Piperazine-piperidines with CXCR3 antagonist activity
View Patent ↗The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
1. A compound selected from the group consisting of:
Compound
Number
STRUCTURE
13
14
15
16
17
18
19
20
22
23
26
30
33
34
and
38
or a pharmaceutically acceptable salt thereof.
2. A compound selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
3. A compound according to claim 1 , selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
4. A pharmaceutical composition comprising at least one compound of claim 1 , or a pharmaceutically acceptable salt thereof, in combination with at least one pharmaceutically acceptable carrier.
5. The pharmaceutical composition of claim 4 , further comprising at least one additional agent, drug, medicament, antibody and/or inhibitor for treating a CXCR3 chemokine receptor mediated disease.
6. A pharmaceutical composition comprising at least one compound of claim 2 , or a pharmaceutically acceptable salt thereof, in combination with at least one pharmaceutically acceptable carrier.
7. The pharmaceutical composition of claim 6 , further comprising at least one additional agent, drug, medicament, antibody and/or inhibitor for treating a CXCR3 chemokine receptor mediated disease.