39229-33-9Relevant articles and documents
Novel bicyclic pyrazoles as potent ALK2 (R206H) inhibitors for the treatment of fibrodysplasia ossificans progressiva
Yamamoto, Hirofumi,Sakai, Naoki,Ohte, Satoshi,Sato, Tomohiro,Sekimata, Katsuhiko,Matsumoto, Takehisa,Nakamura, Kana,Watanabe, Hisami,Mishima-Tsumagari, Chiemi,Tanaka, Akiko,Hashizume, Yoshinobu,Honma, Teruki,Katagiri, Takenobu,Miyazono, Kohei,Tomoda, Hiroshi,Shirouzu, Mikako,Koyama, Hiroo
, (2021/03/01)
Mutant activin receptor-like kinase-2 (ALK2) is associated with the pathogenesis of fibrodysplasia ossificans progressiva, making it an attractive target for therapeutic intervention. We synthesized a new series of bicyclic pyrazoles and evaluated their mutant ALK2 enzyme inhibitory activities, leading to the identification of 8 as the most potent inhibitor. This compound showed moderate microsomal metabolic stability and human ether-a-go-go related gene (hERG) safety. In C2C12 cells carrying mutant ALK2 (R206H), 8 efficiently inhibited the bone morphogenetic protein (BMP)-induced alkaline phosphatase activity.
Pyrazolopyridine compound and use thereof
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Paragraph 0397; 0399; 0400, (2018/11/03)
The present invention relates to a pyrazolopyridine compound and use thereof, and further relates to a pharmaceutical composition comprising the pyrazolopyridine compound. The pyrazolopyridine compound or the pharmaceutical composition can be used as a so
One-pot, regiospecific assembly of (E)-benzamidines from δ- and γ-amino acids via an intramolecular aminoquinazolinone rearrangement
Schroeder, Chad E.,Neuenswander, Sarah A.,Yao, Tuanli,Aubé, Jeffrey,Golden, Jennifer E.
supporting information, p. 3950 - 3955 (2016/06/06)
The efficient generation of novel, N-linked benzamidines resulting from a regiospecific rearrangement of quinazolinones is described. This methodology study explored reaction parameters including the effect of changing solvent and temperature, as well as varying electronic substituents on the structural core. The transformation was extensively optimized in terms of reaction conditions and scope, resulting in a protocol that consistently affords diversely functionalized amidines in high yield. The process permits regional structural derivatization that was previously inaccessible, and the multistep process was also reduced to a telescoped, five-step sequence that efficiently affords pharmacologically unique (E)-benzamidoamidines from N-BOC protected γ- and δ-amino acids.