3-(甲氧基甲氧基)异烟醛 | 666234-13-5

• 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: 3-(甲氧基甲氧基)异烟醛
• 英文名称: 3-methoxymethoxypyridin-4-carbaldehyde
• 英文别名: 3-methoxymethoxypyridine-4-carbaldehyde；3-methoxymethoxypyridine-4-carboxaldehyde；3-(methoxymethoxy)isonicotinaldehyde；3-(methoxymethoxy)pyridine-4-carbaldehyde
• CAS: 666234-13-5
• 化学式: C₈H₉NO₃
• 分子量: 167.164
• InChiKey: VDGILGBFPIUZAI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  48.4
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-(甲氧基甲氧基)异烟醛 在 盐酸 作用下， 以 四氢呋喃 、 2,2,2-三氟乙醇 、 乙腈 为溶剂， 反应 2.0h， 生成 4-{[3-chloro-4-fluorophenylimino]methyl}pyridin-3-ol
  参考文献：
  名称：

  [EN] INHIBITORS OF THE KYNURENINE PATHWAY
  [FR] INHIBITEURS DE LA VOIE DE LA KYNURÉNINE

  摘要：

  本申请提供了吲哚胺2,3-双加氧酶-1和/或吲哚胺2,3-双加氧酶-2和/或色氨酸2,3-双加氧酶的新型抑制剂，以及它们的代谢物，以及药用可接受的盐或前药。还提供了制备这些化合物的方法。治疗有效量的一个或多个公式(I)的化合物可用于治疗由于色氨酸途径失调导致的疾病。公式(I)的化合物通过抑制吲哚胺2,3-双加氧酶-1和/或吲哚胺2,3-双加氧酶-2和/或色氨酸2,3-双加氧酶的酶活性或表达起作用。

  公开号：

  WO2014186035A1
• 作为产物：
  描述：

  3-羟基吡啶 在 正丁基锂 、 四甲基乙二胺 、 potassium tert-butylate 作用下， 以 四氢呋喃 、 正己烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 5.25h， 生成 3-(甲氧基甲氧基)异烟醛
  参考文献：
  名称：

  [EN] NOVEL IMINONITRILE DERIVATIVES
  [FR] NOUVEAUX DÉRIVÉS IMINONITRILE

  摘要：

  该发明涉及一种化合物，其化学式为（I），其中X1至X4和RC至RG的定义如描述和索赔中所述。化合物的化学式（I）可用作药物。

  公开号：

  WO2016027241A1

文献信息

• Novel Approach towards the Synthesis of 3,3a,4,5-Tetrahydroquinolino[4,3-<i>c</i>]isoxazole Derivatives: Application to the Preparation of Previously Unattainable 3a,4-Dihydroazabenzopyrano[4,3-<i>c</i>]isoxazole Scaffolds
  作者：Jesús Alcázar、José Manuel Alonso、José Ignacio Andrés、José Manuel Bartolomé、Javier Fernández

  DOI：10.1055/s-2005-921909

  日期：——

  A novel synthetic approach towards the preparation of 3-substituted-7,8-dimethoxy-3,3a,4,5-tetrahydroquinolino[4,3-c]isoxazole derivatives is reported. Further application of this methodology to the preparation of previously unattainable 3a,4-dihydroazabenzopyrano[4,3-c]isoxazole derivatives is also described.

  报道了一种新颖的合成方法，用于制备3-取代-7,8-二甲氧基-3,3a,4,5-四氢喹啉并[4,3-c]异噁唑衍生物。还描述了该方法在制备先前无法获得的3a,4-二氢氮苯并吡喃并[4,3-c]异噁唑衍生物中的进一步应用。
• [EN] FUSED HETEROCYCLIC ISOXAZOLINE DERIVATIVES AND THEIR USE AS ANTI-DEPRESSANTS<br/>[FR] DERIVES D'ISOXAZOLINE HETEROCYCLIQUES FUSIONNES ET LEUR UTILISATION EN TANT QU'ANTIDEPRESSEURS
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2004018483A1

  公开（公告）日：2004-03-04

  The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of the bicyclic moiety as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherein the variables are defined as in Claim 1. The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity as well as α2-adrenoceptor antagonist activity, compounds according to the invention are also suitable for treatment and/or prophylaxis in diseases where either one of the activities alone or the combination of said activities may be of therapeutic use.

  该发明涉及Formula (I)的融合杂环异氧化烷衍生物，其药学上可接受的酸或碱盐，其立体化异构体以及其N-氧化物形式，更具体地说，通过双环部分的6元环连接到杂环环系统的四氢吡喃异氧化烷，六氢异氧化烷吡啶，四氢硫代吡喃异氧化烷和六氢苯并异氧化烷衍生物，以及它们的制备方法，包含它们的制药组合物以及它们作为药物的用途，特别是用于治疗抑郁症、焦虑症、运动障碍、精神病、帕金森病和体重紊乱，包括厌食症和暴食症，其中变量的定义如权利要求书第1项所述。这些化合物被惊人地证明具有选择性的5-羟色胺（5-HT）再摄取抑制剂活性以及α2-肾上腺素受体拮抗剂活性，根据本发明的化合物也适用于治疗和/或预防在该活性之一或该活性的组合可能具有治疗用途的疾病。
• Fused heterocyclic isoxazoline derivatives and their use as anti-derpressants
  申请人：Andres-Gil Ignacio Jose

  公开号：US20060116378A1

  公开（公告）日：2006-06-01

  The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of the bicyclic moiety as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherein the variables are defined as in Claim 1. The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity as well as α 2 -adrenoceptor antagonist activity, compounds according to the invention are also suitable for treatment and/or prophylaxis in diseases where either one of the activities alone or the combination of said activities may be of therapeutic use.

  本发明涉及公式（I）的融合杂环异噁唑衍生物，其药学上可接受的酸或碱盐，其立体化异构体形式和N-氧化物形式，更具体地，通过双环基团的6元环与杂环环系统融合的四氢吡喃异噁唑，六氢异噁唑吡啶，四氢硫代吡喃异噁唑和六氢苯并异噁唑衍生物，以及其制备方法，包括它们的制药组合物和作为药物的用途，特别是用于治疗抑郁症，焦虑症，运动障碍，精神病，帕金森病和体重障碍，包括厌食症和贪食症，其中变量的定义如权利要求1所述。这些化合物已被证明具有选择性的5-羟色胺（5-HT）再摄取抑制剂活性以及α2-肾上腺素受体拮抗剂活性，根据本发明的化合物也适用于治疗和/或预防单独或联合使用这些活性可能具有治疗用途的疾病。
• INHIBITORS OF THE KYNURENINE PATHWAY
  申请人：CURADEV PHARMA PRIVATE LTD.

  公开号：US20160046596A1

  公开（公告）日：2016-02-18

  The present application provides novel inhibitors of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase, metabolites thereof, and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. A therapeutically effective amount of one or more of the compounds of formula (I) is useful in treating diseases resulting from dysregulation of the kynurenine pathway. Compounds of formula (I) act by inhibiting the enzymatic activity or expression of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase.

  本申请提供了新型的吲哚胺2,3-二氧化酶-1和/或吲哚胺2,3-二氧化酶-2和/或色氨酸2,3-二氧化酶的抑制剂、其代谢物以及药学上可接受的盐或前药。还提供了制备这些化合物的方法。公式（I）中一种或多种化合物的治疗有效量有助于治疗因酪氨酸代谢途径失调而导致的疾病。公式（I）的化合物通过抑制吲哚胺2,3-二氧化酶-1和/或吲哚胺2,3-二氧化酶-2和/或色氨酸2,3-二氧化酶的酶活性或表达来发挥作用。
• Inhibitors of the kynurenine pathway
  申请人：CURADEV PHARMA PRIVATE LTD.

  公开号：US10294212B2

  公开（公告）日：2019-05-21

  The present application provides novel inhibitors of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase, metabolites thereof, and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. A therapeutically effective amount of one or more of the compounds of formula (I) is useful in treating diseases resulting from dysregulation of the kynurenine pathway. Compounds of formula (I) act by inhibiting the enzymatic activity or expression of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxy-genase.

  本申请提供了吲哚胺 2,3-二氧合酶-1和/或吲哚胺 2,3-二氧合酶-2和/或色氨酸 2,3-二氧合酶的新型抑制剂、其代谢物及其药学上可接受的盐或原药。还提供了制备这些化合物的方法。治疗有效量的一种或多种式（I）化合物可用于治疗犬尿氨酸途径失调引起的疾病。式（I）化合物通过抑制吲哚胺 2，3-二氧合酶-1 和/或吲哚胺 2，3-二氧合酶-2 和/或色氨酸 2，3-二氧合酶的酶活性或表达发挥作用。