IP Library › Granted Patent US 8,183,369
Granted Patent B2
US 8,183,369 · App. 12/738,181 · Granted May 22, 2012

4- [3- (4-cyclopropanecarbonyl-piperazine-I-carbonyl) -4 -fluoro-benzyl] -2H-phthalaz in-1-one

Assignee: Kudos Pharmaceuticals Limited
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Quick Facts
Patent No.
US 8,183,369
App. No.
12/738,181
Granted
May 22, 2012
Kind
B2
Abstract

4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form L, methods of obtaining form L, pharmaceutical compositions comprising Form L and methods of using Form L and compositions comprising Form L.

Claims (40)

1. 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form L.

2. The compound of claim 1 having the following characteristic peaks in a powder XRD:

2θ° (±0.1°)

Peak

(λ = 1.5418 Å)

1

14.4

2

17.2

3

17.5

4

18.8

5

  23.0.

3. The compound of claim 1 having the following characteristic peaks in a powder XRD:

2θ° (±0.1°)

Peak

(λ = 1.5418 Å)

1

14.4

2

17.2

3

17.5

4

18.8

5

23.0

6

10.4

7

13.6

8

  25.1.

4. The compound of claim 1 , which has an onset of melting at 198.5° C.±1° C. when heated from 25° C. to 325° C. at 10° C. per minute in DSC.

5. A method of obtaining 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form L from 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A, comprising slurrying 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as either Form A or a mixture of Forms A and L in an organic solvent selected from the group consisting of methanol, ethanol, acetone, acetonitrile and nitromethane; that optionally contains up to 30% water v/v.

6. A pharmaceutical composition comprising a compound having crystalline Form L according to claim 1 and a pharmaceutically acceptable carrier or diluent.

7. A compound having crystalline Form L according to claim 1 for use in a method of treatment of the human or animal body.

8. A compound having crystalline Form L according to claim 1 for the use in a method of inhibiting PARP in the treatment of the human or animal body.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2010
From: QUIGLEY, KATHRYN ANNE
To: ASTRAZENECA UK LIMITED
Reel/Frame 024260/0376 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2010
From: ASTRAZENECA UK LIMITED
To: KUDOS PHARMACEUTICALS LIMITED
Reel/Frame 024260/0424 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2010
From: STILL, EZRA JOHN; CHYALL, LEONARD JESSE
To: APTUIT (KANSAS CITY) LLC
Reel/Frame 024260/0556 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2010
From: APTUIT (KANSAS CITY) LLC
To: KUDOS PHARMACEUTICALS LIMITED
Reel/Frame 024260/0621 →
Continuity (2)
Provisional Application 60980508 · Oct 17, 2007
Related Publication 20100286157A1 · Nov 11, 2010