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US 2010/0303758 A1Published application
Novel Glucocorticoid Receptor Agonists
OwnerPaul Alan Glossop, David Simon Millan +1inventors
InventorsPaul Alan Glossop, David Simon Millan, David Anthony Price
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Abstract
This invention relates to novel glucocorticoid receptor agonists of formula (I): and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
Claims30
A compound of formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 and R2 are independently of each other selected from H, F, Cl and methyl;
- R is selected from —CH2—OH, —O—CH2—CN, —S—CH2—CN, —O—CH2F, —S—CH2F, —O—CH2Cl and —S—CH2Cl;
- X is a direct bond or is selected from —O—, —S—, —CH2—S—, —S—CH2—, —CH2—, —O—CH2, and —CH2—O—;
- Ar1 is a phenyl or a pyridine;
- Ar2 is an aryl group selected from phenyl, pyridine, pyridazine, pyrazine and pyrimidine;
- R3 is H or OH;
- R4 is H or OH;
- and
- R5 is selected from H, CN, halogen, (C1-C4)alkyl, —S—(C1-C4)alkyl, —CONR7R8, —SO2NR7R8 and NHSO2CH3;
- R6 is H or CH3;
- and
- R7 and R8 are the same or are different and are independently selected from H and (C1-C4)alkyl.
10 more elements
A compound of formula (IV):
- wherein
- R1 and R2 are independently of each other selected from H, F, Cl and methyl;
- Y is O or S;
- X is a direct bond or is selected from —O—, —S—, —CH2—S—, —S—CH2—, —CH2—, —O—CH2, and —CH2—O—;
- Ar1 is a phenyl or a pyridine;
- Ar2 is an aryl group selected from phenyl, pyridine, pyridazine, pyrazine and pyrimidine;
- R3 is H or OH;
- R4 is H or OH;
- and
- R5 is selected from H, CN, halogen, (C1-C4)alkyl, —S—(C1-C4)alkyl, —CONR7R8, —SO2NR7R8 and NHSO2CH3;
- R6 is H or CH3;
- and
- R7 and R8 are the same or are different and are independently selected from H and (C1-C4)alkyl.
10 more elements
Dependencies are inferred from the claim text.