7-chloro-2-(4-fluorophenyl)-oxazolo[5,4-d]pyrimidine | 1245318-90-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 7-chloro-2-(4-fluorophenyl)-oxazolo[5,4-d]pyrimidine
• 英文别名: 7-Chloro-2-(4-fluorophenyl)-oxazolo[5,4-d]pyrimidine；7-chloro-2-(4-fluorophenyl)-[1,3]oxazolo[5,4-d]pyrimidine
• CAS: 1245318-90-4
• 化学式: C₁₁H₅ClFN₃O
• 分子量: 249.632
• InChiKey: AGYOZBYXOFNBJJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  51.8
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  7-chloro-2-(4-fluorophenyl)-oxazolo[5,4-d]pyrimidine 、 3-氯-4-氟苯胺 在 crude residue 、 silica gel 、 methanol-dichloromethane 作用下， 以 Tert-butyl alcohol 1,2-dichloroethane 为溶剂， 反应 24.0h， 以to yield the title compound as a white solid (0.1 g, 82%)的产率得到N-(3-chloro-4-fluorophenyl)-2-(4-fluorophenyl)-oxazolo[5,4-d]pyrimidin-7-amine
  参考文献：
  名称：

  THIAZOLOPYRIMIDINE MODULATORS AS IMMUNOSUPPRESSIVE AGENTS

  摘要：

  本发明涉及公式I、II、III或IV的化合物，以及/或其药学上可接受的盐和/或其立体异构体和/或其溶剂化物，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、R11和R12如权利要求书所定义。本发明还涉及它们的制备方法，以及它们的药物组合物。本发明进一步涉及将所述化合物用作生物活性成分，更具体地用作治疗障碍和病理状况的药物，例如免疫和自身免疫障碍、器官和细胞移植排斥等。

  公开号：

  US20120046278A1
• 作为产物：
  描述：

  N-(4,6-dihydroxypyrimidin-5-yl)-4-fluorobenzamide 在 N,N-二异丙基乙胺 、 三氯氧磷 作用下， 反应 3.5h， 以30%的产率得到7-chloro-2-(4-fluorophenyl)-oxazolo[5,4-d]pyrimidine
  参考文献：
  名称：

  ANTI-CANCER ACTIVITY OF NOVEL BICYCLIC HETEROCYCLES

  摘要：

  本发明涉及式I、II、III或IV的化合物，和/或其药用可接受的加合物盐和/或其立体异构体和/或其溶剂化合物，式(I)、(II)、(III)和(IV)中R1、R2、R3、R4、R5、R6、R7、R8、R9、R11和R12如权利要求书中所定义或在发明说明书中详细描述的那样，以及使用所述化合物来治疗或预防增殖性疾病以及用于制造治疗或预防增殖性疾病的药物，特别是像白血病这样的癌症。本发明还涉及所述化合物的药物组合物以及使用所述药物组合物来治疗或预防增殖性疾病。本发明还涉及将所述化合物用作生物活性成分，更具体地用作治疗增殖性疾病和病理状况的药物，例如癌症如白血病等。

  公开号：

  US20140088088A1

文献信息

• THIAZOLOPYRIMIDINE MODULATORS AS IMMUNOSUPPRESSIVE AGENTS
  申请人：Herdewijn Piet

  公开号：US20120046278A1

  公开（公告）日：2012-02-23

  The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 11 , and R 12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.

  本发明涉及式I、II、III或IV的化合物，及/或其药用可接受的加合盐和/或其立体异构体和/或其溶剂化合物，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、R11和R12如权利要求1所定义。本发明还涉及它们的制备方法，以及其药物组合物。本发明进一步涉及所述化合物作为生物活性成分的用途，更具体地作为治疗疾病和病理状况的药物，例如但不限于免疫和自身免疫性疾病、器官和细胞移植排斥反应。
• Thiazolopyrimidine modulators as immunosuppressive agents
  申请人：Herdewijn Piet

  公开号：US08901132B2

  公开（公告）日：2014-12-02

  The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.

  本发明涉及式I、II、III或IV的化合物及/或其药学可接受的加合物盐和/或其立体异构体和/或其溶剂化物，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、R11和R12如权利要求1所定义。本发明还涉及它们的制备方法，以及它们的药物组合物。本发明还涉及将所述化合物用作生物活性成分，更具体地用作治疗障碍和病理状况的药物，例如，但不限于，免疫和自身免疫性疾病，器官和细胞移植排斥反应。
• Thiazolopyrimidine Modulators as Immunosuppressive Agents
  申请人：Herdewijn Piet

  公开号：US20150038494A1

  公开（公告）日：2015-02-05

  The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 11 , and R 12 are as defined in the claim 1 . The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.

  本发明涉及公式I，II，III或IV的化合物，以及/或其药学上可接受的加成盐和/或其立体异构体和/或其溶剂化物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R11和R12如权利要求1所定义。本发明还涉及它们的制备方法，以及其药物组合物。本发明还涉及所述化合物作为生物活性成分的用途，更具体地作为治疗疾病和病理状态的药物，例如，但不限于，免疫和自身免疫性疾病，器官和细胞移植排斥。
• Antiviral activity of bicyclic heterocycles
  申请人：De Jonghe Steven

  公开号：US09193741B2

  公开（公告）日：2015-11-24

  The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of viral disorders and pathologic conditions such as, but not limited to, viral infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.

  本发明涉及公式I、II、III或IV的化合物及/或其药学上可接受的加盐物和/或立体异构体和/或溶剂化物，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、R11和R12在权利要求书中定义或在本发明说明书中详细描述，以及使用所述化合物治疗或预防病毒感染，并将其用于制造治疗或预防病毒感染的药物，特别是RNA病毒家族中属于逆转录病毒科、黄病毒科和小肠病毒科的病毒感染，更好地是人类免疫缺陷病毒1（HIV1）、人类免疫缺陷病毒2（HIV2）、丙型肝炎病毒（HCV）、登革病毒和柯萨奇病毒、鼻病毒和脊髓灰质炎病毒等肠病毒感染。本发明还涉及所述化合物的药物组合物以及使用所述药物组合物治疗或预防病毒感染的用途。本发明还涉及将所述化合物用作生物活性成分，更具体地用作治疗病毒性疾病和病理状况的药物，例如但不限于人类免疫缺陷病毒1（HIV1）、人类免疫缺陷病毒2（HIV2）、丙型肝炎病毒（HCV）、登革病毒和柯萨奇病毒、鼻病毒和脊髓灰质炎病毒等病毒感染。
• Purine analogues and their use as immunosuppressive agents
  申请人：Katholieke Universiteit Leuven, K.U. Leuven R&D

  公开号：EP2923734A1

  公开（公告）日：2015-09-30

  The present invention relates to a compound of formula III or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R7, R8, R9, R11 and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.

  本发明涉及一种式 III 或式 IV 的化合物，和/或其药物可接受的加成盐和/或其立体异构体和/或其溶液、 其中 R7、R8、R9、R11 和 R12 如权利要求 1 所定义。 本发明还涉及其制备方法及其药物组合物。本发明还涉及上述化合物作为生物活性成分的用途，更具体地说是作为治疗紊乱和病理状况的药物，例如但不限于免疫和自身免疫紊乱、器官和细胞移植排斥。