8-(2-bromo-4-isopropyl-phenyl)-4-chloro-2-methyl-pyrrolo[1,2-a]pyrimidine-6-carbonitrile | 860016-44-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯
• 英文名称: 8-(2-bromo-4-isopropyl-phenyl)-4-chloro-2-methyl-pyrrolo[1,2-a]pyrimidine-6-carbonitrile
• 英文别名: 8-(2-bromo-4-propan-2-ylphenyl)-4-chloro-2-methylpyrrolo[1,2-a]pyrimidine-6-carbonitrile
• CAS: 860016-44-0
• 化学式: C₁₈H₁₅BrClN₃
• 分子量: 388.694
• InChiKey: CSMBHXJIAIQGDR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.6
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  41.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  8-(2-bromo-4-isopropyl-phenyl)-4-chloro-2-methyl-pyrrolo[1,2-a]pyrimidine-6-carbonitrile 、 4-氨基庚烷 在 N,N-二异丙基乙胺 作用下， 以 乙醇 为溶剂， 生成 8-(2-bromo-4-isopropyl-phenyl)-2-methyl-4-(1-propyl-butylamino)-pyrrolo[1,2-a]pyrimidine-6-carbonitrile
  参考文献：
  名称：

  [EN] TRIAZA-CYCLOPENTA[CD]INDENE DERIVATIVES
  [FR] DERIVES DE TRIAZA-CYCLOPENTA[CD]INDENE

  摘要：

  本发明的一个目标是提供一种针对CRF受体的拮抗剂，作为治疗或预防CRF参与的疾病的有效药物，如抑郁症、焦虑症、阿尔茨海默病、帕金森病、亨廷顿舞蹈症、进食障碍、高血压、胃肠疾病、药物依赖、癫痫、脑梗塞、脑缺血、脑水肿、头部外伤、炎症、免疫相关疾病、脱发、肠易激综合征、睡眠障碍、皮肤炎症、精神分裂症、疼痛等。以下式[I]所代表的三氮杂环戊二烯衍生物具有高亲和力对CRF受体，并对CRF参与的疾病有效。

  公开号：

  WO2005066178A1

文献信息

• Triaza-cyclopenta [cd] indene derivatives
  申请人：Nakazato Atsuro

  公开号：US20070060602A1

  公开（公告）日：2007-03-15

  An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, dermatitides, schizophrenia, pain, etc. A triaza-cyclopenta[cd]indene derivative represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

  本发明的目的是提供一种CRF受体拮抗剂，作为治疗或预防CRF参与的疾病的有效药物，如抑郁症、焦虑症、阿尔茨海默病、帕金森病、亨廷顿舞蹈症、进食障碍、高血压、胃肠疾病、药物依赖、癫痫、脑梗塞、脑缺血、脑水肿、头部外伤、炎症、免疫相关疾病、脱发、肠易激综合征、睡眠障碍、皮肤炎、精神分裂症、疼痛等。以下式[I]所表示的三氮杂环戊二烯[cd]吲哚衍生物具有高亲和力的CRF受体，并对CRF参与的疾病具有疗效。 [I]
• Triaza-cyclopenta[cd]indene derivatives
  申请人：Taisho Pharmaceutical Co., Ltd.

  公开号：US07365078B2

  公开（公告）日：2008-04-29

  An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, dermatitides, schizophrenia, pain, etc. A triaza-cyclopenta[cd]indene derivative represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved

  本发明的目的是提供一种针对CRF受体的拮抗剂，其作为治疗或预防药物对于CRF被认为参与的疾病如抑郁症、焦虑症、阿尔茨海默病、帕金森病、亨廷顿舞蹈症、进食障碍、高血压、胃肠疾病、药物依赖、癫痫、脑梗塞、脑缺血、脑水肿、头部外伤、炎症、免疫相关疾病、脱发、肠易激综合征、睡眠障碍、皮肤炎、精神分裂症、疼痛等疾病具有高效性。以下式[I]所表示的三氮杂-环戊二烯并[cd]吲哚衍生物具有对CRF受体的高亲和力，对于CRF被认为参与的疾病具有高效性。
• TRIAZA-CYCLOPENTA[CD]INDENE DERIVATIVES
  申请人：TAISHO PHARMACEUTICAL CO., LTD

  公开号：EP1704149B1

  公开（公告）日：2007-03-07
• US7365078B2
  申请人：——

  公开号：US7365078B2

  公开（公告）日：2008-04-29
• [EN] TRIAZA-CYCLOPENTA[CD]INDENE DERIVATIVES<br/>[FR] DERIVES DE TRIAZA-CYCLOPENTA[CD]INDENE
  申请人：TAISHO PHARMA CO LTD

  公开号：WO2005066178A1

  公开（公告）日：2005-07-21

  An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, dermatitides, schizophrenia, pain, etc. A triaza-cyclopenta[cd]indene derivative represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

  本发明的一个目标是提供一种针对CRF受体的拮抗剂，作为治疗或预防CRF参与的疾病的有效药物，如抑郁症、焦虑症、阿尔茨海默病、帕金森病、亨廷顿舞蹈症、进食障碍、高血压、胃肠疾病、药物依赖、癫痫、脑梗塞、脑缺血、脑水肿、头部外伤、炎症、免疫相关疾病、脱发、肠易激综合征、睡眠障碍、皮肤炎症、精神分裂症、疼痛等。以下式[I]所代表的三氮杂环戊二烯衍生物具有高亲和力对CRF受体，并对CRF参与的疾病有效。