N-((2-chloro-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)-2-methoxyethanamine | 1032758-61-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并嘧啶酮衍生物
• 英文名称: N-((2-chloro-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)-2-methoxyethanamine
• 英文别名: (2-Chloro-4-morpholin-4-yl-thieno[3,2-d]pyrimidin-6-ylmethyl)-(2-methoxy-ethyl)-amine；N-[(2-chloro-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl)methyl]-2-methoxyethanamine
• CAS: 1032758-61-4
• 化学式: C₁₄H₁₉ClN₄O₂S
• 分子量: 342.849
• InChiKey: ZDQZRIXKDPITGG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  22
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  87.8
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2-氯-4-(4-吗啉)-噻吩并[3,2-d]嘧啶-6-羧醛 、 2-甲氧基乙胺 以yielded (2-chloro-4-morpholin-4-yl-thieno[3,2-d]pyrimidin-6-ylmethyl)-(2-methoxy-ethyl)-amine, which的产率得到N-((2-chloro-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)-2-methoxyethanamine
  参考文献：
  名称：

  Phosphoinositide 3-kinase inhibitor compounds and methods of use

  摘要：

  公式Ia-d的化合物，其中X为S或O，mor为吗啡啶基团，而R3为单环杂芳基团，包括立体异构体，几何异构体，互变异构体，溶剂化物，代谢物和药学上可接受的盐，对于调节脂质激酶（包括PI3K）的活性以及治疗由脂质激酶介导的癌症等疾病非常有用。本文公开了使用公式Ia-d的化合物进行哺乳动物细胞中的体外，体内和原位诊断，预防或治疗此类疾病或相关病理条件的方法。

  公开号：

  US08383620B2

文献信息

• TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
  申请人：Curis, Inc.

  公开号：US20130102595A1

  公开（公告）日：2013-04-25

  The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.

  本发明提供了一种治疗与K-ras突变相关的癌症的方法，适用于需要该方法的受试者。该方法包括以下步骤：（1）识别患有与K-ras突变相关的癌症的受试者；和（2）向受试者施用（i）PI3激酶抑制剂和（ii）HDAC抑制剂，其中PI3激酶抑制剂和HDAC抑制剂以联合治疗有效的剂量进行施用。
• [EN] TREATMENT OF CANCERS HAVING K-RAS MUTATIONS<br/>[FR] TRAITEMENT DE CANCERS PRÉSENTANT DES MUTATIONS K-RAS
  申请人：CURIS INC

  公开号：WO2011130628A1

  公开（公告）日：2011-10-20

  The present invention provides a method of treating a cancer associated with a K- ras mutation in a subject in need thereof. The method comprises the steps of (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) adminsiterign to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.

  本发明提供了一种治疗与K-ras突变相关的癌症的方法，适用于需要该方法的受试者。该方法包括以下步骤：(1) 鉴定患有与K-ras突变相关的癌症的受试者；和 (2) 给予该受试者 (i) PI3激酶抑制剂和 (ii) HDAC抑制剂，其中PI3激酶抑制剂和HDAC抑制剂以治疗有效的剂量一起给予。
• PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE
  申请人：Bayliss Tracy

  公开号：US20080242665A1

  公开（公告）日：2008-10-02

  Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R 3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

  化学式Ia-d的化合物，其中X为S或O，mor为吗啡啶基团，R3为单环杂芳基团，包括立体异构体、几何异构体、互变异构体、溶剂化物、代谢物和药学上可接受的盐，可用于调节脂质激酶包括PI3K的活性，并用于治疗由脂质激酶介导的癌症等疾病。本文公开了使用化合物Ia-d的方法，用于哺乳动物细胞中体外、体内诊断、预防或治疗这种疾病或相关病理条件。
• PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH A ZINC BINDING MOIETY
  申请人：Cai Xiong

  公开号：US20100222343A1

  公开（公告）日：2010-09-02

  The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

  本实用新型涉及具有基于锌结合基团的脱氮嘌呤、噻吩嘧啶和呋喃嘧啶衍生物及其在治疗与磷脂酰肌醇3-激酶相关的疾病和疾病方面的应用，例如癌症。本实用新型进一步涉及与组蛋白去乙酰化酶相关的疾病和同时涉及组蛋白去乙酰化酶和磷脂酰肌醇3-激酶相关的疾病的治疗。
• Phosphoinositide 3-kinase inhibitors with a zinc binding moiety
  申请人：Curis, Inc.

  公开号：US10336770B2

  公开（公告）日：2019-07-02

  The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

  本申请涉及去氮嘌呤类、噻吩嘧啶类和呋喃嘧啶类与锌结合基的衍生物，以及它们在治疗磷酸肌酸 3- 激酶相关疾病和紊乱（如癌症）中的用途。本申请还涉及组蛋白去乙酰化酶相关疾病以及组蛋白去乙酰化酶和磷酸肌酸 3-激酶相关疾病的治疗。