专利号:US-8748660-B2 优先权日:2012-07-09 标题:Process for the synthesis of antiepileptic drug lacosamide 发明人:MURUGAN MUTHUKRISHNAN; MUJAHID MOHAMMAD; MAJUMDAR PRASHANT PRAMOD 权利人:MURUGAN MUTHUKRISHNAN; MUJAHID MOHAMMAD; MAJUMDAR PRASHANT PRAMOD; COUNCIL SCIENT IND RES 摘要:The present invention relates to the improved and efficient process for the synthesis of antiepileptic drug Lacosamide in high enantiopurity (>98% ee) and better yield. More particularly, the present invention relates to improved and efficient, cost effective process for synthesis of desired (R) isomer of Lacosamide starting from commercially available (S)-benzyl glycidyl ether.
专利号:US-6867202-B1 优先权日:1997-06-25 标 题 :Treatment of insulin resistance 发明人:CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL 权利人:PFIZER 摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-5783577-A 优先权日:1995-09-15 标题 :Synthesis of quinazolinone libraries and derivatives thereof 发明人:HOUGHTEN RICHARD A; OSTRESH JOHN M 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.
专利号:US-5200526-A 优先权日:1987-04-27 标题:Syntheses of optically pure α-amino acids from 3-amino-2-oxetanone salts 发明人:ARNOLD LEE D; VEDERAS JOHN C 权利人:UNIV ALBERTA 摘要:A process for the preparation of optically pure α-amino acids comprising the nucleophilic ring-opening of 3-amino-2-oxetanone salts. N-Protected serine β-lactones are deprotected to form heretofore unknown 3-amino-2-oxetanone and its corresponding salts. In turn these previously unknown 3-amino-2-oxetanone salts may be used in the synthesis of other novel or rare stereochemically-pure free amino acids.
专利号:US-10414720-B2 优先权日:2016-09-28 标题:Process for the preparation of lacosamide 发明人:SATHE DHANANJAY G; DAS ARIJIT; Raikar Sanjay; BHAGWATKAR RAHUL; AHIRE RAMDAS 权利人:UNICHEM LAB LTD 摘要:The present invention relates to an improved process for the synthesis of (R)-Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.