5-甲氧基-4-甲基-3-吡啶胺 | 77903-28-7

• 物质功能分类: 医药中间体 - 吡啶类化合物
• 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: 5-甲氧基-4-甲基-3-吡啶胺
• 英文名称: 3-Amino-5-methoxy-4-methylpyridine
• 英文别名: 5-Methoxy-4-methylpyridin-3-amine
• CAS: 77903-28-7
• 化学式: C₇H₁₀N₂O
• mdl: MFCD14708216
• 分子量: 138.169
• InChiKey: ISYJOJQQEHYXFT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 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：
  48.1
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 危险等级：
  IRRITANT
• 海关编码：
  2933399090
• 危险性防范说明：
  P280,P305+P351+P338,P310
• 危险性描述：
  H302,H315,H319,H332,H335

反应信息

• 作为反应物：
  描述：

  5-甲氧基-4-甲基-3-吡啶胺 在 ferrous(II) sulfate heptahydrate 、 甲烷磺酸 、 sodium 3-nitrobenzenesulfonate 作用下， 以45%的产率得到3-甲氧基-4-甲基-1,5-萘啶
  参考文献：
  名称：

  Discovery of Azetidinyl Ketolides for the Treatment of Susceptible and Multidrug Resistant Community-Acquired Respiratory Tract Infections

  摘要：

  Respiratory tract bacterial strains are becoming increasingly resistant to currently marketed macrolide antibiotics. The current alternative telithromycin (1) from the newer ketolide class of macrolides addresses resistance but is hampered by serious safety concerns, hepatotoxicity in particular. We have discovered a novel series of azetidinyl ketolides that focus on mitigation of hepatotoxicity by minimizing hepatic turnover and time-dependent inactivation of CYP3A isoforms in the liver without compromising the potency and efficacy of 1.

  DOI：

  10.1021/jm900729s
• 作为产物：
  描述：

  3-Methoxy-5-(pivaloylamino)pyridine 在 盐酸 、 正丁基锂 、 正己烷 作用下， 反应 25.5h， 生成 5-甲氧基-4-甲基-3-吡啶胺
  参考文献：
  名称：

  Regioselective metalation of the 4-position of pyridine. New and convenient alkylation and acylation of 3-amino-5-methoxypyridine

  摘要：

  DOI：

  10.1021/jo00330a044

文献信息

• Macrolides
  申请人：Chupak S. Louis

  公开号：US20060135447A1

  公开（公告）日：2006-06-22

  Macrolide compounds per se, as shown below and defined herein, and their use, e.g., as antibacterial and antiprotozoal agents in animals, including humans: Also disclosed are methods of preparing the compounds, intermediates, and pharmaceutical compositions thereof, and methods of treating or preventing disease by administering the compounds to subjects in need. This abstract is only an excerpt and is not limiting of the invention.

  本发明涉及以下Macrolide化合物及其定义，以及它们在动物中，包括人类中作为抗菌和抗原虫剂的用途：还公开了制备这些化合物、中间体和药物组成物的方法，以及通过将这些化合物用于需要的主体治疗或预防疾病的方法。此摘要仅为摘录，不限制本发明。
• Substituted 6,7-dihydropyrazolo[1,5-a]pyrazines as negative allosteric modulators of MGLUR2 receptors
  申请人：Janssen Pharmaceutica NV

  公开号：US10005786B2

  公开（公告）日：2018-06-26

  The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of Formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.

  本发明涉及式 (I) 的新型 6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮衍生物 作为代谢型谷氨酸受体亚型 2（"mGluR2"）的负异位调节剂（NAMs）。本发明还涉及包含此类化合物的药物组合物、制备此类化合物和组合物的工艺，以及使用此类化合物和组合物预防或治疗涉及代谢型受体 mGluR2 亚型的疾病。
• 4,5-annulated 1,2,4-triazolones
  申请人：BAYER AKTIENGESELLSCHAFT

  公开号：US10968216B2

  公开（公告）日：2021-04-06

  The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

  本发明提供通式（I）的三唑酮化合物（其中 R1、R2、R3、R4 和 R5 如本文所定义）、制备所述化合物的方法、用于制备所述化合物的中间体化合物、包含所述化合物的药物组合物和组合物，以及使用所述化合物制造药物组合物，用于治疗或预防疾病，特别是过度增殖性疾病，作为单独制剂或与其他活性成分组合使用。
• A New Series of Orally Bioavailable Chemokine Receptor 9 (CCR9) Antagonists; Possible Agents for the Treatment of Inflammatory Bowel Disease
  作者：S. Barret Kalindjian、Sanjay V. Kadnur、Christopher A. Hewson、Chandregowda Venkateshappa、Suresh Juluri、Rajendra Kristam、Bheemashankar Kulkarni、Zainuddin Mohammed、Rohit Saxena、Vellarkad N. Viswanadhan、Jayashree Aiyar、Donna McVey

  DOI：10.1021/acs.jmedchem.5b01840

  日期：2016.4.14

  Chemokine receptor 9 (CCR9), a cell surface chemokine receptor which belongs to the G protein-coupled receptor, 7-trans-membrane superfamily, is expressed on lymphocytes in the circulation and is the key chemokine receptor that enables these cells to target the intestine. It has been proposed that CCR9 antagonism represents a means to prevent the aberrant immune response of inflammatory bowel disease in a localized and disease specific manner and one which is accessible to small molecule approaches. One possible reason why clinical studies with vercirnon, a prototype CCR9 antagonist, were not successful may be due to a relatively poor pharmacokinetic (PK) profile for the molecule. We wish to describe work aimed at producing new, orally active CCR9 antagonists based on the 1,3-dioxoisoindoline skeleton. This study led to a number of compounds that were potent in the nanomolar range and which, on optimization, resulted in several possible preclinical development candidates with excellent PK properties.
• TAMURA YASUMITSU; FUJITA MASANOBU; CHEN LING-CHING; INOUE MINAKO; KITA YA+, J. ORG. CHEM., 1981, 46, NO 17, 3564-3567
  作者：TAMURA YASUMITSU、 FUJITA MASANOBU、 CHEN LING-CHING、 INOUE MINAKO、 KITA YA+

  DOI：——

  日期：——