CAS: 30653-83-9; Parsalmide

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📜5-氨基水杨酸置于硫酸,Sodium Isopropylate,1-羟基苯并三唑,N,N'-二环己基碳二亚胺体系中,用 水,N,N-二甲基甲酰胺,异丙醇 用作溶剂,化学反应 2.75H,反应生成帕沙米特
参考文献:Synthesis Of Substituted Benzamides As Anti-Inflammatory Agents That Inhibit Preferentially Cyclooxygenase 1 But Do Not Cause Gastric Damage
标题:Synthesis Of Substituted Benzamides As Anti-Inflammatory Agents That Inhibit Preferentially Cyclooxygenase 1 But Do Not Cause Gastric Damage
摘要:Parsalmide (5-Amino-N-Butyl-2-(2-Propynyloxy) Benzamide) (5A),Is A Non-Steroidal Anti-Inflammatory Drug (Nsaid),Commercialised In Italy Until 1985 With The Brand Name Of Synovial(R),That Has Been Widely Used To Treat Arthritic Patient. In Addition,It Was Shown To Spare Gastric Mucosa. Here We Have Synthesised A Series Of Novel Substituted Benzamides,Related To Parsalmide,And Have Evaluated Their Activity In Vitro On Cox-1 And Cox-2 As Well As In Vivo In The Carrageenin-Induced Rat Paw Edema,A Classical In Vivo Anti-Inflammatory Assay. Compounds 5B,11A And 11B,Which Showed A Favourable Profile In Vitro And In Vivo,Were Screened In Comparison With Parsalmide For Gastrointestinal (Gi) Tolerability In Vivo In The Rat. Results Obtained Showed That Parsalmide And Compound 11B Inhibited Both Cox-1 And Cox-2 In Vitro As Well As They Were Active In Vivo. Both Compounds Were Devoid Of Gastric Effect At The Efficacious Dose. In Addition,Both Prevented Indomethacin-Induced Gastric Damage. Thus,These Compounds May Guide The Definition Of A New Leading Structure With Anti-Inflammatory Activity That May Allow Designing New Safer Nsaids. (C) 2001 Editions Scientifiques Et Medicales Elsevier Sas.
Doi:10.1016/s0223-5234(01)01251-X

专利信息

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-9051302-B2
优先权日:2008-01-15
标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
发明人：WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

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-2023097824-A1
优先权日:2020-05-08
标 题:Semi-synthesis and use of racemic hematoxylin
发明人：DURRANT EDWARD E; HEINDL DIETER; HUBER FLORIAN MAURITIUS ERASUMU; KLEIN ERIC; KOSMEDER II JEROME W; VOSS EDGAR
权利人:VENTANA MED SYST INC; ROCHE DIAGNOSTICS OPERATIONS INC
摘要:A racemic hematoxylin formulation is disclosed that includes one or both of a stabilizer compound and an antioxidant. The disclosed composition exhibits sufficient stability to be utilized in an automated staining process. Methods of using and making the stabilized composition also are disclosed.