专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
专利号:US-9284306-B2 优先权日:2012-05-11 标题 :(R)-Nifuratel, its use for the treatment of infections and synthesis of (R) and (S)-Nifuratel 发明人:GAGLIARDI STEFANIA; CONSONNI ALESSANDRA; MAILLAND FEDERICO; BULGHERONI ANNA 权利人:POLICHEM SA 摘要:(R)-Nifuratel is disclosed together with its use as bactericide and bacteriostatic agent as well as the pharmaceutical compositions containing the same; (R)-nifuratel has been surprisingly found to possess a better antimicrobial profile than either nifuratel racemate or (S)-nifuratel. A new procedure for the synthesis of both (R)-Nifuratel and (S)-Nifuratel is also disclosed.
专利号:US-6121054-A 优先权日:1997-11-19 标 题 :Method for separation of liquid and solid phases for solid phase organic syntheses 发明人:LEBL MICHAL 权利人:TREGA BIOSCIENCES INC 摘要:A simple, efficient apparatus and method for separation of solid and liquid phases useful in methods of high-throughput combinatorial organic synthesis of large libraries or megaarrays of organic compounds is disclosed. The apparatus and method are useful, whether as part of an automated, robotic or manual system for combinatorial organic synthesis. In a preferred embodiment, an apparatus and method of removal of liquid phase from solid phase compatible with microtiter plate type array(s) of reaction vessels is disclosed.
专利号:US-9949970-B2 优先权日:2010-09-14 标题 :Synthesis of new benzothiazole derivatives as potential anti-tubercular agents 发明人:KAMAL AHMED; SHETTI RAJESH VCRNC; SWAPNA PONNAMPALLI; AZEEZA SHAIK; REDDY A MALLA; KHAN INSHAD ALI; ABDULLAH SHEIKH TASDUQ; SHARMA SANDEEP; KALIA NITIN PAL 权利人:COUNCIL SCIENT IND RES 摘要:Disclosed are compounds of general formula A useful as potential anti-tubercular agents. The general formula A is
专利号:EP-0043598-B1 优先权日:1980-07-09 标 题:Process for the transformation of furfural or 5-nitro-furfural into furonitrile or 5-nitro-furonitrile 摘要:1. Process for the transformation of furfural or 5-nitro-furfural into furonitrile or 5-nitro-furonitrile, in which furfural or 5-nitro-furfural is brought into contact with a hydroxylamine salt, characterized in that the synthesis of furonitrile or 5-nitro-furonitrile is achieved in a single step, by bringing the furfural or 5-nitro-furfural into contact with the hydroxylamine salt in N-methyl pyrrolidone (N.M.P.), the mixed substances being taken to a temperature of between 120 degreees C and 165 degrees C.
专利号:US-9220714-B2 优先权日:2006-03-16 标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis 发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG 权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND 摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.
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合成参考文献
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