Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-10-31
1999-01-19
Dentz, Bernard
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
549304, 435118, 435126, 514462, 514469, C07D30788, C12P 1704, A61K 3134
Patent
active
058615180
DESCRIPTION:
BRIEF SUMMARY
CROSS REFERENCE TO RELATED APPLICATIONS
This application is the National Stage of pending International Patent Application No. PCT/IB96/00820, filed on Oct. 02, 1995, entitled "Phthalide Compounds and their Production Process", which is a continuation in-part of International Patent Application No. PCT/JP94/01962, filed on Nov. 21, 1994, entitled "Phthalide Compounds and their Production Process", now abandoned.
1. Technical Field
This invention relates to novel phthalide compounds, and particularly to novel phthalide compounds produced by fermentation of a microorganism which has been deposited as FERM BP-4787. This invention also relates to processes for producing the phthalide 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.
2. 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 generally effective in healing ulcers, ulcer relapse occures in up to 90% of patients within a year of discontinuing the H.sub.2 blocker 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 Helicobacter pylori
Therefore, it would be desired to provide a compound having an excellent helicobactericidal activity.
The object of the present invention is to provide novel phthalide compounds having a excellent helicobactericidal activity and a pharmaceutical composition comprising the same. Another object of the present invention is to provide processes for producing the novel phthalide compounds.
BRIEF DISCLOSURE OF THE INVENTION
Accordingly, the present invention provides phthalide compounds of the formula: ##STR1## wherein R is a group of the formula: ##STR2## --(CH.sub.2).sub.3 --C(.dbd.O)--(CH.sub.2).sub.2 --C(.dbd.O)--CH.sub.3, --(CH.sub.2).sub.5 --C(.dbd.O)--(CH.sub.2).sub.2 --C(.dbd.O)--CH.sub.3, --(CH.sub.2).sub.6 --CH(OH)--CH.sub.3 or --(CH.sub.2).sub.6 --C(.dbd.O)--CH.sub.3.
Among the compounds of formula (I) of the present invention, prefer compound of formula (I) wherein R is: ##STR3##
Further, the present invention provides processes for producing the phthalide compounds of formula (I), which comprise cultivating a microorganism having identifying characteristics of FERM BP-4787, or a mutant or recombinant form thereof.
Also, the present invention provides a pharmaceutical composition for use in the treatment of Helicobacter pylori-induced disorders, diseases or adverse conditions caused thereby, such as gastroduodenal disorders including gastric ulcer, duodenal ulcer and gastric cancer, which comprises compounds of formula (I) and a pharmaceutically-acceptable carrier.
DETAILED DESCRIPTION OF THE INVENTION
The microorganism used in this invention is a strain of Phanerochaete velutina FPL 5362 which was obtained from the Forest Products Laboratory of the United States Depart
REFERENCES:
Abstract of Japan Agri. Chem. 4Ep13, 1997.
A. Arnone et al. Chemical abstracts, vol. 112, No. 19, May 7, 1990 Columbus, Ohio abstract No. 175338z,.
A. Arnone et al. Phytochemistry, vol. 29, No. 2, 1990 pp. 613-616.
Dekker Koenraad A.
Inagaki Taisuke
Kojima Nakao
Sakemi Shinichi
Yamauchi Yuji
Benson Gregg C.
Dentz Bernard
Goddard Carl J.
Richardson Peter C.
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