2137975-62-1

Upstream product

• 71001-78-0 3-nitro-4-chloro-5-methoxybenzoic acid 
• 63603-09-8 methyl 4-chloro-3-methoxy-5-nitrobenzoate 

Downstream Products

• 2138299-29-1 (E)-1-(4-(5-carbamoyl-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-(3-hydroxypropoxy)-1H-benzo[d]imidazole-5-carboxamide 

Relevant academic research and scientific papers

STING AGONIST COMPOUNDS AND METHODS OF USE

The present disclosure relates to STING (Stimulator of Interferon Genes) agonist compounds, methods of making the compounds and their methods of use.

Aromatic ring or aromatic heterocyclic imidazole compound, preparation method and pharmaceutical application thereof

The invention relates to a compound containing an aromatic ring or aromatic heterocyclic imidazole structure or pharmaceutically acceptable salt thereof, a preparation method of the compound, a pharmaceutical composition containing the compound and medical application of the compound. The compound disclosed by the invention has the effect of specifically exciting STING protein, and can be used forpreparing medicines for treating diseases related to STING protein functions, like malignant tumors, virus infection and the like.

Heterocyclic amide compound, pharmaceutically acceptable salt thereof, and preparation method and application of heterocyclic amide compound

The invention discloses a heterocyclic amide compound represented by a general formula (I) and a pharmaceutically acceptable salt thereof, also discloses a preparation method of the compound as shownin the formula I and the pharmaceutically acceptable salt thereof, and discloses application of the compound in preparation of medicines for treating diseases related to STING activity, immunologic adjuvants and medicines for activating STIGN. A new choice is provided for clinically screening and/or preparing drugs for STING activity related diseases.

Heterocyclic compound and application thereof

The present disclosure relates to a heterocyclic compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereoisomer, an atropisomer, an optical isomer, a raceme, a polymorphic substance, a solvate or an isotope labeled compound thereof, a pharmaceutical composition containing the heterocyclic compound, and a pharmaceutical use thereof. The heterocyclic compound disclosed by the invention is an immunomodulator, and particularly relates to an immunomodulator of a compound for activating STING.

IMMUNOMODULATOR

The present application discloses an immunomodulator, and specifically discloses a compound depicted by formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. The compound provided in the present application can bind effectively to STING and has a good agonistic action on STING protein, and exhibits a good inhibitory effect on multiple tumors. Thus, the compound provided in the present application serves as a STING agonist and can be used for treating various related conditions. The compound provided in the present invention shows a very promising prospect for application thereof in the preparation of a medicament for treating a disease associated with STING activity (in particular, a medicament for treating an inflammatory disease, an allergic disease, an autoimmune disease, an infectious disease, a cancer or a precancerous syndrome) and in the preparation of an immune adjuvant, providing a novel option for clinically screening and/or preparing drugs for diseases associated with STING activity.

MACROCYCLIC COMPOUNDS AS STING AGONISTS

Disclosed are the macrocyclic compounds having the general Formula (I) and their tautomeric forms, stereoisomers, pharmaceutically acceptable salts, and their combination with suitable medicament, corresponding processes for the synthesis and pharmaceutical compositions and uses of compounds disclosed herein.

STING HETEROCYCLE AGONISTS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the modulation of STING, and the treatment of STING-mediated disorders.

STING PYRAZOLE AGONISTS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the modulation of STING, and the treatment of STING-mediated disorders.

STING AGONISTS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the modulation of STING, and the treatment of STING-mediated disorders.

Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists

Stimulator of interferon genes (STING) is an endoplasmic reticulum-localized adaptor protein (STING receptor) that has been shown to be activated by binding to natural cyclic dinucleotide (CDN) ligands and plays a vital role in innate immune sensing of exogenous or endogenous DNA, which then induces type I interferons and other cytokines. In this paper, we described a series of amidobenzimidazole STING agonists with high potency for the STING receptor and presented the relevant structure-activity relationships (SARs). The relative potencies of compounds 16g, 24b, and 24e were measured by a STING competition binding assay. A more thorough study of the effect on the STING signaling pathway demonstrated that three compounds, 16g, 24b, and 24e, significantly increased the protein levels and mRNA levels of IFN-β, CXCL10, and IL-6, and 24b as a representative compound effectively triggered the phosphorylation of STING, TBK1, and IRF3 in both human peripheral blood mononuclear cells (hPBMCs) and WT THP-1 cells. In addition, compound 24b demonstrated impressive antitumor efficacy in mice with established syngeneic colon tumors by intravenous administration. Furthermore, the pharmacokinetic profile of compound 24b was fully evaluated.