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US 2002/0119994 A1Published application
LFA-1 Antagonist compounds
AssigneeGenentech, Inc.
InventorsDaniel J. Burdick, Mark S. Stanley, David Oare, Mark E. Reynolds, Thomas R. Gadek, James C. Marsters JR.
Life of this patent
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Abstract
The invention relates to novel compounds having formula (I) 1 wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD10 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.
Claims24
A compound of formula (I)
- 47
- wherein
- Cy is a non-aromatic carbocycle or heterocycle optionally substituted with hydroxyl, mercapto, thioalkyl, halogen, oxo, thio, amino, aminoalkyl, amidine, guanidine, nitro, alkyl, alkoxy or acyl;
- X is a divalent hydrocarbon chain optionally substituted with hydroxyl, mercapto, halogen, amino, aminoalkyl, nitro, oxo or thio and optionally interrupted with N, O, S, SO or SO2;
- Y is a carbocycle or heterocycle optionally substituted with hydroxyl, mercapto, halogen, oxo, thio, thioalkyl, amino, aminoalkyl, carbocycle or heterocycle ring, hydrocarbon, a halo-substituted hydrocarbon, amino, amidine, guanidine, cyano, nitro, alkoxy or acyl;
- L is a bond or a divalent hydrocarbon chain optionally substituted hydroxyl, halogen, oxo or thio and optionally interrupted with N, O, S, SO or SO2 or an amino acid residue;
- less than 3 or 5 atoms
- R1 is H, OH, amino, O-carbocycle or alkoxy optionally substituted with amino, a carbocycle or heterocycle;
- R2-5 are independently H, hydroxyl, mercapto, halogen, cyano, amino, amidine, guanidine, nitro or alkoxy;
- or R3 and R4 together form a fused carbocycle or heterocycle optionally substituted with hydroxyl, halogen, oxo, thio, amino, amidine, guanidine or alkoxy;
- R6 is H or a hydrocarbon chain optionally substituted with a carbocycle or a heterocycle;
- and
- salts, solvates and hydrates thereof;
- with the proviso that when Y is phenyl, R2, R4 and R5 are H, R3 is Cl and R1 is OH then X is other than cyclohexyl.
11 more elements
A method according to claim 23, wherein said disease or condition is arthritis, psoriasis, organ transplant rejection, asthma, and inflammatory bowel disease.
Dependencies are inferred from the claim text.