IP Library Granted Patent US 9,556,233
Granted Patent B2
US 9,556,233 · App. 14/915,997 · Granted Jan 31, 2017

Cyclohexapeptide

Inventors: Paulus Bernardus Maria Groen (Echt, NL); Peter Philip Lankhorst (Echt, NL); Burhan Özalp (Echt, NL); Robertus Mattheus De Pater (Echt, NL)
Assignee: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.
C07K7/56
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Quick Facts
Patent No.
US 9,556,233
App. No.
14/915,997
Granted
Jan 31, 2017
Kind
B2
Abstract

The present invention relates to a novel cyclohexapeptide, to a method for the preparation of said cyclohexapeptide and to the use of said cyclohexapeptide.

Claims (14)

1. A compound of general formula (1) or a salt thereof:

wherein R is hydroxyl.

2. The compound of claim 1 , wherein the salt of the compound of formula (1) is a pharmaceutically acceptable salt.

3. The compound of claim 2 , wherein the pharmaceutically acceptable salt is an acid addition salt with an organic acid comprising at least one organic acid selected from the group consisting of acetic, citric, glutamic, lactic, maleic, malic, oxalic, pamoic, propionic, succinic and tartaric acid.

4. The compound of claim 2 , wherein the pharmaceutically acceptable salt is a diacetate.

5. A composition comprising caspofungin hydroxylamine or a salt thereof and a compound of general formula (1):

wherein R is hydrogen.

6. The composition according to claim 5 , wherein the caspofungin hydroxylamine or a salt thereof is present in the composition in an amount of 0.01% to 2% based on weight.

7. A method for the preparation of a compound according to claim 1 comprising contacting caspofungin or a salt thereof with an oxidizing agent.

8. The method according to claim 7 further comprising purifying the compound by chromatography and isolating the compound.

9. The method according to claim 7 , wherein the oxidizing agent is a peroxyacid.

10. The method according to claim 9 , wherein the peroxyacid is at least one selected from the group consisting of m-chloroperoxybenzoic acid, peracetic acid, peroxymonosulphuric acid and peroxyphosphonic acid.

11. An antifungal medicament which comprises an antifungal effective amount of the compound according to claim 1 as an antifungal agent.

12. A method for determining quality of a caspofungin sample which comprises analyzing the caspofungin sample for trace amounts of the caspofungin hydroxylamine using the compound of claim 1 as a reference.

Assignments (2)
CHANGE OF NAME Recorded Apr 2, 2019
From: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.
To: CENTRIENT PHARMACEUTICALS NETHERLANDS B.V.
Reel/Frame 048775/0029 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 2, 2016
From: GROEN, PAULUS BERNARDUS MARIA; LANKHORST, PETER PHILIP; ÖZALP, BURHAN; DE PATER, ROBERTUS MATTHEUS
To: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.
Reel/Frame 037871/0453 →
Priority Claims (1)
EP 13183974 · Sep 11, 2013 · regional
Continuity (1)
Related Publication 20160215021A1 · Jul 28, 2016