ethyl 2,3-dihydrospiro[indene-1,4'-piperidin]-3-ylcarbamate | 1000975-02-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: ethyl 2,3-dihydrospiro[indene-1,4'-piperidin]-3-ylcarbamate
• 英文别名: Ethyl (2,3-dihydrospiro[indene-1,4'-piperidin]-3-yl)carbamate；ethyl N-spiro[1,2-dihydroindene-3,4'-piperidine]-1-ylcarbamate
• CAS: 1000975-02-9
• 化学式: C₁₆H₂₂N₂O₂
• 分子量: 274.363
• InChiKey: QNKSXTJRBFMXGS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  50.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  t-butyl {3-[(6-chloropyridine-3-carbonyl)amino][1,1'-biphenyl]-4-yl}carbamate 、 ethyl 2,3-dihydrospiro[indene-1,4'-piperidin]-3-ylcarbamate 在 二乙基异丙基胺 作用下， 以 二甲基亚砜 为溶剂， 反应 8.0h， 生成 ethyl (1'-{5-[({4-[(t-butoxycarbonyl)amino]biphenyl-3-yl}amino)carbonyl]pyridin-2-yl}-2,3-dihydro-1'H-spiro[indene-1,4'-piperidin]-3-yl)carbamate
  参考文献：
  名称：

  WO2007/136605

  摘要：

  公开号：

文献信息

• Aryl-Fused Spirocyclic Compounds
  申请人：Hamblett Christopher

  公开号：US20090239849A1

  公开（公告）日：2009-09-24

  The present invention relates to a novel class of aryl-fused spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.

  本发明涉及一种新型的芳基螺环化合物类，这些化合物可以抑制组蛋白去乙酰化酶，并适用于选择性诱导终末分化，阻止肿瘤细胞的生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物适用于治疗具有肿瘤细胞增殖特征的患者。本发明的化合物也可能适用于预防和治疗TRX介导的疾病，如自身免疫、过敏和炎症性疾病，并在预防和/或治疗中枢神经系统（CNS）疾病，如神经退行性疾病方面有用。本发明还提供了包含本发明化合物的药物组合物和这些药物组合物的安全剂量方案，这些方案易于遵循，并在体内产生治疗有效量的这些化合物。
• ARYL-FUSED SPIROCYCLIC COMPOUNDS
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2023924B1

  公开（公告）日：2016-08-03
• US8119652B2
  申请人：——

  公开号：US8119652B2

  公开（公告）日：2012-02-21
• [EN] ARYL-FUSED SPIROCYCLIC COMPOUNDS<br/>[FR] COMPOSÉS SPIROCYCLIQUES FUSIONNÉS À ARYLE
  申请人：MERCK & CO INC

  公开号：WO2007136605A2

  公开（公告）日：2007-11-29

  [EN] The present invention relates to a novel class of aryl-fused spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.
  [FR] La présente invention concerne une nouvelle catégorie de composés spirocycliques fusionnés à aryle. Ces composés peuvent inhiber l'histone désacétylase et leur utilisation est appropriée pour induire de manière sélective la différenciation terminale, stopper la croissance cellulaire et/ou induire l'apoptose des cellules néoplasiques, pour ainsi inhiber la prolifération de ces cellules. Ainsi, les composés de l'invention sont utiles pour traiter un patient présentant une tumeur qui se caractérise par la prolifération de cellules néoplasiques. Les composés de l'invention peuvent également être utiles pour prévenir et traiter des troubles dans lesquels la thiorédoxine (TRX) joue un rôle, tels que des troubles auto-immuns, allergiques et inflammatoires, et pour prévenir et/ou traiter des troubles du système nerveux central (SNC) tels que des troubles de neurodégénérescence. L'invention a également pour objet des compositions pharmaceutiques comprenant les composés de l'invention ainsi que des schémas posologiques inoffensifs de ces compositions pharmaceutiques qui sont faciles à suivre et qui conduisent à une administration thérapeutiquement efficace de ces composés in vivo.
• WO2007/136605
  申请人：——

  公开号：——

  公开（公告）日：——