ロミタピドメシル酸塩化学構造式

ロミタピドメシル酸塩

化学名:ロミタピドメシル酸塩

CAS番号.202914-84-9

英語名:BMS 201038-04

CBNumberCB02627605

MFC40H41F6N3O5S

MW789.8260592

MOL File202914-84-9.mol

别名

ロミタピドメシル酸塩

ロミタピドメシル酸塩 (JAN)

メシル酸ロミタピド

ロミタピドメシル酸塩物理性質

貯蔵温度	Inert atmosphere,Room Temperature
溶解性	DMSO:100.0(Max Conc. mg/mL);126.61(Max Conc. mM) Ethanol:100.0(Max Conc. mg/mL);126.61(Max Conc. mM)
外見	Solid
色	White to off-white
CAS データベース	202914-84-9

危険有害性情報のコード(GHS)

ロミタピドメシル酸塩化学特性,用途語,生産方法

効能
脂質異常症治療薬, ミクロソームトリグリセリド輸送タンパク(MTTP)阻害薬
商品名
ジャクスタピッド (AEGERION PHARMACEUTICALS)
説明
Lomitapide is an orally active microsomal triglyceride transfer protein (MTP) inhibitor for the treatment of hypercholesterolemia. The drug was developed by Aegerion Pharmaceuticals Inc. and licensed to Bristol–Myers Squibb Co. and the University of Pennsylvania. Lomitapide effectively lowered LDL–cholesterol, both as a single agent and in combination with commonly prescribed lipid-lowering therapies. Sold under the trade name Juxtapid, the drug offers a new treatment option to patients who cannot tolerate statin therapy or who experience insufficient LDL–cholesterol reduction with the currently available therapies, such as patients with homozygous familial hypercholesterolemia caused by mutations in the LDLR gene.
定義
ChEBI: A methanesulfonate (mesylate) salt prepared from equimolar amounts of lomitapide and methanesulfonic acid. Used as a complement to a low-fat diet and other lipid-lowering treatments in patients with homozygous familial hypercholesterolemia.
合成
Commercial 9H-fluorene-9-carboxylic acid (105) was alkylated with 1,4-dibromobutane in the presence of n-butyl lithium in THF to give 9-(4-bromobutyl)-9H-fluorene-9-carboxylic acid (106) in 85% yield. Next, activation of the acid as the acid chloride followed by coupling with (2,2,2-trifluoroethylamine) provided amide 107 in 71% yield for the two-step sequence. Displacement of the terminal bromide with the appropriate 4-carbamoyl piperidine followed by removal of the Boc group furnished piperidinyl fluorine 108 in high yield. Amine 108 was then reacted with the acid chloride derived from acid 109 (derived from the Suzuki coupling of boronic acid 110 and o-iodobenzoic acid 111) to give lomitapide, and this was followed by salt formation with methanesulfonic acid to afford lomitapide mesylate (XIV).

ロミタピドメシル酸塩生産企業

202914-84-9, ロミタピドメシル酸塩キーワード

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ロミタピドメシル酸塩

危険有害性情報のコード(GHS)

ロミタピドメシル酸塩 化学特性,用途語,生産方法

ロミタピドメシル酸塩 生産企業

202914-84-9, ロミタピドメシル酸塩 キーワード

ロミタピドメシル酸塩化学特性,用途語,生産方法

ロミタピドメシル酸塩生産企業

202914-84-9, ロミタピドメシル酸塩キーワード