3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide;6-phenylpteridine-2,4,7-triamine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 蝶啶及其衍生物
• 英文名称: 3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide;6-phenylpteridine-2,4,7-triamine
• 化学式: C18H19ClN14O
• 分子量: 482.9
• InChiKey: QVJDOWMTTXZFAA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.46
• 重原子数：
  34
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  289
• 氢给体数：
  7
• 氢受体数：
  12

文献信息

• [EN] PYRAZOLO [4, 3-D] PYRIMIDINES USEFUL AS KINASE INHIBITORS<br/>[FR] PYRAZOLO[4,3-D]PYRIMIDINES UTILES EN TANT QU'INHIBITEURS DE KINASES
  申请人：ORIGENIS GMBH

  公开号：WO2012143144A1

  公开（公告）日：2012-10-26

  The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

  本发明涉及一种能够抑制一个或多个激酶，特别是SYK（脾酪氨酸激酶）、LRRK2（富含亮氨酸重复的激酶2）和/或MYLK（肌球蛋白轻链激酶）或其突变体的化合物的新颖化合物（I）的公式。这些化合物在治疗各种疾病中发挥作用。这些疾病包括自身免疫疾病、炎症性疾病、骨疾病、代谢性疾病、神经和神经退行性疾病、癌症、心血管疾病、过敏、哮喘、阿尔茨海默病、帕金森病、皮肤疾病、眼部疾病、传染病和与激素相关的疾病。
• [EN] HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES EN TANT QU'INHIBITEURS DE KINASES
  申请人：ORIGENIS GMBH

  公开号：WO2012143143A1

  公开（公告）日：2012-10-26

  The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

  本发明涉及一种能够抑制一个或多个激酶，特别是SYK（脾酪氨酸激酶）、LRRK2（富含亮氨酸重复激酶2）和/或MYLK（肌球蛋白轻链激酶）或其突变体的化合物的新颖化合物（I）的公式。这些化合物在治疗各种疾病中发挥作用。这些疾病包括自身免疫疾病、炎症性疾病、骨疾病、代谢性疾病、神经和神经退行性疾病、癌症、心血管疾病、过敏、哮喘、阿尔茨海默病、帕金森病、皮肤疾病、眼部疾病、传染病和与激素相关的疾病。
• Combination of sodium chloride and epithelial sodium channel blocker
  申请人：Westfälische Wilhelms-Universität Münster

  公开号：EP2626084A1

  公开（公告）日：2013-08-14

  Provided is a combination of an epithelial sodium channel blocker and sodium chloride. The combination comprises sodium chloride in an amount of 1.5 g or more. Provided is also a method of diagnosing an increased risk of developing hypertension and/or of stratifying the risk of developing hypertension. A further method is a method of determining whether the blood pressure of a subject is sensitive to sodium intake. These methods comprise administering an epithelial sodium channel blocker and sodium chloride to the subject. After waiting for about 10 minutes or more, at least one of systolic and diastolic blood pressure of the subject is determined, and the blood pressure is compared to a control measurement or to a predetermined reference value. A temporary increase in systolic and/or diastolic blood pressure compared to the control measurement indicates a risk of a disorder, or that the blood pressure of the subject is sensitive to sodium intake. Provided is also a kit with a first container that comprises sodium chloride, but is at least essentially void of an epithelial sodium channel blocker. A second container of the kit comprises a combination of an epithelial sodium channel blocker and sodium chloride.

  提供了一种上皮钠通道阻滞剂和氯化钠的组合物。该复方制剂包括氯化钠，用量为 1.5 克或更多。还提供了一种诊断高血压发病风险增加和/或对高血压发病风险进行分层的方法。另一种方法是确定受试者的血压是否对钠摄入敏感的方法。这些方法包括向受试者施用上皮钠通道阻滞剂和氯化钠。等待约 10 分钟或更长时间后，测定受试者的收缩压和舒张压中的至少一种，并将血压与对照测量值或预定参考值进行比较。与对照测量值相比，收缩压和/或舒张压的暂时升高表明存在疾病风险，或受试者的血压对钠摄入量敏感。还提供了一种试剂盒，其第一容器包含氯化钠，但至少基本上不含上皮钠通道阻滞剂。试剂盒的第二个容器由上皮钠通道阻滞剂和氯化钠组合而成。
• Ion channel modulating activity II
  申请人：Fedida David

  公开号：US20050119315A1

  公开（公告）日：2005-06-02

  Methods, compositions, dosing regimes, and routes of administration for the treatment or prevention of arrhythmias. In these methods, arrythmias (e.g. atrial fibrillation, atrial flutter, early afterdepolarizations and prolongation of QT interval) may be reduced or eliminated by administering ion channel modulating compounds to a subject in need thereof. The ion channel modulating compounds may be cycloalkylamine ether compounds, particularly cyclohexylamine ether compounds. Also described are compositions of ion channel modulating compounds and drugs which induce early afterdepolarizations, prolongation of QT interval and/or Torsades de Pointes.

  治疗或预防心律失常的方法、组合物、给药方案和给药途径。在这些方法中，通过对有需要的受试者施用离子通道调节化合物，可减少或消除心律失常（如心房颤动、心房扑动、早期后极化和 QT 间期延长）。离子通道调节化合物可以是环烷基胺醚化合物，特别是环己胺醚化合物。还描述了离子通道调节化合物和药物的组合物，这些组合物会诱发早期后极化、QT间期延长和/或Torsades de Pointes。
• HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS
  申请人：Origenis GmbH

  公开号：EP2699572A1

  公开（公告）日：2014-02-26