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CAS号378-44-9 倍他米松

原戊酸三甲酯,倍他米松置于对甲苯磺酸体系中,用 N,N-二甲基甲酰胺,苯 用作溶剂,化学反应 1.25H,反应生成倍他米松戊酸酯
参考文献:局部抗炎药的研究.三,合成17种α-酰氧基-9α-氟-11β-羟基-16β-甲基-1,4-孕二烯-3,20-二酮21-硫代衍生物和相关化合物.
标题:局部抗炎药的研究.三,合成17种α-酰氧基-9α-氟-11β-羟基-16β-甲基-1,4-孕二烯-3,20-二酮21-硫代衍生物和相关化合物.
摘要:合成了一系列9-α-氟-11β,17α-二羟基-16β-甲基-1,4-孕二烯-3,20-二酮17-酯的21-硫代衍生物和相关化合物,并将其评估为局部抗炎药代理商.这些化合物是由9个α-氟-11β,17α,21-三羟基-16β-甲基-1,4-孕二烯-3,20-二酮(倍他米松i)17-酯衍生物与各种巯基化合物.结构-活性关系研究表明,在21位的硫基和在17位的酯基的结构组合有助于血管收缩活性.在这些化合物中,发现21-甲硫基17-丙酸酯化合物(6)具有最强的活性,比倍他米松17-戊酸酯(bv)更有效.
Doi:10.1248/cpb.37.3286

专利信息

专利号:US-2023159450-A1
优先权日:2020-05-08
标 题 :Dimers for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-6264962-B1
优先权日:1997-12-19
标 题:Use of cinnamic acid or of at least one of its derivatives in a cosmetic composition
发明人：BRETON LIONEL; GIRERD FLORENCE; RENAULT BEATRICE
权利人:OREAL
摘要:The invention relates to the use of cinnamic acid, or of at least one of its derivatives, in a cosmetic composition as an agent for promoting the synthesis of the skin's total lipids. n The invention also relates to a cosmetic composition comprising an effective amount of cinnamic acid or of at least one of its derivatives.

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-8802660-B2
优先权日:2007-03-12
标 题:De novo synthesis of glucocorticoids in the epidermis and its uses and applications
发明人：TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H
权利人:TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H; UNIV NEW YORK
摘要:The present invention relates to methods and compositions that control, i.e., antagonize/inhibit or agonize/stimulate, de novo glucocorticoid production in the skin. Such methods and compositions can be used for the prevention and/or treatment of a variety of skin conditions, including inflammation, acute wounds, chronic non-healing wounds, keloid, fibrotic or hypertrophic scars, and epithelial-derived cancer.

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.