Back to results
US 2004/0110794 A1Published application
Novel piperidine derivatives as modulators of chemokine receptors
AssigneeAstraZeneca AB
InventorsJeremy Burrows, John Cumming
Life of this patent
Estimating the term…
Abstract
The invention provides a compound of formula (I): wherein R1, R2, R3, R3a, R4, R4a, R5, and R6 are as defined; or a pharmaceutically acceptable salt thereof or a solvate thereof; compositions containing these compounds, processes for preparing them and their use as modulators of chemokine activity (especially CCR5 activity). 1
Claims12
A compound of formula (I):
- 18
- wherein:
- R1 is C3-7 cycloalkyl, C5-7 cycloalkenyl, heterocyclyl (itself optionally substituted by C1-4 alkyl), C1-8 alkyl (optionally substituted by C3-6 cycloalkyl, C5-6 cycloalkenyl, phenyl, heteroaryl, S(O)pR7, CO2R8), C3-6 alkenyl (optionally substituted by phenyl, heteroaryl, S(O)qR9, CO2R10) or C3-8 alkynyl;
- R2 is phenyl, heteroaryl, phenyl(C1-4 alkyl) or heteroaryl(C1-4 alkyl);
- R3, R3a, R4 and R4a are, independently, hydrogen or C1-4 alkyl;
- R5 is hydrogen, C1-4 alkyl (optionally substituted by halogen, hydroxy, C1-4 alkoxy, C3-7 cycloalkyl, SH, C1-4 alkylthio, cyano or S(O)q(C1-4 alkyl)), C3-4 alkenyl, C3-4 alkynyl or C3-7 cycloalkyl;
- R6 is phenyl, heteroaryl, phenylNH, heteroarylNH, phenyl(C1-2)alkyl, heteroaryl(C1-2)alkyl, phenyl(C1-2 alkyl)NH or heteroaryl(C1-2 alkyl)NH;
- R7 and R9 are, independently, C1-4 alkyl, or, when p or q is 0, C1-4 acyl;
- R8 and R10 are, independently, hydrogen or C1-4 alkyl;
- wherein the phenyl and heteroaryl rings of any of the foregoing are independently optionally substituted by halo, cyano, nitro, hydroxy, C1-4 alkyl, C1-4 alkoxy, S(O)mC1-4 alkyl, S(O)2NR11R12, NHS(O)2(C1-4 alkyl), NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2, NHC(O)NH2, C(O)NH2, C(O)NH(C1-4 alkyl), NHC(O)(C1-4 alkyl), CO2H, CO2(C1-4 alkyl), C(O)(C1-4 alkyl), CF3, CHF2, CH2F, CH2CF3 or OCF3;
- R11 and R12 are, independently, hydrogen or C1-4 alkyl, or together with a nitrogen or oxygen atom, may join to form a 5- or 6-membered ring which is optionally substituted with C1-4 alkyl, C(O)H or C(O)(C1-4 alkyl);
- m, p and q are, independently, 0, 1 or 2;
- or a pharmaceutically acceptable salt thereof or a solvate thereof.
10 more elements
A pharmaceutical composition which comprises a compound of the formula (I), or a pharmaceutically acceptable salt thereof or solvate thereof, and a pharmaceutically acceptable adjuvant, diluent or carrier.
Dependencies are inferred from the claim text.