- DERIVATIVES OF 4-(IMIDAZO[L,2-A]PYRIDIN-3-YL)-N-(PYRIDINYL)PYRIMIDIN- 2-AMINE AS THERAPEUTIC AGENTS
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A novel class of heteroaryl compounds for use in the prevention and/or treatment of proliferative diseases and conditions including cancers. The compounds are considered to be capable of inhibiting cell proliferation by inhibiting the activity of FLT3 and its mutant forms and/or other protein kinases such as CDKs. The compounds have the general structure I:
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Paragraph 0083-0084; 0096-0097
(2021/01/29)
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- Double (amino-sulfur generation of formic acid ) - 1,3-propane diester compound and its synthetic method, pharmaceutical composition and use thereof
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The invention relates to a bis(aminodithioformate)-1,3-propane diester compound, and synthesis method thereof, a pharmaceutical composition containing the compound and a use, and especially relates to the use in preparing drugs for treating or preventing cancers. The compound is represented as the formula (I), wherein A is selected from substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic group, R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl alkyl or heteroaryl alkyl, or a substituted or unsubstituted heterocyclic ring formed together by the R1, the R2 and an N atom connected with the R1 and the R2.
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Paragraph 0312; 0368-0371
(2016/10/08)
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- 2,3-DISUBSTITUTED PYRIDINE COMPOUNDS AS TGF-BETA INHIBITORS AND METHODS OF USE
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The invention described herein comprises compounds of formula (IV) and a method of treating cancer comprising administering to a subject having cancer one of the compounds in conjunction with another therapeutic treatment of cancer. The compounds (IV) inhibit signaling by a member of the TGF-β superfamily such as Nodal or Activin.
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Paragraph 1302
(2015/11/27)
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- Inhibiting NF-κB-inducing kinase (NIK): Discovery, structure-based design, synthesis, structure-activity relationship, and co-crystal structures
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The discovery, structure-based design, synthesis, and optimization of NIK inhibitors are described. Our work began with an HTS hit, imidazopyridinyl pyrimidinamine 1. We utilized homology modeling and conformational analysis to optimize the indole scaffol
- Li, Kexue,McGee, Lawrence R.,Fisher, Ben,Sudom, Athena,Liu, Jinsong,Rubenstein, Steven M.,Anwer, Mohmed K.,Cushing, Timothy D.,Shin, Youngsook,Ayres, Merrill,Lee, Fei,Eksterowicz, John,Faulder, Paul,Waszkowycz, Bohdan,Plotnikova, Olga,Farrelly, Ellyn,Xiao, Shou-Hua,Chen, Guoqing,Wang, Zhulun
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p. 1238 - 1244
(2013/03/28)
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- THIOZOLIDINEDIONE DERIVATIVES AS P13 KINASE INHIBITORS
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Invented is a method of inhibiting the activity/function of PB kinases using thiozolidinedione derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of thiozolidinedione derivatives.
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Page/Page column 47
(2008/06/13)
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- Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110α inhibitors
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3-{1-[(4-Fluorophenyl)sulfonyl]-1H-pyrazol-3-yl}-2-methylimidazo[1,2-a]pyridine, 2a, was discovered in our chemical library as a novel p110α inhibitor with an IC50 of 0.67 μM, through screening in a scintillation proximity assay. Optimization o
- Hayakawa, Masahiko,Kaizawa, Hiroyuki,Kawaguchi, Ken-ichi,Ishikawa, Noriko,Koizumi, Tomonobu,Ohishi, Takahide,Yamano, Mayumi,Okada, Minoru,Ohta, Mitsuaki,Tsukamoto, Shin-ichi,Raynaud, Florence I.,Waterfield, Michael D.,Parker, Peter,Workman, Paul
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p. 403 - 412
(2008/02/05)
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