342623-32-9

Upstream product

• 5202-89-1 4-chlorobenzenesulfonyl chloride 
• 463-71-8 thiophosgene 

Downstream Products

• 1313233-93-0 C₂₂H₂₃ClN₂O₃S 

Relevant academic research and scientific papers

Identification of Novel Fused Heteroaromatics-Based MALT1 Inhibitors by High-Throughput Screening to Treat B Cell Lymphoma

Development of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) inhibitors is of great value and significance in the treatment of neoplastic disorders and inflammatory and autoimmune diseases. However, there is a lack of effective MALT1 inhibitors in clinic. Herein, a novel class of potent 5-oxo-1-thioxo-4,5-dihydro-1H-thiazolo[3,4-a]quinazoline-based MALT1 inhibitors and their covalent derivatives were first identified and designed through high-throughput screening. We demonstrated that compounds 15c, 15e, and 20c effectively inhibited the MALT1 protease and displayed selective cytotoxicity to activated B cell-like diffuse large B cell lymphoma with low single-digit micromolar potency. Furthermore, compound 20c specifically repressed NF-κB signaling and induced cell apoptosis in MALT1-dependent TMD8 cells in a dose-dependent manner. More importantly, 20c showed good pharmacokinetic properties and antitumor efficacy with no significant toxicity in the TMD8 xenograft tumor model. Collectively, this study provides valuable lead compounds of MALT1 inhibitors for further structural optimization and antitumor mechanism study.

ANT-LIGANDS MOLECULES AND BIOLOGICAL APPLICATIONS

The invention relates to molecules ANT-ligands having a substituted nitrogeneous heterocycle A wherein —A is a substituted pyrazinone of formula I wherein R1 is —(CH2)n —CO—OH; —(CH2)n —CO—OR; —(CH2)n —CO—NHR; —(CH2)n —CO—N(R, R′); —(CH2)n —OH; —(CH2)n —OR; —(CH2)n —OAr; —(CH2)n —C(R,R′) —(CH2)n —OH, R and R′, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het. representing an heterocyclic radical with one or several hetero atoms selected between N, S and O, said phenyl or heterocycle being optionally substituted by one or several atoms, groups or radicals selected from halogen atoms such as Cl, Br, I, or halogenated groups such as —CCl3 or —CF3; one or several —OH, —OR, —COOH or —COOR groups; a phenyl; a linear or branched C1-C12 alkyl radical; —NH—COR; or —CN; said groups occupying the same or different positions on the phenyl or heterocyclic radical; a linear or branched C1-C12 alkyl radical; a linear or branched C2-C12 alkylene radical; —(CH2)n —C3-C6 cycloalkyl radical; —(CH2)n Ar or —(CH2)n Het.; —(CH2)n —NH—CO—R; —(CH2)n —NH2; —(CH2)n—N(R,R′); —(CH2)n—NH—CO—OH; —(CH2)n—NH—CO—OR; —NH—(CH2)n—CO—OH; —NH—(CH2)n—CO—OR; R2 is —(CH2)n-Ar, Ar being such as above defined and being optionally substituted such as above defined; a linear or branched C1-C12 alkyl or C2-C12 alkylene radical with one or several double bonds; —(CH2)n —OH; —(CH2)n —OR; —(CH2)n —CO—Het; —(CH2)n —NH—CO—R; —(CH2)n —NH2; —(CH2)n —N(R,R′); —(CH2)n —CO—OH; —(CH2)n —CO—OR; a linear or branched C1-C12 alkyl radical; —(CH2)n —C(R)=CH—C (R)=CH2, R3 forms a phenyl or an heterocyclic condensed group with the two adjacent carbons of the pyrazinone residue, said condensed group being optionally substituted such as above defined for Ar and Het.; and/or condensed to a cyclohexyl or oxanyl group, in turn optionally substituted such as above defined for Ar; n is 0 or an integer from 1 to 5; or A is a substituted pyrazine of formula II wherein R4 is a —CO—NH—Ar radical, optionally substituted such as above defined; R5 forms a phenyl or heterocyclic group condensed to the two adjacent carbon groups of the pyrazine residue, said phenyl or heterocyclic group being optionally substituted such as above defined, and Ar being such as above defined with respect to formula I or A is a substituted pyridine group of formula III wherein, Ar and R2 are as above defined with respect to formula I.

Pyrimido-Benzimidazole Derivatives and the Use Thereof in the Form of Agonists and Antagonists of Melanocortin Receptors

The invention relates to novel pyrimido-benzimidazole derivatives. Said products exhibit a good affinity for certain melanocortin receptor sub-types, in particular MC4 receptors. Said products represent a particular interest for treating pathological disorders and diseases associated with one or several melanocortin receptors. Pharmaceutical compositions containing said products and the use thereof for a drug preparation are also disclosed.