专利号:US-2008125354-A1 优先权日:2005-11-21 标题 :Selective inhibition of matrix metalloproteinases 发明人:FIELDS GREGG B; HAMMER ROBERT 权利人:UNIV FLORIDA ATLANTIC; UNIV LOUISIANA STATE 摘要:Synthetic triple-helical peptides (THPs) are used for the design and synthesis of triple-helical transition state analog inhibitors. These inhibitors feature a phosphonate ester or phosphinic moiety in place of the scissle bond. These groups inhibit MMPs, and methods been developed for their convenient incorporation within a peptide sequence by solid-phase methods.
专利号:US-4230624-A 优先权日:1977-09-02 标 题 :Process for the synthesis of derivatives of the benzofuran, chromene and isochromene type 发明人:LE CORRE MAURICE; HERCOUET ALAIN; BEGASSE BEATRICE 权利人:ANVAR 摘要:The invention relates to a process for the production of therapeutic compounds of the benzofuran, chromene and isochromene type of the general formula; in which formula, R1 and R3=H, lower alkyl, aralkyl or cycloalkyl R2=H or an organic radical and when D= R1 and R3 may represent an organic radical. The process comprising the cyclization in the liquid phase and in the presence of a base a compound of the formula; in which formula; R'=an alkyl, aryl or aralkyl radical and X-=an anion.
专利号:US-8816129-B2 优先权日:2010-08-06 标 题:PTP1B inhibitors, synthesis thereof and application thereof in preparation of medicaments for treating type 2 diabetes mellitus 发明人:SHI DAYONG; GUO SHUJU; FAN XIAO; LU WEISHEN; CUI YONGCHAO 权利人:SHI DAYONG; GUO SHUJU; FAN XIAO; LU WEISHEN; CUI YONGCHAO; INST OCEANOLOGY CHINESE ACAD 摘要:The present invention relates to chemical total synthesis methods of six novel protein tyrosine phosphatase-1B (PTP1B) inhibitors and application of the inhibitors in the preparation of medicaments for treating type 2 diabetes mellitus (T2DM). The PTP1B inhibitors use one or more of the six compounds represented by the structural formulae 1, 2, 3, 4, 5 and 6, as active components. The compounds can enhance the sensitivity of an insulin receptor by inhibiting the activity of PTP1B, thereby having a favorable therapeutic effect on insulin-resistant T2DM.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-9018249-B2 优先权日:2011-09-13 标题 :SGLT inhibitors 发明人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR 权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD 摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).
专利号:US-2014228303-A1 优先权日:2011-06-13 标题 :Novel sglt inhibitors 发明人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR 权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD 摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).
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