2-N-tert-butyl-6-cyclopropyl-7-[4-(methanesulfonamido)phenyl]-3,4,8,8a-tetrahydro-1H-pyrrolo[1,2-a]pyrazine-2,8-dicarboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯啉
• 英文名称: 2-N-tert-butyl-6-cyclopropyl-7-[4-(methanesulfonamido)phenyl]-3,4,8,8a-tetrahydro-1H-pyrrolo[1,2-a]pyrazine-2,8-dicarboxamide
• 化学式: C₂₃H₃₃N₅O₄S
• 分子量: 475.6
• InChiKey: PAROCIKTQSNZEP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  133
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• 3,4-DIHYDROPYRROLO[1,2-A]PYRAZINE-2,8(1H)-DICARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
  申请人：SANOFI

  公开号：US20140336189A1

  公开（公告）日：2014-11-13

  Compounds corresponding to the general formula (I) wherein R 2 represents a group C 1-10 -alkyl, C 3-10 -cycloalkyl, C 3-7 -cycloalkyl-C 1-6 -alkyl, C 1-6 -alkyl-C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 3-7 -cycloalkyl, C 1-6 -alkylthio-C- 1-10 -alkyl, C 1-6 -alkoxy-C 1-10 -alkyl, hydroxy-C 1-10 -alkyl, hydroxy-C 1-6 -alkyl-C 3-7 -cycloalkyl-C 1-6 -alkyl, hydroxy-C 3-10 -cycloalkyl, C 1-10 -fluoroalkyl or C 3-10 -fluorocycloalkyl; an optionally substituted heterocyclic group; a group C 1-10 -alkyl substituted with an optionally substituted heterocyclic group; X 6 represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C 1-6 -alkyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-6 -alkyl, C 1-6 -fluoroalkyl or cyano; and R 7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt, and the therapeutic use thereof.

  化合物的通式（I）对应于其中R2表示C1-10-烷基，C3-10-环烷基，C3-7-环烷基-C1-6-烷基，C1-6-烷基-C3-7-环烷基，C3-7-环烷基-C3-7-环烷基，C1-6-烷基硫基-C-1-10-烷基，C1-6-烷氧基-C1-10-烷基，羟基-C1-10-烷基，羟基-C1-6-烷基-C3-7-环烷基-C1-6-烷基，羟基-C3-10-环烷基，C1-10-氟代烷基或C3-10-氟代环烷基; 可选取代的杂环基; 被可选取代的杂环基取代的C1-10-烷基; X6表示氢，氟，氯和溴原子或C1-6-烷基，C3-7-环烷基，C3-7-环烷基-C1-6-烷基，C1-6-氟代烷基或氰基的基团; R7表示芳基，例如苯基或萘基，可选取代一个或多个取代基，以盐酸盐或酸加成盐的形式，以及它们的治疗用途。
• CHEMICAL INHIBITORS AGAINST KINASES TO BLOCK TELOMERE ELONGATION IN CANCER
  申请人：THE JOHNS HOPKINS UNIVERSITY

  公开号：US20200078387A1

  公开（公告）日：2020-03-12

  The present invention relates generally to chromosome maintenance and cell viability, and more specifically, to the identification of kinases the inhibition of which blocks telomere elongation. In one aspect, the present invention provides methods for treating cancer. The methods generally comprise the administration of agents that interfere with the lengthening of telomeres in cancer. In a specific embodiment, a method of treating cancer in a subject by interfering with lengthening of telomeres in cancer cells comprises administering to the cells an effective amount of an inhibitor of casein kinase 1 (CK1), wherein the administration of the inhibitor leads to progressive telomere shortening in the cancer cell, thereby treating cancer in the subject. In another embodiment, the method can further comprise administering to the cells an effective amount of an inhibitor of bromodomain-containing protein 4 (BRD4) and/or an inhibitor of the MEK/ERK pathway.
• US8791119B2
  申请人：——

  公开号：US8791119B2

  公开（公告）日：2014-07-29
• US9233965B2
  申请人：——

  公开号：US9233965B2

  公开（公告）日：2016-01-12