1134327-98-2Relevant academic research and scientific papers
Design, Synthesis, and Biological Evaluation of Imidazo[1,2- a]pyridine Derivatives as Novel PI3K/mTOR Dual Inhibitors
Yu, Ya'Nan,Han, Yuqiao,Zhang, Fupo,Gao, Zhenmei,Zhu, Tong,Dong, Suzhen,Ma, Mingliang
, p. 3028 - 3046 (2020/04/09)
PI3K-Akt-mTOR signaling pathway has been validated as an effective targeting pathway for cancer therapy. However, no PI3K/mTOR dual inhibitor has been approved by the FDA yet. Therefore, it is still essential to discover a candidate with good efficacy and low toxicity. In our design, a series of imidazo[1,2-a]pyridine derivatives had been synthesized and subjected to activity assessment in vitro and in vivo. 15a was proved to be a potent PI3K/mTOR dual inhibitor with excellent kinase selectivity, modest plasma clearance, and acceptable oral bioavailability. Besides, 15a displayed significant inhibition of tumor growth in HCT116 and HT-29 xenografts without obvious effect on body weight.
SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
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Paragraph 000624, (2019/06/05)
The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
Substituted heteroaryl compounds and compositions and uses thereof (by machine translation)
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Paragraph 1722; 1727; 1728; 1729; 1730, (2019/06/07)
The invention discloses substituted heteroaryl compounds and compositions thereof and their use. The compounds of formula (I) compound or type shown in (I) a compound represented by stereo isomers, tautomers, nitrogen oxide, solvate, metabolite, pharmaceutically acceptable salt or its prodrug. The invention also provides a pharmaceutical composition, the compounds and pharmaceutical compositions can be regulated protein kinase, particularly Aurora kinase and JAK kinase activity, for the prevention, treatment, treatment and reduce protein kinase, in particular JAK kinase activity mediated diseases or disorders. (by machine translation)
IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS HISTONE DEMETHYLASE INHIBITORS
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Paragraph 0113-0114, (2018/01/15)
This disclosure relates, inter alia, to compounds that inhibit histone demethylase activity. In particular, the disclosure relates to compounds that inhibit histone lysine demethylase KDM5B, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions disclosed herein.
SOLID FORMS OF BICYCLIC HETEROCYCLIC DERIVATIVES AS PDGF RECEPTOR MEDIATORS
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Page/Page column 40, (2014/09/16)
The present invention provides novel solid forms of pharmaceutically active agents and therapeutic uses thereof. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
BICYCLIC HETEROCYCLE DERIVATIVES FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION
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Page/Page column 121; 122, (2013/03/28)
Bicyclic heterocyclic derivatives of formula (I) useful in inhibiting PDGF receptor mediated biological activity. Wherein A is and R1, R1a, R2, R3, R4, R5, R6 and X are as defined herein.
COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
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Paragraph 0434, (2013/03/26)
The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases.
COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
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Paragraph 0432, (2013/03/26)
The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases.
COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
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Page/Page column 86-87, (2013/03/28)
The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases.
COMPOUNDS AND COMPOSITIONS AS PDGFR KINASE INHIBITORS
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Page/Page column 70; 77, (2013/03/28)
The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase
