专利号:US-9388147-B2 优先权日:2009-11-13 标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN 权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ RL 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:US-2009162290-A1 优先权日:2005-09-09 标 题 :Method for the synthesis of penta-pendant enantiomer-pure chelators and process for therapeutically active bioconjugates preparation by a covalent binding thereof 发明人:BENES IVAN; CIHELNIK SIMON; DROZ LADISLAV; SRAMEK MARTIN 权利人:THERAPHARM GMBH 摘要:The present invention provides a method for synthesis and binding methods of pentapendant enantiomer-pure chelators of formula (VII) wherein R 1 , R 2 , R 3 , R 4 are groups forming an adequate enantiomer of the chelator; and X 1 -X 5 , Y 1 -Y 5 , Z 1 -Z 5 each individually forming pendant chelating groups.
专利号:US-9394264-B2 优先权日:2009-11-13 标 题:Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA 权利人:RECEPTOS INC 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:US-2025205158-A1 优先权日:2023-12-26 标 题 :Biodegradable lipids and formulations for delivery of mrna 发明人:ANDERSON DANIEL GRIFFITH; RUDRA ARNAB; GUPTA AKASH; REED KAELAN 权利人:MASSACHUSETTS INST TECHNOLOGY; CHILDRENS MEDICAL CENTER 摘要:Provided herein are compounds, such as compounds of Formulae (I), (I′), (XI), (XII), and (XIII), and pharmaceutically acceptable salts, solvates, tautomers, stereoisomers, and isotopically labeled derivatives thereof, and compositions, methods, uses, and kits thereof. The compounds provided herein are lipids useful for delivery of agents, including polynucleotides such as mRNA, for the treatment and/or prevention of various diseases and conditions (e.g., genetic diseases, proliferative diseases, hematological diseases, neurological diseases, liver diseases, spleen diseases, lung diseases, painful conditions, psychiatric disorders, musculoskeletal diseases, metabolic disorders, inflammatory diseases, and autoimmune diseases). Also provided herein are methods of synthesis of compounds of Formulae (I′), (XI), (XII), (XIII), and (VIII).
专利号:US-6403800-B1 优先权日:1998-02-11 标题 :Synthesis of 1-(2-sulfoethyl)-pyridinium betaine 发明人:KAPPES ELISABETH; BRODT GREGOR; KROENER RUDI; WAGNER NORBERT; HILDEBRANDT SOEREN; BOGENSTAETTER THOMAS 权利人:BASF AG 摘要:Described is a process for preparing 1-(2-sulfoethyl)pyridinium betaine wherein pyridine is reacted with a sulfoethylating agent from the group consisting of carbyl sulfate, ethionic acid and its salt and vinylsulfonic acid and vinylsulfonate, the reaction taking place in aqueous solution or in pyridine.
专利号:US-2010204463-A1 优先权日:2007-08-07 标题 :Preparation Of Synthetic Nucleosides via Pi-Allyl Transition Metal Complex Formation 发明人:LIOTTA DENNIS C; LI YONGFENG 权利人:LIOTTA DENNIS C; LI YONGFENG 摘要:This invention provides highly regioselective and stereoselective processes for preparing synthetic nucleosides. A process for the preparation of synthetic nucleosides is provided that comprises a) preparing a bicycloamide derivative, b) reacting the bicycloamide derivative with a nucleic acid base or heterocyclic base or salt thereof in the presence of a transition metal catalyst to form a cyclopentenecarboxamide, and c) cleaving a carboxamide group from the cyclopentenecarboxamide to form the synthetic nucleoside. The processes according to the invention can be used for the synthesis of a variety of anti-viral agents, including Abacavir, Carbovir, and Entecavir, as well as derivatives thereof.
摘要:Kawęcki, R., Science of Synthesis Knowledge Updates, (2018) 4, 249. 摘要:Giel, M.-C.; Smedley, C. J.; Moses, J. E., Science of Synthesis, (2021) , 463. 摘要:U.S. Environmental Protection Agency. 1998. Extremely Hazardous Substances (EHS) Chemical Profiles and Emergency First Aid Guides. Washington, D.C.: U.S. Government Printing Office.