KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
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초록▼
The present invention relates to a pharmaceutical composition the prevention or treatment of DYRK-related diseases containing a pyridine-based compound as an active ingredient, a pyridine-based compound of the present invention which is used as an active ingredient of the pharmaceutical composition
The present invention relates to a pharmaceutical composition the prevention or treatment of DYRK-related diseases containing a pyridine-based compound as an active ingredient, a pyridine-based compound of the present invention which is used as an active ingredient of the pharmaceutical composition inhibits the activity of DYRK1A with very high efficacy and selectivity, thereby can be used effectively in the prevention or treatment of DYRK-related diseases, such as Down syndrome, degenerative brain diseases, cancer, and metabolic diseases.
대표청구항▼
1. A pharmaceutical composition for the prevention or treatment of DYRK-related diseases comprising a compound or a pharmaceutically acceptable salt thereof represented by formula 1 below as an active ingredient: (in formula 1 above,R1 is a hydrogen or —NR6R7, wherein R6 and R7 are each independentl
1. A pharmaceutical composition for the prevention or treatment of DYRK-related diseases comprising a compound or a pharmaceutically acceptable salt thereof represented by formula 1 below as an active ingredient: (in formula 1 above,R1 is a hydrogen or —NR6R7, wherein R6 and R7 are each independently a hydrogen, a C1-C5 straight or branched chain alkyl or benzyl;R2, R3 and R4 are each independently a hydrogen, a halogen, a C1-C5 straight or branched chain alkyl, —NR8R9, OR8, —CN, —NHC(O)R8, —SO2R8, —OS(O)2R8, pyrrolidine, piperidine, or morpholin, wherein R8 and R9 are each independently a hydrogen, a C1-C5 straight or branched chain alkyl, a C1-C5 straight or branched chain alkynyl, a C6-C12 straight or branched chain alkenyl, a C6-C12 aryl, a C6-C12 aryl substituted with a halogen, or a C6-C12 aryl substituted with a trihalogen methyl;R5 is a hydrogen, a C1-C5 straight or branched chain alkyl, unsubstituted 4-piperidine, acetyl-substituted 4-piperidin; andA is a carbon or a nitrogen). 2. The pharmaceutical composition of claim 1, wherein R1 is a hydrogen or —NR6R7, wherein R6 and R7 are each independently a hydrogen, a C1-C3 straight or branched chain alkyl; R2, R3 and R4 are each independently a hydrogen, —F, —Cl, —Br, —I, a C1-C3 straight or branched chain alkyl, —NR8R9, OR8, —CN, —NHC(O)R8, —SO2R8, —OS(O)2R8, pyrrolidine, piperidin or morpholin, wherein R8 and R9 are each independently a hydrogen, a C1-C5 straight or branched chain alkyl;R5 is a hydrogen, a C1-C3 straight or branched chain alkyl, unsubstituted 4-piperidine or acetyl-substituted 4-piperidin;A is a carbon or a nitrogen. 3. The pharmaceutical composition of claim 1, wherein R1 is a hydrogen or —NR6R7, wherein R6 and R7 are each independently a hydrogen, a C1-C3 straight or branched chain alkyl; R2, R3 and R4 are each independently a hydrogen, —F, —Cl, —Br, —I, a C1-C3 straight or branched chain alkyl;R5 is a hydrogen, a C1-C3 straight or branched chain alkyl, unsubstituted 4-piperidine or acetyl-substituted 4-piperidin;A is a nitrogen. 4. The pharmaceutical composition of claim 1, wherein the DYRK-related disease is at least one disease selected from the group consisting of Down syndrome, degenerative brain diseases, cancer diseases and metabolic diseases. 5. The pharmaceutical composition of claim 4, the degenerative brain disease is Pick's disease, vascular dementia, Alzheimer's disease, Parkinson's disease, Lewy body dementia, frontotemporal dementia, Creutzfeld-Jakob, Huntington's chorea, multiple sclerosis, Guillain-Barre syndrome and Down syndrome. 6. The pharmaceutical composition of claim 4, the cancer disease is selected from the group consisting of lung cancer, bone cancer, pancreatic cancer, skin cancer, head and neck cancer, uterine cancer, ovarian cancer, rectal cancer, cancer of the anal region, stomach cancer, colon cancer, breast cancer, carcinoma of the fallopian tubes, carcinoma of the endometrium, carcinoma of the cervix, carcinoma of the vagina, carcinoma of the vulva, cancer of the esophagus, cancer of the small intestine, cancer of the endocrine system, cancer of the thyroid gland, cancer of the parathyroid gland, cancer of the adrenal gland, sarcoma of soft tissue, cancer of the urethra, cancer of the penis, prostate cancer, chronic or acute leukemia, lymphocytic lymphoma, cancer of the bladder, cancer of the kidney or ureter, renal cell carcinoma, carcinoma of the renal pelvis, neoplasm of the central nervous system (CNS), primary CNS lymphoma, spinal axis tumor, brain stem glioma, pituitary adenoma. 7. The pharmaceutical composition of claim 4, the metabolic disease is selected from the group consisting of obesity, diabetes, hypertension, hyperlipidemia, hypercholesterolemia, arteriosclerosis, fatty liver, heart disease, myocardial infarction, angina. 8. A health functional food composition for the prevention or improvement of DYRK-related diseases comprising a compound or a pharmaceutically acceptable salt thereof represented by the following formula (1) as an active ingredient: (in formula 1,R1 is a hydrogen or —NR6R7, wherein R6 and R7 are each independently a hydrogen, a C1-C5 straight or branched chain alkyl or benzyl;R2, R3 and R4 are each independently a hydrogen, a halogen, a C1-C5 straight or branched chain alkyl, —NR8R9, OR8, —CN, —NHC(O)R8, —SO2R8, —OS(O)2R8, pyrrolidine, piperidine, or morpholin, wherein R8 and R9 are each independently a hydrogen, a C1-C5 straight or branched chain alkyl, a C1-C5 straight or branched chain alkynyl, a C6-C12 straight or branched chain alkenyl, a C6-C12 aryl, a C6-C12 aryl substituted with a halogen, or a C6-C12 aryl substituted with a trihalogen methyl;R5 is a hydrogen, a C1-C5 straight or branched chain alkyl, unsubstituted 4-piperidine, acetyl-substituted 4-piperidin; andA is a carbon or a nitrogen). 9. The health functional food composition of claim 8 wherein R1 is a hydrogen or —NR6R7, wherein R6 and R7 are each independently a hydrogen, a C1-C3 straight or branched chain alkyl; R2, R3 and R4 are each independently a hydrogen, —F, —Cl, —Br, —I, a C1-C3 straight or branched chain alkyl, —NR8R9, OR8, —CN, —NHC(O)R8, —SO2R8, —OS(O)2R8, pyrrolidine, piperidin or morpholin, wherein R8 and R9 are each independently a hydrogen, a C1-C5 straight or branched chain alkyl;R5 is a hydrogen, a C1-C3 straight or branched chain alkyl, unsubstituted 4-piperidine or acetyl-substituted 4-piperidin;A is a carbon or a nitrogen. 10. The health functional food composition of claim 8 wherein R1 is a hydrogen or —NR6R7, wherein R6 and R7 are each independently a hydrogen, a C1-C3 straight or branched chain alkyl; R2, R3 and R4 are each independently a hydrogen, —F, —Cl, —Br, —I, a C1-C3 straight or branched chain alkyl;R5 is a hydrogen, a C1-C3 straight or branched chain alkyl, unsubstituted 4-piperidine or acetyl-substituted 4-piperidin;A is a nitrogen.
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