Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type i Half Binding Mode
General control nonderepressible 2 (GCN2) is a master regulator kinase of amino acid homeostasis and important for cancer survival in the tumor microenvironment under amino acid depletion. We initiated studies aiming at the discovery of novel GCN2 inhibit
Fujimoto, Jun,Kurasawa, Osamu,Takagi, Terufumi,Liu, Xin,Banno, Hiroshi,Kojima, Takuto,Asano, Yasutomi,Nakamura, Akito,Nambu, Tadahiro,Hata, Akito,Ishii, Tsuyoshi,Sameshima, Tomoya,Debori, Yasuyuki,Miyamoto, Maki,Klein, Michael G.,Tjhen, Richard,Sang, Bi-Ching,Levin, Irena,Lane, Scott Weston,Snell, Gyorgy P.,Li, Ke,Kefala, Georgia,Hoffman, Isaac D.,Ding, Steve C.,Cary, Douglas R.,Mizojiri, Ryo
4-ETHYLNYLPYRIDINE DERIVATIVES USEFUL AS GCN2 INHIBITORS
The invention relates to compounds of formula I, wherein the substituents are as defined in more detail in the description. The compounds are potent inhibitors of GCN2 and have excellent pharmacokinetic properties. Compounds are useful for the treatment or prevention of various conditions, especially cancer. The invention further relates to pharmaceutical compositions comprising the compounds of the invention and uses of the compounds and compositions.
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Page/Page column 97; 99-100
(2021/12/31)
ACLY INHIBITORS AND USES THEREOF
The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.
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Paragraph 00242
(2020/06/05)
HETEROCYCLIC COMPOUND
Provided is a heterocyclic compound that may have a GCN2 inhibitory action, and is expected to be useful for the prophylaxis or treatment of GCN2 associated diseases including cancer and the like. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
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Paragraph 0904; 0905; 0906
(2019/06/17)
OXAZEPINE DERIVATIVES HAVING TNAP INHIBITORY ACTIVITY
The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.
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Page/Page column 95-97
(2018/07/29)
SULFONAMIDE COMPOUNDS HAVING TNAP INHIBITORY ACTIVITY
The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.
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Page/Page column 143; 144; 145
(2018/07/29)
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