Tropane derivatives useful in therapy
AssigneeAgouron Pharmaceuticals, Inc.
InventorsPatricia Ann Basford, Peter Thomas Stephenson, Stefan Colin John Taylor, Anthony Wood
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Abstract
The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.
Claims20
A compound of formula (I)
- or a pharmaceutically acceptable salt or solvate thereof wherein:
- X and Y are selected from CH2 and NR4 such that one of X and Y is CH2 and the other is NR4;
- R1 and R4 are independently R5;
- COR5;
- CO2R5;
- CONR6R7;
- SO2R5;
- or (C1-6 alkylene)phenyl, wherein phenyl is substituted by 0 to 3 atoms or groups selected from C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkoxy, C1-6 alkoxycarbonyl, halogen, CF3, OH, CN, NR6R7, COR7, CO2R7 or CONR6R7;
- R2 is phenyl substituted by 0 to 3 atoms or groups selected from C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkoxy, C1-6 alkoxycarbonyl, halogen, CF3, OH, CN, NR6R7, CO2R7 or CONR6R7;
- R3 is C1-4 alkyl substituted by 0 to 3 fluorine atoms;
- R5 is C1-6 alkyl;
- C2-6 alkenyl;
- C2-6 alkynyl;
- C3-7 cycloalkyl;
- a 5 or 6-membered aromatic heterocycle;
- or a 4 to 7-membered saturated heterocycle;
- wherein said alkyl, alkenyl, alkynyl and cycloalkyl are substituted by 0 to 3 atoms or groups selected from oxo, halogen, CF3, OR7, CN, NR6R7, COR7, CO2R7 or CONR6R7;
- wherein said heterocycles contain one to three heteroatoms selected from N, O or S;
- and wherein said heterocycles are substituted by 0 to 3 atoms or groups selected from C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkoxy, C1-6 alkoxycarbonyl, halogen, CF3, OH, CN, NR6R7, COR7, CO2R7 or CONR6R7;
- R6 is H;
- C1-6 alkyl;
- C2-6alkenyl ;
- C2-6 alkynyl;
- C3-7 cycloalkyl;
- a 5 or 6-membered aromatic heterocycle;
- or a 4 to 7-membered saturated heterocycle;
- wherein said alkyl, alkenyl, alkynyl and cycloalkyl are substituted by 0 to 3 atoms or groups selected from oxo, halogen, CF3, OR7, CN, COR7 or CO2R7;
- wherein said heterocycles contain one to three heteroatoms selected from N, O or S;
- and wherein said heterocycles are substituted by 0 to 3 atoms or groups selected from C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkoxy, C1-6 alkoxycarbonyl, halogen, CF3, OH, CN, COR7 or CO2R7;
- R7 is H or C1-6 alkyl;
- or, when R6 and R7 are both attached to the same N atom, NR5R7 may also represent a 5 to 7 membered, saturated, partially unsaturated or aromatic, heterocycle containing from 0 to 2 additional heteroatoms selected from O, N or S.
A pharmaceutical composition comprising a compound of the formula (I) or a pharmaceutically acceptable salt or solvate thereof together with one or more pharmaceutically acceptable excipients, diluents or carriers.
Dependencies are inferred from the claim text.