pyrrolo[2.3-b]pyridine-1-carboxamide | 1542066-93-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: pyrrolo[2.3-b]pyridine-1-carboxamide
• 英文别名: Pyrrolo[2,3-b]pyridine-1-carboxamide
• CAS: 1542066-93-2
• 化学式: C₈H₇N₃O
• 分子量: 161.163
• InChiKey: PWEBVYIWBLUXHJ-UHFFFAOYSA-N

物化性质

• 沸点：
  369.3±34.0 °C(Predicted)
• 密度：
  1.41±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  60.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  7-氮杂吲哚 、 三光气 在 N,N-二异丙基乙胺 、 氨 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 以20%的产率得到pyrrolo[2.3-b]pyridine-1-carboxamide
  参考文献：
  名称：

  [EN] 7-AZAINDOLE DERIVATIVES AS PARP INHIBITORS
  [FR] DÉRIVÉS DE 7-AZAINDOLE UTILISÉS EN TANT QU'INHIBITEURS DE PARP

  摘要：

  本发明涉及公式（I）的7-氮杂吲哚衍生物，包含这种衍生物的药物组合物。该发明进一步涉及用于医学用途的上述药物组合物，更具体地用于治疗癌症疾病，其中对PARP的抑制是有效的。

  公开号：

  WO2015011008A1

文献信息

• [EN] RING-FUSED BICYCLIC PYRIDYL DERIVATIVES AS FGFR4 INHIBITORS<br/>[FR] DÉRIVÉS PYRIDYLE BICYCLIQUES À ANNEAUX FUSIONNÉS UTILISÉS EN TANT QU'INHIBITEURS DE FGFR4
  申请人：NOVARTIS AG

  公开号：WO2015059668A1

  公开（公告）日：2015-04-30

  The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

  本发明提供了化合物(I)或其药学上可接受的盐；制备该化合物的方法及其治疗用途。本发明还提供了药理活性剂的组合物和包含该化合物的药物组合物。
• [EN] GLUTARIMIDE<br/>[FR] GLUTARIMIDE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2019043214A1

  公开（公告）日：2019-03-07

  The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. Present compounds are thus useful for the treatment of various cancers.

  本发明提供了一种与广泛表达的E3连接酶蛋白Cereblon（CRBN）结合并改变CRBN E3泛素连接酶复合物底物特异性的化合物，导致内在下游蛋白的降解。因此，目前的化合物对于治疗各种癌症是有用的。
• [EN] BICYCLIC HETEROCYCLES AS IRAK4 INHIBITORS<br/>[FR] HÉTÉROCYCLES BICYCLIQUES CONVENANT COMME INHIBITEURS DE L'IRAK4
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2013042137A1

  公开（公告）日：2013-03-28

  The present invention provides bicyclic heterocycle kinase enzyme inhibitor compounds of formula (I), which may be therapeutically useful as kinase inhibitor, more particularly IRAK4 inhibitors. ( I ) in which A, R, R1,R2, m, n and p have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting kinase enzyme, more particularly IRAK4 enzyme.The present invention also provides pharmaceutical formulations comprising at least one of the kinase inhibitor compounds of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了公式（I）的双环杂环化酶抑制剂化合物，可能在治疗中作为激酶抑制剂具有治疗作用，更具体地是IRAK4抑制剂。其中 A、R、R1、R2、m、n 和 p 的含义如规范中所给出，并且其在治疗和预防疾病或紊乱方面是有用的，特别是在需要抑制激酶酶有优势的疾病或紊乱中，更具体地是IRAK4酶的使用。本发明还提供了包含至少一种公式（I）的激酶抑制剂化合物的药物配方，以及其与药用载体、稀释剂或赋形剂一起使用。
• Benzazepine derivatives as histamine h3 antagonists
  申请人：Bailey Nicholas

  公开号：US20070060566A1

  公开（公告）日：2007-03-15

  The present invention relates to novel benzazepine derivatives of structure (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders. These compounds act as histamine H3 antagonists.

  本发明涉及具有药理活性的新型苯并氮杂环衍生物(I)的结构，其制备过程，包含它们的组合物以及它们在神经和精神障碍治疗中的应用。这些化合物作为组胺H3拮抗剂。
• 7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors
  作者：Raffaella Cincinelli、Loana Musso、Lucio Merlini、Giuseppe Giannini、Loredana Vesci、Ferdinando M. Milazzo、Nives Carenini、Paola Perego、Sergio Penco、Roberto Artali、Franco Zunino、Claudio Pisano、Sabrina Dallavalle

  DOI：10.1016/j.bmc.2013.12.031

  日期：2014.2

  7-Azaindole-1-carboxamides were designed as a new class of PARP-1 inhibitors. The compounds displayed a variable pattern of target inhibition profile that, in part, paralleled the antiproliferative activity in cell lines characterized by homologous recombination defects. A selected compound (1l; ST7710AA1) showed significant in vitro target inhibition and capability to substantially bypass the multidrug resistance mediated by Pgp. In antitumor activity studies against the MX1 human breast carcinoma growth in nude mice, the compound exhibited an effect similar to that of Olaparib in terms of tumor volume inhibition when used at a lower dose than the reference compound. Treatment was well tolerated, as no deaths or significant weight losses were observed among the treated animals. (C) 2013 Elsevier Ltd. All rights reserved.