2, 4, 5-SUBSTITUTED PYRIMIDINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS EFFECTIVE INGREDIENT FOR PREVENTION OR TREATMENT OF CANCER OR INFLAMMATORY DISEASE

• Main Authors: LEE, Younho, KANG, Sein, SON, Jung Beom, JO, Seo Hyun, JUNG, Myungho, LI, Hua, KIM, Nam Doo, KIM, Joo Bin, SEOK, Jiyoon, JEON, Hyeonho, KIM, Hwan, KIM, Hyunkyung, SEO, Kyung-ah, LEE, Sun-Hwa, KANG, Juhee
• Format: Patent
• Language: English; French; Korean
• Published: 19.09.2019
• 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

The present invention relates to a 2, 4, 5-substituted pyrimidine derivative, a preparation method therefor, and a pharmaceutical composition comprising same as an effective ingredient for prevention or treatment of cancer or inflammatory disease. The compound exhibits high inhibitory activity against wild-type or mutant epidermal growth factor receptor (EGFR) and has an excellent inhibitory effect on JAK3, thus finding useful applications in the treatment of wild-type or mutant EGFR-expressed cancer or cancer or inflammatory disease associated with the activity of JAK3. Particularly, the compound can be useful for the treatment of lung cancer thanks to the excellent inhibitory activity thereof against the growth of lung cancer cell lines. La présente invention concerne un dérivé de pyrimidine substitué en positions 2, 4 et 5, son procédé de préparation, et une composition pharmaceutique le comprenant en tant que principe actif pour la prévention ou le traitement du cancer ou d'une maladie inflammatoire. Le composé présente une activité inhibitrice élevée contre le récepteur du facteur de croissance épidermique (EGFR) de type sauvage ou mutant et a un excellent effet inhibiteur sur JAK3, ce qui lui permet d'avoir des applications utiles dans le traitement du cancer ou du cancer exprimé par EGFR de type sauvage ou mutant ou d'une maladie inflammatoire associée à l'activité de JAK3. En particulier, le composé peut être utile pour le traitement du cancer du poumon grâce à l'excellente activité inhibitrice de celui-ci contre la croissance de lignées cellulaires du cancer du poumon. 2, 4, 5-치환된 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암 또는 염증질환의 예방 또는 치료용 약학적 조성물에 관한 것이다. 상기 화합물은 EGFR(epidermal growth factor receptor) 야생형 또는 돌연변이에 대하여 높은 억제능을 나타내고, JAK3에 대한 억제효과가 우수하므로, EGFR 야생형 또는 EGFR 돌연변이가 발현된 암이나, JAK3의 활성과 관련된 암 또는 염증질환의 치료에 유용하게 사용될 수 있고, 폐암 세포주 증식 억제능이 우수한 바, 특히, 폐암의 치료에 유용하게 사용될 수 있다.