Heterocyclic inhibitors of ERK2 and uses thereof

Details Heterocyclic inhibitors of ERK2 and uses thereof Heterocyclic inhibitors of ERK2 and uses thereof

2008-03-18

2008-03-18

Rao, Deepak (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C546S113000

Reexamination Certificate

active

11077188

ABSTRACT:
Described herein are compounds that are useful as protein kinase inhibitors having the formula:wherein A1, A2, TmR1, X, R2, R3, R9, R12, and R13are as described in the specification. The compounds are especially useful as inhibitors of ERK2, Aurora2, GSK3, CDK2, AKT3, and ROCK protein kinases and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, neurodegenerative disorders, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.

REFERENCES:
patent: WO 99/28315 (1999-06-01), None
patent: WO 01/56993 (2001-08-01), None
patent: WO 01/57022 (2001-08-01), None
patent: WO 02/064586 (2002-08-01), None
patent: WO 02/079193 (2002-10-01), None
Hoshino et al., “Constitutive activation of the 41-/43-KDa mitogen-activated protein kinase signaling pathway in human tumors,” Oncogene, 18:813-22 (1999).
Kortylewski et al., “Mitogen-activated protein kinases control p27/Kip1 expression and growth of human melanoma cells,” Biochemical Journal, 357(Pt 1):297-303 (2001).
Putz et al., “Epidermal growth factor (EGF) receptor blockade inhibits the action of EGF, insulin-like growth factor I, and a protein kinase A activator on the mitogen-activated protein kinase pathway in prostate cancer cell lines,” Cancer Research, 59(1):227-33 (1999).

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