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US 2014/0179631 A1Published application
Derivatives of 1-amino-2-cyclopropylethylboronic acid
AssigneeMillennium Pharmaceuticals, Inc.
InventorsPaul E. Fleming, Jing Li
Life of this patent
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Abstract
The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
Claims21
A compound of formula (I):
- or a pharmaceutically acceptable salt or boronic acid anhydride thereof, wherein:
- A is 0, 1, or 2;
- P is hydrogen or an amino-group-blocking moiety;
- each Ra2 independently is hydrogen, C1-6 aliphatic, C1-6 fluoroaliphatic, —(CH2)m—CH2—RB, —(CH2)m—CH2—NHC(═NR4)NH—Y, —(CH2)m—CH2—CON(R4)2, —(CH2)m—CH2—N(R4)CON(R4)2, —(CH2)m—CH(R6)N(R4)2, —(CH2)m—CH(R5)—OR5, or —(CH2)m—CH(R5)—SR5;
- each Y independently is hydrogen, —CN, —NO2, or —S(O)2—R10;
- each RB independently is a substituted or unsubstituted mono- or bicyclic ring system;
- each R4 independently is hydrogen or a substituted or unsubstituted aliphatic, aryl, heteroaryl, or heterocyclyl group;
- or two R4 on the same nitrogen atom, taken together with the nitrogen atom, form a substituted or unsubstituted 4- to 8-membered heterocyclyl ring having, in addition to the nitrogen atom, 0-2 ring heteroatoms independently selected from N, O, and S;
- each R5 independently is hydrogen or a substituted or unsubstituted aliphatic, aryl, heteroaryl, or heterocyclyl group;
- each R6 independently is a substituted or unsubstituted aliphatic, aryl, or heteroaryl group;
- each R10 independently is C1-6 aliphatic, C6-10 aryl, or —N(R4)2;
- m is 0, 1, or 2;
- and
- Z1 and Z2 are each independently hydroxy, alkoxy, aryloxy, or aralkoxy;
- or Z1 and Z2 together form a moiety derived from a boronic acid complexing agent.
12 more elements
Dependencies are inferred from the claim text.