| 摘要 |
The disclosure relates to a family of 3,5-diaminopyrazole kinase inhibitors comprising a 1,3-imidazole base structure of Formula (IA), wherein R1 – R5 are disclosed in the specification, pharmaceutical salts of these compounds and pharmaceutical compositions comprising said salts. The disclosure also relates to the use of these compounds in treating a RC kinase-mediated disorder, such as asthma, allergic asthma, exercise induced asthma, allergic rhinitis, perennial allergic rhinitis, seasonal allergic rhinitis, atopic dermatitis, contact hypersensitivity, contact dermatitis, conjunctivitis, allergic conjunctivitis, eosinophilic bronchitis, food allergies, eosinophilic gastroenteritis, inflammatory bowel disease, ulcerative colitis, Crohn’s disease, mastocytosis, hyper IgE syndrome, systemic lupus erythematous, psoriasis, acne, multiple sclerosis, allograft rejection, reperfusion injury, chronic obstructive pulmonary disease, Churg-Strauss syndrome, sinusitis, basophilic leukemia, chronic urticaria, basophilic leukocytosis, eczema, arthritis, rheumatoid arthritis, psoriatic arthritis, osteoarthritis, and cardiovascular disorders. Example salts include: 5-((4-hydroxybenzyl)amino)-3-((4-morpholinophenyl)amino)-3H-pyrazole-4-carboxamide, camphorsulfonic acid salt; 5-((4-hydroxybenzyl)amino)-3-((4-morpholinophenyl)amino)-3H-pyrazole-4-carboxamide, phosphoric acid salt; 5-((4-hydroxybenzyl)amino)-3-((4-morpholinophenyl)amino)-3H-pyrazole-4-carboxamide, sulfuric acid salt; 5-((4-hydroxybenzyl)amino)-3-((4-morpholinophenyl)amino)-3H-pyrazole-4-carboxamide, trifluoroacetic acid salt; 5-((4-hydroxybenzyl)amino)-3-((4-morpholinophenyl)amino)-3H-pyrazole-4-carboxamide, tartaric acid salt; 5-((4-hydroxybenzyl)amino)-3-((6-morpholinopyridin-3-yl)amino)-3H-pyrazole-4-carboxamide hyrochloride; 5-((4-hydroxybenzyl)amino)-3-((6-morpholinopyridin-3-yl)amino)-3H-pyrazole-4-carboxamide, methanesulfonic acid salt; 5-((4-hydroxybenzyl)amino)-3-((6-morpholinopyridin-3-yl)amino)-3H-pyrazole-4-carboxamide, phosphoric acid salt; 5-((4-hydroxybenzyl)amino)-3-((6-morpholinopyridin-3-yl)amino)-3H-pyrazole-4-carboxamide, sulfuric acid salt. |
