Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-04-24
1999-08-24
Mach, D. Margaret M.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
514312, C07D215233, A61K 3147
Patent
active
059426195
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to novel quinolone compounds, and particularly to novel quinolone compounds produced by fermentation of a microorganism designated as Amycolata sp., which has been deposited as FERM BP-4785. This invention also relates to processes for producing the quinolone compounds, and a pharmaceutical composition comprising the same, which is useful in the treatment of diseases, disorders and adverse conditions caused by Helicobacter pylori and is particularly useful in the treatment of gastroduodenal disorders, diseases and adverse conditions caused thereby.
BACKGROUND ART
Gastric and duodenal ulcers affect a significant portion of the human population worldwide. Currently, the usual treatment for both gastric and duodenal ulcers involves treatment of the patient with histamine H.sub.2 receptor antagonists (H.sub.2 blockers). While the H.sub.2 blocker therapy is generally effective in healing ulcers, ulcer relapse occurs in up to 90% of patients within a year of discontinuing the therapy. Thus, patients must continue the treatment for many years or risk a recurrence of the ulcer. It is now known that ulcer healing drugs such as colloidal bismuth subcitrate (CBS) are helicobactericidal and that such CBS is used in combination with H.sub.2 blockers to treat ulcers. Additionally, CBS, an H.sub.2 blocker and amoxicillin have been used in combination to treat ulcer patients.
Helicobacter pylori has been recently demonstrated to be a major causative agent in gastric and duodenal ulcers and other gastroduodenal disorders, diseases and adverse conditions. Thus, antibiotic therapy to eliminate Helicobacter pylori from the gastroduodenal tract would remove the root cause of said gastroduodenal disorders, diseases and adverse conditions and eliminate the need for an ulcer patient to continue long and costly treatment with H.sub.2 blockers and the like. None of the foregoing treatments are capable of 100% eradication of Helicobacier plyori. Therefore, it would be desired to provide a compound having an excellent helicobactericidal activity.
The object of the present invention is to provide novel quinolone compounds having an excellent helicobactericidad activity and a pharmaceutical composition comprising the same. Another object of the present invention is to provide processes for producing the novel quinolone compounds.
BRIEF DESCRIPTION OF THE INVENTION
Accordingly, the present invention provides quinolone compounds of the formula: ##STR2## wherein R is a group of the formula: R.sup.1 is H, R.sup.2 is ##STR3## and R.sup.3 is CH.sub.3 ; R.sup.1 is CH.sub.3, R.sup.2 is ##STR4## and R.sup.3 is CH.sub.3 ; R.sup.1 is CH.sub.2 SCH.sub.3, R.sup.2 is ##STR5## and R.sup.3 is CH.sub.3 ; R.sup.1 is CH.sub.3, R.sup.2 is ##STR6## and R.sup.3 is CH.sub.3 ; R.sup.1 is H, R.sup.2 is ##STR7## and R.sup.3 is H; R.sup.1 is CH.sub.3, R.sup.2 is ##STR8## and R.sup.3 is H; R.sup.1 is CH.sub.3, R.sup.2 is ##STR9## and R.sup.3 is H; or R.sup.1 is CH.sub.3, R.sup.2 is ##STR10## and R.sup.3 is H.
Among the compounds of formula (I) of the present invention, preferred is a compound of formula (I) wherein ##STR11## and R.sup.3 is CH.sub.3 ; R.sup.1 is CH.sub.3, R.sup.2 is ##STR12## and R.sup.3 is CH.sub.3 ; or R.sup.1 is CH.sub.3, R.sup.2 is ##STR13## and R.sup.3 is CH.sub.3.
Among these compounds, most preferred is a compound of formula (I) wherein R.sup.1 is H, R.sup.2 is ##STR14## and R.sup.3 is CH.sub.3.
Further, the present invention provides processes for producing the quinolone compounds of formula (I), which comprise cultivating a microorganism having identifying characteristics of FERM BP-4785, or a mutant or recombinant form thereof. This process may further comprise the subsequent step of isolating said quinolone compounds from the fermentation broth.
The present invention is also directed to a culture which belongs to genus Amycolata being capable of producing quinolones, including the culture Amycolata sp. FERM BP-4785.
Also, the present invention provides a pharmaceutical composition for use in
REFERENCES:
Chemical Abstracts 109:92736, coppola, 1988.
Chemical Abstracts 108:142529, Huang, 1987.
Marpat 118:22154, Clemence, 1992.
Marpat 118:22153, Clemence, 1992.
Dekker Koenraad A.
Huang Liang H.
Inagaki Taisuke
Kojima Nakao
Kojima Yasuhiro
Ginsburg Paul H.
M. Mach D. Margaret
Pfizer Inc.
Richardson Peter C.
Zielinski Bryan C.
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