CAS: 219989-84-1; (1S,3S,7S,10R,11S,12S,16R)-7,11-Dihydroxy-8,8,10,12,16-Pentamethyl-3-((E)-1-(2-Methylthiazol-4-yl)Prop-1-En-2-yl)-17-Oxa-4-Azabicyclo[14.1.0]Heptadecane-5,9-Dione

该化合物是一种合成的蛋白酮,一种可与沙毒类似,作为微囊稳定剂的化合物,类似于沙毒,主要用于治疗转移性乳腺癌,特别是在其他疗法失败的情况下.六甲酸丙酮的化学配方为C22H27N3O4S,其分子重量约为429.54克/摩尔.该复合体展示了一种独特的行动机制,它与微囊-图布林子细胞结合,从而抑制其脱聚合作用并扰乱癌症细胞的正常消毒过程.Ixabepilone的特点是它有能力克服往往限制传统止痛剂有效性的抗药机制.它通过静脉注射进行,其半衰竭时间相对较长,可以减少剂量.侧部影响可能包括外围...

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

CAS号219990-25-7 (3S,6R,7S,8S,12... | CAS号1417803-30-5 (3S,6R,7S,8S)-1... | CAS号219990-23-5 (3S,6R,7S,8S,12... | CAS号152044-54-7 埃博霉素B | CAS号277749-45-8 (5R)-5-hydroxy-... | CAS号277749-36-7 (5S)-5-azido-2-... | CAS号277749-43-6 (4S,7R,8S,9S,16... | CAS号350042-12-5 (3S,6R,7S,8S,12...

合成工艺路线路线简述

  • 合成目标产物 Ixabepilone 主要起始原料 Epothilone B
  • (文献来源)合成步骤主要原料 Epothilone B
(S)-4-(3-Amino-2-Methyl-1(E),5-Hexadienyl)-2-Methylthiazole置于2,6-二甲基吡啶,Sodium Periodate,四氧化锇,正丁基锂,三氟甲磺酸三甲基硅酯,碘,Sodium Hexamethyldisilazane,二甲基二环氧乙烷,N-甲基吗啉氧化物,三乙胺,N,N-二异丙基乙胺,9-硼双环[3.3.1]壬烷,Methanaminium,N-[(Dimethylamino)(3H-1,2,3-Triazolo[4,5-B]Pyridin-3-Yloxy)Methylene]-N-Methyl-,Hexafluorophosphate(1-),三氟乙酸体系中,用 四氢呋喃,二氯甲烷,水,丙酮,叔丁醇 用作溶剂,化学反应 37.33H,反应生成伊沙匹隆
参考文献:Us2014/256952
标题:Us2014/256952

海关参考信息

专利信息


专利号:US-11873305-B2
优先权日:2020-06-30
标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.

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-10975069-B2
优先权日:2014-04-01
标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
发明人:HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN
权利人:UNIV WASHINGTON
摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.

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.
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主要参考文献


1: Smaglo BG, Pishvaian MJ. Profile and potential of ixabepilone in the treatment of pancreatic cancer. Drug Des Devel Ther. 2014 Jul 14;8:923-930. eCollection 2014. Review.
2: Valero V. Managing ixabepilone adverse events with dose reduction. Clin Breast Cancer. 2013 Feb;13(1):1-6. doi: 10.1016/j.clbc.2012.09.003. Epub 2012 Oct 24. Review. doi: 10.1016/j.clbc.2011.03.009. Epub 2011 Apr 20. Review. doi: 10.3109/07853890.2011.579151. Epub 2011 May 17. Review. doi: 10.1586/era.11.41. Review. doi: 10.1186/bcr2573. Epub 2010 Oct 22. Review.
7: Fornier M. Ixabepilone plus capecitabine for breast cancer patients with an early metastatic relapse after adjuvant chemotherapy: two clinical trials. Clin Breast Cancer. 2010 Oct 1;10(5):352-8. doi: 10.3816/CBC.2010.n.046. Review. doi: 10.1007/s00280-010-1467-x. Epub 2010 Oct 1. Review.

合成参考文献


摘要:Alimonti A et al; Anticancer Res 25 (5): 3531-2 (2005).
摘要:American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 1138-9
摘要:American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 1137
摘要:Thomson Health Care Inc.; Physicians' Desk Reference 63 ed., Montvale, NJ 2009, p. 915
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
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