Boronate ester compounds and pharmaceutical compositions thereof
AssigneeMillennium Pharmaceuticals, Inc.
InventorsEric L. Elliott, Abu J. Ferdous, Michael J. Kaufman, Sonja A. Komar, Debra L. Mazaik, Quentin J. Mccubbin, Phuong M. Nguyen, Vaithianathan Palaniappan, Raymond D. Skwierczynski, Nobel T. Truong, Csanad M. Varga, Peter N. Zawaneh
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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.
Claims51
A method for treating cancer, the method comprises administering to a patient in need of such treatment a therapeutically effective amount of a compound of formula (II):
- or a pharmaceutically acceptable salt thereof, wherein:
- A is 0;
- P is Rc—C(O)—;
- Rc is RD;
- RD is 2,5-dichlorophenyl;
- Ra is isobutyl;
- Ra1 is hydrogen;
- each Rb1 and Rb2 independently is hydrogen;
- each Rb3 and Rb4 independently is —(CH2)p—CO2H;
- wherein one of carboxylic acids optionally forms a further bond with the boron atom;
- p is 0 or 1;
- and
- n is 0 or 1.
A pharmaceutical composition, the pharmaceutical composition comprises a compound of formula (II):
- or a pharmaceutically acceptable salt thereof, wherein:
- A is 0;
- P is Rc—C(O)—;
- Rc is RD;
- RD is 2,5-dichlorophenyl;
- Ra is isobutyl;
- Ra1 is hydrogen;
- each Rb1 and Rb2 independently is hydrogen;
- each Rb3 and Rb4 independently is —(CH2)p—CO2H;
- wherein one of carboxylic acids optionally forms a further bond with the boron atom;
- p is 0 or 1;
- n is 0 or 1;
- and a pharmaceutically acceptable carrier.
A capsule comprising a compound of formula (II) in an amount of from about 0.2% to about 12%, by weight as a percentage of total weight;
- or a pharmaceutically acceptable salt thereof, wherein:
- A is 0;
- P is Rc—C(O)—;
- Rc is RD;
- RD is 2,5-dichlorophenyl;
- Ra is isobutyl;
- Ra1 is hydrogen;
- each Rb1 and Rb2 independently is hydrogen;
- each Rb3 and Rb4 independently is —(CH2)p—CO2H;
- wherein one of carboxylic acids optionally forms a further bond with the boron atom;
- p is 0 or 1;
- n is 0 or 1;
- and a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.