专利号:US-6225329-B1 优先权日:1998-03-12 标 题 :Modulators of protein tyrosine phosphatases (PTPases) 发明人:RICHTER LUTZ STEFAN; ANDERSEN HENRIK SUNE; VAGNER JOSEF; JEPPESEN CLAUS BEKKER; MOELLER NIELS PETER HUNDAHL; BRANNER SVEN; SU JING; BAKIR FARID; JUDGE LUKE MILBURN 权利人:NOVO NORDISK AS 摘要:The present invention provides novel compounds of Formula 1, compositions containing these compounds, 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, n wherein A, R 1 , R 2 , R 3 , R 4 , R 16 and R 17 are as defined in the specification. 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:WO-9946236-A1 优先权日:1998-03-12 标题 :Modulators of protein tyrosine phosphatases (ptpases) 发明人:RICHTER LUTZ STEFAN; ANDERSEN HENRIK SUNE; VAGNER JOSEF; JEPPESEN CLAUS BEKKER; MOELLER NIELS PETER HUNDAHL; BRANNER SVEN; SU JING; BAKIR FARID; JUDGE LUKE MILBURN 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:EP-1062199-A1 优先权日:1998-03-12 标题 :Modulators of protein tyrosine phosphatases (ptpases) 发明人:RICHTER LUTZ STEFAN; ANDERSEN HENRIK SUNE; VAGNER JOSEF; JEPPESEN CLAUS BEKKER; MOLLER NIELS PETER HUNDAHL; BRANNER SVEN; SU JING; BAKIR FARID; JUDGE LUKE MILBURN 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:WO-2025023769-A1 优先权日:2023-07-25 标 题:Novel synthesis method of 18f-rucaparib 发明人:CHEON CHEOL-HONG; PARK JINJAE; SEO JUAN 权利人:UNIV KOREA RES & BUS FOUND 摘要:The present invention relates to a method for efficiently preparing rucaparib for a PET image. More specifically, the present invention relates to an improved preparation method for synthesizing [18F]-rucaparib in excellent yield by means of a pathway for synthesizing a pinacol boronate derivative, which is a key intermediate, by using, as a starting material, a 2-iodoaniline derivative prepared by a novel synthesis method.
专利号:US-11702394-B2 优先权日:2018-02-23 标 题 :Inhibitors of phospholipid synthesis and methods of use 发明人:GOUW ARVIN; FELSHER DEAN W; JIN FENG; ZARE RICHARD N; MARGULIS KATHERINE; SCHOW STEVEN R; GREENHOUSE ROBERT J; LOUGHHEAD DAVID; RICHARDS STEVEN 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Inhibitors of Glycerol 3-Phosphate Acyltransferase (GPAT) are provided; and methods of use in the treatment of cancer; and treatment of conditions relating to metabolic syndrome and hyperlipidemia.
专利号:US-9096624-B2 优先权日:2009-06-01 标 题:Amino pyrimidine anticancer compounds 发明人:CREW ANDREW P; SHERMAN DAN; APPARI RAMA DEVI; CHEN XIN; CHILUKURI RAMESH; DONG HANQING; FERRARO CATERINA; FOREMAN KENNETH; GUPTA RAMESH C; LI AN-HU; STOLZ KATHRYN M; VOLK BRIAN; ZAHLER ROBERT 权利人:OSI PHARMACEUTICALS LLC 摘要:Compounds of Formula 1, as shown below and defined herein: n n n n n n n n n n n n and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.
[参考文献]: Weidel E, Et Al. Structure Optimization Of 2-Benzamidobenzoic Acids As Pqsd Inhibitors For Pseudomonas Aeruginosa Infections And Elucidation Of Binding Mode By Spr, Std Nmr, And Molecular Docking. J Med Chem. 2013 Aug 8;56(15):6146-55. [参考文献]: Nagahisa Yamaoka, Et Al. Structure-Activity Relationships Of New N-Acylanthranilic Acid Derivatives As Plasminogen Activator Inhibitor-1 Inhibitors. Chem Pharm Bull (Tokyo). 2011;59(2):215-24.
合成参考文献
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 296. 摘要:Gosmini, C.; Corpet, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 631. 摘要:Cruz, F. A.; Dong, V. M., Science of Synthesis, (2019) , 125.