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-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:AU-2022276509-A1 优先权日:2021-05-20 标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
专利号:US-9994558-B2 优先权日:2013-09-20 标题 :Multicyclic compounds and methods of using same 发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).
专利号:US-4778805-A 优先权日:1987-06-18 标题:4,7-benzofurandione derivatives useful as inhibitors of leukotriene synthesis 发明人:ADAMS JULIAN; GUINDON YVAN; BELANGER PATRICE C; BELLEY MICHEL L; ROKACH JOSHUA 权利人:MERCK FROSST CANADA 摘要:4,7-Benzofurandione derivatives of Formula I, pharmaceutical compositions, and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents. Also disclosed are novel intermediates useful for the preparation of the 4,7-benzofurandiones of this invention. ##STR1##
专利号:WO-2022246227-A1 优先权日:2021-05-20 标 题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
1: Piaz VD, Vergelli C, Giovannoni MP, Scheideler MA, Petrone G, Zaratin P. 4-Amino-3(2H)-pyridazinones bearing arylpiperazinylalkyl groups and related compounds: synthesis and antinociceptive activity. Farmaco. 2003 Nov;58(11):1063-71. Japanese. Japanese. Japanese. Japanese. Japanese. Japanese. Japanese. Japanese.
合成参考文献
摘要:Oyo Yakuri. Pharmacometrics., 16(1011), 1978 参考文献:10.1248/yakushi1947.100.1_105 摘要:Hayashi T, Amino M, Yamaguchi A, Ohki M. [Metabolism of 4-ethoxy-2-methyl-5-morpholino-3(2H)-pyridazinone (M73101), a new anti-inflammatory agent. IV. Plasma concentration and absorption in various animals (author's transl)]. Yakugaku Zasshi. 1980 Jan;100(1):105–9. doi: 10.1248/yakushi1947.100.1_105.