4-(4-bromo-3,5-dimethylphenyl)-1-methylpyridin-2(1H)-one | 1458655-18-9

• 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: 4-(4-bromo-3,5-dimethylphenyl)-1-methylpyridin-2(1H)-one
• 英文别名: 4-(4-bromo-3,5-dimethylphenyl)-1-methylpyridin-2-one
• CAS: 1458655-18-9
• 化学式: C₁₄H₁₄BrNO
• 分子量: 292.175
• InChiKey: BDFHBJTUUNVKBZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  {(S)-6-[(R)-7-fluoro-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)indan-1-yloxy]-2,3-dihydrobenzofuran-3-yl}acetic acid methyl ester 、 4-(4-bromo-3,5-dimethylphenyl)-1-methylpyridin-2(1H)-one 、 {(S)-6-[(R)-4-bromo-7-fluoro-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid methyl ester 生成 methyl 2-((S)-6-((R)-4-(2,6-dimethyl-4-(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl)-7-fluoro-2,3-dihydro-1H-inden-1-yloxy)-2,3-dihydrobenzofuran-3-yl)acetate
  参考文献：
  名称：

  Indanyloxydihydrobenzofuranylacetic acids

  摘要：

  本发明涉及一般式I的化合物，其中R1、R2和m基团的定义如权利要求1中所述，具有有价值的药理学特性，特别是与GPR40受体结合并调节其活性。这些化合物适用于治疗和预防可以受该受体影响的疾病，例如代谢性疾病，特别是2型糖尿病。

  公开号：

  US08642585B2
• 作为产物：
  描述：

  2-溴-5-碘-1,3-二甲苯 、 B-(1,2-二氢-1-甲基-2-氧代-4-吡啶)硼酸 、 生成 4-(4-bromo-3,5-dimethylphenyl)-1-methylpyridin-2(1H)-one
  参考文献：
  名称：

  Indanyloxydihydrobenzofuranylacetic acids

  摘要：

  本发明涉及一般式I的化合物，其中R1、R2和m基团的定义如权利要求1中所述，具有有价值的药理学特性，特别是与GPR40受体结合并调节其活性。这些化合物适用于治疗和预防可以受该受体影响的疾病，例如代谢性疾病，特别是2型糖尿病。

  公开号：

  US08642585B2

文献信息

• NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACIDS
  申请人：ECKHARDT Matthias

  公开号：US20130252937A1

  公开（公告）日：2013-09-26

  The present invention relates to compounds of general formula I, wherein the groups R 1 , R 2 and m are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

  本发明涉及一般式I的化合物， 其中基团R 1 ，R 2 和m如权利要求中所定义， 具有有价值的药理特性，特别是结合GPR40受体并调节其活性。这些化合物适用于治疗和预防受该受体影响的疾病，如代谢性疾病，特别是2型糖尿病。
• [EN] NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACID DERIVATIVES AND THEIR USE AS GPR40 RECEPTOR AGONISTS<br/>[FR] NOUVEAUX DÉRIVÉS D'ACIDE INDANYLOXYDIHYDROBENZOFURANNYLACÉTIQUE ET LEUR UTILISATION COMME AGONISTES DU RÉCEPTEUR GPR40
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2013144098A1

  公开（公告）日：2013-10-03

  The present invention relates to compounds of general formula (I), wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

  本发明涉及一般式(I)的化合物，其中基团R1、R2和m的定义如权利要求书中所述，这些化合物具有有价值的药理特性，特别是与GPR40受体结合并调节其活性。这些化合物适用于治疗和预防受该受体影响的疾病，如代谢性疾病，特别是2型糖尿病。
• [EN] INDANYLAMINOAZADIHYDROBENZOFURANYLACETIC ACIDS, PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF DIABETES<br/>[FR] ACIDES INDANYLAMINOAZADIHYDROBENZOFURANYLACÉTIQUES, COMPOSITIONS PHARMACEUTIQUES POUR LE TRAITEMENT DU DIABÈTE
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2018146008A1

  公开（公告）日：2018-08-16

  The present invention relates to compounds of general formula (I), wherein the groups R, R1, R2, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula (I).

  本发明涉及一般式（I）的化合物，其中R、R1、R2、m和n组分的定义如权利要求书1所述，该化合物具有有价值的药理特性，特别是与GPR40受体结合并调节其活性。该化合物适用于治疗和预防可以受到该受体影响的疾病，例如代谢性疾病，特别是2型糖尿病。此外，本发明涉及新的中间体，用于合成式（I）的化合物。
• Pyrazole Compounds for Controlling Invertebrate Pests
  申请人：Soergel Sebastian

  公开号：US20130253012A1

  公开（公告）日：2013-09-26

  The present invention relates to a method for controlling invertebrate pests, in particular arthropod pests and nematodes, by using pyrazole compounds of formula I and the salts thereof, the tautomers thereof, the N-oxides thereof and the salts of the tautomers or N-oxides thereof, wherein X is N or CH, Y is N or CH, Z is N or CH, provided that either only one of X, Y and Z is N or only two adjacent groups of X, Y and Z are N; and wherein Q is a bivalent 5- or 6-membered carbocyclic radical or a 5- or 6-membered heterocyclic radical having one heteroatom moiety which is selected from the group consisting of O, S, N or N—R QN as ring member and 0, 1 or 2 further heteroatom moieties N as ring members, wherein 0, 1, 2 or 3 of the ring members that are carbon atoms may carry a radical R Q , provided that the pyrazole radical and the 6-membered heteroaromatic radical are bound in ortho- or meta-position of Q with respect to each other, if Q is a 6-membered radical; and wherein R A , if present, is C 1 -C 3 -alkyl, C 1 -C 3 -haloalkyl or the like; n is 0, 1 or 2; R N is C 1 -C 3 -alkyl, C 1 -C 2 -haloalkyl, C 1 -C 2 -alkoxy-C 1 -C 2 -alkyl or the like; R t and R u are independently of each other selected from hydrogen, methyl and the like; R QN is hydrogen, C 1 -C 4 -alkyl or the like; R Q is hydrogen, halogen, C 1 -C 4 -alkyl or the like. The present invention further relates to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound of formula I, their salts or N-oxides, and to pyrazole compounds of formula I.

  本发明涉及一种使用式I的吡唑化合物及其盐、互变异构体、N-氧化物及其互变异构体或N-氧化物的盐，控制无脊椎动物害虫，特别是节肢动物害虫和线虫的方法，其中X为N或CH，Y为N或CH，Z为N或CH，只有X、Y和Z中的一个是N或仅有相邻的两个X、Y和Z中的一个是N；Q为二价的5-或6-成员的碳环或一个5-或6-成员的杂环基团，其中一个杂原子基团被选择为O、S、N或N-RQ，作为环成员，0、1或2个进一步的杂原子基团N作为环成员，其中0、1、2或3个是碳原子的环成员可能携带一个基团RQ，只要吡唑基团和6-成员杂环芳基团在Q的正交或间位于彼此相对位置，如果Q是6-成员基团；RA如果存在，则为C1-C3烷基、C1-C3卤代烷基或类似物；n为0、1或2；RN为C1-C3烷基、C1-C2卤代烷基、C1-C2-烷氧基-C1-C2-烷基或类似物；Rt和Ru独立地选择自氢、甲基等；RQN为氢、C1-C4烷基或类似物；RQ为氢、卤素、C1-C4烷基或类似物。本发明还涉及一种保护植物繁殖材料和/或从中生长的植物的方法，包括至少一种式I化合物、它们的盐或N-氧化物，以及式I的吡唑化合物的植物繁殖材料。
• Indanylaminoazadihydrobenzofuranylacetic acids, pharmaceutical compositions for the treatment of diabetes
  申请人：Boehringer Ingelheim International GmbH

  公开号：US10550127B1

  公开（公告）日：2020-02-04

  The present invention relates to compounds of general formula I, wherein the groups R, R1, R2, m and n are defined herein, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

  本发明涉及通式 I 的化合物、 其中基团 R、R1、R2、m 和 n 在此定义，它们具有重要的药理特性，特别是能与 GPR40 受体结合并调节其活性。这些化合物适用于治疗和预防受该受体影响的疾病，如代谢性疾病，特别是 2 型糖尿病。此外，本发明还涉及可用于合成式 I 化合物的新型中间体。