CAS: 52205-73-9; Estramustine Sodium Phosphate

该化合物是一种合成化合物,结合雌激素和氮芥子的特性,使其成为一种独特的乳气化剂,主要用于治疗前列腺癌;化合物作为抗乳粉剂,通过干扰DNA合成和细胞分解而产生作用;磷酸钠通常通过口服方式施用,并因其能够抑制癌症细胞的生长,同时具有某种雌激素诱导活动,从而可能导致与激素变化有关的副作用而闻名;钠盐形式提高了其溶性,增加了其生物利用率;就其化学结构而言,它具有一种磷酸盐组,有助于其药理特性;与许多乳液化剂一样,在治疗期间,监测潜在的副作用,包括胃肠扰动和对血清的影响至关重要.

结构式图片

欧盟法规

ECHA物质ECHA物质C&L通报REACH预注册

合成工艺路线路线简述

    海关参考信息

    专利信息


    专利号:US-8734846-B2
    优先权日:2008-06-16
    标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
    发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
    权利人:BIND BIOSCIENCES INC
    摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

    专利号:US-2013035307-A1
    优先权日:2010-01-26
    标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
    发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
    权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
    摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

    专利号:US-2008214827-A1
    优先权日:2004-02-03
    标 题:Synthesis of Cyanoimino-Benzoimidazoles
    发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
    权利人:EURO CELTIQUE SA
    摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

    专利号:WO-9925385-A1
    优先权日:1997-11-17
    标 题:A method of increasing nucleic acid synthesis with ultrasound
    发明人:UNGER EVAN C; MCCREERY THOMAS; SADEWASSER DAVID
    权利人:IMARX PHARMACEUTICAL CORP
    摘要:The present invention is directed to a method of increasing nucleic acid synthesis in a cell comprising administering to the cell a therapeutically effective amount of ultrasound for a therapeutically effective time such that said administration of said ultrasound results in said increased nucleic acid synthesis. The nucleic acid sequence may comprise an endogenous sequence or an exogenous sequence.

    专利号:US-2021275545-A1
    优先权日:2018-11-21
    标 题 :Method of treating cancer preferably characterized by expression of a fusion protein comprising a member of the e-twenty-six family by administering an agent that inhibits the synthesis and/or activity of cortisol
    发明人:YARDEN YOSEF; SRIVASTAVA SWATI
    权利人:YEDA RES & DEV
    摘要:A method of treating a cancer selected from the group consisting of a myeloid malignancy, a lymphoid malignancy and Ewing's sarcoma is disclosed. The method comprises administering to the subject a therapeutically effective amount of an agent that inhibits the synthesis and/or activity of cortisol.

    专利号:US-6787668-B2
    优先权日:2000-04-13
    标 题 :2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors
    发明人:PITZELE BARNETT S; SIKORSKI JAMES A; WEBBER RONALD KEITH
    权利人:PHARMACIA CORP
    摘要:The present invention is directed to a compound of formula I:or a pharmaceutically acceptable salt thereof, wherein:R1 is selected from the group consisting of H and methyl; andR2 is selected from the group consisting of H and methyl.The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.
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    主要参考文献


    1: Song P, Huang C, Wang Y. The efficacy and safety comparison of docetaxel, cabazitaxel, estramustine, and mitoxantrone for castration-resistant prostate cancer: A network meta-analysis. Int J Surg. 2018 Jun 12. pii: S1743-9191(18)31502-4. doi: 10.1016/j.ijsu.2018.06.010. [Epub ahead of print] doi: 10.26355/eurrev_201804_14706. doi: 10.3892/mco.2017.1480. Epub 2017 Nov 2.
    5: Wei C, Pan Y, Huang H, Li YP. Estramustine phosphate induces prostate cancer cell line PC3 apoptosis by down-regulating miR-31 levels. Eur Rev Med Pharmacol Sci. 2018 Jan;22(1):40-45. doi: 10.26355/eurrev_201801_14098. doi: 10.11406/rinketsu.58.2411. Japanese. doi: 10.1016/j.clgc.2017.10.001. Epub 2017 Oct 16.
    8: Matsumoto T, Hatakeyama S, Ookubo T, Mitsuzuka K, Narita S, Inoue T, Yamashita S, Narita T, Koie T, Kawamura S, Tochigi T, Tsuchiya N, Habuchi T, Arai Y, Ohyama C. Cost-effectiveness comparison between neoadjuvant chemohormonal therapy and extended pelvic lymph node dissection in high-risk prostate cancer patients treated with radical prostatectomy: a multi-institutional analysis. Med Oncol. 2017 Oct 31;34(12):190. doi: 10.1007/s12032-017-1050-y. doi: 10.1016/j.ejps.2017.08.026. Epub 2017 Aug 23. doi: 10.1007/s10147-017-1160-8. Epub 2017 Jul 5.

    合成参考文献


    摘要:Oyo Yakuri. Pharmacometrics., 20(1141), 1980
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