CAS: 410528-02-8; (E)-4-(2-(3-((1H-Pyrazol-1-yl)Methyl)-5,5,8,8-Tetramethyl-5,6,7,8-Tetrahydronaphthalen-2-yl)Vinyl)Benzoic Acid

该化合物是一种选择性的肾酸受体伽马(RAR-G)抗药性抗药性抗药性伽马(RAR-G),为治疗红细胞性骨质进化(FOP)和其他血清分泌紊乱而研制的抗药性抗药性激素,其行动机制包括调节在异常骨质形成中至关重要的BMP和Wnt信号路径.Palovarotene对RAR-G的高度特殊性将非目标效果降到最低,强化其治疗特征.临床研究显示,它能够有效减少异性同位素骨质化体积,并延缓疾病发.复合展览有利于药性活性植物,可预见的吸收和代谢性,支持一次性口服一次.其有针对性的方法为罕见骨质障碍患者提供了有希望的治疗选择,解决未得到满足的医疗需求.

结构式图片

上下游产品

(E)-Methyl-4-[2-(3-Bromomethyl-5,5,8,8-Tetramethyl-5,6,7,8-Tetrahydro-Naphthalen-2-yl)Vinyl]Benzoate 410528-54-0

合成工艺路线路线简述

    📜Methyl 4-[(E)-2-[5,5,8,8-Tetramethyl-3-(Pyrazol-1-Ylmethyl)-6,7-Dihydronaphthalen-2-Yl]Ethenyl]Benzoate 以97的收率获得产物4-[(1E)-2-[5,6,7,8-四氢-5,5,8,8-四甲基-3-(1H-吡唑-1-基甲基)-2-萘基]乙烯基]苯甲酸
    参考文献:Retinoid Compounds (I)
    标题:Retinoid Compounds (I)
    摘要:当前发明提供了新型视黄醇类化合物及其合成方法,治疗或预防肺气肿,癌症和皮肤疾病的方法,以及适用于治疗或预防肺气肿,癌症和皮肤疾病的药物组合物.

    海关参考信息

    专利信息


    专利号:EP-1935869-A1
    优先权日:2000-10-02
    标题:Retinoids for the treatment of emphysema
    发明人:LAPIERRE JEAN MARC; ROTSTEIN MARC; SJOGREN ERIC BRIAN
    权利人:HOFFMANN LA ROCHE
    摘要:The current invention provides novel retinoid compounds and methods for their synthesis, the use of such compounds for the preparation of medicaments for treating or preventing emphysema, cancer and dermatological disorders, methods for such deseases and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.

    专利号:US-6777418-B2
    优先权日:2000-10-02
    标 题:Retinoid compounds (I)
    发明人:LAPIERRE JEAN-MARC; ROTSTEIN DAVID MARK; SJOGREN ERIC BRIAN
    权利人:SYNTEX LLC
    摘要:The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献

    1. Hind, M., and Stinchcombe, S. Palovarotene, a novel retinoic acid receptor gamma agonist for the treatment of emphysema. Curr. Opin. Investig. Drugs 10(11), 1243-1250 (2009). 2. Sinha, S., Uchibe, K., Usami, Y., et al. Effectiveness and mode of action of a combination therapy for heterotopic ossification with a retinoid agonist and an anti-inflammatory agent. Bone 90, 59-68 (2016). 3. Lees-Shepard, J.B., Nicholas, S.-A.E., Stoessel, S.J., et al. Palovarotene reduces heterotopic ossification in juvenile FOP mice but exhibits pronounced skeletal toxicity. Elife 7, e40814 (2018). 4. Chakkalakal, S.A., Uchibe, K., Convente, M.R., et al. Palovarotene inhibits heterotopic ossification and maintains limb mobility and growth in mice with the human ACVR1R206H fibrodysplasia ossificans progressiva (FOP) mutation. J. Bone Miner. Res. 31(9), 1666-1675 (2016). 5. Pavey, G.J., Qureshi, A.T., Tomasino, A.M., et al. Targeted stimulation of retinoic acid receptor-γ mitigates the formation of heterotopic ossification in an established blast-related traumatic injury model. Bone 90, 159-167 (2016).

    合成参考文献


    摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).
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