771579-27-2

Usage

Uses

Used in Pharmaceutical Industry:
2(1H)-Pyridinone, 3-(aminomethyl)-4,6-dimethyl(9CI) is used as a building block for the synthesis of various drugs and biologically active compounds, leveraging its antimicrobial, antifungal, and anti-inflammatory properties. Its potential in the development of new therapeutic agents makes it a valuable asset in creating treatments for a variety of diseases and conditions.
Used in Antimicrobial Applications:
In the field of antimicrobials, 2(1H)-Pyridinone, 3-(aminomethyl)-4,6-dimethyl(9CI) is utilized for its ability to combat microorganisms, providing a foundation for the creation of new antibiotics and antimicrobial agents to address resistant strains and infections.
Used in Antifungal Applications:
2(1H)-Pyridinone, 3-(aminomethyl)-4,6-dimethyl(9CI) is also employed in antifungal applications, where it serves as a key component in the development of treatments for fungal infections, offering an alternative or adjunct to existing antifungal medications.
Used in Anti-inflammatory Applications:
Leveraging its anti-inflammatory properties, 2(1H)-Pyridinone, 3-(aminomethyl)-4,6-dimethyl(9CI) is used in the development of medications aimed at reducing inflammation, which can be beneficial in treating a wide array of inflammatory conditions.

Upstream product

• 769-28-8 2-hydroxy-4,6-dimethyl-3-carbonitrile 
• 769-28-8 3-Cyano-4,6-dimethyl-2(1H)-pyridon 
• 123-54-6 acetylacetone 

Downstream Products

• 1396775-88-4 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(3-(hydroxymethyl)phenyl)-1-isopropyl-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 
• 1396770-90-3 1-(1-benzylpiperidin-4-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(2,2,6,6-tetramethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 
• 1396770-40-3 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-6-(4-(piperazin-1-yl)phenyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 
• 1396770-44-7 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-6-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 
• 1396771-63-3 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(1-phenylethyl)-6-(2,2,6,6-tetramethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 
• 1354821-72-9 N-[(4,6-dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)phenyl]-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 
• 1396770-63-0 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-6-(4-(4-methylpiperazine-1-carbonyl)phenyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 
• 1396770-68-5 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(3-((3-(dimethylamino)propyl)carbamoyl)phenyl)-1-isopropyl-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 
• 1396770-73-2 6-(4-(aminomethyl)phenyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 
• 1396770-76-5 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(((3-(dimethylamino)propyl)(methyl)amino)methyl)phenyl)-1-isopropyl-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 
• 1396770-81-2 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(3-(((3-(dimethylamino)propyl)(methyl)amino)methyl)phenyl)-1-isopropyl-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 
• 1396772-26-1 1-cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-1H-indazole-4-carboxamide 
• 1396772-66-9 1-cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(3-(3-(methylamino)propoxy)phenyl)-1H-indazole-4-carboxamide 
• 1396772-71-6 1-cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(3-(3-(dimethylamino)propoxy)phenyl)-1H-indazole-4-carboxamide 

Relevant academic research and scientific papers

Small molecule compound based on EZH2 protein degradation, and application thereof

The invention discloses a series of small molecule compounds capable of selectively degrading EZH2 protein, and application thereof. The compounds can be prepared into proper pharmaceutical dosage forms for EZH2-mediated related tumor treatment.

EZH2 INHIBITOR AND PHARMACEUTICALLY ACCEPTABLE SALTS AND POLYMORPHIC SUBSTANCES THEREOF, AND APPLICATION OF EZH2 INHIBITOR

The present invention provides an EZH2 inhibitor and pharmaceutically acceptable salts and polymorphic substances thereof, and application of the EZH2 inhibitor. Specifically, the present invention provides N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)m

Discovery of quinolone derivatives as antimycobacterial agents

Tuberculosis (TB), an infectious disease caused byMycobacterium tuberculosis(M. tuberculosis), is an important public health issue. Current first-line drugs administered to TB patients have been in use for over 40 years, whereas second-line drugs display strong side effects and poor compliance. Additionally, designing effective regimens to treat patients infected with multi- and extremely-drug-resistant (MDR and XDR) strains of TB is challenging. In this report, we screened our compound library and identified compound1with antituberculosis activity and a minimal inhibitory concentration (MIC) againstM. tuberculosisof 20 μg mL?1. Structure optimization and the structure-activity relationship of1as the lead compound enabled the design and synthesis of a series of quinolone derivatives,6a1-6a2,6b1-6b36,6c1,6d1-6d14,7a1-7a2,7b1-7b2,7c1,8a1-8a5,9a1-9a4and10a1-10a6. These compounds were evaluatedin vitrofor anti-tubercular activity against theM. tuberculosisH37Rv strain. Among them, compounds6b6,6b12and6b21exhibited MIC values in the range of 1.2-3 μg mL?1and showed excellent activity against the tested MDR-TB strain (MIC: 3, 2.9 and 0.9 μg mL?1, respectively). All three compounds were non-toxic toward A549 and Vero cells (>100 and >50 μg mL?1, respectively). In addition, an antibacterial spectrum test carried out using compound6b21showed that this compound specifically inhibitsM. tuberculosis. These can serve as a new starting point for the development of anti-TB agents with therapeutic potential.

Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma

Traditional EZH2 inhibitors are developed to suppress the enzymatic methylation activity, and they may have therapeutic limitations due to the nonenzymatic functions of EZH2 in cancer development. Here, we report proteolysis-target chimera (PROTAC)-based EZH2 degraders to target the whole EZH2 in lymphoma. Two series of EZH2 degraders were designed and synthesized to hijack E3 ligase systems containing either von Hippel-Lindau (VHL) or cereblon (CRBN), and some VHL-based compounds were able to mediate EZH2 degradation. Two best degraders, YM181 and YM281, induced robust cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphomas, outperforming a clinically used EZH2 inhibitor EPZ6438 (tazemetostat) that was only effective against DLBCL. The EZH2 degraders displayed promising antitumor activities in lymphoma xenografts and patient-derived primary lymphoma cells. Our study demonstrates that EZH2 degraders have better therapeutic activity than EZH2 inhibitors, which may provide a potential anticancer strategy to treat lymphoma.

1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES

The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.

4,5,6-TRI-SUBSTITUTED INDAZOLES DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES

Provided are 4,5,6-tri-substituted indazoles derivatives, a preparation method therefor, and a use thereof in medicines. Specifically, provided are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates, or prodrugs thereof

SULFONYL-SUBSTITUTED BENZOHETEROCYCLIC DERIVATIVE, PREPARATION METHOD AND MEDICAL USE THEREOF

The present invention relates to a sulfonyl-substituted benzoheterocyclic derivative, a preparation method and medical use thereof. Particularly, disclosed is a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, and a preparation method and application thereof. The definition of each group in the formula can be found in the specification and the claims.

Benzoheterocycle-carboxamide-pyridone derivatives and preparation method and applications thereof

The invention belongs to the field of chemical medicine preparation, and concretely relates to benzoheterocycle-carboxamide-pyridone derivatives, a preparation method and applications thereof. The invention provides the benzoheterocycle-carboxamide-pyridone derivatives, and a structure is represented by a formula I. The present invention also provides the preparation method and the applications ofthe above benzoheterocycle-carboxamide-pyridone derivatives. The benzoheterocycle-carboxamide-pyridone derivatives provided by the invention are novel compounds obtained on the basis of a large number of screening, inhibit EZH2 activity, and provide a novel selection for development and application of medicines for resisting tumors and autoimmune diseases.

Indazol-carboxamide-pyridinone derivatives as well as preparation method and applications thereof

The invention belongs to the field of chemical medicine preparation, and concretely relates to indazol-carboxamide-pyridinone derivatives, a preparation method and applications thereof. The inventionprovides the indazol-carboxamide-pyridinone derivatives, and a structure is represented by a formula I. The present invention also provides the preparation method and the applications of the above indazol-carboxamide-pyridinone derivatives. The indazol-carboxamide-pyridinone derivatives provided by the invention are novel compounds obtained on the basis of a large number of screening, inhibit EZH2activity, and provide a novel selection for development and application of medicines for resisting tumors and autoimmune diseases.

Novel EZH2 inhibitor and application thereof

The invention relates to an inhibitor for a wild type of human histone methyltransferase EZH2 and a mutation type of Y641, and the inhibitor is of a structure of formula (I) as shown in the specification. The invention further provides a method and application for treatment cancer or pre-cancerous diseases related to activity of EZH2 with the inhibitor.