公开(公告)号：WO2022218973A2

公开(公告)日：2022-10-20

申请号：PCT/EP2022/059733

申请日：2022-04-12

申请人： MEDIMMUNE LIMITED

发明人： HOWARD, Philip Wilson ,  MASTERSON, Luke ,  TIBERGHIEN, Arnaud Charles

IPC分类号： A61K47/68 ,  A61P35/00 ,  C07D487/04 ,  A61K47/6803 ,  A61K47/6855

摘要： A conjugate of formula (I) wherein Ab is a modified antibody having at least one free conjugation site on each heavy chain; D represents either group D1 or D2. D' represents either group D'1 or D'2.

公开(公告)号：WO2022005545A1

公开(公告)日：2022-01-06

申请号：PCT/US2021/024797

申请日：2021-03-30

申请人： COHEN, David, I.

发明人： COHEN, David, I.

IPC分类号： A61K33/30 ,  A61K31/00 ,  A61K33/32 ,  A61K33/26 ,  A61K33/34 ,  A61K45/06 ,  A61K38/1729 ,  A61K39/39 ,  A61K47/52 ,  A61K47/6811 ,  A61K47/6841 ,  A61K47/6855 ,  A61P31/14 ,  A61P31/16 ,  A61P35/00

摘要： The present invention creates drugs that are both zinc carriers and ionophores, thus capable of delivering zinc intracellularly and in so doing inhibiting COVlD-19 infection. The drug inventions further attack SARS sequelae of COV1D19 infection, such as development of bacterial pneumonias, most prevalent in the elderly, which are attributable to intrapulmonary zinc deficiency. As such, they could be important primary therapies for SARS. The zinc/ionophore porters can be delivered alone, or upon coupling to other antivirals.

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.

公开(公告)号：WO2022233718A2

公开(公告)日：2022-11-10

申请号：PCT/EP2022/061430

申请日：2022-04-29

申请人： MERCK PATENT GMBH

发明人： JAEGER, Sebastian ,  SCHROETER, Christian

IPC分类号： A61K47/68 ,  A61K49/00 ,  A61P35/00 ,  C07K16/32 ,  A61K47/6803 ,  A61K47/6855 ,  A61K47/6889 ,  A61K49/0041 ,  A61K49/0058 ,  C07K2317/52 ,  C07K2317/73 ,  C07K2317/77 ,  C07K2317/92 ,  C07K2317/94

摘要： The invention relates to HER2 targeting Fc antigen binding fragment-drug conjugates (HER2 Fcab-drug conjugates) and the use of the HER2 Fcab-drug conjugates of the present invention for the treatment and/or prevention of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such HER2 Fcab-drug conjugates. Further, the invention relates to HER2 Fcab-label conjugates and diagnostic compositions containing such HER2 Fcab-label conjugates.

公开(公告)号：WO2021260579A1

公开(公告)日：2021-12-30

申请号：PCT/IB2021/055548

申请日：2021-06-23

申请人： ASTRAZENECA UK LIMITED ,  DAIICHI SANKYO COMPANY, LIMITED

发明人： METTETAL II, Jerome Thomas ,  DURANT, Stephen Thomas ,  ASTANEH, Azadeh Cheraghchi Bashi ,  LAU, Alan Yin Kai ,  WALLEZ, Yann

IPC分类号： A61K47/68 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  A61K47/6803 ,  A61K47/6855 ,  A61K47/6889 ,  C07K16/32 ,  C07K2317/24

摘要： A pharmaceutical product for administration of an anti HER2 antibody-drug conjugate in combination with an ATR inhibitor is provided. The anti-HER2 antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an antibody) is conjugated to an anti-HER2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the ATR inhibitor are administered in combination to a subject: Formula (I):

公开(公告)号：WO2021142199A1

公开(公告)日：2021-07-15

申请号：PCT/US2021/012611

申请日：2021-01-08

申请人： MERSANA THERAPEUTICS, INC.

发明人： LOWINGER, Timothy B. ,  DAMELIN, Marc I. ,  TOADER, Dorin

IPC分类号： A61K47/68 ,  A61P35/00 ,  C07K16/30 ,  A61K2039/505 ,  A61K38/07 ,  A61K47/545 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6843 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6869 ,  C07K16/3069 ,  C07K16/32 ,  C07K2317/92

摘要： The present disclosure relates generally to antibody-drug conjugates comprising peptide-containing linkers and to methods of using these conjugates as therapeutics and/or diagnostics. Also disclosed herein are peptide-containing scaffolds useful to conjugate with a targeting moiety (e.g., an antibody), a drug, or both to produce the antibody-drug conjugates.

公开(公告)号：WO2021124210A1

公开(公告)日：2021-06-24

申请号：PCT/IB2020/062123

申请日：2020-12-17

申请人： PFIZER INC.

发明人： LEUNG, Abraham ,  SUNG, Matthew

IPC分类号： A61K47/68 ,  A61P35/00 ,  A61K47/6803 ,  A61K47/6855 ,  A61K47/6857 ,  A61K47/6863 ,  A61K47/6889

摘要： The present disclosure provides for dosing regimens for the treatment of patients with cancer, particularly a HER2-expressing cancer, with an anti-HER2 antibody-drug conjugate (ADC). The present disclosure further provides for methods for the treatment of patients with cancer in which an anti-HER2 ADC is administered. In one embodiment, the anti-HER2 ADC is T(kK183C+K290C)-vc0101 (PF-06804103), in which the antibody T(kK183C+K290C) is linked to the auristatin drug 2-methylalanyl-N-[(3R,4S,5S)-3-methoxy-l-{(2S)-2-[(1R,2R) -1-methoxy-2-methyl-3-oxo-3-{[(1S)-2-phenyl-1-(1,3-thiazol-2-yl) ethyl]amino}propyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N- methyl-L-valinamide (also known as "0101") via the cleavable linker maleimidocaproyl-valine-citrulline-p-aminobenzyloxycarbonyl (also known as "vc").

公开(公告)号：WO2021123506A1

公开(公告)日：2021-06-24

申请号：PCT/FI2020/050857

申请日：2020-12-18

申请人： GLYKOS BIOMEDICAL OY

发明人： SATOMAA, Tero ,  SAARINEN, Juhani ,  HELIN, Jari ,  AITIO, Olli ,  PYNNÖNEN, Henna

IPC分类号： A61K47/68 ,  A61P35/00 ,  A61K47/6803 ,  A61K47/6855

摘要： A conjugate is disclosed. The conjugate may be represented by Formula I: [D-O-L]n-T Formula I wherein D is a payload molecule; O is an oxygen atom of said payload molecule; T is a targeting unit capable of binding a target molecule, cell and/or tissue; and n is at least 1.

公开(公告)号：WO2023044016A2

公开(公告)日：2023-03-23

申请号：PCT/US2022/043820

申请日：2022-09-16

申请人： CSPC DOPHEN CORPORATION

发明人： ZHANG, Wen ,  SUN, Zhaopeng ,  HU, Xixin ,  HUI, Xiwu ,  DAN, Mo ,  YUAN, Can ,  LV, Lu

IPC分类号： C07D487/04 ,  A61K31/437 ,  A61P35/00 ,  A61K47/6803 ,  A61K47/6855 ,  C07K16/46

摘要： The present disclosure provides, in some embodiments, antibody-immune stimulant conjugates for cancer immunotherapy. Methods for making and using the antibody-immune stimulant conjugates are also provided herein.

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.