(2-氯-5-硝基苯基)(4-甲氧苯基)甲酮 | 70132-87-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: (2-氯-5-硝基苯基)(4-甲氧苯基)甲酮
• 英文名称: 2-chloro-4'-methoxy-5-nitro-benzophenone
• 英文别名: 2-chloro-5-nitro-4'-methoxybenzophenone；2-Chlor-4'-methoxy-5-nitro-benzophenon；(2-Chloro-5-nitrophenyl)(4-methoxyphenyl)methanone；(2-chloro-5-nitrophenyl)-(4-methoxyphenyl)methanone
• CAS: 70132-87-5
• 化学式: C₁₄H₁₀ClNO₄
• mdl: MFCD02923676
• 分子量: 291.691
• InChiKey: XOLMZHQBAOKBSS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  72.1
• 氢给体数：
  0
• 氢受体数：
  4

安全信息

• 海关编码：
  2914700090

反应信息

• 作为反应物：
  描述：

  (2-氯-5-硝基苯基)(4-甲氧苯基)甲酮 在 硫酸 、 potassium carbonate 、 溶剂黄146 作用下， 生成 9-(4-甲氧基-苯基)-2-硝基-吖啶
  参考文献：
  名称：

  Ullmann; Ernst, Chemische Berichte, 1906, vol. 39, p. 300

  摘要：

  DOI：
• 作为产物：
  描述：

  2-氯-5-硝基苯甲酸 在 三氯化铝 、 五氯化磷 作用下， 以 氯苯 为溶剂， 反应 49.0h， 生成 (2-氯-5-硝基苯基)(4-甲氧苯基)甲酮
  参考文献：
  名称：

  （苯甲酰基苯基）哌啶：一类新的免疫调节剂。

  摘要：

  已经合成了一系列（苯甲酰基苯基）哌啶，并评估了其作为免疫调节剂的活性。这些化合物中的几种在基于对Con A，PHA和PWM的淋巴细胞促有丝分裂反应的基础上筛选中显示出良好的活性。苯甲酰基部分第4位的氯以及对哌啶核的氨基（或氨基甲酸酯衍生物）似乎对活性至关重要。所描绘的化合物可以被认为是新系列免疫调节剂的第一个实例。

  DOI：

  10.1021/jm00109a004

文献信息

• Bile Acid Recycling Inhibitors for Treatment of Hypercholemia and Cholestatic Liver Disease
  申请人：Lumena Pharmaceuticals, Inc.

  公开号：US20130108573A1

  公开（公告）日：2013-05-02

  Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.

  本文提供了一种治疗或改善高胆固醇血症或胆汁淤积性肝病的方法，即通过向需要的个体施用治疗有效量的顶端钠依赖性胆酸转运蛋白抑制剂（ASBTI）或其药用可接受盐。还提供了一种治疗或改善肝病、降低血清胆酸或肝内胆酸水平、治疗或改善瘙痒、降低肝酶或减少胆红素的方法，即通过向需要的个体施用治疗有效量的ASBTI或其药用可接受盐。
• Synthesis and Antitumor Activity of Novel Benzophenone Derivatives.
  作者：Eiji KUMAZAWA、Kenji HIROTANI、S. Clifford BURFORD、Keiichi KAWAGOE、Tamotsu MIWA、Ikuo MITSUI、Akio EJIMA

  DOI：10.1248/cpb.45.1470

  日期：——

  Novel benzophenone derivatives were synthesized and screened for cytotoxic and antitumor activity. Friedel-Crafts condensation was employed to construct the benzophenone skeleton. Among the compounds synthesized, morpholino and thiomorpholino benzophenones 3a-d exhibited potent cytotoxic activity against P388 murine leukemia and PC-6 human lung carcinoma cells in vitro, and compounds 3a, 3c, and 3j

  合成了新型的二苯甲酮衍生物，并筛选了其细胞毒性和抗肿瘤活性。使用弗瑞德-克来福特（Friedel-Crafts）缩合反应构建二苯甲酮骨架。在合成的化合物中，吗啉代和硫代吗啉代二苯甲酮3a-d在体外对P388鼠白血病和PC-6人肺癌细胞表现出有效的细胞毒活性，而化合物3a，3c和3j腹膜内给药对它们具有显着的抗肿瘤活性。腹膜内接种小鼠P388细胞引起的恶性腹水。
• Benzoyl-phenyl-piperidine derivatives
  申请人：Societe de Recherches Industrielles (S.O.R.I.)

  公开号：US04680402A1

  公开（公告）日：1987-07-14

  Intermediate products usable in particular for preparing corresponding amino derivatives by converting their nitro function, said products being of formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3, which are identical or different, each represent an atom of hydrogen, a halogen, a lower alkyl group or a lower alkoxy group; R.sub.5 and R.sub.6, which are identical or different, each represent an atom of hydrogen, a lower alkyl group, an OH group, a phenyl group or a benzyl group.

  中间产物可用于通过将它们的硝基转化为相应的氨基衍生物而进行制备，所述产物的化学式为：##STR1##其中：R.sub.1、R.sub.2和R.sub.3分别表示氢原子、卤素、较低的烷基基团或较低的烷氧基团的原子，这三者可以相同也可以不同；R.sub.5和R.sub.6分别表示氢原子、较低的烷基基团、羟基、苯基或苄基的原子，这两者可以相同也可以不同。
• Bile Acid Recycling Inhibitors for Treatment of Pediatric Cholestatic Liver Diseases
  申请人：Lumena Pharmaceuticals, Inc.

  公开号：US20130109671A1

  公开（公告）日：2013-05-02

  Provided herein are methods of treating or ameliorating a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a pediatric liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.

  本文提供了一种通过非系统性给予需要治疗或改善儿童胆汁淤积性肝病的个体治疗的方法，该方法包括给予含有顶端钠依赖性胆酸转运体抑制剂（ASBTI）或其药学上可接受的盐的儿科制剂的治疗有效量。此外，还提供了一种治疗或改善儿童肝病、降低血清胆酸或肝胆酸水平、治疗或改善瘙痒、降低肝酶或减少胆红素的方法，该方法包括给予含有ASBTI或其药学上可接受的盐的儿科制剂的治疗有效量。
• BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF PEDIATRIC CHOLESTATIC LIVER DISEASES
  申请人：Lumena Pharmaceuticals, Inc.

  公开号：US20140243281A1

  公开（公告）日：2014-08-28

  Provided herein are pediatric dosage forms for use in the treatment of a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of the pediatric dosage form comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are said pediatric dosage form for use in the treatment of a pediatric liver disease, for use in decreasing the levels of serum bile acids or hepatic bile acids, for use in the treatment of pruritis, for use in reducing liver enzymes or bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.

  本文提供了用于治疗儿童胆汁淤积性肝病的儿童剂型，通过非系统性给予需要治疗的个体含有顶端钠依赖性胆酸转运体抑制剂（ASBTI）或其药学上可接受的盐的治疗有效量的儿童剂型。还提供了该儿童剂型用于治疗儿童肝病，用于降低血清胆酸或肝胆酸水平，用于治疗瘙痒症，用于减少肝酶或胆红素的儿童制剂，通过非系统性给予需要治疗的个体含有ASBTI或其药学上可接受的盐的治疗有效量。