N-(4'-bromo-biphenyl-3-yl)-acetamide | 860745-57-9

• 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: N-(4'-bromo-biphenyl-3-yl)-acetamide
• 英文别名: N-(4'-Brom-biphenyl-3-yl)-acetamid；4'-Brom-3-acetamino-diphenyl；4-bromo-3'-acetylamino-biphenyl；N-[3-(4-bromophenyl)phenyl]acetamide
• CAS: 860745-57-9
• 化学式: C₁₄H₁₂BrNO
• 分子量: 290.159
• InChiKey: FWYPBHSIQGOIBG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  N-(4'-bromo-biphenyl-3-yl)-acetamide 生成 4'-Bromo-4-nitro-biphenyl-3-ylamine
  参考文献：
  名称：

  联苯系列中的取代基效应。第四部分 4'-取代的3-溴-4-硝基联苯的哌啶脱溴反应动力学

  摘要：

  已经制备了一系列的4'-取代的3-溴-4-硝基联苯，并且已经测量了在三个不同温度下在甲醇中哌啶基溴化的速率。动力学数据是由改性哈米特关系令人满意相关（ρ+ 0.35），使用σ p为4'-卤素和σ常数p + 0.32（σ - -σ p）为强吸电子4'-取代基（梅科，内消旋2和NO 2）。与先前报道的在相应的3'-和4'-取代的3-硝基-4-溴代二苯上进行相同反应的结果进行了比较。

  DOI：

  10.1039/p29770000137
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 吡啶 作用下， 生成 N-(4'-bromo-biphenyl-3-yl)-acetamide
  参考文献：
  名称：

  Blakey; Scarborough, Journal of the Chemical Society, 1927, p. 3006

  摘要：

  DOI：

文献信息

• Trisubstituted Benzotriazole Derivatives as Dihydroorotate Oxygenase Inhibitors
  申请人：AURIGENE DISCOVERY TECHNOLOGIES LIMITED

  公开号：US20160200693A1

  公开（公告）日：2016-07-14

  The present invention provides trisubstituted benzotriazole derivatives as dihydroorotate oxygenase inhibitor compounds of formula (I), which may be therapeutically useful as DHODH inhibitors. wherein, R 1 , R 2 and R 3 have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting DHODH. The present invention also provides methods for synthesizing trisubstituted benzotriazole derivatives of formula (I). The present invention also provides pharmaceutical formulations comprising at least one of the DHODH inhibitor compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.

  本发明提供了三取代苯并三唑衍生物作为二氢乳酸脱氢酶氧化酶抑制剂化合物的公式（I），其可能在治疗和预防疾病或紊乱方面具有治疗用途，特别是在抑制DHODH方面具有优势的疾病或紊乱中使用。其中，R1，R2和R3在规范中给出了含义，以及其药学上可接受的盐。本发明还提供了合成公式（I）的三取代苯并三唑衍生物的方法。本发明还提供了包含公式（I）的DHODH抑制剂化合物之一的药物制剂，以及药学上可接受的载体，稀释剂或赋形剂。
• Lincomycin Derivatives and Antimicrobial Agents Comprising the Same as Active Ingredient
  申请人：Umemura Eijirou

  公开号：US20090156512A1

  公开（公告）日：2009-06-18

  This invention provides compounds of formula (I) or its pharmacologically acceptable salt or solvate, wherein A represents aryl or a monocyclic or bicyclic heterocyclic group, R 1 represents a halide, nitro, substituted C 1-6 alkyl, optionally substituted amino, C 1-6 alkyloxycarbonyl, optionally substituted aryl, a heterocyclic group, or heterocyclic carbonyl, R 2 represents a hydrogen atom or C 1-6 alkyl, R 3 represents C 1-6 alkyl, all of R 4 , R 5 , and R 6 represent a hydrogen atom, R 7 represents C 1-6 alkyl, m is 1 or 2, and n is 1. The compounds are novel lincomycin derivatives having a potent activity against resistant pneumococci. The compounds can be used as an antimicrobial agent and are useful for preventing or treating bacterial infectious diseases.

  本发明提供了式（I）的化合物或其药理学上可接受的盐或溶剂，其中A代表芳基或单环或双环杂环基，R1代表卤素、硝基、取代的C1-6烷基、可选取代的氨基、C1-6烷氧羰基、可选取代的芳基、杂环基或杂环羰基，R2代表氢原子或C1-6烷基，R3代表C1-6烷基，R4、R5和R6均代表氢原子，R7代表C1-6烷基，m为1或2，n为1。这些化合物是新型的林可霉素衍生物，对耐药性肺炎球菌具有强大的活性。这些化合物可以用作抗微生物剂，并且对于预防或治疗细菌感染性疾病是有用的。
• LINCOMYCIN DERIVATIVE AND ANTIBACTERIAL AGENT CONTAINING THE SAME AS ACTIVE INGREDIENT
  申请人：Meiji Seika Kaisha, Ltd.

  公开号：EP1970377A1

  公开（公告）日：2008-09-17

  This invention provides compounds of formula (I) or its pharmacologically acceptable salt or solvate, wherein A represents aryl or a monocyclic or bicyclic heterocyclic group, R1 represents a halide, nitro, substituted C1-6 alkyl, optionally substituted amino, C1-6 alkyloxycarbonyl, optionally substituted aryl, a heterocyclic group, or heterocyclic carbonyl, R2 represents a hydrogen atom or C1-6 alkyl, R3 represents C1-6 alkyl, all of R4, R5, and R6 represent a hydrogen atom, R7 represents C1-6 alkyl, m is 1 or 2, and n is 1. The compounds are novel lincomycin derivatives having a potent activity against resistant pneumococci. The compounds can be used as an antimicrobial agent and are useful for preventing or treating bacterial infectious diseases.

  本发明提供了式(I)化合物或其药理学上可接受的盐或溶液，其中 A 代表芳基或单环或双环杂环基团，R1 代表卤化物、硝基、取代的 C1-6 烷基、任选取代的氨基、任选取代的 C1-6 烷氧羰基、任选取代的芳基、杂环基团或杂环羰基，R2 代表氢原子或 C1-6 烷基，R3 代表 C1-6 烷基，R4 代表 C1-6 烷基，R5 代表 C1-6 烷基、C1-6烷氧基羰基、任选取代的芳基、杂环基团或杂环羰基，R2代表氢原子或C1-6烷基，R3代表C1-6烷基，所有R4、R5和R6代表氢原子，R7代表C1-6烷基，m为1或2，n为1。这些化合物是新型的林可霉素衍生物，对耐药性肺炎球菌具有强效活性。这些化合物可用作抗菌剂，用于预防或治疗细菌性传染病。
• Methods of use for trisubstituted benzotriazole derivatives as dihydroorotate oxygenase inhibitors
  申请人：Aurigene Discovery Technologies Limited

  公开号：US11147801B2

  公开（公告）日：2021-10-19

  The present invention provides methods for treating a cancer in a subject and for inhibiting tumor growth, metastasis or a dihydrorotate oxygenase enzyme activity of a tumor or cancer cell. At least one trisubstituted benzotriazole derivative with the formula (I) is administered to the subject or is contacted with the cancer cell. Compounds of formula (I) have substituents R1, R2 and R3 which have the meanings given in the specification, and pharmaceutically acceptable salts thereof.

  本发明提供了治疗受试者癌症和抑制肿瘤生长、转移或肿瘤或癌细胞的二氢氧合酶活性的方法。向受试者施用至少一种式（I）的三取代苯并三唑衍生物或与癌细胞接触。式(I)化合物的取代基R1、R2和R3具有说明书中给出的含义，及其药学上可接受的盐类。
• EP1970377
  申请人：——

  公开号：——

  公开（公告）日：——