Patent
Pyrrolobenzodiazepines as key intermediates in the synthesis of dimeric cytotoxic pyrrolobenzodiazepines
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TLDR
In this article, a method of synthesis of compounds of formula (Ia) or (Ib): and salts, solvates, and chemically protected forms thereof, wherein the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3.Abstract:
Compounds and a method of synthesis of compounds of formula (Ia) or (Ib): and salts, solvates, and chemically protected forms thereof, wherein the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R2 and R3 are independently selected from -H, =O, =CH2, -CN, -R, OR, halo, =CH-R, O-SO2-R, CO2R and COR; R10 is a carbamate-based nitrogen protecting group; and R11 is an oxygen protecting group.read more
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Cysteine engineered antibodies and conjugates
TL;DR: In this paper, the authors presented a method for the design, preparation, screening, and selection of the cysteine engineered antibodies (ThioFab) by replacing one or more amino acids of a parent antibody with non-cross-linked, highly reactive cysteines amino acids.
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Pyrrolobenzodiazepines and conjugates thereof
Abstract: Conjugates and compounds for making conjugates which are PBD molecules linked via the N10 position are disclosed, along with the use of the conjugates for treating proliferative diseases, including cancer
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Cytotoxic agents comprising new tomaymycin derivatives and their therapeutic use
Laurence Gauzy,Robert Yongxin Zhao,Deng Yonghong,Wei Li,Herve Bouchard,Ravi V. J. Chari,Alain Commercon +6 more
TL;DR: The present invention is related to new tomaymycin of formula (I) derivatives, their process of preparation and their therapeutic uses as discussed by the authors, and their use in medical applications.
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Targeted pyrrolobenzodiazapine conjugates
TL;DR: In this article, a conjugate comprising PBDs conjugated to a targeting agent and methods of using such PBD was presented. But the methods of conjugation were not discussed.
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Pyrrolobenzodiazepines used to treat proliferative diseases
Philip Wilson Howard,Luke Masterson,Arnaud Tiberghien,Scott C. Jeffrey,Patrick J. Burke,Peter D. Senter +5 more
TL;DR: Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and conjugates of these compounds.
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Biodegradable, implantable drug delivery depots, and method for preparing and using the same
TL;DR: An implantable drug deliver depot comprising a hydrophilic poly(glutamic acid-co-ethyl glutamate) structure having one or more substances, e.g., drugs and/or diagnostic agents physically contained therein, is designed to release the substance or substances at predetermined rates and in predetermined sequence.
Patent
1,5-benzodiazepine derivatives
TL;DR: The 1,5-Benzodiazepine derivatives have an excellent gastrin and/or CCK-B receptor antagonism and are useful as remedies for gastric ulcer and gastrointestinal movement disorder as discussed by the authors.
Journal ArticleDOI
Design, synthesis, and evaluation of a novel pyrrolobenzodiazepine DNA-interactive agent with highly efficient cross-linking ability and potent cytotoxicity.
Stephen J. Gregson,Philip W. Howard,John A. Hartley,Natalie Brooks,Lesley J. Adams,Terence C. Jenkins,Lloyd R. Kelland,David E. Thurston +7 more
TL;DR: A novel sequence-selective pyrrolobenzodiazepine (PBD) dimer 5 (SJG-136) has been developed that comprises two C2-exo-methylene-substituted DC-81 (3) subunits tethered through their C8 positions via an inert propanedioxy linker that is a highly efficient minor groove interstrand DNA cross-linking agent that is 440-fold more potent than melphalan.
Journal ArticleDOI
Synthesis of DNA-interactive pyrrolo[2,1-c][1,4]benzodiazepines (PBDs).
TL;DR: A significant effort has been made to increase the base-pair span and sequence-selectivity of PBD molecules so that they might be used as gene-targeting agents in biological experiments and possibly as therapeutic agents.