1-Ethyl-1,3-dihydro-2lambda6,1,3-benzothiadiazole-2,2-dione | 1835670-60-4

• 分子结构分类: 有机化合物 - 苯类化合物
• 英文名称: 1-Ethyl-1,3-dihydro-2lambda6,1,3-benzothiadiazole-2,2-dione
• 英文别名: 3-ethyl-1H-2λ6,1,3-benzothiadiazole 2,2-dioxide
• CAS: 1835670-60-4
• 化学式: C₈H₁₀N₂O₂S
• 分子量: 198.24
• InChiKey: ADAYVPNTCLDKIV-UHFFFAOYSA-N

物化性质

• 沸点：
  343.4±25.0 °C(Predicted)
• 密度：
  1.323±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  57.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Arginase Inhibitors and Their Therapeutic Applications
  申请人：OncoArendi Therapeutics S.A.

  公开号：US20170319536A1

  公开（公告）日：2017-11-09

  Disclosed are small molecule therapeutic compounds that are potent inhibitors of arginase 1 and arginase 2 activity. Also disclosed are pharmaceutical compositions comprising the compounds, and methods for using the compounds for treating or preventing a disease or condition associated with arginase activity.

  揭示了一种小分子治疗化合物，它们是较强的精氨酸酶1和精氨酸酶2活性抑制剂。还揭示了包含这些化合物的药物组合物，以及使用这些化合物治疗或预防与精氨酸酶活性相关的疾病或状况的方法。
• SUBSTITUTED AMINO TRIAZOLES USEFUL AS ACIDIC MAMMALIAN CHITINASE INHIBITORS
  申请人：OncoArendi Therapeutics Sp z o.o.

  公开号：US20160176843A1

  公开（公告）日：2016-06-23

  Disclosed are amino triazole compounds substituted by a carboxylate functional group or an bioisosteric polar functional group. Compounds having the carboxylate moiety or carboxylate bioisostere inhibit acidic mammalian chitinase. Also provided are methods of using the compounds to treat asthma reactions caused by allergens.

  本发明涉及一种带有羧酸基团或生物等构极性功能基团的氨基三唑化合物。带有羧酸基团或羧酸生物等构体的化合物能够抑制酸性哺乳动物几丁质酶。同时，本发明还提供了使用这些化合物治疗由过敏原引起的哮喘反应的方法。
• PYRIMIDINE OR PYRIDINE COMPOUNDS, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USES THEREOF
  申请人：Shanghai Shaletech Technology Co., Ltd.

  公开号：EP3216786A1

  公开（公告）日：2017-09-13

  The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).

  本发明公开了一类嘧啶或吡啶化合物、其药学上可接受的盐、立体异构体、原药和溶液、其制备方法和药物组合物及其药物用途。这些化合物可以抑制表皮生长因子受体蛋白酶的变体，从而有效抑制多种肿瘤细胞的生长。这些化合物可用于制备抗肿瘤药物，用于治疗、联合治疗或预防各种不同的癌症。这些化合物可以克服现有的第一代表皮生长因子受体抑制剂（如吉非替尼、厄洛替尼等）引起的耐药性。特别是，这些化合物可用于制备治疗或预防由表皮生长因子受体变体（如 L858R 激活突变体、Exon19 缺失激活突变体和 T790M 耐药突变体）介导的疾病、紊乱、失调或病症的药物。
• PYRIMIDINE COMPOUNDS, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USES THEREOF
  申请人：InventisBio Co., Ltd.

  公开号：EP3885344A2

  公开（公告）日：2021-09-29

  The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).

  本发明公开了一类嘧啶或吡啶化合物、其药学上可接受的盐、立体异构体、原药和溶液、其制备方法和药物组合物及其药物用途。这些化合物可以抑制表皮生长因子受体蛋白酶的变体，从而有效抑制多种肿瘤细胞的生长。这些化合物可用于制备抗肿瘤药物，用于治疗、联合治疗或预防各种不同的癌症。这些化合物可以克服现有的第一代表皮生长因子受体抑制剂（如吉非替尼、厄洛替尼等）引起的耐药性。特别是，这些化合物可用于制备治疗或预防由表皮生长因子受体变体（如 L858R 激活突变体、Exon19 缺失激活突变体和 T790M 耐药突变体）介导的疾病、紊乱、失调或病症的药物。
• Pyrimidine or pyridine compounds, preparation method therefor and pharmaceutical uses thereof
  申请人：INVENTISBIO SHANGHAI LTD.

  公开号：US10179784B2

  公开（公告）日：2019-01-15

  The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. See e.g., Formula I below. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).

  本发明公开了一类嘧啶或吡啶化合物、其药学上可接受的盐、立体异构体、原药和溶液剂、其制备方法和药物组合物及其药物用途。参见下文式 I。这些化合物可以抑制表皮生长因子受体蛋白酶的变体，因此可以有效抑制多种肿瘤细胞的生长。这些化合物可用于制备抗肿瘤药物，用于治疗、联合治疗或预防各种不同的癌症。这些化合物可以克服现有的第一代表皮生长因子受体抑制剂（如吉非替尼、厄洛替尼等）引起的耐药性。特别是，这些化合物可用于制备治疗或预防由表皮生长因子受体变体（如 L858R 激活突变体、Exon19 缺失激活突变体和 T790M 耐药突变体）介导的疾病、紊乱、失调或病症的药物。