152684-25-8Relevant articles and documents
HETERO-HALO INHIBITORS OF HISTONE DEACETYLASE
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Paragraph 223, (2017/01/26)
This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula I, II or any of Compounds 100-128 or any of those in Tables 2 or 3) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.
Aminoheteroaryl benzamides as kinase inhibitors
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Page/Page column 82; 83, (2016/02/15)
The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
NITROGENATED HETEROCYCLIC COMPOUND
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Paragraph 0741, (2015/03/28)
The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
HETEROCYCLIC COMPOUND
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Paragraph 0585, (2015/05/26)
The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the f
SELECTIVE HDAC1 AND HDAC2 INHIBITORS
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, (2014/05/20)
Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold
Jones, Eric D.,Vandegraaff, Nick,Le, Giang,Choi, Neil,Issa, William,MacFarlane, Katherine,Thienthong, Neeranat,Winfield, Lisa J.,Coates, Jonathan A.V.,Lu, Long,Li, Xinming,Feng, Xiao,Yu, Changjiang,Rhodes, David I.,Deadman, John J.
scheme or table, p. 5913 - 5917 (2010/11/18)
HIV integrase inhibitors based on a novel bicyclic pyrimidinone core is presented. Nine variations of the core scaffold are evaluated leading to optimization of the 6:6 core giving compound 48 with an EC50 of 3 nM against wild type HIV infected T-cells.
Discovery of novel benzimidazoles as potent inhibitors of TIE-2 and VEGFR-2 tyrosine kinase receptors
Hasegawa, Masaichi,Nishigaki, Naohiko,Washio, Yoshiaki,Kano, Kazuya,Harris, Philip A.,Sato, Hideyuki,Mori, Ichiro,West, Rob I.,Shibahara, Megumi,Toyoda, Hiroko,Wang, Liping,Nolte, Robert T.,Veal, James M.,Cheung, Mui
, p. 4453 - 4470 (2008/02/13)
We herein disclose a novel chemical series of benzimidazole-ureas as inhibitors of VEGFR-2 and TIE-2 kinase receptors, both of which are implicated in angiogenesis. Structure-activity relationship (SAR) studies elucidated a critical role for the N1 nitrogen of both the benzimidazole (segment E) and urea (segment B) moieties. The SAR results were also supported by the X-ray crystallographic elucidation of the role of the N1 nitrogen and the urea moiety when the benzimidazole-urea compounds were bound to the VEGFR-2 enzyme. The left side phenyl ring (segment A) occupies the backpocket where a 3-hydrophobic substituent was favored for TIE-2 activity.
Chemical compounds
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, (2008/06/13)
Benzimidazole derivatives, which are useful as TIE-2 and/or VEGFR2 inhibitors are described herein. The described invention also includes methods of making such benzimidazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
Synthetic Routes to Nitroamino Precursors of the Food Carcinogen 2-Amino-1-methyl-6-phenyl-1H-imidazopyridine and its 3-Methyl Isomer via Pd(0)-Catalysed Arylation
Linstroem, Stefan,Eriksson, Mikael,Grivas, Spiros
, p. 805 - 812 (2007/10/02)
The synthesis of the novel key intermediates 3-methylamino-2-nitro- and 2-methylamino-3-nitro-5-phenylpyridine, and some of their derivatives substituted in the benzene ring, from 5-bromonicotinic acid, 3-bromo-5-methoxypyridine, 2-chloro-3-nitropyridine, 2-amino-5-bromopyridine or 5-bromo-2-methoxypyridine is described.Palladium(0)-mediated arylation of bromopyridines with areneboronic acids was an essential step in the syntheses.