专利号:US-2005119332-A1 优先权日:1998-03-12 标 题 :Substituted thiophene compounds as modulators of protein tyrosine phosphatases (PTPases) 发明人:JEPPESEN LONE; ANDERSEN HENRIK S; OLSEN OLE H; JUDGE LUKE M; HOLSWORTH DANIEL D; BAKIR FARID; AXE FRANK U; GE YU 摘要:The present invention provides novel compounds of formula 1a, n nnovel 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-2002165398-A1 优先权日:1998-03-12 标题:Modulators of protein tyrosine phosphatases (PTPases) 发明人:JEPPESEN LONE; ANDERSEN HENRIK SUNE; OLSEN OLE HVILSTED; JUDGE LUKE MILBURN; HOLSWORTH DANIEL DALE; BAKIR FARID; AXE FRANK URBAN; GE YU 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. n 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 Alzheimers disease and schizophrenia, and infectious diseases.
专利号:US-4554381-A 优先权日:1982-01-21 标题:Process for sulfonylation of halobenzenes 发明人:DESBOIS MICHEL 权利人:RHONE POULENC SPEC CHIM 摘要:A process for sulfonylation of halobenzenes, in which a halobenzene is reacted with a sulfonic acid, a precursor or a derivative thereof in the presence of boron trifluoride in an amount such that the absolute pressure of boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent. The resultant products are useful as intermediates in the synthesis of compounds having a phytosanitary (e.g., herbicidal) or pharmaceutical activity.
专利号:US-2002128496-A1 优先权日:2001-01-12 标题 :Process for the preparation of matrix metalloproteinase inhibitors 发明人:CHANG SOU-JENG; FERNANDO DILINIE P; GUPTA ASHOK; HILL DAVID R; WITTENBERGER STEVEN J 摘要:The present invention discloses a process for the synthesis of reverse hydroxamate matrix metalloproteinase (MMP) inhibitors.
专利号:US-2022401561-A1 优先权日:2019-09-30 标题 :Protein-macromolecule conjugates and methods of use thereof 发明人:SONG YUNTAO; LI HUI; ZHOU HAIPING; LIAO CHUAN 权利人:BEIJING XUANYI PHARMASCIENCES CO LTD 摘要:The present disclosure provides protein-macromolecule conjugates, releasable linkers, and macromolecules, as defined herein. The disclosed conjugates provide unique properties that ae based at least upon the properties of linker and number of linker-Macromolecule moieties. Also provided herein are a method of synthesis and use of conjugates in treating diseases and disorders.
专利号:EP-1383735-A4 优先权日:2001-05-02 标题 :PROCESSES FOR THE SYNTHESIS OF ACYLANILIDES COMPRISING BICALUTAMIDE AND DERIVATIVES THEREOF
[参考文献]: Carol K Wada, Et Al. Phenoxyphenyl Sulfone N-Formylhydroxylamines (Retrohydroxamates) As Potent, Selective, Orally Bioavailable Matrix Metalloproteinase Inhibitors. J Med Chem. 2002 Jan 3;45(1):219-32.
合成参考文献
摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 984.