专利号:WO-9946268-A1 优先权日:1998-03-12 标题 :MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPases) 发明人:ANDERSEN HENRIK SUNE; JONES TODD KEVIN; HOLSWORTH DANIEL DALE 权利人:NOVO NORDISK AS; ONTOGEN CORP 摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:US-2002019412-A1 优先权日:1998-03-12 标题:Modulators of protein tyrosine phosphatases (ptpases) 发明人:ANDERSEN HENRIK SUNE; JONES TODD KEVIN; HOLSWORTH DANIEL DALE 摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:US-5567830-A 优先权日:1994-02-14 标题 :Process for synthesis of acetylenic carbinols 发明人:UPASANI RAVINDRA B 权利人:COCENSYS INC 摘要:A method for the preparation of an acetylenic alcohol by reaction of 1,2-dibromoethylene with an alkyl, aryl an heteroaryl lithium in an inert solvent, followed by reaction with a carbonyl-containing compound to give an acetylenic alcohol is disclosed.
专利号:US-2024239799-A1 优先权日:2021-04-02 标 题:(s)-1-(5-((pyridin-3-yl)thio)pyrazin-2-yl)-4'h,6'h-spiro[piperidine-4,5'-pyrrolo [1,2-b]pyrazol]-4'-amine derivatives and similar compounds as shp2 inhibitors for the treatment of e.g. cancer 发明人:DI FABIO ROMANO; MONTALBETTI CHRISTIAN; PETROCCHI ALESSIA; GRILLO ALESSANDRO; RANDAZZO PIETRO; ROSSETTI ILARIA; CIAMMAICHELLA ALINA 权利人:C N C C S S C A R L COLLEZIONE NAZ DEI COMPOSTI CHIMICI E CENTRO SCREENING; IRBM S P A 摘要:The present invention relates to compounds of formula (I). The compounds of the formula (I) are e.g. (S)-1-(5-((pyridin-3-yl)thio) pyrazin-2-yl)-41H,6′H-spiro[piperidine-4,5′-pyrrolo[1,2-b]pyrazol]-41-amine derivatives and similar compounds. The present invention also relates to the compounds of formula (I) for use as Src homology phosphotyrosine phosphatase 2 (SHP2) inhibitors in methods of treatment of e.g. cancer, cardiovascular diseases, immunological disorders, autoimmune disorders, fibrosis, ocular disorders, systemic lupus erythematosus, diabetes, neutropenia, and combinations thereof. The present invention also relates to pharmaceutical compositions containing said compounds and to their methods of synthesis.
专利号:US-2010317848-A1 优先权日:2006-12-31 标题:Process for the synthesis of derivatives of 3-amino-tetrahydrofuran-3-carboxylic acid and use thereof as medicaments
专利号:US-2680743-A 优先权日:1951-02-06 标 题 :Synthesis of pyridoxine 发明人:STEVENS PHILIP G 权利人:GEN ANILINE & FILM CORP
[参考文献]: Xue F, Et Al. Structure-Activity Studies Of Cyclic Ketone Inhibitors Of The Serine Protease Plasmin: Design, Synthesis, And Biological Activity. Bioorg Med Chem. 2006 Dec 15;14(24):8467-87.
合成参考文献
摘要:MacMillan, D. W. C.; Beeson, T. D., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 297. 参考文献:10.1515/cclm.2003.248 摘要:Boulat O, Gradwohl M, Matos V, Guignard JP, Bachmann C. Organic acids in the second morning urine in a healthy Swiss paediatric population. Clin Chem Lab Med. 2003 Dec;41(12):1642–58. doi: 10.1515/cclm.2003.248.