1310680-18-2

Upstream product

• 66899-02-3 4,4-dimethylpyrrolidin-2-one 
• 898552-72-2 ethyl 3,3-dimethyl-4-aminobutanoate hydrochloride 
• 130912-54-8 3,3-dimethyl-4-nitro-butyric acid ethyl ester 
• 638-10-8 ethyl 3-methylbut-2-enoate 
• 195447-82-6 4-amino-3,3-dimethylbutanoic acid ethyl ester 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 1609075-11-7 4-nitrophenyl 4-[((tert-butoxy)carbonyl)amino]-3,3-dimethylbutanoate 

Relevant academic research and scientific papers

Structural insight into hybrid peptide ?-helices

Unique ?-helical organizations (11-helices) from β,γ-hybrid peptides composed of chiral β3-amino acids along with achiral 3,3- or 4,4-dimethyl substituted γ-amino acids are disclosed.

Ambidextrous α,γ-Hybrid Peptide Foldamers

Molecular chirality is ubiquitous in nature. The natural biopolymers, proteins and DNA, preferred a right-handed helical bias due to the inherent stereochemistry of the monomer building blocks. Here, we are reporting a rare co-existence of left- and right-handed helical conformations and helix-terminating property at the C-terminus within a single molecule of α,γ-hybrid peptide foldamers composed of achiral Aib (α-aminoisobutyric acid) and 3,3-dimethyl-substituted γ-amino acid (Adb; 4-amino-3,3-dimethylbutanoic acid). At the molecular level, the left- and right-handed helical screw sense of α,γ-hybrid peptides are representing a macroscopic tendril perversion. The pronounced helix-terminating behaviour of C-terminal Adb residues was further explored to design helix–Schellman loop mimetics and to study their conformations in solution and single crystals. The stereochemical constraints of dialkyl substitutions on γ-amino acids showed a marked impact on the folding behaviour of α,γ-hybrid peptides.

AMINO PYRAZOLONE DERIVATIVE HAVING CONDENSED RING STRUCTURE

PROBLEM TO BE SOLVED: To provide a compound that has excellent inhibitory action on ATPase activity of TIP48/TIP49 complex and is therefore useful for the treatment of tumor, or a pharmacologically acceptable salt thereof. SOLUTION: The present invention provides a compound having a structure represented by general formula (I), its pharmacologically acceptable salt, or a pharmaceutical composition comprising the compound (where R3, R4, R5, R6, R7, W, X, Y, and Z are as defined in the specifications). SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT

AMINOPYRAZOLONE DERIVATIVE

The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which has an excellent inhibitory action on the ATPase activity of a TIP48/TIP49 complex and as such, is useful for the treatment of tumors. [Solution] The present invention provides a compound having a structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the present specification.

FUNCTIONALIZED 9-BROMO-CAMPTOTHECIN DERIVATIVES

The present invention relates to new functionalized 9-bromo-camptothecin derivatives which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of these functionalized 9-bromo-camptothecin derivatives in the preparation of conjugates.