1-[1-(tert-butoxycarbonyl)piperidin-4-yl]pyrazole-3-carboxylic acid | 2059970-37-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-[1-(tert-butoxycarbonyl)piperidin-4-yl]pyrazole-3-carboxylic acid
• 英文别名: 1-(1-(Tert-butoxycarbonyl)piperidin-4-YL)-1H-pyrazole-3-carboxylic acid；1-[1-[(2-methylpropan-2-yl)oxycarbonyl]piperidin-4-yl]pyrazole-3-carboxylic acid
• CAS: 2059970-37-3
• 化学式: C₁₄H₂₁N₃O₄
• 分子量: 295.338
• InChiKey: SMNGVKZBJGNAFI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.64
• 拓扑面积：
  84.7
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  1-[1-(tert-butoxycarbonyl)piperidin-4-yl]pyrazole-3-carboxylic acid 、 (Z)-N,N'-diisopropyltert-butoxymethanimidamide 以 二氯甲烷 为溶剂， 以305 mg的产率得到tert-butyl 4-[3-(tert-butoxycarbonyl)pyrazol-1-yl]piperidine-1-carboxylate
  参考文献：
  名称：

  [EN] BIFUNCTIONAL DEGRADERS OF HEMATOPOIETIC PROGENITOR KINASE AND THERAPEUTIC USES THEREOF
  [FR] AGENTS DE DÉGRADATION BIFONCTIONNELS DE LA KINASE PROGÉNITRICE HÉMATOPOÏÉTIQUE ET LEURS UTILISATIONS THÉRAPEUTIQUES

  摘要：

  本公开提供了通过泛素蛋白酶体途径作为HPK1降解剂的双功能化合物，以及治疗受HPK1调节的疾病的方法。

  公开号：

  WO2021226262A1
• 作为产物：
  描述：

  4-溴-N-Boc-哌啶 在 水 、 sodium hydride 、 lithium hydroxide 作用下， 以 四氢呋喃 、 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 生成 1-[1-(tert-butoxycarbonyl)piperidin-4-yl]pyrazole-3-carboxylic acid
  参考文献：
  名称：

  [EN] BIFUNCTIONAL DEGRADERS OF HEMATOPOIETIC PROGENITOR KINASE AND THERAPEUTIC USES THEREOF
  [FR] AGENTS DE DÉGRADATION BIFONCTIONNELS DE LA KINASE PROGÉNITRICE HÉMATOPOÏÉTIQUE ET LEURS UTILISATIONS THÉRAPEUTIQUES

  摘要：

  本公开提供了通过泛素蛋白酶体途径作为HPK1降解剂的双功能化合物，以及治疗受HPK1调节的疾病的方法。

  公开号：

  WO2021226262A1

文献信息

• COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
  申请人：Arvinas, Inc.

  公开号：US20180099940A1

  公开（公告）日：2018-04-12

  The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

  本公开涉及双功能化合物，其用于降解和（抑制）雄激素受体。具体而言，本公开涉及包含一端结合到E3泛素连接酶的谷氨酰腺苷环配体，另一端结合到雄激素受体的部分的化合物，使得雄激素受体与泛素连接酶靠近，以实现雄激素受体的降解（和抑制）。本公开展示了与根据本公开涉及的化合物相关的广泛的药理活性范围，与雄激素受体的降解/抑制一致。
• Compounds and methods for the targeted degradation of androgen receptor
  申请人：Arvinas Operations, Inc.

  公开号：US10844021B2

  公开（公告）日：2020-11-24

  The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

  本公开涉及双功能化合物，它们可用于降解和（抑制）雄激素受体。特别是，本公开涉及的化合物一端含有与 E3 泛素连接酶结合的脑龙配体，另一端含有与雄激素受体结合的分子，这样雄激素受体就被置于泛素连接酶附近，从而实现对雄激素受体的降解（和抑制）。本公开的化合物具有广泛的药理活性，与雄激素受体的降解/抑制作用相一致。
• [EN] COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR<br/>[FR] COMPOSÉS ET PROCÉDÉS POUR LA DÉGRADATION CIBLÉE DU RÉCEPTEUR DES ANDROGÈNES
  申请人：ARVINAS INC

  公开号：WO2018071606A1

  公开（公告）日：2018-04-19

  The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.