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31181-53-0 1401685-43-5 1261799-90-9欧盟法规
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2-Amino-6-methylpyridine 2-methyl-3-pyridinamine 6-chloro-4-methyl-3-nitropyridine 6-methyl-5-nitropyridin-2-ol 3-fluoro-2-methylpyridine 1-oxide 3-fluoropyridine-2-carbaldehyde oxime 3-fluoropyridine-2-carbaldehyde 6-氯-2-甲基-3-硝基吡啶置于tetrafluoroboric Acid,亚硝酸乙酯,Palladium On Carbon,氢气体系中,化学反应生成3-氟-2-甲基吡啶
参考文献:Synthesis Of Some Fluorine-Containing Pyridinealdoximes Of Potential Use For The Treatment Of Organophosphorus Nerve-Agent Poisoning
标题:Synthesis Of Some Fluorine-Containing Pyridinealdoximes Of Potential Use For The Treatment Of Organophosphorus Nerve-Agent Poisoning
摘要:Fluoroheterocyclic Aldoximes Were Screened As Therapeutic Agents For The Treatment Of Anticholinesterase Poisoning. 2-Fluoropyridine-3-And-6-Aldoxime,And 3-Fluoropyridine-2-And-4-Aldoxime,Were Synthesised. Attempts To Obtain 3,5,6-Trifluoropyridine-2,4-Bis(Aldoxime) And-2-Aldoxime,However,Proved Unsuccessful. Pentafluorobenzaldoxime Was Prepared By Oximation Of Pentafluorobenzaldehyde. Acid Dissociation Constants (Pk(A)) And Second-Order Rate Constants (K(Ox)-) Of The Fluorinated Pyridinealdoximes Towards Satin Were Measured. 2,3,5,6-Tetrafluoropyridine-4-Aldoxime Had The Best Profile: Its K(Ox)-Approached That Of The Therapeutic Oxime P2S (310 Vs. 120 L Mol(-1) Min(-1)),But Its Higher Pk(A) (9.1 Vs. 7.8) Fell Short Of The Target Figure Of 8 Required For Reactivation Of Inhibited Acetylcholinesterase In Vivo. N-Alkylation Of The Fluorinated Pyridine-Aldoximes May Reduce Their Pk(A) Nearer To 8 And Enhance Their Therapeutic Potential. Crown Copyright (C) 2011 Published By Elsevier B.V. All Rights Reserved.
Doi:10.1016/j.Jfluchem.2011.05.028
专利信息
专利号:US-12336981-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; DRAGOVICH Peter; GOSSELIN FRANCIS; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; ROTH BRUCE; SMITH CHASE C; WANG ZHONGGUO; YUEN PO-WAI; ZHENG XIAOZHANG
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 illustrative compound of the invention is shown below:
专利号:US-8362019-B2
优先权日:2008-02-01
标 题:Synthesis and anti-proliferative effect of substituted imidazo[4,5-b]pyrazine compounds
发明人:WINFIELD LEYTE L
权利人:SPELMAN COLLEGE; WINFIELD LEYTE L
摘要:This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. In particular, the disclosure provides for substituted imidazo[4,5-b]pyrazine compounds having the general formula n ntheir salts, pharmaceutical compositions, and methods of treatment using the subject compounds and compositions.
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)
专利号:CN-104003934-A
优先权日:2014-06-13
标题 :Synthesis of 6-chloro-3-fluoro-2-pyridinecarboxylic acid
专利号:CN-104003934-B
优先权日:2014-06-13
标题:Synthesis of 6-chloro-3-fluoro-2-pyridinecarboxylic acid