CAS: 181630-15-9; Picoplatin

该化合物是一种基于白金的乳胶化剂,被归类为第二代的白金化合物,旨在克服与诸如皮白素和卡白白素等传统白金药物有关的某些限制,特别是抗药性和毒性方面的限制.皮白质展示了一种独特的行动机制,主要是通过形成DNA交叉链路,它破坏了DNA的复制和转录,最终导致癌症细胞死亡.它的化学结构包括一种丙烯酸皮条,它与其他白金化合物相比,提高了其溶性与生物利用率.皮白质在治疗各种癌症,包括固态肿瘤和转移性癌症的临床前期和临床研究中显示出了希望.它的致癌学表明一种有利的分布特征,而且一般是静脉注射.尽管它已经显示出有效性,但正在进行的研究继续评估其安全状况,最佳剂量疗法和潜在副作用,这可能包括乳胶压和肾中毒病原药,这代表了其他有目标的癌症治疗的发展.

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    专利信息


    专利号:US-2012123121-A1
    优先权日:2009-06-12
    标题:Synthesis of picoplatin
    发明人:LEIGH ALISTAIR J; JOST STEFFEN
    权利人:LEIGH ALISTAIR J; JOST STEFFEN; PONIARD PHARMACEUTICALS INC
    摘要:An improved method for the synthesis of the anticancer drug picoplatin is provided. Condensation of a tetrachloroplatinate salt (TCP), such as potassium tetrachloroplatinate, and 2-picoline, in a solvent, is catalyzed by the presence of oxygen, such as in air, and additionally catalyzed by the presence of a Pt +4 complex, such as potassium hexachloroplatinate. The oxygen can be introduced into the reaction mixture by sparging, optionally with high shear mixing and under an inert gas headspace. The product trichloropicolineplatinate salt (TCPP) is a key intermediate in the synthesis of picoplatin, to which it can be converted by reaction of the TCPP with ammonia.

    专利号:WO-2017100796-A1
    优先权日:2015-12-11
    标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
    权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.

    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

    专利号:US-8828984-B2
    优先权日:2012-11-19
    标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection
    发明人:CHE CHI MING; ZOU TAOTAO
    权利人:UNIV HONG KONG; UNIV HONG KONG
    摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.

    专利号:US-10577387-B1
    优先权日:2018-08-09
    标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment
    发明人:CHE CHI MING; Fung Sin Ki; Chen tian feng
    权利人:UNIV HONG KONG
    摘要:Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

    专利号:US-11286271-B2
    优先权日:2018-07-31
    标 题 :Iridium (III) complexes containing N-heterocyclic carbene ligand, synthesis, and their use thereof in cancer treatment
    发明人:CHE CHI MING; LAM TSZ LUNG; TONG KA CHUNG
    权利人:UNIV HONG KONG
    摘要:Provided herein are Ir(III) complexes comprising N-heterocyclic carbene ligand, method of synthesis of the Ir(III) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Ir(III) complexes under both dark and light conditions. Also provided is a method of detecting the Ir(III) complex in a biological system. Also provided is a method of making the Ir(III) complex. The Ir(III) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

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    主要参考文献


    1: Wheate NJ, Walker S, Craig GE, Oun R. The status of platinum anticancer drugs in the clinic and in clinical trials. Dalton Trans. 2010 Jun 30. [Epub ahead of print] Epub 2010 Apr 6. Review. Epub 2009 Mar 16. Review. Review.

    合成参考文献


    参考文献:10.1007/978-1-59259-735-2_1
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