布纳唑嗪 | 80755-51-7

• 物质功能分类: 原料药 - 循环系统用药 - 抗高血压病药
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 布纳唑嗪
• 中文别名: 布那唑嗪；1-[4-(4-氨基-6,7-二甲氧基-2-喹唑啉基)六氢-1H-1,4-二氮杂卓-1-基]-1-丁酮
• 英文名称: bunazosin
• 英文别名: DDQ；1-(4-amino-6,7-dimethoxy-quinazolin-2-yl)-4-butyryl-[1,4]diazepane；1-[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-1,4-diazepan-1-yl]butan-1-one
• CAS: 80755-51-7
• 化学式: C₁₉H₂₇N₅O₃
• 分子量: 373.455
• InChiKey: RHLJLALHBZGAFM-UHFFFAOYSA-N

物化性质

• 沸点：
  620.6±65.0 °C(Predicted)
• 密度：
  1.221

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  93.8
• 氢给体数：
  1
• 氢受体数：
  7

安全信息

• 储存条件：
  存储条件：2-8°C，避光，干燥。

制备方法与用途

布那松是一种有效的选择性α1肾上腺素受体拮抗剂，而布那唑嗪则常用于抗高血压和降眼压的研究。

反应信息

• 作为反应物：
  描述：

  布纳唑嗪 生成 盐酸布那唑嗪
  参考文献：
  名称：

  MASAFUTA, KIESI;UTIKAVA, KIEXIKO;KAVABATA, YUKEHJ;KANAI, TAKEHO;SUGIMOTO,+

  摘要：

  DOI：
• 作为产物：
  描述：

  哌唑嗪 生成 布纳唑嗪
  参考文献：
  名称：

  Synthetic approaches, functionalization and therapeutic potential of quinazoline and quinazolinone skeletons: The advances continue

  摘要：

  The presence of N-heterocycles as an essential structural motif in a variety of biologically active substances has stimulated the development of new strategies and technologies for their synthesis. Among the various N-heterocyclic scaffolds, quinazolines and quinazolinones form a privileged class of compounds with their diverse spectrum of therapeutic potential. The easy generation of complex molecular diversity through broadly applicable, cost-effective, practical and sustainable synthetic methods in a straightforward fashion along with the importance of these motifs in medicinal chemistry, received significant attention from researchers engaged in drug design and heterocyclic methodology development. In this perspective, the current review article is an effort to recapitulate recent developments in the eco-friendly and green procedures for the construction of highly challenging and potentially bioactive quinazoline and quinazolinone compounds in order to help medicinal chemists in designing and synthesizing novel and potent compounds for the treatment of different disorders. The key mechanistic insights for the synthesis of these heterocycles along with potential applications and manipulations of the products have also been conferred. This article also aims to highlight the promising future directions for the easy access to these frameworks in addition to the identification of more potent and specific products for numerous biological targets. (C) 2014 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2014.10.084
• 作为试剂：
  描述：

  (4,5-dimethyl-2-o-tolyloxymethyl-cyclohexa-1,4-dienyl)-methoxyimino-acetic acid methylester 、 异丙醚 在 布纳唑嗪 作用下， 以 正己烷 、 甲苯 为溶剂， 生成 (4,5-dimethyl-2-o-tolyloxymethyl-phenyl)-methoxyimino-acetic acid methylester
  参考文献：
  名称：

  Phenyl-methoxyimino-acetic acid derivatives as pesticides

  摘要：

  11式化合物，其中：A是CH2O或CH2ON═C(R1)基团；X1和X2分别是C1-C4-烷基；Y是OH、O(C1-C4-烷基)、NH2或NHCH3；R1是C1-C4-烷基、环丙基、氰基、三氟甲基或C1-C4-烷氧基；R是芳基、杂环芳基或杂环烷基，上述基团可能被相同或不同的取代基取代，具有杀菌活性，可用于农业、园艺和卫生领域中对植物病原真菌的控制和预防。

  公开号：

  US20010018452A1

文献信息

• [EN] NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL ANTI-DIABETIC AGENTS<br/>[FR] NOUVEAUX AGENTS ANTIDIABÉTIQUES UTILES AVEC DES DÉRIVÉS DE BENZIMIDAZOLE CYCLIQUES
  申请人：MERCK SHARP & DOHME

  公开号：WO2010051176A1

  公开（公告）日：2010-05-06

  Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

  结构式（I）的新化合物是AMP-蛋白激酶的激活剂，可用于治疗、预防和抑制由AMPK激活的蛋白激酶介导的疾病。本发明的化合物对于治疗2型糖尿病、高血糖、代谢综合征、肥胖、高胆固醇血症和高血压是有用的。
• Dibenzylamine compound and medicinal use thereof
  申请人：Maeda Kimiya

  公开号：US20050059810A1

  公开（公告）日：2005-03-17

  A dibenzylamine compound represented by the formula (1) wherein R 1 and R 2 are each a C 1-6 alkyl group optionally substituted by halogen atoms and the like; R 3 , R 4 and R 5 are each a hydrogen atom, a halogen atom and the like, or R 3 and R 4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R 7 ) (R 8 ) and the like; ring B is an aryl group or a heterocyclic residue; R 6 is a hydrogen atom, a halogen atom, a nitro group, a C 1-6 alkyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.

  一种二苄胺化合物，其化学式如下： 其中，R1和R2分别是C1-6烷基基团，可选择性地被卤原子等取代；R3、R4和R5分别是氢原子、卤原子等，或者R3和R4可以与与之相结合的碳原子一起形成一个具有取代基的同环或异环环；A是-N(R7)(R8)等；环B是芳基或杂环残基；R6是氢原子、卤原子、硝基、C1-6烷基基团等；n是1到3的整数，其前体和药学上可接受的盐表现出选择性和强效的CETP抑制活性，因此，它们可以作为治疗或预防高脂血症或动脉硬化等疾病的药物。
• CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTIC DELIVERY
  申请人：Cerulean Pharma Inc.

  公开号：US20130196906A1

  公开（公告）日：2013-08-01

  Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of a disease or disorder, e.g., autoimmune disease, inflammatory disease, central nervous system disorder, cardiovascular disease, or metabolic disorder. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.

  提供了关于使用CDP-治疗剂偶联物治疗疾病或紊乱的方法，例如自身免疫疾病、炎症性疾病、中枢神经系统紊乱、心血管疾病或代谢紊乱。还提供了CDP-治疗剂偶联物、包含CDP-治疗剂偶联物的颗粒以及包含CDP-治疗剂偶联物的组合物。
• DIARYLMETHYLAMIDE DERIVATIVE HAVING ANTAGONISTIC ACTIVITY ON MELANIN-CONCENTRATING HORMONE RECEPTOR
  申请人：Banyu Pharmaceutical Co., Ltd.

  公开号：EP2272841A1

  公开（公告）日：2011-01-12

  [Problem] To provide a melanin-concentrating hormone receptor antagonist useful as a pharmaceutical agent for central diseases, circulatory diseases, and metabolic diseases. [Means for Resolution] Provided is a diarylmethylamide derivative represented by formula (I): Wherein R1a, R1b, R2a, R2b, R3a, and R3b independently represent a hydrogen atom or the like, R4 represents a hydrogen atom, C1-6 alkyl, or the like, R5 represents a hydrogen atom or the like, Z represents C1-6 alkyl or the like, or R4 and Z together form a 4- to 6-membered nitrogen-containing hetero ring, Y1 represents H or the like, Y2 represents H, or Y1 and Y2 together form - O-CH2-, W represents C, SO, or the like, Ar1 represents 6-membered aryl or the like, Ar2 represents 6-membered aryl or the like, and ring A represents a benzene ring, a pyridine ring, or the like.

  [问题] 提供一种对黑色素浓缩激素受体拮抗剂，用作中枢疾病、循环疾病和代谢疾病的药用制剂。 [解决方法] 提供一种由式(I)表示的二芳基甲酰胺衍生物： 其中R1a、R1b、R2a、R2b、R3a和R3b独立地表示氢原子或类似物，R4表示氢原子、C1-6烷基或类似物，R5表示氢原子或类似物，Z表示C1-6烷基或类似物，或者R4和Z一起形成一个含氮杂环的4-至6-成员环，Y1表示H或类似物，Y2表示H，或者Y1和Y2一起形成-O-CH2-，W表示C、SO或类似物，Ar1表示6-成员芳基或类似物，Ar2表示6-成员芳基或类似物，环A表示苯环、吡啶环或类似物。
• Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia
  申请人：Palani Anandan

  公开号：US20060264489A1

  公开（公告）日：2006-11-23

  A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dyslipidemia.

  具有通式（I）的一种化合物： 或其药学上可接受的盐、溶剂化合物、酯或互变异构体，其中： Q选自以下群组： 和 L选自以下群组： 或其药学上可接受的盐、溶剂化合物、酯或互变异构体，可用于治疗代谢综合征和血脂异常等疾病、疾患或症状。