(2S)-2-amino-3-(1H-imidazol-5-yl)propan-1-ol;hydron;dichloride

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (2S)-2-amino-3-(1H-imidazol-5-yl)propan-1-ol;hydron;dichloride
• 化学式: C6H13Cl2N3O
• 分子量: 214.09
• InChiKey: FRCAFNBBXRWXQA-XRIGFGBMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.12
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  74.9
• 氢给体数：
  5
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3(R)-t-butoxycarbonylamino-N-(2,2-dimethyl-1(S)-(methylcarbamoyl)propyl)succinamic acid benzyl ester 、 、 (2S)-2-amino-3-(1H-imidazol-5-yl)propan-1-ol;hydron;dichloride 、 2-(1H-Benzotriazole-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate 以to furnish 410 mg (92%) of 3(R)-(t-butoxycarbonylamino)-N-[2-hydroxy-1(S)-[(1H-imidazol-4-yl)methyl]ethyl]succinamic acid benzyl ester as a solid which的产率得到3(R)-(t-butoxycarbonylamino)-N-[2-hydroxy-1(S)-[(1H-imidazol-4-yl)methyl]ethyl]succinamic acid benzyl ester
  参考文献：
  名称：

  Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses

  摘要：

  本发明涉及化合物I的配方，其中R1、R2、R3、R4、R5、X、Y和β如下所定义。这些化合物通过将发明化合物的有效量与金属蛋白酶接触来抑制金属蛋白酶的活性。

  公开号：

  US06174915B1

文献信息

• N-SUBSTITUTED PYRROLIDINES
  申请人：Chu Xin-Jie

  公开号：US20120010235A1

  公开（公告）日：2012-01-12

  Compounds of formula and enantiomers and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control, amelioration or prevention of cancer.

  描述了公式的化合物及其对映体和药用可接受的盐，以及含有该化合物及其药用可接受的盐的药物组合物，以及该化合物和药物组合物用于治疗、控制、改善或预防癌症的用途。
• Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their use
  申请人：——

  公开号：US20020019429A1

  公开（公告）日：2002-02-14

  The present invention is directed to compound of the formula I: 1 wherein R 1 , R 2 , R 3 , R 4 , R 5 , X, Y, and 2 are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.

  本发明涉及公式I的化合物：1其中R1、R2、R3、R4、R5、X、Y和2如此定义。这些化合物通过与一定量的本发明化合物接触来抑制金属蛋白酶的活性。
• Metalloproteinase inhibitors, pharmaceutical compositions containing
  申请人：Agouron Pharmaceuticals, Inc.

  公开号：US06008243A1

  公开（公告）日：1999-12-28

  The present invention is directed to compound of the formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, X, Y, and ##STR2## are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.

  本发明涉及式I的化合物：##STR1## 其中R.sub.1、R.sub.2、R.sub.3、R.sub.4、R.sub.5、X、Y和##STR2##如本文所定义。这些化合物通过将发明化合物的有效量与金属蛋白酶接触来抑制金属蛋白酶的活性。
• PRODRUGS OF GUANFACINE
  申请人：Whomsley Rhys

  公开号：US20120065152A1

  公开（公告）日：2012-03-15

  Prodrugs of guanfacine, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for improving the pharmacokinetics of guanfacine or minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration are provided herein.

  本文提供了瓜那非前药、含有这种前药的药物组合物以及一种使用瓜那非前药治疗注意力缺陷多动障碍/反抗行为障碍（ADHD/ODD）的方法。此外，本文还提供了改善瓜那非药物动力学或减少或避免与瓜那非给药相关的不良胃肠副作用的方法。
• Histidinol dehydrogenase protein, DNA and muteins and transgenic plants thereof
  申请人：CIBA-GEIGY AG

  公开号：EP0478502A2

  公开（公告）日：1992-04-01

  The present invention comprises cDNA coding for histidinol dehydrogenase from plants, the final step in histidine biosynthesis. The invention also comprises a novel method of purifying histidinol dehydrogenase from plants to essential honogeneity, the purified histidinol dehydrogenase, an assay for identifying inhibitors of histidinol dehydrogenase, an assay to identify mutants of histidinol dehydrogenase that are not inhibited by inhibitors of wild-type histidinol dehydrogenase, the inhibitors so identified as well as herbicide compositions containing them, the non-inhibited mutants of histidinol dehydrogenase, transgenic crop plants containing the non-inhibited mutants of histidinol dehydrogenase, and methods of treating weeds utilizing the application of histidinol dehydrogenase inhibitors to the transgenic crops containing the non-inhibited mutants of histidinol dehydrogenase.

  本发明包括植物组氨醇脱氢酶的 cDNA 编码，这是组氨酸生物合成的最后一步。本发明还包括一种从植物中纯化组氨醇脱氢酶至基本纯度的新方法、纯化的组氨醇脱氢酶、鉴定组氨醇脱氢酶抑制剂的检测方法、鉴定不受野生型组氨醇脱氢酶抑制剂抑制的组氨醇脱氢酶突变体的检测方法、组氨醇脱氢酶的非抑制突变体、含有组氨醇脱氢酶非抑制突变体的转基因作物植株，以及利用向含有组氨醇脱氢酶非抑制突变体的转基因作物施用组氨醇脱氢酶抑制剂来处理杂草的方法。