952616-39-6Relevant articles and documents
FUSED RING PYRIMIDONE DERIVATIVES FOR USE IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES
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Page/Page column 248; 262, (2022/04/03)
Provided are compounds according to any of Formula (I-1) to (I-7), pharmaceutical compositions comprising at least one of said compounds, their use as a medicament, and their use in treating chronic hepatitis B virus (HBV) infection. Methods for preparing compounds according to any of Formula (I-1) to (I-7) are also provided.
Development of a Scalable Synthesis of an Azaindolyl-Pyrimidine Inhibitor of Influenza Virus Replication
Liang, Jianglin,Cochran, John E.,Dorsch, Warren A.,Davies, Ioana,Clark, Michael P.
, p. 965 - 969 (2016/06/09)
A scalable, asymmetric route for the synthesis of the influenza virus replication inhibitor 2 is presented. The key steps include an enzymatic desymmetrization of cis-1,3-cyclohexanediester in 99% yield and 96% ee, SNAr displacement of a methanesulfinylpyrimidine, and a Curtius rearrangement to form a morpholinyl urea. This high-yielding route allowed us to rapidly synthesize hundreds of grams of 2 in 99% purity to support in vivo studies.
Inhibitors of influenza viruses replication
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, (2016/06/14)
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 (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) 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
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, (2016/10/08)
PROBLEM TO BE SOLVED: To provide inhibitors of influenza virus replication. SOLUTION: 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 comprise administering to the biological sample or patient an effective amount of a compound represented by structural formula (I) or a pharmaceutically acceptable salt thereof, where the values of structural formula (IA) are as described herein. A compound is represented by structural formula (IA) or a pharmaceutically acceptable salt thereof, where the values of structural formula (IA) 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. COPYRIGHT: (C)2015,JPO&INPIT
INHIBITORS OF INFLUENZA VIRUSES REPLICATION
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, (2014/01/08)
Compound according to 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. Uses 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.
INHIBITORS OF INFLUENZA VIRUSES REPLICATION
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, (2012/06/30)
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
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, (2012/06/30)
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
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, (2012/07/14)
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 (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) 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.
Discovery of PF-04449913, a potent and orally bioavailable inhibitor of smoothened
Munchhof, Michael J.,Li, Qifang,Shavnya, Andrei,Borzillo, Gary V.,Boyden, Tracey L.,Jones, Christopher S.,Lagreca, Susan D.,Martinez-Alsina, Luis,Patel, Nandini,Pelletier, Kathleen,Reiter, Larry A.,Robbins, Michael D.,Tkalcevic, George T.
supporting information; experimental part, p. 106 - 111 (2012/04/04)
Inhibitors of the Hedgehog signaling pathway have generated a great deal of interest in the oncology area due to the mounting evidence of their potential to provide promising therapeutic options for patients. Herein, we describe the discovery strategy to overcome the issues inherent in lead structure 1 that resulted in the identification of Smoothened inhibitor 1-((2R,4R)-2-(1H-benzo[d] imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea (PF-04449913, 26), which has been advanced to human clinical studies.
A practical synthesis of [(1 S,3 S)-3-aminocyclohexyl]methanol and 2-[(1 S,3 S)-3-aminocyclohexyl]propan-2-ol, useful intermediates for the preparation of novel m PGES-1 inhibitors
Walker, Daniel P.,Heasley, Steven E.,MacInnes, Allison,Anjeh, Tizah,Lu, Hwang-Fun,Fobian, Yvette M.,Collins, Joe T.,Vazquez, Michael L.,Mao, Michael K.
, p. 2959 - 2962 (2012/01/13)
Microsomal prostaglandin E2 synthase-1 (mPGES-1) is a novel therapeutic target for the treatment of inflammation and pain. During the course of studies aimed at the identification of a suitable mPGES-1 inhibitor for clinical development, a need arose for preparing enantiomerically enriched amino alcohols (S,S)-2 and (S,S)-3. Described herein, a concise synthesis of (S,S)-2 and (S,S)-3 has been developed wherein both amino alcohols are derived from a commercially available, low-cost starting material. Georg Thieme Verlag Stuttgart · New York.
