(3-((3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-6-(2,3-dichlorophenyl)-5-methylpyrazin-2-yl)methanol | 2172651-73-7

• 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: (3-((3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-6-(2,3-dichlorophenyl)-5-methylpyrazin-2-yl)methanol
• 英文别名: [3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-6-(2,3-dichlorophenyl)-5-methylpyrazin-2-yl]methanol
• CAS: 2172651-73-7
• 化学式: C₂₁H₂₆Cl₂N₄O₂
• 分子量: 437.4
• InChiKey: IKUYEYLZXGGCRD-ORAYPTAESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  29
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  84.5
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• [EN] PYRIMIDINONE DERIVATIVES AS SHP2 ANTAGONISTS<br/>[FR] DÉRIVÉS DE PYRIMIDINONE UTILISÉS EN TANT QU'ANTAGONISTES DE SHP2
  申请人：MERCK PATENT GMBH

  公开号：WO2020210384A1

  公开（公告）日：2020-10-15

  The invention relates to pyrimidinone derivatives of the general Formula (II), or a pharmaceutically acceptable salt thereof, the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

  这项发明涉及一般式（II）的嘧啶酮衍生物，或其药学上可接受的盐，以及本发明化合物用于治疗哺乳动物，特别是人类的增殖过度性疾病和紊乱的用途，以及含有这种化合物的药物组合物。
• COMPOUNDS FOR THE TREATMENT OF BRAF-ASSOCIATED DISEASES AND DISORDERS
  申请人：Array BioPharma Inc.

  公开号：US20200407344A1

  公开（公告）日：2020-12-31

  Provided herein are compounds of the Formula I: and pharmaceutically acceptable salts, solvates and polymorphs thereof, wherein L, X 1 , R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined herein, for the treatment of BRAF-associated diseases and disorders, including BRAF-associated tumors, including malignant and benign BRAF-associated tumors of the CNS and malignant extracranial BRAF-associated tumors.

  本文提供了式I的化合物及其药用可接受的盐、溶剂合物和多晶形式，其中L、X1、R1、R2、R3、R4、R5和R6如本文所定义，用于治疗与BRAF相关的疾病和紊乱，包括BRAF相关的肿瘤，包括中枢神经系统的恶性和良性BRAF相关肿瘤以及恶性的颅外BRAF相关肿瘤。
• [EN] COMBINATION THERAPY FOR CANCER TREATMENT<br/>[FR] POLYTHÉRAPIE POUR LE TRAITEMENT DU CANCER
  申请人：HOFFMANN LA ROCHE

  公开号：WO2022258612A1

  公开（公告）日：2022-12-15

  The present invention is directed to the combination therapy of cancer with a BRAF inhibitor and a MEK inhibitor, as well as uses and pharmaceutical compositions thereof.

  本发明涉及使用BRAF抑制剂和MEK抑制剂的联合治疗癌症，以及其用途和制药组合物。
• [EN] COMBINATION OF A PARTICULAR BRAF INHIBITOR (PARADOX BREAKER) AND A PD-1 AXIS BINDING ANTAGONIST FOR USE IN THE TREATMENT OF CANCER<br/>[FR] ASSOCIATION D'UN INHIBITEUR DE BRAF PARTICULIER ("PARADOX BREAKER") ET D'UN ANTAGONISTE DE LIAISON À L'AXE PD-1 POUR UNE UTILISATION DANS LE TRAITEMENT DU CANCER
  申请人：HOFFMANN LA ROCHE

  公开号：WO2022258600A1

  公开（公告）日：2022-12-15

  The present invention is directed to a combination of the BRAF inhibitor N-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy- phenyl]-3-fluoro-pyrrolidine-l-sulfonamide or a pharmaceutically acceptable salt or solvate thereof with a PD-1 axis binding antagonist, and to the use of the combination as a medicament, in particular for the therapeutic and/or prophylactic treatment of cancer.

  本发明涉及一种BRAF抑制剂N-[2-氰基-4-氟-3-(3-甲基-4-氧-喹唑啉-6-基)氧基苯基]-3-氟-吡咯烷-1-磺酰胺或其药学上可接受的盐或溶剂与PD-1轴结合拮抗剂的组合物，并将该组合物用作药物，特别用于治疗和/或预防癌症。
• 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric SHP2 inhibitors
  申请人：Revolution Medicines, Inc.

  公开号：US10590090B2

  公开（公告）日：2020-03-17

  The present disclosure is directed to inhibitors of SHP2, such as pyrazine compounds, and their use in the treatment of disease associated with SHP2 modulation, such as Noonan Syndrome, Leopard Syndrome, juvenile myelomonocytic leukemias, neuroblastoma, melanoma, acute myeloid leukemia and cancers of the breast, lung and colon. Also disclosed are pharmaceutical compositions comprising the same.

  本公开涉及 SHP2 的抑制剂，例如吡嗪化合物，以及它们在治疗与 SHP2 调节相关的疾病中的用途，例如努南综合征、豹综合征、幼年骨髓单核细胞白血病、神经母细胞瘤、黑色素瘤、急性髓性白血病以及乳腺癌、肺癌和结肠癌。还公开了包含上述成分的药物组合物。