cas 1415314-22-5, 6-Chloro-8-iodo-[1,2,4]triazolo[1,5-a]pyridine | Articles data ｜lookchem

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1415314-22-5

Articles about 1415314-22-5Total 5 be found

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HETEROARYLS AND USES THEREOF
The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
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Paragraph 00396

(2015/08/03)

HETEROARYLS AND USES THEREOF
The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
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Paragraph 0547; 0549

(2015/09/22)

TRIAZOLOPYRIDINE COMPOUNDS
The present invention relates to the use of novel triazolopyridine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
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Page/Page column 21

(2012/12/14)

TRIAZOLOPYRIDINE COMPOUNDS
The present invention relates to the use of novel triazolopyridine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
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Page/Page column 37-38

(2013/02/28)

Rational design of highly selective spleen tyrosine kinase inhibitors
A novel approach to design selective spleen tyrosine kinase (Syk) inhibitors is described. Inhibition of spleen tyrosine kinase has attracted much attention as a mechanism for the treatment of autoimmune diseases such as asthma, rheumatoid arthritis, and SLE. Fostamatinib, a Syk inhibitor that successfully completed phase II clinical trials, also exhibits some undesirable side effects. More selective Syk inhibitors could offer safer, alternative treatments. Through a systematic evaluation of the kinome, we identified Pro455 and Asn457 in the Syk ATP binding site as a rare combination among sequence aligned kinases and hypothesized that optimizing the interaction between them and a Syk inhibitor molecule would impart high selectivity for Syk over other kinases. We report the structure-guided identification of three series of selective spleen tyrosine kinase inhibitors that support our hypothesis and offer useful guidance to other researchers in the field.
Lucas, Matthew C.,Goldstein, David M.,Hermann, Johannes C.,Kuglstatter, Andreas,Liu, Wenjian,Luk, Kin Chun,Padilla, Fernando,Slade, Michelle,Villase?or, Armando G.,Wanner, Jutta,Xie, Wenwei,Zhang, Xiaohu,Liao, Cheng
supporting information
p. 10414 - 10423
(2013/02/22)

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Chemical Properties

Density: 2.34±0.1 g/cm3(Predicted)
PKA: 0.35±0.30(Predicted)
PSA: 30.19000
LogP: 1.98730

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