Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-02-28
1998-06-09
Jarvis, William R.A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514331, 514393, 514535, A61K 31445, A61K 31415, A61K 3124
Patent
active
057634599
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/GB93/01013, filed 05/18/93.
This invention relates to a method of treatment of anxiety in mammals, including humans.
European Journal of Pharmacology 146 (1988), 187-188, and Naunyn-Schmiedeberg's Arch. Pharmacol. (1989) 340:403-410, describe a non classical 5-hydroxytryptamine receptor, now designated the 5-HT4 receptor.
EP-A-501322 (Glaxo Group Limited), WO 93/02677, WO 93/03725, WO 93/05038, WO 93/05040 and PCT/GB93/00506 (SmithKline Beecham plc) describe compounds having 5-HT.sub.4 receptor antagonist activity.
For instance, WO 93/02677 describes compounds of formula (I), or a pharmaceutically acceptable salt thereof ##STR1## wherein the dotted circle represents one or two double bonds in any position in the 5-membered ring; X, Y and Z independently represent oxygen, sulphur, nitrogen or carbon, provided that at least one of X, Y and Z represents oxygen, sulphur or nitrogen; U represents nitrogen or carbon; ##STR2## in which: R.sup.1 represents hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, (C.sub.1-6 alk alkoxy, hydroxy (C.sub.1-6) alkyl, halogen, amino, cyano, --CONR.sup.6 R.sup.7 or --SO.sub.2 NR.sup.6 R.sup.7, in which R.sup.6 and R.sup.7 independently represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; C.sub.1-6 alkylcarbonyl; ##STR3## in which R.sup.8 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; from 1 to 5 carbon atoms and optionally containing an --O--, --S--, --NH-- or --Nalkyl-- linkage; and system having carbon bridgehead(s); or is hydrogen or C.sub.1-6 alkyl and the other is hydrogen, C.sub.1-10 alkyl, C.sub.2-6 alkenyl, C.sub.2-6) alkynyl or aryl(C.sub.1-6)alkyl.
WO 93/05040 describes compounds of formula (IIl), or a pharmaceutically acceptable salt thereof ##STR4## wherein X is of sub-formula (a) or (b): ##STR5## wherein L is N or CR.sub.c wherein R.sub.c is hydrogen, C.sub.1-6 alkoxy, halo, C.sub.1-6 alkyl or cyano; alkoxy; C.sub.2-6 alkanoyl, or C.sub.2-6 alkanoyl C.sub.1-3 alkyl; C.sub.1-6 alkyl group, halo, hydroxy or C.sub.1-6 alkoxy; R.sub.5 is hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, nitro, amino or C.sub.1-6 alkylthio; R.sub.6 is hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino;
WO 93/03725 describes compounds of formula (IV) or a pharmaceutically acceptable salt thereof; ##STR6## wherein L is N or CR.sub.S wherein R.sub.S is hydrogen, C.sub.1-6 alkoxy, halogen, C.sub.1-4 alkyl or cyano; alkoxy; C.sub.2-6 alkanoyl or C.sub.2-6 alkanoyl C.sub.1-3 alkyl; C.sub.1-6 alkyl group, halo, hydroxy or C.sub.1-6 alkoxy; or C.sub.1-6 alkylthio; and ##STR7## wherein n.sup.1 is 0, 1, 2, 3 or4; n.sup.2 is2, 3, 4 or 5;
WO 93/05038 describes compounds of formula (V) and pharmaceutically acceptable salts thereof: ##STR8## in which X.sub.1 --(CH.sub.2).sub.x --X.sub.2 forms a 5-7 membered ring wherein: alkoxy; or C.sub.1-6 alkylthio; ##STR9## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon or nitrogen and aralkyl; and heterocyclic bioisostere.
PCT/GB93/00506 describes compound of formula (VI), or a pharmaceutically acceptable salt thereof ##STR10## wherein X is O, S, SO, SO.sub.2, CH.sub.2, CH or NR wherein R is hydrogen or C.sub.1-6 alkyl; alkoxy; ##STR11## wherein n.sup.1 is 1, 2, 3 or 4; n.sup.2 is 0, 1, 2, 3 or 4; n.sup.3 is2, 3, 4 or 5; (CH.sub.2).sub.z --R.sub.10 wherein R.sub.10 is selected from cyano, hydroxyl, C.sub.1-6 alkoxy, phenoxy, C(O)C.sub.1-6 alkyl, COC.sub.6 H.sub.5, --CONR.sub.11 R.sub.12, NR.sub.11 COR.sub.12 , SO.sub.2 NR.sub.11 R.sub.12 or NR.sub.11 SO.sub.2 R.sub.12 wherein R.sub.11 and R.sub.12 are hydrogen or C.sub.1-6 alkyl; and heterocyclic bioisostere.
Some 5-HT.sub.3 receptor antagonists have been disclosed as of potential use in the treatment of anxiety (see GB 2153821A, EP-A-229444 (Glaxo Group Ltd.) and EP-A-201165 (Beecham Group p.l.c)).
We have now discovered that a compound which acts as an antagonist at 5-HT.sub.4 receptors is of potential use in the treatment of anxiety, such as general anxiety disorder (GAD), mixed anx
Baxter Gordon Smith
Kennett Guy Anthony
Jarvis William R.A.
Kinzig Charles M.
Lentz Edward T.
Simon Soma G.
SmithKline Beecham p.l.c.
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