3-氟-2-甲氧基-6-甲基吡啶 | 375368-80-2

• 物质功能分类: 医药中间体 - 杂环化合物 - 吡啶类化合物
• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 3-氟-2-甲氧基-6-甲基吡啶
• 英文名称: 3-fluoro-2-methoxy-6-methylpyridine
• CAS: 375368-80-2
• 化学式: C₇H₈FNO
• mdl: MFCD03095083
• 分子量: 141.145
• InChiKey: DAQMWRIPXIPMAA-UHFFFAOYSA-N

物化性质

• 沸点：
  158.9±35.0 °C(Predicted)
• 密度：
  1?+-.0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.285
• 拓扑面积：
  22.1
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 危险性防范说明：
  P305+P351+P338
• 危险性描述：
  H227,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  3-氟-2-甲氧基-6-甲基吡啶 在 N-溴代丁二酰亚胺(NBS) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 以66.9%的产率得到3-bromo-5-fluoro-6-methoxy-2-methylpyridine
  参考文献：
  名称：

  [EN] 2,3-DIHYDROQUINAZOLIN COMPOUNDS AS NAV1.8 INHIBITORS
  [FR] COMPOSÉS 2,3-DIHYDROQUINAZOLINE EN TANT QU'INHIBITEURS DE NAV1.8

  摘要：

  本发明涉及Nav1.8抑制剂2,3-二氢喹唑啉化合物，其化学公式为(X)；其中Y'、X'、B'、R1'、R2'、R3'、R5'、R6'、R7'和z1如本文所述定义；或其药用可接受的盐或互变异构体形式，相应的药物组合物或制剂，化合物制备的方法或过程，方法，化合物用于，用于治疗疼痛和/或与疼痛相关的或相关的疾病、失调或状况的使用和/或联合治疗方法。

  公开号：

  WO2020261114A1

文献信息

• [EN] 5-AMINO-8-(4-PYRIDYL)-[1,2,4]TRIAZOLO[4,3-C]PYRIMIDIN-3-ONE COMPOUNDS FOR USE AGAINST CANCER<br/>[FR] COMPOSÉS DE 5-AMINO-8-(4-FLUOROPHÉNYL)-[1,2,4]TRIAZOLO [4,3-C]PYRIMIDIN-3-ONE DESTINÉS À ÊTRE UTILISÉS CONTRE LE CANCER
  申请人：ASTRAZENECA AB

  公开号：WO2021191379A1

  公开（公告）日：2021-09-30

  Described herein are triazalone compounds of Formula (I): and pharmaceutically acceptable salts thereof. Methods of making and using compounds of Formula (I) are also described. Compounds of Formula (I) and pharmaceutically acceptable salts thereof can be useful as adenosine receptor antagonists, for example in the treatment of diseases or conditions mediated by the adenosine receptor, such as cancer, movement disorders, or attention disorders.

  本文描述了式（I）的三唑酮化合物及其药学上可接受的盐。还描述了制备和使用式（I）化合物的方法。式（I）的化合物及其药学上可接受的盐可用作腺苷受体拮抗剂，例如在治疗由腺苷受体介导的疾病或症状，如癌症、运动障碍或注意障碍方面。
• 8-AZABICYCLO[3.2.1]OCTANE-8-CARBOXAMIDE DERIVATIVE
  申请人：Horiuchi Yoshihiro

  公开号：US20120225876A1

  公开（公告）日：2012-09-06

  Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof (In the formula, A represents a group that is represented by formula (A-1); R 1a and R 1b may be the same or different and each independently represents a C 1-6 alkyl group which may be substituted by one to three halogen atoms; m and n each independently represents an integer of 0-5; X 1 represents a hydroxyl group or an aminocarbonyl group; Z 1 represents a single bond or the like; and R 2 represents an optionally substituted C 1-6 alkyl group, an optionally substituted C 6-10 aryl group or the like.)

  公开了一种由公式(1)表示的化合物或其药理可接受的盐(在公式中，A代表由公式(A-1)表示的基团；R1a和R1b可以相同或不同，每个独立地表示一个可以由一个到三个卤素原子取代的C1-6烷基；m和n各自独立地表示0-5之间的整数；X1代表羟基或氨基甲酰基；Z1代表单键等；R2代表一个可选地取代的C1-6烷基，一个可选地取代的C6-10芳基等)。
• [EN] COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH APJ RECEPTOR ACTIVITY<br/>[FR] COMPOSÉS ET COMPOSITIONS DESTINÉS AU TRAITEMENT D'ÉTATS PATHOLOGIQUES ASSOCIÉS À UNE ACTIVITÉ DU RÉCEPTEUR DE L'APJ
  申请人：ANNAPURNA BIO INC

  公开号：WO2019169193A1

  公开（公告）日：2019-09-06

  This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor; gene symbol "APLNR"). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition. Non-limiting examples of such diseases, disorders, or conditions include: (i) cardiovascular disease; (ii) metabolic disorders; (iii) diseases, disorders, and conditions associated with vascular pathology; and (iv) organ failure; (v) diseases, disorders, and conditions associated with infections (e.g., microbial infections); and (vi) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular non-limiting examples of such diseases, disorders, or conditions include pulmonary hypertension (e.g., PAH); heart failure; type II diabetes; renal failure; sepsis; and systemic hypertension.

  本公开涉及化学实体（例如，化合物或药学上可接受的盐和/或水合物和/或化合物的前药），其调节（例如，激活）apelin受体（在此处也称为APJ受体；基因符号“APLNR”）。本公开还涉及含有相同化学实体的组合物，以及使用和制备相同的其他方法。这些化学实体可用于治疗患有减少APJ受体活性（例如，抑制或受损的APJ受体信号传导；例如，抑制或受损的apelin-APJ受体信号传导）或内源性apelin下调导致疾病、障碍或病症的主体（例如，人类）。此类疾病、障碍或病症的非限定示例包括：（i）心血管疾病；（ii）代谢紊乱；（iii）与血管病变相关的疾病、障碍和病症；（iv）器官功能衰竭；（v）与感染（例如，微生物感染）相关的疾病、障碍和病症；以及（vi）与前述任何疾病、障碍或病症或在此处公开的任何疾病、障碍或病症并发或合并的疾病、障碍或病症。此类疾病、障碍或病症的更为具体的非限定示例包括肺动脉高压（例如，PAH）；心力衰竭；2型糖尿病；肾功能衰竭；败血症；和全身性高血压。
• [EN] 3-HYDROXYOXINDOLE DERIVATIVES AS CRHR2 ANTAGONIST<br/>[FR] DÉRIVÉS DE 3-HYDROXYOXINDOLE UTILES EN TANT QU'ANTAGONISTES DU CRHR2
  申请人：RAQUALIA PHARMA INC

  公开号：WO2022071484A1

  公开（公告）日：2022-04-07

  The present invention relates to 3-hydroxyoxindole derivatives which have antagonistic activities against CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR2 is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CRHR2 is involved.

  本发明涉及具有对CRHR2拮抗活性的3-羟基氧吲哚衍生物，用于治疗或预防涉及CRHR2的疾病和疾病。该发明还涉及包含这些化合物的药物组合物以及在预防或治疗涉及CRHR2的这些疾病中使用这些化合物和组合物。
• TRIAZOLE DERIVATIVE OR A SALT THEREOF
  申请人：Yoshimura Seiji

  公开号：US20090082367A1

  公开（公告）日：2009-03-26

  [Problem] To provide a compound which may be used in treating diseases in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is concerned, especially diabetes and insulin resistance. [Means for Solution] It was found that a triazole derivative or a pharmaceutically acceptable salt thereof, in which the 3-position of triazole ring is substituted with a trisubstituted methyl group and the 5-position is substituted with a lower alkyl, cycloalkyl or the like, has a strong 11β-HSD1-inhibitory activity. In addition, since the triazole derivative of the present invention shows excellent blood glucose-lowering action, it may be used in the treatment of diabetes and insulin resistance.

  [问题] 提供一种可用于治疗11β-羟基类固醇脱氢酶1型（11β-HSD1）相关疾病，尤其是糖尿病和胰岛素抵抗的化合物。[解决方案] 发现三唑衍生物或其药学上可接受的盐，其中三唑环的3位被三取代甲基基团取代，5位被较低的烷基，环烷基或类似物取代，具有强烈的11β-HSD1抑制活性。此外，由于本发明的三唑衍生物显示出优异的降低血糖作用，因此可用于治疗糖尿病和胰岛素抵抗。