CAS: 247062-33-5; Abaloparatide

该化合物是主要用于治疗骨质疏松症的合成类固醇荷尔蒙相关蛋白(PTHP)的合成类比,主要用于治疗骨质疏松症.它充当了对除虫菊激素1受体(PTH1R)的选择性活化器,通过刺激骨质疏松活动促进骨质形成.临床研究表明它在提高骨质矿密度(BMD)和降低骨质疏松症后期女性骨折风险方面的效力.与其他新陈代谢疗法相比,巴洛对硫化物展示了一种有利于安全且高血清发病率较低的安全特征.它的亚皮内皮管管理和可预测的药用动力进一步增强了其临床效用.该化合物的定向机制和稳健的临床数据支持其作为管理骨质疏松症的宝贵治疗选项的作用.

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      专利号:US-11806387-B1
      优先权日:2022-05-20
      标 题 :Process of making abaloparatide
      发明人：BURKE MATT; CAMPAGNA SILVIO
      权利人:RADIUS HEALTH INC
      摘要:Disclosed herein is an improved process for preparing abaloparatide. The process generally utilizes solid phase peptide synthesis employing an Fmoc-protection scheme. Incorporating a systematic recoupling step of a glutamine residue (Gln 16 ) has been found to minimize the formation of an undesirable des-Gln 16 abaloparatide impurity, which is often obtained in significant quantities in the conventional process.

      专利号:US-11512123-B2
      优先权日:2020-05-11
      标 题:Method for removing water from compound solution and performing conjugate acid conversion
      发明人：HSU YAO-LUNG; HSIEH KUANG-CHAN; CHENG HUI-WEN; Yang zong-han
      权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD
      摘要:The present invention relates to a method for removing water from a compound solution and performing conjugate acid conversion. The method uses a nanometer film to perform reverse osmosis for the compound solution to remove water, and provides a conjugate acid to replace the acidic substances in the compound solution in order to obtain compound conjugate acid salts. The method of the present invention can effectively reduce the water content of the compound solution and replace the conjugate acid of the compound to form the desired compound conjugate acid salt.

      专利号:CN-113880936-A
      优先权日:2021-12-07
      标题:A kind of solid-phase synthesis method of abaparatide

      专利号:CN-113880936-B
      优先权日:2021-12-07
      标 题 :A kind of solid-phase synthesis method of abaparatide

      专利号:CN-111087462-A
      优先权日:2018-10-24
      标题 :A kind of solid-phase synthesis method of abaparatide

      专利号:CN-116023467-A
      优先权日:2022-12-28
      标题:A kind of solid-phase synthesis method of abaloparatide

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      合成参考文献


      参考文献:10.1007/s00198-017-3919-1
      摘要:McClung MR, Wagman RB, Miller PD, Wang A, Lewiecki EM. Observations following discontinuation of long-term denosumab therapy. Osteoporosis International. 2017 Jan 31;28(5):1723–32. doi: 10.1007/s00198-017-3919-1.
      参考文献:10.1016/j.maturitas.2016.12.003
      摘要:Chew CK, Clarke BL. Abaloparatide: Recombinant human PTHrP (1-34) anabolic therapy for osteoporosis. Maturitas. 2017 Mar;97():53–60. doi: 10.1016/j.maturitas.2016.12.003.
      参考文献:10.1016/j.mayocp.2016.10.009
      摘要:Cosman F, Miller PD, Williams GC, Hattersley G, Hu MY, Valter I, Fitzpatrick LA, Riis BJ, Christiansen C, Bilezikian JP, Black D. Eighteen Months of Treatment With Subcutaneous Abaloparatide Followed by 6 Months of Treatment With Alendronate in Postmenopausal Women With Osteoporosis: Results of the ACTIVExtend Trial. Mayo Clin Proc. 2017 Feb;92(2):200–10. doi: 10.1016/j.mayocp.2016.10.009.
      参考文献:10.1007/s00223-018-0422-4
      摘要:Makino A, Takagi H, Takahashi Y, Hase N, Sugiyama H, Yamana K, Kobayashi T. Abaloparatide Exerts Bone Anabolic Effects with Less Stimulation of Bone Resorption-Related Factors: A Comparison with Teriparatide. Calcified Tissue International. 2018 May 03;103(3):289–97. doi: 10.1007/s00223-018-0422-4.
      参考文献:10.1007/s11914-018-0440-1
      摘要:Roberts SJ, Ke HZ. Anabolic Strategies to Augment Bone Fracture Healing. Current Osteoporosis Reports. 2018 May 03;16(3):289–98. doi: 10.1007/s11914-018-0440-1.
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