CAS: 945595-80-2; N-(4-((3-(2-Aminopyrimidin-4-yl)Pyridin-2-yl)Oxy)Phenyl)-4-(4-Methylthiophen-2-yl)Phthalazin-1-Amine

该化合物是一种合成有机化合物,其特征是其复杂的分子结构,包括多个芳香环和功能组.该化合物具有phthalazinamine核心特征,该核心与硫基集团和通过一种醚联系的苯丁基-丙胺基-丙胺基-丙胺基-丙酰胺联系有关.氨基和甲基组的存在有助于其潜在的生物活动.一般而言,这种化合物因其药理特性,包括它们作为各种疾病的潜在治疗剂的作用而受到调查.其外表和功能组的复杂安排表明,它可能表现出与生物目标的具体互动关系,因此对药用化学具有兴趣.此外,其溶性,稳定性和再活性将取决于实验环境中使用的具体条件和溶剂.

结构式图片

物理性质

MSDS等安全信息

欧盟法规

C&L通报

上下游产品

4-(2-chloropyridin-3-yl)pyrimidin-2-amine 4-amino-phenol (E)-1-(2-chloropyridin-3-yl)-3-(dimethylamino)-prop-2-en-1-one 1-chloro-4-(4-methylthiophen-2-yl)phthalazine

合成工艺路线路线简述

  • 149549-12-2 + 945599-45-1 = 945595-80-2
    反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Dimethyl Sulfoxide; 2 H,80 °C
    标题:Preparation Of Crystalline Forms Of N-(4-((3-(2-Amino-4-Pyrimidinyl) - 2-Pyridinyl)Oxy)Phenyl)-4-(4-Methyl-2-Thienyl)-1 -Phthalazinamine Pharmaceutically Acceptable Salts For The Treatment Of Cancer
    参考文献:World Intellectual Property Organization]

    149549-12-2 + 945599-45-1 = 945595-80-2
    反应条件:1.1 Solvents: Tert-Butanol; 16 H,100 °C
    标题:N-(4-((3-(2-Amino-4-Pyrimidinyl)-2-Pyridinyl)Oxy)Phenyl)-4-(4-Methyl-2-Thienyl)-1-Phthalazinamine For Use In The Treatment Of Antimitotic Agent Resistant Cancer
    参考文献:World Intellectual Property Organization]

    149549-12-2 + 945599-45-1 = 945595-80-2
    反应条件:1.1 Solvents: (+/-)-2-Butanol; 6 H,100 °C
    标题:Discovery Of N-(4-(3-(2-Aminopyrimidin-4-Yl)Pyridin-2-Yloxy)Phenyl)-4-(4-Methylthiophen-2-Yl)Phthalazin-1-Amine (Amg 900),A Highly Selective,Orally Bioavailable Inhibitor Of Aurora Kinases With Activity Against Multidrug-Resistant Cancer Cell Lines
    作者:Geuns-Meyer,Stephanie; Cee,Victor J.; Deak,Holly L.; Du,Bingfan; Hodous,Brian L.; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2015 卷标:58(13) 页码:5189-5207]

    149549-12-2 + 945599-45-1 = 945595-80-2
    反应条件:1.1 Solvents: Tert-Butanol; 16 H,100 °C1.2 Reagents: Sodium Carbonate Solvents: Diethyl Ether,Water
    标题:Use Of N-(4-((3-(2-Amino-4-Pyrimidinyl)-2-Pyridinyl)Oxy)Phenyl)-4-(4-Methyl-2-Thienyl)-1-Phthalazinamine In Combination With Histone Deacetylase Inhibitors For Treatment Of Cancer
    参考文献:United States]

    149549-12-2 + 945599-45-1 = 945595-80-2
    反应条件:1.1 Solvents: Tert-Butanol; 16 H,100 °C
    标题:Use Of Amg 900 For The Treatment Of Cancer
    参考文献:World Intellectual Property Organization]

    149549-12-2 + 945599-45-1 = 945595-80-2
    反应条件:1.1 Reagents: Tert-Butanol; 16 H,100 °C
    标题:Use Of N-(4-((3-(2-Amino-4-Pyrimidinyl) -2-Pyridinyl)Oxy)Phenyl)-4-(4-Methyl-2-Thienyl)-1-Phthalazinamine In Combination With Histone Deacetylase Inhibitors For Treatment Of Cancer
    参考文献:World Intellectual Property Organization]

    149549-12-2 + 945599-45-1 = 945595-80-2
    反应条件:1.1 Solvents: Tert-Butanol; 16 H,100 °C
    标题:Preparation Of Substituted Phthalazinamines As Aurora Kinase Modulators
    参考文献:World Intellectual Property Organization]

    = 945595-80-2 [标题:Reaction Conditions
    标题:Preparation Of Substituted Phthalazinamines As Aurora Kinase Modulators
    参考文献:United States
📜3-甲基噻吩置于2,2,6,6-Tetramethylpiperidin-4-Yl Heptanoate,异丙基氯化镁,肼,三氯氧磷体系中,用 四氢呋喃,乙醇,水,二甲基亚砜,乙腈 作为反应溶剂,化学反应 43.0H,反应生成 莪术醇.姜黄醇
参考文献: Crystalline Forms Of N-(4-((3-(2-Amino-4-Pyrimidinyl)-2-Pyridinyl)Oxy)Phenyl)-4-(4-Methyl-2-Thienyl)-1-Phthalazinamine Pharmaceutically Acceptable Salts And Uses Thereof[fr] Formes Cristallines De Sels Pharmaceutiquement Acceptables De La N-(4-((3-(2-Amino-4-Pyrimidinyl)-2-Pyridinyl)Oxy)Phényl)-4-(4-Méthyl-2-Thiényl)-1-Phtalazinamine Et Leurs Utilisations
标题: Crystalline Forms Of N-(4-((3-(2-Amino-4-Pyrimidinyl)-2-Pyridinyl)Oxy)Phenyl)-4-(4-Methyl-2-Thienyl)-1-Phthalazinamine Pharmaceutically Acceptable Salts And Uses Thereof[fr] Formes Cristallines De Sels Pharmaceutiquement Acceptables De La N-(4-((3-(2-Amino-4-Pyrimidinyl)-2-Pyridinyl)Oxy)Phényl)-4-(4-Méthyl-2-Thiényl)-1-Phtalazinamine Et Leurs Utilisations
摘要:本发明涉及药用可接受盐的晶型和共晶型形式,该盐为化合物n-(4-((3-(2-氨基-4-嘧啶基)-2-吡啶基)氧基)苯基)-4-(4-甲基-2-噻吩基)-1-鞣酸苄胺(amg 900),以及包括所述晶型和共晶型形式的药物组合物.该发明还提供了利用这些晶型和组合物治疗癌症的用途,包括各种固体肿瘤和血液癌症,包括骨髓瘤和白血病.

海关参考信息

专利信息


专利号:US-2017107577-A1
优先权日:2014-03-11
标题:Determining Cancer Aggressiveness, Prognosis and Responsiveness to Treatment
发明人：AL-EJEH FARES
权利人:THE COUNCIL OF THE QUEENSLAND INST OF MEDICAL RES
摘要:The invention provides methods of determining the aggressiveness, prognosis and response to therapy for particular cancers, which include comparing the expression levels of one or a plurality of differentially expressed genes from one or more 5 functional metagenes, including a Carbohydrate/Lipid Metabolism metagene, a Cell Signalling metagene, a Cellular Development metagene, a Cellular Growth metagene, a Chromosome Segregation metagene, a DNA Replication/Recombination metagene, an Immune system metagene, a Metabolic Disease metagene, a Nucleic Acid Metabolism metagene, a Post-Translational Modification metagene, a Protein 10 Synthesis/Modification metagene and a Multiple Networks metagene. The method disclosed herein may be particularly suitable as a companion diagnostic for cancer therapies.

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

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主要参考文献


1: Waldon D, Berry L, Lin MH, Schenkel L, Hollis LS, Zhao Z. Gender Effects on Rat Metabolism of AMG 900, an Orally Available Small Molecule Aurora Kinase Inhibitor. Drug Metab Lett. 2011 Oct 21. [Epub ahead of print] Epub 2011 Feb 4. Epub 2010 Oct 8.

合成参考文献


参考文献:10.1016/j.jpba.2012.10.026
摘要:Be X, Moore ES, Zhao Z, Wells MC. LC–MS/MS bioanalytical method development for AMG 900: Resolution of an isobaric interference in rodent in vivo studies. Journal of Pharmaceutical and Biomedical Analysis. 2013 Feb;74():171–7. doi: 10.1016/j.jpba.2012.10.026.
参考文献:10.1016/j.bmcl.2022.128614
摘要:Rybin MJ, Laverde-Paz MJ, Suter RK, Affer M, Ayad NG, Feng Y, Zeier Z. A dual aurora and lim kinase inhibitor reduces glioblastoma proliferation and invasion. Bioorganic & Medicinal Chemistry Letters. 2022 Apr;61():128614. doi: 10.1016/j.bmcl.2022.128614.
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