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US 8,772,536 B2Granted
Proteasome inhibitors
AssigneeMillennium Pharmaceuticals, Inc.
InventorsEdward J. Olhava, Mihaela Diana Danca
Life of this patent
Estimating the term…
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.
Claims42
A process for generating a compound of Formula (v)
- wherein Ring A is selected from the group consisting of
- the process comprising:
- (1) reacting a compound of Formula (i) with a compound of Formula (ii) to form a compound of Formula (iii)
- wherein PG is a protecting group;
- wherein Z1 and Z2, together with the Boron atom to which they are attached, form a boronic ester protecting group;
- wherein X1− is a counter anion;
- (2) deprotecting the compound of Formula (iii) to form a compound of Formula (iiia);
- wherein X2 is a counter anion;
- (3) reacting the compound of Formula (iiia) with a compound of Formula (viii) to form a compound of Formula (iv);
- and
- (4) deprotecting the compound of Formula (iv) to form the compound of Formula (v).
8 more elements
A process for generating a compound of Formula (v)
- wherein Ring A is selected from the group consisting of
- the process comprising:
- (1a) reacting a compound of Formula (viii) with a compound of Formula (vi) to form a compound of Formula (vii)
- wherein PG is a protecting group;
- wherein X2− is a counter anion;
- (2a) deprotecting the compound of Formula (vii) to form a compound of Formula (viia);
- (3a) reacting the compound of Formula (viia) with a compound of Formula (i) to form a compound of Formula (iv)
- wherein Z1 and Z2, together with the Boron atom to which they are attached, form a boronic ester protecting group;
- wherein X1− is a counter anion;
- and
- (4) deprotecting the compound of Formula (iv) to form a compound of Formula (v).
8 more elements
A compound of Formula (iii)
- wherein PG is a protecting group.
A compound of Formula (iiia)
A compound of Formula (iv)
- wherein Ring A is selected from the group consisting of
A compound of Formula (vii)
- wherein PG is a protecting group;
- and
- Ring A is selected from the group consisting of
A compound of Formula (viia)
- wherein Ring A is selected from the group consisting of
Dependencies are inferred from the claim text.