US2004048917A1PendingUtilityA1
New use of compounds as antibacterial agents
Priority: Jun 1, 1999Filed: May 1, 2003Published: Mar 11, 2004
Est. expiryJun 1, 2019(expired)· nominal 20-yr term from priority
A61P 29/00A61P 31/00A61P 31/04A61P 1/04A61K 31/216A61K 31/00A61K 31/4035A61K 31/407A61K 45/06A61K 31/381A61K 31/403A61K 31/21A61K 31/405
47
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Claims
Abstract
The present invention discloses a new use of NO-releasing NSAIDs, especially NO-releasing NSAIDs of the formula I, or a pharmaceutically acceptable salt or enantiomer thereof, for the manufacture of a medicament for the treatment of bacterial infections, especially caused or mediated by Helicobacter pylori. Disclosed is also the new use of a NO-releasing NSAID in combination with an acid susceptible proton pump inhibitor for the treatment of bacterial infections.
Claims
exact text as granted — not AI-modified1 . Use of a NO-releasing NSAID as well as a pharmaceutically acceptable salt or an enantiomer thereof, for the manufacture of a medicament for the treatment of bacterial infections.
2 . Use of a NO-releasing NSAID and an acid susceptible proton pump inhibitor or a salt thereof or an enantiomer or a salt of the enantiomer in the manufacture of pharmaceutical formulations intended for simultaneous, separate, or sequential administration in the treatment of bacterial infections.
3 . Use according to claim 1 or 2 wherein the NO-releasing NSAID is a compound of the formula I
wherein M is selected from anyone of
and X is selected from
linear, branched or cyclic —(CH 2 ) n — wherein n is an integer of from 2 to 10;
—(CH 2 ) m—O—(CH 2 ) p — wherein m and p are integers of from 2 to 10 ; and —CH 2 — p C 6 H 4 —CH 2 —,
or a pharmaceutically acceptable salt or enantiomer thereof.
4 . Use according to claim 3 wherein M in formula I is selected from
5 . Use according to claim 3 or 4 wherein X in formula I is selected from linear —(CH 2 ) n — wherein n is an integer of from 2 to 6, —(CH 2 ) 2 —O—(CH 2 ) 2 — and —CH 2 —pC 6 H 4 —CH 2 —.
6 . Use according to any one of claims 1 - 3 wherein the NO-releasing NSAID is a compound according to any one of the formulas Ia-Iq
7 . Use according to claim 6 , wherein the NO-releasing NSAID is a compound of formula Ia
8 . Use according to claim 2 wherein the acid susceptible proton pump inhibitor is a compound of the formula II
wherein
N in the benzimidazole moiety means that one of the carbon atoms substituted by R 6 -R 9 optionally may be exchanged for a nitrogen atom without any substituents,
R 1 , R 2 and R 3 are the same or different and selected from hydrogen, alkyl, alkoxy optionally substituted by fluorine, alkylthio, alkoxyalkoxy, dialkylamino, piperidino, morpholino, halogen, phenyl and phenylalkoxy;
R 4 and R 5 are the same or different and selected from hydrogen, alkyl and aralkyl;
R 6 ′ is hydrogen, halogen, trifluoromethyl, alkyl and alkoxy;
R 6 -R 9 are the same or different and selected from hydrogen, alkyl, alkoxy, halogen, halo-alkoxy, alkylcarbonyl, alkoxycarbonyl, oxazolyl, trifluoroalkyl, or adjacent groups R 6 -R 9 form ring structures which may be further substituted;
R 10 is hydrogen or forms an alkylene chain together with R 3 and
R 11 and R 12 are the same or different and selected from hydrogen, halogen or alkyl, alkyl groups, alkoxy groups and moities thereof, they may be branched or straight C 1 -C 9 chains or comprise cyclic alkyl groups, such as cycloalkyl-alkyl.
9 . Use according to claim 8 wherein the acid susceptible proton pump inhibitor is selected from omeprazole an alkaline salt thereof, (S)-omeprazole and an alkaline salt thereof.
10 . Use according to claim 8 wherein the acid susceptible proton pump inhibitor is lansoprazole or a pharmaceutically acceptable salt thereof or an enantiomer or a salt of the enantiomer.
11 . Use according to claim 8 wherein the acid susceptible proton pump inhibitor is pantoprazole or a pharmaceutically acceptable salt thereof or an enantiomer or a salt of the enantiomer.
12 . Use according to any one of the preceeding claims 1 to 11 , wherein the bacterial infection is caused or mediated by Helicobacter pylori.
13 . Use according to claim 1 , wherein the amount of NO-releasing NSAID in each dosage form is 0.5-5000 mg.
14 . Use according to claim 13 , wherein the amount of NO-releasing NSAID is 5-1000 mg.
15 . Use according to claim 2 , wherein the amount of NO-releasing NSAID is 0.5-5000 mg and the amount of proton pump inhibitor is 0.1-200 mg together in one dosage form or in two separate dosage forms.
16 . Use according to claim 15 , wherein the amount of NO-releasing NSAID is 5-1000 mg and the amount of proton pump inhibitor is 10-80 mg.
17 . A method for the treatment of a bacterial infection, comprising administering to a patient suffering from said bacterial infection, an effective amount of a NO-releasing NSAID or a pharmaceutically acceptable salt or an enantiomer thereof.
18 . A method for the treatment of a bacterial infection, comprising simultaneously, separately or sequentially administration to a patient suffering from said bacterial infection, an effective amount of a NO-releasing NSAID and an acid susceptible proton pump inhibitor or a salt thereof or an enantiomer or a salt of the enantiomer.
19 . A method according to claim 17 or 18 wherein the NO-releasing NSAID is a compound of the formula I
wherein M is selected from
and X is selected from
linear, branched or cyclic —(CH 2 ) n — wherein n is an integer of from 2 to 10;
—(CH 2 ) m —O—(CH 2 ) p — wherein m and p are integers of from 2 to 10; and —CH 2 — p C 6 H 4 —CH 2 —,
or a pharmaceutically acceptable salt or enantiomer thereof.
20 . A method according to claim 19 wherein M in formula I is selected from
21 . A method according to claim 19 or 20 wherein X in formula I is selected from linear —(CH 2 ) n — wherein n is an integer of from 2 to 6, —(CH 2 ) 2 —O—(CH 2 ) 2 — and —CH 2 — p C 6 H 4 —CH 2 —.
22 . A method according to any one of claim 17 - 19 , wherein the NO-releasing NSAID is a compound according to any one of the formulas Ia-Iq
23 . A method according to claim 22 , wherein the NO-releasing NSAID is a compound of formula Ia
24 . A method according to claim 18 wherein the acid susceptible proton pump inhibitor is a compound of the formula II
wherein
N in the benzimidazole moiety means that one of the carbon atoms substituted by R 6 -R 9 optionally may be exchanged for a nitrogen atom without any substituents;
R 1 , R 2 and R 3 are the same or different and selected from hydrogen, alkyl, alkoxy optionally substituted by fluorine, alkylthio, alkoxyalkoxy, dialkylamino, piperidino, morpholino, halogen, phenyl and phenylalkoxy;
R 4 and R 5 are the same or different and selected from hydrogen, alkyl and aralkyl;
R 6 ′ is hydrogen, halogen, trifluoromethyl, alkyl and alkoxy;
R 6 -R 9 are the same or different and selected from hydrogen, alkyl, alkoxy, halogen, haloalkoxy, alkylcarbonyl, alkoxycarbonyl, oxazolyl, trifluoroalkyl, or adjacent groups R6-R 9 form ring structures which may be further substituted;
R 10 is hydrogen or forms an alkylene chain together with R 3 and R 11 and R 12 are the same or different and selected from hydrogen, halogen or alkyl, alkyl groups, alkoxy groups and moities thereof, they may be branched or straight C 1 -C 9 chains or comprise cyclic alkyl groups, such as cycloalkyl-alkyl.
25 . A method according to claim 24 wherein the acid susceptible proton pump inhibitor is selected from omeprazole an alkaline salt thereof, (S)-omeprazole and an alkaline salt thereof.
26 . A method according to claim 24 wherein the acid susceptible proton pump inhibitor is lansoprazole or a pharmaceutically acceptable salt thereof or an enantiomer or a salt of the enantiomer.
27 . A method according to claim 24 wherein the acid susceptible proton pump inhibitor is pantoprazole or a pharmaceutically acceptable salt thereof or an enantiomer or a salt of the enantiomer.
28 . A method according to any one of the preceeding claims 17 to 27 , wherein the bacterial infection is caused or mediated by Helicobacter pylori.
29 . A method according to claim 17 , wherein the amount of NO-releasing NSAID in each dosage form is 0.5-5000 mg.
30 . A method according to claim 29 , wherein the amount of NO-releasing NSAID is 5-1000 mg.
31 . A method according to claim 18 , wherein the amount of NO-releasing NSAID is 0.5-5000 mg and the amount of proton pump inhibitor is 0.1-200 mg together in one dosage form or in two separate dosage forms.
32 . A method according to claim 31 , wherein the amount of NO-releasing NSAID is 5-1000 mg and the amount of proton pump inhibitor is 10-80 mg.
33 . A pharmaceutical formulation suitable for use in the treatment of bacterial infections, comprising a NO-releasing NSAID or a pharmaceutically acceptable salt or an enantiomer thereof as active agent.
34 . A pharmaceutical formulation suitable for use in the treatment of bacterial infections, comprising a NO-releasing NSAID and an acid susceptible proton pump inhibitor or a salt thereof or an enantiomer or a salt of the enantiomer as active agents.
35 . A pharmaceutical formulation according to claim 25 or 26 wherein the NO-releasing NSAID is a compound of the formula I
wherein M is selected from
and X is selected from
linear, branched or cyclic —(CH 2 ) n — wherein n is an integer of from 2 to 10;
—(CH 2 ) m —O—(CH 2 ) p — wherein m and p are integers of from 2 to 10; and —CH 2 — p C 6 H 4 —CH 2 —;
or a pharmaceutically acceptable salt or enantiomer thereof.Join the waitlist — get patent alerts
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