(2S,3R)-2-amino-3-methyl-1-(1,3-thiazolidin-3-yl)pentan-1-one | 251571-80-9

• 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: (2S,3R)-2-amino-3-methyl-1-(1,3-thiazolidin-3-yl)pentan-1-one
• CAS: 251571-80-9
• 化学式: C₉H₁₈N₂OS
• 分子量: 202.32
• InChiKey: WCRLBFHWFPELKW-SFYZADRCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  71.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Combination of a dpp IV inhibitor and an antiobesity or appetite regulating agent
  申请人：Holmes Grenville David

  公开号：US20070149451A1

  公开（公告）日：2007-06-28

  The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising of a DPP IV inhibitor or a pharmaceutically acceptable salt thereof and an antiobesity agent, or an appetite regulating agent, or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention, delay of progression or treatment of diseases and disorders selected from the group consisting of hypertension, congestive heart failure, left ventricular hypertrophy, peripheral arterial disease, diabetes, especially type 2 diabetes mellitus, diabetic retinopathy, macular degeneration, cataract, diabetic nephropathy, glomerulosclerosis, chronic renal failure, diabetic neuropathy, syndrome X, premenstrual syndrome, coronary heart disease, angina pectoris, thrombosis, atherosclerosis, myocardial infarction, transient ischemic attacks, stroke, vascular restenosis, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertryglyceridemia, insulin resistance, impaired glucose metabolism, conditions of impaired glucose tolerance, conditions of impaired fasting plasma glucose, obesity, erectile dysfunction, skin and connective tissue disorders, foot ulcerations and ulcerative colitis, endothelial dysfunction and impaired vascular compliance.
• Use of Organic Compounds
  申请人：Hughes Edward Thomas

  公开号：US20070254944A1

  公开（公告）日：2007-11-01

  A method for improving glucose control by administering metformin in combination with a DPP-IV inhibitor to a patient in need thereof, in an amount sufficient to control the glucose level over an extended period of time.
• Direct Compression Formulation And Process
  申请人：Kowalski James

  公开号：US20080038341A1

  公开（公告）日：2008-02-14

  Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of being directly compressed with specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus presents formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.
• Combination of Organic Compounds
  申请人：Burkey Bryan

  公开号：US20080070922A1

  公开（公告）日：2008-03-20

  The present invention relates to a combination, comprising; i) DPP IV inhibitor or a pharmaceutically acceptable salt thereof, and ii) at least one PDGF receptor tyrosine kinase inhibitor or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention, delay of progression or treatment of a disease or condition selected from insulin resistance, impaired glucose metabolism (IGT), conditions of impaired glucose tolerance, conditions of impaired fasting plasma glucose, diabetes particularly type 1 or type 2 diabetes mellitus, obesity, diabetic retinopathy, macular degeneration, cataracts, diabetic nephropathy, glomerulosclerosis, diabetic neuropathy, erectile dysfunction, premenstrual syndrome, coronary heart disease, hypertension, angina pectoris, myocardial infarction, stroke, vascular restenosis, skin and connective tissue disorders, foot ulcerations and ulcerative colitis, endothelial dysfunction and impaired vascular compliance, and vascular events, cardiovascular morbidity or mortality associated with diabetes (e.g. type I or II) or IGT.
• Direct Compression Formulation and Process
  申请人：Kowalski James

  公开号：US20080193529A1

  公开（公告）日：2008-08-14

  Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of being directly compressed with a glitazone and specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus presents formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.