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1. WO2020222393 - NOVEL TENOFOVIR ALAFENAMIDE SALT AND PREPARATION METHOD THEREFOR

Publication Number WO/2020/222393
Publication Date 05.11.2020
International Application No. PCT/KR2019/018435
International Filing Date 24.12.2019
IPC
C07F 9/6561 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6561containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
C07C 309/35 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
309Sulfonic acids; Halides, esters, or anhydrides thereof
01Sulfonic acids
28having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
33of six-membered aromatic rings being part of condensed ring systems
34formed by two rings
35Naphthalene sulfonic acids
A61K 31/675 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61P 31/18 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
18for HIV
A61P 31/20 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
20for DNA viruses
CPC
A61K 31/675
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61P 31/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
18for HIV
A61P 31/20
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
20for DNA viruses
C07C 309/35
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
309Sulfonic acids; Halides, esters, or anhydrides thereof
01Sulfonic acids
28having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
33of six-membered aromatic rings being part of condensed ring systems
34formed by two rings
35Naphthalene sulfonic acids
C07F 9/65616
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6561containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
65616containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
Applicants
  • 유니셀랩 주식회사 UNICEL LAB CO., LTD. [KR]/[KR]
Inventors
  • 안지훈 AN, Ji Hun
  • 고민주 KO, Min Ju
Agents
  • 조현중 JHO, Hyun Joong
Priority Data
10-2019-005103730.04.2019KR
Publication Language Korean (KO)
Filing Language Korean (KO)
Designated States
Title
(EN) NOVEL TENOFOVIR ALAFENAMIDE SALT AND PREPARATION METHOD THEREFOR
(FR) NOUVEAU SEL DE TÉNOFOVIR ALAFÉNAMIDE ET SON PROCÉDÉ DE PRÉPARATION
(KO) 신규한 테노포비어 알라펜아미드 염 및 이의 제조방법
Abstract
(EN)
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.
(FR)
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
(KO)
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.
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