(R)-Ranolazine

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (R)-Ranolazine
• 英文别名: ranolazine；N-(2,6-dimethylphenyl)-2-[4-[(2R)-2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl]acetamide
• 化学式: C₂₄H₃₃N₃O₄
• 分子量: 427.544
• InChiKey: XKLMZUWKNUAPSZ-HXUWFJFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  31
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  74.3
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2,6-二甲基氯代乙酰苯胺 在 Candida antartica lipase in the form of CLEA 、 sodium dodecyl-sulfate 、 potassium carbonate 作用下， 以 甲醇 、 水 、 甲苯 为溶剂， 反应 64.0h， 生成 (R)-Ranolazine
  参考文献：
  名称：

  脂酶介导的化学酶促合成化学方法合成（S）-雷诺嗪，作为一种抗心绞痛药物

  摘要：

  在基于计算机模拟的生物催化方法中，以对映纯形式合成药物和药物中间体是一种有机化学途径上的合理化方法。在这项研究中，基于酶配体的...

  DOI：

  10.1039/c6ra06879k

文献信息

• DISUBSTITUTED TRIFLUOROMETHYL PYRIMIDINONES AND THEIR USE
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20160221965A1

  公开（公告）日：2016-08-04

  The present application relates to novel 2,5-disubstituted 6-(trifluoromethyl)pyrimidin-4(3H)-one derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular, renal, inflammatory and fibrotic diseases.

  本申请涉及新颖的2,5-二取代6-(三氟甲基)嘧啶-4(3H)-酮衍生物，其制备方法，其单独或与其他药物联合用于治疗和/或预防疾病，以及用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管、肾脏、炎症和纤维化疾病。
• [EN] 1-AKAN-2-OL SUBSTITUTED PIPERAZINE AND PIPERIDINE COMPOUNDS<br/>[FR] COMPOSES PIPERAZINE ET PIPERAZINE 1-AKAN-2-OL SUBSTITUES
  申请人：CV THERAPEUTICS INC

  公开号：WO2005061470A1

  公开（公告）日：2005-07-07

  Disclosed are novel substituted heterocyclic derivatives having the structure of Formula (I): The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.

  揭示了具有以下结构的新型取代杂环衍生物（I）的化合物：这些化合物对于治疗各种疾病状态有用，特别是心血管疾病，如心房和心室心律失常，间歇性跛行，普林兹梅塔（变异）心绞痛，稳定和不稳定心绞痛，运动诱发性心绞痛，充血性心脏病，糖尿病和心肌梗死。
• METHOD FOR THE PREPARATION OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NAPHTHYRIDINE-3-CARBOXAMIDE AND THE PURIFICATION THEREOF FOR USE AS AN ACTIVE PHARMACEUTICAL INGREDIENT
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20180244670A1

  公开（公告）日：2018-08-30

  The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I)

  本发明涉及一种用于制备式(I)的(4S)-4-(4-氰基-2-甲氧基苯基)-5-乙氧基-2,8-二甲基-1,4-二氢-1,6-萘啉-3-羧酰胺的新型改进工艺。
• [EN] AMINO PYRAZINE DERIVATIVES AS PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS<br/>[FR] DÉRIVÉS AMINÉS DE PYRAZINE UTILISABLES EN TANT QU'INHIBITEURS DE LA PHOSPHATIDYLINOSITOL 3-KINASE
  申请人：NOVARTIS AG

  公开号：WO2015162459A1

  公开（公告）日：2015-10-29

  The present invention provides compounds of formula (I) which inhibit the activity of PI 3-kinase gamma isoform, which are useful for the treatment of diseases mediated by the activation of PI 3-kinase gamma isoform.

  本发明提供了一种公式（I）的化合物，该化合物抑制PI 3-激酶γ同工酶的活性，对于治疗由PI 3-激酶γ同工酶激活介导的疾病是有用的。
• SUBSTITUTED BIPIPERIDINYL DERIVATIVES
  申请人：Bayer Pharma Aktiengesellschaft

  公开号：US20160318866A1

  公开（公告）日：2016-11-03

  The invention relates to novel substituted bipiperidinyl derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardiac vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.

  该发明涉及新型取代的双哌啶衍生物，涉及它们的制备方法，涉及它们用于治疗和/或预防疾病以及用于制备治疗和/或预防疾病的药物的用途，特别是用于治疗和/或预防糖尿病微血管病变、四肢糖尿病溃疡，特别是促进糖尿病足溃疡愈合、糖尿病心力衰竭、糖尿病冠状微血管心脏疾病、外周和心脏血管疾病、血栓栓塞疾病和缺血、外周循环障碍、雷诺现象、CREST综合征、微循环障碍、间歇性跛行以及外周和自主神经病变的治疗和/或预防。