专利号:US-8686157-B2 优先权日:2003-02-10 标题:Processes for the facile synthesis of diaryl amines and analogues thereof 发明人:SNOONIAN JOHN R; OLIVER-SHAFFER PATRICIA ANN 权利人:SNOONIAN JOHN R; OLIVER-SHAFFER PATRICIA ANN; VERTEX PHARMA 摘要:The present invention relates to processes for the facile synthesis of diaryl amines and analogues thereof. The processes of the present invention produce diaryl amines in high yield and purity. The present invention also relates to intermediates useful in the process of the present invention.
专利号:EP-1404682-B1 优先权日:2001-06-29 标题:Method of inhibiting ptp 1b and/or t-cell ptp and/or other ptpases with an asp residue at position 48 发明人:HANSEN THOMAS KRUSE; OLSEN OLE HVILSTED; PETERSEN ANDERS KLARSKOV; LAU JESPER; ANDERSEN HENRIK SUNE; MOLLER NIELS PETER HUNDAHL 权利人:NOVO NORDISK AS 摘要:This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al., Proc. Natl. Acad. Sci. USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1. This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.
专利号:US-2003064979-A1 优先权日:2001-06-29 标题 :Method of inhibiting PTP 1B and /or T-cell PTP and/or other PTPases with an Asp residue at position 48 发明人:HANSEN THOMAS KRUSE; OLSEN OLE HVILSTED; PETERSEN ANDERS KLARSKOV; LAU JESPER; ANDERSEN HENRIK SUNE; MOLLER NIELS PETER HUNDAHL 摘要:This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al, Proc Natl Acad Sci USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1 n n n This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.
专利号:US-2025236897-A1 优先权日:2022-02-16 标 题 :Processes for preparation of avacopan and intermediates thereof 发明人:GYUJTO IMRE; PAAL TIHAMER; JUHASZ ZSUZSA POTARINE; ESZENYI DANIEL; ZAHUCZKY GABOR JOZSEF; KONDOR ZOLTAN; RENGASAMY VADIVELAN; PRAJAPATI RAMKARAN; DAUND VAIBHAV SURESH; SAINGER SHACHI; KADU RUSHIKESH; SHARMA VISHAL 权利人:TEVA PHARMACEUTICALS INT GMBH 摘要:The present disclosure encompasses a process for chiral resolution of racemic amines, particularly ethyl 2-(4-((tert-butoxycarbonyl)amino)phenyl)piperidine-3-carboxylate, into its desired isomer, ethyl (2R,3S)-2-(4-((tert-butoxycarbonyl)amino)phenyl)-piperidine-3-carboxylate, which is an intermediate useful in the synthesis of Avacopan.
专利号:US-5248781-A 优先权日:1992-09-21 标题 :Preparation of substituted anilino-nicotinic acid derivatives 发明人:MCKILLOP ALEXANDER 权利人:UNIV PRINCETON 摘要:Substituted anilino-nicotinic acid derivatives are readily prepared from the condensation of two intermediates, 2-alkyl-3-perfluoroalkyl-anilines and alkyl 2-chloronicotinates. The 2-alkyl-3-perfluoroalkyl-aniline intermediate can be prepared via a novel three step synthesis. 3-Perfluoroalkyl-anilines are reacted with an amine directing protecting group reagent to protect the amine. The protected amine is then alkylated, and finally, the directing group is removed to form the 2-alkyl-3-perfluoroalkyl-aniline intermediate. The 2-alkyl-3-perfluoroalkyl-aniline intermediate is condensed with the alkyl 2-chloronicotinate to form the anilino-nicotinic acid derivative.
专利号:US-2007173649-A1 优先权日:2003-02-10 标 题:Processes for the facile synthesis of diaryl amines and analogues thereof