Cyclic sulfone derivatives as inhibitors of matrix...

Details Cyclic sulfone derivatives as inhibitors of matrix... Cyclic sulfone derivatives as inhibitors of matrix...

2006-03-21

2006-03-21

Berch, Mark L. (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C544S054000, C544S057000, C544S058200, C544S059000, C544S060000, C544S061000, C544S062000, C514S227800, C514S228200, C549S014000, C549S078000

Reexamination Certificate

active

07015217

ABSTRACT:
The present application describes novel cyclic sulfone derivatives of formula I:or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof. In formula I, A is selected from —COR5, —CO2H, —CO2R6, —C(O)NHOH, —C(O)NHOR5, —C(O)NHOR6, —NHRa, —N(OH)COR5, —N(OH)CHO, —SH, —CH2SH, —S(O)(═NH)Ra, —S(═NH)2Ra, —SC(O)Ra, —PO(OH)2, and —PO(OH)NHRa; B is a thiomorpholine ring; X is absent or is CR3R4; and Ua, Xa, Ya, Za, R1, R2, Rb, and q are defined in the present specification.

REFERENCES:
patent: WO 00/40576 (2000-07-01), None
patent: WO 01/60808 (2001-08-01), None
Robert A. Greenwald {Annals of New York Academy of Sciences 878:413-419 (1999)}.
Skiles et al. {Current Medicinal Chemistry, 8, 425-474 (2001)}.
Moro et al. (Neurosignals 2003; 12:53-58).
Lou et al. {Mini Reviews in Medicinal Chemistry, 2003, 3, 609-620}.
Coussens et al. {SCIENCE vol. 295, 29 Mar., pp. 2387-2392, (2002)}.
Chalmers (TiPS vol. 17, pp. 166-172 Apr. 1996).

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