N,N-diethyl-4-(3-hydroxylphenyl-piperidin-4-ylidene-methyl)-benzamide | 364757-38-0

• 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: N,N-diethyl-4-(3-hydroxylphenyl-piperidin-4-ylidene-methyl)-benzamide
• 英文别名: N,N-diethyl-4-[(3-hydroxyphenyl)-piperidin-4-ylidenemethyl]benzamide
• CAS: 364757-38-0
• 化学式: C₂₃H₂₈N₂O₂
• 分子量: 364.488
• InChiKey: KPXQZCSYNPWFFY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  52.6
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• Hydroxyphenyl-piperidin-4-ylidene-methyl-benzamide derivatives for the treatment of pain
  申请人：——

  公开号：US20030187022A1

  公开（公告）日：2003-10-02

  Compounds of general formula I 1 R 1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, triazolyl and thiazolyl; where each R 1 phenyl ring and R 1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C 1 -C 6 alkyl, NO 2 , CF 3 , C 1 -C 6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

  通式I1R1的化合物中，R1可选择自苯基、吡啶基、噻吩基、呋喃基、咪唑基、三唑基和噻唑基中的任意一种；其中每个R1苯环和R1杂环环可能选择性地且独立地进一步被1、2或3个取代基所取代，所选取代基可为直链和支链的C1-C6烷基、NO2、CF3、C1-C6烷氧基、氯、氟、溴和碘。苯环和杂环环上的取代作用可以发生在所述环系统的任何位置；本申请中披露和声称了这些化合物，以及包含这些新化合物的盐和药物组合物，以及它们在治疗中的应用，特别是在疼痛管理中。
• 4-(Phenyl-piperidin-4-ylidene-methyl)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders
  申请人：——

  公开号：US20040142967A1

  公开（公告）日：2004-07-22

  Compounds of general formula I R 1 is selected from any one of phenyl, pyridinyl, pyrroloyl, thienyl, furanyl, imidazolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R 1 phenyl ring and R 1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C 1 -C 6 alkyl, NO 2 , CF 3 , C 1 -C 6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.

  通式I的化合物，其中R1可从苯基、吡啶基、吡咯基、噻吩基、呋喃基、咪唑基、三唑基、噻唑基和吡啶N-氧化物中选择；其中每个R1苯环和R1杂环环可以选择并独立地进一步取代1、2或3个取代基，所述取代基可选择直链或支链C1-C6烷基、NO2、CF3、C1-C6烷氧基、氯、氟、溴和碘。苯环和杂环环上的取代基可以在任何位置上发生；本申请公开和声明了这些化合物的盐和药物组合物，并将其用于治疗，特别是用于疼痛、焦虑和功能性胃肠疾病的管理。
• 8-(Biaryl)quinoline pde4 inhibitors
  申请人：Dube Daniel

  公开号：US20050234238A1

  公开（公告）日：2005-10-20

  8-(biaryl) quinolines wherein the bi-aryl group at the 8-position is in a meta relationship to the quinoline group, are PDE4 inhibitors useful in the treatment of asthma, chronic bronchitis, chronic obstructive pulmonary disease, eosinophilic granuloma, psoriasis and other benign or malignant proliferative skin diseases, endotoxic shock, laminitis in horses, colic in horses, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and brain, inflammatory arthritis, chronic glomerulonephritis, atopic dermatitis, urticaria, adult respiratory distress syndrome, chronic obstructive pulmonary disease in animals, diabetes insipidus, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, arterial restenosis, ortherosclerosis, atherosclerosis, neurogenic inflammation, pain, cough, rheumatoid arthritis, ankylosing spondylitis, transplant rejection, graft versus host disease, hypersecretion of gastric acid, bacterial, fungal induced sepsis, viral induced sepsis, fungal induced septic shock, viral induced septic shock, inflammation-mediated chronic tissue degeneration, cytokine-mediated chronic tissue degeneration, osteoarthritis, cancer, cachexia, muscle wasting, depression, memory impairment, tumour growth, or cancerous invasion of normal tissues. In another aspect, the present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and cognition enhancing amount of a phosphodiesterase-4 inhibitor.

  8-(联苯基)喹啉中，8位位置的联苯基与喹啉基团呈间位关系，是PDE4抑制剂，可用于治疗哮喘、慢性支气管炎、慢性阻塞性肺疾病、嗜酸性粒细胞肉芽肿、银屑病和其他良性或恶性增生性皮肤疾病、内毒素休克、马蹄疾病、马腹绞痛、败血症休克、溃疡性结肠炎、克罗恩病、心肌和脑再灌注损伤、炎性关节炎、慢性肾小球肾炎、特应性皮炎、荨麻疹、成人呼吸窘迫综合症、动物慢性阻塞性肺疾病、尿崩症、过敏性鼻炎、过敏性结膜炎、春季结膜炎、动脉再狭窄、动脉硬化、神经源性炎症、疼痛、咳嗽、类风湿性关节炎、强直性脊柱炎、移植排斥、移植物抗宿主病、胃酸分泌过多、细菌、真菌引起的败血症、病毒引起的败血症、真菌引起的败血性休克、病毒引起的败血性休克、炎症介导的慢性组织退化、细胞因子介导的慢性组织退化、骨关节炎、癌症、消瘦、肌肉消耗、抑郁症、记忆障碍、肿瘤生长或癌细胞侵袭正常组织。另一方面，本发明还涉及一种增强健康受试者认知能力的方法，包括给予安全的认知增强剂量的磷酸二酯酶-4抑制剂。特别地，本发明涉及一种增强健康受试者记忆、学习、保留、回忆、意识和判断能力的方法，包括给予安全的认知增强剂量的磷酸二酯酶-4抑制剂。
• HYDROXYPHENYL-PIPERIDIN-4-YLIDENE-METHYL-BENZAMIDE DERIVATIVES FOR THE TREATEMENT OF PAIN
  申请人：AstraZeneca AB

  公开号：EP1282616A1

  公开（公告）日：2003-02-12
• 4-(PHENYL-PIPERIDIN-4-YLIDENE-METHYL)-BENZAMIDE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF PAIN, ANXIETY OR GASTROINTESTINAL DISORDERS
  申请人：AstraZeneca AB

  公开号：EP1395576B1

  公开（公告）日：2005-08-31