Substituted Pyrazoles as Modulators of Chemokine Receptors
OwnerAnthony B. Pinkerton, Rowena Cube +4inventors
InventorsAnthony B. Pinkerton, Rowena Cube, John Hutchinson, Dehua Huang, Jean-Michel Vernier, Dong-Ming Shen
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Abstract
Substituted pyrazole compounds such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.
Claims7
A compound represented by Formula (I):
- wherein:
- R1 and R2 are each independently selected from —(C0-6alkyl)-W—(C6-14aryl), —(C0-6alkyl)-W-heterocycle and —(C0-6alkyl)-W—(C3-7cycloalkyl);
- R3 and R4 are each independently selected from —C0-6alkyl, —(C0-6alkyl)-W—(C1-6alkyl), —(C0-6alkyl)-W—(C3-7cycloalkyl), —(C0-6alkyl)-W—(C6-14aryl), —(C0-6alkyl)-W-heterocycle, and —C(O)OR6;
- where each of R1, R2, R3 and R4 is independently unsubstituted or substituted with 1-7 substituents, where each of said 1-7 substituents is independently selected from halo, hydroxy, —O—C1-3alkyl, trifluoromethyl, —C1-3alkyl, —CO2R6, —CN, —N(R6)2, —NR6COR6, —NRSO2R6, and —CONR6;
- R5 is selected from hydrogen, —C0-6alkyl, —(C0-6alkyl)—(C6-14aryl), —(C0-6alkyl)-heterocycle, —(C0-6alkyl)-C3-7cycloalkyl and —(C0-6alkyl)-CO2R6;
- R6 is independently selected from C1-6alkyl and NR5C(N)NH2, or two R6 join to form a ring selected from pyrrolidinyl, piperidinyl and azepanyl;
- X is CH2, N, O or S;
- W is selected from a single bond, —O—, —S—, —SO—, —SO2—, —CO—, —CO2—, —CONR6— and —NR6—;
- and
- n is 0-6;
- or a pharmaceutically acceptable salt or an individual diastereomer thereof.
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt or individual diastereomer thereof.
Dependencies are inferred from the claim text.