IP Library Patent Application 12117452
Patent Application
App. No. 12/117,452

COMBINATION THERAPY WITH PARP INHIBITORS

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Quick Facts
Patent No.
US None
App. No.
12/117,452
Abstract

The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with temozolomide (TMZ).

Claims (7)

1 . A method of treating bone metastasis in a mammal comprising administering thereto a PARP inhibitor of formula (I)

or a therapeutically acceptable salt thereof, wherein

R 1 , R 2 , and R 3 are independently selected from the group consisting of hydrogen, alkenyl, alkoxy, alkoxycarbonyl, alkyl, alkynyl, cyano, haloalkoxy, haloalkyl, halogen, hydroxy, hydroxyalkyl, nitro, NR A R B , and (NR A R B )carbonyl;

A is a nonaromatic 4, 5, 6, 7, or 8-membered ring that contains 1 or 2 nitrogen atoms and, optionally, one sulfur or oxygen atom, wherein the nonaromatic ring is optionally substituted with 1, 2, or 3 substituents selected from the group consisting of alkenyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkyl, alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, cyano, haloalkoxy, haloalkyl, halogen, heterocycle, heterocyclealkyl, heteroaryl, heteroarylalkyl, hydroxy, hydroxyalkyl, nitro, NR C R D , (NR C R D )alkyl, (NR C R D )carbonyl, (NR C R D )carbonylalkyl, and (NR C R D )sulfonyl; and

R A , R B , R C , and R D are independently selected from the group consisting of hydrogen, alkyl, and alkycarbonyl;

and temozolomide (TMZ).

2 . The method of claim 1 wherein the PARP inhibitor of formula (I) is 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 21, 2008
From: DONAWHO, CHERRIE K.; GIRANDA, VINCENT L.
To: ABBOTT LABORATORIES
Reel/Frame 021263/0059 →