- CROSS-LINKED PYRROLOBENZODIAZEPINE DIMER (PBD) DERIVATIVE AND ITS CONJUGATES
-
A novel cross-linked cytotoxic agents, pyrrolobenzo-diazepine dimer (PBD) derivatives, and their conjugates to a cell-binding molecule, a method for preparation of the conjugates and the therapeutic use of the conjugates.
- -
-
Page/Page column 128
(2020/01/31)
-
- CONJUGATION LINKERS CONTAINING 2,3-DIAMINOSUCCINYL GROUP
-
Provided is a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (adual-linker) containing a 2, 3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.
- -
-
Page/Page column 185
(2020/05/19)
-
- A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
-
The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
- -
-
Paragraph 000353; 000354
(2021/03/02)
-
- A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
-
The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
- -
-
Page/Page column 11; 179
(2019/07/17)
-
- CONJUGATION OF A CYTOTOXIC DRUG WITH BIS-LINKAGE
-
What provided is the conjugation of cytotoxic to a cell-binding molecule with a bis-linker(dual-linker) as shown in Formula (I). It provides bis-linkage methods of making a conjugate of a cytotoxic drug molecule to a cell-binding agent in a specific manner. It also relates to application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease.
- -
-
Paragraph 0529-0531
(2020/01/08)
-
- CONJUGATION LINKERS, CELL BINDING MOLECULE-DRUG CONJUGATES CONTAINING THE LIKERS, METHODS OF MAKING AND USES SUCH CONJUGATES WITH THE LINKERS
-
The present invention relates to linkers having a group of propiolyl, substituted acryl (acryloyl), or disubstituted propanoyl, and using such linkers for the conjugation of compounds, in particular, cytotoxic agents to a cell-binding molecule.
- -
-
Page/Page column 151; 152
(2018/05/27)
-
- DERIVATIVES OF AMANITA TOXINS AND THEIR CONJUGATION TO A CELL BINDING MOLECULE
-
Derivatives of Amernita toxins of Formula (I), wherein, formula (a) R 1, R 2, R 3, R 4, R 5, R 6, R 7, R 8, R 9, R 10, X, L, m, n and Q are defined herein. The preparation of the derivatives. The therapeutic use of the derivatives in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.
- -
-
Page/Page column 143
(2017/04/11)
-
- SPECIFIC CONJUGATION LINKERS, SPECIFIC IMMUNOCONJUGATES THEREOF, METHODS OF MAKING AND USES SUCH CONJUGATES THEREOF
-
The present invention relates to novel linkers containing a 2,3-disubstituted succinic group, or 2-monosubstituted, or 2,3-disubstituted fumaric or maleic (trans (E)- or cis (Z)- butenedioic), or acetylenedicarboxyl group for conjugation of a cytotoxic agent, and/or one or more different functional molecules per linker to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule specifically. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.
- -
-
Page/Page column 103-104
(2016/05/24)
-
- Scalable and cost-effective synthesis of a linker for bioconjugation with a peptide and a monoclonal antibody
-
An efficient, scalable, and cost-effective synthesis of a linker employed in a bioconjugation process with a peptide and a monoclonal antibody is presented. Several routes were investigated that resulted in the identification of a short synthesis to a key acid intermediate from inexpensive and readily available starting materials. The final coupling of this acid with an aniline to afford the desired linker has been optimized to produce multi-gram quantities of material for clinical studies. The very limited purifications needed for both intermediates and final product make this route amenable to scale. Georg Thieme Verlag Stuttgart New York.
- Magano, Javier,Conway, Brian G.,Farrand, Douglas,Lovdahl, Michael,Maloney, Mark T.,Pozzo, Mark J.,Teixeira, John J.,Rizzo, John,Tumelty, David
-
p. 1399 - 1406
(2014/06/09)
-
- Design and synthesis of novel photoaffinity probes for study of the target proteins of oleanolic acid
-
To explore the molecular mechanisms of oleanolic acid, two novel photoaffinity probes were synthesized based on the structure-activity relationship reported previously. Their potency were evaluated in an enzyme inhibition assay against rabbit muscle glycogen phosphorylase a (RMGPa), a known target protein of oleanolic acid. The inhibitory activity of probe 2 was only about two-fold less potent than the mother compound oleanolic acid. The photoaffinity labeling experiments were also performed and two proteins were specifically tagged by probe 2. The results suggest that the synthesized probes could be used as powerful tools to isolate and identify the target proteins of oleanolic acid.
- Zhang, Liying,Zhang, Yingxia,Dong, Jizhe,Liu, Jun,Zhang, Luyong,Sun, Hongbin
-
supporting information; experimental part
p. 1036 - 1039
(2012/03/26)
-
- Gadolinium-doped LipoCEST agents: A potential novel class of dual 1H-MRI probes
-
A novel class of paramagnetic liposome-based systems acting as dual T 1 and CEST 1H-MRI contrast agents is described. The vesicles contain a shift reagent in the aqueous core and a Gd-complex on the external surface conjugated throug
- Terreno, Enzo,Boffa, Cinzia,Menchise, Valeria,Fedeli, Franco,Carrera, Carla,Castelli, Daniela Delli,Digilio, Giuseppe,Aime, Silvio
-
supporting information; experimental part
p. 4667 - 4669
(2011/06/20)
-
- Synthesis of N-propynyl analogues of peptide nucleic acid (PNA) monomers and their use in the click reaction to prepare N-functionalized PNAs
-
Application of the click reaction for coupling a 2-(2-aminoethoxy)ethoxy (AEE) function to thyminyl, cytosinyl and adeninyl peptide nucleic acid (PNA) monomer analogues bearing a N-propynyl group, in place of the original N-2-aminoethyl moiety, has been explored. The N-propynyl PNA analogues were prepared from glycine ethyl ester hydrochloride and the structure of the thyminyl derivative was confirmed by X-ray diffraction. These monomers were employed in click reactions with Boc-protected AEE azide to afford the corresponding triazolyl-linked PNA-AEE conjugates in yields ranging from 64 to 76%. [1,4]-Regiochemistry was verified from a NOESY correlation experiment.
- Howarth, Nicola M.,Ricci, Jennyfer
-
scheme or table
p. 9588 - 9594
(2011/12/14)
-
- Membrane receptor probes: Solid-phase synthesis of biotin-Asp-PEG-arvanil derivatives
-
(Chemical Equation Presented) A modular, flexible solid-phase synthetic route for the preparation of biotinylated cross-linking probes of membrane receptors is described. The route utilizes an orthogonal protection strategy employing a Pd[0] cleavable all
- Visintin, Cristina,Aliev, Abil E.,Riddall, Dieter,Baker, David,Okuyama, Masahiro,Hoi, Pui Man,Hiley, Robin,Selwood, David L.
-
p. 1699 - 1702
(2007/10/03)
-
- Macrocyclic polymer complexing agents, their complexes, process for their production and pharmaceutical agents containing these compounds
-
Polymeric compounds of general formula I in which M stands for the radical of a macrocyclic complexing agent, A stands for a backbone molecule, which shows a deficit of n amino groups, n hydroxy groups or n carboxy groups, n stands for the numbers 1 to 40
- -
-
-