Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-01-14
1994-12-27
Lee, Mary C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514302, 514303, 514367, 514375, 514395, 546 23, 548113, C07D23504, C07D22104, A61K 31415, A61K 3144
Patent
active
053766652
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to novel phosphonic diester derivatives.
PRIOR ART
The phosphonic diester derivatives of the invention are novel compounds not heretofore described in the literature.
DISCLOSURE OF THE INVENTION
The object of the invention is to provide compounds of value as medicines as will be described hereinafter.
The present invention provides a phosphonic diester derivative of the following general formula (1): ##STR2## [wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each represents a hydrogen atom, a lower alkyl group, a phenyl group, a lower alkoxy group, a halogen-substituted lower alkyl group, a halogen-substituted lower alkoxy group, a lower alkanoyl group, a benzoyl group, a (lower)alkoxycarbonyl group, a nitro group, a halogen atom, a (lower)alkylthio group, a phenyl(lower)alkoxy group, a carbamoyl group or a (lower)alkoxycarbonyl(lower)alkoxy group; R.sup.4 represents a hydrogen atom, a lower alkyl group or a phenyl(lower) alkyl group; R.sup.5 and R.sup.6 are the same or different and each represents a lower alkoxy group, a phenyl group, a phenoxy group, a phenyl(lower)alkoxy group or a hydroxyl group; A represents a carbon atom or a nitrogen atom; B represents a group of the formula .dbd.NR.sup.7 (where R.sup.7 represents a hydrogen atom, a lower alkyl group or a phenyl(lower)alkyl group), an oxygen atom or a sulfur atom; Y represents a group of the formula C.dbd.O or a group of SO.sub.2 ; X represents an oxygen atom or a bond; Z represents a lower alkylene group optionally having a lower alkyl or phenyl(lower)alkyl group as a substituent or a bond; provided, however, that X and Z do not concurrently represent bonds]
Each of the groups relevant to the above general formula (1) includes the following exemplary species.
The lower alkyl group includes straight- or branched-chain lower alkyl groups such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl and so on.
The lower alkoxy group includes methoxy, ethoxy, propoxy, isopropoxy, butoxy, pentyloxy, hexyloxy and so on.
The halogen-substituted lower alkyl group includes trifluoromethyl, pentafluoroethyl, heptafluoropropyl, nonafluorobutyl, undecafluoropentyl, tridecafluorohexyl and so on.
The halogen-substituted lower alkoxy group includes trifluoromethoxy, pentafluoroethoxy, heptafluoropropoxy, nonafluorobutoxy, undecafluoropentyloxy, tridecafluorohexyloxy and so on.
The lower alkanoyl group includes acetyl, propionyl, butyryl, valeryl, pivaloyl, hexanoyl, heptanoyl and so on.
The lower alkoxycarbonyl group includes methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, butoxycarbonyl, pentyloxycarbonyl, hexyloxycarbonyl and so on.
The phenyl(lower)alkyl group includes benzyl, 2-phenylethyl, 3-phenylpropyl, 4-phenylbutyl, 5-phenylpentyl, 6-phenylhexyl and so on.
The halogen atom includes fluorine, clorine, bromine and iodine.
The lower alkylthio group includes methylthio, ethylthio, propylthio, butylthio, pentylthio, hexylthio and so on.
The phenyl(lower)alkoxy group includes benzyloxy, 2-phenylethoxy, 3-phenylpropoxy, 4-phenylbutoxy, 5-phenylpentyloxy, 6-phenylhexyloxy and so on.
The lower alkoxycarbonyl(lower)alkoxy group includes methoxycarbonylmethoxy, 2-ethoxycarbonylethoxy, 3-ethoxycarbonylpropoxy, 4-ethoxycarbonylbutoxy, 5-ethoxycarbonylpentyloxy, 6-ethoxycarbonylhexyloxy, 2-butoxycarbonylethoxy, hexyloxycarbonylmethoxy and so on.
The lower alkylene group optionally having a lower alkyl or phenyl(lower)alkyl group as a substituent includes methylene, ethylene, trimethylene, tetramethylene, pentamethylene, hexamethylene, ethylidene, propylidene, butylidene, pentylidene, hexylidene, heptylidene, 2-phenylethylidene, 3-phenylpropylidene, 4-phenylbutylidene, 5-phenylpentylidene, 6-phenylhexylidene, 7-phenylheptylidene and so on.
The phosphonic diester derivative of general formula (1) according to the present invention has excellent hypolipidemic and hypoglycemic activities and is, therefore, useful for the treatment and prevention of various types of hyperlipide
REFERENCES:
CA 117(19):192072d Preparation . . . acids, Fujita et al., p. 826, 1992.
28-Heterocycles, vol. 110, 198, pp. 692-693, 110: 57664p, "(Pyridinylmethyl)sulfinylbenzimidazole derivatives as antiulcer agents, their preparation and formulations containing them", 1986.
Inoue Yasuhide
Kurogi Yasuhisa
Miyata Kazuyoshi
Naba Chieko
Shoji Yasuo
Lee Mary C.
McKane Joseph K.
Otsuka Pharmaceutical Factory Inc.
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