NOVEL TENOFOVIR ALAFENAMIDE SALT AND PREPARATION METHOD THEREFOR

The present inventors have researched and made efforts to overcome the problems of currently commercially available tenofovir alafenamide hemifumarate, such as low water solubility and an oral absorption rate of only 1%, and to develop a novel salt form capable of enhancing a pharmacological effect....

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Bibliographische Detailangaben
Hauptverfasser:	AN, Ji Hun, KO, Min Ju
Format:	Patent
Sprache:	eng ; fre ; 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 researched and made efforts to overcome the problems of currently commercially available tenofovir alafenamide hemifumarate, such as low water solubility and an oral absorption rate of only 1%, and to develop a novel salt form capable of enhancing a pharmacological effect. As a result, tenofovir alafenamide heminapadisylate having water solubility 240 times that of tenofovir alafenamide hemifumarate can be used as a therapeutic or preventive pharmaceutical composition that is useful for the treatment of HIV-1 infection and chronic hepatitis B. La présente invention vise à résoudre les problèmes liés à l'hémifumarate de ténofovir alafénamide actuellement disponible dans le commerce, tels qu'une faible solubilité dans l'eau et un taux d'absorption orale de seulement 1 %, et à développer une nouvelle forme de sel permettant d'améliorer un effet pharmacologique. Par conséquent, l'héminapadisylate de ténofovir alafénamide, ayant une solubilité dans l'eau équivalente à 240 fois celle de l'hémifumarate de ténofovir alafénamide, peut être utilisé en tant que composition pharmaceutique thérapeutique ou préventive utile pour le traitement d'une infection par le VIH-1 et d'une hépatite B chronique 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.