3-oxo-N-(5-phenyl-1,2,4-thiadiazol-3-yl)spiro[2-benzofuran-1,4'-piperidine]-1'-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: 3-oxo-N-(5-phenyl-1,2,4-thiadiazol-3-yl)spiro[2-benzofuran-1,4'-piperidine]-1'-carboxamide
• 化学式: C₂₁H₁₈N₄O₃S
• 分子量: 406.5
• InChiKey: HBTPBWKAVPMXQK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  29
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  113
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Novel spiro compounds
  申请人：——

  公开号：US20020188124A1

  公开（公告）日：2002-12-12

  Compounds of the general formula (I): 1 wherein Ar 1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.

  通式(I)的化合物： 1 其中Ar 1 代表可选地取代的芳基或杂芳基； n代表0或1； T、U、V和W各自独立地代表氮原子或可选地取代的次甲基基团，其中至少有两个代表所述次甲基基团； X代表次甲基或羟基取代的次甲基； Y代表可选地取代的亚氨基或氧原子被描述和声称。这些新型的螺环化合物作为神经肽Y受体拮抗剂以及用于治疗各种心血管疾病、中枢神经系统疾病、代谢性疾病等的药物是有用的。
• NOVEL SPIRO COMPOUNDS
  申请人：——

  公开号：US20020052371A1

  公开（公告）日：2002-05-02

  Compounds of the general formula (I): 1 (wherein Ar 1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W represent independently nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or nitrogen; Y represents optionally substituted imino or oxygen atom) exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis and the like, central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal and the like, metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia and the like, sexual and reproductive dysfunction, gastro-intestinal disorder, respiratory disorder, inflammation or glaucoma, and the like.

  通式（I）化合物（其中Ar1代表可选取代的芳基或杂环芳基；n代表0或1；T、U、V和W独立地代表氮原子或可选取代的甲基基团，其中至少有两个代表所述甲基基团；X代表甲基或氮原子；Y代表可选取代的亚胺基或氧原子）表现出NPY拮抗活性，并且可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，如高血压、肾病、心脏病、血管痉挛、动脉硬化等，中枢神经系统疾病，如暴食症、抑郁症、焦虑症、癫痫、痴呆、疼痛、酗酒、戒断等，代谢性疾病，如肥胖症、糖尿病、激素异常、高胆固醇血症、高脂血症等，性和生殖功能障碍、胃肠道疾病、呼吸系统疾病、炎症或青光眼等。
• Integrated electrode and cell immobilization device equipped with the integrated electrode
  申请人：——

  公开号：US20040209352A1

  公开（公告）日：2004-10-21

  An integrated electrode capable of immobilizing an isolated cell and/or a cultured cell on the electrode without giving any damage to its cell membrane, and capable of detecting an electrophysiological activity of the immobilized cell with sufficient sensitivity is provided. An integrated electrode having a substrate equipped with at least one electric conductor, and a wiring part which leads an electrical signal out from the aforementioned electric conductor, in which the integrated electrode can detect an electrical signal resulting from an electrophysiological change of a cell immobilized on the surface of the aforementioned electric conductor, and at least a part of the surface of the aforementioned electric conductor is coated with a dielectric material, with the aforementioned dielectric material being a positively charged polymer material, and the aforementioned cell being an isolated cell and/or a cultured cell.

  本发明提供了一种集成电极，它能将离体细胞和/或培养细胞固定在电极上而不损伤其细胞膜，并能以足够的灵敏度检测被固定细胞的电生理活动。一种集成电极，其基板上装有至少一个电导体，以及一个将电信号从上述电导体引出的接线部分，其中集成电极可检测固定在上述电导体表面的细胞的电生理变化产生的电信号，上述电导体表面的至少一部分涂有介电材料，上述介电材料为带正电荷的聚合物材料，上述细胞为离体细胞和/或培养细胞。
• Method of immobilizing cell
  申请人：——

  公开号：US20040224367A1

  公开（公告）日：2004-11-11

  A method of the immobilization is provided in which a cell can be immobilized with high accuracy in a state where its activity is maintained, even in a minute region, or a region that constitutes a complicated pattern. A method of the immobilization of a cell in which a cell is immobilized in a desired region among the surface of a substrate, which includes the step of forming a masking layer in a region except for the aforementioned desired region on the surface of the aforementioned substrate (St 2 ), the step of immobilizing the aforementioned cell through bringing a solution containing the aforementioned cells into contact with the surface of the aforementioned substrate and the surface of the aforementioned masking layer (St 4 , St 5 ), and the step of adjusting the pH of the aforementioned solution to give the condition which permits separation of the aforementioned masking layer from the aforementioned substrate without loss of the activity of the aforementioned cell (St 6 ).

  本发明提供了一种固定细胞的方法，在这种方法中，即使在微小区域或构成复杂图案的区域，也能以保持细胞活性的状态高精度地固定细胞。一种固定细胞的方法，其中细胞被固定在基底表面的所需区域中，该方法包括在上述基底（St 2 将含有上述细胞的溶液与上述基底表面和上述掩蔽层表面接触，从而固定上述细胞的步骤（St 4 ，St 5 调整上述溶液的 pH 值，使其达到允许上述掩蔽层与上述基底分离而又不损失上述细胞活性的条件 （步骤 6）。 6 ).
• Combination therapy for the treatment of obesity
  申请人：MacNeil J. Douglas

  公开号：US20050288213A1

  公开（公告）日：2005-12-29

  The present invention relates to compositions comprising a NPY5 antagonist of formula I or II and an anti-obesity agent, useful for the treatment and prevention of diabetes, obesity and obesity-related disorders. The present invention further relates to methods of treating or preventing obesity and obesity-related disorder in a subject in need thereof by administering a composition of the present invention. The present invention further provides for pharmaceutical compositions, medicaments, and kits useful in carrying out these methods.

  本发明涉及由式 I 或式 II 的 NPY5 拮抗剂和抗肥胖药组成的组合物。 和一种抗肥胖剂，可用于治疗和预防糖尿病、肥胖症和肥胖相关疾病。本发明进一步涉及通过施用本发明的组合物治疗或预防有需要的受试者的肥胖和肥胖相关疾病的方法。本发明进一步提供了用于实施这些方法的药物组合物、药剂和试剂盒。