- 4-Substituted quinazoline derivatives as novel EphA2 receptor tyrosine kinase inhibitors
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Erythropoietin-producing hepatocellular receptor tyrosine kinase subtype A2 (EphA2) is an attractive therapeutic target for suppressing tumor progression. In our efforts to discover novel small molecules to inhibit EphA2, a class of compound based on 4-substituted quinazoline containing 7-(morpholin-2-ylmethoxy) group was identified as a novel hit by high throughput screening campaign. Structural modification of parent quinazoline scaffolds by introducing substituents on aniline displayed potent inhibitory activities toward EphA2.
- Lim, Chae Jo,Oh, Kwang-Seok,Ha, Jae Du,Lee, Jeong Hyun,Seo, Ho Won,Chae, Chong Hack,Kim, Dae-Ghon,Lee, Mi-Jin,Lee, Byung Ho
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Read Online
- BIFUNCTIONAL MOLECULES CONTAINING AN E3 UBIQUITINE LIGASE BINDING MOIETY LINKED TO A BCL6 TARGETING MOIETY
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Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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Paragraph 00387; 00388
(2021/04/23)
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- PHARMACEUTICALLY ACTIVE PYRAZOLO-TRIAZINE AND/OR PYRAZOLO-PYRIMIDINE DERIVATIVES
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The present invention relates to pyrazolo [1,5 -a] [1,3,5 ]triazine and pyrazolo[1,5-a] pyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazo lo [1,5-a][1,3,5 ]triazine and pyrazolo [1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.
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Page/Page column 33; 57
(2019/11/04)
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- 2-Aryloxymethylmorpholine histamine H3 antagonists
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The synthesis and biological activity of a new series of 2-aryloxymethylmorpholine histamine H3 antagonists is described. The new compounds are high affinity histamine H3 ligands that penetrate the CNS and occupy the histamine H3 receptor in rat brain.
- Letavic, Michael A.,Keith, John M.,Ly, Kiev S.,Bonaventure, Pascal,Feinstein, Mark A.,Lord, Brian,Miller, Kirsten L.,Motley, S. Timothy,Nepomuceno, Diane,Sutton, Steven W.,Carruthers, Nicholas I.
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scheme or table
p. 5796 - 5799
(2009/11/30)
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- [2-ω-phenylalkyl)phenoxy]alkylamines: Synthesis and dual dopamine2 (D2) and 5-hydroxytryptamine2 (5-HT2) receptor antagonistic activities
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A series of [2-(ω-phenylalkyl)phenoxy]alkylamines was synthesized and their 5-hydroxytryptamine2 (5-HT2) and/or dopamine2 (D2) receptor antagonistic activities were examined in vitro. [2-(4- Phenylbutyl)phenoxy]
- Tanaka, Naoki,Goto, Riki,Ito, Rie,Hayakawa, Miho,Ogawa, Taketoshi,Fujimoto, Koichi
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p. 639 - 646
(2007/10/03)
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- Coumarin derivatives, their preparation and their use in the treatment of cerebrovascular disorders
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Compounds of formula (I): [in which: A is a group of formula (II) or (III): R1, R2 and R3 are hydrogen, lower alkyl or halogen; R4 is hydrogen, lower alkyl or aralkyl; R5 and R6 are hydrogen or lower alkyl; R7 a
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