A New salt form of Tenofovir alafenamide Method for Preparing or Use Thereof

The present inventors have been researched to develop a novel salt form which overcomes problems of low water solubility of tenofovir alafenamide hemifumarate currently on the market and only 1% of oral absorption rate thereof, and increases a pharmacological effect. As a result, provided is tenofov...

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Hauptverfasser:	AN JI HUN, KO MIN JU
Format:	Patent
Sprache:	eng ; kor
Schlagworte:	ACYCLIC OR CARBOCYCLIC COMPOUNDS ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM CHEMISTRY 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:	The present inventors have been researched to develop a novel salt form which overcomes problems of low water solubility of tenofovir alafenamide hemifumarate currently on the market and only 1% of oral absorption rate thereof, and increases a pharmacological effect. As a result, provided is tenofovir alafenamide heminapadisilate having water solubility 240 times higher than that of the tenofovir alafenamide hemifumarate. The tenofovir alafenamide heminapadisilate can be efficiently used as a pharmaceutical composition for treating or preventing HIV-1 infection and chronic hepatitis B. 본 발명자들은 현재 시판되고 있는 테노포비어 알라펜아미드 헤미푸마르산염의 낮은 수용해도 및 1%밖에 되지 않은 경구 흡수율의 문제점을 극복하여 약리적 효과를 높일 수 있는 신규한 염 형태를 개발하기 위해 연구 노력한 결과 테노포비어 알라펜아미드 헤미푸마르산 보다 수용해도가 240배 증가 된 테노포비어 알라펜아미드 헤미나파다실레이트로서 HIV-1 감염 및 만성 B형 간염의 치료에 유용한 치료 또는 예방용 약제학적 조성물로 사용될 수 있다.