IP Library Granted Patent US 8,138,351
Granted Patent B2
US 8,138,351 · App. 12/599,970 · Granted Mar 20, 2012

Treatment of duchenne muscular dystrophy

Assignee: Summit Corporation PLC
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Quick Facts
Patent No.
US 8,138,351
App. No.
12/599,970
Granted
Mar 20, 2012
Kind
B2
Abstract

Provided is a process for the preparation of 5-(ethylsulfonyl)-2-(naphthalen-2-yl) benzo[d] oxazole useful in the treatment of Duchenne muscular dystrophy.

Claims (13)

1. A process for the preparation of a compound of formula (I)

comprising a cyclisation of a compound of formula (II)

in the presence of an acid catalyst.

2. The process according to claim 1 , wherein the acid catalyst is methanesulfonic acid or p-toluenesulfonic acid.

3. The process according to claim 1 , wherein the process takes place in a solvent which is heated under reflux.

4. The process according to claim 3 , wherein the solvent is a mixture of xylenes.

5. The process according to claim 1 wherein water produced as a by-product of the cyclisation is removed.

6. The process according to claim 5 wherein the water is removed by use of Dean-Stark apparatus.

7. The process according to claim 1 , wherein the compound of formula (II) is synthesised in a solvent and subsequently cyclised without intermediate purification of the compound of formula (II) or removal of the solvent.

8. The process according to claim 1 , wherein the compound of formula (II) is prepared by the reaction of an aminoalcohol of formula (III)

with an acyl derivative of formula (IV) wherein X represents a leaving group

9. The process according to claim 8 , wherein X represents halogen.

10. The process according to claim 8 , wherein X represents Cl.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 7, 2018
From: SUMMIT THERAPEUTICS PLC
To: SUMMIT (OXFORD) LIMITED
Reel/Frame 044859/0983 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 30, 2010
From: BIOMARIN IGA LIMITED
To: SUMMIT CORPORATION PLC
Reel/Frame 025435/0152 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 5, 2010
From: WYNNE, GRAHAM MICHAEL; WEYMOUTH-WILSON, ALEXANDER CHARLES; CLARKSON, ROBERT; VAN WELL, RENATE; WREN, STEPHEN PAUL; DE MOOR, OLIVIER
To: SUMMIT CORPORATION PLC
Reel/Frame 024039/0058 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 5, 2010
From: SUMMIT CORPORATION PLC
To: BIOMARIN IGA LIMITED
Reel/Frame 024039/0102 →
Priority Claims (1)
GB 0715937.9 · Aug 15, 2007 · national
Continuity (1)
Related Publication 20100267961A1 · Oct 21, 2010