5-amino-2-(2-pyridylmethoxy)pyridine | 200711-16-6

• 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
• 英文名称: 5-amino-2-(2-pyridylmethoxy)pyridine
• 英文别名: 6-[(pyridin-2-yl)methoxy]pyridin-3-amine；2-(pyridin-2-ylmethoxy)-5-aminopyridine；5-amino-2-(pyridin-2-ylmethoxy)pyridine；6-(pyridine-2-ylmethoxy)-pyridine-3-ylamine；5-Amino-2-(pyridin-2-ylmethyloxy)pyridine；6-(pyridin-2-ylmethoxy)pyridin-3-amine
• CAS: 200711-16-6
• 化学式: C₁₁H₁₁N₃O
• 分子量: 201.228
• InChiKey: KWCHHSFRDFQMCY-UHFFFAOYSA-N

物化性质

• 沸点：
  392.5±32.0 °C(Predicted)
• 密度：
  1.235±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  61
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-amino-2-(2-pyridylmethoxy)pyridine 在 三乙胺 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 2.0h， 生成 5-Bromo-1-[2-(pyridin-2-ylmethyloxy)pyridin-5-ylcarbamoyl]-indoline
  参考文献：
  名称：

  1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists

  摘要：

  Bisarylmethoxyethers have been identified with nanomolar 5-HT2C affinity and selectivity over both 5-HT2A and 5-HT2B receptors. Compounds such as 1, 2, 8, 12, 14 and 18 have potent oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function and their therapeutic potential is currently under further investigation. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00365-6
• 作为产物：
  描述：

  2-羟基-5-硝基吡啶 在 铁粉 、 sodium hydride 、 溶剂黄146 、 三氯氧磷 作用下， 以 甲醇 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 1.33h， 生成 5-amino-2-(2-pyridylmethoxy)pyridine
  参考文献：
  名称：

  Structure-Based Ligand Design of Novel Bacterial RNA Polymerase Inhibitors

  摘要：

  Bacterial RNA polymerase (RNAP) is essential for transcription and is an antibacterial target for small molecule inhibitors. The binding region of myxopyronin B (MyxB), a bacterial RNAP inhibitor, offers the possibility of new inhibitor design. The molecular design program SPROUT has been used in conjunction with the X-ray cocrystal structure of Thermus thermophilus RNAP with MyxB to design novel inhibitors based on a substituted pyridyl-benzamide scaffold. A series of molecules, with molecular masses <350 Da, have been prepared using a simple synthetic approach. A number of these compounds inhibited Escherichia coli RNAP.

  DOI：

  10.1021/ml200087m

文献信息

• NOVEL INDOL CARBOXYLIC ACID BISPYRIDYL CARBOXAMIDE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD AND COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT
  申请人：SEONG Churlmin

  公开号：US20090258876A1

  公开（公告）日：2009-10-15

  Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT 2c receptors, act selectively on the 5-HT 2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT 2c receptors.

  本公开涉及一种新的吲哚羧酸双吡啶羧酰胺衍生物，其制备方法，以及包含该衍生物作为活性成分的用于预防或治疗肥胖、泌尿系统疾病和中枢神经系统疾病的组合物。根据本发明的吲哚羧酸双吡啶羧酰胺衍生物具有高亲和力5-HT2c受体，对5-HT2c受体选择性作用，这些衍生物很少出现由其他受体引起的不良反应。由于这些衍生物有效抑制5-羟色胺活性，它们可能对治疗或预防肥胖；泌尿系统疾病，如尿失禁、早泄、勃起功能障碍和前列腺增生；以及与5-HT2c受体相关的中枢神经系统疾病，如抑郁症、焦虑症、关注症、恐慌症、癫痫、强迫症、偏头痛、睡眠障碍、戒毒、阿尔茨海默病和精神分裂症可能有用。
• Hydroxyformamidine derivatives and medicines containing the same
  申请人：——

  公开号：US20030186979A1

  公开（公告）日：2003-10-02

  Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or participates in causing cell proliferation are provided. The present invention relates to hydroxyamidine compounds represented by the formula: 1 wherein R 1 represents a group represented by the formula: R 2 —(CH 2 ) m — (wherein R 2 represents a C 3-8 cycloalkyl group, a C 2-6 alkoxycarbonyl group, a C 2-10 alkenyl group, a C 2-6 alkynyl group, a substituted or non-substituted aryl group, or the like, and m is an integer of 1 to 8), a group represented by the formula: R 3 -A- (wherein R 3 represents a hydrogen atom, a C 1-6 alkoxy group, a C 3-8 cycloalkoxy group, or the like, and A represents a straight-chain C 2-10 alkylene group which may be substituted with a C 1-6 alkyl group or a trifluoromethyl group), or a C 3-8 cycloalkyl group, and X represents an oxygen atom or a sulfur atom, or pharmaceutically acceptable salts thereof, and relates to medicines including the same as active ingredients.

  本发明提供了用于抑制20-HETE产生的药物，20-HETE参与肾脏和脑血管等主要器官的微血管收缩或扩张，或参与细胞增殖的过程。本发明涉及由以下式子表示的羟基胺化合物：1其中R1表示以下式子表示的基团：R2—(CH2)m—（其中R2表示C3-8环烷基，C2-6烷氧羰基基团，C2-10烯基基团，C2-6炔基基团，取代或未取代的芳基团等，m为1至8的整数），以下式子表示的基团：R3-A-（其中R3表示氢原子，C1-6烷氧基基团，C3-8环烷氧基基团等，A表示直链C2-10烷基基团，该基团可以被C1-6烷基基团或三氟甲基基团取代），或C3-8环烷基，X表示氧原子或硫原子，或其药学上可接受的盐，并涉及将其作为活性成分的药物。
• [EN] INDOLINE DERIVATIVES USEFUL AS 5-HT-2C RECEPTOR ANTAGONISTS<br/>[FR] DERIVES DE L'INDOLINE UTILES COMME ANTAGONISTES DES RECEPTEURS 5HT-2C
  申请人：SMITHKLINE BEECHAM PLC

  公开号：WO1997048700A1

  公开（公告）日：1997-12-24

  (EN) The invention relates to heterocyclic compounds of formula (I) or a salt thereof wherein R1 is hydrogen or C1-6 alkyl; R2, R3 and R4 groups are independently hydrogen, halogen or C1-6 alkyl optionally substituted by one or more fluorine atoms, having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders such as anxiety.(FR) L'invention concerne des composés hétérocycliques de formule (I), dans laquelle R1 est hydrogène ou alkyle C1-C6, et les groupes R2, R3 et R4 sont indépendamment hydrogène, halogène ou alkyle C1-C6 éventuellement substitués par un ou plusieurs atomes de fluor, et leurs sels, ces composés ayant une activité pharmacologique. L'invention concerne également des procédés permettant de les préparer et des compositions les contenant, ainsi que leur utilisation dans le traitement des troubles du système nerveux central tels que l'angoisse.

  本发明涉及式（I）的杂环化合物或其盐，其中R1是氢或C1-6烷基；R2、R3和R4基团独立地是氢、卤素或C1-6烷基，可选地被一个或多个氟原子取代，具有药理活性，还涉及其制备方法、含有它们的组合物以及它们在治疗中枢神经系统疾病如焦虑症中的使用。
• Indoline derivatives useful as 5-HT-2C receptor antagonists
  申请人：SmithKline Beecham p.l.c.

  公开号：US20020035134A1

  公开（公告）日：2002-03-21

  The invention relates to heterocyclic compounds of formula (I) or a salt thereof wherein R 1 is hydrogen or C 1-6 alkyl; R 2 , R 3 and R 4 groups are independently hydrogen, halogen or C 1-6 alkyl optionally substituted by one or more fluorine atoms, having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders such as anxiety. 1

  本发明涉及式（I）的杂环化合物或其盐，其中R1为氢或C1-6烷基；R2、R3和R4基团独立地为氢、卤素或C1-6烷基，可选地被一个或多个氟原子取代，具有药理活性，制备它们的方法，包含它们的组合物以及它们在治疗中枢神经系统障碍（如焦虑症）中的用途。
• [EN] ISOINDOLINONE COMPOUNDS AND IMAGING AGENTS FOR IMAGING HUNTINGTIN PROTEIN<br/>[FR] COMPOSÉS D'ISOINDOLINONE ET AGENTS D'IMAGERIE POUR L'IMAGERIE DE LA PROTÉINE HUNTINGTINE
  申请人：CHDI FOUNDATION INC

  公开号：WO2022216947A1

  公开（公告）日：2022-10-13

  Provided herein are certain isoindolinone compounds and imaging agents useful for detecting a disease or condition associated with protein aggregation, compositions thereof, and methods of their use.

  本文提供了某些异吲哚啉酮化合物和成像剂，用于检测与蛋白质聚集相关的疾病或病况，以及它们的组成物和使用方法。