IP Library Granted Patent US 7,235,567
Granted Patent B2
US 7,235,567 · App. 10/755,066 · Granted Jun 26, 2007

Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist

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 7,235,567
App. No.
10/755,066
Granted
Jun 26, 2007
Kind
B2
Abstract

A crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist compound, which exhibits a powder x-ray diffraction profile substantially the same as that shown in FIG. 1 , or which exhibits a differential scanning calorimtery profile substantially the same as that shown in FIG. 3 , and is represented by the formula for Compound 2: and processes for preparing Compound 2 are disclosed. Pharmaceutical compositions comprising the polymorph of the bisulfate salt and at least one excipient or carrier, and methods of using the polymorph of Compound 2 to treat a variety of physiological disorders, such as thrombosis, are also disclosed.

Claims (9)

1. A crystalline polymorph Form 1 of Compound 2 of the formula:

that exhibits a powder x-ray diffraction pattern having characteristic peak locations of 11.2, 16.4, 19.2 and 21.0 degrees 2θ.

2. The crystalline polymorph of Compound 2 of claim 1 that exhibits a powder x-ray diffraction pattern having characteristic peak locations of 9.9, 11.2, 16.4, 19.2, 21.0, 22.1, 23.7 and 26.7 degrees 2θ.

3. The crystalline polymorph of Compound 2 of claim 1 that exhibits a powder x-ray diffraction pattern having characteristic peak locations of 9.9, 11.2, 12.6, 14.5, 16.4, 19.2, 21.0, 22.1, 23.7, 26.7, 28.2 and 30.8 degrees 2θ.

4. The crystalline polymorph of Compound 2 of claim 1 that exhibits a powder x-ray diffraction pattern substantially the same as the powder x-ray diffraction pattern shown in FIG 1 .

5. A crystalline polymorph Form 1 of Compound 2 of the formula:

that exhibits a differential scanning calorimetry pattern substantially the same as the differential scanning calorimetry pattern shown in FIG. 3 .

6. A pharmaceutical composition comprising the crystalline polymorph Form 1 of Compound 2 according to claim 1 , and at least one excipient or carrier.

7. A purified form of the crystalline polymorph Form 1 of Compound 2 of claim 1 .

Assignments (9)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2020
From: ARALEZ PHARMACEUTICALS TRADING DAC
To: TOPROL ACQUISITION LLC
Reel/Frame 054027/0047 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 10, 2020
From: TOPROL ACQUISITION LLC
To: XSPIRE PHARMA, LLC
Reel/Frame 053731/0376 →
RECEIVING PARTY/ASSIGNEE ADDRESS CHANGE FOR ASSIGNMENT RECORDED AT REEL/FRAME 039767/0695 Recorded Aug 31, 2018
From: MERCK SHARP & DOHME CORP.
To: ARALEZ PHARMACEUTICALS TRADING DAC
Reel/Frame 046989/0669 →
CORRECTIVE ASSIGNMENT TO CORRECT THE CONVEYING PARTY PREVIOUSLY RECORDED AT REEL: 046696 FRAME: 0772. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Aug 30, 2018
From: ARALEZ PHARMACEUTICALS TRADING DESIGNATED ACTIVITY COMPANY
To: DEERFIELD MANAGEMENT COMPANY, L.P., AS ADMINISTRATIVE AGENT
Reel/Frame 046988/0741 →
SECURITY INTEREST Recorded Aug 24, 2018
From: ARALEZ PHARMACEUTICAL TRADING DAC
To: DEERFIELD MANAGEMENT COMPANY, L.P., AS ADMINISTRATIVE AGENT
Reel/Frame 046696/0772 →
SECURITY INTEREST Recorded Sep 29, 2016
From: ARALEZ PHARMACEUTICALS TRADING DAC
To: DEERFIELD PRIVATE DESIGN FUND III, L.P.; DEERFIELD INTERNATIONAL MASTER FUND, L.P.; DEERFIELD PARTNERS, L.P.
Reel/Frame 039892/0309 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 16, 2016
From: MERCK SHARP & DOHME CORP.
To: ARALEZ PHARMACEUTICALS TRADING DAC
Reel/Frame 039767/0695 →
CHANGE OF NAME Recorded Aug 30, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028884/0151 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 22, 2005
From: THIRUVENGADAM, TIRUVETTIPURAM K; WU, WENXUE; WANG, TAO; CHIU, JOHN S; BOGDANOWICH-KNIPP, SUSAN; PAVLOVSKY, ANASTASIA; GREENLEE, WILLIAM J; GRAZIANO, MICHAEL P; KOSOGLOU, TEDDY; CHINTALA, MADHU; CHACKALAMANNIL, SAMUEL
To: SCHERING CORPORATION
Reel/Frame 016299/0023 →