934178-96-8Relevant academic research and scientific papers
Synthesis of Differentially Protected Azatryptophan Analogs via Pd2(dba)3/XPhos Catalyzed Negishi Coupling of N-Ts Azaindole Halides with Zinc Derivative from Fmoc-Protected tert-Butyl (R)-2-Amino-3-iodopropanoate
Nimje, Roshan Y.,Vytla, Devaiah,Kuppusamy, Prakasam,Velayuthaperumal, Rajeswari,Jarugu, Lokesh Babu,Reddy, China Anki,Chikkananjaiah, Nanjundaswamy Kanikahalli,Rampulla, Richard A.,Cavallaro, Cullen L.,Li, Jianqing,Mathur, Arvind,Gupta, Anuradha,Roy, Amrita
, p. 11519 - 11530 (2020)
Unnatural amino acids play an important role in peptide based drug discovery. Herein, we report a class of differentially protected azatryptophan derivatives synthesized from N-tosyl-3-haloazaindoles 1 and Fmoc-protected tert-butyl iodoalanine 2 via a Neg
INHIBITORS OF INFLUENZA VIRUS REPLICATION, APPLICATION METHODS AND USES THEREOF
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Paragraph 00290, (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.
INHIBITORS OF INFLUENZA VIRUS REPLICATION AND USES THEREOF
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Paragraph 00233, (2018/09/21)
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 treatment of influenza.
Influenza virus replication inhibitor and application thereof
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Paragraph 0656; 0658-0660, (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.
HETEROCYCLIC INDOLES FOR USE IN INFLUENZA VIRUS INFECTION
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, (2017/06/30)
The current invention relates to a compound of formula (I) which can be used for the treatment of, or against viral influenza infections.
ARYL SUBSTITUTED PYRIMIDINES FOR USE IN INFLUENZA VIRUS INFECTION
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, (2017/09/24)
The invention relates to compounds having the structure of formula (I) which can be used for the treatment of or against influenza infections.
PYRROLOPYRIMIDINES FOR USE IN INFLUENZA VIRUS INFECTION
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Paragraph 0048; 0052-0053, (2017/09/20)
The invention relates to compounds having the structure of formula (I) which can be used for the treatment of or against influenza infections.
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 (2015/10/05)
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.
DEAZAPURINES USEFUL AS INHIBITORS OF JANUS KINASES
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Page/Page column 40-41; Sheet 1/9, (2010/11/26)
The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
