4-(aminomethyl)tetrahydro-2H-pyran-4-carboxamide | 1030364-98-7

• 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: 4-(aminomethyl)tetrahydro-2H-pyran-4-carboxamide
• 英文别名: 4-(aminomethyl)oxane-4-carboxamide
• CAS: 1030364-98-7
• 化学式: C₇H₁₄N₂O₂
• mdl: MFCD11099461
• 分子量: 158.2
• InChiKey: XXPGVMATNNHWMS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.857
• 拓扑面积：
  78.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-(aminomethyl)tetrahydro-2H-pyran-4-carboxamide 在 4-二甲氨基吡啶 、 伯吉斯试剂 作用下， 以 四氢呋喃 、 N-甲基吡咯烷酮 、 二氯甲烷 、 乙腈 为溶剂， 反应 21.0h， 生成 4-(aminomethyl)tetrahydro-2H-pyran-4-carbonitrile trifluoroacetic acid salt
  参考文献：
  名称：

  US2014/275082

  摘要：

  公开号：

文献信息

• [EN] PYRROLO CARBOXAMIDES AS MODULATORS OF ORPHAN NUCLEAR RECEPTOR RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORϒ, NR1F3) ACTIVITY AND FOR THE TREATMENT OF CHRONIC INFLAMMATORY AND AUTOIMMUNE DISEASES<br/>[FR] PYRROLOCARBOXAMIDES EN TANT QUE MODULATEURS DE L'ACTIVITÉ D'UN RÉCEPTEUR ORPHELIN GAMMA (RORϒ, NR1F3) APPARENTÉ AU RÉCEPTEUR NUCLÉAIRE ORPHELIN RAR ET DESTINÉS AU TRAITEMENT DE MALADIES INFLAMMATOIRES CHRONIQUES ET AUTO-IMMUNES
  申请人：PHENEX PHARMACEUTICALS AG

  公开号：WO2013079223A1

  公开（公告）日：2013-06-06

  The invention provides modulators for the orphan nuclear receptor RORϒ and methods for treating RORϒ mediated diseases by administrating these novel RORϒ modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.

  本发明提供了针对孤儿核受体RORϒ的调节剂，以及通过向需要的人或哺乳动物施用这些新型RORϒ调节剂来治疗RORϒ介导的疾病的方法。具体而言，本发明提供了式(1)的吡咯甲酰胺化合物及其对映体、非对映体、N-氧化物、互变异构体、溶剂化物和药用可接受的盐。
• Substituted Dihydroimidazoles and their Use in the Treatment of Tumors
  申请人：Chamoin Sylvie

  公开号：US20100075966A1

  公开（公告）日：2010-03-25

  The invention relates to dihydroimidazoles of formula rac-(I), wherein the radicals and symbols are as defined herein; their use as inhibitors of the interaction of the MDM2 protein with a p53-like peptide, new pharmaceutical formulations comprising said compounds, said compounds for use in the therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of proliferative diseases or for the manufacture of pharmaceutical formulations useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide, a pharmaceutical formulation e.g. useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide comprising said compound, methods of treatment comprising administration of said compounds to a warm-blooded animal, and/or processes for the manufacture of said compounds.

  该发明涉及式rac-(I)的二氢咪唑，其中基团和符号如本文所定义；它们作为MDM2蛋白与类p53肽的相互作用抑制剂的用途，包括所述化合物的新药物配方，所述化合物用于治疗温血动物，特别是人类，它们用于治疗增殖性疾病或用于制造对MDM2蛋白与类p53肽相互作用调节有响应的药物配方，例如用于治疗对MDM2蛋白与类p53肽相互作用调节有响应的增殖性疾病的药物配方，包括所述化合物，包括所述化合物的治疗方法，包括将所述化合物用于温血动物的给药，和/或所述化合物的制造方法。
• CARBOXAMIDE OR SULFONAMIDE SUBSTITUTED THIAZOLES AND RELATED DERIVATIVES AS MODULATORS FOR THE ORPHAN NUCLEAR RECEPTOR ROR[GAMMA]
  申请人：Phenex Pharmaceuticals AG

  公开号：US20150175562A1

  公开（公告）日：2015-06-25

  The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide or sulfonamide containing cyclic compounds of Formula (1), (1′), (100), (100′), (200) and (200′) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof.

  本发明提供了用于孤儿核受体RORy的调节剂，并通过向需要治疗RORy介导的疾病的人类或哺乳动物注射这些新型RORy调节剂的方法。具体而言，本发明提供了公式（1）、（1'）、（100）、（100'）、（200）和（200'）的含有羧酰胺或磺酰胺的环状化合物及其对映异构体、互异构体、互变异构体、/V-氧化物、溶剂化物和药学上可接受的盐。
• PYRROLO CARBOXAMIDES AS MODULATORS OF ORPHAN NUCLEAR RECEPTOR RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORy, NR1F3) ACTIVITY AND FOR THE TREATMENT OF CHRONIC INFLAMMATORY AND AUTOIMMUNE DISEASES
  申请人：PHENEX PHARMACEUTICALS AG

  公开号：US20140349987A1

  公开（公告）日：2014-11-27

  The invention provides modulators for the orphan nuclear receptor ROR γ and methods for treating ROR γ mediated diseases by administrating these novel ROR γ modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.

  该发明提供了用于孤儿核受体RORγ的调节剂，并通过向需要此类治疗的人或哺乳动物中施用这些新型RORγ调节剂的方法来治疗RORγ介导的疾病。具体而言，本发明提供了公式（1）的吡咯羧酰胺化合物及其对映体、二对映异构体、N-氧化物、互变异构体、溶剂化物和药学上可接受的盐。
• CARBOXAMIDE OR SULFONAMIDE SUBSTITUTED NITROGEN-CONTAINING 5-MEMBERED HETEROCYCLES AS MODULATORS FOR THE ORPHAN NUCLEAR RECEPTOR ROR GAMMA
  申请人：PHENEX PHARMACEUTICALS AG

  公开号：US20150344423A1

  公开（公告）日：2015-12-03

  The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide containing cyclic compounds of Formula (1) to Formula (5) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof.

  本发明提供了用于孤儿核受体RORy的调节剂，并通过向需要治疗RORy介导的疾病的人类或哺乳动物施用这些新型RORy调节剂来治疗这些疾病的方法。具体而言，本发明提供了公式（1）至公式（5）的含有羧酰胺的环状化合物及其对映体、二对映异构体、互变异构体、/V-氧化物、溶剂化物和药学上可接受的盐。