4-Hydroxy-2-oxa-8-azaspiro[4.5]decane-8-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂螺癸烷衍生物
• 英文名称: 4-Hydroxy-2-oxa-8-azaspiro[4.5]decane-8-carboxylic acid
• 英文别名: 4-hydroxy-2-oxa-8-azaspiro[4.5]decane-8-carboxylic acid
• 化学式: C₉H₁₅NO₄
• 分子量: 201.22
• InChiKey: GBQLXEFQWSEUER-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  70
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• PYRIMIDINE-FUSED CYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
  申请人：SHANGHAI BLUERAY BIOPHARMA CO., LTD.

  公开号：US20210053989A1

  公开（公告）日：2021-02-25

  Disclosed in the present disclosure are a pyrimidine-fused cyclic compound or a pharmaceutically acceptable salt, hydrate, prodrug, stereoisomer, solvate or isotope labeled compound thereof. Also provided in the present disclosure are a preparation method for the compound, a composition comprising the compound and a use of the compound for the preparation of a medicament for the prevention and/or treatment of a disease or condition associated with abnormal SHP2 activity.

  本公开涉及一种嘧啶融合的环状化合物或其药用可接受的盐、水合物、前药、立体异构体、溶剂合物或同位素标记化合物。本公开还提供了该化合物的制备方法、包含该化合物的组合物以及该化合物用于制备与异常SHP2活性相关的疾病或病况的药物的用途。
• [EN] COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2<br/>[FR] COMPOSÉS ET COMPOSITIONS POUR INHIBER L'ACTIVITÉ DE SHP2
  申请人：NOVARTIS AG

  公开号：WO2016203404A1

  公开（公告）日：2016-12-22

  The present invention relates to compounds of formula I. The compounds are inhibitors of the Src Homolgy-2 phosphatase (SHP2) and thus useful in the treatment of Noonan Syndrome, Leopard Syndrome and cancer.

  本发明涉及式I的化合物。这些化合物是Src同源-2磷酸酶（SHP2）的抑制剂，因此在努南综合征、豹纹综合征和癌症的治疗中有用。
• [EN] N-AZASPIROCYCLOALKANE SUBSTITUTED N-HETEROARYL COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2<br/>[FR] COMPOSÉS N-HÉTÉROARYLE SUBSTITUÉS PAR UN N-AZASPIROCYCLOALCANE ET COMPOSITIONS POUR INHIBER L'ACTIVITÉ DE SHP2
  申请人：NOVARTIS AG

  公开号：WO2015107495A1

  公开（公告）日：2015-07-23

  The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

  本发明涉及式I的化合物：其中p、q、Y1、Y2、R1、R2a、R2b、R3a、R3b、R4a、R4b、R5a、R5b、R7和R8在发明摘要中有定义；能够抑制SHP2活性。本发明还提供了一种制备本发明化合物的方法，包括这种化合物的药物制剂以及在管理与SHP2异常活性相关的疾病或疾病中使用这种化合物和组合物的方法。
• HETEROCYCLIC INHIBITORS OF PTPN11
  申请人：Board of Regents, The University of Texas System

  公开号：US20170342078A1

  公开（公告）日：2017-11-30

  The present invention relates to compounds which may be useful as inhibitors of PTPN11 for the treatment or prevention of cancer and other PTP-mediated diseases. Disclosed herein are new compounds and compounds based on pyrazolopyrazines and their application as pharmaceuticals for the treatment of disease.

  本发明涉及化合物，可用作PTPN11的抑制剂，用于治疗或预防癌症和其他PTP介导的疾病。本文披露了基于吡唑并吡嗪的新化合物和化合物，并将其应用于治疗疾病的制药。
• PYRIMIDINE-4(3H)-KETONE HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF IN MEDICINE AND PHARMACOLOGY
  申请人：Beijing InnoCare Pharma Tech Co., Ltd.

  公开号：EP4092024A1

  公开（公告）日：2022-11-23

  The present invention relates to pyrimidin-4(3H)-one heterocyclic compounds for inhibiting or regulating SHP2, preparation methods thereof, and pharmaceutical use thereof. Specifically, the present invention relates to compounds represented by general formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof, a method of applying the compounds or pharmaceutically acceptable salts thereof for treating and/or preventing SHP2-mediated diseases, particularly cancers, and preparation methods for the compounds or pharmaceutically acceptable salts thereof. The present invention further relates to use of the compounds or pharmaceutically acceptable salts thereof, or the pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof in the preparation of medicaments for treating and/or preventing SHP2-mediated diseases. Herein, all substituents in the general formula (I) are as defined in the description.

  本发明涉及用于抑制或调节SHP2的嘧啶-4(3H)-酮杂环化合物、其制备方法及其药物用途。具体地说，本发明涉及通式(I)代表的化合物及其药学上可接受的盐、含有该化合物或其药学上可接受的盐的药物组合物、应用该化合物或其药学上可接受的盐治疗和/或预防SHP2介导的疾病，特别是癌症的方法，以及该化合物或其药学上可接受的盐的制备方法。本发明进一步涉及本发明化合物或其药学上可接受的盐或含有本发明化合物或其药学上可接受的盐的药物组合物在制备治疗和/或预防SHP2介导的疾病的药物中的用途。在此，通式（I）中的所有取代基均如描述中所定义。