SA 6817

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: SA 6817
• 英文别名: (2S)-2-[3-[(2S)-2-carboxy-2-hydroxyethyl]-3-isobutylureido]-3-(2-naphthyl)propionic acid；(2S)-2-[[[(2S)-2-carboxy-2-hydroxyethyl]-(2-methylpropyl)carbamoyl]amino]-3-naphthalen-2-ylpropanoic acid
• 化学式: C₂₁H₂₆N₂O₆
• 分子量: 402.447
• InChiKey: YSCAUSDTOSSZRE-ROUUACIJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  29
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  127
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• NOVEL 1,3-DIALKYLUREA DERIVATIVE HAVING HYDROXYL GROUP
  申请人：SANTEN PHARMACEUTICAL CO., LTD.

  公开号：EP0738711A1

  公开（公告）日：1996-10-23

  The present invention relates to compounds represented by the formula [I] and salts thereof, wherein R1 and R4 each represents a carboxyl group which can be converted into ester, amide or hydroxamic acid; R2 represents a lower alkyl group or a phenyl-lower alkyl group; R3 represents a hydrogen atom, a lower alkyl group, an amino-lower alkyl group, a lower alkylamino-lower alkyl group, a hydroxy-lower alkyl group, a mercapto-lower alkyl group, a carboxy-lower alkyl group, a lower alkoxycarbonyl-lower alkyl group, an imidazolyl-lower alkyl group, an indolyl-lower alkyl group, (substituted) phenyl group, (substituted) phenyl-lower alkyl group, (substituted) naphtyl group, or (substituted) naphtyl-lower alkyl group. The compounds of the present invention have inhibitory effects on endopeptidase 24.11 and are useful as therapeutic agents for cardiovascular disease such as heart failure and hypertension, renal disease such as renal failure, gastroenteric disorder such as diarrhea and hyperchlorhydria, endocrine and metabolic disease such as obesity, and autoimmune disease such as rheumatism, and as analgestics for myosalgia, migraine.

  本发明涉及式 [I] 所代表的化合物及其盐类、 其中 R1 和 R4 分别代表可转化为酯、酰胺或羟肟酸的羧基；R2 代表低级烷基或苯基-低级烷基；R3 代表氢原子、低级烷基、氨基-低级烷基、低级烷氨基-低级烷基、羟基-低级烷基、巯基-低级烷基、羧基-低级烷基、低级烷氧羰基-低级烷基、咪唑基-低级烷基、吲哚基-低级烷基、（取代）苯基、（取代）苯基-低级烷基、（取代）萘基或（取代）萘基-低级烷基。 本发明的化合物对内肽酶 24.11 具有抑制作用，可作为心血管疾病（如心力衰竭和高血压）、肾脏疾病（如肾功能衰竭）、肠胃疾病（如腹泻和高氯血症）、内分泌和代谢疾病（如肥胖）以及自身免疫性疾病（如风湿病）的治疗剂，也可作为肌痛、偏头痛的镇痛剂。
• Compositions of a chromene or phenyl acetic acid cyclooxygenase-2 selective inhibitor and an ACE inhibitor for the treatment of central nervous system damage
  申请人：Stephenson T. Diane

  公开号：US20050070543A1

  公开（公告）日：2005-03-31

  The present invention provides compositions and methods for the treatment of central nervous system damage in a subject. More particularly, the invention provides a combination therapy for the treatment of a central nervous system ischemic condition or a central nervous system traumatic injury comprising the administration to a subject of an ACE inhibitor in combination with a chromene or phenyl acetic acid cyclooxygenase-2 selective inhibitor.

  本发明提供了治疗受试者中枢神经系统损伤的组合物和方法。 更具体地说，本发明提供了一种用于治疗中枢神经系统缺血性疾病或中枢神经系统创伤性损伤的组合疗法，包括向受试者施用 ACE 抑制剂与铬烯或苯乙酸环氧化酶-2 选择性抑制剂。
• [EN] COMPOSITIONS OF A CHROMENE OR PHENYL ACETIC ACID CYCLOOXYGENASE-2 SELECTIVE INHIBITOR AND AN ACE INHIBITOR FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DAMAGE<br/>[FR] COMPOSITIONS CONSTITUEES D'UN INHIBITEUR CHROMENE OU ACIDE PHENYLACETIQUE SELECTIF DE LA CYCLOOXYGENASE-2 ET D'UN INHIBITEUR DE ACE POUR TRAITER LES LESIONS DU SYSTEME NERVEUX CENTRAL
  申请人：PHARMACIA CORP

  公开号：WO2005016249A2

  公开（公告）日：2005-02-24

  The present invention provides compositions and methods for the treatment of central nervous system damage in a subject. More particularly, the invention provides a combination therapy for the treatment of a central nervous system ischemic condition or a central nervous system traumatic injury comprising the administration to a subject of an ACE inhibitor in combination with a chromene or phenyl acetic acid cyclooxygenase-2 selective inhibitor.