IL99471A - Pharmaceutical compositions for treating helicobacter bacteria infections containing 5-fluoromethoxy-2-(3,4-dimethoxy-2-pyridyl)methylsulphinyl)-1h-benzimidazole and salts thereof in combination with an antimicrobial agent - Google Patents
Pharmaceutical compositions for treating helicobacter bacteria infections containing 5-fluoromethoxy-2-(3,4-dimethoxy-2-pyridyl)methylsulphinyl)-1h-benzimidazole and salts thereof in combination with an antimicrobial agentInfo
- Publication number
- IL99471A IL99471A IL9947191A IL9947191A IL99471A IL 99471 A IL99471 A IL 99471A IL 9947191 A IL9947191 A IL 9947191A IL 9947191 A IL9947191 A IL 9947191A IL 99471 A IL99471 A IL 99471A
- Authority
- IL
- Israel
- Prior art keywords
- salts
- benzimidazole
- combination
- dimethoxy
- pyridyl
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
Abstract
The invention concerns the use of compound of formula (I), in which the substituents and symbols are as defined in the specification, against Helicobacter bacteria.
Description
PHARMACEUTICAL COMPOSITIONS FOR TREATING HELICOBACTER BACTERIA, CONTAINING 5-FLU0R0METH0XY-2-((3,4-DIMETH0XY-2-PYRIDYL) METHYLSULPHINYL) -1H-BENZIMIDAZ0LE AND SALTS THEREOF, IN COMBINATION WITH AN ANTIMICROBIAL AGENT 7_.-πρ7η7ϋ:)κ DTU DV WX2 on'n'pm 7iT eTD7TJ3-iH - 1 - 99471/3 Scope of application o ^the invention ί The invention relates to new oral drug forms . The new drug forms are employed for the treatment of diseases of the stomach and/or intestine caused by Helicobacter bacteria.
Pyridylmethylsulphinyl-ia-benzimidazoles which have gastric acid secretion-inhibiting properties are described in a large number of patent applications . The following patent applications and patents may be mentioned in particular here in connection with the present invention: EP-A-134 400 (= IL 71774 ), EP-A-127 763 (= IL 71665 ), EP-B-166 287 (= IL 75400 ), EP-A-201 575 ( = IL 76839. ), WO89/05299 and W089/11479. - European Patent Application ΞΡ-Α-382 489 describes and claims the suitability of certain pyridylmethylsulphinyl-ΙΞ-benzimidazoles , which are substituted in the benzimidazole part, if desired, by methoxy or trifluoromethyl, for the treatment of infectious diseases caused by bacteria of the Campylobacter (= Helicobacter) strain. International Patent Application WO90/09175 discloses the use of omeprazole in the treatment of infectious diseases, in particular those caused by Campylobacter pylori.
Because the pyridylmethylsulphinyl-lH-benzimidazoles have a low stability and are easily decomposed by acid, various patent applications (e.g. IL 82910 o ΞΡ-Α-247 983) refer to the need to administer these active compounds in a form which is resistant to gastric juice in the case of oral administration. An "enteric coated" formulation is also used in the abovementioned EP-A-382 489 as the oral presentation form for combating Campylobacter.
Description of the invention The invention relates to a pharmaceutical composition to be administered orally for combating Helicobacter bacteria comprising as active ingredient a compound - 2 - 99471/ 2 containing 5-difluoro-methoxY-2- [ ( 3 , 4-dimethoxY-2-pyridyl ) -methylsulphinyl]-lH-benzimidazole and/or its pharmacologically tolerated salt, in combination with an antimicrobial agent chosen from the group comprising penicillin G, gentamycin, erythromycin, nitrofurazone, nitrofurantoin, furazolidone, metronidazole and amoxycillin.
A preferred embodiment of the present invention provides a pharmaceutical composition to be administered orally for combatting Helicobacter pylori, containing 5-difluoro-methoxy-2- [ ( 3 , 4-dimethoxy-2-pyridy1 ) -methy1-sulphinyl] -ΙΗ-benzimidazole, in combination with amoxycillin.
The invention also provides a process for the preparation of pharmaceutical preparations which contain one or more compounds as described herein as the active compound and customary excipients, characterized in that the active compound which has been prepared in a known manner is mixed with the customary excipients and the mixture is converted into a medicament to be administered orally for combatting Helicobacter bacteria.
Preferred possible salts for compounds of the present invention are all the pharmacologically tolerated acid addition salts. Salts which may be mentioned in particular are the pharmacologically tolerated salts of the inorganic and organic acids usually used in galenics. Examples of such suitable salts are water-soluble and water-insoluble acid addition salts, such as the hydrochloride, hydrobromide , hydriodide, phosphate, nitrate, sulphate, acetate, citrate, gluconate, benzoate, hibenzate, fendizoate, butyrate, sulphosalicylate, maleate, laurate, malate, fumarate, succinate, oxalate, tartrate, amsonate, - 3 - 99471/2 embonate, metembonate, stearate, tosylate, 2-hydroxy-3-naphthoate, 3-hydroxy-2-naphthoate or mesylate.
Preferred possible salts for compounds of the present invention are pharmacologically tolerated basic salts, in particular, pharmacologically tolerated salts with the inorganic and organic bases usually used in galenics. Examples of basic salts which may be mentioned are the lithium, sodium, potassium, calcium, aluminium, magnesium, titanium, ammonium or guanidinium salts.
Among the Helicobacter strains against which the compounds of the present invention have proved to be active, the Helicobacter pylori strain may be mentioned in particular as being preferred.
Examples which may be mentioned of medicaments to be administered orally are tablets, coated tablets, hard and soft capsules, for example of gelatine, dispersible powders, granules, aqueous and oily suspensions, emulsions, solutions or syrups, it being advantageous for the tablets, coated tablets, capsules or granules to be such that they readily dissolve in gastric juice and release the active compound in the stomach.
For combined treatment of gastric diseases which are based both on an increased secretion of gastric acid and on damage to the stomach by Helicobacter pylori, there may also be mentioned those drug formulations to be administered orally which contain active compounds of the present invention both in a form which is resistant to gastric juice and in a form which is not resistant to gastric juice simultaneously in an individual dose. Examples which may be mentioned are tablets which contain the active compound both - 4 - 99471/3 in a core which is resistant to gastric juice and in a shell which is not resistant to gastric juice, or capsules filled with pellets or (mini) tablets which are resistant to gastric juice and those which are not reistant to gastric juice.
In human medicine, the active compounds are in general administered in a daily dose of about 0.05 to about 5, preferably 0.,1 to 2.5 mg/kg of body weight, if available . in the form of several, preferably 2 to 6, individual doses to achieve the desired result.
If the compounds of the present invention and/or their salts are to be employed for the treatment of diseases of the stomach, based on the presence of Helicobacter pylori, the medicaments to be administered can also contain one or more pharmacologically active constituents of other groups of medicaments.
Combination of the compounds of the present invention and/or their salts with antimicrobial substances which have an action against Helicobacter pylori, such as, for example, penicillin G, gentamycin, erythromycin, nitrofurazone, nitrofurantoin, furazolidone, metronidazole, and in particular amoxycillin, with the aim of intensifying the main action in the super-additive sense, is to be emphasized in particular in this "ooiinectionT Combination of the active compound 5-difluoromethoxy-2-[ ( 3 , 4-dimethoxy-2-pyridyl) -methylsulphinyl] -lH-benzimidazole [= pantoprazole (INN)] and its salts with substances having an antimicrobial action, in particular with amoxycillin, is particularly preferred in this connection, and the invention therefore furthermore relates to this combination. - 5 - 99471/3 It has been found, surprisingly, that the compounds of the present invention are considerably more active against Helicobacter bacteria in an acid medium than in a neutral medium, and that they accordingly - in contrast to the doctrine found in the prior art - should appropriately not be administered in a form which is resistant to gastric juice.
The invention thus preferably relates to the use of the compounds described herein and their pharmacologically tolerated salts for the preparation of medicaments which are not in a formulation which is resistant to gastric juice, and which are to be administered orally for combatting Helicobacter bacteria.
The medicaments to be administered orally are prepared using the active compounds of the present invention in a manner which is known per se to the expert.
Claims (3)
1. A pharmaceutical composition to be administered orally for combatting Helicobacter bacteria, containing 5-difluoro-methoxy-2- [ ( 3 , 4-dimethoxy-2-pYridyl)methylsulphinyl3 -1H-benzimidazole and/or its pharmacologically tolerated salt, in combination with an antimicrobial agent chosen from the group comprising penicillin G, gentamycin, erythromycin, nitrofurazone, nitrofurantoin, furazolidone, metronidazole and amoxycillin.
2. A pharmaceutical composition to be administered orally for combatting Heliobacter pylori, containing 5-difluoro-methoxy-2-[ ( 3 , 4-dimethoxy-2-pyridyl)methylsulphinyl] -1H-benzimidazole , in combination with amoxycillin.
3. A process for the preparation of pharmaceutical preparations which contain one or more compounds according to claim 1 or 2 as the active compound and customary excipients, characterized in that the active compound which has been prepared in a known manner is mixed with the customary excipients and the mixture is converted into a medicament to be administered orally for combatting Heliobacter bacteria. for the Applicant: WOLFF, BREGMA AND GOLLER
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH299390 | 1990-09-14 | ||
| CH222691 | 1991-07-25 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL99471A0 IL99471A0 (en) | 1992-08-18 |
| IL99471A true IL99471A (en) | 1996-03-31 |
Family
ID=25689847
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL9947191A IL99471A (en) | 1990-09-14 | 1991-09-12 | Pharmaceutical compositions for treating helicobacter bacteria infections containing 5-fluoromethoxy-2-(3,4-dimethoxy-2-pyridyl)methylsulphinyl)-1h-benzimidazole and salts thereof in combination with an antimicrobial agent |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP0548103B1 (en) |
| JP (1) | JPH06500547A (en) |
| AT (1) | ATE209914T1 (en) |
| AU (1) | AU8445791A (en) |
| CA (1) | CA2092694C (en) |
| CY (1) | CY2363B1 (en) |
| DE (1) | DE59109225D1 (en) |
| DK (1) | DK0548103T3 (en) |
| ES (1) | ES2169022T3 (en) |
| IE (1) | IE913232A1 (en) |
| IL (1) | IL99471A (en) |
| NZ (1) | NZ239772A (en) |
| WO (1) | WO1992004898A1 (en) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW276996B (en) * | 1992-04-24 | 1996-06-01 | Astra Ab | |
| WO1994019346A1 (en) * | 1993-02-17 | 1994-09-01 | Byk Gulden Lomberg Chemische Fabrik Gmbh | Substituted heteroarylalkylthiopyridines for controlling helicobacter bacteria |
| WO1994027606A1 (en) * | 1993-05-28 | 1994-12-08 | Unisearch Limited | Method of treating helicobacter pylori infection |
| JPH0717971A (en) * | 1993-07-02 | 1995-01-20 | Takeda Chem Ind Ltd | Imidazole derivative, production and use thereof |
| EP0711282B1 (en) | 1993-07-28 | 2002-06-05 | Aventis Pharma Limited | Compounds as pde iv and tnf inhibitors |
| DE69424487T2 (en) * | 1993-09-09 | 2001-01-18 | Takeda Chemical Industries Ltd | Formulation containing an antibacterial and an antiulcus active ingredient |
| US6489346B1 (en) | 1996-01-04 | 2002-12-03 | The Curators Of The University Of Missouri | Substituted benzimidazole dosage forms and method of using same |
| US5840737A (en) | 1996-01-04 | 1998-11-24 | The Curators Of The University Of Missouri | Omeprazole solution and method for using same |
| WO1997040039A1 (en) * | 1996-04-23 | 1997-10-30 | Yoshitomi Pharmaceutical Industries, Ltd. | Pyridine compounds and medicinal uses thereof |
| US8993599B2 (en) | 2003-07-18 | 2015-03-31 | Santarus, Inc. | Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using them |
| US8906940B2 (en) | 2004-05-25 | 2014-12-09 | Santarus, Inc. | Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using them |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL85472A (en) * | 1987-03-09 | 1991-06-30 | Procter & Gamble | Pharmaceutical compositions for treating gastrointestinal disorders |
| AU3690289A (en) * | 1988-05-25 | 1989-12-12 | Byk Gulden Lomberg Chemische Fabrik Gmbh | New fluoralkoxy compounds |
| JP2694361B2 (en) * | 1989-02-09 | 1997-12-24 | アストラ アクチエボラグ | Antibacterial agent |
| DK0382489T3 (en) * | 1989-02-10 | 1995-01-16 | Takeda Chemical Industries Ltd | Monoclonal Anti-Human Papillomavirus Antibody, Hybridoma Cell Producing This, and Method of Preparation thereof |
-
1991
- 1991-09-06 AT AT91914905T patent/ATE209914T1/en not_active IP Right Cessation
- 1991-09-06 WO PCT/EP1991/001689 patent/WO1992004898A1/en active IP Right Grant
- 1991-09-06 DE DE59109225T patent/DE59109225D1/en not_active Expired - Lifetime
- 1991-09-06 CA CA002092694A patent/CA2092694C/en not_active Expired - Lifetime
- 1991-09-06 EP EP91914905A patent/EP0548103B1/en not_active Expired - Lifetime
- 1991-09-06 JP JP3514343A patent/JPH06500547A/en active Pending
- 1991-09-06 AU AU84457/91A patent/AU8445791A/en not_active Abandoned
- 1991-09-06 DK DK91914905T patent/DK0548103T3/en not_active Application Discontinuation
- 1991-09-06 ES ES91914905T patent/ES2169022T3/en not_active Expired - Lifetime
- 1991-09-12 NZ NZ239772A patent/NZ239772A/en not_active IP Right Cessation
- 1991-09-12 IL IL9947191A patent/IL99471A/en not_active IP Right Cessation
- 1991-09-13 IE IE323291A patent/IE913232A1/en not_active IP Right Cessation
-
2003
- 2003-05-30 CY CY0300045A patent/CY2363B1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP0548103A1 (en) | 1993-06-30 |
| ES2169022T3 (en) | 2002-07-01 |
| WO1992004898A1 (en) | 1992-04-02 |
| CA2092694C (en) | 2005-04-05 |
| EP0548103B1 (en) | 2001-12-05 |
| NZ239772A (en) | 1997-03-24 |
| IE913232A1 (en) | 1992-02-25 |
| DK0548103T3 (en) | 2002-04-02 |
| DE59109225D1 (en) | 2002-01-17 |
| IL99471A0 (en) | 1992-08-18 |
| ATE209914T1 (en) | 2001-12-15 |
| CY2363B1 (en) | 2004-06-04 |
| CA2092694A1 (en) | 1992-03-15 |
| AU8445791A (en) | 1992-04-15 |
| JPH06500547A (en) | 1994-01-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed | ||
| KB | Patent renewed | ||
| KB | Patent renewed | ||
| EXP | Patent expired |