N-(2-chlorophenyl)pyrazolo[1,5-a]pyridine-3-carboxamide | 902295-69-6

• 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-(2-chlorophenyl)pyrazolo[1,5-a]pyridine-3-carboxamide
• CAS: 902295-69-6
• 化学式: C₁₄H₁₀ClN₃O
• 分子量: 271.706
• InChiKey: CPQRFZBWMKEHSA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  46.4
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(2-chlorophenyl)pyrazolo[1,5-a]pyridine-3-carboxamide 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 反应 2.0h， 生成 2-chloro-N-(pyrazolo[1,5-a]pyridin-3-ylmethyl)aniline
  参考文献：
  名称：

  EphB3受体酪氨酸激酶抑制剂的构效关系研究

  摘要：

  吡唑并[1,5- a ]吡啶的 2-氯苯胺衍生物的构效关系研究表明，通过保留 2-氯苯胺并向 5吡唑并[1,5- a ]吡啶的-位。此外，用咪唑并[1,2- a ]吡啶替代吡唑并[1,5- a ]吡啶具有良好的耐受性，并导致小鼠肝微粒体稳定性增强。EphB3 抑制两种杂环系列的构效关系相似。细胞培养中的代表性类似物也证明了激酶抑制活性。一个模拟 ( 32, LDN-211904) 还分析了对一组 288 种激酶的抑制活性，发现对酪氨酸激酶具有很高的选择性。总体而言，这些研究为检查 EphB3 受体的体外、细胞和潜在的体内激酶依赖性功能提供了有用的分子探针。

  DOI：

  10.1016/j.bmcl.2009.09.010

文献信息

• Methods of treating Crohn's disease or ulcerative colitis by administering inhibitors of tumor necrosis factor-like cytokine 1A (TL1A)
  申请人：PROMETHEUS BIOSCIENCES, INC.

  公开号：US11136386B2

  公开（公告）日：2021-10-05

  Provided are methods, systems, and kits for selecting a patient for treatment with a therapeutic agent based on a presence of a genotype associated with a positive therapeutic response to the therapeutic agent. The therapeutic agent, in some embodiments, is an inhibitor of TL1A activity or expression, such as for example, an anti-TL1A antibody.

  本文提供的方法、系统和试剂盒用于根据是否存在与对治疗剂的阳性治疗反应相关的基因型，选择患者接受治疗剂的治疗。在某些实施方案中，治疗剂是 TL1A 活性或表达的抑制剂，例如抗 TL1A 抗体。
• TL1A PATIENT SELECTION METHODS, SYSTEMS, AND DEVICES
  申请人：Prometheus Biosciences, Inc.

  公开号：US20200362025A1

  公开（公告）日：2020-11-19

  Provided are methods, systems, and kits for selecting a patient for treatment with a therapeutic agent based on a presence of a genotype associated with a positive therapeutic response to the therapeutic agent. The therapeutic agent, in some embodiments, is an inhibitor of TL1A activity or expression, such as for example, an anti-TL1A antibody.
• METHODS AND SYSTEMS FOR CHARACTERIZING SEVERE CROHN'S DISEASE
  申请人：CEDARS-SINAI MEDICAL CENTER

  公开号：US20210079473A1

  公开（公告）日：2021-03-18

  The present disclosure describes methods, devices and systems of diagnosing, prognosing, and treating subjects with moderate to severe forms of Crohn's disease (CD) that is characterized by stricturing and internal penetrating disease phenotypes. Also described are methods and kits for characterizing a subtype of CD, and identifying a subject as being suitable for a therapy to treat the CD.
• METHODS OF TREATING REFRACTORY INFLAMMATORY DISEASE USING TRANSCRIPTOMIC AND GENETIC RISK SIGNATURES
  申请人：CEDARS-SINAI MEDICAL CENTER

  公开号：US20210277477A1

  公开（公告）日：2021-09-09

  Disclosed herein are methods, kits and compositions for treating an inflammatory disease. These methods, kits and compositions may be particularly useful for subjects carrying a risk genotype and/or expressing a transcriptomic risk signature that is indicative of severe inflammatory disease phenotypes for which existing treatment options are limited.
• [EN] METHODS OF TREATING INFLAMMATORY BOWEL DISEASES THAT TARGET RIPK2<br/>[FR] MÉTHODES DE TRAITEMENT DE MALADIES INTESTINALES INFLAMMATOIRES CIBLANT LA RIPK2
  申请人：CEDARS SINAI MEDICAL CENTER

  公开号：WO2020139748A1

  公开（公告）日：2020-07-02

  Described herein are methods, systems, compositions, and kits useful for the diagnosis and/or treatment of inflammatory bowel diseases, including Crohn's disease and ulcerative colitis in a subject, with an antagonist of RIPK2 activity or expression. The present disclosure relates to methods and systems for identifying and stratifying patients suitable for treatment with the antagonist to RIPK2 activity or expression, as described herein.