Depsipeptide derivatives, production thereof and use thereof

Details Depsipeptide derivatives, production thereof and use thereof Depsipeptide derivatives, production thereof and use thereof

1994-09-12

1996-05-07

Russel, Jeffrey E.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Cyclic peptides

530323, A61K 3812, A61K 3815, C07K 1102

Patent

active

055147739

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to new depsipeptide derivatives having antiparasitic activity.


BACKGROUND ART

Japanese Kokai Tokkyo Koho 3-35796 discloses depsipeptide derivative prepared by culturing microorganisms.


DISCLOSURE OF INVENTION

The object compound of the present invention, depsipeptide derivatives can be represented by the following general formula (I). ##STR2## wherein A is benzyl group which has suitable substituent(s) or phenyl group which may have suitable substituent(s), group which may have suitable substituent(s),
According to the present invention, the object compound of depsipeptide derivatives (I) can be prepared by processes which are illustrated in the following schemes.
It should be indicated that any of D-configured compound, L-configured compound and/or DL-configured compound are in the extent of the present invention; however, for the convenience, only D-configured compounds and L-configured compounds are explained in the process for preparation as follows. ##STR3## wherein A, A.sup.a, B, C and D are each as defined above, and lower alkoxy, and lower alkoxy, group which has mono- or di-lower alkylamino and lower alkoxy, cyclic amino and lower alkoxy, hydroxy and lower alkoxy,
Throughout the present specification, the amino acid, peptides, protective groups, condensing agents, etc. are indicated by the abbreviations according to the IUPAC-IUB (Commission on Biological Nomenclature) which are in common use in the field of art.
Moreover, unless otherwise indicated, the amino acids and their residues when shown by such abbreviations are meant to be L-configured compounds and residues, and when shown by D- abbreviations, they are meant to be D-configured compounds and residues.
In the present invention, there are employed the following abbreviations. .beta.-(p-methoxyphenyl)lactic acid! .beta.-(p-dimethylaminophenyl)lactic acid! .beta.-(p-piperazinophenyl)lactic acid! .beta.-(p-pyrrolidinophenyl)lactic acid .beta.-(p-nitrophenyl)lactic acid! .beta.-(p-aminophenyl)lactic acid! .beta.-(p-diethylaminophenyl)lactic acid! .beta.-(p-di-n-hexylaminophenyl)lactic acid! .beta.-(p-1H-pyrrol-1-yl)phenyl)lactic acid! .beta.-(p-hydroxyphenyl)lactic acid! .beta.-(p-ethoxyphenyl)lactic acid! .beta.-(p-n-hexyloxyphenyl)lactic acid! .beta.- p-(2-methoxyethoxy)phenyl!lactic acid! .beta.-{p- 2-(2-methoxyethoxy)ethoxy!phenyl}lactic acid! .beta.-(o-methoxyphenyl)lactic acid! .beta.-(m-methoxyphenyl)lactic acid! .beta.-(3,4-dimethoxyphenyl)lactic acid! .beta.-(2,4-dimethoxyphenyl)lactic acid! .beta.-(3,4-methylenedioxyphenyl)lactic acid! .beta.-(3-dimethylamino-4-methoxyphenyl)lactic acid! acid .beta.- 3,4-bis(dimethylamino)phenyl!lactic acid! .beta.-(o-fluorophenyl)lactic acid! .beta.-(m-fluorophenyl)lactic acid! .beta.-(p-fluorophenyl)lactic acid! .beta.-(p-morpholinophenyl)lactic acid!
Suitable salts of the compound (I) are conventional non-toxic, pharmaceutically acceptable salt 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, cesium salt, etc.), an alkali 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, dicyclohexylamine salt, N,N'-dibenzylethylenediamine salt, etc.), etc.; an inorganic acid addition salt (e.g. hydrochloride, hydrobromide, sulfate, phosphate, etc.); an organic carboxylic or sulfonic acid addition salt (e.g. formate, acetate, trifluoroacetate, maleate, tartrate, methanesulfonate, benzenesulfonate, p-toluenesulfonate, etc.); a salt with a basic or acidic amino acid (e.g. arginine, aspartic acid, glutamic acid,etc.); and the like.
In the above and subsequent descriptions of the present specification, suitable examples and illustrations of the various definitions which the present invention include within the scope thereof are explained in detail as follows.
The

REFERENCES:
patent: 5116815 (1992-05-01), Takagi et al.

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