专利号:US-2012177593-A1 优先权日:2009-07-20 标 题 :Synthesis of dendrimer conjugates 发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH 权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
专利号:WO-9964032-A1 优先权日:1998-06-08 标题 :Combinatorial synthesis of multibinding libraries 发明人:CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN 权利人:ADVANCED MEDICINE INC; CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN 摘要:Disclosed are methods for synthesizing large collections of diverse multimeric compounds as well as iterative processes for evaluating key molecular constraints imparting multibinding properties to multimeric compounds. Also disclosed are libraries of multimeric compounds which can be evaluated for imparting multibinding properties.
专利号:WO-0112817-A1 优先权日:1999-08-12 标题:Evolution and use of enzymes for combinathorial and medicinal chemistry 发明人:KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL 权利人:MAXYGEN INC; LIU LU; KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL 摘要:This invention provides libraries of recombinant derivatizing enzymes that are useful for biocatalytic synthesis of derivatives oforganic molecules, including lead compounds for pharmaceutical use. The recombinant derivatizing enzymes catalyze reactions such as modification or replacement of functional groups on the organicmolecules, or addition of chemical moieties onto preexisting functional groups. The use of recombinant enzyme libraries enables one to obtain enzymes that catalyze the formation of organic molecule derivatives that could not otherwise be made using only naturally occurring enzymes.
专利号:US-7579461-B2 优先权日:2004-01-15 标题:Processes for the preparation of rocuronium bromide and intermediates thereof 发明人:ADAR ELIEZER; SONDACK DAVID; FRIEDMAN ODED; MANASCU IOSEF; FIZITZKI TAMIR; FREGER BORIS; ARAD ODED; WEISMAN ALEXANDER; KASPI JOSEPH 权利人:CHEMAGIS LTD 摘要:A novel process for preparing (2β,3α,5α,16β,17β)-17-acetoxy-3-hydroxy-2-(4-morpholinyl)-16-(1-pyrrolidinyl) androstane, a known intermediate in the synthesis of the skeletal muscle relaxant rocuronium bromide, is disclosed.
专利号:US-2012232225-A1 优先权日:2009-08-26 标 题:Synthesis and isolation of dendrimer systems 发明人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL 权利人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis and isolation of dendrimer systems. In particular, the present invention is directed to novel dendrimer conjugates with defined and limited numbers of ligand conjugates and high levels of structural uniformity, methods of synthesizing the same, compositions comprising the conjugates, as well systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)).
专利号:EP-1200395-B1 优先权日:1999-07-28 标 题:Urea derivatives as inhibitors of ccr-3 receptor 发明人:PADIA JANAK; HOCKER MICHAEL D; OHASHI HIROSHI; NISHITOBA TSUYOSHI; SAWA EIJI 权利人:KIRIN BREWERY 摘要:Urea and thiourea derivatives inhibit cell function of the chemokine receptor CCR-3. These compounds offer an effective means for treating a range of diseases thought to be mediated by the CCR-3 receptor. A variety of useful urea and thiourea derivatives can be synthesized using liquid and solid phase synthesis protocols.
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