3-azabicyclo[4.1.0]heptan-2-one | 31681-11-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: 3-azabicyclo[4.1.0]heptan-2-one
• 英文别名: 3-Azabicyclo[4.1.0]heptan-2-one
• CAS: 31681-11-5
• 化学式: C₆H₉NO
• 分子量: 111.144
• InChiKey: ADZAHAGYKIKDBM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  8
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  3,6-difluoro-9-(oxiran-2-ylmethyl)-9H-carbazole 、 3-azabicyclo[4.1.0]heptan-2-one 反应 16.0h， 生成 3-(3-(3,6-difluoro-9H-carbazol-9-yl)-2-hydroxypropyl)-3-azabicyclo[4.1.0]heptan-2-one
  参考文献：
  名称：

  含咔唑的酰胺和脲：发现隐花色素调节剂作为降糖药

  摘要：

  合成了一系列新型的含咔唑的酰胺和脲。这些化合物的结构-活性关系研究导致了强效隐色调节剂的鉴定。基于所需的药代动力学/药效学参数和在db / db小鼠中的功效研究结果，选择化合物50进行进一步分析。

  DOI：

  10.1016/j.bmcl.2017.12.051

文献信息

• 1,2,3,4-TETRAHYDROQUINOXALINE DERIVATIVE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
  申请人：Abbisko Therapeutics Co., Ltd.

  公开号：US20220009894A1

  公开（公告）日：2022-01-13

  A 1,2,3,4-tetrahydroquinoxaline derivative having a structure as represented by formula (I), preparation method therefor and application thereof. These compounds can be widely applied to preparation of drugs for treating one or more tumors, cancers, metabolic diseases, autoimmune diseases or disorders, and a new generation of RORγt agonist drugs is expected to be developed.

  一种具有如公式（I）所示结构的1,2,3,4-四氢喹喔啉衍生物，其制备方法及应用。这些化合物可以广泛应用于制备用于治疗一个或多个肿瘤、癌症、代谢性疾病、自身免疫疾病或紊乱的药物，预计将开发出新一代RORγt激动剂药物。
• FGFR4 INHIBITOR, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
  申请人：Abbisko Therapeutics Co., Ltd.

  公开号：US20190270742A1

  公开（公告）日：2019-09-05

  Provided are an FGFR4 inhibitor having the structure of formula (I), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and can be widely used in the preparation of a drug for treating cancers, especially prostate cancer, liver cancer, pancreatic cancer, esophageal carcinomas, gastric cancer, lung cancer, breast cancer, ovarian carcinomas, colon cancer, skin cancer, glioblastomas or rhabdomyosarcomas, and is expected to be developed into a new generation of FGFR4 inhibitor drugs.

  提供一种具有结构式（I）的FGFR4抑制剂，以及其制备方法和用途。该化合物对FGFR4激酶活性具有非常强的抑制作用，并具有非常高的选择性，可以广泛用于制备用于治疗癌症的药物，特别是前列腺癌、肝癌、胰腺癌、食管癌、胃癌、肺癌、乳腺癌、卵巢癌、结肠癌、皮肤癌、胶质母细胞瘤或横纹肌肉瘤，并有望被开发成新一代的FGFR4抑制剂药物。
• N-(AZAARYL)CYCLOLACTAM-1-CARBOXAMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
  申请人：Abbisko Therapeutics Co., Ltd.

  公开号：US20200071302A1

  公开（公告）日：2020-03-05

  An N-(azaaryl)cyclolactam-1-carboxamide derivative having a structure of formula (I), a preparation method therefor, and a use thereof are disclosed in the application. Each substituent are defined in the specification and claims. The series of compounds of the application can be widely applied in the preparation of drugs for treating cancer, tumor, autoimmune disease, metabolic disease or metastatic disease, particularly for treating ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic disease, neurodegenerative disease, primary tumor site metastasis or osseous metastasis cancer, and are expected to be developed into a new generation of CSF-1R inhibitor drugs.

  本申请公开了具有结构式（I）的N-(azaaryl)cyclolactam-1-羧酰胺衍生物，其制备方法及用途。每个取代基在规范和权利要求中有定义。本申请中的化合物系列可广泛应用于制备用于治疗癌症、肿瘤、自身免疫疾病、代谢性疾病或转移性疾病的药物，特别适用于治疗卵巢癌、胰腺癌、前列腺癌、乳腺癌、宫颈癌、胶质母细胞瘤、多发性骨髓瘤、代谢性疾病、神经退行性疾病、原发肿瘤部位转移或骨转移癌症，并有望开发成为新一代CSF-1R抑制剂药物。
• NITROGEN HETEROARYL DERIVATIVE HAVING CSF1R INHIBITORY ACTIVITY, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
  申请人：Abbisko Therapeutics Co., Ltd.

  公开号：US20200140431A1

  公开（公告）日：2020-05-07

  This application describes a nitrogen heteroaryl derivative having CSF1R inhibitory activity, and a preparation method therefor and an application thereof. Compounds in the present invention has a structure represented by formula (I) as below, and the definition on substituents is as stated in the description and the claims. The compounds in the this application can be widely applied to preparation of drugs for treating cancer, tumor, autoimmune disease, metabolic disease, or metastatic disease, in particular ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic disease, neurodegenerative disease, metastasis of primary tumor sites, or osseous metastatic cancer, and a new generation of CSF1R inhibitor drugs is expected to be developed.

  该应用描述了一种具有CSF1R抑制活性的氮杂芳基衍生物，以及其制备方法和应用。本发明中的化合物具有以下式(I)所代表的结构，取代基的定义如描述和权利要求中所述。本申请中的化合物可以广泛应用于制备用于治疗癌症、肿瘤、自身免疫疾病、代谢性疾病或转移性疾病的药物，特别是卵巢癌、胰腺癌、前列腺癌、乳腺癌、宫颈癌、胶质母细胞瘤、多发性骨髓瘤、代谢性疾病、神经退行性疾病、原发性肿瘤部位的转移、或骨转移癌，预计将开发出新一代CSF1R抑制剂药物。
• [EN] IMMUNOSUPPRESSANT, AND PREPARATION METHOD THEREFOR AND USE THEREOF<br/>[FR] IMMUNOSUPPRESSEUR, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION<br/>[ZH] 一种免疫抑制剂、其制备方法和应用
  申请人：ABBISKO THERAPEUTICS CO LTD

  公开号：WO2021254005A1

  公开（公告）日：2021-12-23

  一种式(Ⅰ)结构免疫抑制剂、其制备方法和应用。本发明系列化合物可广泛应用于制备预防和/或治疗由PD-1/PD-L1信号通路介导的癌症或肿瘤、免疫相关疾病及紊乱、传染性疾病、感染性疾病或代谢性疾病的药物，有望开发成新一代PD-1/PD-L1抑制剂。