708279-23-6

Usage

Uses

Used in Pharmaceutical Industry:
4-methyl-N-(4-nitrophenyl)-1-Piperazineacetamide is used as a key intermediate in the synthesis of Desmethyl Nintedanib, which is an impurity of Intedanib. Intedanib is an antitumor agent that has potential applications in cancer treatment.
Additionally, Desmethyl Nintedanib has been used in the study of synthesizing indolinones as triple angiokinase inhibitors, which are compounds with potential therapeutic applications in various diseases, including cancer. This highlights the importance of 4-methyl-N-(4-nitrophenyl)-1-Piperazineacetamide in the development of novel therapeutic agents for the treatment of various medical conditions.

Upstream product

• 109-01-3 1-methyl-piperazine 
• 3598-91-2 N-(4-nitrophenyl)bromoacetamide 
• 100-01-6 4-nitro-aniline 
• 17329-87-2 2-chloro-N-(4-nitro-phenyl)-acetamide 

Downstream Products

• 262368-25-2 N-(4-aminophenyl)-2-(4-methylpiperazin-1-yl)acetamide 

Relevant academic research and scientific papers

PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS AND THEIR THERAPEUTICAL APPLICATIONS

The present invention provides kinase inhibitors with anti-proliferative activity comprising substituted pyrimidine derivatives and pharmaceutically-acceptable formulations thereof. In addition, the invention provides methods for making novel compounds and methods for using the compounds.

Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120)

Inhibition of tumor angiogenesis through blockade of the vascular endothelial growth factor (VEGF) signaling pathway is a newtreatment modality in oncology. Preclinical findings suggest that blockade of additional pro-angiogenic kinases, such as fibroblast and platelet-derived growth factor receptors (FGFR and PDGFR), may improve the efficacy of pharmacological cancer treatment. Indolinones substituted in position 6 were identified as selective inhibitors of VEGF-, PDGF-, and FGF-receptor kinases. In particular, 6-methoxycarbonyl-substituted indolinones showed a highly favorable selectivity profile. Optimization identified potent inhibitors of VEGF-related endothelial cell proliferation with additional efficacy on pericyctes and smooth muscle cells. In contrast, no direct inhibition of tumor cell proliferation was observed. Compounds 2 (BIBF 1000) and 3 (BIBF 1120) are orally available and display encouraging efficacy in in vivo tumor models while being well tolerated. The triple angiokinase inhibitor 3 is currently in phase III clinical trials for the treatment of nonsmall cell lung cancer.