Substituted pyrrolidine-2-one compounds
US8049019B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Oct 27, 2009 |
| Grant date | Nov 1, 2011 |
| Priority date | — |
| Expiry date | Jan 11, 2030 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D317/72
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide:wherein R1, R8, R9, R10, andare as described herein. Compounds that are useful intermediates of the process are also provided herein.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.