1,2,3,4-tetrahydro-isoquinoline-7-sulfonic acid dimethylamide | 300553-45-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 四氢异喹啉
• 英文名称: 1,2,3,4-tetrahydro-isoquinoline-7-sulfonic acid dimethylamide
• 英文别名: N,N-dimethyl-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
• CAS: 300553-45-1
• 化学式: C₁₁H₁₆N₂O₂S
• mdl: MFCD11577104
• 分子量: 240.326
• InChiKey: GLUYRXISHOQGNW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.454
• 拓扑面积：
  57.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (R)-1-(4-chloro-pyrimidin-2-yl)-ethyl acetate 、 1,2,3,4-tetrahydro-isoquinoline-7-sulfonic acid dimethylamide 在 三乙胺 作用下， 以 异丙醇 为溶剂， 以327 mg (92%)的产率得到(R)-1-[4-(7-dimethylsulfamoyl-3,4-dihydro-1H-isoquinolin-2-yl)-pyrimidin-2-yl]-ethyl acetate
  参考文献：
  名称：

  Sorbitol dehydrogenase inhibitors

  摘要：

  本发明涉及式I的山梨醇脱氢酶抑制化合物，其中R1、R2和R3如规范中定义。本发明还涉及含有这些化合物的药物组合物，以及通过向患有糖尿病且因此有发展这些并发症风险的哺乳动物投与这些化合物来治疗或预防糖尿病并发症，特别是糖尿病神经病变、糖尿病肾病、糖尿病微血管病、糖尿病大血管病和糖尿病心肌病。本发明还涉及一种含有本发明式I化合物与醛糖还原酶抑制剂的组合物的药物组合物，以及用于治疗或预防糖尿病并发症的方法。本发明还涉及一种含有本发明式I化合物与NHE-1抑制剂的组合物的药物组合物，以及用于治疗心肌病和其他相关心脏问题的方法。本发明还涉及合成式I化合物的某些中间体以及制备这些中间体的方法。

  公开号：

  US06414149B1
• 作为产物：
  描述：

  2-trifluoroacetyl-1,2,3,4-tetrahydro-isoquinoline-7-sulfonic acid dimethylamide 在 potassium carbonate 作用下， 以 甲醇 、 水 为溶剂， 以214 mg (89%)的产率得到1,2,3,4-tetrahydro-isoquinoline-7-sulfonic acid dimethylamide
  参考文献：
  名称：

  Sorbitol dehydrogenase inhibitors

  摘要：

  本发明涉及式I的山梨醇脱氢酶抑制化合物，其中R1、R2和R3如规范中定义。本发明还涉及含有这些化合物的药物组合物，以及通过向患有糖尿病且因此有发展这些并发症风险的哺乳动物投与这些化合物来治疗或预防糖尿病并发症，特别是糖尿病神经病变、糖尿病肾病、糖尿病微血管病、糖尿病大血管病和糖尿病心肌病。本发明还涉及一种含有本发明式I化合物与醛糖还原酶抑制剂的组合物的药物组合物，以及用于治疗或预防糖尿病并发症的方法。本发明还涉及一种含有本发明式I化合物与NHE-1抑制剂的组合物的药物组合物，以及用于治疗心肌病和其他相关心脏问题的方法。本发明还涉及合成式I化合物的某些中间体以及制备这些中间体的方法。

  公开号：

  US06414149B1

文献信息

• [EN] 2-SULFONYLAMINO-4-HETEROARYL BUTYRAMIDE ANTAGONISTS OF CCR10<br/>[FR] ANTAGONISTES DE 2-SULFONYLAMINO-4-HÉTÉROARYL BUTYRAMIDE DE CCR10
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2009126675A1

  公开（公告）日：2009-10-15

  This invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein R1, R2, R4. Ar and Het are as defined herein. The invention also relates to methods of using the compound of formula (I) to treat a diseases and disorders that are mediated or sustained through the activity of CCR10.

  本发明涉及一种具有式（I）的化合物及其药学上可接受的盐，其中R1、R2、R4、Ar和Het如本文中所定义。该发明还涉及使用式（I）的化合物治疗通过CCR10活性介导或维持的疾病和紊乱的方法。
• [EN] AMINOPYRIMIDINES AS SORBITOL DEHYDROGENASE INHIBITORS<br/>[FR] AMINOPYRIMIDINES COMME INHIBITEURS DE SORBITOL DESHYDROGENASE
  申请人：PFIZER PROD INC

  公开号：WO2000059510A1

  公开（公告）日：2000-10-12

  This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula (I), wherein R?1, R2 and R3¿ are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefor at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula (I) of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula (I) of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula (I) and to processes for preparing those intermediates.

  本发明涉及式（I）的山梨醇脱氢酶抑制剂，其中R1、R2和R3在说明书中定义。本发明还涉及含有这些化合物的药物组合物，以及通过将这些化合物用于患有糖尿病并因此有患上这些并发症风险的哺乳动物进行治疗或预防糖尿病并发症，特别是糖尿病神经病变、糖尿病肾病、糖尿病微血管病、糖尿病大血管病和糖尿病心肌病的方法。本发明还涉及一种包含本发明式（I）化合物和醛还原酶抑制剂的药物组合物以及用于治疗或预防糖尿病并发症的方法。本发明还涉及一种包含本发明式（I）化合物和NHE-1抑制剂的药物组合物以及用于治疗心肌病和其他心脏相关问题的方法。本发明还涉及用于合成式（I）化合物的某些中间体以及制备这些中间体的方法。
• Sorbitol dehrydrogenase inhibitors
  申请人：Chu-Moyer Margaret Y.

  公开号：US06936600B2

  公开（公告）日：2005-08-30

  This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, wherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.

  本发明涉及公式I的山梨醇脱氢酶抑制剂化合物，其中R1、R2和R3如规范中所定义。本发明还涉及包含这些化合物的制药组合物以及通过向患有糖尿病且因此有发展这些并发症的风险的哺乳动物投与这些化合物来治疗或预防糖尿病并发症，特别是糖尿病神经病变、糖尿病肾病、糖尿病微血管病、糖尿病大血管病和糖尿病心肌病的方法。本发明还涉及包括本发明的公式I化合物与醛糖还原酶抑制剂的组合物的制药组合物以及用于治疗或预防糖尿病并发症的方法。本发明还涉及包括本发明的公式I化合物与NHE-1抑制剂的组合物的制药组合物以及用于治疗心肌病和其他与心脏有关的问题的方法。本发明还涉及用于合成公式I化合物的某些中间体以及制备这些中间体的方法。
• 2-SULFONYLAMINO-4-HETEROARYL BUTYRAMIDE ANTAGONISTS OF CCR10
  申请人：Abeywardane Asitha

  公开号：US20110275800A1

  公开（公告）日：2011-11-10

  This invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein R 1 , R 2 , R 4 . Ar and Het are as defined herein. The invention also relates to methods of using the compound of formula (I) to treat a diseases and disorders that are mediated or sustained through the activity of CCR 10 .

  本发明涉及公式(I)的化合物及其药学上可接受的盐，其中R1、R2、R4、Ar和Het的定义如本文所述。本发明还涉及使用公式(I)的化合物治疗通过CCR10活性介导或持续的疾病和障碍的方法。
• AMINOPYRIMIDINES AS SORBITOL DEHYDROGENASE INHIBITORS
  申请人：Pfizer Products Inc.

  公开号：EP1185275A1

  公开（公告）日：2002-03-13