40788-04-3Relevant academic research and scientific papers
Scalable Approach to Fluorinated Heterocycles with Sulfur Tetrafluoride (SF4)
Ahunovych, Volodymyr,Boretskyi, Andrii,Bugera, Maksym,Klipkov, Anton A.,Mykhailiuk, Pavel K.,Razhyk, Bohdan,Semenov, Sergey,Tarasenko, Karen,Trofymchuk, Serhii
, p. 12181 - 12198 (2021/09/13)
A general approach to fluorinated (hetero)aromatic derivatives is elaborated. The key reaction is a deoxofluorination of substituted acetophenones with sulfur tetrafluoride (SF4). In contrast to previous deoxofluorination methods, this transformation is fast, scalable (up to 70 g), and high-yielding. More than 100 novel or previously hardly accessible fluorinated heterocycles, interesting for medicinal chemistry and agrochemistry, were synthesized.
Design, Synthesis, Dynamic Docking, Biochemical Characterization, and in Vivo Pharmacokinetics Studies of Novel Topoisomerase II Poisons with Promising Antiproliferative Activity
Arencibia, Jose M.,Brindani, Nicoletta,Franco-Ulloa, Sebastian,Nigro, Michela,Kuriappan, Jissy Akkarapattiakal,Ottonello, Giuliana,Bertozzi, Sine Mandrup,Summa, Maria,Girotto, Stefania,Bertorelli, Rosalia,Armirotti, Andrea,De Vivo, Marco
, p. 3508 - 3521 (2020/04/30)
We previously reported a first set of hybrid topoisomerase II (topoII) poisons whose chemical core merges key pharmacophoric elements of etoposide and merbarone, which are two well-known topoII blockers. Here, we report on the expansion of this hybrid mol
CYCLOPROPANECARBOXAMIDO-SUBSTITUTE AROMATIC COMPOUNDS AS ANTI-TUMOR AGENTS
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Paragraph 0434; 0435, (2015/07/22)
Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
CYCLOPROPANECARBOXAMIDO-SUBSTITUTE AROMATIC COMPOUNDS AS ANTI-TUMOR AGENTS
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Page/Page column 93, (2014/01/17)
Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
Tricyclic Compounds As mPGES-1 Inhibitors
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Page/Page column 35, (2012/05/07)
The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
NEW CARBONYLATED (AZA)CYCLOHEXANES AS DOPAMINE D3 RECEPTOR LIGANDS
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Page/Page column 79, (2008/06/13)
The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.
QUINAZOLIN-4-ONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Page/Page column 36, (2008/06/13)
The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
A Novel Carbonyl to CF2 Transformation Using BrF3
Rozen, Shlomo,Mishani, Eyal,Bar-Haim, Arie
, p. 2918 (2007/10/02)
This work demonstrates that BrF3 is very efficient in converting various carbonyls through their azines, oxime methyl ethers, or various hydrazones into the corresponding CF2 moiety.
Substituted anilides as anti-androgens
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, (2008/06/13)
This application relates to certain 4'-substituted and to 3',4'-disubstituted anilides, to methods for their preparation and to methods for their use as anti-androgens.
Antiandrogenic agents and method for the treatment of androgen dependent disease states
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, (2008/06/13)
This application relates to certain 4''-substituted and to 3'',4''-disubstituted anilides, to methods for their preparation and to methods for their use as antiandrogens. These substituted anilides are useful in the treatment of androgen dependent disease states, such as benign prostatic hypertrophy, hirsutism, acne and the like.
