PEFICITINIB游离态 | 944134-74-1

• 物质功能分类: 生物化工 - 生化试剂 - 激动剂抑制剂
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 中文名称: PEFICITINIB游离态
• 中文别名: 培菲替尼
• 英文名称: Peficitinib
• 英文别名: 4-[[(1R,3S)-5-hydroxy-2-adamantyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
• CAS: 944134-74-1；944118-01-8
• 化学式: C₁₈H₂₂N₄O₂
• 分子量: 326.4
• InChiKey: DREIJXJRTLTGJC-JQCLMNFQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  104
• 氢给体数：
  4
• 氢受体数：
  4

文献信息

• KINASE INHIBITORS
  申请人：Respivert Limited

  公开号：US20170291917A1

  公开（公告）日：2017-10-12

  There are provided compounds of formula I, wherein T, A, Q, Z, G, R 4 , R 5a , R 5b and n have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

  提供了化合物I的公式，其中T、A、Q、Z、G、R4、R5a、R5b和n的含义如描述中所示，这些化合物具有抗炎活性（例如，通过抑制p38丝裂原活化蛋白激酶酶家族中的一个或多个成员；Syk激酶；以及酪氨酸激酶Src家族的成员之一）并且在治疗中有用，包括在药物组合中，特别是用于治疗炎症性疾病，包括肺部、眼睛和肠道的炎症性疾病。
• CRYSTAL OF FUSED PYRIDINE COMPOUND SALT
  申请人：Kikuchi Takashi

  公开号：US20130102628A1

  公开（公告）日：2013-04-25

  [Problem] A salt or crystal of a compound which is highly stable in a solid state and useful as a bulk material for the preparation of a pharmaceutical product is provided. [Means for Solution] 4-[(1R,2s,3S,5s,7s)-5-Hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide succinate, 4-[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrobromide, and 4-[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride and crystals thereof are useful as a bulk material for the preparation of a solid preparation, in particular, a solid dispersion preparation. Furthermore, the crystal of the hydrobromide has excellent stability in a solid state and is useful as a bulk material for the preparation of a pharmaceutical product.

  提供了一种在固态中高度稳定且作为制备药物产品的大块材料有用的化合物的盐或晶体。解决方法为：4-[(1R,2s,3S,5s,7s)-5-羟基-2-重氮基]氨基}-1H-吡咯并[2,3-b]吡啶-5-羧酰胺琥珀酸盐，4-[(1R,2s,3S,5s,7s)-5-羟基-2-重氮基]氨基}-1H-吡咯并[2,3-b]吡啶-5-羧酰胺溴化物，以及4-[(1R,2s,3S,5s,7s)-5-羟基-2-重氮基]氨基}-1H-吡咯并[2,3-b]吡啶-5-羧酰胺盐酸盐及其晶体可作为制备固体制剂，特别是固体分散制剂的大块材料。此外，溴化物的晶体在固态中具有优异的稳定性，并可作为制备药物产品的大块材料。
• HETEROCYCLIC JANUS KINASE 3 INHIBITORS
  申请人：Inoue Takayuki

  公开号：US20090270376A1

  公开（公告）日：2009-10-29

  The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).

  本发明提供了一种化合物(I)的公式，具有优异的JAK3抑制活性，并可用作治疗和/或预防各种免疫疾病，包括自身免疫性疾病、炎症性疾病和过敏性疾病的活性成分。根据本发明的化合物具有抑制JAK3的活性，因此可用作治疗或预防由不良细胞因子信号传递引起的疾病的活性成分（例如，在器官/组织移植期间的排斥反应、自身免疫性疾病、多发性硬化症、类风湿性关节炎、牛皮癣、哮喘、特应性皮炎、阿尔茨海默病和动脉粥样硬化疾病），或由异常细胞因子信号传递引起的疾病（例如癌症和白血病）。
• KINASE INHIBITOR
  申请人：RESPIVERT LIMITED

  公开号：US20160096805A1

  公开（公告）日：2016-04-07

  There is provided a compound of formula I, which compound has antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

  提供了一种化合物I的公式，该化合物具有抗炎活性（例如通过抑制p38丝裂原激活蛋白激酶酶家族中的一个或多个成员、Syk激酶和酪氨酸激酶Src家族的成员之一），并可用于治疗，包括在药物组合中，特别是用于治疗炎症性疾病，包括肺部、眼部和肠道的炎症性疾病。
• PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION
  申请人：Astellas Pharma Inc.

  公开号：EP2979698A1

  公开（公告）日：2016-02-03

  A pharmaceutical composition containing, as the active ingredient, 4-[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, of which the solubility in an acidic pH region is different from that in a neutral pH region, with rapid disintegration property and rapid drug dissolution property as well as the expectation of a good drug dosing compliance, is provided. The pharmaceutical composition for oral administration of the present invention contains 4-[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide or a pharmaceutically acceptable salt thereof, and a hydrophilic lubricant, and is useful as a pharmaceutical composition for oral administration with rapid disintegration property and rapid drug dissolution property as well as the expectation of a good drug dosing compliance.

  本发明提供了一种含有 4-[(1R,2s,3S,5s,7s)-5-羟基-2-金刚烷基]氨基}-1H-吡咯并[2,3-b]吡啶-5-甲酰胺作为活性成分的药物组合物，该药物组合物在酸性 pH 值区域的溶解度不同于在中性 pH 值区域的溶解度，具有快速崩解特性和快速药物溶解特性，并有望实现良好的药物剂量依从性。本发明的口服药物组合物含有 4-[(1R,2s,3S,5s,7s)-5-羟基-2-金刚烷基]氨基}-1H-吡咯并[2,3-b]吡啶-5-甲酰胺或其药学上可接受的盐，以及亲水性润滑剂，可作为口服药物组合物使用，具有快速崩解特性和快速药物溶出特性，以及良好的药物剂量依从性。