📜N'1,N'3-Dibenzoyl-N'1,N'3-Dimethylmalonohydrazide置于高氯酸,Sodium Sulfide,盐酸体系中,用 水,丙酮 作为反应溶剂,化学反应 0.5H,反应生成 伊利司莫 参考文献:Syntheses And Antitumor Activities Of N'1,N'3-Dialkyl-N'1,N'3-Di-(Alkylcarbonothioyl) Malonohydrazide: The Discovery Of Elesclomol 标题:Syntheses And Antitumor Activities Of N'1,N'3-Dialkyl-N'1,N'3-Di-(Alkylcarbonothioyl) Malonohydrazide: The Discovery Of Elesclomol 摘要:A Series Of N'(1),N'(3)-Dialkyl-N'(1),N'(3)-Di(Alkylcarbonothioyl) Malonohydrazides Have Been Designed And Synthesized As Anticancer Agents By Targeting Oxidative Stress And Hsp70 Induction. Structure-Activity Relationship (Sar) Studies Lead To The Discovery Of Sta-4783 (Elesclomol),A Novel Small Molecule That Has Been Evaluated In A Number Of Clinical Trials As An Anticancer Agent In Combination With Taxol. (C) 2013 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2013.07.032
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-7709683-B2 优先权日:2005-05-16 标 题:Synthesis of bis(thio-hydrazide amide) salts 发明人:CHEN SHOUJUN; XIA ZHI-QIANG 权利人:SYNTA PHARMACEUTICALS CORP 摘要:A method of preparing a bis(thio-hydrazide amide) disalt includes the steps of combining a neutral bis(thio-hydrazide amide), an organic solvent and a base to form a bis(thio-hydrazide amide) solution; and combining the solution and methyl tert-butyl ether, thereby precipitating a disalt of the bis(thio-hydrazide amide). n In some embodiments, a method of preparing a bis(thio-hydrazide amide) disalt includes the steps of combining a neutral bis(thio-hydrazide amide) and an organic solvent selected from methanol, ethanol, acetone, and methyl ethyl ketone to make a mixture; adding at least two equivalents of a base selected from sodium hydroxide, potassium hydroxide, sodium methoxide, potassium methoxide, sodium ethoxide and potassium ethoxide to the mixture, thereby forming a solution; and combining the solution and methyl tert-butyl ether to precipitate the disalt of the bis(thio-hydrazide amide). n The disclosed methods do not require lyophilization and the solvents used in the process can be more readily removed to low levels consistent with pharmaceutically acceptable preparation.
专利号:US-7652168-B2 优先权日:2001-07-10 标 题 :Synthesis of taxol enhancers 发明人:CHEN SHOUJUN; SUN LIJUN; XIA ZHI-QIANG; KOVA KEIZO; ONO MITSUNORI 权利人:SYNTA PHARMACEUTICALS CORP 摘要:Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound. The hydrazide starting compound is represented by Structural Formula (I): n nThe thiohydrazide product compound is represented by Structural Formula (II):n n nIn Structural Formulas (I)-(II), R 1 and R 2 are independently an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R 1 and R 2 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. When R 2 is an aryl group or a substituted aryl group, then R 5 is a hydrazine protecting group; and when R 2 is an aliphatic or substituted aliphatic group, then R 5 is —H or a hydrazine protecting group. R 10 is —H or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent.
专利号:US-2022363662-A1 优先权日:2021-04-20 标题 :Compounds as lxr agonists 发明人:PUJALA BRAHMAM; SATHE BALAJI DASHRATH; DANODIA ABHINANDAN; GUPTA ASHU; SONI SANJEEV; KUMAR VIVEK; ANSARI AMANTULLAH; KHAN FARHA; SARKAR ARINDAM; PAYGHAN PAVAN V 权利人:INTEGRAL BIOSCIENCES PRIVATED LTD 摘要:The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.
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).