Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-05-02
1999-01-05
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142375, 5142395, 544111, 544170, A61K 31535, C07D41300, C07D26530
Patent
active
058563245
DESCRIPTION:
BRIEF SUMMARY
This is a 371 application of PCT/EP 95/04255 filed on Sep. 30, 1995.
The present invention relates to the use of dioxomorpholines for combating endoparasites, to new dioxomorpholines and to processes for their preparation.
Certain dioxomorpholines and processes for their preparation are already known (compare, for example, Liebigs Ann. Chem. 1952 (1982), Makromol. Chem., Rapid Commun., 6 (1985), 607; Tetrachedron, 37 (1981), 2797; WO 9403441A1), but nothing has been disclosed to date pertaining to the use of these compounds against endoparasites.
The present invention relates to: ##STR2## in which R.sup.1 and R.sup.2 independently of one another represent hydrogen, straight-chain or branched alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, which are optionally substituted, optionally substituted, aralkyl, aryl, heteroaryl or heteroarylalkyl, which are optionally substituted, represent a 5- or 6-membered ring, which can optionally be substituted, straight-chain or branched alkyl, alkenyl, cycloalkyl, cycloalkylalkyl aryl, arylalkyl, heteroaryl or heteroarylalkyl, which are optionally substituted, substituted, ##STR3## in which R.sup.1 and R.sup.2 independently of one another represent hydrogen, straight-chain or branched alkyl having up to 8 carbon atoms, halogenoalkyl, hydroxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, aryloxyalkyl, mercaptoalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, carboxyalkyl, alkoxycarbonylalkyl, arylalkoxycarbonylalkyl, carbamoylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, guanidinoalkyl, which can optionally be substituted by one or two benzyloxycarbonyl radicals or by one, two, three or four alkyl radicals, alkoxycarbonylaminoalkyl, 9-fluoroenyl-methoxycarbonyl(Fmoc)aminoalkyl, alkenyl, cycloalkyl or cycloalkylalkyl, or represent optionally substituted aryl, arylalkyl, heteroaryl or heteroarylalkyl, aralkyl, aryl, heteroaryl or heteroarylalkyl, which are optionally substituted, represent a 5- or 6-membered ring, which can optionally be substituted, straight-chain or branched alkyl having up to 8 carbon atoms, halogenoalkyl, hydroxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, aryloxyalkyl, mercaptoalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, carboxyalkyl, alkoxycarbonylalkyl, arylalkoxycarbonylalkyl, carbamoylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, guanidinoalkyl, which can optionally be substituted by one or two benzyloxycarbonyl radicals or by one, two, three or four alkyl radicals, alkoxycarbonylaminoalkyl, 9-fluorenylmethoxycarbonyl(Fmoc)aminoalkyl, alkenyl, cycloalkyl or cycloalkylalkyl, or represent optionally substituted aryl, arylalkyl, heteroaryl or heteroarylalkyl, medicine.
The invention furthermore relates to: ##STR4## in which R.sup.1 represents hydrogen, straight-chain or branched alkyl having up to 8 carbon atoms, halogenoalkyl, hydroxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, aryloxyalkyl, mercaptoalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, carboxyalkyl, alkoxycarbonylalkyl, arylalkoxycarbonylalkyl, carbamoylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, guanidinoalkyl, which can optionally be substituted by one or two benzyloxycarbonyl radicals or by one, two, three or four alkyl radicals, alkoxycarbonylaminoalkyl, 9-fluorenylmethoxycarbonyl(Fmoc)aminoalkyl, alkenyl, cycloalkyl or cycloalkylalkyl, or represents optionally substituted aryl, arylalkyl, heteroaryl or heteroarylalkyl, 8 carbon atoms, halogenoalkyl, hydroxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, aryloxyalkyl, mercaptoalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, carboxyalkyl, alkoxycarbonylalkyl, arylalkoxycarbonylalkyl, carbamoylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, guanidinoalkyl, which can optionally be substituted by one or two benzyloxycarbonyl radicals or by one, two, three or four alkyl radicals, alkoxycarbonylaminoalkyl, 9-fluorenylmethoxycarbonyl(Fmoc)aminoalkyl, alkenyl, cycloalkyl or cycloalkylalkyl, or represents optionally substituted ary
REFERENCES:
Makromol. Chem. Rapid Commun. 6, 9, Helder, et al. (1985).
Makromol. Chem. Rapid Commun. 6, 607, Yonezawa, et al. (1985).
Makomol. Chem. 191, 1813, In't. Veld, et al. (1990).
Hasumi et al., "Lateritin . . . ", Journal of Antibiotics, vol. 46, No. 12 (Dec. 1993), pp. 1782-1787.
Chemical Abstracts, vol. 78, No. 9, Mar. 5, 1973, Abstract No. 58777; Shemyakin M.M. et al., "Synthesis and antimicrobial activity of analogs of enniatin antibiotics", pp. 2320-2334.
Chemical Abstracts, vol. 66, No. 18, May 1, 1967, Abstract No. 80398 M.M. Shemyakin, et al. "Depsipeptides. Mass spectrometric study of cyclodepsipeptides, 2,5-dioxomorpholines.", pp. 1539-1543.
Tetrahedron Letters, Bd. 26, Nr. 43, 1985, pp. 5257-5260, H.-G. Lerchen, et al. "Stereoselektive Synthese von D-Alpha-Hydroxycarbonsauren enthaltenden Depsipeptiden aus L-Aminosauren."
Harder Achim
Jeschke Peter
Mencke Norbert
Plant Andrew
Scherkenbeck Jurgen
Bayer Aktiengesellschaft
Ngo Tamthom T.
Shah Mukund J.
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