131885-33-1Relevant academic research and scientific papers
INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR KINASES
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Paragraph 001332, (2021/12/28)
Provided herein are heteroaryl inhibitors of fibroblast growth factor receptor kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
2, 4-DI-(NITROGEN CONTAINING GROUP) SUBSTITUTED PYRIMIDINE COMPOUND AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0232, (2018/07/29)
Provided are a 2, 4-di-(nitrogen containing group) substituted pyrimidine compound represented by a general formula (I), a pharmaceutically acceptable salt and a stereoisomer thereof, a preparation method thereof, and a use thereof in preparation of anti-tumor drugs. The compound having a structural feature shown in the general formula (I) can selectively suppress activity of mutant epidermal growth factor receptors (EGFR), including single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. The compound has a weak suppression effect on wild-type EFGR and a very high selectivity, and thus it has a potential to be used in preparation of drugs for treating EGFR mutant tumors, especially non-small cell lung cancer (NSCLC) comprising a T790M EGFR mutation.
BENZIMIDAZOLONE COMPOUNDS HAVING 5-HT4 RECEPTOR AGONISTIC ACTIVITY
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Page/Page column 60, (2010/02/11)
This invention provides a compound of the formula (I) or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointe
Characterization of a new class of selective nonsteroidal progesterone receptor agonists
Dong, Yu,Roberge, Jacques Y.,Wang, Zhaoqing,Wang, Xiaodong,Tamasi, Joseph,Dell, Vanessa,Golla, Rajasree,Corte, James R.,Liu, Yalei,Fang, Tianan,Anthony, Monique N.,Schnur, Dora M.,Agler, Michele L.,Dickson Jr., John K.,Lawrence, R. Michael,Prack, Margaret M.,Seethala, Ramakrishna,Feyen, Jean H.M.
, p. 201 - 217 (2007/10/03)
The identification of a new series of selective nonsteroidal progesterone receptor (PR) agonists is reported. Using a high-throughput screening assay based on the measurement of transactivation of a mouse mammary tumor virus promoter-driven luciferase reporter (MMTV-Luc) in human breast cancer T47D cells, a benzimidazole-2-thione analog was identified. Compound 1 showed an apparent EC50 of 53nM and efficacy of 93% with respect to progesterone. It binds to PR with high affinity (Ki=89nM), but had no or very low affinity for other steroid hormone receptors. Structure-activity relationship studies of a series of benzimidazole-2-thione analogs revealed critical positions for high PR binding affinity and transactivation potency as well as receptor selectivity, as exemplified by 25. Compound 25 binds to human PR with high affinity (Ki=28nM) and had at least >1000-fold selectivity for PR versus other steroid receptors. Molecular modeling studies suggested that these agonists overlap favorably with progesterone in the ligand-binding domain of PR. In T47D cells, compound 25 acted as a full agonist in the MMTV-Luc reporter assay, as well as in the induction of endogenous alkaline phosphatase activity with apparent EC50 values of 4 and 9nM, respectively. In the immature rat model, compound 25 provided a significant suppression of estrogen-induced endometrium hypertrophy as measured by luminal epithelial height. In contrast, compound 25 was inactive in the luteinizing hormone release assay in young ovariectomized rats. These benzimidazole-2-thione analogs constitute a new series of nonsteroidal PR agonists with an excellent steroid receptor selectivity profile. The differential activities observed in the in vivo progestogenic assays in rat models suggest that these analogs can act as selective PR modulators.
3-Phenyl-substituted imidazo[1,5-a]quinoxalin-4-ones and imidazo[1,5- a]quinoxaline ureas that have high affinity at the GABA(A)/benzodiazepine receptor complex
Jacobsen, E. Jon,Stelzer, Lindsay S.,Belonga, Kenneth L.,Carter, Donald B.,Im, Wha Bin,Sethy, Vimala H.,Tang, Andrew H.,Von Voigtlander, Philip F.,Petke, James D.
, p. 3820 - 3836 (2007/10/03)
A series of imidazo[1,5-a]quinoxalin-4-ones and imidazo[1,5- a]quinoxaline ureas containing substituted phenyl groups at the 3-position was developed. Compounds within the imidazo-[1,5-a]quinoxaline urea series had high affinity for the GABA(A)/benzodiaze
