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-6323311-B1 优先权日:1999-09-22 标题:Synthesis of insulin derivatives 发明人:LIU FENG; KIM SUNG WAN; BAUDYS MIROSLAV 权利人:UNIV UTAH RES FOUND 摘要:A method for the “one-potâ€? synthesis of insulin derivatives wherein insulin is modified at the α-amino group of the PheB1 residue is described. The method comprises protecting the α-amino group of the GlyA1 residue and the ε-amino group of the LysB29 residue by reaction of insulin with a cyclic anhydride of a dicarboxylic acid in the presence of a tertiary amine. The protected insulin is then reacted with an activated hydrophilic compound, preferably an activated polyethylene glycol, resulting in a conjugate of the hydrophilic compound coupled to the PheB1 residue of insulin. The protecting groups are then removed from the conjugate under mild acidic conditions, and the resulting insulin derivative can be purified by conventional methods. Monosubstituted insulin derivatives wherein polyethylene glycol or derivatives thereof or glycosides are coupled to the PheB1 residue of insulin are also described.
专利号:US-2014275582-A1 优先权日:2013-03-14 标 题 :Chiral 2-arylpropyl-2-sulfinamide and chiral n-2-arylpropyl-2-sulfinylimines and synthesis thereof 发明人:LI GUIGEN 权利人:LI GUIGEN; UNIV TEXAS TECH; NANJING UNIVERSITY INST OF CHEMISTRY AND BIOMEDICAL SCIENCES 摘要:Provided herein are novel chiral sulfinamide and imine compounds. Also provided herein are methods of synthesizing novel chiral sulfinamide and imine compounds comprising simplified purification methods when compared to prior methods. The novel chiral sulfinamide and imine compounds are useful, for example, in the synthesis of complex natural products and pharmaceutical important compounds.
专利号:US-6469065-B1 优先权日:1996-02-02 标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use 发明人:GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.
专利号:US-2021369846-A1 优先权日:2018-10-26 标 题 :New Ammonium Salts Of Fluorinated Organic Acids, Method Of Their Synthesis and Application 发明人:STEFANEK AGATA; CIACH TOMASZ; LECZYCKAWILK KATARZYNA; CZARNOCKA-SNIADALA SYLWIA; GRAFSTEIN JOANNA; DRESLER MAGDALENA; NOWAK ALEKSANDRA; WGLINKSKI JAKUB 权利人:NANOSANGUIS 摘要:The exemplary arrangements relate to ammonium salts of partially fluorinated organic acids. The exemplary arrangements also relate to methods of synthesis of the ammonium salts of partially fluorinated organic acids. The exemplary arrangements also relate to methods of use of the ammonium salts of partially fluorinated organic acids to produce stabilizing emulsions of the oil-in-water and/or water-in-oil type. The exemplary arrangements also relate to methods of use and applications of the ammonium salts of partially fluorinated organic acids, for example use as stabilizing agents in blood substitute preparations.
专利号:US-9216953-B2 优先权日:2012-11-02 标题 :Chiral 2-arylpropyl-2-sulfinamide and chiral N-2-arylpropyl-2-sulfinylimines and synthesis thereof 发明人:LI GUIGEN; PINDI SURESH 权利人:LI GUIGEN; PINDI SURESH 摘要:Provided herein are novel chiral sulfinamide and imine compounds. Also provided herein are methods of synthesizing novel chiral sulfinamide and imine compounds comprising simplified purification methods when compared to prior methods. The novel chiral sulfinamide and imine compounds are useful, for example, in the synthesis of complex natural products and pharmaceutical important compounds.