500229-32-3

Upstream product

• 71-43-2 benzene 
• 140195-91-1 ethyl N-benzoyl-L-phenylalanyl-L-alaninate 
• 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 
• 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 
• 777057-10-0 (E)-(S)-4-{[(S)-2-((S)-2-Amino-3-methyl-3-phenyl-butyrylamino)-3,3-dimethyl-butyryl]-methyl-amino}-2,5-dimethyl-hex-2-enoic acid ethyl ester 

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

Pyruvamide Compounds as Inhibitors of Dust Mite Group 1 Peptidase Allergen and Their Use

The present invention pertains generally to the field of therapeutic compounds and more specifically to certain pyruvamide compounds of the formula (X) (for convenience, collectively referred to herein as “PVA compounds”), which, inter alia, inhibit a dust mite Group 1 peptidase allergen (e.g., Der p 1, Der f 1, Eur m 1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit a dust mite Group 1 peptidase allergen, and in the treatment of diseases and disorders that are mediated by a dust mite Group 1 peptidase allergen; that are ameliorated by the inhibition of a dust mite Group 1 peptidase allergen; asthma; rhinitis; allergic conjunctivitis; atopic dermatitis; an allergic condition which is triggered by dust mites; an allergic condition which is triggered by a dust mite Group 1 peptidase allergen; and canine atopy.

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.

Synthesis and antimitotic/cytotoxic activity of hemiasterlin analogues

The antimitotic sponge tripeptide hemiasterlin (1) and a number of structural analogues have been synthesized and evaluated in cell-based assays for both cytotoxic and antimitotic activity in order to explore the SAR for this promising anticancer drug lead. One synthetic analogue, SPA110 (8), showed more potent in vitro cytotoxicty and antimitotic activity than the natural product hemiasterlin (1), and consequently it has been subjected to thorough preclinical evaluation and targeted for clinical evaluation. The details of the synthesis of hemiasterlin (1) and the analogues and a discussion of how their biological activities vary with their structures are presented in this paper.