AZD 1446;3-(5-Chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane | 1025007-04-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: AZD 1446;3-(5-Chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane
• 英文别名: 2,3,3a,4,6,6a-hexahydro-1H-pyrrolo[3,4-c]pyrrol-5-yl-(5-chlorofuran-2-yl)methanone
• CAS: 1025007-04-8
• 化学式: C₁₁H₁₃ClN₂O₂
• 分子量: 240.68
• InChiKey: GTUIQNHJSXQMKW-UHFFFAOYSA-N

物化性质

• 沸点：
  387.8±42.0 °C(Predicted)
• 密度：
  1.323±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  45.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Imidazole Substituted Pyrimidines
  申请人：Arvidsson Per I

  公开号：US20100267723A1

  公开（公告）日：2010-10-21

  A compound of formula (I) wherein R 1 is hydrogen or fluoro; R 2 and R 3 are independently selected from hydrogen or methyl, or a pharmaceutically acceptable salt thereof; pharmaceutical formulations containing said compound; the use of said compound in therapy; the use for the treatment of conditions associated with glycogen synthase kinase-3 related disorders, such as Alzheimer's disease, as well as methods of treatment of said disorders, comprising administering to subjects in need of such treatment, a therapeutically effective amount of said compound.

  式（I）的化合物，其中R1为氢或氟；R2和R3分别选择自氢或甲基，或其药用可接受的盐；含有该化合物的药物配方；该化合物在治疗中的使用；用于治疗与糖原合酶激酶-3相关疾病的条件，如阿尔茨海默病，以及治疗上述疾病的方法，包括向需要该治疗的受试者施用该化合物的治疗有效量。
• OXAZOLO[4,5-c]PYRIDINE SUBSTITUTED PYRAZINE
  申请人：Ahlin Kristofer

  公开号：US20110118275A1

  公开（公告）日：2011-05-19

  The present invention relates to a compound of formula (I) wherein R 1 is hydrogen or methyl, or a pharmaceutically acceptable salt thereof, pharmaceutical formulations containing said compound, to the use of said active compound in therapy, as well as intermediates.

  本发明涉及一种化合物的公式(I)，其中R1为氢或甲基，或其药用盐，含有该化合物的药物配方，以及在治疗中使用该活性化合物，以及中间体。
• [EN] IMIDAZOLE SUBSTITUTED PYRIMIDINE HAVING A HIGH GSK3 INHIBITING POTENCY AS WELL AS PAN-KINASE SELECTIVITY<br/>[FR] PYRIMIDINE SUBSTITUÉE PAR IMIDAZOLE AYANT UNE PUISSANCE ÉLEVÉE D'INHIBITION DE LA GSK3 AINSI QU'UNE SÉLECTIVITÉ PAN-KINASES
  申请人：ASTRAZENECA AB

  公开号：WO2012050517A1

  公开（公告）日：2012-04-19

  The present invention relates to a new compound of formula (I) as a free base or a pharmaceutically acceptable salt thereof, in an essentially pure and isolated form, a pharmaceutical composition containing a compound of formula (I), to the use of said active compound in therapy, to the use for the treatment of conditions associated with glycogen synthase kinase-3 related disorders, such as Alzheimer's disease, as well as for the method of treatment of said disorders, comprising administering to a mammal, including human in need of such treatment, a therapeutically effective amount of said compound.

  本发明涉及一种新的化合物，其化学式为(I)，作为自由碱或其药用可接受盐，在基本纯净和分离形式中存在，含有化合物(I)的药物组合物，以及将该活性化合物用于治疗，用于治疗与糖原合酶激酶-3相关紊乱有关的疾病，如阿尔茨海默病，以及治疗该类紊乱的方法，包括向需要该治疗的哺乳动物，包括人类，给予所述化合物的治疗有效量。
• NICOTINIC ACETYLCHOLINE RECEPTOR SUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES
  申请人：Mazurov Anatoly

  公开号：US20100081683A1

  公开（公告）日：2010-04-01

  Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteoraryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the a4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).

  本文公开了化合物、包括这些化合物的制药组合物的制备方法和使用方法。这些化合物是酰胺化合物，可以从某些杂环羧酸和某些二氮杂双环烷制备而成。这些化合物表现出选择性，并与中枢神经系统(CNS)的a4β2亚型的神经尼古丁受体结合亲和力高。这些化合物和组合物可用于治疗和/或预防各种疾病或疾病，特别是CNS疾病。这些化合物可以：（i）改变患者大脑尼古丁胆碱能受体的数量，（ii）表现出神经保护作用，（iii）当以有效量使用时，不会产生明显的不良副作用（例如显著增加血压和心率、对胃肠道产生显著负面影响以及对骨骼肌产生显著影响等副作用）。
• Imidazole Substituted Pyrimidines Useful in the Treatment of Glycogen Synthase Kinase-3 Related Disorders such as Alzheimer's Disease
  申请人：Burrows Jeremy Nicholas

  公开号：US20120077813A1

  公开（公告）日：2012-03-29

  The present invention relates to a new compound of formula (I) wherein R 1 is hydrogen or fluoro; R 2 and R 3 are independently selected from hydrogen or methyl; or a pharmaceutically acceptable salt thereof, pharmaceutical formulations containing said compound, to the use of said active compound in therapy, to the use for the treatment of conditions associated with glycogen synthase kinase-3 related disorders, such as Alzheimer's disease, as well as for the method of treatment of said disorders, comprising administering to a mammal, including human in need of such treatment, a therapeutically effective amount of said compound.

  本发明涉及一种新的化合物，其化学式为（I），其中R1是氢或氟；R2和R3分别选择氢或甲基；或其药学上可接受的盐，含有该化合物的制药配方，以及将该活性化合物用于治疗的用途，用于治疗与糖原合成酶激酶-3相关疾病有关的疾病，例如阿尔茨海默病，以及治疗该疾病的方法，包括向需要此类治疗的哺乳动物，包括人类，给予该化合物的治疗有效量。