7-chloro-2-methyl-2H-pyrazolo[4,3-d]pyrimidine | 923282-41-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并嘧啶类
• 英文名称: 7-chloro-2-methyl-2H-pyrazolo[4,3-d]pyrimidine
• 英文别名: 7-Chloro-2-methyl-2H-pyrazolo[4,3-d]pyrimidine；7-chloro-2-methylpyrazolo[4,3-d]pyrimidine
• CAS: 923282-41-1
• 化学式: C₆H₅ClN₄
• 分子量: 168.585
• InChiKey: ZXVUORXEWWBPEP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  43.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  7-chloro-2-methyl-2H-pyrazolo[4,3-d]pyrimidine 、 (S)-2-amino-4-(cyclopropyl(4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)butyl)amino)butanoic acid trifluoroacetate 在 碳酸氢钠 作用下， 以 四氢呋喃 、 水 为溶剂， 生成 (S)-4-(cyclopropyl(4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)butyl)amino)-2-((2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7-yl)amino)butanoic acid
  参考文献：
  名称：

  [EN] EXPANDED DOSAGE REGIMENS FOR INTEGRIN INHIBITORS
  [FR] POSOLOGIES ÉTENDUES POUR DES INHIBITEURS DE L'INTÉGRINE

  摘要：

  本发明涉及用于日常给药的化合物剂型，其化合物为式（A）和式（I）的化合物或其盐，其中R1、R2、R10、R11、R12、R13、R14、R15、R16、q和p如本文所述。式（A）、式（I）的化合物和其制备的药物组合物是αvβ6整合素抑制剂，可用于治疗纤维化，如特发性肺纤维化（IFF）和非特异性间质性肺炎（NSIP）。

  公开号：

  WO2022232838A1

文献信息

• Pyrazolo pyrimidines useful as aurora kinase inhibitors
  申请人：Oslob D. Johan

  公开号：US20070027166A1

  公开（公告）日：2007-02-01

  The present invention provides compounds having the formula: wherein A-B together represent one of the following structures: wherein one of is a double bond, as valency permits; and R 2 , R 4 , X 1A , X 2A , X 1B , X 2B , L 1 , L 2 , Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., Aurora), and thus are useful, for example, for the treatment of Aurora mediated diseases.

  本发明提供具有以下结构的化合物：其中A-B一起代表以下结构之一：其中之一是双键，根据价性而定；而R2、R4、X1A、X2A、X1B、X2B、L1、L2、Y和Z如此处所定义，以及其制药组合物，如此处总体描述和所述的亚类，这些化合物可用作蛋白激酶（例如Aurora）的抑制剂，因此可用于例如治疗由Aurora介导的疾病。
• AMINO ACID COMPOUNDS AND METHODS OF USE
  申请人：Pliant Therapeutics, Inc.

  公开号：US20190276449A1

  公开（公告）日：2019-09-12

  The invention relates to compounds of formula (A) and formula (I): or a salt thereof, wherein R 1 , R 2 , R 10 , R 11 , R 12 , R 13 , R 14 , R 15 , R 16 , q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).

  该发明涉及以下化合物的公式(A)和公式(I)：或其盐，其中R1、R2、R10、R11、R12、R13、R14、R15、R16、q和p如本文所述。公式(A)、公式(I)的化合物及其药物组合物是αvβ6整合素抑制剂，可用于治疗纤维化疾病，如特发性肺纤维化（IPF）和非特异性间质性肺炎（NSIP）。
• [EN] DOSAGE FORMS AND REGIMENS FOR AMINO ACID COMPOUNDS<br/>[FR] FORMES POSOLOGIQUES ET SCHÉMAS DE TRAITEMENT POUR DES COMPOSÉS D'ACIDES AMINÉS
  申请人：PLIANT THERAPEUTICS INC

  公开号：WO2020210404A1

  公开（公告）日：2020-10-15

  The invention relates to dosage forms for daily administration of compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are ανβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP),

  该发明涉及用于每日给药的化合物(A)和化合物(I)的剂型：或其盐，其中R1、R2、R10、R11、R12、R13、R14、R15、R16、q和p如本文所述。化合物(A)、化合物(I)及其药物组成物是ανβ6整合素抑制剂，可用于治疗纤维化疾病，如特发性肺纤维化（IPF）和非特异性间质性肺炎（NSIP）。
• [EN] TREATMENT OF RESPIRATORY DISEASES WITH AMINO ACID COMPOUNDS<br/>[FR] TRAITEMENT DE MALADIES RESPIRATOIRES AVEC DES COMPOSÉS ACIDES AMINÉS
  申请人：PLIANT THERAPEUTICS INC

  公开号：WO2021225912A1

  公开（公告）日：2021-11-11

  The invention relates to methods of therapy using compounds of formula (I) and formula (II): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (II) and pharmaceutical compositions thereof are integrin inhibitors that are useful in therapy for a condition, for example, caused by or associated with an infectious agent, shock, pancreatitis, or trauma. The condition can include one or more of pulmonary fibrosis associated with rheumatoid arthritis or progressive familial intrahepatic cholestasis (PFIC).

  该发明涉及使用化合物的疗法方法的公式(I)和公式(II)：或其盐，其中R1、R2、R10、R11、R12、R13、R14、R15、R16、q和p如此处所述。公式(II)的化合物及其药物组成物是整合素抑制剂，可用于治疗某种疾病，例如由感染性因子、休克、胰腺炎或创伤引起或相关的疾病。该疾病可能包括与类风湿性关节炎或进行性家族性肝内胆汁淤积症（PFIC）相关的肺纤维化。
• Amino acid compounds and methods of use
  申请人：Pliant Therapeutics, Inc.

  公开号：US10793564B2

  公开（公告）日：2020-10-06

  The invention relates to compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).

  本发明涉及式（A）和式（I）化合物： 或其盐，其中 R1、R2、R10、R11、R12、R13、R14、R15、R16、q 和 p 如本文所述。式（A）、式（I）化合物及其药物组合物是αvβ6整合素抑制剂，可用于治疗纤维化，如特发性肺纤维化（IPF）和非特异性间质性肺炎（NSIP）。