trans-tert-butyl-4-fluoro-3-hydroxypiperidine-1-carboxylate

• 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: trans-tert-butyl-4-fluoro-3-hydroxypiperidine-1-carboxylate
• 英文别名: Tert-butyl 4-fluoro-3-hydroxypiperidine-1-carboxylate
• 化学式: C₁₀H₁₈FNO₃
• 分子量: 219.256
• InChiKey: FZAKOAFETOZBLC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  49.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2,4-二氯-7-(2-三甲基锡乙氧基甲基)-7H-吡咯并[2,3-d]嘧啶 、 trans-tert-butyl-4-fluoro-3-hydroxypiperidine-1-carboxylate 在 sodium hydride 作用下， 以 四氢呋喃 为溶剂， 反应 2.5h， 以83.1%的产率得到trans-tert-butyl-3-((2-chloro-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-4-fluoropiperidine-1-carboxylate
  参考文献：
  名称：

  Oxy-fluoropiperidine Derivative as Kinase Inhibitor

  摘要：

  本发明涉及以下化学式1所表示的化合物或其药学上可接受的盐，而根据本发明的化合物可以用于预防或治疗与激酶抑制作用相关的疾病。

  公开号：

  US20200308177A1

文献信息

• [EN] INHIBITORS OF MUTANT FORMS OF EGFR<br/>[FR] INHIBITEURS DE FORMES MUTANTES DE L'EGFR
  申请人：BLUEPRINT MEDICINES CORP

  公开号：WO2021133809A1

  公开（公告）日：2021-07-01

  The present disclosure provides a compound represented by structural formula (I) : or a pharmaceutically acceptable salt thereof useful for treating a cancer.

  本公开提供了一种由结构公式（I）表示的化合物：或其药用可接受的盐，用于治疗癌症。
• [EN] PYRROLOPYRIDINES AS KINASE INHIBITORS<br/>[FR] PYRROLOPYRIDINES EN TANT QU'INHIBITEURS DE KINASE
  申请人：ARRAY BIOPHARMA INC

  公开号：WO2009140320A1

  公开（公告）日：2009-11-19

  Compounds of Formula (I) are useful for inhibition of CHKl and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

  公式（I）的化合物对于CHKl和/或CHK2的抑制是有用的。本文揭示了使用公式（I）的化合物及其立体异构体和药学上可接受的盐，以进行哺乳动物细胞中的体外、体内和原位诊断、预防或治疗这些疾病，或相关的病理条件的方法。
• NOVEL HETEROCYCLYL COMPOUNDS
  申请人：Aebi Johannes

  公开号：US20110092698A1

  公开（公告）日：2011-04-21

  The invention is concerned with novel bicyclic compounds of formula (I), wherein n, m, p, A, L, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 7 , R 8 , R 9 , and R 10 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor may be used, for example, in the prevention and/or treatment of inflammatory diseases, particularly peripheral arterial occlusive diseases or atherothrombosis.

  这项发明涉及式(I)的新颖双环化合物，其中n、m、p、A、L、R1、R2、R3、R4、R5、R6、R7、R7、R8、R9和R10如描述和索赔中所定义，并且其生理上可接受的盐。这些化合物是CCR2受体、CCR5受体和/或CCR3受体的拮抗剂，例如可用于预防和/或治疗炎症性疾病，特别是外周动脉闭塞疾病或动脉粥样硬化形成。
• SUBSTITUTED THIAZOLIDINEDIONE INDAZOLES, INDOLES AND BENZOTRIAZOLES AS ESTROGEN-RELATED RECEPTOR-a MODULATORS
  申请人：Bignan Gilles

  公开号：US20110294780A1

  公开（公告）日：2011-12-01

  The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

  本发明涉及式(I)的化合物，制备这些化合物的方法，组合物，中间体及其衍生物，并用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿关节炎，感染性关节炎，儿童关节炎，银屑病性关节炎，反应性关节炎），与骨相关的疾病（包括与骨形成有关的疾病），乳腺癌（包括对抗雌激素治疗无效的癌症），心血管疾病，软骨相关疾病（如软骨损伤/丧失，软骨退化以及与软骨形成有关的疾病），软骨发育不良，软骨肉瘤，慢性腰部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺疾病，糖尿病，能量稳态紊乱，痛风，假性痛风，脂质紊乱，代谢综合征，多发性骨髓瘤，肥胖，骨关节炎，遗传性骨发育不全，骨溶解性骨转移，软骨软化症，骨质疏松症，帕金森病，牙周病，多肌痛风，Reiter综合征，重复性应激损伤，高血糖，血糖水平升高和胰岛素抵抗等病症的方法。
• [EN] 1, 7 - DIAZACARBAZOLES AND THEIR USE IN THE TREATMENT OF CANCER<br/>[FR] 1,7-DIAZACARBAZOLES ET LEUR UTILISATION DANS LE TRAITEMENT DU CANCER
  申请人：HOFFMANN LA ROCHE

  公开号：WO2011073263A1

  公开（公告）日：2011-06-23

  The invention relates to 1, 7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk 1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

  这项发明涉及式(I)、(I-a)和(I-b)的1,7-二氮杂咔唑化合物，这些化合物可用作激酶抑制剂，更具体地用作检查点激酶1（chk 1）抑制剂，因此可用作癌症治疗剂。该发明还涉及含有这些化合物的组合物，更具体地是含有这些化合物的药物组合物，以及使用它们来治疗各种癌症和过度增殖性疾病的方法，以及使用这些化合物进行哺乳动物细胞的体外、体内和体外诊断或治疗以及相关病理情况的方法。