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| 化学名: | ラノラジン | | 英語化学名: | Ranolazine | | 别名: | 1- 3-(2-Methoxyphenoxy)-2-hydroxypropyl -4- ...;1-Piperazineacetamide,N-(2,6-dimethylphenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]-;N-(2,6-dimethylphenyl)-2-[4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl]ethanamide;N-(2,6-diMethylphenyl)-2-{4-[(2R)-2-hydroxy-3-(2-Methoxyphenoxy)propyl]piperazin-1-yl}acetaMide;Ranolazine(Ranexa);100MG/500MG/1KG;Ranolazine
N-(2,6-Dimethylphenyl)-2-[4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl]acetamide;Ranolazine (100 mg) | | CAS番号: | 95635-55-5 | | 分子式: | C24H33N3O4 | | 分子量: | 427.54 | | EINECS: | 620-450-7 | | カテゴリ情報: | Aromatics;Heterocycles;Intermediates & Fine Chemicals;Inhibitors;RANEXA;Pharmaceuticals;Antianginal;API;APIs | | Mol File: | 95635-55-5.mol |  |
| 融点 | 119-1200C | | 沸点 | 624.1±55.0 °C(Predicted) | | 比重(密度) | 1.174±0.06 g/cm3(Predicted) | | 貯蔵温度 | Sealed in dry,Room Temperature | | 溶解性 | DMSO (Slightly), Methanol (Slightly) | | 外見 | Solid | | 酸解離定数(Pka) | 14.06±0.20(Predicted) | | 色 | White | | CAS データベース | 95635-55-5(CAS DataBase Reference) |
| | ラノラジン Usage And Synthesis |
| 効能 | 血管拡張薬 | | 説明 | Ranolazine is an orally available, extended release drug for the treatment of
chronic angina in patients who have failed to respond to prior angina therapy.
Chronic stable angina (CSA) is a common symptom of coronary artery disease
wherein plaques in the coronary vasculature restrict blood flow to the heart,
which in turn leads to insufficient oxygenation of the heart, typically during
physical exertion or emotional stress. A vast majority of the existing anti-anginal
and anti-ischemic therapies aim to correct the imbalance between myocardial
oxygen demand and supply through mechanisms that produce reductions in
heart rate or blood pressure. | | 化学的特性 | White Solid | | Originator | Roche Bioscience (US) | | 使用 | antianginal, antiischemic | | 定義 | ChEBI: N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide is an aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline. It is a monocarboxylic acid amide, an aromatic amide, a N-alkylpiperazine, a secondary alcohol and a monomethoxybenzene. | | brand name | Ranexa (Sensus). | | 一般的な説明 | Ranolazine, N-(2,6-dimethylphenyl)-2-[4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl]acetamide (Ranexa), is an antianginal medication thatwas approved by the Food and Drug Administration (FDA)in January 2006 for the treatment of chronic angina.Ranolazine is believed to elicit its effects by altering thetranscellular late sodium current. This, in turn, alters thesodium-dependent calcium channels during myocardial ischemia.Thus, ranolazine indirectly prevents the calciumoverload that is associated with cardiac ischemia.Ranolazine is metabolized by the cytochrome CYP3A enzymesin the liver. | | 臨床応用 | Add on therapy for angina | | 合成 | Two syntheses,
one from the inventors at Roche and other from a group in Hungary, of Ranolazine have been described in the
patent literature. The original synthesis is highlighted in the
Scheme. Reaction of 2,6-dimethylaniline 46 with chloroacetyl
chloride (47) in the presence of triethylamine for 4h at
0oC gave amide 48 in 82% yield. This chloro amide 48 was
reacted with piperazine in refluxing ethanol for 2 h to give
piperazinyl amide 50. Reaction of amide 50 with epoxide
intermediate 53, prepared by reacting 2-methoxy phenol 51
with epichlorohydrin, in refluxing isopropanol for 3 h followed
by treatment with HCl/methanol gave ranolazine dihydrochloride
(VII) in 73% yield. 
| | 薬物相互作用 | Potentially hazardous interactions with other drugs
Anti-arrhythmics: avoid with disopyramide.
Antibacterials: concentration possibly increased
by clarithromycin and telithromycin - avoid
concomitant use; concentration reduced by
rifampicin - avoid.
Antifungals: concentration increased by ketoconazole
and possibly itraconazole, posaconazole and
voriconazole - avoid.
Antivirals: concentration possibly increased by
atazanavir, darunavir, fosamprenavir, indinavir,
lopinavir, ritonavir, saquinavir and tipranavir - avoid.
Beta-blockers: avoid with sotalol.
Ciclosporin: concentration of both drugs possibly
increased.
Grapefruit juice: concentration of ranolazine possibly
increased - avoid.
Statins: concentration of simvastatin increased -
maximum dose of simvastatin is 20 mg.
Tacrolimus: concentration of tacrolimus increased. | | 代謝 | Extensively metabolised in the gastrointestinal tract and
liver. Four main metabolites have been identified.
Approximately 75% of a dose is excreted in the urine with
the remainder in the faeces. |
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