CAS: 63269-31-8; 3-[(R)-Dimethylamino-[(1R,2R)-2-Hydroxycyclohexyl]Methyl]Phenol

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      专利号:US-2012165520-A1
      优先权日:2010-12-23
      标题:Process for the synthesis of prodrugs of opioids
      发明人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS
      权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS
      摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.

      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:WO-2022246227-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-10363247-B2
      优先权日:2015-08-18
      标 题:(S,E)-3-(6-aminopyridin-3-yl)-N-((5-(4-(3-fluoro-3-methylpyrrolidine-1-carbonyl)phenyl-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylamide for the treatment of cancer
      发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM
      权利人:KARYOPHARM THERAPEUTICS INC
      摘要:The invention generally relates to substituted benzofuranyl compounds and, more particularly, to a compound represented by Structural Formula 1a: (I) or a pharmaceutically acceptable salt thereof. The invention also includes the synthesis and use of the compound of Structural Formula 1a, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of diseases or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T-Cell mediated autoimmune disease) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.

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      合成参考文献


      参考文献:10.1016/0014-2999(85)90684-3
      摘要:Thomas Haskins J, Moyer JA, Muth EA, Sigg EB. DMI, Wy-45,030, Wy-45,881 and ciramadol inhibit locus coeruleus neuronal activity. European Journal of Pharmacology. 1985 Sep;115(2-3):139–46. doi: 10.1016/0014-2999(85)90684-3.
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