1383446-11-4

Upstream product

• 1383446-10-3 3-bromo-5-fluoro-1-trityl-1H-pyrazolo[3,4-b]pyridine 
• 73183-34-3 bis(pinacol)diborane 
• 791644-48-9 2-chloro-5-fluoronicotinonitrile 
• 1034667-22-5 5-fluoro-1H-pyrazolo[3,4-b]pyridine-3-amine 
• 1350653-23-4 5-fluoro-3-iodo-1H-pyrazolo[3,4-b]pyridine 
• 1256822-80-6 3-bromo-5-fluoro-1H-pyrazolo[3,4-b]pyridine 

Downstream Products

• 1383485-63-9 N-((1R,3S)-3-(3,5-difluoro-6-(5-fluoro-1-trityl-1H-pyrazolo[3,4-b]pyridin-3-yl)pyridin-2-ylamino)cyclohexyl)-1-methyl-1H-imidazole-4-carboxamide 
• 1383485-79-7 N-((1R,3S)-3-(3,5-difluoro-6-(5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-yl)pyridin-2-ylamino)cyclohexyl)-1-methyl-1H-imidazole-4-carboxamide 
• 1383485-56-0 (1R,3S)-3-(3,5-difluoro-6-(5-fluoro-1-trityl-1H-pyrazolo[3,4-b]pyridin-3-yl)pyridin-2-ylamino)cyclohexanecarboxylic acid 
• 1383485-77-5 (1R,3S)-3-(3,5-difluoro-6-(5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-yl)pyridin-2-ylamino)cyclohexanecarboxylic acid 
• 1383485-52-6 C₄₁H₃₄F₂N₆O₂ 
• 1383485-55-9 (1R,3S)-ethyl 3-(3,5-difluoro-6-(5-fluoro-1-trityl-1H-pyrazolo[3,4-b]pyridin-3-yl)pyridin-2-ylamino)cyclohexanecarboxylate 
• 1383485-59-3 (2S,3S)-3-(3-fluoro-6-(5-fluoro-1-trityl-1H-pyrazolo[3,4-b]pyridin-3-yl)pyridin-2-ylamino)bicyclo[2.2.2]octane-2-carboxylic acid 

Relevant academic research and scientific papers

ANTI-INFLUENZA VIRUS PYRIMIDINE DERIVATIVE

The present invention discloses a class of anti-influenza virus compounds, and the use thereof in the preparation of a drug for treating diseases associated with influenza viruses. In particular, the present invention discloses a compound represented by formula (I) and a pharmaceutically acceptable salt thereof.

CRYSTAL FORM AND SALT FORM OF PYRIDOIMIDAZOLE COMPOUND AND PREPARATION METHOD THEREFOR

Disclosed are a crystal form and a salt form of a pyrazolopridine compound, and a preparation method therefor. Further included is the use of the crystal form in preparing anti-influenza virus drugs.

INHIBITORS OF INFLUENZA VIRUS REPLICATION AND USES THEREOF

Provided herein is inhibitors of influenza virus replication and uses thereof. Specifically, provided herein a novel class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.

Influenza virus replication inhibitor and application thereof

The invention relates to an influenza virus replication inhibitor and application thereof, and particularly relates to a compound serving as an influenza virus replication inhibitor, a preparation method thereof, a pharmaceutical composition containing the compound, and application of the compound and the pharmaceutical composition to influenza treatment.

Novel 2-Substituted 7-Azaindole and 7-Azaindazole Analogues as Potential Antiviral Agents for the Treatment of Influenza

JNJ-63623872 (2) is a first-in-class, orally bioavailable compound that offers significant potential for the treatment of pandemic and seasonal influenza. Early lead optimization efforts in our 7-azaindole series focused on 1,3-diaminocyclohexyl amide and urea substitutions on the pyrimidine-7-azaindole motif. In this work, we explored two strategies to eliminate observed aldehyde oxidase (AO)-mediated metabolism at the 2-position of these 7-azaindole analogues. Substitution at the 2-position of the azaindole ring generated somewhat less potent analogues, but reduced AO-mediated metabolism. Incorporation of a ring nitrogen generated 7-azaindazole analogues that were equipotent to the parent 2-H-7-azaindole, but surprisingly, did not appear to improve AO-mediated metabolism. Overall, we identified multiple 2-substituted 7-azaindole analogues with enhanced AO stability and we present data for one such compound (12) that demonstrate a favorable oral pharmacokinetic profile in rodents. These analogues have the potential to be further developed as anti-influenza agents for the treatment of influenza.

INHIBITORS OF INFLUENZA VIRUSES REPLICATION

Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

INHIBITORS OF INFLUENZA VIRUSES REPLICATION

Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

INHIBITORS OF INFLUENZA VIRUSES REPLICATION

Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.