(2R)-6-methyl-6-azaspiro[2.5]octan-2-amine

• 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: (2R)-6-methyl-6-azaspiro[2.5]octan-2-amine
• 化学式: C₈H₁₆N₂
• 分子量: 140.23
• InChiKey: OSJIDMBLQNTFLE-SSDOTTSWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] SHP2 PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF<br/>[FR] INHIBITEURS DE PHOSPHATASE SHP2 ET LEURS PROCÉDÉS D'UTILISATION
  申请人：RELAY THERAPEUTICS INC

  公开号：WO2018057884A1

  公开（公告）日：2018-03-29

  The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the invention. The present invention further relates to, but is not limited to, methods for suppressing tumor cell growth, ameliorating the pathogenesis of systemic lupus erythematosus, and the treatment of various other disorders, including Noonan syndrome, diabetes, neutropenia, neuroblastoma, melanoma, juvenile leukemia, juvenile myelomonocytic leukemia, chronic myelomonocytic leukemia, acute myeloid leukemia, and other cancers associated with SHP2 deregulation with the compounds and compositions of the invention, alone or in combination with other treatments. Other cancers associated with SHP2 deregulation include HER2-positive breast cancer, triple-negative breast cancer, ductal carcinoma of the breast, invasive ductal carcinoma of the breast, non-small cell lung cancer, esophageal cancer, gastric cancer, squamous-cell carcinoma of the head and neck (SCCHN), and colon cancer.

  本发明涉及新颖化合物及其药物组合物，以及利用该发明的化合物和组合物抑制SHP2磷酸酶活性的方法。本发明还涉及但不限于抑制肿瘤细胞生长的方法，改善系统性红斑狼疮的发病机制，以及利用本发明的化合物和组合物治疗包括努南综合征、糖尿病、中性粒细胞减少症、神经母细胞瘤、黑色素瘤、儿童白血病、儿童单核细胞白血病、慢性单核细胞白血病、急性髓系白血病等各种其他疾病的方法，单独或与其他治疗方法结合使用。与SHP2失调相关的其他癌症包括HER2阳性乳腺癌、三阴性乳腺癌、乳腺导管癌、浸润性乳腺导管癌、非小细胞肺癌、食管癌、胃癌、头颈部鳞状细胞癌和结肠癌。
• [EN] PYRAZOLO[3,4-B]PYRAZINE DERIVATIVES AS SHP2 PHOSPHATASE INHIBITORS<br/>[FR] DÉRIVÉS DE PYRAZOLO [3,4-B] PYRAZINE EN TANT QU'INHIBITEURS DE LA PHOSPHATASE SHP2
  申请人：RELAY THERAPEUTICS INC

  公开号：WO2018081091A1

  公开（公告）日：2018-05-03

  The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the invention. The present invention further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds ad compositions of the invention.

  本发明涉及新化合物及其药物组合物，以及利用本发明的化合物和组合物抑制SHP2磷酸酶活性的方法。本发明还涉及但不限于利用本发明的化合物和组合物治疗与SHP2失调相关的疾病的方法。
• [EN] ION CHANNEL INHIBITORY COMPOUNDS, PHARMACEUTICAL FORMULATIONS AND USES<br/>[FR] COMPOSÉS INHIBITEURS DE CANAUX IONIQUES, FORMULATIONS PHARMACEUTIQUES, ET UTILISATIONS
  申请人：AFASCI INC

  公开号：WO2017083867A1

  公开（公告）日：2017-05-18

  The present invention is directed towards new chemical entities which primarily inhibit the human T-type calcium channels and differentially modulate other key ion channels to control cell excitability, and abnormal neuronal activity particularly involved in the development and maintenance of persistent or chronic pain, and / or neurological disorders. These novel compounds are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which these ion channels are involved. The invention is also directed towards pharmaceutical formulations comprising these compounds and the uses of these compounds.

  本发明主要针对新的化学实体，其主要抑制人类T型钙通道，并差异调节其他关键离子通道，以控制细胞兴奋性，以及参与持续性或慢性疼痛的发展和维持，和/或神经系统疾病的异常神经元活动。这些新颖化合物对治疗和预防这些离子通道参与的神经和精神疾病和疾病具有用处。该发明还涉及包含这些化合物的药物配方以及这些化合物的用途。