2-Chloro-6-methoxy-3-methyl-5-nitropyridine

• 分子结构分类: 有机化合物 - 有机1,3-偶极化合物 - 烯丙基型1,3-偶极有机化合物
• 英文名称: 2-Chloro-6-methoxy-3-methyl-5-nitropyridine
• 英文别名: 2-chloro-6-methoxy-3-methyl-5-nitropyridine
• 化学式: C7H7ClN2O3
• 分子量: 202.59
• InChiKey: NXUBYBOIURHPJO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  67.9
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• [EN] NEW 6-MEMBERED HETEROAROMATIC SUBSTITUTED CYANOINDOLINE DERIVATIVES AS NIK INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS DE CYANOINDOLINE À SUBSTITUTION HÉTÉROAROMATIQUE À 6 CHAÎNONS UTILISÉS COMME INHIBITEURS DE NIK
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2017125534A1

  公开（公告）日：2017-07-27

  The present invention relates to pharmaceutical agents of formula (I), useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-KB-inducing kinase (NIK - also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.

  本发明涉及公式（I）的药物制剂，用于治疗和/或预防哺乳动物，特别是用于治疗癌症、炎症性疾病、代谢性疾病和自身免疫性疾病的NF-KB诱导激酶（NIK - 也称为MAP3K14）抑制剂。该发明还涉及包含这些化合物的药物组合物，以及利用这些化合物或药物组合物预防或治疗癌症、炎症性疾病、包括肥胖和糖尿病在内的代谢性疾病以及自身免疫性疾病的用途。
• 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors
  申请人：Janssen Pharmaceutica NV

  公开号：US11001569B2

  公开（公告）日：2021-05-11

  The present invention relates to pharmaceutical agents of formula (I), useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as a cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.

  本发明涉及式(I)的药物制剂，可用于哺乳动物的治疗和/或预防，尤其涉及NF-κB诱导激酶（NIK-又称MAP3K14）的抑制剂，可用于治疗癌症、炎症性疾病、代谢性疾病和自身免疫性疾病等疾病。本发明还涉及包含此类化合物的药物组合物，以及使用此类化合物或药物组合物预防或治疗癌症、炎症性疾病、代谢紊乱（包括肥胖和糖尿病）和自身免疫性疾病等疾病。
• [EN] EGFR INHIBITOR AND APPLICATION THEREOF<br/>[FR] INHIBITEUR D'EGFR ET SON UTILISATION<br/>[ZH] EGFR抑制剂及其应用
  申请人：JIANGSU SIMCERE PHARM CO LTD

  公开号：WO2020216371A1

  公开（公告）日：2020-10-29

  本发明涉及作为第四代(T790M/C797S突变)EGFR激酶抑制剂及其医药用途，具体公开了式(I)所示化合物或其药学上可接受的盐。本发明化合物在EGFR Del19/T790M/C797S和L858R/T790M/C797S异常突变引起的疾病上有着较好的疗效。
• [EN] PYRIMIDINE DERIVATIVE HAVING PROTEIN KINASE INHIBITORY ACTIVITY, AND THERAPEUTIC PHARMACEUTICAL COMPOSITION COMPRISING SAME<br/>[FR] DÉRIVÉ DE PYRIMIDINE AYANT UNE ACTIVITÉ INHIBITRICE DE PROTÉINE KINASE, ET COMPOSITION PHARMACEUTIQUE THÉRAPEUTIQUE LE COMPRENANT<br/>[KO] 단백질 키나아제 저해 활성을 갖는 피리미딘 유도체 및 이를 포함하는 치료용 약학 조성물
  申请人：[en]THERAPEX CO., LTD.;[ko]주식회사 테라펙스

  公开号：WO2022211573A1

  公开（公告）日：2022-10-06

  본 발명은 EGFR을 포함한 단백질 키나아제 저해활성을 갖는 신규 삼치환된 피리미딘 유도체와 이의 약학적으로 허용된 염을 유효성분으로 함유하는 비정상 세포 성장으로 유발되는, 폐암을 포함한 암 질환의 예방 및 치료용 약학적 조성물에 관한 것이다. 본 발명의 신규 화합물의 단백질 키나아제 저해 활성은 우수하다. 특히, 본 발명의 신규 화합물은 약물 내성을 갖는 다양한 EGFR 돌연변이종 (exon 19 deletion-T790M-C797S-EGFR, L858R-T790M-C797S-EGFR, exon 19 deletion-T790M-EGFR 및 L858R-T790M-EGFR을 포함하는 EGFR 돌연변이종들)들에 대하여 우수한 억제 효과를 보유하고 있으며, 이들 EGFR 돌연변이종들에 의해서 유발되는 암 질환의 예방 및 치료제로서 유용하다.