IP Library Granted Patent US 8,080,654
Granted Patent B2
US 8,080,654 · App. 13/112,281 · Granted Dec 20, 2011

Macrocyclic quinoxaline compounds as HCV NS3 protease inhibitors

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Quick Facts
Patent No.
US 8,080,654
App. No.
13/112,281
Granted
Dec 20, 2011
Kind
B2
Abstract

The present invention relates to macrocyclic a compound of formula (I) and its use as inhibitors of the hepatitis C virus (HCV) NS3 protease, and in treating or preventing HCV infections.

Claims (13)

1. A method of preparing a compound of formula (I):

said method comprising:

reacting (1aR,5S,8S,10R,22aR)-5-tert-butyl-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxylic acid

with (1R,2S)-1-Amino-N-(cyclopropylsulfonyl)-2-vinylcyclopropanecarboxamide hydrochloride

2. The method of claim 1 , wherein the reacting is conducted in the presence of at least one reagent selected from the group consisting of diisopropylethylamine (DIEA), dimethylamino pyridine (DMAP) and O-benzotriazol-1-yl-N,N,N′,N′-tetramethyluronium tetrafluoroborate (TBTU).

3. The method of claim 1 , wherein the reacting is conducted in the presence of diisopropylethylamine (DIEA), dimethylamino pyridine (DMAP) and O-benzotriazol-1-yl-N,N,N′,N′-tetramethyluronium tetrafluoroborate (TBTU).

4. A method of preparing a pharmaceutically acceptable salt of a compound of formula (I):

said method comprising:

reacting a compound of formula (I) with a metal alkoxide to form a salt or the compound of formula (I).

5. The method of claim 4 , wherein the metal alkoxide is a potassium alkoxide.

6. The method of claim 5 , wherein the potassium alkoxide is a potassium tert-butoxide.

7. A compound prepared by the method of claim 1 .

8. A compound prepared by the method of claim 4 .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 2, 2014
From: ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.
To: MSD ITALIA S.R.L.
Reel/Frame 032806/0388 →
CHANGE OF NAME Recorded Aug 29, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028866/0511 →
MERGER Recorded Aug 27, 2012
From: MERCK SHARP & DOHME CORP.
To: SCHERING CORPORATION
Reel/Frame 028850/0515 →