8-oxa-2-azaspiro[4.5]decan-1-one | 1555334-83-2

• 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: 8-oxa-2-azaspiro[4.5]decan-1-one
• CAS: 1555334-83-2
• 化学式: C₈H₁₃NO₂
• mdl: MFCD26938035
• 分子量: 155.197
• InChiKey: ILDSGCMBFCWJOI-UHFFFAOYSA-N

物化性质

• 沸点：
  360.6±35.0 °C(Predicted)
• 密度：
  1.14±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.875
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  8-oxa-2-azaspiro[4.5]decan-1-one 在 N-甲基二环己基胺 、 1,3-双(二苯基膦)丙烷 、 palladium diacetate 、 N,N-二异丙基乙胺 、 三氯氧磷 作用下， 以 乙二醇二甲醚 、 1,2-二氯乙烷 为溶剂， 反应 2.0h， 生成 5’-acetyl-7’-fluoro-1‘,2,2’,3,5,6-hexahydro-9’H-spiro[pyran-4,3’-pyrrolo[2,1-b]quinazolin]-9’-one
  参考文献：
  名称：

  SUBSTITUTED SPIROCYCLIC-PYRROLOQUINAZOLINONES AND SPIROCYCLIC-PIPERIDINOQUINAZOLINONES

  摘要：

  Disclosed herein are substituted spirocyclic-pyrroloquinazolinones and spirocyclic-piperidinoquinazolinones of formula (I), methods for their preparation, and uses thereof.

  公开号：

  WO2024148150A1

文献信息

• [EN] SUBSTITUTED FURANOPYRIMIDINE COMPOUNDS AS PDE1 INHIBITORS<br/>[FR] COMPOSÉS FURANOPYRIMIDINE SUBSTITUÉS UTILISÉS EN TANT QU'INHIBITEURS DE PDE1
  申请人：DART NEUROSCIENCE LLC

  公开号：WO2019104285A1

  公开（公告）日：2019-05-31

  Substituted furanopyrimidine chemical entities of Formula (I): wherein Ra has any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by PDE1 activity or dopaminergic signaling; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training protocols; and treating peripheral disorders, including cardiovascular, renal, hematological, gastroenterological, liver, cancer, fertility, and metabolic disorders.

  化学实体的呋喃嘧啶替代物的化学结构如下（I）：其中Ra具有以下所述的任何值，并含有此类化学实体的组合物；制备它们的方法；以及它们在广泛应用中的使用，包括代谢和反应动力学研究；检测和成像技术；放射性治疗；调节和治疗由PDE1活性或多巴胺信号传导介导的疾病；治疗神经系统疾病，中枢神经系统疾病，痴呆症，神经退行性疾病和依赖创伤的功能丧失；治疗中风，包括中风康复期间的认知和运动缺陷；促进神经保护和神经恢复；增强认知和运动训练的效率，包括动物技能训练方案；以及治疗周围疾病，包括心血管，肾脏，血液，胃肠，肝脏，癌症，生育和代谢性疾病。
• [EN] SUBSTITUTED BENZOXAZOLE AND BENZOFURAN COMPOUNDS AS PDE7 INHIBITORS<br/>[FR] COMPOSÉS DE BENZOXAZOLE ET DE BENZOFURANE SUBSTITUÉS UTILISÉS EN TANT QU'INHIBITEURS DE PDE7
  申请人：DART NEUROSCIENCE LLC

  公开号：WO2019014305A1

  公开（公告）日：2019-01-17

  Substituted benzoxazole and benzofuran chemical entities of Formula (I): wherein, V, W, X, Y, Z, and m have any of the values described herein and compositions comprising such chemical entities; processes for making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; and the treatment of one or more disorders, including neurological, cognitive, immunological, and inflammatory disorders, as well as other conditions and diseases involving PDE7 or cyclic nucleotide signaling.

  式（I）中的取代苯并噁唑和苯并呋喃化学实体：其中，V、W、X、Y、Z和m可以具有本文描述的任何值，以及包含这些化学实体的组合物；制备它们的方法；以及它们在广泛的方法中的应用，包括代谢和反应动力学研究；检测和成像技术；放射性治疗；以及治疗一个或多个疾病，包括神经、认知、免疫和炎症性疾病，以及涉及PDE7或环核苷酸信号的其他状况和疾病。
• HIGHLY ACTIVE CSF1R INHIBITOR COMPOUND
  申请人：Adlai Nortye Biopharma Co., Ltd.

  公开号：EP3744718A1

  公开（公告）日：2020-12-02

  ABSTRACT The present invention relates to a CSF1R inhibitor, and in particular to a highly active CSF1R inhibitor compound having the structure of formula (I). Said compound of the present invention has high inhibitory activity on CSF1R.

  摘要 本发明涉及一种 CSF1R 抑制剂，尤其涉及一种具有式（I）结构的高活性 CSF1R 抑制剂化合物。本发明的所述化合物对 CSF1R 具有高抑制活性。
• BICYCLIC LACTAMS AS RECEPTOR-INTERACTING PROTEIN-1 (RIP1) KINASE INHIBITORS FOR TREATING E.G. INFLAMMATORY DISEASES
  申请人：F. Hoffmann-La Roche AG

  公开号：EP3760625A1

  公开（公告）日：2021-01-06

  The invention provides compounds having the general formula (I) wherein R1, X, Z1, L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and the compounds for use in methods of medical treatment. The present compounds are receptor-interacting protein-1 (RIP1) kinase inhibitors useful for treating e.g. inflammatory diseases, such as e.g. irritable bowel disorders (IBD), irritable bowel syndrome (IBS), Crohn's disease, ulcerative colitis, myocardial infarction, stroke, traumatic brain injury, atherosclerosis, ischemia-reperfusion injury of kidneys, liver and lungs, cisplatin-induced kidney injury, sepsis, systemic inflammatory response syndrome (SIRS), pancreatits, psoriasis, retinitis pigmentosa, retinal degeneration, chronic kidney diseases, acute respiratory distress syndrome (ARDS), chronic obstructive pulmonary disease (COPD). The present description discloses the preparation of exemplary and reference compounds, as well as pharmacological data thereof (e.g. pages 116 to 1221; examples 1 to 793; examples A to C; tables). An exemplary compound is e.g. 5a-methyl-N-((S)-5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-1,4,4a,5,5a,6-hexahydrocyclopropa[f]indazole-3-carboxamide (example 1)

  本发明提供具有通式 (I) 的化合物 其中 R1、X、Z1、L、n、A 环、B 环和 C 环如本文所述；包括本发明化合物的药物组合物；以及本发明化合物在医疗方法中的用途。 本化合物是受体相互作用蛋白-1（RIP1）激酶抑制剂，可用于治疗炎症性疾病，例如肠易激综合征 (IBS)、克罗恩病、溃疡性结肠炎、心肌梗塞、中风、脑外伤、动脉粥样硬化、肾脏、肝脏和肺部缺血再灌注损伤、顺铂诱导的肾损伤、败血症、全身性炎症性休克、溃疡性结肠炎等、败血症、全身炎症反应综合征（SIRS）、胰腺炎、银屑病、色素性视网膜炎、视网膜变性、慢性肾脏疾病、急性呼吸窘迫综合征（ARDS）、慢性阻塞性肺病（COPD）。 本说明书公开了示例化合物和参考化合物的制备方法及其药理数据（如第 116 页至第 1221 页；例 1 至例 793；例 A 至例 C；表）。 示例化合物如 5a-甲基-N-((S)-5-甲基-4-氧代-2,3,4,5-四氢苯并[b][1,4]氧氮杂卓-3-基)-1,4,4a,5,5a,6-六氢环丙基[f]吲唑-3-甲酰胺（例 1）
• Substituted cyclohexyl compounds as NOP inhibiiors
  申请人：Dart NeuroScience, LLC

  公开号：US11365191B2

  公开（公告）日：2022-06-21

  Substituted cyclohexyl chemical entities of Formula (I): wherein Ra, G, and Rb have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.

  式(I)的取代环己基化学实体：其中 Ra、G 和 Rb 具有本文所述的任一值，以及包含此类化学实体的组合物；其制造方法；及其在多种方法中的用途，包括代谢和反应动力学研究；检测和成像技术；放射性疗法；调节和治疗由痛觉素活性或多巴胺信号传导介导的疾病；治疗神经系统疾病、神经退行性疾病、抑郁症和精神分裂症；提高认知和运动训练的效率；治疗外周疾病，包括肾脏、呼吸系统、胃肠道、肝脏、泌尿生殖系统、代谢和炎症性疾病。