布替君 | 7433-10-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 中文名称: 布替君
• 英文名称: Butidrine
• 英文别名: 2-sec-Butylamino-1-<5,6,7,8-tetrahydro-<2>naphthyl>-aethanol；1-<5.6.7.8-Tetrahydro-naphthyl-(2)>-2-sek.-butylamino-aethanol；6-(2-sec-Butylamino-1-hydroxyethyl)tetralin；2-(butan-2-ylamino)-1-(5,6,7,8-tetrahydronaphthalen-2-yl)ethanol
• CAS: 7433-10-5
• 化学式: C₁₆H₂₅NO
• 分子量: 247.381
• InChiKey: GVNYSERWAKVROD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  18
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  <5,6,7,8-Tetrahydro-<2>naphthyl>-glykolsaeureamid 在 palladium on activated charcoal lithium aluminium tetrahydride 、 氢气 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 生成 布替君
  参考文献：
  名称：

  Casagrande; Ferrari, Farmaco, Edizione Scientifica, 1966, vol. 21, # 3, p. 229 - 248

  摘要：

  DOI：

文献信息

• Nitric Oxide Releasing Prodrugs of Therapeutic Agents
  申请人：SATYAM Apparao

  公开号：US20110263526A1

  公开（公告）日：2011-10-27

  The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.

  本发明涉及已知药物或治疗剂的一氧化氮释放前药，其在此处表示为式(I)的化合物，其中药物或治疗剂包含一个或多个功能基团，独立地选自羧酸、氨基、羟基和巯基。该发明还涉及制备一氧化氮释放前药（式(I)的化合物）的方法，含有它们的药物组合物以及使用这些前药的方法。
• Method for treating resistant hypertension
  申请人：Gerber Michael J.

  公开号：US20070196510A1

  公开（公告）日：2007-08-23

  A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

  提供了一种降低临床诊断为顽固性高血压患者血压的方法。该方法包括将达卢生坦作为辅助药物与基础抗高血压治疗方案联合给药，该基础方案包括至少一种利尿剂和至少两种抗高血压药物，这些药物选自至少两类：(a) ACE抑制剂和血管紧张素II受体阻滞剂，(b) β-肾上腺素能受体阻滞剂，以及(c) 钙通道阻滞剂。达卢生坦以有效剂量和频率口服给药，与基础治疗方案结合，能够使选自谷值坐位收缩压、谷值坐位舒张压、24小时动态收缩压、24小时动态舒张压、日间最高收缩压和日间最高舒张压的一个或多个血压参数至少降低约3 mmHg。
• [EN] COMBINATION OF (S)-AMLODIPINE AND A BETA-BLOCKER, AND METHODS FOR REDUCING HYPERTENSION<br/>[FR] COMBINAISON DE (S)-AMLODIPINE ET D'UN BETABLOQUANT, ET PROCEDES POUR LA REDUCTION DE L'HYPERTENSION
  申请人：SEPRACOR INC

  公开号：WO2005099699A1

  公开（公告）日：2005-10-27

  One aspect of the present invention relates to pharmaceutical compositions comprising optically pure (S)-amlodipine and a beta-blocker. In a preferred embodiment, the beta-blocker is atenolol or bisprolol. Another aspect of the present invention relates to pharmaceutical compositions consisting essentially of at least one pharmaceutically acceptable carrier, optically pure (S)-amlodipine and a beta-blocker. In a preferred embodiment, the beta-blocker is atenolol or bisoprolol. The pharmaceutical compositions of the invention are useful, e.g., in the treatment of hypertension. In addition, the present invention also relates to a method of treating a patient suffering from hypertension or a related cardiac disorder, comprising co-administering to a patient in need thereof a therapeutically effective amount of optically pure (S)-amlodipine and a beta-blocker. In certain embodiments of the compositions and methods, said optically pure (S)-amlodipine is optically pure (S)-amlodipine malate, or a polymorph, pseudopolymorph or solvate thereof.

  本发明的一个方面涉及包含光学纯（S）-氨氯地平和β受体阻断剂的制药组合物。在一个首选实施例中，β受体阻断剂为阿托伐他汀或比索洛尔。本发明的另一个方面涉及基本上由至少一种药用载体、光学纯（S）-氨氯地平和β受体阻断剂组成的制药组合物。在一个首选实施例中，β受体阻断剂为阿托伐他汀或比索洛尔。本发明的制药组合物可用于治疗高血压等疾病。此外，本发明还涉及一种治疗患有高血压或相关心脏疾病的患者的方法，包括向需要的患者共同给予光学纯（S）-氨氯地平和β受体阻断剂的治疗有效量。在某些组合物和方法的实施例中，所述的光学纯（S）-氨氯地平为光学纯（S）-氨氯地平苹果酸盐，或其多晶形、伪多晶形或溶剂化合物。
• IMAGE-GUIDED THERAPY OF MYOCARDIAL DISEASE: COMPOSITION, MANUFACTURING AND APPLICATIONS
  申请人：Yang David J.

  公开号：US20090238756A1

  公开（公告）日：2009-09-24

  Compositions and methods for imaging and for chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns agents comprising a targeting moeity comprising a beta-adrenergic receptor targeting compound conjugated or embedded with ethylenediamine. The present invention also concerns methods of application of such agents for imaging and treatment of cardiovascular diseases, and kits for preparing a radiolabeled therapeutic or diagnostic agent.

  揭示了用于成像、化疗和放疗的构成物和方法。更具体地，本发明涉及含有靶向单元的试剂，该靶向单元包括与乙二胺共轭或嵌入的β-肾上腺素受体靶向化合物。本发明还涉及应用这种试剂进行心血管疾病成像和治疗的方法，以及用于制备放射标记治疗或诊断试剂的试剂盒。
• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。