73183-34-3 + 17321-93-6 = 108-52-1 + 944401-55-2 反应条件:1.1 Reagents: Potassium Acetate Catalysts: Dichloro[1,1′-Bis(Diphenylphosphino)Ferrocene]Palladium(Ii) Dichloromethane Addu... Solvents: 1,4-Dioxane; 18 H,115 °C 标题:Identification Of Nvp-Bkm120 As A Potent,Selective,Orally Bioavailable Class I Pi3 Kinase Inhibitor For Treating Cancer 作者:Burger,Matthew T.; Pecchi,Sabina; Wagman,Allan; Ni,Zhi-Jie; Knapp,Mark; Et Al 参考文献:Acs Medicinal Chemistry Letters 日期:2011 卷标:2(10) 页码:774-779
专利号:US-10287265-B2 优先权日:2015-03-09 标 题 :Enantiomers of 8-hydroxyquinoline derivatives and the synthesis thereof 发明人:Puskás László; Kanizsai István; PILLOT THIERRY; GYURIS Márió; Szabó András; Takács Ferenc; Hackler László 权利人:AVIDIN CO LTD; SONEAS RES CO LTD; SYNAGING SAS 摘要:Our invention relates to novel enantiomer derivatives of 8-hydroxyquinoline derivatives with general formula (I) and (II) and the synthesis thereof and pharmaceutically acceptable salts and metal complexes thereof, and the medicinal and/or pharmaceutical compositions comprising these compounds. n n n n n n n n n n The essence of the subject matter of the invention relates to the fact that prior art discloses the biological effect and characteristics only of the racemic products, the novel enantiomer derivatives according to the invention appear in our application for the first. n The subject matter of the invention furthermore relates to a novel, stereoselective synthesis for the preparation of the novel enantiomer derivatives according to the invention. The novel medicinal and/or pharmaceutical compositions comprising these enantiomers are suitable for the treatment of the named diseases, and the enanatiomers are used for manufacture of these compositions. These applications for manufacture of the compositions are also the subject matters of the invention. The compounds according to the invention can be used preferably as cytoprotective, neuroprotective, cardioprotective, anxiolytic and antidepressant agent for treatment of neuropsychiatric and neurologic diseases and diseases in connections with transplantations and with ischemia and reperfusion injuries thereof, and inhibition of organ, advantageously skin graft rejection. According to our studies the R-enantiomer has either sole or high biological effect in some cases.
专利号:US-9550000-B2 优先权日:2011-09-09 标题 :Compositions, methods, and systems for the synthesis and use of imaging agents 发明人:ROBINSON SIMON P; YU MING 权利人:ROBINSON SIMON P; YU MING; LANTHEUS MEDICAL IMAGING INC 摘要:The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18 F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-6797820-B2 优先权日:1999-12-17 标 题:Succinate compounds, compositions and methods of use and preparation 发明人:PATEL DINESH; JACOBS JEFFREY W; JAIN RAKESH; NI ZHI-JIE; YUAN ZHENGYU 权利人:VICURON PHARM INC 摘要:Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The hydroxymates are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as matrix metalloproteinases (MMPs). Methods of synthesis and of use of the compounds are also disclosed.
专利号:US-6562844-B2 优先权日:1998-01-23 标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:WO-0144179-A1 优先权日:1999-12-17 标题 :Novel succinate compounds, compositions and methods of use and preparation 发明人:JAIN RAKESH; NI ZHI-JIE; PATEL DINESH V; YUAN ZHENGYU 权利人:VERSICOR INC; JACOBS JEFFREY W; JAIN RAKESH; NI ZHI JIE; PATEL DINESH V; YUAN ZHENGYU 摘要:Novel hydroxamic acid compounds of Formula (I) are disclosed. These hydroxamates inhibit peptide deformylase (PDF), an enzyme present in prokaryotes. The hydroxymates are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as matrix metalloproteinases (MMPs). Methods of synthesis and of use of the compounds are also disclosed.
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 354. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 447. 摘要:Hay, M. B.; Hicks, J. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 161. 摘要:Yi, C. S., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 253. 摘要:J. R. Marshall and J. Walker. J. Chem. Soc. 1951, 1004.