| 摘要 |
THE PRESENT INVENTION RELATES TO NOVEL FUSED AZOLEPYRIMIDINE DERIVATIVES, PROCESSES FOR PREPARING THEM AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM. THE FUSED AZOLEPYRIMIDINE DERIVATIVES OF THE PRESENT INVENTION EXHIBIT ENHANCED POTENCY FOR PHOSPHOTIDYLINOSITOL-3-KINASE (PI3K) INHIBITION, ESPECIALLY FOR PI3K- INHIBITION AND CAN BE USED FOR THE PROPHYLAXIS AND TREATMENT OF DISEASES ASSOCIATED WITH PI3K AND PARTICULARLY WITH PI3K- ACTIVITY. MORE SPECIFICALLY, THE AZOLE DERIVATIVES OF THE PRESENT INVENTION ARE USEFUL FOR TREATMENT AND PROPHYLAXIS OF DISEASES AS FOLLOWS: INFLAMMATORY AND IMMUNO-REGULATORY DISORDERS, SUCH AS ASTHMA, ATOPIC DERMATITIS, RHINITIS, ALLERGIC DISEASES, CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), SEPTIC SHOCK, JOINT DISEASES, AUTO-IMMUNE PATHOLOGIES SUCH AS RHEUMATOID ARTHRITIS, AND GRAVES’ DISEASE, CANCER, MYO-CARDIAL CONTRACTILITY DISORDERS, HEART FAILURE, THROMBOEMBOLISM, ISCHEMIA, AND ATHEROSCLEROSIS. THE COMPOUNDS OF THE PRESENT INVENTION ARE ALSO USEFUL FOR PULMONARY HYPERTENSION, RENAL FAILURE, CARDIAC HYPERTOPHY, AS WELL AS NEURODEGENERATIVE DISORDERS SUCH AS PARKINSON’S DISEASE, ALZHEIMER’S DISEASE, DIABETES AND FOCAL ISCHEMIA, SINCE THE DISEASES ALSO RELATE TO PI3K ACTIVITY IN A HUMAN OR ANIMAL SUBJECT.
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