N-[4-(3-amino-1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2-fluoro-5-methyl-benzenesulfonamide | 1426214-91-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-[4-(3-amino-1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2-fluoro-5-methyl-benzenesulfonamide
• 英文别名: N-[4-(3-amino-1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2-fluoro-5-methylbenzenesulfonamide；N-[4-(3-Amino-1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2-fluoro-5-methyl-benzenesulfonamide；N-[4-(3-amino-2H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2-fluoro-5-methylbenzenesulfonamide
• CAS: 1426214-91-6
• 化学式: C₁₈H₁₅FN₆O₂S
• 分子量: 398.421
• InChiKey: DSWGOVYHCBKYGU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  135
• 氢给体数：
  3
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  N-[4-(3-amino-1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2-fluoro-5-methyl-benzenesulfonamide 、 对氯苯异氰酸酯 在 1,3-二甲基-2-咪唑啉酮 作用下， 反应 16.0h， 生成 1-(4-chlorophenyl)-3-[6-[4-[(2-fluoro-5-methyl-phenyl)sulfonylamino]phenyl]-1H-pyrazolo[3,4-b]pyrazin-3-yl]urea
  参考文献：
  名称：

  N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals

  摘要：

  公开号：

  EP2570415B1
• 作为产物：
  描述：

  6-(4-aminophenyl)-1H-pyrazolo[3,4-b]pyrazin-3-ylamine hydrochloride 、 2-氰基-5-甲基苯磺酰氯 在 吡啶 作用下， 以 二氯甲烷 为溶剂， 反应 16.0h， 以220 mg的产率得到N-[4-(3-amino-1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2-fluoro-5-methyl-benzenesulfonamide
  参考文献：
  名称：

  [EN] N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS
  [FR] N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHÉNYL]-SULFONAMIDES ET LEUR UTILISATION COMME PRODUITS PHARMACEUTIQUES

  摘要：

  本发明涉及公式（I）中的N-[4-(1H-吡唑并[3,4-b]吡嗪-6-基)-苯基]-磺酰胺，其中Ar，R1，R2和n在权利要求书中所示的含义。公式（I）中的化合物是有价值的药理活性化合物，可以调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶亚型1（SGK-1，SGK1）的活性，并且适用于治疗SGK活性不当的疾病，例如退行性关节疾病或炎症过程，如骨关节炎或风湿病。本发明还涉及制备公式（I）中化合物的方法，它们作为药物的用途以及包含它们的制剂。

  公开号：

  WO2013041502A1

文献信息

• N-[4-(1H-吡唑并[3,4-b]吡嗪-6-基)-苯基]-磺 酰胺类及其作为药物的用途
  申请人：赛诺菲

  公开号：CN103012407B

  公开（公告）日：2016-06-29

  本发明涉及具有式I的N-[4-(1H-吡唑并[3，4-b]吡嗪-6-基)-苯基]-磺酰胺类，其中，Ar，R1，R2和n具有如权利要求中所示含义。式I的化合物是有价值的具有药理学活性的化合物，其调节蛋白激酶活性，特别是血清及糖皮质激素调节激酶的活性(SGK)，尤其是血清及糖皮质激素调节激酶同工型1(SGK-1，SGK1)的活性，并且这些化合物适合于治疗SGK活性不适当的疾病，例如退化性关节疾病或炎症过程如骨关节炎或风湿病。本发明进一步涉及制备式I的化合物的方法，它们作为药物的用途以及包含它们的药物组合物。
• [EN] N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS<br/>[FR] N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHÉNYL-SULFONAMIDES ET LEURS UTILISATION COMME PRODUITS PHARMACEUTIQUES
  申请人：SANOFI SA

  公开号：WO2013041119A1

  公开（公告）日：2013-03-28

  The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]- sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的N-[4-(1H-吡唑啉[3,4-b]吡唑啉-6-基)-苯基]-磺酰胺，其中Ar、R1、R2和n具有权利要求中所示的含义。式I的化合物是有价值的药理活性化合物，可调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，尤其是血清和糖皮质激素调节激酶同工型1（SGK-1，SGK1），适用于治疗SGK活性不恰当的疾病，例如退行性关节疾病或炎症过程，如骨关节炎或风湿病。本发明还涉及制备式I的化合物的方法，它们作为药物的用途，以及包含它们的药用组合物。
• N-[4-(1H-PYRAZOLO[3,4-b]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS
  申请人：NAZARE Marc

  公开号：US20130072493A1

  公开（公告）日：2013-03-21

  The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及公式I中的N-[4-(1H-吡唑并[3,4-b]吡嗪-6-基)-苯基]-磺酰胺，其中Ar、R1、R2和n在权利要求中有所示的含义。公式I中的化合物是有价值的药理活性化合物，可以调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶同工酶1（SGK-1，SGK1）的活性，并适用于治疗SGK活性不当的疾病，例如退行性关节疾病或炎症过程，如骨关节炎或风湿病。本发明还涉及制备公式I中化合物的方法，它们作为药物的用途以及包含它们的制药组合物。
• N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS
  申请人：SANOFI

  公开号：US20140288083A1

  公开（公告）日：2014-09-25

  The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及公式I的N-[4-(1H-吡唑并[3,4-b]吡嗪-6-基)-苯基]-磺酰胺，其中Ar，R1，R2和n在权利要求中所示。公式I的化合物是有价值的药理活性化合物，可以调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶亚型1（SGK-1，SGK1）的活性，并适用于治疗SGK活性不当的疾病，例如退行性关节疾病或炎症过程，如骨关节炎或风湿病。本发明还涉及制备公式I的化合物的方法，它们作为药物的用途以及包含它们的制药组合物。
• N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals
  申请人：SANOFI

  公开号：US09174993B2

  公开（公告）日：2015-11-03

  The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式(I)的N-[4-(1H-吡唑并[3,4-b]吡嗪-6-基)-苯基]-磺酰胺化合物，其中Ar，R1，R2和n在权利要求书中所示。式(I)的化合物是有价值的药理活性化合物，能够调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶亚型1（SGK-1，SGK1）的活性，并且适用于治疗SGK活性不当的疾病，例如退行性关节疾病或炎症过程，如骨关节炎或风湿病。本发明还涉及制备式(I)化合物的方法，它们作为药物的用途，以及包含它们的制药组合物。