专利号:US-8138272-B2 优先权日:2006-05-22 标 题:Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds 发明人:KONRADI ANDREI W; SMITH JENIFER L 权利人:KONRADI ANDREI W; SMITH JENIFER L; ELAN PHARM INC 摘要:This invention provides an improved synthesis of polymer conjugates of formula (I), n nof agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treating primary or secondary alcohol substituents of active compounds with polymeric nucleophiles using “Mitsunobuâ€? or related reaction conditions.
专利号:US-6872716-B2 优先权日:2000-09-11 标题:Antipsychotic sulfonamide-heterocycles, and methods of use thereof 发明人:WU XINHE; AQUILA BRIAN M; SHAO LIMING; RADEKE HEIKE; CUNY GREGORY D; HAUSKE JAMES R; XIE ROGER L 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.
专利号:WO-2021062168-A1 优先权日:2019-09-25 标 题 :Synthetic sphingolipid inspired molecules with heteroaromatic appendages, methods of their synthesis and methods of treatment 发明人:EDINGER AIMEE; HANESSIAN STEPHEN 权利人:UNIV CALIFORNIA; UNIV MONTREAL 摘要:Small molecules compounds and methods of their synthesis are provided. Formulations and medicaments are also provided that are directed to the treatment of disease, such as, for example, neoplasms, cancers, and other diseases. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration.
专利号:US-10450282-B2 优先权日:2015-08-06 标题:Stereospecific process for 3-heterocyclylcycloaliphatic-1,2-diols 发明人:OHLMEYER MICHAEL; ZAWARE NILESH; KASTRINSKY DAVID 权利人:ICAHN SCHOOL MED MOUNT SINAI 摘要:A process for the stereoselective synthesis of chiral 3-heterocyclyl-1,2-dihydroxy cyclohexanes is disclosed. The process involves reacting a tricyclic nitrogenous heterocycle with an allyl carbonate in the presence of a chiral palladium catalyst followed by oxidation of the olefinic bond to provide 3-heterocyclyl-1,2-dihydroxy cyclohexanes, cyclopentanes and corresponding alicyclic heterocycles. Also disclosed are methods for converting the heterocyclyl-1,2-dihydroxy cyclohexanes to 2-amino-6-(heteroaryl)cyclohexanols (and related cyclic compounds).
专利号:EP-1836163-B1 优先权日:2004-12-23 标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin 发明人:BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER 权利人:NOVARTIS AG 摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.
专利号:US-10246411-B2 优先权日:2014-10-29 标 题:(Z)-3,4,5-trimethoxystyrylbenzenesulfonamides as potential anticancer agents 发明人:KAMAL AHMED; RASALA MAHESH; RATNA REDDY CHALLA; BHARATH KUMAR GAJJELA; SASTRY VISWESWARA; BASHA SHAIK ANVER; SANTHOSH REEDY VANGALA 权利人:COUNCIL SCIENT IND RES 摘要:This present invention relates to (Z)-3,4,5-Trimethoxystyrylbenzenesulfonamides of general formula A. The invention also provides the synthesis of (Z)-3,4,5-trimethoxystyrylbenzenesulfonamides useful as potential antitumor agents against human cancer cell lines and a process for the preparation thereof.
参考标题:Base-Mediated Tandem Sulfonylation And Oximation Of Alkenes In Water 作者:Bin Wang,Lin Tang,Liyan Liu,Yanan Li,Yu Yang,Zhiyong Wang 摘要:A Base-Mediated Bifunctionalization Of Alkenes For The Synthesis Of α-Sulfonylethanone Oximes Was Developed In Water Under Metal-Free Conditions. This Reaction Features A Wide Substrate Scope And Facile Starting Materials To Afford The Desired Products In High Yields.
合成参考文献
参考文献:10.1055/s-0040-1706790 摘要:Selective Activation of Protein Phosphatase 2A Complexes. Synfacts. 2020 Aug 18;16(09):1103. doi: 10.1055/s-0040-1706790.