IP Library Granted Patent US 7,084,120
Granted Patent B2
US 7,084,120 · App. 09/745,776 · Granted Aug 1, 2006

Prodrugs of DP IV-inhibitors

Assignee: Probiodrug AG
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Quick Facts
Patent No.
US 7,084,120
App. No.
09/745,776
Granted
Aug 1, 2006
Kind
B2
Abstract

Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy.

Claims (10)

1. A prodrug compound that is an inhibitor of the enzymatic activity of dipeptidyl peptidase IV (DP IV), which compound has the general formula A—B—C, wherein

A is an amino acid,

B is a chemical bond between A and C or is an amino acid, and

C is a stable inhibitor of DP IV without C-terminal phosphonate residue.

2. The compound according to claim 1 wherein said stable inhibitor is present in a salt form.

3. A pharmaceutical composition for oral administration containing the prodrug compound of claim 1 in combination with one or more pharmaceutical carriers or excipients.

4. The compound of claim 1 wherein said compound comprises said stable inhibitor of DP IV within a composition comprising said prodrug, said prodrug inhibiting the degradation and increasing the activity of said stable inhibitors.

5. The compound according to claim 1 wherein A—B is a dipeptide of formula Ile-Pro.

6. The compound according to claim 1 wherein said stable inhibitor is aminoacylthiazolidide.

7. The compound according to claim 1 wherein B is proline.

Assignments (8)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 9, 2005
From: PROBIODRUG AG
To: PROSIDION LIMITED
Reel/Frame 017045/0252 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 9, 2005
From: PROBIODRUG AG
To: PROSIDION LIMITED
Reel/Frame 016536/0621 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 9, 2005
From: PROBIODRUG AG
To: PROSIDION LIMITED
Reel/Frame 016547/0581 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 9, 2005
From: PROBIODRUG AG
To: PROSIDION LIMITED
Reel/Frame 016561/0783 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 14, 2005
From: PROBIODRUG AG
To: PROSIDION LIMITED
Reel/Frame 016536/0107 →
ASSIGNOR INCORRECT - REEL/FRAME 011415/0536 Recorded May 21, 2002
From: DEMUTH, HANS-ULRICH; HOFFMANN, TORSTEN; SCHLENZIG, DAGMAR; MANHART, SUSANNE
To: PROBIODRUG
Reel/Frame 012912/0676 →
CHANGE OF NAME Recorded Mar 6, 2002
From: PROBIODRUG GESELLSCHAFT FUR ARZNEIMITTELFORSCHUNG MBH
To: PROBIODRUG AG
Reel/Frame 012673/0628 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 21, 2000
From: DEMUTH, HANS-ULRICH; HOFFMANN, TORSTEN; SCHLENZIG, DAGMAR; KRUBER, SUSANNE
To: PROBIODRUG
Reel/Frame 011415/0536 →
Priority Claims (2)
DE 198 28 113 · Jun 24, 1998 · national
WO PCT/EP99/04382 · Jun 24, 1999 · international
Continuity (1)
Related Publication 20020049164A1 · Apr 25, 2002