Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – C-o-group doai
Patent
1999-09-02
2000-09-19
Lambkin, Deborah C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
C-o-group doai
514717, 514679, 514684, 568807, 568659, 568661, 568332, A61K 31045, A61K 3112, C07C 3334, C07C 4100, C07C 4976
Patent
active
061213306
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to 5-hydroxy-alkyl-substituted phenyls, to processes for their preparation and to their use in medicaments.
The publication U.S. Pat. No. 5,169,857 A2 discloses 7-(polysubstituted pyridyl)-6-heptenoates for the treatment of arteriosclerosis, lipoproteinaemia and hyperlipoproteinaemia. Moreover, the preparation of 7-(4-aryl-3-pyridyl)-3,5-dihydroxy-6-heptenoate is described in the publication EP 325 130 A2. Furthermore, polyarylbenzenes are disclosed in the publication J.Org.Chem. (1979), 44(26), 4749-52.
The present invention, accordingly, provides 5-hydroxy-alkyl-substituted phenyls of the general formula (I) ##STR1## in which A represents aryl having 6 to 10 carbon atoms which is optionally substituted up to 5 times by identical or different substituents from the group consisting of halogen, hydroxyl, trifluoromethyl, trifluoromethoxy, nitro, or by straight-chain or branched alkyl, acyl, hydroxyalkyl or alkoxy having in each case up to 7 carbon atoms, or by a group of the formula --NR.sup.3 R.sup.4 in which hydrogen, phenyl, or straight-chain or branched alkyl having up to 6 carbon atoms, substituted by nitro, halogen, trifluoromethyl or trifluoromethoxy, or represents a radical of the formula ##STR2## in which R.sup.5, R.sup.6 and R.sup.9 are identical or different and each represents cycloalkyl having 3 to 6 carbon atoms or aryl having 6 to 10 carbon atoms or forms a 5- to 7-membered, optionally benzo-fused, saturated or unsaturated, mono-, bi- or tricyclic heterocycle having up to 4 carbon atoms from the group consisting of S, N and O, where the cycles, in the case of the nitrogen-containing rings also via the N-function, are optionally substituted up to 5 times by identical or different substituents from the group consisting of halogen, trifluoromethyl, nitro, hydroxyl, cyano, carboxyl, trifluoromethoxy, straight-chain or branched acyl, alkyl, alkylthio, alkylalkoxy, alkoxy and alkoxycarbonyl having in each case up to 6 carbon atoms, by aryl having 6 to 10 carbon atoms or by an optionally benzo-fused aromatic 5- to 7-membered heterocycle having up to 3 heteroatoms from the group consisting of S, N and/or O, and/or by a group of the formula --OR.sup.10, --SR.sup.11, --SO.sub.2 R.sup.12 or --NR.sup.13 R.sup.14, in which represents aryl having 6 to 10 carbon atoms which for its part is substituted up to 2 times by identical or different substituents from the group consisting of phenyl, halogen or by straight-chain or branched alkyl having up to 4 carbon atoms, R.sup.3 and R.sup.4 given above, or ##STR3## T represents straight-chain or branched alkyl or alkenyl having in each case 2 to 10 carbon atoms which are optionally substituted up to 2 times by hydroxyl, trifluoromethoxy, straight-chain or branched alkoxy having up to 5 carbon atoms or a radical of the formula --NR.sup.15 R.sup.16, in which R.sup.3 and R.sup.4 given above, or .dbd.NR.sup.17, in which having in each case up to 6 carbon atoms, branched alkyl having up to 8 carbon atoms, or formula --NR.sup.18, in which to 6 carbon atoms or phenyl, straight-chain or branched alkyl having up to 8 carbon atoms which is optionally substituted by cycloalkyl having 3 to 8 carbon atoms or hydroxyl, or represents phenyl which is optionally substituted by halogen or trifluoromethyl, having in each case up to 6 carbon atoms or represents a radical of the formula --NR.sup.19 R.sup.20 or ##STR4## in which R.sup.19 and R.sup.20 have the meanings of R.sup.3 and R.sup.4 given above and are identical to or different from these, and atoms which is substituted by hydroxyl, substituted by halogen, nitro, cyano, trifluoromethyl, trifluoromethoxy, straight-chain or branched alkyl, alkoxy, acyl or alkoxycarbonyl having in each case up to 6 carbon atoms, hydroxyl, carboxyl or by a group of the formula --NR.sup.21 R.sup.22, in which R.sup.3 and R.sup.4 given above,
The 5-hydroxy-alkyl-substituted phenyls according to the invention may also be present in the form of their salts. In general, salts of organic or inorganic bases or acids may be men
REFERENCES:
patent: 5006530 (1991-04-01), Angerbauer et al.
patent: 5169857 (1992-12-01), Angerbauer et al.
patent: 5401746 (1995-03-01), Angerbauer et al.
patent: 5494605 (1996-02-01), Kurihara et al.
patent: 5739166 (1998-04-01), Reitz et al.
J. Org. Chem. (1979), 44(26), 4749-52.
Dinchuk, et al., BBA 1255 (1995) 301-310.
Angerbauer Rolf
Bischoff Hilmar
Brandes Arndt
Bremm Klaus-Dieter
Logers Michael
Bayer Aktiengesellschaft
Lambkin Deborah C.
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