去谷胃泌素 | 51987-65-6

• 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
• 中文名称: 去谷胃泌素
• 英文名称: Desglugastrin
• 英文别名: 5-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
• CAS: 51987-65-6
• 化学式: C₄₉H₆₁N₉O₁₃
• 分子量: 984.1
• InChiKey: BRUVESZIOCJLDB-GJPUTSFASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  71
• 可旋转键数：
  28
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  357
• 氢给体数：
  12
• 氢受体数：
  13

文献信息

• Substituted benzimidazoles
  申请人：Gant Thomas G.

  公开号：US20090258897A1

  公开（公告）日：2009-10-15

  Disclosed herein are substituted benzimidazole-based proton pump modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

  本文揭示了一种基于苯并咪唑的质子泵调节剂的化合物I，其制备方法，药物组合物及使用方法。
• Inhibitors of the gastric H+, K+-atpase with enhanced therapeutic properties
  申请人：Gant G. Thomas

  公开号：US20070082929A1

  公开（公告）日：2007-04-12

  Chemical syntheses and medical uses of novel inhibitors of the gastric H + , K + -ATPase for the treatment and/or management of duodenal ulcers, heartburn, acid reflux, other conditions mediated by gastric acid secretion and/or psoriasis are described.

  描述了用于治疗和/或管理十二指肠溃疡、胃灼热、酸反流、其他由胃酸分泌介导的疾病以及牛皮癣的新型胃H+、K+-ATP酶抑制剂的化学合成和医学用途。
• SUBSTITUTED BENZIMIDAZOLES
  申请人：Gant Thomas G.

  公开号：US20080255200A1

  公开（公告）日：2008-10-16

  Disclosed herein are substituted benzimidazole-based proton pump modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

  本文揭示了基于取代苯并咪唑的质子泵调节剂的化合物I的公式，其制备过程，药物组合物以及使用方法。
• INHIBITORS OF THE GASTRIC H+, K+-ATPASE WITH ENHANCED THERAPEUTIC PROPERTIES
  申请人：Gant Thomas G.

  公开号：US20090215831A1

  公开（公告）日：2009-08-27

  Chemical syntheses and medical uses of novel inhibitors of the gastric H + , K + -ATPase for the treatment and/or management of duodenal ulcers, heartburn, acid reflux, other conditions mediated by gastric acid secretion and/or psoriasis are described.

  本文描述了一些新型胃H+、K+-ATP酶抑制剂的化学合成和医疗用途，用于治疗和/或管理十二指肠溃疡、心灵烦躁、酸反流、其他由胃酸分泌介导的疾病和/或银屑病。
• Biologically active lysine containing octapeptides
  申请人：The Administrators of The Tulane University Educational Fund

  公开号：EP0203031A2

  公开（公告）日：1986-11-26

  Novel compositions of the formula wherein A represents an L, D or DL amino-acid selected from the group consisting of Ala, Val, Phe, p-CI-Phe, Trp, Pro, Ser, Thr, Glu, Gly, Beta Ala, Abu, N-Me Ala, 5-F-Trp, 5-Br-Trp, 5-Cl-Trp, their acetylated derivatives or a pharmaceutically acceptable acid addition salt thereof; B represents an L, D or DL amino acid amide selected from the group consisting of Thr NH2, Val NH,, Pro NH2, HO-Pro NH2, Ser NH2, Tyr NH2, Trp NH2, 5-F-Trp NH,, For-Trp NH., Ala NH2, Gly NH2, Me Ala NH2; X represents L-Phe or L-Tyr, Y represents L-Thr or L-Val; Z is L, D or DL-5-F-Trp, 5-Br-Trp, 5-C1-Trp, 5-I-Trp or D-Trp; and C" and C' represent L or D Cys, Abu, Asp or Lys; provided that where C' is Cys, C" is also Cys and where C' or C" are other than Cys, C" is different from C' and is other than Cys and the pharmaceutically acceptable acid addition salts thereof; are useful as agents for inhibiting the release of growth hormone, for the treatment of gastrointestinal disorders and for therapy of certain cancers and the management of diabetes. These biologically active octapeptides all possess a terminal amino acid amide at position 8 and are prepared by solid phase methods.

  式中的新型组合物 式中 A 代表选自以下组别的 L、D 或 DL 氨基酸：Ala、Val、Phe、p-CI-Phe、Trp、Pro、Ser、Thr、Glu、Gly、Beta Ala、Abu、N-Me Ala、5-F-Trp、5-Br-Trp、5-Cl-Trp、它们的乙酰化衍生物或其药学上可接受的酸加成盐； B 代表选自 Thr NH2、Val NH、Pro NH2、HO-Pro NH2、Ser NH2、Tyr NH2、Trp NH2、5-F-Trp NH、For-Trp NH、Ala NH2、Gly NH2、Me Ala NH2 所组成的组的 L、D 或 DL 氨基酸酰胺； X 代表 L-Phe或 L-Tyr、 Y 代表 L-Thr 或 L-Val Z 是 L、D 或 DL-5-F-Trp、5-Br-Trp、5-C1-Trp、5-I-Trp 或 D-Trp；以及 C "和 C'代表 L 或 D Cys、Abu、Asp 或 Lys；条件是当 C' 是 Cys 时，C "也是 Cys，当 C' 或 C "不是 Cys 时，C "不同于 C'，也不是 Cys 及其药学上可接受的酸加成盐；可用作抑制生长激素释放、治疗胃肠道疾病、治疗某些癌症和糖尿病的药物。这些具有生物活性的八肽都在第 8 位具有一个末端氨基酸酰胺，并通过固相方法制备。