Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1988-07-14
1991-01-29
Lee, Mary C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
562621, C07C 8310, A61K 31185
Patent
active
049887335
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to certain compounds which are hydroxamic acid aryl derivatives, to processes for their preparation, to pharmaceutical formulations containing them, and to their use in medicine and in other applications.
A class of agents defined in European Pat. No. 55418 are described therein as dual inhibitors of the lipoxygenase and cyclo-oxygenase enzymes of the mammalian arachidonic acid metabolism and were found to exhibit anti-inflammatory and related activities. Other compounds which have been described as lipoxygenase and/or cyclo-oxygenase inhibitors include certain naphthyloxy derivatives, for example, as described in U.S. Pat. No. 3,740,437 or in Proc. Ann. Symp. Inst. Basic Med. Sci., Royal College of Surgeons of England, October 1982, pp. 263-274. Compounds described in the latter reference include the compound known as nafazatrom.
European patent application No. 86301895 describes a class of compounds which are inhibitors of the lipoxygenase and/or cyclo-oxygenase enzymes. We have now found that within the class of compounds described in the European application, there is a sub-class of compounds whose exceptional activity with regard to the inhibition of lipoxygenase and/or cyclo-oxygenase renders them particularly useful for certain medical and non-medical applications.
According to the European application, there is provided a compound of formula (I) also 1;
Ar represents either: substituted by one or more substituents independently selected from C.sub.1-4 alkyl (which may be substituted by one or more halogen atoms), C.sub.1-4 alkoxy, halo, nitro, amino, carboxy, C.sub.1-4 alkoxycarbonyl and hydroxy, or independently selected from phenyl (optionally substituted by one or more substituents independently selected from those specified as optional substituents in (i) above) and those optional substituents specified in (i) above: CH.sub.2 S--, --OCH.sub.2 --, --CONH--, --NHCO--, --CO--, or --CH.sub.2 NH--; substituted by one or more substituents independently selected from those specified as optional substituents in definition (i) of Ar; said carbonyl group from any carbonyl group in Q as defined below; ##STR3## in which one of m and n is 0 and the other is 1, and when n is 1 and m is 0, R.sup.1 and R.sup.2 are independently selected from hydrogen and C.sub.1-4 alkyl, with the possibility that R.sup.2 may also be C.sub.5-7 cycloalkyl, C.sub.1-4 alkyl, groups as defined for Ar above and groups of formula --COR.sup.3 in which R.sup.3 is selected from C.sub.1-4 alkyl (optionally substituted by a carboxy or C.sub.1-4 alkoxycarbonyl group) and groups of formula --N(R.sup.4)R.sup.5 in which R.sup.4 is hydrogen or C.sub.1-4 alkyl and R.sup.5 represents hydrogen, C.sub.1-4 alkyl, or phenyl optionally substituted by one or more substituents independently selected from those specified as optional substituents in definition (i) of Ar, and R.sup.2 is selected from hydrogen, C.sub.1-4 alkyl, amino, C.sub.1-4 alkylamino, di--C.sub.1-4 alkylamino C.sub.5-7 cycloalkylamino, C.sub.5-7 cycloalkyl ( C.sub.1-4 alkyl) amino. anilino, N--C.sub.1-4 alkylanilino and groups as defined for Ar above; and groups of formula ##STR4## in which Z is a C.sub.2-5 alkylene chain in which one of the carbon atoms may be replaced by a hetero atom; subject matter, namely:
______________________________________ EP 0 161 939 A
GB 1 226 344 GB 1 427 114
GB 1 278 739 GB 1 437 783
GB 1 315 830 GB 1 444 492
GB 1 382 996 GB 2 047 234 A
GB 1 396 726
US 3 600 437 US 3 972 934
US 3 821 289 US 3 978 116
US 3 890 377
JP 57035543 JP 57062239
______________________________________
Tetrahedron, 1970, 26 (23), 5653-64,
Eur. J. Med. Chem. Chimica. Therapeutica, 1975, 10 (2), 125-128,
Eur. J. Med. Chem. Chimica. Therapeutica, 1970, 13 (2), 211-13,
J. Chem. Eng. Data, 1985, 30, 237-9,
Chem. Biol. Hydroxamic Acids [Proc. Int. Symp.], 1981, 51-62,
Arzneim. Forsch., 1978, 28 (11), 2087-92.
We have now found that within the class of compounds described in European patent application No. 86301895, there is a sub-cla
REFERENCES:
patent: 4738986 (1988-04-01), Kneen et al.
J. Med. Chem. 1988, p. 3-5, Orally Active Hydroxamic Acid Inhibitors of Leukotriene Biosynthesis, Summers et al.
Jackson William P.
Salmon John A.
Brown Donald
Burroughs Wellcome Co.
Lee Mary C.
Northington-Davis Zinna
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