专利号:WO-2015183067-A1 优先权日:2014-05-30 标题 :Synthesis of analogues of y-amino acids and resulting products 发明人:FERNÃ?NDEZ ZERTUCHE MARIO; TOVAR GUDIÑO ERIKA; TRUJILLO FERRARA JOSÉ GUADALUPE; GUEVARA SALAZAR JUAN ALBERTO 权利人:UNIV AUTÓNOMA DEL ESTADO DE MORELOS 摘要:The invention relates to a compound of formula (see formula), suitable for use as drugs in the treatment of chronic neurodegenerative disorders of the Huntington's disease, Parkinson's disease and epilepsy type, inter alia . The invention relates to novel methods for the synthesis of said analogues and the pharmaceutically acceptable solvates and salts thereof.
专利号:US-2014336369-A1 优先权日:2011-06-28 标题:Process for preparing heparinoids and intermediates useful in the synthesis thereof 发明人:KOVI RAVISHANKER; NAIK ASHISH; PATEL BRIJESH; MADALA MURALIKRISHNA 权利人:APICORE US LLC 摘要:Processes are disclosed for the synthesis of the Factor Xa anticoagulant fondaparinux and related compounds. Protected pentasaccharide intermediates and efficient and scalable processes for the industrial scale production of fondaparinux sodium by conversion of the protected pentasaccharide intermediates via a sequence of deprotection and sulfonation reactions are provided.
专利号:US-9346851-B2 优先权日:2008-02-22 标 题 :Chemical modification of proteins 发明人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN 权利人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN; RP SCHERER TECHNOLOGIES LLC 摘要:The invention relates to methods for selectively converting a cysteine residue in a peptide or protein to the dehydroalanine (Dha) residue. The method also works on selenocysteine and substituted cysteine and selenocysteine residues, resulting in the Dha residue which may be converted to any natural or unnatural amino acid residue desired without the alteration of the remainder of the peptide or protein. The invention also allows ligation of a desired peptide at any point rather than at a point where there should be a naturally occurring cysteine, thereby allowing native chemical ligation to be used in the synthesis of peptides that do not contain cysteine. The methodology allows for the synthesis of very large peptides.
专利号:US-2009143426-A1 优先权日:2007-12-04 标 题:Synthesis of 1,3,6-trisubstituted-2-carboxyquinol-4-ones as selective ET A antagonists and their use as medicaments 发明人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN 权利人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN 摘要:The invention discloses the composition and preparation of various 1,3,6-trisubstituted-2-carboxy-quinol-4-ones of the formula 1 where R is H, alkyl, haloalkyl or hydroxyalkyl, R′ is alkyl, nitro, halogen or NR 2 ′″ where R′″ is alkyl or cycloalkyl, and R″ is H or alkyl. The composition of the invented compounds as methods of antagonizing the action of endothelin-1 to treat cardiovascular, pulmonary diseases and obstetric disorders and preterm labor and preeclampsia in mammals is disclosed.
专利号:US-8067616-B2 优先权日:2006-04-06 标 题 :Total synthesis of salinosporamide A and analogs thereof 发明人:LING TAOTAO; MACHERLA VENKATA RAMI REDDY; POTTS BARBARA CHRISTINE; MANAM RAMA RAO; MCARTHUR KATHERINE A 权利人:LING TAOTAO; MACHERLA VENKATA RAMI REDDY; POTTS BARBARA CHRISTINE; MANAM RAMA RAO; MCARTHUR KATHERINE A; NEREUS PHARMACEUTICALS INC 摘要:The present invention relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs from a compound of formula (V).
专利号:WO-2009145624-A1 优先权日:2008-05-30 标题:Use of activated carbon dioxide in the oxidation of compounds having a hydroxy group 发明人:DE JONG BOUWE; MALMSTROEM MAGNUS KRISTIAN 权利人:INOVIAKEM B V; DE JONG BOUWE; MALMSTROEM MAGNUS KRISTIAN 摘要:The invention pertains to a process for the oxidation of a compound having a hydroxy group, said process comprising the steps of: (a) oxidising said compound having a hydroxy group; (b) reducing carbon dioxide at a cathode; wherein steps (a) and(b) are effected in the presence of an ionic liquid. The course of the reaction may be directed, such as stimulating or suppressing oligomerization, resulting in the controlled synthesis of a wide variety of products, e.g. dialkyl carbonates, and lactic acid and/or lactide (which may be further converted to acrylic acid).