专利号:US-5866723-A 优先权日:1991-09-25 标 题 :Benzoyl derivatives and synthesis thereof 发明人:HAMPER BRUCE C; LESCHINSKY KINDRICK L 权利人:MONSANTO CO 摘要:The present invention relates to novel 4-halo-2-fluoro-5-alkylbenzoyl compounds and their methods of manufacture. These compounds are useful for the preparation of agricultural chemicals and medicines, particularly as intermediates for an active class of aryl-haloalkylpyrazole and aryl alkylsulfonylpyrazole herbicides.
专利号:US-9771356-B2 优先权日:2012-09-21 标题 :Inhibitors of beta-hydroxylase for treatment of cancer 发明人:WANDS JACK R; DE LA MONTE SUZANNE; AIHARA ARIHIRO; OLSEN MARK JON; THOMAS JOHN-MICHAEL 权利人:RHODE ISLAND HOSPITAL; UNIV MIDWESTERN 摘要:The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydroxylase (e.g., Asparatyl (asparaginyl) β-hydroxylase (ASPH)), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.
专利号:US-11279687-B2 优先权日:2010-09-03 标题:Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; YUEN PO-WAI 权利人:VALO HEALTH INC; GENENTECH INC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An embodiment of the invention is the provision of a compound of Formula IIIA.
专利号:US-4369322-A 优先权日:1978-12-15 标 题 :Process for the production of substituted acetonitriles 发明人:SCHALKE PETER; KLEEMANN AXEL 权利人:DEGUSSA 摘要:The known synthesis for the production of aromatic substituted acetonitriles by reaction of aromatic substances with cyanogen chloride in the gas phase is improved by feeding the starting materials in gaseous form and separated from each other into the reactor. The process can be used to synthesize in general aromatic and especially hetero-aromatic substituted acetonitrile.
专利号:US-9676721-B2 优先权日:2010-09-03 标题 :Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG 权利人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
专利号:US-9555039-B2 优先权日:2011-05-09 标题:Piperidine derivatives and compositions for the inhibition of nicotinamide phosphoribosyltransferase (NAMPT) 发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; KUNTZ JUDITH D; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG 权利人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; KUNTZ JUDITH D; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below: Formula (I)
[参考文献]: Chang Soon Huh, Et Al. Spectroscopic Identification Of Benzyl-Type Radicals Generated By Corona Discharge Of 2-Chloro-4-Fluorotoluene. J Chem Phys. 2012 May 7;136(17):174306.
合成参考文献
摘要:Tomás-Gamasa, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 37.