Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1995-02-05
1997-04-29
Gibson, Sharon
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
540542, 544 92, 544244, A61K 31675, C07F 96512
Patent
active
056249187
DESCRIPTION:
BRIEF SUMMARY
This application is a National Phase filling of PCT/JP94/00883, which was filed in the International Phase May 31, 1994.
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.
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 phosphonic diester derivative of the following general formula (1): ##STR2## wherein A represents an oxygen atom or a sulfur atom; R.sup.1, R.sup.2, R.sup.9 and R.sup.10 are the same or different and they each represent a hydrogen atom, a lower alkoxy group, a nitro group, a lower alkyl group, a halogen-substituted lower alkyl group or a halogen atom; R.sup.3 represents a phenyl group, --B--R.sup.6 (wherein B represents an oxygen atom or a sulfur atom and R.sup.6 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, a phenyl group, a phenyl(lower)alkyl group optionally having a halogen atom as a substituent on the phenyl ring, a phenoxy(lower)alkyl group, a lower alkoxycarbonyl(lower)alkyl group, a carboxy(lower)alkyl group or a lower alkenyl group) or --NR.sup.7 R.sup.8 (wherein R.sup.7 and R.sup.8 are the same or different and they each represent a hydrogen atom, a lower alkyl group, an amino group or a cycloalkyl group or combinedly represent a lower alkylene group); and R.sup.4 and R.sup.5 are the same or different and they each represent a hydrogen atom or a lower alkyl group.
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 cycloalkyl group includes cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl and so on.
The lower alkoxy group includes methoxy, ethoxy, propoxy, butoxy, pentyloxy, hexyloxy and so on.
The phenyl(lower)alkyl group optionally having a halogen atom as a substituent on the phenyl ring includes benzyl, .alpha.-phenetyl, .beta.-phenetyl, 3-phenylpropyl, 4-phenylbutyl, 5-phenylpentyl, 6-phenylhexyl, 2-bromobenzyl, 2-fluorobenzyl, 2-chlorobenzyl, 2-iodobenzyl, 3-bromobenzyl, 3-fluorobenzyl, 3-chlorobenzyl, 3-iodobenzyl, 4-bromobenzyl, 4-fluorobenzyl, 4-chlorobenzyl, 4-iodobenzyl, 4-bromo-3-fluorobenzyl, 4-bromo-2-fluorobenzyl, 3-bromo-4-fluorobenzyl, 2-bromo-4-fluorobenzyl, 4-bromo-3-chlorobenzyl, 4-bromo-2-chlorobenzyl, 3-bromo-4-chlorobenzyl, 2-bromo-4-chlorobenzyl, 4-bromo-3-iodobenzyl, 4-bromo-2-iodobenzyl, 3-bromo-4-iodobenzyl, 2-bromo-4-iodobenzyl, 4-bromo-3-fluoro-.alpha.-phenetyl, 4-bromo-3-fluoro-.beta.-phenetyl, 3-(4-bromo-3-fluorophenyl)propyl, 4-(4-bromo-2-fluorophenyl)butyl, 5-(4-bromo-3-fluorophenyl)pentyl, 6(4-bromo-2-fluorophenyl)hexyl and so on.
The phenoxy(lower)alkyl group includes phenoxymethyl, 2-phenoxyethyl, 3-phenoxylpropyl, 4-phenoxybutyl, 5-phenoxypentyl, 6-phenoxyhexyl and so on.
The lower alkylene group includes methylene, ethylene, trimethylene, tetramethylene, pentamethylene, hexamethylene and so on.
The halogen-substituted lower alkyl group includes chloromethyl, bromomethyl, fluoromethyl, iodomethyl, dichloromethyl, dibromomethyl, difluoromethyl, diiodomethyl, trichloromethyl, tribromomethyl, trifluoromethyl, triiodomethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, 3-bromopropyl, 4,4-dichlorobutyl, 5,5,5-trifluoropentyl, 6-iodohexyl and so on.
The lower alkoxycarbonyl(lower)alkyl group includes methoxycarbonylmethyl, ethoxycarbonylmethyl, propoxycarbonylmethyl, butoxycarbonylmethyl, pentyloxycarbonylmethyl, hexyloxycarbonylmethyl, 1-(methoxycarbonyl)ethyl, 2-(methoxycarbonyl)ethyl, 3-(methoxycarbonyl)propyl, 4-(methoxycarbonyl)butyl, 5-(methoxycarbonyl)pentyl, 6-(methoxycarbonyl)hexyl, 1-(ethoxycarbonyl)ethyl, 2-(ethoxycarbonyl)ethyl, 3-(ethoxycarbonyl)propyl, 4-(ethoxycarbonyl)butyl, 5-(et
REFERENCES:
patent: 4232010 (1980-11-01), Tsukamoto et al.
patent: 4434162 (1984-02-01), Tsukamoto et al.
patent: 4822780 (1989-04-01), Tsuda et al.
patent: 4971957 (1990-11-01), Tsutsumi et al.
patent: 5081112 (1992-01-01), Tsutsumi et al.
Otsuka Seiyaku Kogyo KK Derwent Abstract of JP 02-11590 (Jan. 1990).
Otsuka Pharm. Co. Derwent Abstract of JP 03-236394A (Oct. 1991).
Otsuka Pharm. Co. Derwent Abstract of JP 04-243888A (Aug. 1992).
Otsuka Seiyaku Kogyo KK Derwent Abstract of JP 04-244090 (Sep. 1992).
Otsuka Seiyaku Kogyo KK Derwent Abstract of JP 04-356495A (Dec. 1992).
Otsuka Seiyaku Kogyo KK Derwent Abstract of JP 05-43589A (Feb. 1993).
Otsuka Seiyaku Kogyo KK Derwent Abstract of JP 05-97883A (Apr. 1993).
Tsutsumi et al., Chemical Abstracts, vol. 113, No. 6602, Abstract for JP 02,11,590 (Jan. 16, 1990).
Dia et al., Chemical Abstracts, vol. 116, No. 99337, Abstract for JP 03,236,394 (Oct. 22, 1991).
Shoji et al., Chemical Abstracts, vol. 118, No. 38912, Abstract for JP 04,243,888 (Jan. 24, 1991).
Myata et al., Chemical Abstracts, vol. 118, No. 7195 Abstract for JP 04,244,090 (Oct. 1, 1992).
Myata et al., Chemical Abstracts, vol. 119, No. 95360 Abstract for JP 05,43,589 (Feb. 23, 1993).
Tsuda et al., Chemical Abstracts, vol. 119, No. 95829 Abstract for JP 04,356,495 (Dec. 10, 1992).
Myata et al. Chemical Abstracts, vol. 119, No. 160570 Abstract for JP 05,97,883 (Apr. 20, 1993).
Inoue Yasuhide
Iwamoto Takeshi
Kanaya Jun
Kondo Mitsuyoshi
Kurogi Yasuhisa
Gibson Sharon
Myers Richard S.
Otsuka Pharmaceutical Factory Inc.
LandOfFree
Phosphonic diester derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Phosphonic diester derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Phosphonic diester derivatives will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-705782