1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine | 863654-15-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine
• 英文别名: 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[(R)-3-amino-piperidin-1-yl]-xanthine；2-[[8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-2,6-dioxopurin-1-yl]methyl]pyridine-3-carbonitrile
• CAS: 863654-15-3
• 化学式: C₂₂H₂₄N₈O₂
• 分子量: 432.485
• InChiKey: ISVBJQYIQQKSGK-MRXNPFEDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  32
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  124
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine 在 盐酸 作用下， 以 乙醇 、 甲基叔丁基醚 、 异丙醇 为溶剂， 以89%的产率得到1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[(R)-3-amino-piperidin-1-yl]-xanthine monohydrochloride
  参考文献：
  名称：

  8-(3-AMINO-PIPERIDIN-1-YL)-XANTHINES, THEIR PREPARATION, AND THEIR USE AS PHARMACEUTICALS

  摘要：

  本发明涉及8-[3-氨基哌啶-1-基]-黄嘌呤及其生理上可接受的盐，特别是其盐酸盐。

  公开号：

  US20070027168A1
• 作为产物：
  描述：

  1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-phthalimido-piperidin-1-yl)-xanthine 在 C.I.酸性橙108 作用下， 以 甲苯 为溶剂， 反应 2.0h， 以86.2%的产率得到1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine
  参考文献：
  名称：

  8-(3-AMINO-PIPERIDIN-1-YL)-XANTHINES, THEIR PREPARATION, AND THEIR USE AS PHARMACEUTICALS

  摘要：

  本发明涉及8-[3-氨基哌啶-1-基]-黄嘌呤及其生理上可接受的盐，特别是其盐酸盐。

  公开号：

  US20070027168A1

文献信息

• TREATMENT OF METABOLIC DISORDERS IN EQUINE ANIMALS
  申请人：REICHE Dania Birte

  公开号：US20140303096A1

  公开（公告）日：2014-10-09

  The present invention relates to SGLT2 inhibitor or a pharmaceutically acceptable form thereof for use in the treatment and/or prevention of a metabolic disorder of an equine animal. In particular, the present invention relates the SGLT2 inhibitor or a pharmaceutically acceptable form thereof for use in the treatment and/or prevention of insulin resistance, hyperinsulinemia, impaired glucose tolerance, dyslipidemia, dysadipokinemia, subclinical inflammation, systemic inflammation, low grade systemic inflammation, obesity, and/or regional adiposity in an equine animal.

  本发明涉及SGLT2抑制剂或其药用可接受形式，用于治疗和/或预防马类动物的代谢紊乱。具体而言，本发明涉及SGLT2抑制剂或其药用可接受形式，用于治疗和/或预防马类动物的胰岛素抵抗、高胰岛素血症、糖耐量受损、血脂异常、脂联素异常、亚临床炎症、全身炎症、低级全身炎症、肥胖和/或局部脂肪堆积。
• TREATMENT OF METABOLIC DISORDERS IN FELINE ANIMALS
  申请人：Boehringer Ingelheim Vetmedica GmbH

  公开号：US20150164856A1

  公开（公告）日：2015-06-18

  The present invention relates to one or more SGLT2 inhibitors or pharmaceutically acceptable forms thereof for use in the treatment and/or prevention of a metabolic disorder in a feline animal, preferably wherein the metabolic disorder is one or more selected from the group consisting of: ketoacidosis, pre-diabetes, diabetes mellitus type 1 or type 2, insulin resistance, obesity, hyperglycemia, impaired glucose tolerance, hyperinsulinemia, dyslipidemia, dysadipokinemia, subclinical inflammation, systemic inflammation, low grade systemic inflammation, hepatic lipidosis, atherosclerosis, inflammation of the pancreas, neuropathy and/or Syndrome X (metabolic syndrome) and/or loss of pancreatic beta cell function and/or wherein the remission of the metabolic disorder, preferably diabetic remission, is achieved and/or maintained.

  本发明涉及一种或多种SGLT2抑制剂或其药用可接受形式，用于治疗和/或预防猫科动物的代谢紊乱，最好是其中代谢紊乱是来自以下组合的一种或多种：酮症酸中毒、糖尿病前期、糖尿病1型或2型、胰岛素抵抗、肥胖、高血糖、糖耐量受损、高胰岛素血症、血脂异常、脂联素异常、亚临床炎症、全身炎症、低级全身炎症、肝脂肪变性、动脉粥样硬化、胰腺炎、神经病变和/或综合征X（代谢综合征）和/或胰岛β细胞功能丧失，其中代谢紊乱的缓解，最好是糖尿病缓解，被实现和/或维持。
• PHARMACEUTICAL COMPOSITION COMPRISING A GLUCOPYRANOSYL-SUBSTITUTED BENZENE DERIVATIVE
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP3939577A1

  公开（公告）日：2022-01-19

  The invention relates to a pharmaceutical composition according to the claim 1 comprising a glucopyranosyl-substituted benzene derivative in combination with a DPP IV inhibitor which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.

  该发明涉及根据权利要求1的药物组合物，包括一种葡萄糖吡喃基取代苯衍生物与一种适用于治疗或预防从以下选定的一种或多种疾病的DPP IV抑制剂的组合物，所述疾病包括1型糖尿病、2型糖尿病、糖耐量受损和高血糖。此外，本发明涉及预防或治疗代谢紊乱及相关疾病的方法。
• 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
  申请人：Himmelsbach Frank

  公开号：US20050234108A1

  公开（公告）日：2005-10-20

  The present invention relates to substituted xanthines of general formula wherein R is defined as in claim 1 , the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

  本发明涉及通式所示的取代黄嘌呤，其中R如权利要求书中所定义，其互变体、立体异构体、其混合物和盐具有有价值的药理特性，特别是对酶二肽基肽酶-IV（DPP-IV）活性的抑制作用。
• PROCESS FOR THE PREPARATION OF CHIRAL 8-(3-AMINOPIPERIDIN-1-YL)-XANTHINES
  申请人：PFRENGLE Waldemar

  公开号：US20130178485A1

  公开（公告）日：2013-07-11

  The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.

  本发明涉及一种改进的方法，用于制备对映纯的8-(3-氨基哌啶-1-基)-黄嘌呤。