1259279-57-6Relevant articles and documents
Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases
Farmer, Luc J.,Ledeboer, Mark W.,Hoock, Thomas,Arnost, Michael J.,Bethiel, Randy S.,Bennani, Youssef L.,Black, James J.,Brummel, Christopher L.,Chakilam, Ananthsrinivas,Dorsch, Warren A.,Fan, Bin,Cochran, John E.,Halas, Summer,Harrington, Edmund M.,Hogan, James K.,Howe, David,Huang, Hui,Jacobs, Dylan H.,Laitinen, Leena M.,Liao, Shengkai,Mahajan, Sudipta,Marone, Valerie,Martinez-Botella, Gabriel,McCarthy, Pamela,Messersmith, David,Namchuk, Mark,Oh, Luke,Penney, Marina S.,Pierce, Albert C.,Raybuck, Scott A.,Rugg, Arthur,Salituro, Francesco G.,Saxena, Kumkum,Shannon, Dean,Shlyakter, Dina,Swenson, Lora,Tian, Shi-Kai,Town, Christopher,Wang, Jian,Wang, Tiansheng,Wannamaker, M. Woods,Winquist, Raymond J.,Zuccola, Harmon J.
, p. 7195 - 7216 (2015)
While several therapeutic options exist, the need for more effective, safe, and convenient treatment for a variety of autoimmune diseases persists. Targeting the Janus tyrosine kinases (JAKs), which play essential roles in cell signaling responses and can contribute to aberrant immune function associated with disease, has emerged as a novel and attractive approach for the development of new autoimmune disease therapies. We screened our compound library against JAK3, a key signaling kinase in immune cells, and identified multiple scaffolds showing good inhibitory activity for this kinase. A particular scaffold of interest, the 1H-pyrrolo[2,3-b]pyridine series (7-azaindoles), was selected for further optimization in part on the basis of binding affinity (Ki) as well as on the basis of cellular potency. Optimization of this chemical series led to the identification of VX-509 (decernotinib), a novel, potent, and selective JAK3 inhibitor, which demonstrates good efficacy in vivo in the rat host versus graft model (HvG). On the basis of these findings, it appears that VX-509 offers potential for the treatment of a variety of autoimmune diseases.
ANTI-INFLUENZA VIRUS PYRIMIDINE DERIVATIVE
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, (2021/02/05)
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.
FORMULATIONS OF AZAINDOLE COMPOUNDS
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, (2021/01/22)
The present invention relates to pharmaceutical compositions, each comprising a multitude of granules that make up an intragranular phase of the composition, wherein the granules are produced by fluid bed granulation and comprise a HCI salt of Compound (1
PYRROLO[2,3-B]PYRIDIN DERIVATIVES AS INHIBITORS OF INFLUENZA VIRUS REPLICATION
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, (2020/02/16)
Provided herein are compounds of Formula A, B or C that can inhibit the replication of influenza viruses, reduce the amount of influenza viruses, and/or treat influenza.
Novel heterocyclic compounds and medicinal application of same as anti-influenza virus inhibitors
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, (2019/03/10)
The invention provides heterocyclic compounds represented by a formula (I) as described in the specification or a pharmaceutically acceptable salt thereof, a preparation method thereof, and application of the heterocyclic compounds to the preparation of m
Heterocyclic compounds and, their compositions and their use as anti-influenza virus drugs (by machine translation)
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, (2020/01/03)
The invention provides a class of heterocyclic (I) compounds or pharmaceutically acceptable salts thereof as shown in formula (I) or a preparation method thereof as well A as a preparation method and application of the compounds in. preparation of drugs for treating or, preventing influenza viruses RNA. (by machine translation)
Influenza virus replication inhibitors and uses thereof (by machine translation)
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, (2019/10/01)
The invention provides a compound as an influenza virus replication inhibitor, a method for preparing the same, a pharmaceutical composition containing the compound and application. (by machine translation)
INHIBITORS OF INFLUENZA VIRUS REPLICATION, APPLICATION METHODS AND USES THEREOF
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, (2018/03/25)
The invention provides 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 manufacture of medicaments for treating of influenza.
Influenza virus replication inhibitor and application thereof
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, (2018/11/22)
The invention provides a type of compounds serving as an influenza virus replication inhibitor, a preparation method of the compounds, a pharmaceutical composition comprising the compounds, and application of the compounds and the pharmaceutical composition thereof in treatment of influenza.
PYRROLOPYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF INFLUENZA VIRUS REPLICATION
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, (2018/11/22)
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 a safe and effective amount of a compound represented by any of Formulas l-lll, or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a safe and effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.