| abstract |
Claim 1: A compound of formula (1), wherein: X is a CH or N; Y is halo, trifluorphenoxy or tetrafluorphenoxy; R2 is straight or branched C1-6 alkyl; R3 is hydrogen, halo, OCF3, CN or CF3; and R4 is hydrogen, halo, OCF3, SR, CN, CF3, Ar or T-Ar; where: T is O or S; R is a straight or branched C1-6 alkyl; Ar is a phenyl ring optionally substituted with 1 to 3 groups selected from halo, CH3, CF3, CN, OMe, OCF3 and NR5R6; and R5 and R6 are each independently H or C1-6 straight or branched chain alkyl, or R5 and R6, taken together, form a 5 to 7 member ring that optionally contains up to 3 heteroatoms selected from O, S, NH and N (C1-6 straight or branched chain alkyl); whenever Y is halo, then R3 and R4 are not simultaneously hydrogen. Claim 21: A pharmaceutical composition comprising: a) a compound according to any one of claims 1 to 20; b) a pharmaceutically acceptable carrier, adjuvant or vehicle. Claim 22: A method of treating a disease in a patient, wherein said disease is selected from a disease regulated by IL-1, a disease regulated by apoptosis, an inflammatory disease, an autoimmune disease, a destructive bone disorder, a proliferative disorder , an infectious disease, a degenerative disease, a disease associated with cell death, a disease by ingestion of excess dietary alcohol, a viral regulated disease, retinal disorders, uveitis, inflammatory peritonitis, osteoarthritis, pancreatitis, asthma, syndrome adult respiratory failure, glomerulonephritis, rheumatoid arthritis, systemic lupus erythematosus, scleroderma, chronic thyroiditis, Grave disease, autoimmune gastritis, diabetes, autoimmune hemolytic anemia, autoimmune neutropenia, thrombocytopenia, chronic active hepatitis, myasthenia gravis, inflammatory bowel disease, Crohn, psoriasis, derma atopic titis, pathological scarring, graft versus host disease, organ transplant rejection, organ apoptosis after burn damage, osteoporosis, leukemia and related disorders, myelodysplastic syndrome, multiple myeloma-related bone disorder, acute myelogenous leukemia, myelogenous leukemia Chronic, metastatic melanoma, Kaposi's sarcoma, multiple myeloma, hemorrhagic shock, sepsis, septic shock, burns, siguelosis, Alzheimer's disease, Parkinson's disease, Huntington's disease, Kennedy disease, prion disease, cerebral ischemia, epilepsy, ischemia myocardium, acute and chronic heart disease, myocardial infarction, congestive heart failure, atherosclerosis, aortocoronary bypass (bypass), spinal muscular atrophy, amyotrophic lateral sclerosis, multiple sclerosis, HIV-related encephalitis, aging, alopecia, neurological damage due to stroke, ulcerati colitis goes, traumatic brain damage, spinal cord damage, hepatitis B, hepatitis C, hepatitis G, yellow fever, dengue fever, or Japanese encephalitis, various forms of liver disease, kidney disease, polycystic kidney disease, duodenal ulcer disease and gastric associated with H. Pylori, HIV infection, tuberculosis, meningitis, organ failure, treatment of complications associated with aortocoronary bypass (bypass), and immunotherapy for the treatment of various forms of cancer; wherein said method comprises the step of administering to said patient a pharmaceutical composition according to claim 21. Claim 31: A method of preparing a compound of formula (1), wherein said method comprises: reacting an acid or acid derivative of formula (2), with an amino alcohol of formula (4), to provide a compound of formula (3); converting intermediate (3) into compound (1), wherein: X is CH or N; Y is halo, trifluorphenoxy or tetrafluorphenoxy; R2 is straight or branched C1-6 alkyl; R3 is hydrogen, halo, OCF3, CN or CF3; and R4 is hydrogen, halo, OCF3, SR, CN, CF3, Ar or T-Ar; where: T is O or S; R is a straight or branched C1-6 alkyl; Ar is a phenyl ring optionally substituted with 1 to 3 groups selected from halo, CH3, CF3, CN, OMe, OCF3 and NR5R6; R5 and R6 are each independently H or C1-6 straight or branched chain alkyl, or R5 and R6, taken together, form a 5 to 7 member ring that optionally contains up to 3 heteroatoms selected from O, S , NH and N (C1-6 straight or branched chain alkyl); and R7 is a suitable protecting group; provided that when Y is halo, then R3 and R4 are not simultaneously hydrogen. Claim 32: A compound of formula (5), wherein: X is CH or N; R2 is straight or branched C1-6 alkyl; R3 is hydrogen, halo, OCF3, CN or CF3; and R4 is hydrogen, halo, OCF3, SR, CN, CF3, Ar or T-Ar; where: T is O or S; R is a straight or branched C1-6 alkyl; Ar is a phenyl ring optionally substituted with 1 to 3 groups selected from halo, CH3, CF3, CN, OMe, OCF3 and NR5R6; and R5 and R6 are each independently H or C1-6 straight or branched chain alkyl, or R5 and R6, taken together, form a 5 to 7 member ring that optionally contains up to 3 heteroatoms selected from O, S, NH and N (C1-6 straight or branched chain alkyl). |