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1. WO2020196946 - LONG-ACTING FATTY ACID-BINDING GNRH DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

Publication Number WO/2020/196946
Publication Date 01.10.2020
International Application No. PCT/KR2019/003527
International Filing Date 26.03.2019
IPC
A61K 47/54 2017.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
A61K 47/69 2017.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
69the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
A61P 5/24 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
24of the sex hormones
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 15/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders; Contraceptives
02for disorders of the vagina
A61P 13/08 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
08of the prostate
Applicants
  • 노벨파마 주식회사 NOVEL PHARMA INC. [KR]/[KR]
Inventors
  • 진동규 JIN, Dong Kyu
Agents
  • 장덕순 CHANG, Duck Soon
  • 김시훈 KIM, Si Hoon
Priority Data
Publication Language Korean (KO)
Filing Language Korean (KO)
Designated States
Title
(EN) LONG-ACTING FATTY ACID-BINDING GNRH DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
(FR) DÉRIVÉ DE GNRH DE LIAISON AUX ACIDES GRAS À ACTION PROLONGÉE ET COMPOSITION PHARMACEUTIQUE CONTENANT CELUI-CI
(KO) 지속형 지방산 결합 GnRH 유도체 및 이를 포함하는 약제학적 조성물
Abstract
(EN)
One aspect of the present disclosure relates to a novel long-acting fatty acid-binding gonadotrophin-releasing hormone (GnRH) derivative of GnRH and a pharmaceutical composition comprising same. The present disclosure is expected to greatly contribute to reducing the frequency or dosage of medicines in the treatment of sex hormone-dependent diseases through excellent bioavailability, prolonged blood half-life, and remarkably excellent sex hormone-dependent disease treatment effects of the fatty acid-binding GnRH derivative. In particular, it will be possible to overcome the disadvantages of existing GnRH sustained-release preparations that have side effects of residual tenderness and pain at an injection site.
(FR)
Un aspect de la présente invention concerne un nouveau dérivé d'hormone de libération de gonadotrophines (GnRH) de liaison aux acide gras à action prolongée et une composition pharmaceutique le comprenant. La présente invention a pour but de contribuer grandement à réduire la fréquence ou le dosage de médicaments dans le traitement des maladies dépendant de l'hormone sexuelle par l'intermédiaire d'une excellente biodisponibilité, d'une demi-vie dans le sang prolongée, et grâce à des effets nettement excellents de traitement de la maladie dépendant de l'hormone sexuelle par le dérivé de GnRH de liaison aux acides gras. En particulier, il est possible de surmonter les inconvénients des préparations à libération prolongée de GnRH existantes ont pour effets secondaires une sensation résiduelle et une douleur au niveau du site d'injection.
(KO)
본 개시는 일 측면에 있어서, 생식샘자극 호르몬 방출 호르몬(gonadotrophin-releasing hormone; GnRH)의 신규한 지속형 지방산 결합 GnRH 유도체 및 이를 포함하는 약제학적 조성물에 관한 것이다. 본 개시는 지방산 결합 GnRH 유도체의 우수한 생체 이용률, 증가한 혈중 반감기, 현저하게 우수한 성 호르몬-의존성 질환 치료 효과를 통해 성 호르몬-의존성 질환 치료에 있어 의약의 투약 빈도수나 투약량 감소 등에 크게 기여할 것으로 기대된다. 특히, 기존의 주사 부위의 잔존감과 통증의 부작용을 가지고 있던 GnRH 서방형 제제들의 단점을 극복할 수 있을 것이다.
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