HIF-1 Novel purine derivative compounds as HIF-1 protein inhibitor

• Main Authors: LEE JAE SANG, KIM SHIN AE, LEE BONG YONG, KIM A REUM, NAM GYEONG SUG, LEE JAE UN
• Format: Patent
• Language: English; Korean
• Published: 19.01.2024
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; 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

본 발명은 HIF-1 단백질 억제제 또는 혈관신생 유도인자 VEGF 억제제로서의 퓨린 유도체 화합물 및 이를 포함하는 관련 질환의 예방 또는 치료용 약학 조성물을 제공한다. 본 발명의 신규한 퓨린 유도체 화합물은 저산소 상태에서 안정화되는 전사인자인 HIF-1α 및 하위 유전자인 혈관신생 유도인자 VEGF의 발현에 있어서 우수한 억제 효과를 나타내는 것이 확인되어, HIF-1α 단백질 및 혈관신생 유도인자 VEGF 관련 질환의 예방 또는 치료 용도로 유용하게 사용될 수 있다. The present invention provides a purine derivative compound as a HIF-1 protein inhibitor or an inhibitor against VEGF as an angiogenesis inducer, and a pharmaceutical composition for the prevention or treatment of related diseases, comprising same. The novel purine derivative compound of the present invention was confirmed to exhibit an excellent inhibitory effect against the expression of HIF-1α, which is a transcription factor stabilized in hypoxia, and the angiogenesis inducer VEGF, which is a downstream gene, and thus can be effectively used for the prevention or treatment of diseases related to the HIF-1α protein and the angiogenesis inducer VEGF.