- HISTONE DEMETHYLASE INHIBITORS
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This disclosure relates to compounds that inhibit histone demethylase activity. In particular, the disclosure relates to compounds that inhibit histone lysine demethylase KDM5B, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions disclosed herein.
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Paragraph 0434-0436
(2017/09/08)
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- BICYCLIC HETEROCYCLE DERIVATIVES AS BROMODOMAIN INHIBITORS
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The invention relates to novel bicyclic heterocycle derivatives of formula (I) wherein Cy1,Cy2, R1,R2 and L have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are usefulas bromodomain inhibitors in the treatment or prevention of diseases or disorders where bromodomain inhibition is desired.
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Page/Page column 35; 36
(2017/01/23)
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- Copper-Catalyzed Reductive Cross-Coupling of Nonactivated Alkyl Tosylates and Mesylates with Alkyl and Aryl Bromides
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A copper-catalyzed reductive cross-coupling reaction of nonactivated alkyl tosylates and mesylates with alkyl and aryl bromides was developed. It provides a practical method for efficient and cost-effective construction of aryl-alkyl and alkyl-alkyl C=C bonds with stereocontrol from readily available substrates. When used in an intramolecular fashion, the reaction enables convenient access to various substituted carbo- or heterocycles, such as 2,3-dihydrobenzofuran and benzochromene derivatives.
- Liu, Jing-Hui,Yang, Chu-Ting,Lu, Xiao-Yu,Zhang, Zhen-Qi,Xu, Ling,Cui, Mian,Lu, Xi,Xiao, Bin,Fu, Yao,Liu, Lei
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supporting information
p. 15334 - 15338
(2016/02/18)
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- FURAN-2-CARBOXYLIC ACID DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
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This invention relates to a furan-2-carboxylic acid derivative capable of activating AMP-activated protein kinase (AMPK), which is useful for the prevention and treatment of metabolic syndromes including diabete, obesity, hyperlipidemia, hypercholesterole
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Page/Page column 8-9
(2010/11/30)
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- Processes for the preparation of (R)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol"
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The present invention provides various processes for the preparation of (R)-±-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol. These processes may be characterized by the following scheme:
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Page/Page column 26
(2010/11/25)
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- Novel processes for the preparation of (R)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol
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The present invention provides various processes for the preparation of (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol. These processes may be characterized by the following scheme:
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- Novel processes for the preparation or (R)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol
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The present invention provides various processes for the preparation of (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol. These processes may be characterized by the following scheme:
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- Synthesis of (+/-)--9-halogeno-2-methyl-1,2,3,4,4a,5,6,10b,11,12,12a-dodecahydronaphthoisoquinolines
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Treatment of 5-(2-arylethyl)-1,2,3,4,5,6,7,8-octahydroisoquinolines with 48percent HBr resulted in isomerisation of the double bond and subsequent cyclisation at position 6 of the octahydroisoquinoline ring system to give (+/-)--9-halogeno-2-methyl-1,2,3,4,4a,4b,5,6,10b,11,12,12a-dodecahydronaphtho2,1-f>isoquinolines.The products obtained represent novel analogues of aza-D-homoestranes.No reaction was observed with the corresponding 5,5-disubstituted octahydroisoquinolines.An X-ray crystallographic study of compound 10 (X = Br) is described.
- Patrick, Graham L.
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p. 1273 - 1280
(2007/10/02)
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