[S-(R*,R*)]-Azepane-1-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环庚烷
• 英文名称: [S-(R*,R*)]-Azepane-1-carboxylic acid
• 英文别名: (S)-Azepane-1-carboxylic acid；azepane carboxylic acid；hexahydro-(1H)-azepine carboxylic acid；Azepane-1-carboxylic Acid
• 化学式: C₇H₁₃NO₂
• 分子量: 143.186
• InChiKey: MEOZFUYXLCDYGA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] FUSED TRICYCLIC BENZIMIDAZOLES DERIVATIVES AS MODULATORS OF TNF ACTIVITY<br/>[FR] DÉRIVÉS BENZIMIDAZOLES TRICYCLIQUES CONDENSÉS COMME MODULATEURS DE L'ACTIVITÉ DU TNF
  申请人：UCB BIOPHARMA SPRL

  公开号：WO2015086525A1

  公开（公告）日：2015-06-18

  A series of tricyclic benzimidazole derivatives, in particular dihydro-1H- imidazo [1,2-a]benzimidazo le, dihydro-1H-pyrrolo [1,2-a]benzimidazo le, dihydro-1H- pyrazino[1,2-a]benzimidazole, dihydro-1H-[1,4]oxazino[4,3-a]benzimidazole and dihydrothiazolo[3,4-a]benzimidazolem, and analogues thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

  一系列的三环苯并咪唑衍生物，特别是二氢-1H-咪唑[1,2-a]苯并咪唑、二氢-1H-吡咯[1,2-a]苯并咪唑、二氢-1H-吡嗪[1,2-a]苯并咪唑、二氢-1H-[1,4]恶嗪[4,3-a]苯并咪唑和二氢噻唑[3,4-a]苯并咪唑及其类似物，作为人类肿瘤坏死因子α活性的强效调节剂，因此在治疗和/或预防各种人类疾病中具有益处，包括自身免疫和炎症性疾病；神经学和神经退行性疾病；疼痛和痛觉障碍；心血管疾病；代谢性疾病；眼科疾病；以及肿瘤学疾病。
• [EN] IMIDAZOPYRIDINE DERIVATIVES AS MODULATORS OF TNF ACTIVITY<br/>[FR] DÉRIVÉS D'IMIDAZOPYRIDINE UTILISABLES EN TANT QUE MODULATEURS DE L'ACTIVITÉ TNF
  申请人：UCB PHARMA SA

  公开号：WO2014009295A1

  公开（公告）日：2014-01-16

  A series of imidazo[l,2-a]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

  一系列式(I)的咪唑并[1,2-a]吡啶衍生物，作为人类TNFa活性的有效调节剂，因此在治疗和/或预防各种人类疾病方面具有益处，包括自身免疫和炎症性疾病；神经学和神经退行性疾病；疼痛和伤害感知性疾病；心血管疾病；代谢性疾病；眼科疾病；以及肿瘤学疾病。
• [EN] SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1<br/>[FR] PYRIDINES SUBSTITUÉES EN TANT QU'INHIBITEURS DE DNMT1
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2017216726A1

  公开（公告）日：2017-12-21

  The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

  该发明涉及取代吡啶衍生物。具体而言，该发明涉及符合以下式（Iar）的化合物：（Iar）其中Yar、X1ar、X2ar、R1ar、R2ar、R3ar、R4ar和R5ar如本文所定义；或其药学上可接受的盐或前药。该发明的化合物是DNMT1的选择性抑制剂，可用于治疗癌症、癌前综合征、β血红蛋白病、镰状细胞病、镰状细胞贫血、β地中海贫血以及与DNMT1抑制相关的疾病。因此，该发明进一步涉及包含该发明化合物的药物组合物。该发明还进一步涉及使用该发明化合物或包含该发明化合物的药物组合物抑制DNMT1活性和治疗相关疾病的方法。
• HETEROCYCLIC COMPOUND
  申请人：TAKEDA PHARMACEUTICAL COMPANY LIMITED

  公开号：US20160159773A1

  公开（公告）日：2016-06-09

  The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.

  本发明提供了一种用于预防或治疗自身免疫性疾病（例如牛皮癣、类风湿关节炎、炎症性肠病、干燥综合征、贝赫切特病、多发性硬化症、系统性红斑狼疮等）等的药剂，其具有优越的Tyk2抑制作用。 本发明涉及一种由下式表示的化合物 其中每个符号如规范中定义的，或其盐。
• [EN] COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES<br/>[FR] COMPOSÉS, SELS CORRESPONDANTS ET MÉTHODES POUR LE TRAITEMENT DE MALADIES
  申请人：ACADIA PHARM INC

  公开号：WO2019040107A1

  公开（公告）日：2019-02-28

  The present disclosure relates to compounds according to Formula (I), useful for treating diseases.

  本公开涉及按照式（I）的化合物，用于治疗疾病。