Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1998-06-26
1999-11-16
Ambrose, Michael G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
514 80, 514 81, 514 85, 514 92, 544337, 548113, 548119, 549 6, A61K 3167, A61K 31675, C07F 96553, C07F 96539
Patent
active
059858583
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND ART
The phosphonic diester derivatives of the invention are novel compounds not heretofore described in any literature.
The object of the invention is to provide compounds of value as medicines as will be described hereinafter.
DISCLOSURE OF THE INVENTION
The present invention provides a novel derivative represented by the following formula (1): ##STR2## wherein R.sup.1 represents a cycloalkyl group; a phenyl group which may have 1 to 3 substituents selected from the group consisting of a lower alkoxy group, a lower alkyl group, a halogen atom, a halogen-substituted lower alkyl group, a lower alkanoyl group, a nitro group, a benzoyl group, a cyano group, an N-lower alkylcarbamoyl group, an N-phenyl-lower alkylcarbamoyl group, an N-(halogen-substituted phenyl)carbamoyl group and an N,N-di-lower alkylcarbamoyl group; a 1,3,4-thiadiazol-2-yl group having a halogen-substituted lower alkyl group as a substituent; a thiazolyl group; a pyridyl group which may be substituted by a halogen atom; a benzothiazol-2-yl group having 1 to 2 lower alkoxy groups on the phenyl ring; or a 4,5-dihydrothieno[3,2-e]benzothiazol-2-yl group; R.sup.2 represents a hydrogen atom or a phenyl lower alkyl group; R.sup.3 and R.sup.4 each represents a lower alkyl group; and A represents a heterocyclic ring selected from the group consisting of a pyrazine ring, a thiophene ring and a phenyl-substituted thiazole ring.
Each of the groups in the above formula (1) includes the following exemplary species.
The cycloalkyl group includes cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl and like C.sub.3-8 cycloalkyl groups.
The lower alkyl group includes methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl and like C.sub.1-6 straight- or branched-chain alkyl groups.
The lower alkoxy group includes methoxy, ethoxy, propoxy, butoxy, tert-butoxy, pentyloxy, hexyloxy and like C.sub.1-6 straight- or branched-chain alkoxy groups.
The halogen atom includes fluorine, chlorine, bromine and iodine.
The halogen-substituted lower alkyl group includes the above lower alkyl groups having 1 or more halogen atoms as substituents, such as trifluoromethyl, pentafluoroethyl, heptafluoropropyl, nonafluorobutyl, undecafluoropentyl and tridecafluorohexyl.
The lower alkanoyl group includes acetyl, propionyl, butyryl, valeryl, pivaloyl, hexanoyl, heptanoyl and like C.sub.2-7 alkanoyl groups.
The N-lower alkylcarbamoyl group includes N-methylcarbamoyl, N-ethylcarbamoyl, N-propylcarbamoyl, N-butylcarbamoyl, N-pentylcarbamoyl, N-hexylcarbamoyl and the like.
The N-phenyl-lower alkylcarbamoyl group includes N-benzylcarbamoyl, N-(2-phenylethyl)carbamoyl, N-(3-phenylpropyl)carbamoyl, N-(4-phenylbutyl)carbamoyl, N-(5-phenylpentyl)carbamoyl, N-(6-phenylhexyl)carbamoyl and the like.
The N-(halogen-substituted phenyl)carbamoyl group includes N-(4-chlorophenyl)carbamoyl, N-(3-chlorophenyl)carbamoyl, N-(2-chlorophenyl)carbamoyl, N-(4-fluorophenyl)carbamoyl, N-(4-bromophenyl)carbamoyl, N-(4-iodophenyl)carbamoyl and the like.
The N,N-di-lower alkylcarbamoyl group includes N,N-dimethylcarbamoyl, N,N-diethylcarbamoyl, N,N-dipropylcarbamoyl, N,N-dibutylcarbamoyl, N,N-dipentylcarbamoyl, N,N-dihexylcarbamoyl, N-methyl-N-ethylcarbamoyl and the like.
The phenyl lower alkyl group includes benzyl, 1-phenylethyl, 2-phenylethyl, 3-phenylpropyl, 4-phenylbutyl, 5-phenylpentyl, 6-phenylhexyl and the like.
The thiazolyl group includes 2-thiazolyl, 4-thiazolyl and 5-thiazolyl.
The 1,3,4-thiadiazol-2-yl group having a halogen-substituted lower alkyl group includes 5-trifluoromethyl-1,3,4-thiadiazol-2-yl, 5-pentafluoroethyl-1,3,4-thiadiazol-2-yl, 5-heptafluoropropyl-1,3,4-thiadiazol-2-yl, 5-nonafluorobutyl-1,3,4-thiadiazol-2-yl, 5-undecafluoropentyl-1,3,4-thiadiazol-2-yl, 5-tridecafluorohexyl-1,3,4-thiadiazol-2-yl and the like.
The pyridyl group which may be substituted by a halogen atom includes 2-pyridyl, 3-pyridyl, 4-pyridyl, 5-bromo-2-pyridyl, 5-chloro-2-pyridyl, 5-fluoro-2-pyridyl, 5-iodo-2-pyridyl, 5-bromo-3-pyridyl, 3-bromo-4-pyridyl
REFERENCES:
patent: 4971957 (1990-11-01), Tsutsumi et al.
patent: 5480874 (1996-01-01), Shoji et al.
Inoue Yasuhide
Miki Shinya
Miyata Kazuyoshi
Sakai Yasuhiro
Sato Keigo
Ambrose Michael G.
Otsuka Pharmaceutical Factory Inc.
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