918538-05-3Relevant articles and documents
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies
Daelemans, Dirk,De Clercq, Erik,Gao, Ping,Ginex, Tiziana,Huang, Boshi,Jiang, Xiangyi,Kang, Dongwei,Liu, Xinyong,Luque, F. Javier,Pannecouque, Christophe,Zhan, Peng,Zhang, Jian
, p. 13604 - 13621 (2021/09/28)
Two series of new pyridyl-bearing fused bicyclic analogues designed to target the dual-tolerant regions of the non-nucleoside reverse transcriptase inhibitor (NNRTI)-binding pocket were synthesized and evaluated for their anti-HIV activities. Several comp
2 - amino-pyrrolo [1, 2 - f] [1, 2, 4] triazine compounds, synthetic method and application
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Paragraph 0066; 0075; 0076, (2017/07/01)
The invention discloses 2-aminopyrrolo[1,2-f][1,2,4]triazine compounds, and a synthesis method and application thereof, particularly 2-aminopyrrolo[1,2-f][1,2,4]triazine compounds, or pharmaceutically acceptable salts, hydrate, solvate or prodrug thereof.
Substituted heteroaryl compounds and compositions and uses thereof
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, (2017/12/27)
The invention provides a substituted heteroaryl compound and a composition thereof, and applications of the compound and the composition. The compound is a compound as shown in a formula I, or stereoisomer, tautomer, oxynitride, solvate, metabolite, pharmaceutically-acceptable salt or prodrug of the compound as shown in the formula I. The invention also provides a pharmaceutical composition containing the above-mentioned compound; and the above-mentioned compound and the pharmaceutical composition are capable of adjusting the activity of JAK kinases and are applied in prevention, treatment, therapy and alleviation of JAK kinase mediated diseases or disorders.
Heterocyclic amines Hedgehog signal pathway inhibitor
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, (2017/10/06)
The invention relates to the field of biological medicine, in particular to a heterocyclic amine compound and an application thereof, namely a general formula (I) compound and acceptable salt in the pharmaceutical field. The compound can be used in the Hedgehog signal transduction inhibitor application and various medical applications (please see the formula in the specification). The invention further relates to a preparation method with the general formula (I).
Synthesis and medical application of pyrrolo-[2,1-f] [1,2,4] triazine mother nucleus compound
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, (2017/07/31)
The invention discloses a synthesis and medical application of pyrrolo-[2,1-f] [1,2,4] triazine mother nucleus compound. The compound belongs to a novel-structure compound. The synthesis method is high in operating safety, mild in reaction condition and suitable for industrial production. The activity and the selectivity of BTK kinase and the in-vitro proliferation activity of a leukemia cell line are test, it is verified that the compound has the selective and irreversible inhibition effect on the BTK kinase, and has the different-degree inhibition effect on leukemia cells. According to measurement, the compound also has the good anti-arthritic activity on a collagen-induced arthritis (rCIA) model. The pyrrolo-[2,1-f] [1,2,4] triazine mother nucleus compound can be used for preparing medicine for treating arthritis and leukemia.
MECHANISTIC TARGET OF RAPAMYCIN SIGNALING PATHWAY INHIBITORS AND THERAPEUTIC APPLICATIONS THEREOF
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, (2018/04/11)
Selective mTOR inhibitors of formulas (I)-(III), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from abnormal cell growth, functions, or behaviors mediated by an mTOR kinase and/or one or more PI3K enzyme, are provided. Such diseases and disorder include cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
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, (2016/12/22)
The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of a JAK-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of JAK-mediated disease.
Design, synthesis, and evaluation of pyrrolo[2,1-f][1,2,4]triazine derivatives as novel hedgehog signaling pathway inhibitors
Xin, Minhang,Zhang, Liandi,Tang, Feng,Tu, Chongxing,Wen, Jun,Zhao, Xinge,Liu, Zhaoyu,Cheng, Lingfei,Shen, Han
, p. 1429 - 1440 (2014/03/21)
A novel series of Hh signaling pathway inhibitors were designed by replacing the pyrimidine skeleton of our earlier reported lead compound 1 with pyrrolo[2,1-f][1,2,4]triazine scaffold. Starting from this new scaffold, SAR exploration was investigated based on structural modification on A-ring, C-ring and D-ring. And several much potent compounds were studies in vivo to profile their pharmacokinetic properties. Finally, optimization leads to the identification of compound 19a, a potent Hh signaling pathway inhibitor with superior potency in vitro and satisfactory pharmacokinetic properties in vivo.
PYRROLOTRIAZINE KINASE INHIBITORS
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, (2011/04/19)
The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS AND METHODS OF TREATING KINASE-ASSOCIATED CONDITIONS THEREWITH
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Page/Page column 15, (2008/06/13)
The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one ki