5-Chloro-6'-Methyl-3-(4-(Methylsulfonyl)Phenyl)-2,3'-Bipyridin-6-Yl 4-Methylbenzenesulfonate 反应生成依托考昔 参考文献: Process For Making Etoricoxib[fr] Procédé De Préparation D'étoricoxib 标题: Process For Making Etoricoxib[fr] Procédé De Préparation D'étoricoxib 摘要:该发明涉及一种新型工艺和中间体,用于制备具有药用价值的化合物etoricoxib(化学式(1)),该工艺基于使用化合物(4)作为试剂和化合物(5)作为中间体.
专利号:US-2012177593-A1 优先权日:2009-07-20 标 题 :Synthesis of dendrimer conjugates 发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH 权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-9024030-B2 优先权日:2012-01-13 标题 :Process for the synthesis of etoricoxib 发明人:MAO ZHENMIN; LAN TIAN; LIU LANFANG; YAN LONG; BECKER STEFAN 权利人:TIEFENBACHER ALFRED E GMBH & CO KG; SHANGHAI GOLDEN PHARMATECH CO LTD; SHANGHAI GOLDEN PHARMATECH CO LTD 摘要:The present invention relates to a process for the synthesis of the anti-inflammatory agent 5-chloro-3-(4-methanesulfonylphenyl)-6′-methyl-[2,3′]bipyridine, referred to as compound of formula (1) or etoricoxib, which is a pharmaceutically active ingredient inhibiting cyclooxygenase-2. In particular, the application concerns a novel process of making the compound of formula (1) by oxidizing a compound of formula (4).
专利号:US-2004006137-A1 优先权日:2002-06-28 标题:Asymmetric synthesis of amino-pyrrolidinones and a crystalline, free-base amino-pyrrolidinone 发明人:WALTERMIRE ROBERT E; CAMPAGNA SILVIO; SAVAGE SCOTT A; BORDAWEKAR SHAILENDRA; MADUSKUIE THOMAS P; DESIKAN SRIDHAR; ANDERSON STEPHEN R 摘要:A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below is described. n n n These compounds are useful as intermediates for MMP and TACE inhibitors. n Crystalline, free-base form of Compound J ((2R)-2-((3R)-3-amino-3-{-[(2-methyl-4-quinolinyl)methoxy]phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide): n n n which is useful as a TACE inhibitor, pharmaceutical compositions comprising the same, and methods of using the same for treating inflammatory diseases are also described.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:WO-2017100796-A1 优先权日:2015-12-11 标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI 权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.
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