1-[5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazol-3-yl]-2-phenylethanone | 1047670-34-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-[5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazol-3-yl]-2-phenylethanone
• CAS: 1047670-34-7
• 化学式: C₂₄H₁₇Cl₃N₂O
• 分子量: 455.771
• InChiKey: GTXRPIMCNZXFIC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.4
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  34.9
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  N-methoxy-N-methyl-1-(2,4-dichlorophenyl)-5-(4-chlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide 、 溴甲苯 在 magnesium 作用下， 以 四氢呋喃 为溶剂， 生成 1-[5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazol-3-yl]-2-phenylethanone
  参考文献：
  名称：

  WO2008/99139

  摘要：

  公开号：

文献信息

• [EN] 1,5-DIARYL-PYRAZOLES AND THEIR USE AS CANNABINOID RECEPTOR NEUTRAL ANTAGONISTS<br/>[FR] 1,5-DIARYL-PYRAZOLES ET LEUR UTILISATION COMME ANTAGONISTES NEUTRES DES RÉCEPTEURS CANNABINOÏDES
  申请人：UNIV ABERDEEN

  公开号：WO2010020762A1

  公开（公告）日：2010-02-25

  The present invention pertains to cannabinoid (CB) receptor and cannabinoid-like receptor neutral antagonists, and especially CB1 neutral antagonists of Formula (I). The present invention also pertains to these compounds for use in the treatment of diseases and disorders that are ameliorated by treatment with a neutral antagonist of the cannabinoid type 1 (CB1) receptor or a non-CB1/non-CB2 cannabinoid-like receptor, for example: an eating disorder; obesity; cardiovascular disease; a disease or disorder characterised by an addiction component; addiction; withdrawal; smoking addiction; smoking withdrawal; drug addiction; drug withdrawal; smoking cessation therapy; a bone disease or disorder; osteoporosis, Paget' s disease of bone; bone related cancer; breast cancer; breast cancer metastases; breast cancer which has metastasised to bone; cancer associated with activation or inactivation of a non-CB1/non-CB2 cannabinoid-like receptor,

  本发明涉及大麻素（CB）受体和类大麻素受体中和拮抗剂，特别是公式（I）的CB1中和拮抗剂。本发明还涉及这些化合物在治疗通过使用大麻素类型1（CB1）受体的中和拮抗剂或非CB1/非CB2类大麻素受体得到改善的疾病和疾病的使用，例如：进食障碍；肥胖；心血管疾病；由成瘾成分特征的疾病或障碍；成瘾；戒断；吸烟成瘾；戒烟；药物成瘾；戒毒；戒烟疗法；骨骼疾病或障碍；骨质疏松症，Paget骨病；与激活或失活非CB1/非CB2类大麻素受体相关的癌症。
• 1,5-Diaryl-Pyrazoles As Cannabinoid Receptor Neutral Antagonists Useful As Therapeutic Agents
  申请人：Greig Iain Robert

  公开号：US20100022611A1

  公开（公告）日：2010-01-28

  The present invention pertains to cannabinoid (CB) receptor neutral antagonists, and especially CB1 neutral antagonists, and including, for example, certain 1,5 -di-aryl-pyrazole compounds. The present invention also pertains to the use of such compounds in the treatment of diseases and disorders that are ameliorated by treatment with a neutral antagonist of the cannabinoid type 1 (CB1) receptor, for example: an eating disorder; obesity; a disease or disorder characterised by an addiction component; addiction; withdrawal; smoking addiction; smoking withdrawal; drug addiction; drug withdrawal; smoking cessation therapy; a bone disease or disorder; osteoporosis, Paget's disease of bone; bone related cancer; a disease or disorder with an inflammatory or autoimmune component; rheumatoid arthritis; inflammatory bowel disease; psoriasis; a psychiatric disease or disorder; anxiety; mania; schizophrenia; a disease or disorder characterised by impairment of memory and/or loss of cognitive function; memory impairment; loss of cognitive function; Parkinson's disease; Alzheimer's disease; dementia; a cardiovascular disease or disorder; congestive heart failure; cardiac hypertrophy; and myocardial infarction.

  本发明涉及大麻素（CB）受体中和拮抗剂，特别是CB1中和拮抗剂，包括例如某些1,5-二芳基吡唑化合物。本发明还涉及使用这些化合物治疗通过与大麻素类型1（CB1）受体的中和拮抗剂治疗改善的疾病和疾病，例如：进食障碍；肥胖症；以成瘾成分为特征的疾病或疾病；成瘾；戒断；吸烟成瘾；戒烟；药物成瘾；药物戒断；戒烟疗法；骨疾病或疾病；骨质疏松症，骨的帕吉特病；与骨有关的癌症；具有炎症或自身免疫成分的疾病或疾病；类风湿性关节炎；炎症性肠病；牛皮癣；精神疾病或疾病；焦虑症；狂躁症；精神分裂症；以记忆受损和/或认知功能丧失为特征的疾病或疾病；记忆障碍；认知功能丧失；帕金森病；阿尔茨海默病；痴呆；心血管疾病或疾病；充血性心力衰竭；心脏肥大；心肌梗塞。
• [EN] 1,5-DIARYL-PYRAZOLES AS CANNABINOID RECEPTOR NEUTRAL ANTAGONISTS USEFUL AS THERAPEUTIC AGENTS<br/>[FR] 1,5-DIARYL-PYRAZOLES COMME ANTAGONISTES NEUTRES DES RÉCEPTEURS CANNABINOÏDES, UTILES COMME AGENTS THÉRAPEUTIQUES
  申请人：UNIV ABERDEEN

  公开号：WO2008099139A1

  公开（公告）日：2008-08-21

  [EN] The present invention pertains to cannabinoid (CB) receptor neutral antagonists, and especially CB1 neutral antagonists, and including, for example, certain 1,5-di-aryl-pyrazole compounds. The present invention also pertains to the use of such compounds in the treatment of diseases and disorders that are ameliorated by treatment with a neutral antagonist of the cannabinoid type 1 (CB1) receptor, for example: an eating disorder; obesity; a disease or disorder characterised by an addiction component; addiction; withdrawal; smoking addiction; smoking withdrawal; drug addiction; drug withdrawal; smoking cessation therapy; a bone disease or disorder; osteoporosis, Paget's disease of bone; bone related cancer; a disease or disorder with an inflammatory or autoimmune component; rheumatoid arthritis; inflammatory bowel disease; psoriasis; a psychiatric disease or disorder; anxiety; mania; schizophrenia; a disease or disorder characterised by impairment of memory and/or loss of cognitive function; memory impairment; loss of cognitive function; Parkinson's disease; Alzheimer's disease; dementia; a cardiovascular disease or disorder; congestive heart failure; cardiac hypertrophy; and myocardial infarction.
  [FR] La présente invention porte sur des antagonistes neutres des récepteurs cannabinoïdes (CB) et, en particulier, sur des antagonistes neutre des CB1, et comprenant, par exemple, certains composés 1,5-di-aryl-pyrazoles. La présente invention porte également sur l'utilisation de tels composés dans le traitement de maladies et troubles qui sont améliorés par le traitement par un antagoniste neutre des récepteurs cannabinoïdes de type 1 (CB1), par exemple : un trouble de l'alimentation ; l'obésité ; une maladie ou un trouble caractérisé par un composant d'addiction ; l'addiction ; le sevrage ; l'addiction à la cigarette ; le sevrage de la cigarette ; l'addiction aux médicaments ; le sevrage des médicaments ; la thérapie de cessation de fumer ; une maladie ou un trouble osseux ; l'ostéoporose ; la maladie de Paget de l'os ; le cancer apparenté à l'os ; une maladie ou un trouble avec un composant inflammatoire ou auto-immun ; l'arthrite rhumatoïde ; la maladie inflammatoire de l'intestin ; le psoriasis, une maladie ou un trouble psychiatrique ; l'anxiété ; la manie ; la schizophrénie ; une maladie ou un trouble caractérisé par l'affectation de la mémoire et/ou la perte de la fonction cognitive ; l'affectation de la mémoire ; la perte de fonction cognitive ; la maladie de Parkinson ; la maladie d'Alzheimer ; la démence ; une maladie ou un trouble cardiovasculaire ; la maladie cardiaque congestive ; l'hypertrophie cardiaque ; et l'infarctus du myocarde.
• WO2008/99139
  申请人：——

  公开号：——

  公开（公告）日：——