IP Library Granted Patent US 8,772,445
Granted Patent B2
US 8,772,445 · App. 12/863,319 · Granted Jul 8, 2014

Production and use of antitumoral cyclodepsipeptides

Inventors: Johannes Imhoff (Preetz, DE); Zhiguo Yu (Shenyang, CN); Gerhard Lang (Gurwolf, CH); Jutta Wiese (Eutin, DE); Holger Kalthoff (Kiel, DE); Stefanie Klose (Wolfsburg, DE)
Assignee: Helmholtz-Zentrum Fuer Ozeanforschung Kiel (Geomar)
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Quick Facts
Patent No.
US 8,772,445
App. No.
12/863,319
Granted
Jul 8, 2014
Kind
B2
Abstract

A compound having the general structure R 1 , R 2 , R 3 and R 4 being selected from the group consisting of a hydrogen atom (H) and a C 1 -C 20 alkyl, and R 5 being a phenyl radical.

Claims (25)

1. A compound having the general structure

R 1 , R 2 , R 3 and R 4 being selected from the group consisting of a hydrogen atom (H) and a C 1 -C 20 alkyl,

and

R 5 being a phenyl radical.

2. The compound according to claim 1 , characterized in that at least one of R 1 , R 2 , R 3 and R 4 is a C 1 -C 20 alkyl having a substituent selected from the group consisting of an acyl radical, a formyl, acetyl, trichloroacetyl, fumaryl, maleyl, succinyl, or benzoyl group, a halogen radical, an aminoalkyl group, a hydroxyl group, an ether group or a carboxyl group.

3. The compound according to claim 1 having the following formula

including its diastereomeres.

4. The compound according to claim 1 having the following formula

including its diastereomeres.

5. A method for producing a compound having the general structure

R 1 , R 2 , R 3 and R 4 being selected from the group consisting of a hydrogen atom (H) and a C 1 -C 20

alkyl,

and

R 5 being a phenyl radical

characterized by the following steps:

a. cultivating a fungus of the species Scopulariopsis and

b. isolating the compound from the culture medium and/or the fungus.

6. The method according to claim 5 , characterized in that the fungus is Scopulariopsis brevicaulis.

7. A method of treating pancreatic or intestinal cancer by administering a substance having the general structure

R 1 , R 2 , R 3 and R 4 being selected from the group consisting of a hydrogen atom (H) and a C 1 -C 20 alkyl,

and

R 5 being a phenyl radical

as an antitumor agent.

8. The method of claim 7 wherein the substance is administered for the treatment of pancreatic cancer.

9. The compound according to claim 1 , characterized in that R 5 is a phenyl radical having a substituent selected from the group consisting of an acyl radical, a formyl, acetyl, trichloroacetyl, fumaryl, maleyl, succinyl, or benzoyl group, a halogen radical, an aminoalkyl group, a hydroxyl group, an ether group or a carboxyl group.

Assignments (2)
CHANGE OF NAME Recorded Dec 31, 2013
From: LEIBNIZ-INSTITUT FUER MEERESWISSENSCHAFTEN
To: HELMHOLTZ-ZENTRUM FUER OZEANFORSCHUNG KIEL (GEOMAR)
Reel/Frame 031894/0829 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 30, 2010
From: IMHOFF, JOHANNES; YU, ZHIGUO; LANG, GERHARD; WIESE, JUTTA; KALTHOFF, HOLGER; KLOSE, STEFANIE
To: LEIBNITZ-INSTITUT FUER MEERESWISSENSCHAFTEN
Reel/Frame 025401/0743 →
Priority Claims (1)
DE 10 2008 005 097 · Jan 18, 2008 · national
Continuity (1)
Related Publication 20110077205A1 · Mar 31, 2011