IP Library Granted Patent US 8,575,351
Granted Patent B2
US 8,575,351 · App. 13/376,093 · Granted Nov 5, 2013

Active metabolite of a thrombin receptor antagonist

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Quick Facts
Patent No.
US 8,575,351
App. No.
13/376,093
Granted
Nov 5, 2013
Kind
B2
Abstract

Disclosed herein is an active metabolite (“M20”) of a molecule that is useful as a thrombin receptor antagonist: Also disclosed are formulations of this compound, synthetic routes to this compound, and methods of treating a variety of cardiovascular conditions, including acute coronary syndrome and peripheral arterial disease, and of effecting secondary prevention, by orally administering the active metabolilte.

Claims (9)

1. A compound of the following formula:

or a pharmaceutically acceptable salt or hydrate thereof in an isolated or purified form.

2. The free base of the compound according to claim 1 .

3. A pharmaceutically acceptable salt of the compound according to claim 1 .

4. A hydrate form of the compound according to claim 1 .

5. A pharmaceutical composition comprising an effective amount of a compound of the formula

or a pharmaceutically acceptable salt or hydrate thereof, and a pharmaceutically acceptable carrier.

6. The pharmaceutical composition according to claim 5 , which further comprises one or more additional cardiovascular agents.

7. The pharmaceutical composition according to claim 6 , wherein said cardiovascular agent is aspirin, clopidogrel, prasugrel, or the pharmaceutically acceptable salts hydrates of said agents.

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 Mar 20, 2013
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 030047/0520 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 19, 2013
From: PENNER, NATALIA A.; NGUYEN VORONIN, KIMBERLY
To: SCHERING CORPORATION
Reel/Frame 030042/0027 →