POLYMORPH OF PHARMACEUTICAL

PROBLEM TO BE SOLVED: To provide a novel crystalline polymorph of ritonavir, which is a human immunodeficiency virus (HIV) protease inhibitor, and a method for its preparation.SOLUTION: A crystalline polymorph of (2S,3S,5S)-5-(N-(N-((N-methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)carbonyl)-L-vali...

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Hauptverfasser:	BAUER JOHN F, NARAYANAN BIKSHANDARKOIL A, ALLEN KIMBERLY A, SPIWEK HARRY O, SALEKI-GERHARDT AZITA, BAUER PHILIP E, BURKAR SANJAY R, PATEL KETAN
Format:	Patent
Sprache:	eng ; jpn
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	PROBLEM TO BE SOLVED: To provide a novel crystalline polymorph of ritonavir, which is a human immunodeficiency virus (HIV) protease inhibitor, and a method for its preparation.SOLUTION: A crystalline polymorph of (2S,3S,5S)-5-(N-(N-((N-methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)carbonyl)-L-valinyl)amino)-2-(N-((5-thiazolyl)-methoxycarbonyl)amino)-1,6-diphenyl-3-hydroxyhexane has characteristic peaks in a powder X-ray diffraction pattern at values of 2θ of 8.67°±0.1°, 9.88°±0.1°, 16.11°±0.1°, 16.70°±0.1°, 17.36°±0.1°, 17.78°±0.1°, 18.40°±0.1°, 18.93°±0.1°, 20.07°±0.1°, 20.65°±0.1°, 21.71°±0.1°, and 25.38°±0.1°.SELECTED DRAWING: None 【課題】ヒト免疫不全症ウイルス（ＨＩＶ）プロテアーゼ阻害剤であるリトナビルの新規な結晶性多型体ならびにその調製法の提供。【解決手段】粉末Ｘ線回折パターンにおいて、２θの値が、８．６７°±０．１°、９．８８°±０．１°、１６．１１°±０．１°、１６．７０°±０．１°、１７．３６°±０．１°、１７．７８°±０．１°、１８．４０°±０．１°、１８．９３°±０．１°、２０．０７°±０．１°、２０．６５°±０．１°、２１．７１°±０．１°および２５．３８°±０．１°である特徴的なピークを有する（２Ｓ，３Ｓ，５Ｓ）−５−（Ｎ−（Ｎ−（（Ｎ−メチル−Ｎ−（（２−イソプロピル−４−チアゾリル）メチル）アミノ）カルボニル）−Ｌ−バリニル）アミノ）−２−（Ｎ−（（５−チアゾリル）メトキシカルボニル）アミノ）−１，６−ジフェニル−３−ヒドロキシヘキサンの結晶性多型体。【選択図】なし