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1. 发明申请

WO2022164316A1 SEMICARBAZONE-BASED SAPONIN CONJUGATE 审中-公开
公开(公告)号：WO2022164316A1
公开(公告)日：2022-08-04
申请号：PCT/NL2022/050039
申请日：2022-01-26
申请人： SAPREME TECHNOLOGIES B.V.
发明人： HERMANS, Guy , POSTEL, Ruben , VAN DE LANGEMHEEN, Helmus , ASADIAN BIRJAND, Mazdak
IPC分类号： A61K47/54 , A61K47/55 , A61P35/00 , C07H3/00
摘要： The invention relates to a saponin conjugate comprising a saponin derivative based on a saponin comprising a triterpene aglycone and at least one of a first saccharide chain and a second saccharide chain linked to the aglycone core structure, wherein the saponin derivative comprises an aglycone core structure comprising an aldehyde functional group which aldehyde functional group has been transformed to a semicarbazone functional group, the saponin conjugate further comprising a proteinaceous molecule capable of binding to a cell-surface molecule. The invention also relates to a composition comprising the saponin conjugate. In addition, the invention relates to a pharmaceutical combination comprising said composition comprising the saponin conjugate and a pharmaceutical composition comprising for example an ADC or an antibody-oligonucleotide conjugate (AOC). The invention also relates to a pharmaceutical composition comprising the saponin conjugate and comprising for example an ADC or an AOC. The invention also relates to the pharmaceutical combination or pharmaceutical composition, for use as a medicament. The invention also relates to the saponin conjugate comprising the saponin derivative, a proteinaceous molecule capable of binding to a cell surface molecule (endocytic receptor), and further comprising an effector moiety such as an oligonucleotide. The invention also relates to an in vitro or ex vivo method for transferring a molecule from outside a cell to inside said cell.

2. 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.

3. 发明申请

WO2021259925A1 CONJUGATE OF SAPONIN AND SINGLE-DOMAIN ANTIBODY, PHARMACEUTICAL COMPOSITION COMPRISING SAID CONJUGATE, THERAPEUTIC USE THEREOF 审中-公开
公开(公告)号：WO2021259925A1
公开(公告)日：2021-12-30
申请号：PCT/EP2021/066985
申请日：2021-06-22
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 , A61K47/55 , A61K47/59 , A61K47/64 , A61K47/549 , A61K47/595 , A61K47/6415 , A61K47/643
摘要： The invention relates to a conjugate for transferring a saponin of the monodesmosidic triterpene glycoside type or of the bidesmosidic triterpene glycoside type from outside a cell into said cell, the conjugate comprising a single-domain antibody, capable of binding to said cell, covalently bound to a saponin. The invention also relates to a pharmaceutical combination comprising a first pharmaceutical composition comprising the conjugate of the invention and a second pharmaceutical composition comprising an active pharmaceutical ingredient, or to a pharmaceutical composition comprising the conjugate of the invention and an active pharmaceutical ingredient. In addition, the invention relates to the pharmaceutical combination of the invention or the pharmaceutical composition of the invention, for use as a medicament, or for use in the treatment or the prophylaxis of a cancer, an auto-immune disease, an infection, an enzyme deficiency, a gene defect. 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 the application of the conjugate of the invention. Finally, the invention relates to a kit of parts, comprising the pharmaceutical combination of the invention or the pharmaceutical composition of the invention, or the conjugate of the invention, and instructions for use thereof.

4. 发明申请

WO2021261995A1 COMBINATION OF AN ANTIBODY-DRUG CONJUGATE AND AN ANTIBODY-SAPONIN CONJUGATE 审中-公开
公开(公告)号：WO2021261995A1
公开(公告)日：2021-12-30
申请号：PCT/NL2021/050391
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 , A61K47/55 , A61P35/00 , A61K45/06 , A61K47/68 , A61K47/549 , A61K47/554 , A61K47/6845 , A61K47/6855
摘要： The invention relates to a therapeutic combination comprising: (a) a first pharmaceutical composition comprising a conjugate comprising a first binding molecule for binding to a first binding site of a cell- surface molecule and the conjugate comprising a saponin bound to said first binding molecule, wherein the saponin is a triterpene glycoside; and (b) a second pharmaceutical composition comprising a conjugate comprising a second binding molecule different from the first binding molecule, the second binding molecule comprising a second binding region different from the first binding region, for binding to a second binding site of said cell-surface molecule different from the first binding site of said cell- surface molecule, and the conjugate comprising an effector molecule covalently bound to said second binding molecule. The invention also relates to a pharmaceutical composition comprising said two conjugates. In addition, the invention relates to the pharmaceutical combination or the pharmaceutical composition of the invention for use as a medicament. Furthermore, the invention relates to the pharmaceutical combination or the pharmaceutical composition of the invention, for use in the treatment or prevention of a cancer, an autoimmune disease, a disease relating to (over)expression of a protein, a disease relating to an aberrant cell such as a tumor cell or a diseased liver cell, a disease relating to a mutant gene, a disease relating to a gene defect, a disease relating to a mutant protein, a disease relating to absence of a (functional) protein, a disease relating to a (functional) protein deficiency.

5. 发明申请

WO2021014026A2 BIOACTIVE SAPONIN LINKED TO A FUNCTIONAL MOIETY 审中-公开
公开(公告)号：WO2021014026A2
公开(公告)日：2021-01-28
申请号：PCT/EP2020/071145
申请日：2020-07-27
申请人： SAPREME TECHNOLOGIES B.V. , CHARITÉ - UNIVERSITÄTSMEDIZIN BERLIN
发明人： FUCHS, Hendrik , POSTEL, Ruben
IPC分类号： A61K47/54 , A61K47/55 , A61K47/59 , A61K47/64 , A61K47/549 , A61K47/593 , A61K47/595 , A61K47/60 , A61K47/6415 , A61K47/642 , A61K47/643 , A61K47/6807 , A61K47/6825 , A61K47/6849 , A61K47/6855 , A61K47/6885 , A61K47/6889
摘要： The invention relates to an endosomal and/or lysosomal escape enhancing conjugate comprising a saponin optionally linked to a targeting molecule such as an antibody and optionally linked to an effector molecule such as a toxinor an oligonucleotide. The invention also relates to a therapeutic combination of such an endosomal and/or lysosomal escape enhancing conjugate of the invention and a functionalized binding molecule comprising an effector molecule, wherein the endosomal and/or lysosomal escape enhancing conjugate comprises an enhancer of said effector molecule, i.e. a saponin. In particular the invention relates to such a therapeutic combination for use as a medicament, in particular for use in the treatment of a tumour. The invention further relates to a method of treating cancer or an autoimmune disease by administering an effective dose of the therapeutic combination to a patient in need thereof or by administering an effective dose of the endosomal and/or lysosomal escape enhancing conjugate comprising a saponin complexed with a targeting molecule such as an immunoglobulin specific for a tumor-cell surface molecule and complexed with an effector molecule, to a patient in need thereof. The invention also relates to a functionalized saponin with endosomal/lysosomal escape enhancing activity.

6. 发明申请

WO2021014019A1 SAPONIN DERIVATIVES WITH IMPROVED THERAPEUTIC WINDOW 审中-公开
公开(公告)号：WO2021014019A1
公开(公告)日：2021-01-28
申请号：PCT/EP2020/071045
申请日：2020-07-24
申请人： SAPREME TECHNOLOGIES B.V. , CHARITÉ - UNIVERSITÄTSMEDIZIN BERLIN
发明人： POSTEL, Ruben , HERMANS, Guy , FUCHS, Hendrik
IPC分类号： A61K47/55 , A61K47/59 , A61K47/64 , A61K47/54 , A61K31/7034
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.

7. 发明申请

WO2020126620A2 IMPROVED ANTIBODY-OLIGONUCLEOTIDE CONJUGATE 审中-公开
公开(公告)号：WO2020126620A2
公开(公告)日：2020-06-25
申请号：PCT/EP2019/084242
申请日：2019-12-09
申请人： SAPREME TECHNOLOGIES B.V. , CHARITÉ - UNIVERSITÄTSMEDIZIN BERLIN
发明人： POSTEL, Ruben , FUCHS, Hendrik
IPC分类号： A61K47/59 , A61K47/64 , A61K47/68 , A61P35/00
摘要： The invention relates to a ligand-effector moiety provided with at least one saponin and antibody-effector moiety provided with at least one saponin. An aspect of the invention is a composition comprising the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention. The invention also relates to an antibody-drug conjugate comprising covalently linked saponin and to an antibody-oligonucleotide conjugate comprising covalently linked saponin. An aspect of the invention relates to a pharmaceutical composition comprising the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention, and optionally further comprising a pharmaceutically acceptable excipient. The invention also relates to the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin, for use as a medicament. The invention also relates to the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention for use in the treatment or prophylaxis of a cancer.

8. 发明申请

WO2022265493A1 CONJUGATE OF SAPONIN, OLIGONUCLEOTIDE AND GALNAC 审中-公开
公开(公告)号：WO2022265493A1
公开(公告)日：2022-12-22
申请号：PCT/NL2022/050127
申请日：2022-03-08
申请人： SAPREME TECHNOLOGIES B.V.
发明人： POSTEL, Ruben , HERMANS, Guy , VAN DE LANGEMHEEN, Helmus , ASADIAN BIRJAND, Mazdak
IPC分类号： A61K47/54 , A61K47/55 , A61P35/00 , A61K47/549
摘要： The invention relates to a conjugate comprising a saponin covalently linked to a ligand for ASGPR, the ligand comprising at least one GalNAc moiety, and comprising an oligonucleotide covalently linked to the saponin and the ligand for ASGPR. In addition, the invention relates to a pharmaceutical composition comprising the conjugate of the invention. Furthermore, the invention relates to a pharmaceutical composition of the invention for use as a medicament. The invention also relates to a pharmaceutical composition of the invention for use in the treatment or prophylaxis of a disease or health problem in which an expression product is involved of for example genes: apoB, HSP17, TTR, PCSK9, ALAS1, AT3, GO, CC5, X gene of HBV, S gene of HBV, AAT and LDH, and for use in the treatment or prophylaxis of for example a cancer, an infectious disease, a viral infection, hypercholesterolemia, primary hyperoxaluria, haemophilia A, haemophilia B, AAT related liver disease, acute hepatic porphyria, TTR amyloidosis, complement-mediated disease, hepatitis B infection, or an auto-immune disease. The invention also relates to an in vitro or ex vivo method for transferring the oligonucleotide conjugate of the invention from outside a cell to inside said cell.

9. 发明申请

WO2022055352A1 SEMICARBAZONE-BASED SAPONIN CONJUGATE 审中-公开
公开(公告)号：WO2022055352A1
公开(公告)日：2022-03-17
申请号：PCT/NL2021/050550
申请日：2021-09-09
申请人： SAPREME TECHNOLOGIES B.V.
发明人： HERMANS, Guy , POSTEL, Ruben , VAN DE LANGEMHEEN, Helmus , ASADIAN BIRJAND, Mazdak
IPC分类号： A61K47/54 , A61K47/55 , A61P35/00 , C07H3/00
摘要： The invention relates to a saponin derivative based on a saponin comprising a triterpene aglycone and at least one of a first saccharide chain and a second saccharide chain linked to the aglycone core structure, wherein the saponin derivative comprises an aglycone core structure comprising an aldehyde functional group which has been transformed to a semicarbazone functional group. 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 a GalNAc-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 or an auto-immune disease, a cardiovascular disease or hypercholesterolemia, or in a method for lowering LDL-cholesterol in the circulation of a subject. The invention also relates to a saponin conjugate comprising a proteinaceous molecule, capable of binding to a cell, and optionally comprising an effector moiety such as an oligonucleotide. The invention also relates to a saponin conjugate comprising GalNAc and an oligonucleotide.

10. 发明申请

WO2021259944A1 CONJUGATE OF A SINGLE DOMAIN ANTIBODY, A SAPONIN AND AN EFFECTOR MOLECULE, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, THERAPEUTIC USE OF SAID PHARMACEUTICAL COMPOSITION 审中-公开
公开(公告)号：WO2021259944A1
公开(公告)日：2021-12-30
申请号：PCT/EP2021/067030
申请日：2021-06-22
申请人： SAPREME TECHNOLOGIES B.V. , CHARITÉ - UNIVERSITÄTSMEDIZIN BERLIN
发明人： POSTEL, Ruben , HERMANS, Guy , FUCHS, Hendrik
IPC分类号： A61K47/55 , A61K47/59 , A61K47/64 , A61K47/54 , A61K47/549 , A61K47/595 , A61K47/6415 , A61K47/643
摘要： The invention relates to a conjugate for transferring an effector molecule from outside a cell into said cell, the conjugate comprising at least one effector molecule to be transferred into the cell, at least one saponin of the mono-desmosidic triterpene glycoside type or the bi-desmosidic triterpene glycoside type, and at least one single-domain antibody (sdAb), covalently bound to each other, wherein the sdAb is capable of binding to a cell-surface molecule of said cell. The invention also relates to a pharmaceutical composition comprising the conjugate of the invention. Furthermore, the invention relates to a pharmaceutical composition of the invention, for use as a medicament. In addition, the invention relates to a pharmaceutical composition of the invention, for use in the treatment or the prophylaxis of any one or more of: a cancer, an auto-immune disease such as rheumatoid arthritis, an enzyme deficiency, a disease related to an enzyme deficiency, a gene defect, a disease relating to a gene defect, an infection such as a viral infection, hypercholesterolemia, primary hyperoxaluria, haemophilia A, haemophilia B, alpha-1 antitrypsin related liver disease, acute hepatic porphyria, an amyloidosis and transthyretin- mediated amyloidosis. The invention also relates to an in vitro or ex vivo method for transferring the conjugate from outside a cell to inside said cell or for transferring the effector molecule comprised by the conjugate of the invention from outside a cell to inside said cell, preferably to the cytosol of said cell.

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