呋喃并[3,2-b]吡啶-2(3H)-酮 | 88011-96-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 呋喃并[3,2-b]吡啶-2(3H)-酮
• 中文别名: 呋喃并[3,2-B]吡啶-2(3H)-酮
• 英文名称: 2-oxo-2,3-dihydrofuro<3,2-b>pyridine
• 英文别名: Furo[3,2-B]pyridin-2(3H)-one；3H-furo[3,2-b]pyridin-2-one
• CAS: 88011-96-5
• 化学式: C₇H₅NO₂
• 分子量: 135.122
• InChiKey: FNPYPLBPZILBRT-UHFFFAOYSA-N

物化性质

• 熔点：
  145-146 °C
• 沸点：
  269℃
• 密度：
  1.360
• 闪点：
  116℃

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  39.2
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  呋喃并[3,2-b]吡啶-2(3H)-酮 、 乙酸酐 反应 5.0h， 生成 2-oxo-3-acetyl-2,3-dihydrofuro<3,2-b>pyridine
  参考文献：
  名称：

  Desideri; Manna; Stein, European Journal of Medicinal Chemistry, 1983, vol. 18, # 4, p. 295 - 299

  摘要：

  DOI：
• 作为产物：
  描述：

  3-acetoxypyridine-2-malononitrile 在 吡啶 、 硫酸 、 水 、 对甲苯磺酰氯 作用下， 反应 23.0h， 生成 呋喃并[3,2-b]吡啶-2(3H)-酮
  参考文献：
  名称：

  Desideri; Manna; Stein, European Journal of Medicinal Chemistry, 1983, vol. 18, # 4, p. 295 - 299

  摘要：

  DOI：

文献信息

• [EN] 3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR<br/>[FR] MODULATEURS ALLOSTÉRIQUES DE TYPE 3-(1H-PYRAZOL-4-YL)PYRIDINE DU RÉCEPTEUR MUSCARINIQUE M4 D'ACÉTYLCHOLINE
  申请人：MERCK SHARP & DOHME

  公开号：WO2019005587A1

  公开（公告）日：2019-01-03

  The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

  本发明涉及吡唑-4-基吡啶化合物，这些化合物是M4肌制酸乙酰胆碱受体的变构调节剂。本发明还涉及所述化合物在潜在治疗或预防M4肌制酸乙酰胆碱受体参与的神经和精神疾病中的用途。本发明还涉及包含这些化合物的组合物。本发明还涉及这些组合物在潜在预防或治疗M4肌制酸乙酰胆碱受体参与的疾病中的用途。
• EZH2 Inhibitors
  申请人：Mirati Therapeutics, Inc.

  公开号：US20180265517A1

  公开（公告）日：2018-09-20

  The present invention relates to compounds that inhibit EZH2 activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.

  本发明涉及抑制EZH2活性的化合物。具体地，本发明涉及化合物、药物组合物和使用方法，例如使用本发明的化合物和药物组合物治疗癌症的方法。
• [EN] 5-(PYRIDIN-3-YL)OXAZOLE ALLOSTERIC MODULATORS OF M4 MUSCARINIC ACETYLCHOLINE RECEPTOR<br/>[FR] MODULATEURS ALLOSTÉRIQUES DE 5-(PYRIDIN-3-YL)OXAZOLE DU RÉCEPTEUR MUSCARINIQUE M4 DE L'ACÉTYLCHOLINE
  申请人：MERCK SHARP & DOHME

  公开号：WO2019000238A1

  公开（公告）日：2019-01-03

  Provided are 5-(pyridin-3-yl) oxazole compounds, the compositions comprising these compounds and the uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

  提供了含有5-(吡啶-3-基)噁唑化合物的组合物，这些化合物的组合物以及这些组合物在潜在预防或治疗M4肌胆碱受体参与的疾病中的用途。
• Furanopyridine derivatives and methods of use
  申请人：Nunes J. Joseph

  公开号：US20060046977A1

  公开（公告）日：2006-03-02

  The present invention relates to furanopyridine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of modulating Lck and ACK-1 enzymes and of treating various related diseases and conditions, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, comprising administering to the mammal a therapeutically effective amount a compound of Formula I, as described above, and methods of manufacturing medicaments comprising the compound of Formula I.

  本发明涉及具有一般式I的呋喃吡啶化合物，以及其立体异构体、互变异构体、溶剂合物、药学上可接受的盐和衍生物，以及其前药。该发明还包括包含一种式I化合物的药物组合物，调节Lck和ACK-1酶的方法，以及治疗各种相关疾病和症状的方法，包括炎症、T细胞激活抑制、增殖、关节炎、器官移植、缺血或再灌注损伤、心肌梗死、中风、多发性硬化、炎症性肠病、克罗恩病、狼疮、过敏、1型糖尿病、牛皮癣、皮炎、哈希蒙氏甲状腺炎、干燥综合征、自身免疫性甲状腺功能亢进症、艾迪生病、自身免疫性疾病、肾小球肾炎、过敏性疾病、哮喘、花粉热、湿疹、癌症、结肠癌、胸腺瘤等，在哺乳动物体内，包括向哺乳动物体内施用上述式I化合物的治疗有效量，并制备包含式I化合物的药物的方法。
• Oxazole and oxadiazole cephalosporins
  申请人：Eli Lilly and Company

  公开号：US04406898A1

  公开（公告）日：1983-09-27

  Broad spectrum cephalosporin antibiotics represented by the betaine structure of the formula ##STR1## wherein R is a 5-membered amino-substituted heterocyclic containing oxygen and nitrogen; R' is e.g., hydrogen or C.sub.1 -C.sub.4 alkyl; and bicyclicpyridinium is a thienopyridinium or a furopyridinium group; are prepared by reacting a silylated 3-iodomethyl cephalosporin with a thienopyridine, e.g., thieno[2,3-b]pyridine or a furopyridine. The compounds are potent antibacterials against gram-positive and gram-negative organisms. Pharmaceutical compositions and a method for treating bacterial infections are also provided.

  以甜菜碱结构为代表的广谱头孢菌素抗生素，其化学式为##STR1##其中R是含氧和氮的5元杂环氨基取代基；R'是氢或C.sub.1-C.sub.4烷基；双环吡啶是噻吩吡啶或呋吩吡啶基团；通过将硅化的3-碘甲基头孢菌素与噻吩吡啶，例如噻吩[2,3-b]吡啶或呋吩吡啶反应制备。这些化合物对革兰氏阳性和阴性细菌都有很强的抗菌作用。还提供了制药组合物和治疗细菌感染的方法。