IP Library › Granted Patent US 8,440,829
Granted Patent B2
US 8,440,829 · App. 13/347,886 · Granted May 14, 2013

PI3 kinase/mTOR dual inhibitor

Inventors: David Anthony Barda (Indianapolis, IN); Mary Margaret Mader (Fishers, IN)
Assignee: Eli Lilly and Company
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Quick Facts
Patent No.
US 8,440,829
App. No.
13/347,886
Granted
May 14, 2013
Kind
B2
Abstract

The present invention provides an imidazo[4,5-c]quinolin-2-one compound, or a pharmaceutically acceptable salt thereof, that inhibits both PI3K and mTOR and, therefore, is useful in the treatment of cancer.

Claims (6)

1. A compound which is 8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one, or a pharmaceutically acceptable salt thereof.

2. The compound according to claim 1 which is 8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one.

3. The compound according to claim 2 which is 8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one in crystalline form characterized by a X-ray powder diffraction pattern having characteristic peaks, in 2θ±0.2, occurring at 8.57 and one or more of 9.06, 15.93, 18.29, and 18.87.

4. A pharmaceutical composition comprising a compound which is 8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo [4,5-c]quinolin-2-one, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient.

5. The pharmaceutical composition according to claim 4 comprising the compound which is 8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one.

6. The pharmaceutical composition according to claim 5 comprising the compound which is 8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one in crystalline form characterized by a X-ray powder diffraction pattern having characteristic peaks, in 2θ±0.2, occurring at 8.57 and one or more of 9.06, 15.93, 18.29, and 18.87.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 11, 2012
From: BARDA, DAVID ANTHONY; MADER, MARY MARGARET
To: ELI LILLY AND COMPANY
Reel/Frame 027514/0819 →
Continuity (2)
Provisional Application 61432958 · Jan 14, 2011
Related Publication 20120184577A1 · Jul 19, 2012