Golvatinib tartrate | 1007601-96-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: Golvatinib tartrate
• 英文别名: (2R,3R)-2,3-dihydroxybutanedioic acid;1-N'-[2-fluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
• CAS: 1007601-96-8
• 化学式: C37H43F2N7O10
• 分子量: 783.8
• InChiKey: JYFKDBFPRXMUAM-LREBCSMRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.63
• 重原子数：
  56
• 可旋转键数：
  11
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  234
• 氢给体数：
  7
• 氢受体数：
  15

反应信息

• 作为产物：
  描述：

  N-[2-氟-4-[[2-[[[4-(4-甲基哌嗪-1-基)哌啶-1-基]羰基]氨基]吡啶-4-基]氧基]苯基]-N'-(4-氟苯基)环丙烷-1,1-二甲酰胺 、 、 L-酒石酸 、 水 在 乙醇 作用下， 以 乙醇 为溶剂， 反应 17.75h， 以to provide the titled compound as colorless crystals (66.7 mg, 85.1%)的产率得到Golvatinib tartrate
  参考文献：
  名称：

  Pyridine derivatives and pyrimidine derivatives (3)

  摘要：

  以下化合物的公式，其盐或其水合物具有出色的肝细胞生长因子受体（HGFR）抑制活性，并表现出抗肿瘤活性、抑制血管生成活性和癌症转移抑制活性。[R1代表3-至10-成员非芳香杂环基团或类似物；R2和R3代表氢；R4、R5、R6和R7可以相同也可以不同，每个代表氢、卤素、C1-6烷基或类似物；R8代表氢或类似物；R9代表3-至10-成员非芳香杂环基团或类似物；n表示1或2；X表示-CH═、氮或类似物。]

  公开号：

  US07855290B2

文献信息

• Novel pyridine derivatives and pyrimidine derivatives (3)
  申请人：Matsushima Tomohiro

  公开号：US20080319188A1

  公开（公告）日：2008-12-25

  A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R 1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R 2 and R 3 represent hydrogen; R 4 , R 5 , R 6 , and R 7 may be the same or different and each represents hydrogen, halogen, C 1-6 alkyl or the like; R 8 represents hydrogen or the like; R 9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH═, nitrogen or the like.]

  以下化合物，其盐或水合物，具有优异的肝细胞生长因子受体（HGFR）抑制活性，表现出抗肿瘤活性、抑制血管生成活性和癌症转移抑制活性。[其中，R1代表3-至10-成员的非芳香族杂环基团等；R2和R3代表氢；R4、R5、R6和R7可以相同或不同，每个代表氢、卤素、C1-6烷基或类似物；R8代表氢或类似物；R9代表3-至10-成员的非芳香族杂环基团等；n代表1或2的整数；X代表-CH═，氮或类似物。]
• NOVEL PYRIDINE DERIVATIVES AND PYRIMIDINE DERIVATIVES (3)
  申请人：MATSUSHIMA Tomohiro

  公开号：US20100075944A1

  公开（公告）日：2010-03-25

  A compound represented by the following formula, or a salt thereof or a hydrate of the foregoing, has excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity, and cancer metastasis inhibitory activity. R 1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R 2 and R 3 represent hydrogen; R 4 , R 5 , R 6 , and R 7 may be the same or different and each represents hydrogen, halogen, C 1-6 alkyl or the like; R 8 represents hydrogen or the like; R 9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH═, nitrogen or the like.

  以下化合物的分子式，或其盐或水合物，具有出色的肝细胞生长因子受体（HGFR）抑制活性，并表现出抗肿瘤活性、抑制血管生成活性和癌症转移抑制活性。其中，R1代表3-10个成员的非芳香杂环基团等；R2和R3代表氢；R4、R5、R6和R7可以相同也可以不同，每个代表氢、卤素、C1-6烷基或类似物；R8代表氢或类似物；R9代表3-10个成员的非芳香杂环基团等；n代表1或2的整数；X代表-CH═、氮或类似物。
• Synergistic drug combination for the treatment of cancer
  申请人：Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

  公开号：EP2425830A1

  公开（公告）日：2012-03-07

  The present invention relates to synergistic drug combinations and the use of said drug combinations for the treatment of proliferative diseases.

  本发明涉及增效药物组合以及使用所述药物组合治疗增殖性疾病。
• METHOD FOR THE PROGNOSIS AND TREATMENT OF CANCER METASTASIS
  申请人：Fundació Institut de Recerca Biomèdica (IRB Barcelona)

  公开号：EP3825692A1

  公开（公告）日：2021-05-26

  The present invention relates to a method for the prognosis of bone metastasis in triple negative (including basal-like) breast cancer or, alternatively, ER+ breast cancer (including luminal A and B) which comprises determining if the c-MAF gene is amplified in a primary tumor sample. Likewise, the invention also relates to a method for determining the tendency to develop bone metastasis with respect to metastasis in other organs, which comprise determining the c-MAF gene expression level, amplification or translocation. The invention also relates to a method for predicting early bone metastasis in a subject suffering breast cancer. The invention also relates to a c-MAF inhibitor as therapeutic agent for use in the treatment of triple negative (including basal-like) breast cancer metastasis or, alternatively, ER+ breast cancer (including luminal A and B) metastasis. The invention relates to kits for predicting bone metastasis and predicting the clinical outcome of a subject suffering from bone metastasis. Finally, the invention relates to a method for typing of a subject suffering breast cancer and for classifying a subject from breast cancer into a cohort.

  本发明涉及一种三阴性（包括基底样）乳腺癌或ER+乳腺癌（包括管腔A型和B型）骨转移的预后判断方法，该方法包括确定原发肿瘤样本中c-MAF基因是否扩增。同样，本发明还涉及一种确定骨转移倾向与其他器官转移倾向的方法，其中包括确定 c-MAF 基因的表达水平、扩增或易位。本发明还涉及一种预测乳腺癌患者早期骨转移的方法。本发明还涉及一种用于治疗三阴性（包括基底样）乳腺癌转移或ER+乳腺癌（包括管腔A和B）转移的c-MAF抑制剂。本发明涉及用于预测骨转移和预测骨转移患者临床结果的试剂盒。最后，本发明涉及一种对乳腺癌患者进行分型和将乳腺癌患者归入队列的方法。
• Method for the diagnosis, prognosis and treatment of lung cancer metastasis
  申请人：Fundació Institut de Recerca Biomèdica (IRB Barcelona)

  公开号：US10006091B2

  公开（公告）日：2018-06-26

  The present invention relates to a method for the diagnosis or the prognosis of metastasis in lung cancer which comprises determining if the c-MAF gene is amplified in a primary tumor sample. Likewise, the invention also relates to a method for the diagnosis or the prognosis of metastasis in lung cancer, as well as to a method for determining the tendency to develop bone metastasis with respect to metastasis in other organs, which comprise determining the c-MAF gene expression level. Finally, the invention relates to the use of a c-MAF inhibitor as therapeutic target for treating the lung cancer.

  本发明涉及肺癌转移的诊断或预后方法，该方法包括确定原发肿瘤样本中 c-MAF 基因是否扩增。同样，本发明还涉及一种诊断或预后肺癌转移的方法，以及一种确定相对于其他器官转移的骨转移倾向的方法，该方法包括确定 c-MAF 基因的表达水平。最后，本发明涉及使用 c-MAF 抑制剂作为治疗肺癌的靶点。