| 97683-31-3

• 分子结构分类: 有机化合物 - 碳氢化合物 - 不饱和烃
• CAS: 97683-31-3
• 化学式: C15H18NaO3S
• 分子量: 301.4
• InChiKey: ZIPRJZAWCYYGAV-UHFFFAOYSA-N

物化性质

• 熔点：
  153 °C

计算性质

• 辛醇/水分配系数(LogP)：
  3.34
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  62.8
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2904100000

文献信息

• 5-Amidino-N-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative, medicinal composition containing the same, pharmaceutical use thereof, and intermediate therefor
  申请人：Okazaki Kosuke

  公开号：US20060111446A1

  公开（公告）日：2006-05-25

  The present invention relates to a 5-amidino-N-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R 1 is a hydrogen atom or a lower alkyl group; R 2 represents a hydrogen atom, an optionally substituted lower alkyl group, etc.; R 3 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or a hydroxy group, etc., or a pharmaceutically acceptable salt thereof, which exerts a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

  本发明涉及一种5-酰胺基-N-(2-氨基苯乙基)-2-羟基苯磺酰胺衍生物，其通式表示为：其中R1为氢原子或低碳基；R2表示氢原子、可选取代的低碳基等；R3为二(低碳基)氨基基团、低碳基、环烷基等；Q为氢原子或可选取代的低碳基；Z为氢原子或羟基等，或其药学上可接受的盐，具有强效和选择性的激活血凝因子X抑制活性，并可用作预防或治疗与激活血凝因子X相关的疾病的药物，以及包含该药物的制药组合物、其药用和中间体。
• Preventive or therapeutic agent for kidney disease
  申请人：Koizumi Takashi

  公开号：US20050107354A1

  公开（公告）日：2005-05-19

  The present invention relates to an agent for the prevention or treatment of a renal disease comprising as an active ingredient a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R 1 is a hydrogen atom or an optionally substituted alkyl group; R 2 is a dialkylamino group, an alkyl group, a cycloalkyl group, an optionally substituted aryl group etc.; T is an oxygen atom, a sulfur atom etc.; Q is a hydrogen atom or an optionally substituted alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof which has an inhibitory effect on mesangial cell proliferation and a decreasing effect on protein excretion in urine, and are useful for preventing or treating of various renal diseases such as IgA nephropathy, diabetic nephropathy, nephritic syndrome and the like.

  本发明涉及一种用于预防或治疗肾脏疾病的药剂，其包含作为活性成分的5-酰胺基-2-羟基苯磺酰胺衍生物，其表示为通式： 其中，R1是氢原子或可选取代的烷基基团；R2是二烷基氨基基团、烷基基团、环烷基团、可选取代的芳基基团等；T是氧原子、硫原子等；Q是氢原子或可选取代的烷基基团；Z是氢原子、羟基等，或其药学上可接受的盐，具有对系膜细胞增殖的抑制作用和对尿蛋白排泄的降低作用，适用于预防或治疗各种肾脏疾病，如IgA肾病、糖尿病肾病、肾炎综合症等。
• 5-amidino-n-(2-aminophenethyl)-n-hydroxy-benzenesulffonamide derivative, medical composition containing the same, pharmaceutical use thereof and intermediate therefor
  申请人：——

  公开号：US20040242455A1

  公开（公告）日：2004-12-02

  The present invention relates to a 5-amidino-N-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative represented by the general formula: 1 wherein R 1 is a hydrogen atom or a lower alkyl group; R 2 represents a hydrogen atom, an optionally substituted lower alkyl group, etc.; R 3 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or a hydroxy group, etc., or a pharmaceutically acceptable salt thereof, which exerts a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

  本发明涉及一种由通式1表示的5-酰胺基-N-(2-氨基苯乙基)-2-羟基苯磺酰胺衍生物，其中R1是氢原子或较低的烷基；R2表示氢原子、可选取代的较低烷基等；R3是二(较低烷基)氨基基团、较低烷基基团、环烷基等；Q是氢原子或可选取代的较低烷基；Z是氢原子或羟基等，或其药学上可接受的盐，该化合物具有强效和选择性的激活血凝因子X抑制活性，并可用作预防或治疗与激活血凝因子X相关的疾病的药物，以及包含该化合物的制药组合物、其药物用途和中间体。
• 5-amidino-2-hydroxybenzenesulfonamide derivatives medicinal compoistions containing the same medicinal use thereof and intermediates in the production thereof
  申请人：Uchida Masahiko

  公开号：US20050014787A1

  公开（公告）日：2005-01-20

  The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R 1 is an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkenyl group, a cycloalkyl group or a lower acyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same and an intermediate thereof. These compounds are useful as preventives or remedies for various diseases such as brain infarction, cerebral thrombosis, cerebral embolism, TIA, cerebral vascular jerk, Alzheimer's diseases, myocardial infarction, heart attack, heart failure, thrombosis, pulmonary infarction and pulmonary embolism.

  本发明涉及一种5-酰胺基-2-羟基苯磺酰胺衍生物，其通式表示为：其中，R1是可选取的取代的低烷基，可选取的取代的低烷氧基，可选取的取代的低烯基，环烷基或低酰基等；Q是氢原子或可选取的取代的低烷基；Z是氢原子或羟基等，或其药学上可接受的盐。该衍生物具有强效和选择性的激活血凝因子X抑制活性，可用作预防或治疗与激活血凝因子X相关的疾病的药物，以及包含该衍生物和其中间体的制药组合物。这些化合物可用作各种疾病的预防或治疗，例如脑梗死、脑血栓形成、脑栓塞、短暂性脑缺血发作、脑血管抽搐、阿尔茨海默病、心肌梗死、心脏病发作、心力衰竭、血栓形成、肺梗死和肺栓塞。
• METHOD FOR PROMOTING GASTROINTESTINAL FUNCTION AND METHOD FOR SCREENING FOR PROMOTER OF GASTROINTESTINAL FUNCTION
  申请人：Tanaka Tatsuro

  公开号：US20090018161A1

  公开（公告）日：2009-01-15

  The present invention provides a more effective gastrointestinal function promoter. The present invention also provides a method for the prophylaxis or improvement of functional gastrointestinal disorders, a method for appetite regulation and the like. The present invention also provides a method for screening for a substance capable of promoting a gastrointestinal function. The present invention provides a gastrointestinal function promoter containing a T1R agonist as an active ingredient and a method for the prophylaxis or improvement of functional gastrointestinal disorders, a method for appetite regulation and the like by administering a T1R agonist. The present invention also provides a method of screening for a substance capable of promoting a gastrointestinal function which method uses a cell expressing T1R receptor.

  本发明提供了一种更有效的肠道功能促进剂。本发明还提供了一种预防或改善功能性肠道疾病的方法，以及一种食欲调节等方法。本发明还提供了一种筛选能够促进肠道功能的物质的方法。本发明提供了一种含有T1R激动剂作为活性成分的肠道功能促进剂，以及通过给予T1R激动剂来预防或改善功能性肠道疾病、调节食欲等方法。本发明还提供了一种筛选能够促进肠道功能的物质的方法，该方法使用表达T1R受体的细胞。