Heterocyclic substituted piperazines with CXCR3 antagonist activity

US8207170B2 · kind B2 · utility

Assignees

• SCHERING CORPORATION · US
• Pharmacopeia Drug Discovery, Inc. · US

Inventors

• Seong Heon Kim · Livingston, US
• Gopinadhan N. Anilkumar · Edison, US
• Michael K. C. Wong · New Brunswick, US
• Qingbei Zeng · Shanghai, CN
• Stuart B. Rosenblum · West Orange, US
• Joseph A. Kozlowski · Princeton, US
• Yuefei Shao · Princeton, US
• Brian F. McGuinness · Plainsboro, US
• Douglas W. Hobbs · Yardley, US

Key dates

• Filing date: Nov 23, 2010
• Grant date: Jun 26, 2012
• Expiry date: Nov 23, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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.