专利号:WO-9943409-A1 优先权日:1998-02-27 标 题:Hplc fractionation of complex chemical mixtures 发明人:COOK PHILLIP DAN; CUMMINS LENDELL L; GRIFFEY RICHARD H; KAWASAKI ANDREW M; GAUS HANS; AN HAOYUN 权利人:ISIS PHARMACEUTICALS INC; COOK PHILLIP DAN; CUMMINS LENDELL L; GRIFFEY RICHARD H; KAWASAKI ANDREW M; GAUS HANS; AN HAOYUN 摘要:The rapid deconvolution of complex chemical mixtures, such as combinatorial libraries prepared via solution-phase simultaneous addition of functionalities is demonstrated using HPLC. Libraries containing 25-216 members were screened for biological activity and active libraries are fractionated into discreet pools using preferred reversed-phase HPLC. The entire process can be completed from a single synthesis of 15-50 mg, without the need for fixed positions, serial synthesis, or tagging.
专利号:WO-2013080218-A1 优先权日:2011-11-28 标 题 :Novel intermediates and process for the preparation of lapatinib and its pharmaceutically acceptable salts 发明人:LAHIRI SASWATA; GUPTA NITIN; SINGH HEMANT KUMAR; HANDA VISHAL; SANGHANI SUNIL 权利人:FRESENIUS KABI ONCOLOGY LTD 摘要:The present invention discloses novel intermediates and processes for the synthesis of Lapatinib and its pharmaceutically acceptable salts thereof.
专利号:US-6774125-B2 优先权日:1998-06-22 标 题:Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; THOMPSON RICHARD C; WILKIE STEPHEN C; BRITTON THOMAS C; PORTER WARREN J; HUFFMAN GEORGE W; LATIMER LEE H 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6509331-B1 优先权日:1998-06-22 标题:Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; THOMPSON RICHARD C; WILKIE STEPHEN C; BRITTON THOMAS C; PORTER WARREN J; HUFFMAN GEORGE W; LATIMER LEE H 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-7390801-B2 优先权日:1996-12-23 标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THORSETT EUGENE D; PLEISS MICHAEL A; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES A; REEL JON K; DRESSMAN BRUCE A; DROSTE JAMES J; HENRY STEVEN S; STUCKY RUSSELL D; PORTER WARREN J 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6150129-A 优先权日:1996-08-01 标 题 :Antimicrobial determination of N-(aminoalkyl) and/or N-(Amidoalkyl) dinitrogen heterocyclic compositions 发明人:COOK PHILLIP DAN; KAWASAKI ANDREW M; KUNG PEI PEI 权利人:ISIS PHARMACEUTICALS INC 摘要:Compositions are provided comprising novel di-nitrogen heterocycle compounds containing N-(aminoalkyl) and/or N-(amidoalkyl) groups. An additional situs of functionality is also provided. The compounds and compositions of the invention are useful as antibacterial and other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents including employment as species for effecting combinatorial synthesis.