3,4-dichloro-N-(((3S,5S)-1-(3,5-dichlorobenzyl)-2-oxo-3-(piperidin-1-ylmethyl)-1,4-diazepan-5-yl)methyl)benzamide | 1185653-09-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 3,4-dichloro-N-(((3S,5S)-1-(3,5-dichlorobenzyl)-2-oxo-3-(piperidin-1-ylmethyl)-1,4-diazepan-5-yl)methyl)benzamide
• 英文别名: 3,4-dichloro-N-[[(3S,5S)-1-[(3,5-dichlorophenyl)methyl]-2-oxo-3-(piperidin-1-ylmethyl)-1,4-diazepan-5-yl]methyl]benzamide
• CAS: 1185653-09-1
• 化学式: C₂₆H₃₀Cl₄N₄O₂
• 分子量: 572.362
• InChiKey: BEJFVMYSYMLGCF-URXFXBBRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  36
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  64.7
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] METHODS OF MODULATING THE ACTIVITY OF THE MC1 RECEPTOR AND TREATMENT OF CONDITIONS RELATED TO THIS RECEPTOR<br/>[FR] PROCÉDÉ DE MODULATION DE L'ACTIVITÉ DU RÉCEPTEUR MC1 ET TRAITEMENT DES CONDITIONS ASSOCIÉES AU DIT RÉCEPTEUR
  申请人：MIMETICA PTY LTD

  公开号：WO2010096853A1

  公开（公告）日：2010-09-02

  The present invention provides compounds of Formula (I) that are useful for binding and/or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC1R is beneficial. Such diseases and/or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain.

  本发明提供了一种具有式（I）的化合物，该化合物对结合和/或调节黑色素皮质素-1受体（MC1R）的生物活性是有用的。本发明的化合物可用于治疗调节MC1R有益的疾病和/或症状。这些疾病和/或症状包括但不限于，色素沉着过多（包括雀斑），色素沉着不足（包括白癜风），黑色素瘤，基底细胞癌，鳞状细胞癌，红细胞生成性原卟啉症，多形性光疹，太阳性荨麻疹，光敏性，晒伤，炎症性疾病，异常成纤维细胞活动和疼痛。
• [EN] METHODS OF MODULATING THE ACTIVITY OF THE MC3 AND/OR MC4 RECEPTORS AND TREATMENT OF CONDITIONS RELATED TO THESE RECEPTORS<br/>[FR] PROCÉDÉS DE MODULATION DE L'ACTIVITÉ DES RÉCEPTEURS MC3 ET/OU MC4 ET TRAITEMENT DES CONDITIONS ASSOCIÉES AUX DITS RÉCEPTEURS
  申请人：MIMETICA PTY LTD

  公开号：WO2010096854A1

  公开（公告）日：2010-09-02

  The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-3 receptor (MC3R) and / or the melanocortin-4 receptor (MC4R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC3R and / or MC4R is beneficial. Such diseases and/or conditions include, but are not limited to, obesity, eating disorders (such as cachexia, anorexia, weight gain, weight loss), metabolic syndrome, diabetes, sexual dysfunction (such as erectile dysfunction and female sexual dysfunction), anxiety, depression, inflammation, addiction and alcohol intake.

  本发明提供了一种化合物，其化学式为（I），可用于调节黑色素皮质素-3受体（MC3R）和/或黑色素皮质素-4受体（MC4R）的生物活性。本发明的化合物可用于治疗调节MC3R和/或MC4R有益的疾病和/或症状。这些疾病和/或症状包括但不限于肥胖、进食障碍（如虚弱、厌食、体重增加、体重减少）、代谢综合征、糖尿病、性功能障碍（如勃起功能障碍和女性性功能障碍）、焦虑、抑郁、炎症、成瘾和饮酒。
• METHODS OF MODULATING THE ACTIVITY OF THE MC1 RECEPTOR AND TREATMENT OF CONDITIONS RELATED TO THIS RECEPTOR
  申请人：Blaskovich Mark Arnold Thomas

  公开号：US20120141392A1

  公开（公告）日：2012-06-07

  The present invention provides compounds of Formula (I) that are useful for binding and/or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC1R is beneficial. Such diseases and/or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain.

  本发明提供了一种化合物，其化学式为（I），可用于结合和/或调节黑色素皮质激素受体（MC1R）的生物活性。本发明的化合物可用于治疗调节MC1R有益的疾病和/或症状。这些疾病和/或症状包括但不限于，色素沉着过多（包括雀斑），色素沉着不足（包括白癜风），黑色素瘤，基底细胞癌，鳞状细胞癌，红细胞生成性原卟啉症，多形性光疹，太阳性荨麻疹，光敏性，晒伤，炎症性疾病，异常成纤维细胞活性和疼痛。
• 3-AMINOALKYL-1,4-DIAZEPAN-2-ONE MELANOCORTIN-5 RECEPTOR ANTAGONISTS
  申请人：Blaskovich Mark Arnold Thomas

  公开号：US20090221557A1

  公开（公告）日：2009-09-03

  The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases.

  本发明提供了一种公式（I）的化合物，该化合物对调节黑色素皮质素-5受体（MC5R）的生物活性有用。本发明的化合物可用于治疗下调MC5R有益的疾病和/或症状。这些疾病和/或症状包括但不限于痤疮、脂溢性皮炎、皮肤癌和炎症性疾病。
• METHODS OF MODULATING THE ACTIVITY OF THE MC5 RECEPTOR AND TREATMENT OF CONDITIONS RELATED TO THIS RECEPTOR
  申请人：Blaskovich Mark Arnold Thomas

  公开号：US20090221558A1

  公开（公告）日：2009-09-03

  The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases.

  本发明提供的I式化合物可用于调节黑色素细胞激素5受体（MC5R）的生物活性。本发明的化合物可用于治疗下调MC5R有益的疾病和/或病况。此类疾病和/或病况包括但不限于痤疮、皮脂溢出、脂溢性皮炎、癌症和炎症性疾病。