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US 6,649,640 B2Granted
Isoxazole compositions useful as inhibitors of ERK
AssigneeVertex Pharmaceuticals Incorporated
InventorsMichael Hale, James Janetka, Francois Maltais, Jingrong Cao
Life of this patent
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Abstract
Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
Claims10
A compound of formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- Ht is pyrrol-3-yl;
- said pyrrol-3-yl having R3 and QR4 substituents;
- A—B is N—O or O—N;
- R1 is hydrogen or NHR;
- T is a valence bond;
- Q is —C(O)— or —SO2—;
- each R is independently selected from hydrogen or an optionally substituted aliphatic group having one to six carbons;
- R2 is an aryl group substituted with up to three R8 substituents;
- R3 is hydrogen;
- R4 is —NHR6;
- R6 is —(CH2)yCH(R7)2;
- y is 0-6;
- each R7 is independently selected from R, aryl, or hydroxyalkyl, wherein said aryl ring is optionally substituted with halogen, R′, OR′, CO2R′, or SO2R′, wherein each R′ is independently selected from hydrogen or a C1-6 aliphatic group;
- and
- each R8 is independently selected from halogen, —R′, or —OR′;
- wherein each R′ is independently selected from hydrogen or an optionally substituted aliphatic group.
14 more elements
Dependencies are inferred from the claim text.