LONG-ACTING FATTY ACID-PEPTIDE DERIVATIVE AND USE THEREOF

• Main Authors: KIM, Wan Seop, YOO, Tae Hyoung, KWON, Oh Chan
• Format: Patent
• Language: English; French; Korean
• Published: 13.07.2023
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to a long-acting fatty acid-peptide derivative and use thereof and, in particular, to a long-acting GLP-1/GLP-2 dual agonist, use thereof for treating intestinal diseases, intestinal damage, or gastric diseases, and the like. The fatty acid-peptide derivative of the present invention, which is an agonist for both GLP-1 and GLP-2 receptors, effectively stimulates GLP-1 and GLP-2 receptors known as targets for short bowel syndrome, has an excellent in-vivo long-acting effect compared to existing drugs, and exhibits a significantly superior therapeutic effect compared to a negative control and a positive control in a short bowel syndrome animal model, and thus can be effectively used in the prevention, amelioration and treatment of intestinal diseases and gastric diseases. La présente invention concerne un dérivé peptidique d'acide gras à action prolongée et son utilisation et, en particulier, un agoniste double de GLP-1/GLP-2 à action prolongée, son utilisation pour le traitement de maladies intestinales, de lésions intestinales ou de maladies gastriques, et analogues. Le dérivé peptidique d'acide gras selon la présente invention, qui est un agoniste pour les deux récepteurs GLP-1 et GLP-2, stimule de manière efficace les récepteurs GLP-1 et GLP-2 connus en tant que cibles pour le syndrome de l'intestin court, a un excellent effet d'action prolongée in vivo par rapport aux médicaments existants, et présente un effet thérapeutique significativement supérieur par rapport à un témoin négatif et un témoin positif dans un modèle animal de syndrome de l'intestin court, et peut ainsi être utilisé de manière efficace dans la prévention, le soulagement et le traitement de maladies intestinales et de maladies gastriques. 본 발명은 지속형 지방산-펩타이드 유도체 및 이의 용도에 관한 것으로, 구체적으로 지속형 GLP-1/GLP-2 이중 작용제 및 이의 장질환, 장손상, 또는 위질환 치료 용도 등에 관한 것이다. 본 발명의 지방산-펩타이드 유도체는 GLP-1과 GLP-2 수용체 모두에 대한 작용제로서, 단장증후군의 타겟으로 알려진 GLP-1 및 GLP-2 수용체를 효과적으로 자극하며, 기존 약물 대비 생체 내 우수한 효력 지속 효과를 가지고, 단장증후군 동물 모델에서 음성 대조군 및 양성 대조군과 비교하여 현저히 우수한 치료 효과를 나타내는 바, 장질환 및 위질환의 예방, 개선 및 치료에 유용하게 이용할 수 있다.