5-Tert-butyl-5-azaspiro[2.4]heptane

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 5-Tert-butyl-5-azaspiro[2.4]heptane
• 英文别名: 5-tert-butyl-5-azaspiro[2.4]heptane
• 化学式: C₁₀H₁₉N
• 分子量: 153.26
• InChiKey: NRBHPXQPSOPKTA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• Prodrugs Of Bicyclic Substituted Pyrimidine Type PDE-5 Inhibitors
  申请人：XUANZHU PHARMA CO., LTD.

  公开号：US20160046654A1

  公开（公告）日：2016-02-18

  Provided are prodrugs of a bicyclic substituted pyrimidine type PDE-5 inhibitors, pharmaceutically acceptable salts or stereoisomers thereof. Also provided are methods for preparing these prodrug compounds, pharmaceutical preparations, and pharmaceutical compositions, as well as a use of these compounds, pharmaceutical preparations and pharmaceutical compositions in the manufacture of medicaments for treatment and/or prophylaxis of sexual dysfunction and lower urinary tract symptoms.

  提供了一种双环替代嘧啶型PDE-5抑制剂的前药，其药用盐或立体异构体。还提供了制备这些前药化合物、制药制剂和制药组合物的方法，以及这些化合物、制药制剂和制药组合物在制造用于治疗和/或预防性功能障碍和下尿路症状的药物中的用途。
• INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR AND USE THEREOF
  申请人：Nanjing TransThera Biosciences Co. Ltd.

  公开号：US20190209564A1

  公开（公告）日：2019-07-11

  Provided are an irreversible inhibitor of a fibroblast growth factor receptor (FGFR) as indicated by formula I, a pharmaceutically acceptable salt, a stereoisomer, a pharmaceutical preparation, a pharmaceutical composition and an application thereof. R 1 , R 2 , R 3 , R 4 , ring A, Ar, ring B and warhead are as defined in the specification. The compound has high-efficiency and high-selectivity inhibition of a fibroblast growth factor receptor and can be applied to treatment of abnormal FGF/FGFR-mediated diseases, in particular the treatment of cancers.

  提供了一种不可逆的成纤维细胞生长因子受体（FGFR）抑制剂，如式I所示，以及其药学上可接受的盐、立体异构体、药物制剂、药物组合物及其应用。R1、R2、R3、R4、环A、Ar、环B和弹头如说明书中所定义。该化合物对成纤维细胞生长因子受体具有高效和高选择性的抑制作用，可用于治疗异常FGF/FGFR介导的疾病，特别是癌症的治疗。
• 9-AMINOMETHYL SUBSTITUTED TETRACYCLINE COMPOUNDS
  申请人：Zhang Hui

  公开号：US20140179638A1

  公开（公告）日：2014-06-26

  The present invention relates to 9-aminomethyl substituted tetracycline compounds represented by formula (I), or pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as well as a method for preparing these compounds and a pharmaceutical composition comprising the same. The present invention relates also to a use of these compounds in the preparation of a medicament for the treatment and/or prophylaxis of tetracycline drug-sensitive disease. wherein, R 2a , R 2b , R 3 , R 4a , R 4b , R 5 , R 6a , R 6b , R 7 , R 8 , R 9a , R 9b , R 10 , R 11 , R 12 , R 13a and R 13b are each independently as defined in the description.

  本发明涉及由式(I)表示的9-氨甲基取代四环素化合物，或其药学上可接受的盐、前药、溶剂化合物或异构体，以及制备这些化合物的方法和包含其的药物组合物。本发明还涉及这些化合物在制备用于治疗和/或预防四环素药物敏感疾病的药物中的用途。其中，R2a、R2b、R3、R4a、R4b、R5、R6a、R6b、R7、R8、R9a、R9b、R10、R11、R12、R13a和R13b各自独立地如描述中所定义。
• QUINAZOLINE DERIVATIVE AS TYROSINE-KINASE INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
  申请人：Wu Frank

  公开号：US20140161801A1

  公开（公告）日：2014-06-12

  The invention relates to a quinazoline derivative represented by the general formula (I), a pharmaceutical acceptable salt and a stereoisomer thereof as tyrosine kinase inhibitor, wherein R 1 , R 2 , R 3 , R 3′ , R 4 , R 5 , R 6 , X, L, T, Z and q are as defined in the specification. The invention also relates to a process for preparing the same, a pharmaceutical composition and a pharmaceutical formulation containing the derivative, use of the derivative for treating excessive proliferative diseases and chronic obstructive pulmonary disease and use of the derivative in the manufacture of a medicament for treating excessive proliferative diseases and chronic obstructive pulmonary disease.

  该发明涉及一种喹唑啉衍生物，其通式表示为(I)，作为酪氨酸激酶抑制剂的药用可接受盐和立体异构体，其中R1、R2、R3、R3'、R4、R5、R6、X、L、T、Z和q如规范中所定义。该发明还涉及一种制备该衍生物的方法，包含该衍生物的药用组合物和药用配方，以及将该衍生物用于治疗过度增殖性疾病和慢性阻塞性肺病，以及将该衍生物用于制造用于治疗过度增殖性疾病和慢性阻塞性肺病的药物。
• DIHYDROQUINOXALINE BROMODOMAIN RECOGNITION PROTEIN INHIBITOR, PREPARATION METHOD AND USE THEREOF
  申请人：SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACDEMY OF SCIENCES

  公开号：US20200031802A1

  公开（公告）日：2020-01-30

  The present invention relates to dihydroquinoxaline bromodomain recognition protein inhibitor, preparation method and use thereof. The inhibitor of the present invention is compound represented by general formula (I), or stereoisomer, pharmaceutically acceptable salt, prodrug, solvate, hydrate and crystal form thereof. The definition of each substituent is as described in the description and claims. The compound represented by general formula (I) of the present invention may inhibit bromodomain recognition protein and may be used for preparing medicament which regulates the apparent state of cells and treats series of diseases and symptoms which are mediated by the bromodomain recognition protein.

  本发明涉及二氢喹喔啉溴结构域识别蛋白抑制剂，其制备方法及用途。本发明的抑制剂是由通式（I）表示的化合物，或其立体异构体、药学上可接受的盐、前药、溶剂化合物、水合物和晶型形式。每个取代基的定义如描述和索赔中所述。本发明的通式（I）表示的化合物可能抑制结构域识别蛋白，并可用于制备调节细胞表观状态并治疗由结构域识别蛋白介导的一系列疾病和症状的药物。