IP Library › Granted Patent US 7,531,507
Granted Patent B2
US 7,531,507 · App. 11/267,063 · Granted May 12, 2009

Acylated nonadepsipeptides containing pyridyl alanine residues

Assignee: AiCuris GmbH & Co. KG
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Quick Facts
Patent No.
US 7,531,507
App. No.
11/267,063
Granted
May 12, 2009
Kind
B2
Abstract

The invention relates to nonadepsipeptides and processes for their preparation, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular bacterial infectious diseases.

Claims (26)

1. A compound of the formula

in which

R 1 is hydrogen, and

R 2 is 2-ethyl-2-methylbut-1-yl, 2,2-diethylbut-1-yl, 2,2-dimethylpent- l-yl or trimethylsilylmethyl,

or

R 1 is trifluoromethyl, and

R 2 is 2,2-dimethyiprop- l-yl, 2,2-dimethylbut- l-yl, 2-ethyl-2-methylbut- l-yl, 2,2-diethylbut- l-yl, 2,2-dimethylpent- l-yl or trimethylsilylmethyl,

or one of its salts.

2. The compound according to claim 1 , wherein

R 1 is hydrogen, and

R 2 is trimethylsilylmethyl,

or

R 1 is trifluoromethyl, and

R 2 is 2,2-dimethylprop-1 -yl, 2,2-dimethylbut-1 -yl or trimethylsilylmethyl.

3. The compound according to claim 1 , wherein

R 1 is hydrogen, and

R 2 is 2-ethyl-2-methylbut-1 -yl, 2,2-diethylbut-1 -yl or trimethylsilylmethyl.

4. The compound according to claim 1 having the following structure 3-(trimethylsilyl)- D -alanyl-3-(pyridin-3 -yl)- L -alanyl-de( 1 - D -leucyl-2- L -leucyl)lysobactin

or one of its salts.

5. A process for preparing a compound of the formula (I) according to claim 1 , comprising reacting the compound of the formula

with a compound of the formula

in which R 1 and R 2 have the meaning indicated in claim 1 , and X 1 is halogen or hydroxy.

6. A medicament comprising a compound according to any of claims 1 to 4 in combination with an inert, non-toxic, pharmaceutically suitable excipient.

7. The medicament according to claim 6 for the treatment of bacterial infections.

8. A method for controlling bacterial infections in humans and animals in need thereof by administration of an antibacterially effective amount of at least one compound according to any of claims 1 to 4 .

9. A method for controlling bacterial infections in humans and animals in need thereof by administration of an antibacterially effective amount of a medicament according to claim 6 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 18, 2006
From: BAYER HEALTHCARE AG
To: AICURIS GMBH & CO. KG
Reel/Frame 018648/0669 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 10, 2006
From: VON NUSSBAUM, FRANZ; BRUNNER, NINA; ENDERMANN, RAINER; FURSTNER, CHANTAL; HARTMANN, ELKE; PAULSEN, HOLGER; RAGOT, JACQUES; SCHIFFER, GUIDO; SCHUHMACHER, JOACHIM; SVENSTRUP, NIELS; TELSER, JOACHIM; ANLAUF, SONJA; BRUNING, MICHAEL-ALEXANDER
To: BAYER HEALTHCARE AG
Reel/Frame 017902/0389 →
Priority Claims (1)
DE 10 2004 053 407 · Nov 5, 2004 · national
Continuity (1)
Related Publication 20060264358A1 · Nov 23, 2006