Jenny Jinyi Tan

US Patent:

20130178461, Jul 11, 2013

Filed:

Mar 1, 2013

Appl. No.:

13/781815

Inventors:

Roland Joseph Billedeau - Santa Clara CA, US
Christine E. Brotherton-Pleiss - Sunnyvale CA, US
Fariborz Firooznia - Florham Park NJ, US
Stephen Deems Gabriel - Morristown NJ, US
Xiaochun Han - Cedar Grove NJ, US
Ramona Hilgenkamp - Montclair NJ, US
Saul Jaime-Figueroa - Morris Plains NJ, US
Buelent Kocer - Shanghai, CN
Francisco Javier Lopez-Tapia - Mahwah NJ, US
Yan Lou - Pleasanton CA, US
Lucja Orzechowski - Kinnelon NJ, US
Timothy D. Owens - San Carlos CA, US
Jenny Tan - New Providence NJ, US
Peter Michael Wovkulich - Nutley NJ, US

Assignee:

Hoffmann-La Roche Inc. - Nutley NJ

International Classification:

C07D 401/14
C07D 405/14
C07D 487/04

US Classification:

51421021, 544114, 5142352, 544238, 51425204, 514249

Abstract:

This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I:wherein, variables X, R, and Y, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.