1'-BOC-5-氯-1,2-二氢-2-氧代-螺[3H-吲哚-3,4'-哌啶] | 346701-12-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 中文名称: 1'-BOC-5-氯-1,2-二氢-2-氧代-螺[3H-吲哚-3,4'-哌啶]
• 英文名称: tert-butyl 5-chloro-2-oxospiro[indoline-3,4'-piperidine]-1'-carboxylate
• 英文别名: tert-butyl 5-chloro-2-oxo-1,2-dihydrospiro[indole-3,4'-piperidine]-1'-carboxylate；1'-Boc-5-chloro-1,2-dihydro-2-oxo-spiro[3H-indole-3,4'-piperidine]；tert-butyl 5-chloro-2-oxospiro[1H-indole-3,4'-piperidine]-1'-carboxylate
• CAS: 346701-12-0
• 化学式: C₁₇H₂₁ClN₂O₃
• 分子量: 336.818
• InChiKey: RNXZBWKYWNTRSG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  58.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1'-BOC-5-氯-1,2-二氢-2-氧代-螺[3H-吲哚-3,4'-哌啶] 在 盐酸 、 sodium hydride 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 甲醇 、 mineral oil 为溶剂， 反应 1.0h， 生成 5-chloro-1-methyl-spiro[indoline-3,4'-piperidine]-2-one hydrochloride
  参考文献：
  名称：

  [EN] SPIRO PIPERIDINE DERIVATIVES AS INHIBITORS OF APOL1 AND METHODS OF USING SAME
  [FR] DÉRIVÉS DE SPIRO PIPÉRIDINE UTILISÉS EN TANT QU'INHIBITEURS DE APOL1 ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  The disclosure provides at least one compound, tautomer, deuterated derivative, or pharmaceutically acceptable salt chosen from compounds of Formula I, tautomers thereof, deuterated derivatives of those compounds or tautomers, and pharmaceutically acceptable salts of any of the foregoing, compositions comprising the same, and methods of using the same, including uses in treating APOL1-mediated diseases, including pancreatic cancer, focal segmental glomerulosclerosis (FSGS), and/or non-diabetic kidney disease (NDKD).

  公开号：

  WO2023154314A1
• 作为产物：
  描述：

  1’-BOC-1,2-二氢-2-氧代-螺[3H-吲哚-3,4’-哌啶] 在 N-氯代丁二酰亚胺 作用下， 以 氯仿 为溶剂， 以9 %的产率得到1'-BOC-5-氯-1,2-二氢-2-氧代-螺[3H-吲哚-3,4'-哌啶]
  参考文献：
  名称：

  [EN] SPIRO PIPERIDINE DERIVATIVES AS INHIBITORS OF APOL1 AND METHODS OF USING SAME
  [FR] DÉRIVÉS DE SPIRO PIPÉRIDINE UTILISÉS EN TANT QU'INHIBITEURS DE APOL1 ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  The disclosure provides at least one compound, tautomer, deuterated derivative, or pharmaceutically acceptable salt chosen from compounds of Formula I, tautomers thereof, deuterated derivatives of those compounds or tautomers, and pharmaceutically acceptable salts of any of the foregoing, compositions comprising the same, and methods of using the same, including uses in treating APOL1-mediated diseases, including pancreatic cancer, focal segmental glomerulosclerosis (FSGS), and/or non-diabetic kidney disease (NDKD).

  公开号：

  WO2023154314A1

文献信息

• [EN] SPIROHETEROCYCLIC DERIVATIVES AS CRHR2 ANTAGONIST<br/>[FR] DÉRIVÉS SPIROHÉTÉROCYCLIQUES UTILISÉS COMME ANTAGONISTES DE CRHR2
  申请人：RAQUALIA PHARMA INC

  公开号：WO2021145401A1

  公开（公告）日：2021-07-22

  The present invention relates to spiroheterocyclic derivatives which have antagonistic activities against CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR2 is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CRHR2 is involved.

  本发明涉及对CRHR2具有拮抗活性的螺环杂环衍生物，用于治疗或预防涉及CRHR2的疾病和疾病。该发明还涉及包含这些化合物的药物组合物以及在预防或治疗涉及CRHR2的疾病中使用这些化合物和组合物。
• [EN] APOL1 INHIBITORS AND METHODS OF USE<br/>[FR] INHIBITEURS D'APOL1 ET MÉTHODES D'UTILISATION
  申请人：[en]MAZE THERAPEUTICS, INC.

  公开号：WO2023141432A2

  公开（公告）日：2023-07-27

  Provided herein are compounds of formula (II): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, whereinm, n, p, R1, R2, R3, L1, L2, L3, R4, X1, X2, X3, and X4are as defined herein. Also provided are methods of preparing compounds of formula (II), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided are methods of inhibiting APOL1 and methods of treating an APOL1 -mediated disease, disorder, or condition in an individual.
• [EN] SPIRO PIPERIDINE DERIVATIVES AS INHIBITORS OF APOL1 AND METHODS OF USING SAME<br/>[FR] DÉRIVÉS DE SPIRO PIPÉRIDINE UTILISÉS EN TANT QU'INHIBITEURS DE APOL1 ET LEURS PROCÉDÉS D'UTILISATION
  申请人：[en]VERTEX PHARMACEUTICALS INCORPORATED

  公开号：WO2023154314A1

  公开（公告）日：2023-08-17

  The disclosure provides at least one compound, tautomer, deuterated derivative, or pharmaceutically acceptable salt chosen from compounds of Formula I, tautomers thereof, deuterated derivatives of those compounds or tautomers, and pharmaceutically acceptable salts of any of the foregoing, compositions comprising the same, and methods of using the same, including uses in treating APOL1-mediated diseases, including pancreatic cancer, focal segmental glomerulosclerosis (FSGS), and/or non-diabetic kidney disease (NDKD).