/or a second saccharide chain, and comprising: an aglycone core structure comprising an aldehyde group which has been derivatised; and/or the first saccharide chain wherein the first saccharide chain comprises a carboxyl group, which has been derivatised; and/or the second saccharide chain wherein the second saccharide chain comprises at least one acetoxy group which has been derivatised. The invention also relates to a first pharmaceutical composition comprising the saponin derivative of the invention. In addition, the invention relates to a pharmaceutical combination comprising the first pharmaceutical composition of the invention and a second pharmaceutical composition comprising any one or more of an antibody-toxin conjugate, a receptor-ligand – toxin conjugate, an antibody-drug conjugate, a receptor-ligand – drug conjugate, an antibody-oligonucleotide conjugate or a receptor-ligand – oligonucleotide conjugate. The invention also relates to the first pharmaceutical composition or the pharmaceutical combination of the invention, for use as a medicament, or use in the treatment or prophylaxis of a cancer, an infectious disease, viral infection, hypercholesterolemia, primary hyperoxaluria, haemophilia A, haemophilia B, alpha-1 antitrypsin related liver disease, acute hepatic porphyria, transthyretin-mediated amyloidosis, or an autoimmune disease. Furthermore, the invention relates to an in vitro or ex vivo method for transferring a molecule from outside a cell to inside said cell, comprising contacting said cell with the molecule and with a saponin derivative of the invention.

7. 发明申请

WO2021260054A2 SAPONIN DERIVATIVES FOR USE IN MEDICINE 审中-公开
公开(公告)号：WO2021260054A2
公开(公告)日：2021-12-30
申请号：PCT/EP2021/067227
申请日：2021-06-23
申请人： SAPREME TECHNOLOGIES B.V. , CHARITÉ - UNIVERSITÄTSMEDIZIN BERLIN
发明人： POSTEL, Ruben , HERMANS, Guy , FUCHS, Hendrik
IPC分类号： A61K47/54 , A61K47/68 , A61P43/00 , A61K31/00 , A61K36/36 , A61K38/1808 , A61K47/549 , A61K47/6807 , A61K47/6825 , A61K47/6849 , A61K47/6855 , C07H15/00 , C07J63/00
摘要： The invention relates to a saponin derivative based on a saponin comprising a triterpene aglycone and a first saccharide chain and/or a second saccharide chain, and comprising: an aglycone core structure comprising an aldehyde group which has been derivatised; and/or the first saccharide chain wherein the first saccharide chain comprises a carboxyl group, which has been derivatised; and/or the second saccharide chain wherein the second saccharide chain comprises at least one acetoxy group which has been derivatised. The invention also relates to a first pharmaceutical composition comprising the saponin derivative of the invention. In addition, the invention relates to a pharmaceutical combination comprising the first pharmaceutical composition of the invention and a second pharmaceutical composition comprising any one or more of an antibody-toxin conjugate, a receptor-ligand – toxin conjugate, an antibody-drug conjugate, a receptor-ligand – drug conjugate, an antibody-oligonucleotide conjugate or a receptor-ligand – oligonucleotide conjugate. The invention also relates to the first pharmaceutical composition or the pharmaceutical combination of the invention, for use as a medicament, or use in the treatment or prophylaxis of a cancer, an infectious disease, viral infection, hypercholesterolemia, primary hyperoxaluria, haemophilia A, haemophilia B, alpha-1 antitrypsin related liver disease, acute hepatic porphyria, transthyretin-mediated amyloidosis, or an auto-immune disease. Furthermore, the invention relates to an in vitro or ex vivo method for transferring a molecule from outside a cell to inside said cell, comprising contacting said cell with the molecule and with a saponin derivative of the invention.

8. 发明申请

WO2023279099A1 OLIGONUCLEOTIDE CONJUGATES TARGETED TO THE TRANSFERRIN RECEPTOR 审中-公开
公开(公告)号：WO2023279099A1
公开(公告)日：2023-01-05
申请号：PCT/US2022/073377
申请日：2022-07-01
申请人： DENALI THERAPEUTICS INC.
发明人： BARKER, Scarlett , DENNIS, Mark S. , DEVOS, Sarah L. , ESTRADA, Anthony A. , KARIOLIS, Mihalis S. , MAHON, Cathal S. , NILEWSKI, Lizanne G. , PARK, Joshua I. , SHAN, Lu , THAYER, Mai B. , TONG, Raymond Ka Hang , TRAN, Hai L. , WELLS, Robert C. , ZUCHERO, Joy Yu
IPC分类号： A61K47/68 , A61P25/28 , C07K16/28 , C07K16/40 , C12N15/00 , A61K2039/505 , A61K47/6807 , A61K47/6849 , C07K19/00 , C07K2317/24 , C07K2317/52 , C07K2317/55 , C07K2317/90 , C07K2319/00
摘要： Provided herein are conjugates comprising proteins that bind to a transferrin receptor and oligonucleotides that are capable of modulating the expression of a target gene or sequence, as well as methods of use thereof.

9. 发明申请

WO2022226420A2 AN FC GLYCAN REMODELING FOR SITE-SPECIFIC ANTIBODY CONJUGATION AND APPLICATIONS THEREOF 审中-公开
公开(公告)号：WO2022226420A2
公开(公告)日：2022-10-27
申请号：PCT/US2022/026213
申请日：2022-04-25
申请人： UNIVERSITY OF MARYLAND, COLLEGE PARK
发明人： WANG, Lai-Xi , ZHANG, Xiao
IPC分类号： A61K38/45 , C07K16/18 , C07K16/30 , C12N9/10 , C12Q1/48 , A61K47/6803 , A61K47/6807 , A61K47/6849 , A61K47/6855 , A61K47/6883 , A61K47/6889 , C07K16/00 , C12N9/00
摘要： The present disclosure provides a one-pot chemoenzymatic method for site-specific modification and conjugation of antibodies at their Fc glycan site to produce structurally well-defined antibody conjugates carrying defined drugs and other entities. The method is enabled by the discovery that certain endoglycosidases have the ability to both deglycosylate an antibody and to recognize selectively modified small disaccharide oxazolines for transglycosylation on antibodies without hydrolysis of the resulting products.

10. 发明申请

WO2022032175A1 METHODS FOR THE SYNTHESIS OF PROTEIN-DRUG CONJUGATES 审中-公开
公开(公告)号：WO2022032175A1
公开(公告)日：2022-02-10
申请号：PCT/US2021/045074
申请日：2021-08-06
申请人： CIDARA THERAPEUTICS, INC.
发明人： BORCHARDT, Allen , HUGHES, Robert, Michael
IPC分类号： A61K47/68 , A61K47/64 , A61K47/56 , A61P31/16 , A61K47/6803 , A61K47/6807
摘要： The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.

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