IP Library Granted Patent US 7,268,126
Granted Patent B2
US 7,268,126 · App. 11/233,835 · Granted Sep 11, 2007

Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-ce]indol-6-one

Assignees: Agouron Pharmaceuticals, Inc.; Cancer Research Technology Ltd.
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 7,268,126
App. No.
11/233,835
Granted
Sep 11, 2007
Kind
B2
Abstract

The present invention relates to novel polymorphic and amorphous forms of a phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.

Claims (6)

1. A crystalline phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, wherein the crystalline phosphate salt is selected from the group consisting of polymorph Form I, Form II, Form III, Form V, and Form VI.

2. The crystalline phosphate salt of claim 1 , wherein the crystalline phosphate salt is a substantially pure polymorph of Form II.

3. The crystalline phosphate salt of claim 1 , wherein the crystalline phosphate salt has a X-ray powder diffraction pattern comprising peaks at diffraction angles (2θ) of 11.2, 14.0, 20.1, and 23.1.

4. The crystalline phosphate salt of claim 1 , wherein the crystalline phosphate salt has a X-ray powder diffraction pattern comprising peaks at diffraction angles (2θ) essentially the same as shown in FIG. 4 .

5. A phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, wherein the salt is a substantially pure amorphous form.

6. A solid form of a phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, wherein the solid form comprises at least two of the following forms: polymorph Forms I, II, III, V, VI, or an amorphous form.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 22, 2018
From: LIU, JIA; NAYYAR, NARESH; GUO, MING; WU, ZHEN-PING; BORER, BENNETT CHAPLIN; SRIRANGAM, APARNA NADIG; MITCHELL, MARK BRYAN; LI, YI
To: AGOURON PHARMACEUTICALS, INC.; CANCER RESEARCH TECHNOLOGY LIMITED; PFIZER INC.
Reel/Frame 047259/0455 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 22, 2018
From: LIU, JIA; NAYYAR, NARESH; GUO, MING; WU, ZHEN-PING; BORER, BENNETT CHAPLIN; SRIRANGAM, APARNA NADIG; MITCHELL, MARK BRYAN; LI, YI; CHU, JAN-JON
To: AGOURON PHARMACEUTICALS, INC.; CANCER RESEARCH TECHNOLOGY LIMITED; PFIZER INC.
Reel/Frame 047259/0483 →
CHANGE OF NAME Recorded Mar 8, 2016
From: AGOURON PHARMACEUTICALS, INC.
To: AGOURON PHARMACEUTICALS, LLC
Reel/Frame 038033/0099 →
Continuity (3)
Provisional Application 6061245900 · Sep 22, 2004
Provisional Application 6067929600 · May 9, 2005
Related Publication 20060100198A1 · May 11, 2006