专利号:US-8546532-B2 优先权日:2008-04-17 标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders 发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS 权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
专利号:US-2013035307-A1 优先权日:2010-01-26 标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers 发明人:PRESTWICH GLENN D; KENNEDY THOMAS P 权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P 摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
专利号:US-7411031-B2 优先权日:2001-11-23 标 题 :Synthesis of polyanhydrides 发明人:UHRICH KATHRYN E; SCHMELTZER ROBERT C; ANASTASIOU THEODORE JAMES 权利人:UNIV RUTGERS 摘要:The present invention provides a method for forming compounds of Formulan nHO—C(â•?O)R 1 —X—R 2 —X—R 1 —C(â•?O)—O—Hn nwherein compound (I) can be polymerized to provide a polymer that contains therapeutically active compounds. In the compounds of the invention, each R 1 is group that will provide the therapeutically active compound upon hydrolysis of the polymer; each X is independently an ester linkage or an amide linkage; and R 2 is a linking group.
专利号:US-8754197-B2 优先权日:2004-07-07 标题:Synthesis of azo bonded immunoregulatory compounds 发明人:RIGGS-SAUTHIER JENNIFER A; EKWURIBE NNOCHIRI N 权利人:RIGGS-SAUTHIER JENNIFER A; EKWURIBE NNOCHIRI N; BIOCON LTD 摘要:Methods are disclosed for preparing compounds of Formula I: n nwhere R 1 , R 3 , and R 4 are independently hydrogen or C 1 to C 4 alkyl, and R 2 is:n n nwhere R 5 is selected from the group consisting of hydrogen and C 1 to C 4 alkyl, orn n nwhere R 6 , R 7 and R 8 are independently hydrogen or C 1 to C 4 alkyl; or the esters or pharmacologically acceptable salts thereof. The compounds and or their metabolites can be used to treat or prevent various diseases, particularly inflammatory conditions of the GI tract.
专利号:US-7309799-B2 优先权日:2004-06-01 标 题:Methods for the synthesis of milnacipran and congeners thereof 发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V 权利人:COLLEGIUM PHARMACEUTICAL INC 摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.
1: El-Kawy OA, Ibrahim IT, Farah K. Technetium-99 m labeling and evaluation of olsalazine: a novel agent for ulcerative colitis imaging. J Labelled Comp Radiopharm. 2015 Jun 30;58(8):336-41. doi: 10.1002/jlcr.3306. Epub 2015 Jun 1. doi: 10.1002/cmdc.201300555. Epub 2014 Jan 31. doi: 10.1021/jacs.6b03523. Epub 2016 Aug 3. doi: 10.1007/s11096-013-9778-8. Epub 2013 Apr 27. doi: 10.1016/j.jchromb.2015.11.001. Epub 2015 Nov 4. Review. doi: 10.1016/j.ijpharm.2011.04.028. Epub 2011 Apr 22. Review.
合成参考文献
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