IP Library Granted Patent US 8,349,852
Granted Patent B2
US 8,349,852 · App. 12/683,317 · Granted Jan 8, 2013

Quinazolinone derivatives useful as vanilloid antagonists

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Quick Facts
Patent No.
US 8,349,852
App. No.
12/683,317
Granted
Jan 8, 2013
Kind
B2
Abstract

There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile and a method of preparing it.

Claims (6)

1. The crystal form B of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile having structural formula I(B);

characterized by an X-ray diffraction pattern having three or more peaks at 2θ values selected from 9.3, 10.6 and 14.4±0.2°2θ.

2. A method of preparing a compound of formula I(B) in crystal form B according to claim 1 which comprises crystallising the compound of formula I(B) from a solution thereof in water and a water miscible organic solvent.

3. A pharmaceutical composition comprising, as active ingredient, an effective amount of the compound of formula 1(B) in crystal form B according to claim 1 , optionally together with a pharmaceutically acceptable carrier.

4. The crystal form B of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile having structural formula I(B) according to claim 1 characterized by an X-ray diffraction pattern having three or more peaks at 2θ values selected from 9.3, 10.6, 14.4, 15.5, 17.9, 19.9, 23.4±0.2°2θ.

5. A pharmaceutical composition comprising, as active ingredient, an effective amount of the compound of formula 1(B) in crystal form B according to claim 4 , optionally together with a pharmaceutically acceptable carrier.

Assignments (5)
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Dec 23, 2025
From: BAUSCH + LOMB IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A., AS COLLATERAL AGENT
Reel/Frame 074050/0573 →
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Dec 23, 2025
From: BAUSCH + LOMB IRELAND LIMITED
To: CITIBANK, N.A., AS NOTES COLLATERAL AGENT
Reel/Frame 074050/0682 →
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Dec 23, 2025
From: BAUSCH + LOMB IRELAND LIMITED
To: CITIBANK, N.A., AS NOTES COLLATERAL AGENT
Reel/Frame 074050/0709 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 6, 2023
From: NOVARTIS AG
To: BAUSCH + LOMB IRELAND LIMITED
Reel/Frame 065790/0208 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 14, 2010
From: CHEN, WEICHUN; KIM, HONG-YONG; LIANG, JESSICA; MUTZ, MICHAEL; PRASHAD, MAHAVIR; TOWLER, CHRISTOPHER; WU, RUOQIU
To: NOVARTIS AG
Reel/Frame 024528/0464 →