奈拉米诺 | 86140-10-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 中文名称: 奈拉米诺
• 中文别名: 耐那米若
• 英文名称: 1-(indazol-4-yloxy)-3-[2-(2,6-dimethylphenylamino)-ethylamino]-propan-2-ol
• 英文别名: neraminol；1-[2-(2,6-dimethylanilino)ethylamino]-3-(1H-indazol-4-yloxy)propan-2-ol
• CAS: 86140-10-5
• 化学式: C₂₀H₂₆N₄O₂
• 分子量: 354.452
• InChiKey: QKSHPHAGYABOBC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  26
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  82.2
• 氢给体数：
  4
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  1-(2-benzylindazol-4-yloxy)-3-[2-(2,6-dimethylphenylamino)-ethylamino]-propan-2-ol 生成 奈拉米诺
  参考文献：
  名称：

  WIEDEMANN, F.;MICHEL, H.;WECKERLE, W.;STREIN, K.

  摘要：

  DOI：

文献信息

• 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。
• Indazoloxypropanolamine derivatives and use in combating, and for the
  申请人：Boehringer Mannheim GmbH

  公开号：US04479962A1

  公开（公告）日：1984-10-30

  The present invention provides heteroaryloxypropanolamines and pharmaceutical compositions containing them, for combating, and for the prophylaxis of, cardiac and circulatory diseases. The heteroaryloxypropanolamines of the present invention are of the general formula: ##STR1## wherein A is a bi- or tricyclic heteroaromatic radical, which is optionally partly hydrogenated, X is a straight-chained or branched alkylene chain containing 2 to 6 carbon atoms, R.sub.1 and R.sub.2, which can be the same or different, are hydrogen atoms or lower alkyl or benzyl radicals, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or lower alkyl, benzyl, formyl, lower alkanoyl, cyano, hydroxymethyl, lower alkoxycarbonyl or carbamoyl radicals or the divalent substituents sulfur or oxygen and R.sub.6, R.sub.7 and R.sub.8, which can be the same or different, are hydrogen or halogen atoms, lower alkyl, nitro, amino, lower alkylthio or lower alkoxy radicals or R.sub.6 and R.sub.7 together represent an optionally unsaturated trimethylene chain; and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.

  本发明提供了杂环氧基丙胺和含有它们的制药组合物，用于对抗和预防心脏和循环系统疾病。本发明的杂环氧基丙胺的一般式如下：##STR1##其中A是一个双环或三环杂芳基基团，可以选择部分氢化，X是一个含有2到6个碳原子的直链或支链烷基链，R.sub.1和R.sub.2可以相同或不同，是氢原子或低级烷基或苄基基团，R.sub.3、R.sub.4和R.sub.5可以相同或不同，是氢原子或低级烷基、苄基、甲酰基、低级烷酰基、氰基、羟甲基、低级烷氧羰基或氨基甲酰基基团或二价取代基硫或氧，R.sub.6、R.sub.7和R.sub.8可以相同或不同，是氢或卤素原子、低级烷基、硝基、氨基、低级烷硫基或低级烷氧基基团或R.sub.6和R.sub.7一起代表一个可选的不饱和三亚甲基链；以及其药理学上可接受的盐。本发明还提供了制备这些化合物的方法，以及含有它们的制药组合物。
• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• [EN] CYCLOPROPYL MODULATORS OF P2Y12 RECEPTOR<br/>[FR] MODULATEURS CYCLOPROPYLÉS DU RÉCEPTEUR P2Y12
  申请人：AUSPEX PHARMACEUTICALS INC

  公开号：WO2011017108A2

  公开（公告）日：2011-02-10

  The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

  本发明涉及新的环丙基P2Y12受体调节剂，其制药组合物以及使用方法。
• CYCLOPROPYL MODULATORS OF P2Y12 RECEPTOR
  申请人：Auspex Pharmaceuticals, Inc.

  公开号：US20160193212A1

  公开（公告）日：2016-07-07

  The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

  本发明涉及P2Y12受体活性的新环丙基调节剂，其制药组合物以及使用方法。