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US 7,608,633 B2Granted
Heteroaryl-substituted acetone derivatives as inhibitors of phospholipase A2
AssigneeMerckle GmbH
InventorsMatthias Lehr, Joachim Ludwig
Life of this patent
Estimating the term…
Abstract
The invention relates to novel heteroaryl substituted acetone derivatives which inhibit the enzyme phospholipase A2, pharmaceutical preparations containing these compounds and a method of producing these compounds.
Claims18
A compound of formula I
- wherein
- Q represents R1, OR1, SR1, SOR1, SO2R1, NR9R1 or a straight-chain C1-31 alkyl or C2-31 alkenyl or alkinyl group which is optionally interrupted by 1 or 2 groups, independently selected from O, S, SO, SO2, NR9 and aryl which are optionally substituted with 1 or 2 substituents R4, and which are optionally substituted with 1-4 C1-6 alkyl groups and/or 1 or 2 aryl groups, wherein the aryl groups is optionally substituted with 1 or 2 substituents R4;
- Ar represents an aryl group selected from the group consisting of a phenyl, naphthyl, biphenyl, and 5-membered heterocylic ring and 6-membered heterocyclic ring, said aryl group containing 1 to 3 atoms selected from O, N, or S and optionally annellated using a benzene ring and further which is optionally substituted with 1 or 2 substituents R4;
- X represents N or CR5;
- Y represents N or CR6;
- R1 represents H or an aryl group which is optionally substituted with 1 or 2 substituents R4;
- R2 and R3 a) independently stand for H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or R7—W, or b) together with the carbon atoms to which they are bound, form a 5- or 6-membered aromatic or heteroaromatic ring which is optionally substituted with 1 or 2 substituents R4;
- R4 represents C1-6 alkyl, halogen, CF3, CN, NO2, OR9, S(O)0R9, COR9, COOR9, CONR9R10, SO3R9, SO2NR9R10, tetrazolyl or R7—W
- R5 represents H or R4;
- R6 represents H, C1-6 alkyl, halogen, CF3, CN, NO2, OR9, S(O)0R9, COR9, COOR9, CONR9R10, SO3R9, SO2NR9R10, tetrazolyl or R8—W;
- R7 represents C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl;
- R8 represents C2-6 alkyl, C2-6 alkenyl or C2-6 alkynyl;
- R9 represents H, C1-6 alkyl or aryl;
- R10 represents H or C1-6 alkyl;
- W represents COOH, SO3H or tetrazolyl;
- and
- o represents 0, 1 or 2;
- and the pharmaceutically compatible salts and esters thereof.
15 more elements
Dependencies are inferred from the claim text.