194785-79-0Relevant academic research and scientific papers
SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
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Page/Page column 61, (2012/02/01)
This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
Design and optimization of potent and orally bioavailable tetrahydronaphthalene raf inhibitors
Gould, Alexandra E.,Adams, Ruth,Adhikari, Sharmila,Aertgeerts, Kathleen,Afroze, Roushan,Blackburn, Christopher,Calderwood, Emily F.,Chau, Ryan,Chouitar, Jouhara,Duffey, Matthew O.,England, Dylan B.,Farrer, Cheryl,Forsyth, Nancy,Garcia, Khristofer,Gaulin, Jeffery,Greenspan, Paul D.,Guo, Ribo,Harrison, Sean J.,Huang, Shih-Chung,Iartchouk, Natalia,Janowik, Dave,Kim, Mi-Sook,Kulkarni, Bheemashankar,Langston, Steven P.,Liu, Jane X.,Ma, Li-Ting,Menon, Saurabh,Mizutani, Hirotake,Paske, Erin,Renou, Christelle C.,Rezaei, Mansoureh,Rowland, R. Scott,Sintchak, Michael D.,Smith, Michael D.,Stroud, Stephen G.,Tregay, Ming,Tian, Yuan,Veiby, Ole P.,Vos, Tricia J.,Vyskocil, Stepan,Williams, Juliet,Xu, Tianlin,Yang, Johnny J.,Yano, Jason,Zeng, Hongbo,Zhang, Dong Mei,Zhang, Qin,Galvin, Katherine M.
supporting information; experimental part, p. 1836 - 1846 (2011/05/30)
Inhibition of mutant B-Raf signaling, through either direct inhibition of the enzyme or inhibition of MEK, the direct substrate of Raf, has been demonstrated preclinically to inhibit tumor growth. Very recently, treatment of B-Raf mutant melanoma patients with a selective B-Raf inhibitor has resulted in promising preliminary evidence of antitumor activity. This article describes the design and optimization of tetrahydronaphthalene-derived compounds as potent inhibitors of the Raf pathway in vitro and in vivo. These compounds possess good pharmacokinetic properties in rodents and inhibit B-Raf mutant tumor growth in mouse xenograft models.
PREPARATION OF AMINOTETRALIN COMPOUNDS
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Page/Page column 12, (2010/08/08)
The present invention relates to synthetic processes for preparation of aminotetralin compounds with kinase inhibitory activity. The invention also provides synthetic intermediates useful in the processes of the invention.
Synthesis and antifungal activities of novel 2-aminotetralin derivatives
Yao, Bin,Ji, Haitao,Cao, Yongbin,Zhou, Youjun,Zhu, Jü,Lü, Jiaguo,Li, Yaowu,Chen, Jun,Zheng, Canhui,Jiang, Yuanying,Liang, Rongmei,Tang, Hui
, p. 5293 - 5300 (2008/03/18)
Novel 2-aminotetralin derivatives were synthesized as antifungal agents. The 2-aminotetralin scaffold was chemically designed to mimic the tetrahydroisoquinoline ring of the lead molecule described before. Their antifungal activities were evaluated in vitro by measuring the minimal inhibitory concentrations (MICs). Compounds 10a, 12a, 12c, 13b, and 13d are more potent than fluconazole against seven testing human fungal pathogens. Compound 10b exhibits much higher antifungal activities against all of the four fluconazole-resistant clinic Candida albicans strains than the control drugs including amphotericin B, terbinafine, ketoconazole, and itraconazole. The mode of action of some compounds to the potential receptor lanosterol 14α-demethylase (CYP51) was investigated by molecular docking. The studies presented here provide a new structural type for the development of novel antifungal compounds. Furthermore, 10b was evaluated in vivo by a rat vaginal candidiasis model, and it was found that 10b significantly decreases the number of fungal colony counts.
The practical synthesis of a uterine relaxant, Bis( 2-{[(2S)-2-({(2R)-2-hydroxy-2-[4-hydroxy-3-(2-hydroxyethyl) -phenyl]ethyl}amino) -1,2,3,4-tetrahydronaphthalen-7-yl]oxy}-N,N-dimethylacetamide) sulfate (KUR-1246)
Yanagi, Takashi,Kikuchi, Ken,Takeuchi, Hideki,Ishikawa, Takehiro,Nishimura, Toshihiro,Yamamoto, Iwao
, p. 1018 - 1023 (2007/10/03)
The synthetic route for a uterine relaxant, bis(2-{[ (2S)-2-({(2R)-2-hydroxy-2-[4-hydroxy-3- (2-hydroxyethyl)-phenyl]ethyl}amino) -1,2,3,4-tetrahydronaphthalen-7-y1]oxy}-N,N-dimethylacetamide) sulfate (KUR-1246), was established by the coupling of optically active components, the bromohydrin 14 and the amine 24. We now describe the practical synthesis of these two optically active components. Bromohydrin 14 was obtained by the asymmetric borane reduction of the prochiral phenacyl bromide 13 using a catalyst prepared from aluminum triethoxide and a chiral amino alcohol. The other optically active component 24 was prepared from (S)-AMT.
Process for the preparation of phenylethanolaminotetralins
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, (2008/06/13)
A process for the preparation of phenylethanolaminotetralins of formula STR1 wherein X is hydrogen, a halogen, a trifluoromethyl or a lower alkyl group and R° is hydrogen or a methyl group substituted by a carboxy or a lower carbalkoxy group, which compri
Aryloxypropanolaminotetralins, a process for their preparation and pharmaceutical compositions containing them
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, (2008/06/13)
Aryloxypropanolaminotetralins with beta-antagonist activity of the formula STR1 wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described.A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.
Conformationally Restricted and Conformationally Defined Tyramine Analogues as Inhibitors of Phenylethanolamine N-Methyltransferase
Ye, Qizhuang,Grunewald, Gary L.
, p. 478 - 486 (2007/10/02)
In a search for a selective inhibitor for the epinephrine synthesizing enzyme phenylethanolamine N-methyltransferase (PNMT; EC 2.1.1.28), phenolic 2-aminotetralins (12-15 as conformationally restricted analogues of tyramine) and phenolic benzobicyclo3.2.
