ERK1 ERK2 HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER

• Main Authors: THOMPSON SCOTT K, HALLUR GURULINGAPPA, MULLANGI RAMESH, SMITH ROGER A, ZAINUDDIN MOHD, MULAKALA CHANDRIKA, DEWANG PURUSHOTTAM M, KETHIRI RAGHAVA REDDY, VENKATESAN ARANAPAKAM M, REDDY SANJEEVA P
• Format: Patent
• Language: English; Korean
• Published: 02.03.2021
• 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 출원은 신규한 헤테로사이클릭 화합물 및 이의 약학적으로 허용가능한 염을 제공한다. 또한 이러한 화합물의 제조 방법이 제공된다. 이러한 화합물은 ERK1/2의 억제에 유용한다. 필요로 하는 환자에게 치료 유효량의 하나 이상의 화학식 I의 화합물(식 중, X, Y, Z, J, M, 및 R1 내지 R8은본원에서 정의됨)을 투여함으로써, 이러한 화합물은 RAS/RAF/MEK/ERK 경로의 조절이상과 연관된 상태의 치료에 유효하다. 이러한 화합물을 이용하여 다양한 상태가 치료될 수 있고, 비정상적 세포 증식을 특징으로 하는 질환이 포함된다. 하나의 구현예에서, 질환은 암이다. [화학식 I] JPEGpat00562.jpg4088 The present application provides a compound that is N-(2-amino-1-(3 -chloro-5 -fluorophenyl)ethyl)-1-(5-methyl-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)-1H-imidazole-4-carboxamide (shown below), or a pharmaceutically acceptable salt or stereoisomer thereof. Also provided are methods for preparing the compound. The compound is useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of the compound, the compouns is effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using the compound and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.