1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-2-pyrrolidin-2-yl-2-[4-(trifluoromethyl)phenyl]ethanone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-2-pyrrolidin-2-yl-2-[4-(trifluoromethyl)phenyl]ethanone
• 化学式: C₂₅H₃₀F₃N₅O₂
• 分子量: 489.5
• InChiKey: FEMSWPPUYTTWKZ-JIFINUTQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  35
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  81.6
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS
  申请人：Genentech, Inc.

  公开号：US20140080829A1

  公开（公告）日：2014-03-20

  The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

  本发明提供了I式化合物，包括互变异构体、已分离的对映体、非同构体、溶剂化物、代谢物、盐及其药学上可接受的前药。同时，还提供了使用本发明化合物作为AKT蛋白激酶抑制剂以及用于治疗高增殖性疾病，如癌症的方法。
• COMBINATIONS OF AKT INHIBITOR COMPOUNDS AND CHEMOTHERAEPTUC AGENTS, AND METHODS OF USE
  申请人：Lin Kui

  公开号：US20150064171A1

  公开（公告）日：2015-03-05

  The invention provides combinations comprising a) compound of formula (I) or a pharmaceutically acceptable salt thereof wherein R 1 , R 2 , R 5 , R 10 , and A have any of the values defined in the specification; and b) one or more agents selected from 5-FU, a platinum agent, leucovorin, irinotecan, docetaxel, doxorubicin, gemcitabine, SN-38, capecitabine, temozolomide, paclitaxel, bevacizumab, pertuzumab, tamoxifen, rapamycin and lapatinib. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.

  本发明提供组合物，其中包括a)式（I）化合物或其药学上可接受的盐，其中R1、R2、R5、R10和A的值在规范中定义；和b)选择自5-FU、铂类药物、亚叶酸、伊立替康、多西他赛、多柔西汀、吉西他滨、SN-38、卡培他滨、替莫唑胺、紫杉醇、贝伐珠单抗、珀妥珠单抗、他莫昔芬、雷帕霉素和拉帕替尼的一种或多种药剂。这些组合物特别适用于治疗高增殖性疾病，如癌症。
• COMBINATIONS OF AKT INHIBITOR COMPOUNDS AND ERLOTINIB, AND METHODS OF USE
  申请人：Nannini Michelle

  公开号：US20140221386A1

  公开（公告）日：2014-08-07

  The invention provides A combination of a) a compound of Formula (I) or a pharmaceutically acceptable salt thereof; and b) erlotinib or a pharmaceutically acceptable salt thereof for the prophylactic or therapeutic treatment of a hyperproliferative disorder, such as cancer.

  本发明提供了以下组合物：a) 公式 (I) 化合物或其药学上可接受的盐；和 b) erlotinib 或其药学上可接受的盐，用于预防或治疗高增殖性疾病，如癌症。
• COMBINATIONS OF AKT INHIBITOR COMPOUNDS AND CHEMOTHERAPEUTIC AGENTS, AND METHODS OF USE
  申请人：Genentech, Inc.

  公开号：US20160228440A1

  公开（公告）日：2016-08-11

  The invention provides combinations comprising a) compound of formula I: or a pharmaceutically acceptable salt thereof wherein R 1 , R 2 , R 5 , R 10 , and A have any of the values defined in the specification; and b) one or more agents selected from 5-FU, a platinum agent, leucovorin, irinotecan, docetaxel, doxorubicin, gemcitabine, SN-38, capecitabine, temozolomide, paclitaxel, bevacizumab, pertuzumab, tamoxifen, rapamycin and lapatinib. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.

  本发明提供了以下组合物：a) 公式I的化合物：或其药学上可接受的盐，其中R1、R2、R5、R10和A具有规范中定义的任何值；和b) 从5-FU、铂类药物、亚叶酸、伊立替康、多西他赛、阿霉素、吉西他滨、SN-38、卡培他滨、替莫唑胺、紫杉醇、贝伐珠单抗、珀妥珠单抗、他莫昔芬、雷帕霉素和拉帕替尼中选择的一个或多个药物。这些组合物特别适用于治疗增生性疾病，如癌症。
• Combinations of AKT inhibitor compounds and chemotherapeutic agents, and methods of use
  申请人：Genentech, Inc.

  公开号：US10092567B2

  公开（公告）日：2018-10-09

  The invention provides combinations comprising a) compound of formula I: or a pharmaceutically acceptable salt thereof wherein R1, R2, R5, R10, and A have any of the values defined in the specification; and b) one or more agents selected from 5-FU, a platinum agent, leucovorin, irinotecan, docetaxel, doxorubicin, gemcitabine, SN-38, capecitabine, temozolomide, paclitaxel, bevacizumab, pertuzumab, tamoxifen, rapamycin and lapatinib. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.

  本发明提供的组合物包含 a) 式 I 的化合物： 或其药学上可接受的盐，其中 R1、R2、R5、R10 和 A 具有说明书中定义的任一值；以及 b) 一种或多种选自 5-FU、铂类制剂、亮菌甲素、伊立替康、多西他赛、多柔比星、吉西他滨、SN-38、卡培他滨、替莫唑胺、紫杉醇、贝伐珠单抗、培妥珠单抗、他莫昔芬、雷帕霉素和拉帕替尼的制剂。这些复方制剂尤其适用于治疗过度增殖性疾病，如癌症。