CAS: 366-77-8; 3-(4-Fluorobenzoyl)Propionic Acid

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4-(4-氟苯基)丁酸 4-(4-Fluorophenyl)Butanoic Acid 589-06-0

📜溴哌利多置于rat Liver Microsomes体系中,用 Phosphate Buffer 用作溶剂,化学反应 0.5H,反应生成3-(4-氟苯甲酰基)丙酸
参考文献:Role Of Cyp3A In Bromperidol Metabolism In Rat In Vitro And In Vivo
标题:Role Of Cyp3A In Bromperidol Metabolism In Rat In Vitro And In Vivo
摘要:1. The Aim Was To Identify Whether Cyp3A Metabolizes Bromperidol (Bp),An Antipsychotic Drug,To Form 4-Fluorobenzoyl-Propionic Acid (Fbpa) In Hepatic Microsomes From 8-Week-Old Male Sprague-Dawley Rats And To Investigate Whether An Inhibitor Or An Inducer Of Cyp3A Affects Bp Pharmacokinetics In Rat.2. In An In Vitro Study,Only Troleandomycin Showed Marked Inhibition Of Fbpa Formation Among Several Specific Cyp Isozyme Inhibitors Studied Including Troleandomycin,Diethyldithiocarbamate,Furafylline And Quinine. Anti-Rat Cyp3A2 Serum Inhibited Fbpa Formation By 80 %,Whereas Other Anti-Rat Cyp Sera (1A1,1A2,2B1,2C11,2E1) Only Slightly Inhibited It.3. In A Pharmacokinetic Study,Bp Half-Life Was Prolonged To 137% Of The Average Control Value By 7-Day Treatment With Erythromycin,A Cyp3A Inhibitor,And Shortened To 58 % Of The Control By 2-Day Treatment With Dexamethasone,A Cyp3A Inducer. Bp Clearance Was Reduced To 68 % Of The Control By Erythromycin And Was Increased To 145 % Of Control By Dexamethasone.4. These Results Suggested That Bp Biotransformation Is Catalysed Mainly By Cyp3A To Form Fbpa In Rat And That The Modification Of This Enzyme Activity Would Affect The Pharmacokinetics Of Bp.
Doi:10.1080/004982599238281

专利信息

专利号:US-2008032964-A1
优先权日:2006-04-10
标题:Process for the synthesis of azetidinone
发明人：KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO
权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO
摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.

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:WO-2017063910-A1
优先权日:2015-10-16
标题:Agonists of the chemokine receptor cxcr3
发明人：TSCHAMMER NUSKA; MILANOS LAMPROS; BROX REGINE
权利人:Friedrich-Alexander-Universität Erlangen-Nürnberg
摘要:The present invention relates to agonists of the chemokine receptor CXCR3, methods of their synthesis and uses thereof.

专利号:US-11884628-B2
优先权日:2019-05-16
标题 :Method for synthesizing lactam derivatives without use of catalyst
发明人：YANG SONG; LI HU; WU HONGGUO
权利人:UNIV GUIZHOU
摘要:Disclosed is a simple synthesis method of lactam derivatives, comprising: with formamide functioning as both an amine source and a hydrogen source (hydrolyzed to produce formic acid), carrying out a cycloamination reaction on a raw material keto acid in the absence of a solvent or a catalyst to simply synthesize a lactam derivative. Compared with previous reports, the present disclosure has the following advantages: the time required for the reaction is greatly shortened, the selectivity is remarkably improved, a conversion rate of a keto acid derivative is greater than 99%, and the yield of the lactam derivative can reach 70% to 94%.

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:US-9217012-B2
优先权日:2009-04-08
标题 :Inhibitors of protein tyrosine phosphatases
发明人：ZHANG ZHONG-YIN; ZHANG SHENG
权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP
摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.