- The discovery of potent small molecule cyclic urea activators of STING
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STING mediates innate immune responses that are triggered by the presence of cytosolic DNA. Activation of STING to boost antigen recognition is a therapeutic modality that is currently being tested in cancer patients using nucleic-acid based macrocyclic STING ligands. We describe here the discovery of 3,4-dihydroquinazolin-2(1H)-one based 6,6-bicyclic heterocyclic agonists of human STING that activate all known human variants of STING with high potency.
- Banerjee, Monali,Basu, Sourav,Ghosh, Rajib,Middya, Sandip,Pryde, David C.,Shrivastava, Ritesh,Surya, Arjun,Yadav, Dharmendra B.
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supporting information
(2022/02/07)
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- Novel synthesis method of 3-fluoropyridine-2-methanol
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The invention relates to the field of compound preparation, in particular to a novel synthesis method of 3-fluoropyridine-2-methanol. The 3-fluoropyridine-2-methanol has a structure as shown in a formula V. According to the synthesis method, cheap quinolinic acid is used as an initial raw material, the target product namely 3-fluoropyridine-2-methanol is obtained through the steps of anhydride, esterification, ammoniation, amino fluorination, ester group reduction, and the like, and the structure of the target product is characterized by 1HNMR and 13CNMR. The synthetic method is a brand new synthetic method of 3-fluoropyridine-2-methanol, and has the advantages of low cost, simple technology, high yield, good quality, and high industrialization value.
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- TETRAHYDROCARBAZOLE DERIVATIVES USEFUL AS ANDROGEN RECEPTOR MODULATORS
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The present invention provides a compound of the formula: Formula I or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or ex
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Page/Page column 165
(2010/11/25)
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- IMIDAZOPYRIDINE COMPOUND
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The present invention provides an imidazopyridine compound represented by formula (I), wherein R1 and R2 each independently represent a C1-6 alkyl group et al; R3 and R4 each independently represent a hydrogen atom, a methyl et al; Ar1 is a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Ar2 represents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents -(CH2)m et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.
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Page/Page column 36
(2008/06/13)
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- Method for inhibition of HIV related viruses
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Treatment of AIDS, inhibition of the replication of HIV and related viruses thereof, and formulations using thiourea derivative compounds or salts thereof is disclosed. Also disclosed are novel thiourea derivative compounds.
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- 2--1H-thienoimidazoles. A Novel Class of Gastric H+/K+-ATPase Inhibitors
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2-thienoimidazoles were synthesized and investigated as potential inhibitors of gastric H+/K+-ATPase.The isomers of the two possible thienoimidazole series were found to be potent inhibitors of gastric acid secretion in vitro and in vivo.Structure-activity relationships indicate that especially lipophilic alkoxy, benzyloxy, and phenoxy substituents with additional electron-demanding properties in the 4-position of the pyridine moiety combined with an unsubstituted thienoimidazole lead to highly active compounds with a favorable chemical stability.Various substitution patterns in the thienoimidazole moiety result in lower biological activity.The heptafluorobutyloxy derivative saviprazole (HOE 731, 5d) was selected for further development and is currently undergoing clinical evaluation.Comprehensive pharmacological studies indicate a pharmacodynamic profile different to omeprazole, the first H+/K+-ATPase blocker introduced on the market.
- Weidmann, Klaus,Herling, Andreas W.,Lang, Hans-Jochen,Scheunemann, Karl-Heinz,Rippel, Robert,et al.
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p. 438 - 450
(2007/10/02)
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