8-oxabicyclo[3.2.1]octan-3-ol | 1172846-34-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氧烷类
• 英文名称: 8-oxabicyclo[3.2.1]octan-3-ol
• CAS: 1172846-34-2
• 化学式: C₇H₁₂O₂
• 分子量: 128.171
• InChiKey: CSGTZGMKSPXFEQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  9
• 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：
  29.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  8-oxabicyclo[3.2.1]octan-3-ol 、 N-(3-氯-4-氟苯基)-7-氟-6-硝基-4-喹唑啉胺 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 反应 0.5h， 以100%的产率得到7-(8-oxabicyclo[3.2.1]octan-3-yloxy)-N-(4-(3-chloro-4-fluorophenyl))-6-nitroquinazolin-4-amine
  参考文献：
  名称：

  QUINAZOLINE DERIVATIVES SUBSTITUTED BY ANILINE, PREPARATION METHOD AND USE THEREOF

  摘要：

  该发明涉及被苯胺取代的喹唑啉衍生物，其由下式（I）所表示，以及其药用可接受的盐和立体异构体，其中R1、R2、R3、R4、R5、R6、L和n这些基团具有规范中给定的含义。该发明还涉及制备方法、药物组合物、药物制剂以及用于治疗过度增生和慢性阻塞性肺疾病的药物制备的用途，以及用于治疗过度增生和慢性阻塞性肺疾病的用途。

  公开号：

  US20130184297A1
• 作为产物：
  描述：

  Glauber's salt 、 8-氧杂双环[3.2.1]辛烷-3-酮 以 四氢呋喃 为溶剂， 生成 8-oxabicyclo[3.2.1]octan-3-ol
  参考文献：
  名称：

  EP1342717

  摘要：

  公开号：

文献信息

• [EN] THIENOPYRIMIDINE DERIVATIVES AS ACC INHIBITORS AND USES THEREOF<br/>[FR] DÉRIVÉS DE THIÉNOPYRIMIDINE SUBSTITUÉS UTILISÉS EN TANT QU'INHIBITEURS D'ACC ET LEURS UTILISATIONS
  申请人：GILEAD SCIENCES INC

  公开号：WO2021030142A1

  公开（公告）日：2021-02-18

  The present disclosure relates generally to compounds that bind to Acetyl-CoA Carboxylase (ACC) and act as inhibitors of ACC. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of ACC, including liver diseases such as non-alcoholic fatty liver disase (NAFLD) and non-alcoholic steatohepatitis (NASH).

  本公开涉及一般与结合乙酰辅酶A羧化酶（ACC）并作为ACC的抑制剂的化合物有关。此外，本公开还涉及利用这些化合物制备药物以治疗通过结合ACC引起的疾病和/或状况，包括非酒精性脂肪肝病（NAFLD）和非酒精性脂肪性肝炎（NASH）等肝病。
• Benzimidazole derivatives
  申请人：——

  公开号：US20040044056A1

  公开（公告）日：2004-03-04

  This invention relates to the compounds represented by a general formula [I]: 1 [in which A 1 and A 2 represent optionally fluorine-substituted methine or the like; B represents halogen, cyano, lower alkyl or the like; D represents optionally substituted heterocyclic group or the like; and G represents C 3 -C 20 aliphatic group such as alicyclic group]. These compounds inhibit nociceptin activities due to their high affinity to nociceptin receptor, and are useful as analgesic, antiobestic, corebral function improver, drugs for treatment of alzheimer's disease and dementia, remedies for schizophrenia and neurodegenerative diseases, antidepressant, remedies for diabetes insipidus, polyuria, hypotension and so on.

  本发明涉及由一般式[I]表示的化合物：1[其中，A1和A2表示选择性氟代甲基或类似物；B表示卤素，氰基，低碳烷基或类似物；D表示选择性取代的杂环基团或类似物；G表示C3-C20脂肪族基团，例如脂环族基团]。这些化合物由于对痛觉受体具有高亲和力而抑制了痛觉肽活性，并且可用作镇痛剂，抗肥胖剂，脑功能改善剂，治疗阿尔茨海默病和痴呆症的药物，治疗精神分裂症和神经退行性疾病的药物，抗抑郁剂，治疗尿崩症，多尿症，低血压等的药物。
• [EN] BRIDGED COMPOUNDS AS KRAS G12D INHIBITOR AND DEGRADER AND THE USE THEREOF<br/>[FR] COMPOSÉS PONTÉS EN TANT QU'INHIBITEUR ET DÉGRADEUR DE KRAS G12D ET LEUR UTILISATION
  申请人：BEIGENE LTD

  公开号：WO2022148422A1

  公开（公告）日：2022-07-14

  Provided herein are Bridged Compounds having the following structures: (I) wherein R1a, R1b, R1c, R1d, R2a, R2b, R2c, R2d, R3a, R3b, R3c, R3d, R4, R5, R6, R7, R8, m1, m2, m3, n2, n3, n4, q, X1, X2, Y1, Y2, L1and ring A are as defined herein, compositions comprising an effective amount of a Bridged Compound, and methods for treating or preventing various diseases, e.g., pancreatic cancer, or a condition treatable or preventable by inhibition of the function of KRAS protein. In another aspect, a Bridged Compound is useful for treating or preventing a condition treatable or preventable by inhibition of the function of KRAS protein with G12D mutation. In another aspect, a Bridged Compound is useful for treating or preventing a condition treatable or preventable by inhibition of a RAS/MAPK pathway.

  本文提供了具有以下结构的桥接化合物：（I），其中R1a，R1b，R1c，R1d，R2a，R2b，R2c，R2d，R3a，R3b，R3c，R3d，R4，R5，R6，R7，R8，m1，m2，m3，n2，n3，n4，q，X1，X2，Y1，Y2，L1和环A的定义如本文所述，包含有效量的桥接化合物的组合物，以及用于治疗或预防各种疾病的方法，例如胰腺癌或可通过抑制KRAS蛋白功能来治疗或预防的疾病。在另一个方面，桥接化合物可用于治疗或预防可通过抑制具有G12D突变的KRAS蛋白功能来治疗或预防的疾病。在另一个方面，桥接化合物可用于治疗或预防可通过抑制RAS / MAPK途径来治疗或预防的疾病。
• BENZIMIDAZOLE DERIVATIVES
  申请人：BANYU PHARMACEUTICAL CO., LTD.

  公开号：EP1342717A1

  公开（公告）日：2003-09-10

  This invention relates to the compounds represented by a general formula [I]:    [in which A1 and A2 represent optionally fluorine-substituted methine or the like; B represents halogen, cyano, lower alkyl or the like; D represents optionally substituted heterocyclic group or the like; and G represents C3-C20 aliphatic group such as alicyclic group]. These compounds inhibit nociceptin activities due to their high affinity to nociceptin receptor, and are useful as analgesic, antiobestic, corebral function improver, drugs for treatment of alzheimer's disease and dementia, remedies for schizophrenia and neurodegenerative diseases, antidepressant, remedies for diabetes insipidus, polyuria, hypotension and so on.

  本发明涉及通式[I]所代表的化合物： [其中 A1 和 A2 代表任选氟取代的甲基或类似物；B 代表卤素、氰基、低级烷基或类似物；D 代表任选取代的杂环基团或类似物；G 代表 C3-C20 脂肪族基团，例如脂环族基团]。这些化合物由于与痛觉素受体的高亲和力而抑制痛觉素的活性，可用作镇痛剂、抗镇静剂、改善大脑核心功能的药物、治疗老年痴呆症和痴呆症的药物、治疗精神分裂症和神经退行性疾病的药物、抗抑郁剂、治疗糖尿病、多尿、低血压等。
• Quinazoline derivatives substituted by aniline, preparation method and use thereof
  申请人：XUANZHU PHARMA CO., LTD.

  公开号：US10507209B2

  公开（公告）日：2019-12-17

  The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.

  本发明涉及由苯胺取代的喹唑啉衍生物，这些衍生物由下式(I)表示，其药物可接受盐和立体异构体，其中R1、R2、R3、R4、R5、R6、L和n这些基团具有说明书中给出的含义。本发明还涉及治疗过度增生和慢性阻塞性肺病药物的制备方法、药物组合物、药物制剂和制备用途及其治疗过度增生和慢性阻塞性肺病的用途。