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リバーロキサバン

リバーロキサバン 化学構造式
366789-02-8
CAS番号.
366789-02-8
化学名:
リバーロキサバン
别名:
リバーロキサバン;リバロキサバン;リバーロキサバン (JAN)
英語化学名:
Rivaroxaban
英語别名:
CS-273;Xarelto;Rivaroxaba;Rivaroxban;Rivaroxaban;BAY 59-7939;Rivarobaxan;Rivanoxaban;(S)-Rivaroxaban;Rivaroxaban API
CBNumber:
CB91176772
化学式:
C19H18ClN3O5S
分子量:
435.88
MOL File:
366789-02-8.mol

リバーロキサバン 物理性質

融点 :
228-229°C
沸点 :
732.6±60.0 °C(Predicted)
比重(密度) :
1.460±0.06 g/cm3(Predicted)
貯蔵温度 :
Inert atmosphere,2-8°C
酸解離定数(Pka):
13.36±0.46(Predicted)

安全性情報

有毒物質データの 366789-02-8(Hazardous Substances Data)

リバーロキサバン 価格

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入

リバーロキサバン 化学特性,用途語,生産方法

用途

リバーロキサバン(Rivaroxaban)は経口抗凝固薬の一つである。最初に開発された直接第Xa因子阻害薬(英語版)である。商品名イグザレルト。消化管からの吸収率が高く、投与4時間後に第Xa因子の阻害効果が最大となり、効果は8?12時間持続する。 リバーロキサバンは血中の遊離第Xa因子およびプロトロンビナーゼ(英語版)複合体に結合した第Xa因子を共に阻害するよう最適化されたオキサゾリジノン(英語版)誘導体である。直接第Xa因子阻害選択性が高く、生物学的利用能も高いので、速やかに効果が発現する。第Xa因子の阻害は凝固系の内因性経路および外因性経路を両方阻害して、トロンビン生成および血栓形成を共に抑制する。リバーロキサバンはトロンビン(活性化第II因子)を阻害せず、また血小板に対して作用しないことが示されている。

効能

抗血栓薬, 第Xa因子阻害薬

商品名

イグザレルト (バイエル薬品); イグザレルト (バイエル薬品)

説明

Rivaroxaban is an orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM), which is a crucial component of the intrinsic and extrinsic pathways of the blood coagulation cascade. It demonstrates >10,000-fold greater selectivity for Factor Xa compared to other related serine proteases. In various animal arterial and venous thrombosis models, rivaroxaban is reported to inhibit thrombin formation without prolonging bleeding time and has been approved for clinical use as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.

説明

Venous thromboembolism continues to be a major health concern despite conventional anticoagulation therapies. Rivaroxaban is a recent market introduction that directly inhibits FXa with high potency (Ki=0.4 nM; IC50=0.7 nM) and selectivity>10,000-fold over other related serine proteases (thrombin, trypsin, plasmin, FVIIa, FIXa, FXIa, urokinase, and activated protein C). From the X-ray crystal structure, the central oxazolidinone moiety anchors the drug through two hydrogen bonds to Gly219 and directs the morpholinone group into the S4 pocket and the chlorothiophene portion into the S1 pocket. These key components may be coupled together synthetically by a couple of routes. Condensation of 3-morpholinone with 4-fluoronitrobenzene followed by catalytic hydrogenation provides N-(p-aminophenyl)morpholinone for subsequent reaction with (S)-2-(phthalimidomethyl)oxirane. With establishment of the aminoalcohol adduct, cyclization with 1,1′-carbonyldiimidazole generates the central oxazolidinone. Deprotection and acylation with 5-chlorothiophene-2-carbonyl chloride affords rivaroxaban.

化学的特性

White Solid

Originator

Bayer (Germany)

使用

anti-coagulant; Factor X inhibitor,Rivaroxaban is an orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM), which is a crucial component of the intrinsic and extrinsic pathways of the blood coagulation cascade.It demonstrates >10,000-fold greater selectivity for Factor Xa compared to other related serine proteases.In various animal arterial and venous thrombosis models, rivaroxaban is reported to inhibit thrombin formation without prolonging bleeding time and has been approved for clinical use as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.

使用

A novel antithrombotic agent. A highly potent and selective, direct FXa inhibitor

定義

ChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant u ed for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery.

brand name

Xarelto

副作用

Regarding safety, there was no statistical difference in the incidence of major postoperative bleeding between any of the rivaroxaban dose groups and enoxaparin although there did appear to be a dose dependency in the rivaroxaban set. In addition to bleeding and subsequent posthemorrhagic anemia, presenting as weakness, paleness, asthenia, dizziness, headache, or unexplained swelling, other common adverse events included nausea, increased GGT, and an increase in transglutaminase. Owing to its mechanism of action, there is a bleeding risk, so the drug is contraindicated in patients with clinically active bleeding. Rivaroxaban is also contraindicated in pregnant and breast-feeding women and in patients with hepatic disease associated with coagulopathy and clinically relevant bleeding risk.

Chemical Synthesis

Rivaroxaban is a recent market introduction that directly inhibits FXa with high potency (Ki 0.4 nM; IC50 0.7 nM) and selectivity, W10,000-fold over other related serine proteases (thrombin, trypsin, plasmin, FVIIa, FIXa, FXIa, urokinase, and activated protein C). From the X-ray crystal structure, the central oxazolidinone moiety anchors the drug through two hydrogen bonds to Gly219 and directs the morpholinone group into the S4 pocket and the chlorothiophene portion into the S1 pocket. These key components may be coupled together synthetically by a couple of routes. Condensation of 3-morpholinone with 4-fluoronitrobenzene followed by catalytic hydrogenation provides N-(p-aminophenyl)morpholinone for subsequent reaction with (S)-2-(phthalimidomethyl)oxirane. With establishment of the aminoalcohol adduct, cyclization with 1,1 -carbonyldiimidazole generates the central oxazolidinone. Deprotection and acylation with 5-chlorothiophene-2-carbonyl chloride affords rivaroxaban. The drug is formulated in 10-mg tablets for once-daily oral administration to patients undergoing elective hip or knee replacement surgery to prevent VTE.

リバーロキサバン 上流と下流の製品情報

原材料

準備製品


リバーロキサバン 生産企業

Global( 555)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Hebei Yirun Sega Biological Technology Co. Ltd
19932103556 +8619932103556
+8619932103556 linda@yrsjbiotech.com CHINA 1691 58
Baoji Guokang Healthchem co.,ltd
09178656283
cngksw@aliyun.com CHINA 9464 58
Nanjing Gold Pharmaceutical Technology Co. Ltd.
025-84209270 15906146951
025-84209270 wgp@nanjing-pharmaceutical.com CHINA 115 55
Shanghai Bojing Chemical Co.,Ltd.
+86-21-37122233
+86-21-37127788 Candy@bj-chem.com CHINA 497 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com China 22607 55
Jiangsu Zhongbang Pharmaceutical Co., Ltd.
025-87151996
025-87151996 zbsales@chinaredsun.com CHINA 32 55
Shanghai Time Chemicals CO., Ltd.
+8618017249410 +86-021-57951555
+86-021-57951555 jack.li@time-chemicals.com China 1807 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com China 9165 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070
product@chemlin.com.cn CHINA 3013 60

366789-02-8(リバーロキサバン)キーワード:


  • 366789-02-8
  • (S)-Rivaroxaban
  • (S)-5-Chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)-oxazolidin-5-yl)methyl)thiophene-2-carbox
  • RIVAROXABAN STAGE-IV [5-CHLORO-N-({5S)-2-OXO-3-[4-(3-OXO-4-MORPHOLINYL)PHENYL]-1,3-OXAZOLIDIN-5-YL}-METHYL)-2(AS PER INV
  • 5-Chloro-N-[[(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-5-oxazolidinyl]methyl]-2-thiophenecarboxamide
  • BAY 59-7939
  • Rivaroxaban Isomer
  • Rivaroxaban
  • 5-Chloro-N-(((5S)-2-oxo-3-(4-(3-oxomorpholin-4-yl)phenyl)-1,3-oxazolidin-5-yl)methyl)thiophene-2-carboxamide
  • 2-Thiophenecarboxamide, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-5-oxazolidinyl]methyl]
  • Xarelto
  • (S)-5-chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)thiophene-2-carboxamide
  • (S)-5-Chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)-oxazolidin-5-yl)methyl)thiophene-2-carboxami
  • Rivaroxaban (BAY59-7939)
  • Rivarobaxan
  • Rivaroxaban(Xarelto)
  • Rivaroxaba
  • Rivaroxaban API
  • Rivaroxban
  • Rivaroxaban, >=99%
  • CS-273
  • BAY 59-7939 (Rivaroxaban)
  • 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]oxazolidin-5-yl]methyl]thioph
  • Rivaroxaban intermediates
  • Rivanoxaban
  • (S)-5-chloro-N-{[2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]oxazolidin-5-yl]methyl} thiophene-2-carboxamide
  • Rivaroxaban fandachem
  • 5-Chloro-N-[[(S)-3-(4-(3-oxomorpholin-4-yl)phenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]-thiophene-2-carboxamide
  • Rivaroxaban USP/EP/BP
  • 2-Amino-15-picoline
  • 5-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide
  • リバーロキサバン
  • リバロキサバン
  • リバーロキサバン (JAN)
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