N-(3-dimethylaminobenzoyl)-3-(4-aminophenyl)butyrate | 177653-31-5

• 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-(3-dimethylaminobenzoyl)-3-(4-aminophenyl)butyrate
• 英文别名: 4-[4-(3-dimethylamino-benzoylamino)-phenyl]-butyric acid；4-{4-[3-(Dimethylamino)benzamido]phenyl}butanoic acid；4-[4-[[3-(dimethylamino)benzoyl]amino]phenyl]butanoic acid
• CAS: 177653-31-5
• 化学式: C₁₉H₂₂N₂O₃
• 分子量: 326.395
• InChiKey: ZTNGOCKLOFPLDU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  24
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  69.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  3-二甲基氨基苯甲酰氯 在 sodium hydroxide 、 三乙胺 作用下， 反应 4.0h， 生成 N-(3-dimethylaminobenzoyl)-3-(4-aminophenyl)butyrate
  参考文献：
  名称：

  4-[4-[(2-Hydroxybenzoyl)amino]phenyl]butyric Acid as a Novel Oral Delivery Agent for Recombinant Human Growth Hormone

  摘要：

  A series of N-acetylated, non-alpha, aromatic amino acids was prepared and shown to promote the absorption of recombinant human growth hormone (rhGH) from the gastrointestinal tract. Seventy compounds in this family were tested in vivo in rats. Of the compounds tested, 4-[4-[(2-hydroxybenzoyl)amino]phenyl]butyric acid was identified as a preclinical candidate and was used to demonstrate the oral delivery of rhGH in primates. A significant positive correlation was found between the relative log k' of the delivery agents, as determined by HPLC on an immobilized artificial membrane (IAM) column, and serum rhGH concentrations following oral or colonic dosing in rats. Structure-activity relationships have also been developed on the basis of electronic effects and hydrogen-bonding characteristics of the aromatic amide substituents.

  DOI：

  10.1021/jm960038f

文献信息

• AROMATIC AMIDE DERIVATIVE
  申请人：Fujimaki Nobuko

  公开号：US20110071304A1

  公开（公告）日：2011-03-24

  A compound represented by the following general formula (I) (R 1 and R 2 represent hydrogen atom, an alkyl group, a halogen atom, etc.; R 3 and R 4 represent hydrogen atom, an alkyl group, an alkoxy group, or an alkenyl group; R 5 represents hydrogen atom, an alkyl group, or nitro group, and R 6 represents hydrogen atom or an alkyl group), which acts on the transcription process of genes.

  由以下一般式（I）表示的化合物（其中R1和R2代表氢原子、烷基基团、卤原子等；R3和R4代表氢原子、烷基基团、烷氧基团或烯基基团；R5代表氢原子、烷基基团或硝基基团，R6代表氢原子或烷基基团），该化合物对基因的转录过程具有作用。
• Solid pharmaceutical dosage forms comprising bisphosphonates and modified amino acid carriers
  申请人：Ahmed Hashim

  公开号：US20070049557A1

  公开（公告）日：2007-03-01

  The present invention provides novel solid pharmaceutical dosage forms for oral administration comprising a bisphosphonate, or a pharmaceutically acceptable salt thereof, which bisphosphonate is present in an amount not therapeutically effective when the bisphosphonate is orally administered alone; and a modified amino acid carrier, or a pharmaceutically acceptable salt thereof, which modified amino acid carrier is present in an amount effective to facilitate absorption of the bisphosphonate in the gastrointestinal tract such that the bisphosphonate is therapeutically effective. The ratio of bisphosphonate to modified amino acid carrier is from about 1:30 to about 1:1, respectively. These novel solid pharmaceutical dosage forms are useful in the treatment or control of bone diseases and particular disorders in calcium metabolism, including, for example, osteoporosis, hypercalcaemia of cancer, and the treatment of metastatic bone pain. The present invention also provides a method for treating these diseases employing the solid pharmaceutical dosage forms and a method for preparing the pharmaceutical dosage forms.
• COMPOSITIONS AND METHODS FOR TREATMENT OF DISEASES AND CONDITIONS EMPLOYING ORAL ADMINISTRATION OF SODIUM PENTOSAN POLYSULFATE AND OTHER PENTOSAN POLYSULFATE SALTS
  申请人：PARSONS C. Lowell

  公开号：US20170189443A1

  公开（公告）日：2017-07-06

  The present invention is directed to a pharmaceutical composition comprising: (1) a therapeutically effective quantity of sodium pentosan polysulfate; (2) a quantity of a penetration enhancer sufficient to improve the bioavailability of the sodium pentosan polysulfate; and (3) optionally, a pharmaceutically acceptable carrier and to methods for the oral administration of sodium pentosan polysulfate with improved bioavailability for the treatment of interstitial cystitis and other urinary tract diseases and conditions. Such compositions and methods allow the administration of sodium pentosan polysulfate at lower dosages to reduce the frequency and severity of side effects.
• US8722723B2
  申请人：——

  公开号：US8722723B2

  公开（公告）日：2014-05-13
• US9370492B2
  申请人：——

  公开号：US9370492B2

  公开（公告）日：2016-06-21