N-(4-{[(6s)-2-(Hydroxymethyl)-4-Oxo-4,6,7,8-Tetrahydro-1h-Cyclopenta[g]quinazolin-6-Yl](Prop-2-Yn-1-Yl)amino}benzoyl)-L-Gamma-Glutamyl-D-Glutamic Acid | 501332-69-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-(4-{[(6s)-2-(Hydroxymethyl)-4-Oxo-4,6,7,8-Tetrahydro-1h-Cyclopenta[g]quinazolin-6-Yl](Prop-2-Yn-1-Yl)amino}benzoyl)-L-Gamma-Glutamyl-D-Glutamic Acid
• 英文别名: (2R)-2-[[(4S)-4-carboxy-4-[[4-[[(6S)-2-(hydroxymethyl)-4-oxo-3,6,7,8-tetrahydrocyclopenta[g]quinazolin-6-yl]-prop-2-ynylamino]benzoyl]amino]butanoyl]amino]pentanedioic acid
• CAS: 501332-69-0
• 化学式: C₃₂H₃₃N₅O₁₀
• 分子量: 647.6
• InChiKey: NVHRBQOZEMFKLD-CUYJMHBOSA-N

物化性质

• 熔点：
  174 °C(Solv: methanol (67-56-1); water (7732-18-5))
• 密度：
  1.49±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  47
• 可旋转键数：
  15
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.34
• 拓扑面积：
  235
• 氢给体数：
  7
• 氢受体数：
  11

文献信息

• Synthesis of Cyclopentaquinazolines
  申请人：Kerschen James Alan

  公开号：US20130211082A1

  公开（公告）日：2013-08-15

  A method of producing 6-amino-cyclopenta[g]quinazolines, in enantiomerically enriched form, is provided. In particular, the method may be applicable to the synthesis of N-N-4-[N-((6S)-2-hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclo-penta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino]benzoyl}-L-γ-glutamyl}-D-glutamic acid (ONX-0801).

  提供一种以对映体富集形式生产6-氨基环戊[g]喹唑啉的方法。特别是，该方法可适用于合成N-N-4-[N-((6S)-2-羟甲基-4-氧代-3,4,7,8-四氢-6H-环戊[g]喹唑啉-6-基)-N-(丙-2-炔基)氨基]苯甲酰}-L-γ-谷氨酰}-D-谷氨酸(ONX-0801)的合成。
• Platinum-resistant cancer treatment
  申请人：BTG International Limited

  公开号：US11026948B2

  公开（公告）日：2021-06-08

  A compound of formula I or a pharmaceutically acceptable salt or ester thereof is provided for the treatment of cancer wherein (i) the cancer is one that has the characteristic of being a type prone to being or becoming refractory or resistant to platinum drug based therapy and (ii) the treatment is with a dose of between 1 mg/m2 and 30 mg/m2 of compound per patient body surface area per administration. Method of treatment and novel dosage forms are also provided. Particularly treated arc ovarian cancers, particularly those expressing a-folate receptors, including epithelial ovarian, fallopian tube or peritoneal cancer.

  本发明提供了一种用于治疗癌症的式 I 化合物或其药学上可接受的盐或酯，其中 (i) 癌症是一种对铂类药物治疗具有难治性或耐药性的癌症，(ii) 治疗剂量为每个患者体表面积每次给药 1 mg/m2 至 30 mg/m2 化合物。还提供了治疗方法和新型剂型。特别治疗弧形卵巢癌，尤其是表达叶酸受体的卵巢癌，包括上皮性卵巢癌、输卵管癌或腹膜癌。
• Monocyclic thieno, pyrido, and pyrrolo pyrimidine compounds and methods of use and manufacture of same
  申请人：Duquesne University of the Holy Spirit

  公开号：US11078214B2

  公开（公告）日：2021-08-03

  The present invention provides a compound of Formula XXVII: wherein X is CH2 or O, and R1 is H or CH3; or a salt or a hydrate of the compound, and further provides a pharmaceutical composition comprising the compound of Formula XXVII and one or more acceptable pharmaceutical carriers. A method of treating a patient having cancer comprising administering a therapeutically effective amount of a compound of Formula XXVII, or a pharmaceutical composition comprising a compound of Formula XXVII and one or more acceptable pharmaceutical carriers to the patient is disclosed.

  本发明提供了一种式 XXVII 的化合物： 其中X为CH2或O，R1为H或CH3；或该化合物的盐或水合物，并进一步提供了一种药物组合物，该组合物包含式XXVII化合物和一种或多种可接受的药物载体。本发明公开了一种治疗癌症患者的方法，包括向患者施用治疗有效量的式XXVII化合物或包含式XXVII化合物和一种或多种可接受的药物载体的药物组合物。
• CYCLOPENTA[G]QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF RHEUMATOID ARTHRITIS OR ACUTE MYELOID LEUKAEMIA
  申请人：BTG International Limited

  公开号：EP2293807B1

  公开（公告）日：2012-05-09
• SYNTHESIS OF CYCLOPENTAQUINAZOLINES
  申请人：BTG International Limited

  公开号：EP2595966B1

  公开（公告）日：2020-10-28