876343-82-7Relevant academic research and scientific papers
CHEMICAL COMPOUNDS
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Paragraph 0384-0386; 0450, (2021/04/02)
The present disclosure describes novel compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the disclosure have activity as Janus kinase (JAK) inhibitors and are useful in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described herein are methods of treating inflammation, auto-immune diseases, cancer, and other conditions susceptible to inhibition of JAK by administering a compound herein described.
CHEMICAL COMPOUNDS
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Paragraph 0115-0117, (2020/12/01)
The present invention describes novel compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the invention have activity as Janus kinase (JAK) inhibitors and are useful in the in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described herein are methods of treating inflammation, auto-immune diseases, cancer, and other conditions susceptible to inhibition of JAK by administering a compound herein described.
PYRROLO[2,3-B]PYRIDINE COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER
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Paragraph 00153; 00165, (2019/03/05)
The present application relates to a compound of Formula I, or a salt, hydrate or solvate thereof, as defined herein. The present compounds are found to have pharmacological effects, particularly at MRCK. Further provided are pharmaceutical compositions comprising said compounds. The present invention also relates to the use of these compounds as therapeutic agents, in particular, for the treatment and/or prevention of proliferative diseases, such as cancer.
Design and synthesis of potent RSK inhibitors
Jain, Rama,Mathur, Michelle,Lan, Jiong,Costales, Abran,Atallah, Gordana,Ramurthy, Savithri,Subramanian, Sharadha,Setti, Lina,Feucht, Paul,Warne, Bob,Doyle, Laura,Basham, Stephen,Jefferson, Anne B.,Appleton, Brent A.,Lindvall, Mika,Shafer, Cynthia M.
, p. 3197 - 3201 (2018/10/08)
Utilizing the already described 3,4-bi-aryl pyridine series as a starting point, incorporation of a second ring system with a hydrogen bond donor and additional hydrophobic contacts yielded the azaindole series which exhibited potent, picomolar RSK2 inhib
PYRROLO[2,3-C]PYRIDINES AND RELATED ANALOGS AS LSD-1 INHIBITORS
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Paragraph 0201; 0204; 0205, (2018/12/13)
The present disclosure provides compounds represented by Formula I and II: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, X, W, Y, and Z are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I and II for use to treat a condition or disorder responsive to LSD1 inhibition such as cancer.
TAM KINASE INHIBITORS
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, (2018/11/10)
Described herein are compounds, methods of making such compounds, compositions (e.g., pharmaceutical compositions/medicaments) that include such compounds, and methods of using such compounds to treat diseases, such as cancer.
Design and synthesis of tricyclic jak3 inhibitors with picomolar affinities as novel molecular probes
Gehringer, Matthias,Pfaffenrot, Ellen,Bauer, Silke,Laufer, Stefan A.
, p. 277 - 281 (2014/04/03)
The Janus kinase (JAK) signaling pathway is of particular importance in the pathology of inflammatory diseases and oncological disorders, and the inhibition of Janus kinase 3 (JAK3) with small molecules has proven to provide therapeutic immunosuppression. A novel class of tricyclic JAK inhibitors derived from the 3-methyl-1,6-dihydrodipyrrolo[2,3-b:2',3'-d]pyridine scaffold was designed based on the tofacitinib-JAK3 crystal structure by applying a rigidization approach. A convenient synthetic strategy to access the scaffold via an intramolecular Heck reaction was developed, and a small library of inhibitors was prepared and characterized using in vitro biochemical as well as cellular assays. IC50 values as low as 220 pm could be achieved with selectivity for JAK3 over other JAK family members. Both activity and selectivity were confirmed in a cellular STAT phosphorylation assay, providing also first-time data for tofacitinib. Our novel inhibitors may serve as tool compounds and useful probes to explore the role of JAK3 inhibition in pharmacodynamics studies.
Discovery of a novel azaindole class of antibacterial agents targeting the ATPase domains of DNA gyrase and Topoisomerase IV
Manchester, John I.,Dussault, Daemian D.,Rose, Jonathan A.,Boriack-Sjodin, P. Ann,Uria-Nickelsen, Maria,Ioannidis, Georgine,Bist, Shanta,Fleming, Paul,Hull, Kenneth G.
scheme or table, p. 5150 - 5156 (2012/09/07)
We present the discovery and optimization of a novel series of bacterial topoisomerase inhibitors. Starting from a virtual screening hit, activity was optimized through a combination of structure-based design and physical property optimization. Synthesis
PYRROLOPYRIDINES AS KINASE INHIBITORS
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Page/Page column 59, (2009/09/04)
Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Formula, (I).
Pyrrolopyridine kinase inhibiting compounds
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Page/Page column 77-78, (2010/11/27)
Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least one of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mek1, PDK-1, GSK3β, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-1R, Ron, Met, and KDR kinases in animals, including humans, for the treatment and/or prevention of various diseases and conditions such as cancer.
