1125632-87-2

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 369-36-8 6-fluoro-3-nitroaniline 
• 4548-45-2 2-chloro-5-nitropyridine 
• 1125632-86-1 tert-butyl-N-((tert-butoxy)carbonyl)-N-(2-fluoro-5-nitrophenyl)carbamate 

Downstream Products

• 1125633-41-1 C₂₇H₂₂ClFN₆O₃S 
• 1125632-88-3 tert-butyl [5-({2-[(cyclopropylcarbonyl)amino][1,3]thiazolo[5,4-b]pyridin-5-yl}amino)-2-fluorophenyl]carbamate 
• 1228465-67-5 N-(5-{[4-fluoro-3-({[4-(trifluoromethyl)phenyl]carbamoyl}amino)phenyl]amino}[1,3]thiazolo[5,4-b]pyridin-2-yl)cyclopropanecarboxamide 
• 1228465-66-4 N-(5-{[3-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-4-fluorophenyl]amino}[1,3]thiazolo[5,4-b]pyridin-2-yl)cyclopropanecarboxamide 
• 1125632-90-7 N-{5-[(3-amino-4-fluorophenyl)amino][1,3]thiazolo[5,4-b]pyridin-2-yl}cyclopropanecarboxamide 
• 1228465-65-3 N-(5-{[4-fluoro-3-({[4-(trifluoromethoxy)phenyl]carbamoyl}amino)phenyl]amino}[1,3]thi azolo[5,4-b]pyridin-2-yl)cyclopropanecarboxamide 

Relevant academic research and scientific papers

Bioisosteric Replacement of Arylamide-Linked Spine Residues with N-Acylhydrazones and Selenophenes as a Design Strategy to Novel Dibenzosuberone Derivatives as Type i 1/2 p38α MAP Kinase Inhibitors

The recent disclosure of type I 1/2 inhibitors for p38α MAPK demonstrated how the stabilization of the R-spine can be used as a strategy to greatly increase the target residence time (TRT) of inhibitors. Herein, for the first time, we describe N-acylhydrazone and selenophene residues as spine motifs, yielding metabolically stable inhibitors with high potency on enzymatic, NanoBRET, and whole blood assays, improved metabolic stability, and prolonged TRT.

SUBSTITUTED 3-((3-AMINOPHENYL)AMINO)PIPERIDINE-2,6-DIONE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH

Provided herein are piperidine dione compounds having the following structure (I) wherein RN, R1, R2, R3, R4, L,V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.

MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO

This disclosure relates to the field of moiecuies having pesticida i utility against pests in Phyla Arthropoda, Moliusca, and hJematoda, processes to produce such moiecuies, intermediates used In such processes, pesticidai compositions containing such molecules, and processes of using such pesticidai compositions against such pests. These pesticidai compositions may be used, for example, as acaricldes, insecticides, miticides, moilusclcides, and nematicides. This document discloses moiecuies having the following formula ("Formula One").

Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives

Our aim was to discover RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors that possess strong activity and sufficient oral absorption, and thus, we selected a 5-amino-linked thiazolo[5,4-d]pyrimidine derivative as the lead compound because of its potential kinase inhibitory activities and its desired solubility. The novel tertiary 1-cyano-1-methylethoxy substituent was designed to occupy the hydrophobic region of 'back pocket' of BRAF on the basis of the X-ray co-crystal structure data of BRAF. In addition, we found that N-methylation of the amine linker could control the twisted molecular conformation leading to improved solubility. These approaches produced N-methyl thiazolo[5,4-b]pyridine-5-amine derivative 5. To maximize the in vivo efficacy, we attempted salt formation of 5. Our result indicated that the besylate monohydrate salt form (5c) showed significant improvement of both solubility and oral absorption. Owing to the improved physicochemical properties, compound 5c demonstrated regressive antitumor efficacy in a HT-29 xenograft model.

HETEROCYCLIC COMPOUND AND USE THEREOF

A compound represented by formula (I) or a salt thereof, which has a potent Raf inhibitory activity. In formula (I), R1 represents an optionally substituted C1-6 alkyl, etc.; X represents —O— or —NR2— (wherein R2 represents a hydrogen atom or a C1-6 alkyl); Y represents a group represented by formula 2 (2ii or 2ii) (wherein ring A represents an optionally substituted benzene ring; Z represents a group represented by (1) —NR3CO—W1—, (2) —NR3CO—W1—O—, (3) —NR3CO—W1—O—W2—, (4) —NR3CO—W1—S—, (5) —NR3CO—W1—NR4—, (6) —NR3COO—, (7) —NR3COO—W1—, (8) —NR3CO—CO—, or (9) —NR3CONR4— (wherein R3 and R4 each represents a hydrogen atom, etc., and W1 and W2 each represents an optionally substituted C1-6 alkylene, etc.); and R5 represents an optionally substituted five- or six-membered ring group.