4-methoxy-3-methyl-benzoic acid amide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-methoxy-3-methyl-benzoic acid amide
• 英文别名: 4-Methoxy-3-methyl-benzoesaeure-amid；4-Methoxy-3-methyl-benzamid；4-Methoxy-3-methylbenzamide
• 化学式: C₉H₁₁NO₂
• mdl: MFCD09600240
• 分子量: 165.192
• InChiKey: KXWRQYVEKWWYHO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.222
• 拓扑面积：
  52.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-methoxy-3-methyl-benzoic acid amide 在 potassium carbonate 作用下， 生成 4-甲氧基-3-甲基苯甲酸
  参考文献：
  名称：

  Gattermann; Hess, Justus Liebigs Annalen der Chemie, 1888, vol. 244, p. 65

  摘要：

  DOI：
• 作为产物：
  描述：

  N-甲氨基甲酰氯 、 2-甲基苯甲醚 在 二硫化碳 、 三氯化铝 作用下， 生成 4-methoxy-3-methyl-benzoic acid amide
  参考文献：
  名称：

  Gattermann; Hess, Justus Liebigs Annalen der Chemie, 1888, vol. 244, p. 65

  摘要：

  DOI：

文献信息

• [EN] 4-ETHYNYLPYRIDINE DERIVATIVES USEFUL AS GCN2 INHIBITORS<br/>[FR] DÉRIVÉS DE 4-ÉTHYNYLPYRIDINE UTILES EN TANT QU'INHIBITEURS DE GCN2
  申请人：IP2IPO INNOVATIONS LTD

  公开号：WO2021250399A1

  公开（公告）日：2021-12-16

  The invention provides compounds of formula I, wherein the substituents are as set out in further detail in the specification. The compounds are potent inhibitors of GCN2 and they have excellent pharmacokinetic properties. The compounds are useful for the treatment or prevention of a variety of conditions, particularly cancer. The invention further provides pharmaceutical compositions comprising the compounds of the invention and uses of the compounds and the compositions.

  该发明提供了公式I的化合物，其中取代基的详细设置在说明书中进一步详细说明。这些化合物是GCN2的有效抑制剂，具有优异的药代动力学性质。这些化合物可用于治疗或预防各种疾病，特别是癌症。该发明还提供了包括该发明的化合物的药物组合物以及化合物和组合物的用途。
• substituted arylamide oxazepinopyrimidone derivatives
  申请人：Sanofi-Aventis

  公开号：EP2085399A1

  公开（公告）日：2009-08-05

  A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C1-3 alkyl group, a sulphur atom, a methylene group optionally substituted by one or two groups chosen from a C1-6 alkyl group, a hydroxyl group, a C1-6 alkoxy group, a C1-2 perhalogenated alkyl group or an amino group; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted by a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R3 represents a benzene ring or a naphthalene ring; the rings being optionally substituted R4 represents a hydrogen atom or a C1-6 alkyl group; and n represents 0 to 3 and their therapeutic use.

  一种由公式(I)表示的嘧啶酮衍生物或其盐，或其溶剂化物或水合物：其中：Y代表两个氢原子，一个硫原子，一个氧原子或C1-2烷基和一个氢原子；Z代表键，一个氧原子，一个被氢原子或C1-3烷基取代的氮原子，一个硫原子，一个亚甲基基团，该基团可选地被来自C1-6烷基、羟基、C1-6烷氧基、C1-2全氟烷基或氨基的一种或两种基团取代；R1代表2、3或4-吡啶环或2、4或5-嘧啶环，该环可选地被C1-6烷基、C1-6烷氧基或卤素原子取代；R2代表氢原子、C1-6烷基或卤素原子；R3代表苯环或萘环；环可选地被取代；R4代表氢原子或C1-6烷基；n代表0至3及其治疗用途。
• Trisubstituted amine compound
  申请人：Nakamura Yoshinori

  公开号：US20090029994A1

  公开（公告）日：2009-01-29

  The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R 1 is an optionally substituted alkyl group, and the like; and R 2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.

  本发明涉及一般式(1)的化合物，其中Y是亚甲基基团等；A是可选择取代的杂环基团等；B是可选择取代的苯基团等；R1是可选择取代的烷基团等；R2是可选择取代的氨基团等；或其药学上可接受的衍生物，该化合物具有胆固醇酯转移蛋白（CETP）的抑制活性，因此可用于动脉粥样硬化疾病、高脂血症或异常脂质血症的预防和/或治疗等。
• MEDICAMENT FOR TREATMENT OF NEURODEGENERATIVE DISEASES
  申请人：MUTO Susumu

  公开号：US20080234233A1

  公开（公告）日：2008-09-25

  A medicament for preventive and/or therapeutic treatment of neurodegenerative diseases such as Alzheimer's disease or the like which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein A represents hydrogen atom or acetyl group, E represents a 2,5-di-substituted or a 3,5-di-substituted phenyl group, or a monocyclic or a fused polycyclic heteroaryl group which may be substituted, provided that the compound wherein said heteroaryl group is circle around (1)} a fused polycyclic heteroaryl group wherein the ring which binds directly to —CONH— group in the formula (I) is a benzene ring, circle around (2)} unsubstituted thiazol-2-yl group, or circle around (3)} unsubstituted benzothiazol-2-yl group is excluded, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —CONH-E wherein E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —CONH-E wherein E has the same meaning as that defined above.

  这是一种用于预防和/或治疗神经退行性疾病，如阿尔茨海默病等的药物，其包括以下通式（I）所表示的化合物中所选的一种作为活性成分，以及其药学上可接受的盐、水合物和溶剂化合物：其中，A代表氢原子或乙酰基，E代表2,5-二取代或3,5-二取代苯基，或单环或融合的多环杂环芳基，可以取代，但是当所述杂环芳基为圆圈1}在公式（I）中直接结合—CONH—基团的环为苯环，圆圈2}未取代的噻唑-2-基团，或圆圈3}未取代的苯并噻唑-2-基团时，排除在外，环Z代表一个芳烃，除了由公式—O-A所表示的基团和由公式—CONH-E所表示的基团外，还可以有一个或多个取代基，其中A具有上述定义的相同含义，E具有上述定义的相同含义，或者代表一个杂芳烃，除了由公式—O-A所表示的基团和由公式—CONH-E所表示的基团外，还可以有一个或多个取代基。
• ANTIALLERGIC AGENTS
  申请人：Muto Susumu

  公开号：US20080090779A1

  公开（公告）日：2008-04-17

  A medicament for the preventive and/or therapeutic treatment of allergic diseases and/or endometriosis and/or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above.

  一种预防和/或治疗过敏性疾病和/或子宫内膜异位症和/或子宫肌瘤的药物，其包括以下通式（I）所表示的化合物或其药学上可接受的盐、水合物和溶剂化物作为活性成分，其中X表示连接基，其主链中原子数为2至5（该连接基可以被取代），A表示氢原子或乙酰基，E表示芳基或取代的杂芳基，环Z表示苯环，除了由公式-O-A表示的基团，该苯环还可以具有一个或多个取代基团，其中A的含义与上述定义相同，而由公式-X-E表示的基团中，每个X和E的含义也与上述定义相同，或者是一个杂环，除了由公式-O-A表示的基团，该杂环还可以具有一个或多个取代基团，其中A的含义与上述定义相同，而由公式-X-E表示的基团中，每个X和E的含义也与上述定义相同。