2488-22-4

Upstream product

• 21691-50-9 Ala-OtBu 
• 28819-05-8 (S)-2-benzyloxycarbonylamino-propionic acid methyl ester 
• 26607-51-2 N-benzyloxycarbonyl-D-alanine 
• 13404-22-3 tert-butyl L-alaninate hydrochloride 
• 1142-20-7 N-Cbz-Ala 
• 1168-87-2 benzyloxycarbonylalanine p-nitrophenyl ester 

Relevant academic research and scientific papers

Effect of Linker Stereochemistry on the Activity of Indolinobenzodiazepine Containing Antibody-Drug Conjugates (ADCs)

Antibody-drug conjugates (ADCs) that incorporate potent indolinobenzodiazepine DNA alkylators as the payload component are currently undergoing clinical evaluation. In one ADC design, the payload molecules are linked to the antibody through a peptidase-labile l-Ala-l-Ala linker. In order to determine the role of amino acid stereochemistry on antitumor activity and tolerability, we incorporated l- and d-alanyl groups in the dipeptide, synthesized all four diastereomers, and prepared and tested the corresponding ADCs. Results of our preclinical evaluation showed that the l-Ala-l-Ala configuration provided the ADC with the highest therapeutic index (antitumor activity vs toxicity).

EFFICIENT PROCESS FOR PREPARING CELL-BINDING AGENT-CYTOTOXIC AGENT CONJUGATES

The present invention provides a novel method for preparing a cell-binding agent cytotoxic agent conjugate. The method comprises the step of reacting a cell-binding agent with a cytotoxic agent or a cytotoxic agent-linker compound having a reactive group

CYTOTOXIC BIS-BENZODIAZEPINE DERIVATIVES AND CONJUGATES THEREOF WITH CELL-BINDING AGENTS FOR INHIBITING ABNORMAL CELL GROWTH OR FOR TREATING PROLIFERATIVE DISEASES

The invention relates to benzodiazepine derivatives with antiproliferative activity and more specifically to benzodiazepine compounds of formulae (I), (II), (TI) and (T2). The invention also provides conjugates of the benzodiazepine compounds linked to a

Substrate-directed lewis-acid catalysis for peptide synthesis

A Lewis-acid-catalyzed method for the substrate-directed formation of peptide bonds has been developed, and this powerful approach is utilized for the new "remote" activation of carboxyl groups under solvent-free conditions. The presented method has the following advantages: (1) the high-yielding peptide synthesis uses a tantalum catalyst for any amino acids; (2) the reaction proceeds without any racemization; (3) the new substrate-directed chemical ligation using the titanium catalyst is applicable to convergent peptide synthesis. These advantages overcome some of the unresolved problems in classical peptide synthesis.

CYTOTOXIC BENZODIAZEPINE DERIVATIVES AND CONJUGATES THEREOF

The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formulae (I) and (II). The invention also provides conjugates of the benzodiazepine compounds linked to a

Stereocontrolled [11C]Alkylation of N-Terminal Glycine Schiff Bases To Obtain Dipeptides

The use of various quaternary ammonium salts as chiral phase-transfer catalysts allowed effective and stereoselective radiochemical [11C]alkylation to obtain functionalized dipeptides. We herein report a broadly applicable procedure for the asymmetric [11C]alkylation of dipeptides to give labeled N-terminal peptides by using different [11C]alkyl halides. Contended stereoselectivities of the reactions were observed by using 11C-labeled alkyl halides, [11C]methyl iodide and [11C]benzyl iodide, and diastereomeric ratios with different specialized catalysts of 95:5 and 90:10 were achieved, respectively. Accordingly, the straightforward synthesis of enantioenriched compounds should play a vital role in peptide-based radiopharmaceutical development and positron emission tomography imaging.

ANTI-CD 123 ANTIBODIES AND CONJUGATES AND DERIVATIVES THEREOF

The present disclosure generally relates to antibodies, antigen-binding fragments thereof, polypeptides, and immunoconjugates that bind to CD 123 antigen (the a chain of the interleukine 3 receptor, or IL-3Ra). The present disclosure also relates to methods of using such CD123-binding molecules for diagnosing and treating diseases, such as B-cell malignancies.

PHARMACEUTICAL FORMULATIONS AND METHODS OF USE THEREOF

This disclosure is directed to antibody-drug conjugates. More specifically, this disclosure is directed to compositions comprising (i) antibody-drug conjugates comprising benzodiazepines, and (ii) a small hydrophobic molecule, methods of treatment using the compositions, and methods of formulating the compositions. Furthermore, this disclosure is directed to methods of reducing reversible self-association in antibodies and in antibody-drug conjugates.

GCC-TARGETED ANTIBODY-DRUG CONJUGATES

This invention relates to antibody-drug conjugates capable of delivering cytotoxic compounds to cancers expressing the guanylyl cyclase C (GCC) transmembrane cell surface receptor.

CONJUGATES COMPRISING CELL-BINDING AGENTS AND CYTOTOXIC AGENTS

The invention relates to novel cell-binding agent-cytotoxic agent conjugates, wherein the cell-binding agent (CBA) is covalently linked to the cytotoxic agent through an aldehyde group obtained from oxidation of a 2-hydroxyethylamine moiety on the CBA. Th