abstract |
A compound for use in the treatment or prevention of a disease selected from the group consisting of: psoriasis, atopic dermatitis, psoriatic arthritis, arthritis, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis, neurodegenerative disorder, congestive heart failure, stroke , aortic valve stenosis, kidney failure, pancreatitis, allergy, anemia, atherosclerosis, a metabolic disease, a cardiovascular disease, a complication related to chemotherapy / radiation, type I diabetes, type II diabetes, a liver disease, a gastrointestinal disorder , an ophthalmological disease, allergic conjunctivitis, diabetic retinopathy, Sjögren's syndrome, uveitis, a lung disease, an HIV-related cachexia renal disease, cerebral malaria, ankylosing spondylitis, lupus, dermatitis, leprosy, fibromyalgia, contact dermatitis, eczema, dry eye disease and Behcet's disease; in a human or animal, the compound having a structure: in which R1 is a member selected from a negative charge, a salt counterion, H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl , substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; R4a is a member selected from H, methyl, ethyl and substituted or unsubstituted aryl and substituted or unsubstituted arylalkyl; R10a is a member selected from H, halogen, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted arylalkoxy, substituted or unsubstituted arylthio, and substituted or unsubstituted aryl alkylthio; or a pharmaceutically acceptable salt thereof; wherein "alkyl" is a cyclic or straight or branched chain hydrocarbon radical, or a combination thereof, having the number of carbon atoms; wherein "aryl" is an aromatic substituent having 1 to 3 rings that fuse together or covalently bind; wherein "heteroaryl" is an aryl group containing one to four heteroatoms selected from B, N, O and S, in which the nitrogen and sulfur atoms are optionally oxidized and the nitrogen atom or atoms are optionally quaternized ; wherein the substituents for the alkyl, heteroalkyl cycloalkyl and heterocycloalkyl radicals are selected from the group consisting of: OR ', = O, = NR', = N-OR ', -NR'R ", -SR', - halogen , -OC (O) R ', -C (O) R', 35 -CO2R ', -CONR'R ", -OC (O) NR'R", -NR "C (O) R', -NR '-C (O) NR "R"', -NR "C (O) 2R ', -NR-C (NR'R" R "') = NR" ", -NRC (NR'R") = NR "', -S (O) R', - S (O) 2R ', -S (O) 2NR'R", -NRSO2R', -CN and -NO2 in a number from zero to (2m '+ 1), where m 'is the total number of carbon atoms in said radical; wherein R ', R ", R'" and R "" are each independently selected from hydrogen, unsubstituted heteroalkyl, unsubstituted aryl, unsubstituted alkyl, alkoxy or thioalkoxy groups, or arylalkyl groups; and when R 'and R "are attached to the same nitrogen atom, they can be combined with the nitrogen atom to form a 5-, 6- or 7-member ring; in which the substituents for the aryl and heteroaryl groups are selected from the group consisting of: halogen, OR ', = O, = NR', = N-OR ', - NR'R ", -SR', -halogen, -OC (O) R ', - C (O) R' , -CO2R ', -CONR'R ", - OC (O) NR'R", - NR "C (O) R', -NR'-C (O) NR" R "', -NR" C ( O) 2R ', -NR-C (NR'R "R"') = NR "", -NR-C (NR'R ") = NR" ', - S (O) R', -S (O ) 2R ', -S (O) 2NR'R ", -NRSO2R', -CN, -NO2, -R ', -N3, -CH (Ph) 2, fluoro (C1-C4) alkoxy and fluorine (C1- C4) alkyl, in a number ranging from zero to the total number of open valences in the aromatic ring system, and in which R ', R ", R'" and R "" are independently selected from hydrogen, non-alkyl substituted, unsubstituted heteroalkyl, unsubstituted aryl and unsubstituted heteroaryl. |