Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Cyclic peptides
Patent
1997-05-21
2000-08-22
Davenport, Avis M.
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Cyclic peptides
514 9, 514 11, A61K 3800, A61K 3812, C07K 500, C07K 700
Patent
active
061074586
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to new polypeptide compound and a pharmaceutically acceptable salt thereof which are useful as a medicament.
BACKGROUND ART
In U.S. Pat. No. 5,376,634, there are disclosed the polypeptide compound and a pharmaceutically acceptable salt thereof, which have antimicrobial activities (especially antifungal activity).
DISCLOSURE OF INVENTION
The present invention relates to new polypeptide compound and a pharmaceutically acceptable salt thereof.
More particularly, it relates to new polypeptide compound and a pharmaceutically acceptable salt thereof, which have antimicrobial activities [especially, antifungal activities, in which the fungi may include Aspergillus, Cryptococcus, Candida, Mucor, Actinomyces, Histoplasma, Dermatophyte, Malassezia, Fusarium and the like.], inhibitory activity on .beta.-1,3-glucan synthase, and further which are expected to be useful for the prophylactic and/or therapeutic treatment of Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal, to a process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for the prophylactic and/or therapeutic treatment of infection diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
The object polypeptide compound used in the present invention are new and can be represented by the following general formula [I]: ##STR2## wherein R.sup.1 is a lower alkanoyl substituted with unsaturated 6-membered heteromonocyclic group containing at least one nitrogen atom which may have one or more suitable substituent(s); have one or more suitable substituent(s); containing at least one oxygen atom which may have one or more suitable substituent(s); containing 1 to 3 sulfur atom(s) which may have one or more suitable substituent(s); containing 2 or more nitrogen atom(s) which may have one or more suitable substituent(s); group containing at least one nitrogen atom which may have one or more suitable substituent(s); substituent(s); suitable substituent(s), in which ar(C.sub.2 -C.sub.6) alkanoyl may have one or more suitable substituent(s); suitable substituent(s), in which aroyl may have one or more suitable substituent(s); heterocyclic group may have one or more suitable substituent(s); substituent(s); substituent(s); having higher alkoxy; suitable substituent(s); heterocyclicoxy may have one or more suitable substituent(s); alkoxy(lower)alkoxy; alkoxy; having lower alkoxy; higher alkyl; which (C.sub.2 -C.sub.6) alkanoyl may have amino or protected amino.
The new polypeptide compound [I] and a pharmaceutically acceptable salt thereof can be prepared by the process as illustrated in the following reaction scheme or can be prepared by elimination reaction of amino protective group in R.sup.1. ##STR3## wherein R.sup.1 is as defined above.
Suitable pharmaceutically acceptable salts of the object polypeptide compound [I] are conventional non-toxic salts and may include a salt with a base or an acid addition salt such as a salt with an inorganic base, for example, an alkali metal salt (e.g., sodium salt, potassium salt, etc.), an alkaline earth metal salt (e.g., calcium salt, magnesium salt, etc.), an ammonium salt; a salt with an organic base, for example, an organic amine salt (e.g., triethylamine salt, pyridine salt, picoline salt, ethanolamine salt, triethanolamine salt, dichclohexylamine salt, N,N'-dibenzylethylenediamine salt, etc.); and inorganic acid addition salt (e.g., hydrochloride, hydrobromide, sulfate, phosphate, etc.); an organic carboxylic sulfonic acid addition salt (e.g., formate, acetate, trifluoroacetate, maleate, tartrate, fumarate, methanesulfonate, benzenesulfonate, toluenesulfonate, etc.); a salt with a basic or acidic amino acid (e.g., arginine, aspartic acid, glutamic acid, etc.).
In the above and subsequent descriptions of the present specification, suitable examples and illustration of the various definitions which the present invention inten
REFERENCES:
patent: 5376634 (1994-12-01), Iwamoto et al.
Ohki Hidenori
Takasugi Hisashi
Tomishima Masaki
Yamada Akira
Davenport Avis M.
Fujisawa Pharmaceutical Co. Ltd.
LandOfFree
Cyclic hexapeptides having antibiotic activity does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Cyclic hexapeptides having antibiotic activity, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Cyclic hexapeptides having antibiotic activity will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-582456