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:US-5169779-A 优先权日:1991-02-08 标 题:Process for the preparation of methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxy-phenyl)propionate 发明人:ZARD LYDIA; TIXIDRE ARLETTE; ROSSEY GUY; WICK ALEXANDER 权利人:SYNTHELABO 摘要:A process for the preparation of methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, which comprises subjecting the dextrorotatory (2S,3R) enantiomer, present in a starting mixture containing both the levorotatory (2R,3S and dextrorotatory (2S,3R) enantiomers, to a transesterification reaction, in an anhydrous medium and in the presence of an enzyme which does not affect the levorotatory (2R,3S) enantiomer. The latter is an intermediate for the synthesis of compounds such as Diltiazem.
专利号:US-2011040105-A1 优先权日:2008-04-16 标题 :Processes useful for the synthesis of (r)-1--2-methyl-pyrrolidine 发明人:HUBER CHRISTIAN H; KHULMAN YOUNG MI; TANDEL SAGUN K; JOHANNSEN STEPHEN R; WANG TINGMIN; ANGELL PAUL 权利人:ARENA PHARM INC 摘要:Processes useful for making a pharmaceutically useful compound according to Formula (I), forms of such a compound, and intermediates useful in such processes are described.
专利号:EP-0383803-B1 优先权日:1987-10-28 标题 :Oligonucleotide-polyamide conjugates 发明人:HARALAMBIDIS JIM; TREGEAR GEOFFREY WILLIAM 权利人:HOWARD FLOREY INST OF 摘要:Oligonucleotide-polyamide conjugates of the formula X-L-Y, where X is a polyamide, Y is an oligonucleotide, and L is a linker which forms a covalent bond with the amino-terminus of the polyamide X and the 3' phosphate group of the oligonucleotide Y. Conjugates may be synthesized by assembling a polyamide on a solid support matrix, adding a suitable linker molecule, followed by synthesis of the oligonucleotide. Methods for detecting specific polynucleotides with oligonucleotide-polyamide conjugates are also described.
专利号:US-5525465-A 优先权日:1987-10-28 标 题:Oligonucleotide-polyamide conjugates and methods of production and applications of the same 发明人:HARALAMBIDIS JIM; TREGEAR GEOFFREY W 权利人:FLOREY HOWARD INST 摘要:Oligonucleotide-polyamide conjugates of the formula X--L--Y, where X is a polyamide, Y is an oligonucleotide, and L is a linker which forms a covalent bond with the amino-terminus of the polyamide X and the 3' phosphate group of the oligonucleotide Y. Conjugates may be synthesized by assembling a polyamide on a solid support matrix, adding a suitable linker molecule, followed by synthesis of the oligonucleotide. Methods for detecting specific polynucleotides with oligonucleotide-polyamide conjugates are also described.
专利号:US-2015352230-A1 优先权日:2013-01-11 标 题:Synthesis and isolation of dendrimer based imaging systems 发明人:MULLEN DOUGLAS GURNETT; BAKER JR JAMES R; BANASZAK HOLL MARK M; HUANG BAOHUA; DOUGHERTY CASEY; BALL JACK 权利人:UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).