228266-37-3

Upstream product

• 186581-53-3 diazomethane 
• 228266-36-2 tert-butyl {(2S)-3-methyl-1-oxo-1-[(4S)-2-oxo-4-(propane-2-yl)-1,3-oxazolidine-3-yl]- 3-phenylbutane-2-yl}carbamate 
• 71-43-2 benzene 
• 228266-35-1 (4S)-3-[(2S)-2-azido-3-methyl-3-phenylbutanoyl]-4-(propane-2-yl)-1,3-oxazolidine-2-one 
• 228266-34-0 (4S)-3-(3-methyl-3-phenylbutanoyl)-4-(propane-2-yl)-1,3-oxazolidine-2-one 
• 1010-48-6 3-methyl-3-phenylbutanoic acid 
• 541-47-9 3-Methylbutenoic acid 

Downstream Products

• 228266-38-4 N-(tert-butoxycarbonyl)-N,β,β-trimethyl-L-phenylalanine 

Relevant academic research and scientific papers

The antibody-drug conjugate hemiasterlin derivatives and their pharmaceutically (by machine translation)

[Problem] to give one specific target cell cytotoxic, normal cells to the cytotoxic is suppressed, the antibody-drug conjugate medicine hemiasterlin derivatives. (2) Formula [a]:[In the formula, mAb antibody expressed, q is 1 - 8 represents an integer of, h are 1 - 5 represents an integer of, g is an alanine residue (Ala) to represent, g is 1 - 4 represents an integer of, Y is a single bond or a formula (Y-a 1) is represented by the group, Z is formula (Z-a 1), equation (Z-a 2), equation (Z-a 3), formula (Z-a 4), formula (Z-a 5), type (Z-a 6), formula (Za-a 1), equation (Za-in 2), equation (Za-a 3), formula (Za-a 4), formula (Za-a 5), type (Za d 6), formula (Za-a 7), type (Za-in 8), or a group represented by formula (Za-a 10) (Za-a 9) formula a] is expressed by, antibody-drug conjugate or its pharmaceutically acceptable salt containing a drug. [Drawing] no (by machine translation)

MEDICINE CONTAINING ANTIBODY DRUG CONJUGATE CONTAINING HEMIASTERLIN DERIVATIVE

PROBLEM TO BE SOLVED: To provide medicines containing an antibody drug conjugate containing a hemiasterlin derivative, in which specific cytotoxicity to target cells is given, while cytotoxicity to normal cells is suppressed. SOLUTION: Provided is a medicine represented by formula (2-1), and containing an antibody drug conjugate or a pharmaceutically acceptable salt thereof [where, mAb represents an antibody, q represents an integer from 1 to 8, b represents an integer from 1 to 5, Z is a group represented by formula (Z-1), formula (Z-2), formula (Z-3), formula (Za-1), formula (Za-2), formula (Za-3), formula (Za-4), or formula (Za-5)]. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT

HEMIASTERLIN ANALOGS

This invention provides analogs of hemiasterlin, methods of synthesis of the analogs and use of the analogs as a cytotoxic anti-mitotic agents.

Conjugates of ligand linker and cytotoxic agent and related composition and methods of use

A conjugate comprising a ligand, a linker, and a cytotoxic agent, in which the linker is FALA, VLALA, ALAL, ALALA, ChaLALA, ChaChaLAL, NalChaLAL or NalLALA; a composition thereof; a method of delivering a cytotoxic agent in a cell-specific manner; and a method of treating cancer in a mammal.