9H-Fluoren-9-Ylmethyl (2S,4S)-4-[4-(5-Methyl-2-Phenylpyrazol-3-yl)Piperazin-1-Yl]-2-(1,3-Thiazolidine-3-Carbonyl)Pyrrolidine-1-Carboxylate置于哌啶体系中,用 二氯甲烷 作为反应溶剂,以10.5 G的收率获得产物特力利汀 参考文献:Process For The Preparation Of Teneligliptin 标题:Process For The Preparation Of Teneligliptin 摘要:一种制备替格列奉的方法.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-11466046-B2 优先权日:2014-10-08 标题 :14-membered ketolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.
专利号:US-2012095211-A1 优先权日:2010-09-22 标 题 :Substituted proline inhibitors of hepatitis c virus replication 发明人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D 权利人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D; INTERMUNE INC 摘要:The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.
专利号:US-7595326-B2 优先权日:2005-04-18 标题 :Synthesis of novel tubulin polymerization inhibitors: benzoylphenylurea (BPU) sulfur analogs 发明人:KHAN SAEED R; HALLUR GURULINSAPPA; HIDALGO MANUEL; JIMENO ANTONIO 权利人:CHAMPIONS BIOTECHNOLOGY INC 摘要:A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6 n and 7 d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6 n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6 n retained significant ability to inhibit tubulin assembly, with an IC 50 of 2.1 μM.
专利号:US-7125986-B2 优先权日:1997-12-29 标题:Penicillanic acid derivative compounds and methods of making 发明人:BUYNAK JOHN D; RAO AKIREDDY SRINIVASA; DOPPALAPUDI VENKATA RAMANA 权利人:UNIV SOUTHERN METHODIST 摘要:Compounds of formula I: n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
专利号:US-9422321-B2 优先权日:2010-09-07 标题 :Pyrimidine nucleoside derivatives, synthesis methods and uses thereof for preparing anti-tumor and anti-virus medicaments 发明人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE 权利人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE; HIGH & NEW TECH RES CENTER HENAN ACAD OF SCIENCES; ZHENGZHOU GRANLEN PHARMATECH LTD; UNIV ZHENGZHOU 摘要:The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: n nAlso disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.
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合成参考文献
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