CAS: 172673-20-0; Fosaprepitant

该化合物是一种合成化合物,主要用作抗乳剂,防止与化疗有关的恶心和呕吐;是一种先生药,这意味着它会转化成体内的活性形态;Fosapritant 功能是...

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    专利号:US-2022118123-A1
    优先权日:2019-02-22
    标 题 :Combination of ar antagonists and targeted thorium conjugates
    发明人:HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
    权利人:BAYER AG; BAYER AS
    摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.

    专利号:US-2010160247-A1
    优先权日:2008-06-17
    标题 :Synthesis of deuterated morpholine derivatives

    专利号:US-9453009-B2
    优先权日:2008-06-17
    标题 :Synthesis of deuterated morpholine derivatives
    发明人:LIU JULIE F; TANG XUEJUN; HARBESON SCOTT L; MASSE CRAIG E
    权利人:CONCERT PHARMACEUTICALS INC
    摘要:The present invention is directed to a process for preparing a 2,26,6-d 4 -morpholine derivative represented by Structural Formula (I): n nor a salt thereof.

    专利号:US-2015099714-A1
    优先权日:2008-06-17
    标 题 :Synthesis of deuterated morpholine derivatives

    专利号:US-8354557-B2
    优先权日:2008-06-17
    标题 :Synthesis of deuterated morpholine derivatives

    专利号:WO-2009154754-A2
    优先权日:2008-06-17
    标题:Synthesis of deuterated morpholine derivatives
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    主要参考文献


    1: Weinstein C, Jordan K, Green SA, Camacho E, Khanani S, Beckford-Brathwaite E, Pong A, Noga SJ, Rapoport BL. Evaluation of factors contributing to the response to fosaprepitant in a heterogeneous, moderately emetogenic chemotherapy population: an exploratory analysis of a randomized phase III trial. Support Care Cancer. 2018 May 28. doi: 10.1007/s00520-018-4242-x. [Epub ahead of print] doi: 10.1016/j.critrevonc.2018.02.001. Epub 2018 Feb 7. Review. doi: 10.2147/DDDT.S155875. eCollection 2018.
    8: O'Sullivan CC, Van Houten HK, Sangaralingham LR, Leal AD, Shinde S, Liu H, Ettinger D, Loprinzi CL, Ruddy KJ. Ten-Year Trends in Antiemetic Prescribing in Patients Receiving Highly Emetogenic Chemotherapy. J Natl Compr Canc Netw. 2018 Mar;16(3):294-299. doi: 10.6004/jnccn.2017.7043. doi: 10.1155/2017/5703528. Epub 2017 Dec 19.
    10: Yamamoto K, Yamatodani A. Strain differences in the development of cisplatin-induced pica behavior in mice. J Pharmacol Toxicol Methods. 2018 May - Jun;91:66-71. doi: 10.1016/j.vascn.2018.01.559. Epub 2018 Jan 31. doi: 10.1634/theoncologist.2017-0378. Epub 2018 Jan 12.

    合成参考文献


    参考文献:10.1007/s10637-018-0607-8
    摘要:Molinos-Quintana A, Trujillo-Hacha P, Piruat JI, Bejarano-García JA, García-Guerrero E, Pérez-Simón JA, Muñoz M. Human acute myeloid leukemia cells express Neurokinin-1 receptor, which is involved in the antileukemic effect of Neurokinin-1 receptor antagonists. Invest New Drugs. 2019 Feb;37(1):17–26. doi: 10.1007/s10637-018-0607-8.
    参考文献:10.1186/s12913-019-4281-0
    摘要:Kashiwa M, Matsushita R. Cost-utility analysis of palonosetron in the antiemetic regimen for cisplatin-containing highly emetogenic chemotherapy in Japan. BMC Health Services Research. 2019 Jul 01;19(1):438. doi: 10.1186/s12913-019-4281-0.
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