1-(4-ureidobenzoyl)piperazine derivatives

US8759352B2 · kind B2 · utility

Assignees

• MERCK SHARP & DOHME B.V. · NL
• PHARMACOPEIA, LLC · US

Inventors

• Andrew Cooke · Doylestown, US
• David Jonathan Bennett · Watertown, US
• Andrew Stanley Edwards · Lanark, GB
• Andrew Roughton · Port Hope, CA
• Irina Neagu · Plainsboro, US
• Jui-Hsiang Chan · Plainsboro, US
• Koc-Kan Ho · Mount Kisco, US
• Nasrin Ansari · Monmouth Junction, US
• Michelle L. Morris · Lawrenceville, US
• Yajing Rong · Monmouth Junction, US
• Michael Ohlmeyer · Plainsboro, US

Key dates

• Filing date: Aug 26, 2009
• Grant date: Jun 24, 2014
• Expiry date: Jul 27, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D333/38
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C1-8)alkyl, (C3-8)cycloalkyl or (C3-8)cycloalkyl(C1-3)alkyl, each of which may be substituted by hydroxy, cyano or halogen; R2 represents 1 or 2 optional halogens; R3 is (C1-6)alkyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.