IP Library › Granted Patent US 9,006,391
Granted Patent B2
US 9,006,391 · App. 13/264,064 · Granted Apr 14, 2015

Method for the preparation of cyclopeptides

Inventors: Robertus Mattheus De Pater (Delft, NL); Dhiredj Chandre Jagesar (Leiden, NL); Thomas Van Der Does (Wilnis, NL)
Assignee: DSM Sinochem Pharmaceuticals Netherlands B.V.
C07K7/56
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Quick Facts
Patent No.
US 9,006,391
App. No.
13/264,064
Granted
Apr 14, 2015
Kind
B2
Abstract

The present invention relates to a method for preparing cyclopeptides by means of protection with a substituted boronic acid. The present invention also discloses novel boronate esters of cyclopeptides of general formula (8).

Claims (9)

1. A compound of the general formula (8)

wherein R 1 is C(O)R 2 ,

R 2 is C 9 -C 21 alkyl, C 9 -C 21 alkenyl, C 1 -C 10 alkoxyphenyl, C 1 -C 10 alkoxynaphthyl or C 1 -C 10 alkoxyterphenyl,

R 3 is benzimidazol-2-yl, benzothiazol-2-yl, 1-methylimidazol-2-yl, 4-methoxyphenyl or phenyl,

R 4 is OH or —SR3,

R 5 is cyclohexyl, or 4-tert-butylphenyl,

X is O or H,H.

2. The compound according to claim 1 , wherein R 1 is C(O)(CH 2 ) 8 CH(CH 3 )CH 2 CH(CH)CH 2 CH 3 .

3. The compound according to claim 1 , wherein R 4 is OH or —S-phenyl.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 25, 2012
From: DSM IP ASSETS B.V.
To: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.
Reel/Frame 028638/0486 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2011
From: DE PATER, ROBERTUS MATTHEUS; JAGESAR, DHIREDJ CHANDRE; VAN DER DOES, THOMAS
To: DSM IP ASSETS B.V.
Reel/Frame 027049/0782 →
Priority Claims (1)
EP 09159630 · May 7, 2009 · regional
Continuity (1)
Related Publication 20120059146A1 · Mar 8, 2012