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Discovery and Evaluation of Pyrazolo[3,4- d ]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2019 Dec 11; Vol. 11 (10), pp. 1863-1868. Date of Electronic Publication: 2019 Dec 11 (Print Publication: 2020). - Publication Year :
- 2019
-
Abstract
- The identification and lead optimization of a series of pyrazolo[3,4- d ]pyridazinone derivatives are described as a novel class of potent irreversible BTK inhibitors, resulting in the discovery of compound 8 . Compound 8 exhibited high potency against BTK kinase and acceptable PK profile. Furthermore, compound 8 demonstrated significant in vivo efficacy in a mouse-collagen-induced arthritis (CIA) model.<br />Competing Interests: The authors declare no competing financial interest.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 11
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 33062165
- Full Text :
- https://doi.org/10.1021/acsmedchemlett.9b00395