Bo Ram Lee,Bong-Yong Lee,Hoe Chul Jung,Hye Young Han,Hyn Jung Lee,Hyun Joo Son,Jae Sun Kin,Je Ho Ryu,Joon Ho Sa,Ju Young Lee,Jung A Lee,Kem Ho Ryu,Nam Ho Ryu,Shin Ae Kim,Sung Hoon Park,Won-No Youn,Yon
申请号:
BR112012028527
公开号:
BR112012028527A2
申请日:
2011.05.04
申请国别(地区):
BR
年份:
2020
代理人:
摘要:
amide compound, pharmaceutical composition and 11beta-hsd1 inhibitor comprising said compound and uses of said compound are provided picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing them, a pharmaceutical composition containing them, and a medical use of the compound as an agent for the prevention, regulation and treatment of diseases related to the regulation of glucocorticoids by the use of selective inhibitory activity of the compound for an 11 (beta) -hsd1 enzyme. the picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11 (beta) -hsd1 enzymes, and are useful in an agent for the prevention, regulation and treatment of diseases related to the regulation of glucocorticoids in which human-derived 11 (beta) -hsd1 enzymes are involved, for example, in metabolic syndromes such as type 1 and type 2 diabetes, late diabetes complications, latent autoimmune adult diabetes (lada), insulin tolerance syndromes, obesity, tolerance impaired glucose (igt), deficient fasting glucose (ifg), impaired glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc.composto de amida, composição farmacêutica e inibidor de 11beta-hsd1 compreendendo o dito composto e usos do dito composto são fornecidos compostos de picolinamida e pirimidina-4-carboxamida, um método para a preparação dos mesmos, uma composição farmacêutica que contém os mesmos, e um uso médico do composto como um agente para a prevenção, regulação e tratamento de doenças relacionadas à regulação de glicocorticoides pelo uso de atividade inibidora seletiva do composto para uma enzima 11(beta)-hsd1. os compostos de picolinamida e pirimidina-4-carboxamida da presente invenção são inibidores seletivos de enzimas 11(beta)-hsd1 derivadas de humanos, e são úteis em um agente para a prevenção, regulação e tratamento de doenças relacionadas à regulação de glicocorticoide em que as enzimas 11(beta)-hsd1 derivadas de humanos estão env