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US 2004/0063759 A1Published application
Novel piperidine derivatives
AssigneePfizer Inc.
InventorsLaura C. Blumberg, Matthew F. Brown, Matthew M. Hayward, Christopher S. Poss
Life of this patent
Estimating the term…
Abstract
A compound of the formula 1 wherein a, b, c R1, R2, R3, R4, R5, R6, R7, Q, W, Y, and Z are defined as above, useful as potent and selective inhibitors of MIP-1α (CCL3) binding to its receptor CCR1 found on inflammatory and immunomodulatory cells (preferably leukocytes and lymphocytes).
Claims15
A compound of the formula
- 23
- or pharmaceutically acceptable salts, tautomers, and pro-drugs thereof;
- wherein
- a is 1, 2, 3, 4or 5;
- b is 0, 1, 2, 3, or 4;
- c is 0 or 1;
- Q is (C1-C6)alkyl;
- W is (C6-C10)aryl or (C2-C9)heteroaryl;
- Y is oxygen, or NR8 wherein R8 is hydrogen or (C1-C6)alkyl;
- Z is oxygen or NR9, where R9 is hydrogen, (C1-C6)alkyl, or acetyl;
- each R1 is independently selected from the group consisting of:
- hydrogen, halo, cyano, nitro, trifluoromethyl, trifluoromethoxy, (C1-C6)alkyl, hydroxy, (C1-C6)alkylcarbonyloxy, and (C1-C6)alkoxy;
- R2, R3, R4 and R5 are each independently hydrogen or (C1-C6)alkyl optionally substituted with 1 to 3 halo groups;
- each R6 is independently selected from a list consisting of:
- hydrogen, halo, (C1-C6)alkyl optionally substituted with 1 to 3 halo groups;
- cyano, (C1-C6)alkoxy, aminocarbonyl, carboxy, (C1-C6)alkylcarbonyl, or (C1-C6)alkoxy optionally substituted by 1 to 3 halo groups;
- and
- R7 is selected from a list consisting of hydrogen, halo, (C1-C6)alkyl optionally substituted with 1 to 3 halo groups, [(C1-C6)alkyl]2amino(C1-C6)alkylaminocarbonyl, amino(C1-C6)alkylaminocarbonyl, (C1-C6)alkylamino(C1-C6)alkylaminocarbonyl cyano, (C1-C6)alkoxy, aminocarbonyl, (C1-C6)alkylaminocarbonyl, [(C1-C6)alkyl]2aminocarbonyl, (C1-C6)alkylsulfonylamino, (C1-C6)alkylsulfonylaminocarbonyl, ureido, aminosulfonyl, [(C1-C6)alkyl]2aminosulfonyl, (C1-C6)alkylaminosulfonyl, [(C1-C6)alkyl]2aminocarbonyl(C1-C6)alkylaminocarbonyl, (C1-C6)alkylaminocarbonyl(C1-C6)alkylaminocarbonyl, aminocarbonyl(C1-C6)alkylaminocarbonyl, (C1-C6)alkylsulfonylamino, hydroxy(C1-C6)alkylcarbonylamino, ureido(C1-C6)alkylaminocarbonyl, [(C1-C6)alkyl]2ureido(C1-C6)alkylaminocarbonyl, (C1-C6)alkylureido(C1-C6)alkylaminocarbonyl, (C2-C9)heteroarylaminocarbonyl, carboxy, (C1-C6)alkoxy(C1-C6)alkyl(C2-C9)heterocyclecarbonyl, (C2-C9)heterocyclecarbonyl, hydroxy(C2-C9)heterocyclecarbonyl, aminocarbonyl(C2-C9)heterocyclecarbonyl, carboxy(C2-C9)heterocyclecarbonyl, amino(C2-C9)heteroaryl(C1-C6)alkyl, (C1-C6)alkylamino(C2-C9)heteroaryl(C1-C6)alkyl, [(C1-C6)alkyl]2amino(C2-C9)heteroaryl(C1-C6)alkyl, (C2-C9)heteroarylamino(C1-C6)alkyl, (C2-C9)heteroarylaminocarbonyl(C1-C6)alkoxy, (C1-C6)alkylsulfonylaminocarbonyl(C1-C6)alkoxy, aminocarbonyl(C1-C6)alkoxy, carboxy(C1-C6)alkoxy, aminosulfonyl, (C1-C6)alkylcarbonylaminosulfonyl, hydroxy(C1-C6)alkylcarbonylaminosulfonyl, (C1-C6)alkoxycarbonylaminosulfonyl, (C1-C6)alkoxy(C1-C6)alkylcarbonylaminosulfonyl, hydroxysulfonyl, hydroxy, hydroxy(C1-C6)alkylaminocarbonyl, carboxy(C2-C9)heterocycloxy or [carboxy][amino](C1-C6)alkoxy, aminocarbonyl(C1-C6)alkylcarbonylamino, (C1-C6)alkylaminocarbonyl(C1-C6)alkylcarbonylamino, [(C1-C6)alkyl]2aminocarbonyl(C1-C6)alkylcarbonylamino, amino(C1-C6)alkylcarbonylamino, (C1-C6)alkylamino(C1-C6)alkylcarbonylamino, [(C1-C6)alkyl]2amino(C1-C6)alkylcarbonylamino, ureido(C1-C6)alkylcarbonylamino, (C1-C6)alkylureido(C1-C6)alkylcarbonylamino, [(C1-C6)alkyl]2ureido(C1-C6)alkylcarbonylamino, amino(C1-C6)alkylsulfonylamino, amino(C1-C6)alkylcarbonylaminosulfonyl, (C1-C6)alkylamino(C1-C6)alkylcarbonylaminosulfonyl, [(C1-C6)alkyl]2amino(C1-C6)alkylcarbonylaminosulfonyl, aminosulfonylamino, (C1-C6)alkylaminosulfonylamino, [(C1-C6)alkyl]2aminosulfonylamino, (C2-C9)heterocycloxy, (C2-C9)heteroaryloxy, (C2-C9)heterocycleamino, (C2-C9)heteroarylamino, amino(C1-C6)alkoxy, (C1-C6)alkylamino(C1-C6)alkoxy, [(C1-C6)alkyl]2amino(C1-C6)alkoxy, amino(C1-C6)alkylamino, (C1-C6)alkylcarbonylamino(C1-C6)alkylamino, ureido(C1-C6)alkylamino, hydroxy(C1-C6)alkylamino, (C1-C6)alkoxy(C1-C6)alkylamino, and (C1-C6)alkylsulfonylamino(C1-C6)alkylamino;
- with the proviso that at least one of R2, R3, R4, and R5 is (C1-C6)alkyl.
16 more elements
Dependencies are inferred from the claim text.