IL17 and IFN-gamma inhibition for the treatment of autoimmune inflammation
Inventors
Leban, Johann • Tasler, Stefan • Baumgartner, Roland • Saeb, Wael • Chevrier, Carine
Assignees
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Publication Number
US-8592456-B2
Publication Date
2013-11-26
Expiration Date
Abstract
The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
Core Innovation
The invention relates to compounds of formula (I) and pharmaceutically acceptable salts or solvates thereof. The compounds are defined by structural variables R1, Ar, Z, and Y, with R1 selected from aryl, heteroaryl, cycloalkyl, heterocyclyl or alkyl, optionally substituted by one or more substituents R′, and R1 not piperidinyl. Ar is aryl, cycloalkyl, heterocyclyl or heteroaryl, optionally substituted by one or more substituents R′.
In formula (I), Z is selected from H, halogen, —CR3O, —N(R3)2, —CN, —C(S)R3, carbonyl and thiocarbonyl-containing groups, amino and sulfonyl-related groups, and Y is H, halogen, haloalkyl, alkyl, or alkylester, optionally substituted by one or more substituents R′. The substituent definitions for R′ and R3 specify broad classes of groups, and R1, Ar, Z and Y may not comprise more than three coupled substituents R′ and/or R3.
The document further includes specific exemplified compounds within the claimed chemical scope, including substituted isoxazole, pyrazole, carboxylate, carboxamide, and carbothioate derivatives, with aryl and heteroaryl substitutions such as chlorophenyl, fluorophenyl, difluorophenyl, tetrafluorophenyl, pyridyl, and trifluoromethyl-containing motifs. It also includes example compounds and reported characterization data, together with biological testing sections and references to synthesis-route schemes in the disclosed examples.
Claims Coverage
The consolidated claim coverage centers on a general Formula (I) compound genus with defined R1, Ar, Z and Y classes, an exclusion of piperidinyl at R1, and a cap of not more than three coupled substituents across R1, Ar, Z and Y. Additional independent claims narrow the genus by fixing Y to an alkylester and by reciting specific enumerated compounds, with pharmaceutically acceptable salt or solvate coverage.
Compound of formula (I) with restricted substituent classes
A compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is aryl, heteroaryl, cycloalkyl, heterocyclyl or alkyl, optionally substituted by one or more substituents R′, and R1 is not piperidinyl; Ar is aryl, cycloalkyl, heterocyclyl or heteroaryl, optionally substituted by one or more substituents R′; Z is selected from H, halogen, —CR3O, —N(R3)2, —CN, —C(S)R3, carbonyl and thiocarbonyl-containing groups, amino and sulfonyl-related groups, and Y is H, halogen, haloalkyl, alkyl, or alkylester, optionally substituted by one or more substituents R′; R′ and R3 each independently represent defined substituent classes; and R1, Ar, Z and Y may not comprise more than three coupled substituents R′ and/or R3.
Compound of formula (I) with Y as alkylester
A compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein Y is alkylester, optionally substituted by one or more substituents R′, with the same R1, Ar, Z, R′ and R3 definitions and the same coupled-substituent limit.
Specific enumerated compounds and their pharmaceutically acceptable salts or solvates
A compound that is one of the specifically listed compounds, including named substituted isoxazole, pyrazole, carboxylate, carboxamide, and carbothioate derivatives, or a pharmaceutically acceptable salt or solvate thereof.
Overall, the claims cover a Formula (I) compound genus with defined structural-variable sets and a coupled-substituent limit, a narrower Formula (I) subset where Y is an alkylester, and a separately enumerated set of specific compounds, each with salt or solvate coverage.
Stated Advantages
Documented Applications
No documented applications found
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