Abstract: Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, 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.
Type:
Grant
Filed:
May 13, 2005
Date of Patent:
April 20, 2010
Assignee:
Merck & Co., Inc.
Inventors:
Stephen D. Goble, Sander G. Mills, Lihu Yang, Alexander Pasternak, Celine Bonnefous, Theodore M Kamenecka, Jean-Michel Vernier, John H. Hutchinson, Essa Hu, Steven Govek
Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Type:
Grant
Filed:
October 13, 1998
Date of Patent:
August 15, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Jeffrey M. Bergman, Christopher J. Dinsmore, Samuel L. Graham