tert-butyl 4-(3-nitro-4-fluorophenyl)-3,6-dihydro-1(2H)-pyridine carboxylate | 643746-91-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: tert-butyl 4-(3-nitro-4-fluorophenyl)-3,6-dihydro-1(2H)-pyridine carboxylate
• 英文别名: tert-butyl 4-(5-nitro-4-fluorophenyl)-3,6-dihydro-1(2H)-pyridine carboxylate；tert-butyl 4-(4-fluoro-3-nitrophenyl)-3,6-dihydro-1(2H)-pyridinecarboxylate；tert-butyl 4-(4-fluoro-3-nitrophenyl)-3,6-dihydro-2H-pyridine-1-carboxylate
• CAS: 643746-91-2
• 化学式: C₁₆H₁₉FN₂O₄
• 分子量: 322.336
• InChiKey: MPMVXQFLIHGFHO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  75.4
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  tert-butyl 4-(3-nitro-4-fluorophenyl)-3,6-dihydro-1(2H)-pyridine carboxylate 在 盐酸 、 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 、 1,4-二氧六环 为溶剂， 反应 21.0h， 生成 2-Methyl-1-[2-nitro-4-(1,2,3,6-tetrahydropyridin-4-yl)anilino]propan-2-ol
  参考文献：
  名称：

  [EN] NEW BENZIMIDAZOLE COMPOUNDS AND DERIVATIVES AS EGFR INHIBITORS
  [FR] NOUVEAUX COMPOSÉS DE BENZIMIDAZOLE ET LEURS DÉRIVÉS EN TANT QU'INHIBITEURS D'EGFR

  摘要：

  本发明涵盖了式（I）（I）的化合物，其中基团R1至R5具有权利要求和说明书中给出的含义，它们作为突变EGFR的抑制剂的用途，含有这种化合物的药物组合物以及它们作为药物/医用品的用途，特别是作为治疗和/或预防肿瘤疾病的药剂。

  公开号：

  WO2019162323A1
• 作为产物：
  描述：

  4-溴-1-氟-2-硝基苯 、 N-Boc-1,2,5,6-四氢吡啶-4-硼酸频哪醇酯 在 1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物 、 sodium carbonate 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 16.0h， 以91%的产率得到tert-butyl 4-(3-nitro-4-fluorophenyl)-3,6-dihydro-1(2H)-pyridine carboxylate
  参考文献：
  名称：

  [EN] NEW BENZIMIDAZOLE COMPOUNDS AND DERIVATIVES AS EGFR INHIBITORS
  [FR] NOUVEAUX COMPOSÉS DE BENZIMIDAZOLE ET LEURS DÉRIVÉS EN TANT QU'INHIBITEURS D'EGFR

  摘要：

  本发明涵盖了式（I）（I）的化合物，其中基团R1至R5具有权利要求和说明书中给出的含义，它们作为突变EGFR的抑制剂的用途，含有这种化合物的药物组合物以及它们作为药物/医用品的用途，特别是作为治疗和/或预防肿瘤疾病的药剂。

  公开号：

  WO2019162323A1

文献信息

• [EN] SECONDARY AMINO ANILINIC PIPERIDINES AS MCH1 ANTAGONISTS AND USES THEREOF<br/>[FR] PIPERIDINES AMINOANILINIQUES SECONDAIRES UTILISEES COMME ANTAGONISTES DE LA MCH1 ET UTILISATIONS CORRESPONDANTES
  申请人：SYNAPTIC PHARMACEUTICAL CORPOR

  公开号：WO2004005257A1

  公开（公告）日：2004-01-15

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compounds of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject=s depression and/or anxiety. This invention further provides a method of treating a subject suffering from a urinary disorder.

  本发明涉及对黑素集中激素-1（MCH1）受体具有选择性的拮抗剂化合物。该发明提供了一种含有治疗有效量的本发明化合物和药用辅料的药物组合物。本发明还提供了一种通过结合治疗有效量的本发明化合物和药用辅料制成的药物组合物。本发明进一步提供了一种制作含有治疗有效量的本发明化合物和药用辅料的药物组合物的方法。本发明还提供了一种减少主体体质量的方法，包括向主体施用有效减少主体体质量的本发明化合物的量。本发明还提供了一种治疗患有抑郁和/或焦虑的主体方法，包括向主体施用有效治疗主体的抑郁和/或焦虑的本发明化合物的量。本发明还提供了一种治疗患有尿路障碍的主体方法。
• Secondary amino anilinic piperidines as mch1 antagonists and uses thereof
  申请人：Marzabadi R. Mohammad

  公开号：US20050245743A1

  公开（公告）日：2005-11-03

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compounds of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject=s depression and/or anxiety. This invention further provides a method of treating a subject suffering from a urinary disorder.

  本发明涉及一种选择性抗黑色素浓集激素-1（MCH1）受体的化合物。本发明提供一种药物组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明提供一种由本发明化合物的治疗有效量和药学上可接受的载体组成的药物组合物。本发明还提供一种制备药物组合物的方法，包括将本发明化合物的治疗有效量和药学上可接受的载体组合。本发明还提供一种减轻受试者体重的方法，包括向受试者投予本发明化合物的有效量以减轻受试者的体重。本发明还提供一种治疗患有抑郁症和/或焦虑症的受试者的方法，包括向受试者投予本发明化合物的有效量以治疗受试者的抑郁症和/或焦虑症。本发明还提供一种治疗患有泌尿系统疾病的受试者的方法。
• Secondary amino anilinic piperidines as MCH1 antagonists and uses thereof
  申请人：H. Lunbeck A/S

  公开号：US07473698B2

  公开（公告）日：2009-01-06

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compounds of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject=s depression and/or anxiety. This invention further provides a method of treating a subject suffering from a urinary disorder.

  该发明涉及选择性拮抗黑色素浓集激素-1（MCH1）受体的化合物。该发明提供了一种制药组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。该发明提供了一种制药组合物的制备方法，包括将本发明化合物的治疗有效量和药学上可接受的载体结合。该发明还提供了一种减少受试者体重的方法，包括向受试者施用本发明化合物的有效量以减少受试者的体重。该发明还提供了一种治疗患有抑郁症和/或焦虑症的受试者的方法，包括向受试者施用本发明化合物的有效量以治疗受试者的抑郁症和/或焦虑症。该发明还提供了一种治疗患有尿液障碍的受试者的方法。
• US7473698B2
  申请人：——

  公开号：US7473698B2

  公开（公告）日：2009-01-06
• [EN] NEW BENZIMIDAZOLE COMPOUNDS AND DERIVATIVES AS EGFR INHIBITORS<br/>[FR] NOUVEAUX COMPOSÉS DE BENZIMIDAZOLE ET LEURS DÉRIVÉS EN TANT QU'INHIBITEURS D'EGFR
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2019162323A1

  公开（公告）日：2019-08-29

  The present invention encompasses compounds of formula (I) (I), wherein the groups R1 to R5 have the meanings given in the claims and specification, their use as inhibitors of mutant EGFR, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

  本发明涵盖了式（I）（I）的化合物，其中基团R1至R5具有权利要求和说明书中给出的含义，它们作为突变EGFR的抑制剂的用途，含有这种化合物的药物组合物以及它们作为药物/医用品的用途，特别是作为治疗和/或预防肿瘤疾病的药剂。