3920-39-6

Usage

Uses

Used in Pharmaceutical Synthesis:
1-Methyl-4-nitro-1H-pyrazole-3-carboxamide is used as a building block in the pharmaceutical industry for the development of new drugs. Its unique structure and properties make it a valuable component in the synthesis of various medicinal compounds, contributing to the discovery of novel therapeutic agents.
Used in Agrochemical Synthesis:
In the agrochemical industry, 1-Methyl-4-nitro-1H-pyrazole-3-carboxamide is utilized as a key intermediate in the synthesis of pesticides and other crop protection agents. Its incorporation into these products can enhance their effectiveness in controlling pests and diseases, thereby improving agricultural productivity.
Used in Anti-inflammatory Applications:
1-Methyl-4-nitro-1H-pyrazole-3-carboxamide has been investigated for its potential anti-inflammatory properties. It may be used as an active pharmaceutical ingredient in the development of anti-inflammatory drugs, helping to alleviate inflammation and related symptoms in various conditions.
Used in Antitumor Applications:
Research has also explored the compound's potential antitumor properties, suggesting its use as a chemotherapeutic agent. 1-Methyl-4-nitro-1H-pyrazole-3-carboxamide may be employed in the development of anticancer drugs, targeting tumor cells and inhibiting their growth and proliferation.

Upstream product

• 400877-57-8 1-methyl-4-nitro-1H-pyrazole-3-carboxylic acid methyl ester 
• 4598-86-1 1-methyl-4-nitro-1H-pyrazole-3-carboxylic acid 

Downstream Products

• 1357086-83-9 5-{[(4-methoxy-phenyl)carbamoyl]amino}-8-(furan-2-yl)-2-methyl-2H-pyrazolo[3,4-e][1,2,4]triazolo[1,5-c]pyrimidine 
• 3920-40-9 4-amino-1-methyl-1H-pyrazole-3-carboxamide 
• 151599-40-5 1-methyl-4-nitro-1H-pyrazole-3-carbonitrile 
• 1201935-84-3 4-amino-1-methyl-1H-pyrazole-3-carbonitrile 

Relevant academic research and scientific papers

Design and synthesis of Imidazo[1,2-b]pyridazine IRAK4 inhibitors for the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma

Harboring MYD88 L265P mutation triggers tumors growth through the activation of NF-κB by interleukin-1 receptor associated kinase 4 (IRAK4) in diffuse large B-cell lymphoma (DLBCL), highlighting IRAK4 as a therapeutic target for tumors driven by aberrant MYD88 signaling. Herein, we report the design, synthesis, and structure?activity relationships of imidazo[1,2-b]pyridazines as potent IRAK4 inhibitors. The representative compound 5 exhibited excellent IRAK4 potency (IRAK4 IC50 = 1.3 nM) and favorable kinase selectivity profile. It demonstrated cellular selectivity for activated B cell–like (ABC) subtype DLBCL with MYD88 L265P mutation in cytotoxicity assay. The kinase inhibitory efficiency of compound 5 was further validated by Western blot analysis of phosphorylation of IRAK4 and downstream signaling in OCI-LY10 and TMD8 cells. Besides, combination of compound 5 and BTK inhibitor ibrutinib synergistically reduced the viability of TMD8 cells. These results indicated that compound 5 could be a promising IRAK4 inhibitor for the treatment of mutant MYD88 DLBCL.

Design, synthesis and biological evaluation of pyridone–aminal derivatives as MNK1/2 inhibitors

Excessive phosphorylation of eukaryotic translation initiation factor 4E (eIF4E) plays a major role in the dysregulation of mRNA translation and the activation of tumor cell signaling. eIF4E is exclusively phosphorylated by mitogen-activated protein kinase interacting kinases 1 and 2 (MNK1/2) on Ser209. So, MNK1/2 inhibitors could decrease the level of p-eIF4E and regulate tumor-associated signaling pathways. A series of pyridone–aminal derivatives were synthesized and evaluated as MNK1/2 inhibitors. Several compounds exhibited great inhibitory activity against MNK1/2 and selected compounds showed moderate to excellent anti-proliferative potency against hematologic cancer cell lines. In particular, compound 42i (MNK1 IC50 = 7.0 nM; MNK2 IC50 = 6.1 nM) proved to be the most potent compound against TMD-8 cell line with IC50 value of 0.91 μM. Furthermore, 42i could block the phosphorylation level of eIF4E in CT-26 cell line, and 42i inhibited the tumor growth of CT-26 allograft model significantly. These results indicated that compound 42i was a promising MNK1/2 inhibitor for the potent treatment of colon cancer.

Imidazopyridazine IRAK4 inhibitor, and preparation method and application thereof

The invention belongs to the field of medicines, and especially relates to an imidazopyridazine compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and an applicationof a medicinal composition of the compound or the salt in the treatment of tumors, inflammations, immunity and other diseases. The imidazopyridazine compound is a novel protein kinase IRAK4 inhibitor, and can selectively inhibit IRAK4 and downstream signaling pathways thereof. The compound has the structural formula I.

HYDROXYL PURINE COMPOUNDS AND USE THEREOF

Disclosed are a series of hydroxyl purine compounds and the use thereof as PDE2 or TNFα inhibitors, in particular, the compounds as shown in formula (I), or tautomers thereof or pharmaceutically acceptable salts thereof.

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.

PYRAZOLOPYRIMIDINE INHIBITORS OF IRAK4 ACTIVITY

The present invention relates to pyrazolopyrimidine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

THIENOPYRAZINE INHIBITORS OF IRAK4 ACTIVITY

The present invention relates to thienopyrazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

PYRROLOPYRIDAZINE INHIBITORS OF IRAK4 ACTIVITY

The present invention relates to pyrrolopyridazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

PYRROLOTRIAZINE INHIBITORS OF IRAK4 ACTIVITY

The present invention relates to pyrrolotriazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

NITROGEN CONTAINING HETEROARYL COMPOUNDS

The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the descripti