N2,N4-DIPHENYLPYRIMIDINE-2,4-DIAMINE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT FOR PREVENTION OR TREATMENT OF CANCER

• Main Authors: DUGGIRALA, Krishna Babu, JEON, Byeong Uk, LEE, Kwangho, SHIN, Inji, JUNG, Myoung Eun, KIM, Hwan, CHOI, Gildon, CHAE, Chong Hak, CHOE, Hyeon Jeong, PARK, Chae Won, CHO, Byoung Chul
• Format: Patent
• Language: English; French; Korean
• Published: 20.12.2018
• Subjects: CHEMISTRY; FOODS OR FOODSTUFFS; FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BYSUBCLASSES A23B - A23J; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OFNUTRITIVE QUALITIES, PHYSICAL TREATMENT; THEIR TREATMENT, NOT COVERED BY OTHER CLASSES

The present invention relates to a N2,N4-diphenylpyrimidine-2,4-diamine derivative, a method for preparing same, and a pharmaceutical composition containing same as an active ingredient for the prevention or treatment of cancer. The derivative shows a relatively weak EGFR activity inhibitory effect on wild-type EGFR, high inhibitory ability on EGFR mutation, and high inhibitory ability on even FLT3 or FLT3 mutation, and thus can be favorably used in the treatment of cancer with EGFR mutation or cancer with FLT3 or mutation thereof, and the derivative shows a synergy effect at the time of combinative administration, and thus can be favorably used in the treatment of combinative administration. La présente invention concerne un dérivé de N2,N4-diphénylpyrimidine-2,4-diamine, son procédé de préparation, et une composition pharmaceutique le contenant comme principe actif pour la prévention ou le traitement du cancer. Le dérivé présente un effet inhibiteur de l'activité d'EGFR relativement faible sur l'EGFR de type sauvage, une capacité inhibitrice élevée sur la mutation de l'EGFR, et une capacité inhibitrice élevée même sur FLT3 ou sur la mutation FLT3, et peut ainsi être utilisé favorablement dans le traitement du cancer à mutation de l'EGFR ou du cancer à FLT3 ou à mutation FLT3, et le dérivé présente un effet de synergie au moment de son administration combinée, et peut ainsi être favorablement utilisé dans le traitement par administration combinée. 본 발명은 N2,N4-디페닐피리미딘-2,4-디아민 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물에 관한 것이다. 상기 유도체가 야생형 EGFR에 대하여 상대적으로 약한 EGFR 활성억제효과를 나타내면서, EGFR 돌연변이에 대하여 높은 억제능을 나타내며, FLT 3 및 FLT3의 돌연변이에 대하여도 높은 억제능을 나타내므로, EGFR 돌연변이가 발생된 암이나 FLT 3 또는 이의 돌연변이가 발생된 암의 치료에 유용하게 사용될 수 있고, 병용투여시에 시너지 효과를 나타내므로, 병용투여 치료에도 유용하게 사용될 수 있다.