128883-86-3

Upstream product

• 18595-34-1 tert-butyl fluoroformate 
• 1904-31-0 methyl-1 amino-3 pyrazole 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 128883-83-0 3-((tert-butoxycarbonyl)amino)-1-methyl-1H-pyrazole-5-carboxylic acid 

Relevant academic research and scientific papers

Design and Synthesis of a Series of Novel Macrocycle Janus Kinase 2 Inhibitors

Macrocycle has attracted the attention of many researchers in the field of medicinal chemistry due to its unique advantages and good prospects, but the difficulties in drug design and synthesis of macrocycle limit its applications. In this study, a series of macrocyclic derivatives designed from anaplastic lymphoma kinase (ALK) inhibitor lorlatinib were synthesized as Janus kinase 2 (JAK2) selective inhibitors. Among them, 17f had the best inhibitory activity (IC50 = 0.177 μmol·L–1) and selectivity for JAK2 over JAK1 and JAK3, which indicated that design of the macrocyclic derivatives might be a feasible strategy for the discovery of novel selective JAK2 inhibitors.

PESTICIDALLY ACTIVE MESOIONIC HETEROCYCLIC COMPOUNDS

A compound of formula I, (I), wherein the substituents are as defined in claim (1), and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides.

NOVEL COMPOUNDS

The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 is a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

NOVEL COMPOUNDS

The present invention relates to substituted 5-membered nitrogen containing heteroaryl compounds, such as sulfonyl triazoles, where the heteroaryl ring is further substituted, optionally via a linking group such as -NH-, with a cyclic group which in turn is substituted at the α-position. The present invention further relates to associated salts, solvates, prodrugs and pharmaceutical compositions, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.

COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR

Compounds of Formula (I) or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein A, J, R1, R2, R3, R4, R5, R6, R7, R9, X, m and n are as described herein, compositions thereof, and methods and uses thereof.

MACROCYCLIC COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISEASES

The compounds and salts of the present invention inhibit kinases, especially the anaplastic lymphoma kinase (ALK) and the HGF receptor tyrosine kinase (RTK) c-Met, and are useful for treating or ameliorating abnormal cell proliferative disorders, such as

The Preparation of Partially Protected 3-Amino-1-methylpyrazole-5-carboxylic Acids to be Used as Intermediates in the Synthesis of Analogues of Distamycin A

Partially protected 3-amino-1-methylpyrazole-5-carboxylic acid derivatives have been prepared by a convenient route from 3-amino-1-methylpyrazole.The structures of these compounds have been correlated with recent work in the field.Such derivatives, blocke