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US 8,008,307 B2Granted
Heteroaryl compounds useful as inhibitors of E1 activating enzymes
AssigneeMillennium Pharmaceuticals, Inc.
InventorsChristopher F. Claiborne, Stephen Critchley, Courtney Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
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Abstract
This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
Claims17
A chemical entity which is a compound having the formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- X is —NH— or —O—;
- Ra is hydrogen or —OH;
- Rc is hydrogen or —OH;
- W is —NH—, —N(R1)— or —O—, wherein R1 is C1-4 aliphatic;
- one of D and E is —N═and the other is —C(Rh)═;
- each Rh is independently hydrogen, halo or C1-4 aliphatic;
- R8 is hydrogen or C1-4 aliphatic;
- each Rp is independently halo or C1-4 aliphatic;
- each R8p is independently halo;
- C1-4 aliphatic optionally substituted with —OR5x or —C(O)—N(R4x)(R4y), wherein R5x is hydrogen or C1-4 alkyl, R4x is hydrogen or C1-4 alkyl, and R4y is hydrogen or C1-4 alkyl;
- —OR 5x wherein R5x is hydrogen or C1-4 alkyl;
- or —C(O)—N(R4x)(R4y) wherein R4x is hydrogen or C1-4 alkyl and R4y is hydrogen or C1-4 alkyl;
- s is 0, 1 or 2;
- and
- t is 0, 1 or 2.
13 more elements
Dependencies are inferred from the claim text.