13603-45-7Relevant articles and documents
COMPOUNDS FOR TREATING HUNTINGTON'S DISEASE
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Page/Page column 188, (2019/01/06)
The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted bicyclic heteroaryl compounds of Formula (I), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
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Page/Page column 50; 51, (2015/02/02)
This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatmen
ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
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Page/Page column 48, (2014/07/22)
This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. Epigenetic modifications play an important role in the regulation of many cellular processes including cell proliferation, differentiation, and cell survival. Global epigenetic modifications are common in cancer, and include global changes in DNA and/or histone methylation, dysregulation of non-coding RNAs and nucleosome remodeling leading to aberrant activation or inactivation of oncogenes, tumor suppressors and signaling pathways.
Syntheses of 4- and 6-substituted thiazolo[4,5-c]pyridines
Huang, Yuhua,Bennett, Frank,Girijavallabhan, Vinay,Alvarez, Carmen,Chan, Tze-Ming,Osterman, Rebecca,Senior, Mary,Kwong, Cecil,Bansal, Namita,George Njoroge,MacCoss, Malcolm
scheme or table, p. 2800 - 2802 (2010/07/04)
A general synthetic approach to 4,6-substituted thiazole[4,5-c]pyridines, involving a novel one-pot thiol deprotection-cyclization key step, is described.
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 3. Discovery of a novel series of N-alkyl-N-[(fluorophenoxy)benzyl]-N'-arylureas with weak toxicological effects on adrenal glands
Tanaka, Akira,Terasawa, Takeshi,Hagihara, Hiroyuki,Ishibe, Noriko,Sawada, Masae,Sakuma, Yuri,Hashimoto, Masaharu,Takasugi, Hisashi,Tanaka, Hirokazu
, p. 4408 - 4420 (2007/10/03)
A series of N-alkyl-N-[(fluorophenoxy)benzyl]-N'-arylureas were prepared and evaluated for their ability to inhibit intestinal acyl-CoA:cholesterol O- acyltransferase and to inhibit accumulation of cholesteryl esters in macrophages in vitro. In vivo hypocholesterolemic activity was assessed in cholesterol-fed rats by oral administration as a dietary admixture and/or by gavage in a PEG400 vehicle. Modification of the alkyl substituent on the N'- aryl moiety and on the urea nitrogen significantly influenced macrophage assay in vitro. Toxicological study revealed a distinct relationship between macrophage assay and the toxicity observed in adrenal glands of rabbits treated with representatives of this series of compounds. Investigations utilizing the macrophage assay as an indicator for adrenal toxicity led to the identification of compounds 1g (FR190809) and 1k (FR186485, or FR195249 as its hydrochloride salt) as potent, nonadrenotoxic, orally efficacious ACAT inhibitors irrespective of the administration method.
Platelet activating factor antagonists
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, (2008/06/13)
Platelet activating factor antagonists of formula (I): STR1 wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C1 -C4 alkyl, C1 -C4 alkoxy, aryl (C1 -C4) alkoxy, fluoro (C1 -C4) alkoxy, C1 -C4 alkylthio, C1 -C4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring; R1 and R2 are each independently H or C1 -C6 alkyl, or R1 and R2 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C1 -C4 alkyl) piperazinyl or N-(C2 -C4 alkanoyl)-piperazinyl group; or R2 is H or C1 -C4 alkyl and R1 is CN, C3 -C7 cycloalkyl, aryl, heteroaryl or a C1 -C4 alkyl group substituted by one or more substituents selected from C3 -C7 cycloalkyl, C1 -C4 alkoxycarbonyl, aryl or heteroaryl; Z is selected from C1 -C6 alkoxy, aryl (C1 -C4) alkoxy, hydroxy, and --NR4 R5 wherein each of R4 and R5 is independently H or C1 -C6 alkyl, or R4 and R5 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl or N-(C1 -C4 alkyl) piperazinyl group; Y is 1,4 phenylene or pyridine-2,5-diyl, and X is a 5 or 6 membered aromatic heterocyclic group containing one or more nitrogen atoms in its ring; which ring may be fused to a benzene ring or to a further 5- or 6-membered aromatic heterocyclic ring containing one or more nitrogen atoms, at least one of said heterocyclic rings optionally also containing an oxygen or sulphur atom, and being optionally substituted with one or more substituents selected from C1 -C4 alkyl, C1 -C4 alkoxy, halo, CF3 and CN; and their pharmaceutically acceptable salts.
1,4-dihydropyridine derivatives
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, (2008/06/13)
The invention provides compounds of the formula STR1 and pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by halo; R1 is C1 -C4 alkyl; is hydrogen, C5 -C7 cycloalkyl, benzyl
Pyrido[3,4-e]-1,2,4-triazines and related heterocycles as potential antifungal agents
Reich,Fabio,Lee,Kuck,Testa
, p. 2474 - 2485 (2007/10/02)
The preparation and biological activities of a series of pyrido[3,4-e]-1,2,4-triazines, 1,2,4-triazino[5,6-c]quinolines, and related fused triazines are described. Methyl, amino, and acylamino substituents were placed in the pyridyl ring of the former system. Other structural modifications included various alkyl, cycloalkyl, substituted phenyl, and heterocyclic groups in the 3-position of these ring systems. In agar dilution assays, actives in this series inhibited strains of Candida, Aspergillus, Mucor, and Trychophyton species at MIC's of ≤ 16 μg/mL.