Patent classifications
A61K47/68035
ASYMMETRIC CONJUGATE COMPOUNDS
The invention relates to compound of formula (I):
A-X.sub.1-L-X.sub.2B (I)
and salts, solvates and tautomers thereof, which are useful as medicaments, in particular as anti-proliferative agents and for use as a drug in an antibody-drug conjugate; wherein A is a group selected from:
##STR00001##
X.sub.1 and X.sub.2 are independently selected from O, S, NR.sub.28, CR.sub.28R.sub.29, CR.sub.28R.sub.29O, C(?O), C(?O)NR.sub.28, NR.sub.28C(?O), C(O)R.sup.AC(O)NH, C(O)R.sup.ANHC(O), C(O)NHR.sup.AC(O), NHC(O)R.sup.AC(O), NHC(O)R.sup.AC(O)NH, NHC(O)R.sup.ANHC(O), C(O)NHR.sup.ANHC(O), C(O)NHR.sup.AC(O)NH, OC(O) and C(O)O or is absent;
L is selected from an amino acid, a peptide chain having from 2 to 12 amino acids, a paraformaldehyde chain (OCH.sub.2).sub.1-24, a polyethylene glycol chain (OCH.sub.2CH.sub.2).sub.1-12 and (CH.sub.2).sub.mY.sup.6(CH.sub.2).sub.n wherein Y.sup.6 is selected from (CH.sub.2).sub.z and a group (L1) a group (L1) that is selected from arylene, monocyclic heteroarylene, monocyclic cycloalkylene, monocyclic cycloalkenylene and monocyclic heterocyclylene groups optionally substituted with up to three optional substituent groups; and
B is a polycyclic group selected from:
##STR00002##
Selective sulfonation of benzodiazepine derivatives
The invention relates to novel methods of preparing cell-binding agent-cytotoxic agent conjugates, wherein the cytotoxic agent is an imine-containing cytotoxic agent bearing a maleimide group. In some embodiments, the cell-binding agent (CBA) is covalently linked to the cytotoxic agent through an engineered Cys, such as an engineered Cys in the heavy chain CH3 domain, at a position corresponds to the EU/OU numbering position 442 (or C442) on an antibody CBA. The invention also provides conjugates prepared by the methods of the present invention, compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the conjugates of the invention.
COMBINATION OF CD33 ANTIBODY DRUG CONJUGATES WITH CHEMOTHERAPEUTIC AGENTS
This invention relates to treatment of cancer using a CD33 antibody drug conjugate in combination with chemotherapeutic agents.
PYRROLOBENZODIAZEPINE CONJUGATES
A conjugate of formula (I): L-(D.sup.L).sub.p (I) wherein L is a Ligand unit, D is a Drug Linker unit of formula (II) wherein p is an integer of from 1 to 20.
##STR00001##
COMBINATIONS OF CD33 ANTIBODY DRUG CONJUGATES WITH HYPOMETHYLATING AGENTS
This invention relates to treatment of cancer using a CD33 antibody drug conjugate in combination with hypomethylating agents.
METHODS OF PREVENTING METHIONINE OXIDATION IN IMMUNOCONJUGATES
The present invention generally relates to methods of preventing methionine oxidation in immunoconjugates. The present invention also relates to pharmaceutical compositions of immunoconjugates in which the amount of methionine oxidation is minimized.
ANTI-huLRRC15 ANTIBODY DRUG CONJUGATES AND METHODS FOR THEIR USE
The present disclosure provides antibodies, antibody binding fragments, and antibody drug conjugates that bind human LRRC15, their methods of making, and their uses to treat patients having cancer.
ANTI-huLRRC15 ANTIBODY DRUG CONJUGATES AND METHODS FOR THEIR USE
The present disclosure provides antibodies, antibody binding fragments, and antibody drug conjugates that bind human LRRC15, their methods of making, and their uses to treat patients having cancer.
ANTI-huLRRC15 ANTIBODY DRUG CONJUGATES AND METHODS FOR THEIR USE
The present disclosure provides antibodies, antibody binding fragments, and antibody drug conjugates that bind human LRRC15, their methods of making, and their uses to treat patients having cancer.
PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF
This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.