Details for Patent: 5,756,525

Title:	Compounds for treating eating disorders
Abstract:	A method is provided for the treatment and/or prophylaxis of cardiovascular diseases or eating disorders in a human or non-human mammal, which comprises administering to a human or non-human mammal in need thereof, an effective, non-toxic amount of a compound of formula (I): ##STR1## or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof and/or a pharmaceutically acceptable solvate thereof, in which A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group; R.sup.1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond; A.sup.2 represents a benzene ring having in total up to five substituents; and n represents an integer in the range of from 2 to 6.
Inventor(s):	Hindley; Richard Mark (Epsom, GB2), Cawthorne; Michael Antony (Epsom, GB2)
Assignee:	Beecham Group plc (Brentford, GB2)
Filing Date:	Dec 12, 1996
Application Number:	08/764,148
Claims:	1. A method for the treatment and/or prophylaxis of eating disorders by regulating appetite or food intake in a human or non-human mammal in which blood glucose levels are not elevated, in which said disorder is associated with under-eating, which comprises administering to said human or non-human mammal in need thereof, an effective, non-toxic amount of a compound of formula (I): ##STR93## or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof and/or a pharmaceutically acceptable solvate thereof, wherein: A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group; R.sup.1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond; A.sup.2 represents a benzene ring having in total up to five substitutents; and n represents an integer in the range of from 2 to 6. 2. A method according to claim 1, wherein A.sup.1 in the compound of formula (I) represents a substituted or unsubstituted, single or fused ring aromatic heterocyclyl group comprising up to 4 hetero atoms in the ring selected from oxygen, sulphur or nitrogen. 3. A method according to claim 1, wherein A.sup.1 in the compound of formula (I) represents a moiety of formula (a), (b) or (c): ##STR94## wherein: R.sup.4 and R.sup.5 each independently represents a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group or when R.sup.4 and R.sup.5 are each attached to a carbon atom, then R.sup.4 and R.sup.5 together with the carbon atoms to which they are attached form a benzene ring wherein each carbon atom represented by R.sup.4 and R.sup.5 together may be substituted or unsubstituted; and in the moiety of formula (a) X represents oxygen or sulphur. 4. A method according to claim 3, wherein R.sup.4 and R.sup.5 in (a), (b) or (c) each independently represent hydrogen, alkyl or a substituted or unsubstituted phenyl group. 5. A method according to claim 3, wherein R.sup.4 and R.sup.5 in (a), (b) or (c) together represent a moiety of formula (d): ##STR95## wherein R.sup.6 and R.sup.7 each independently represent hydrogen, halogen, substituted or unsubstituted alkyl or alkoxy. 6. A method according to claim 5, wherein R.sup.6 and R.sup.7 in (d) each represent hydrogen. 7. A method according to claim 1, wherein A.sup.2 in the compound of formula (I) represents a moiety of formula (e): ##STR96## wherein R.sup.8 and R.sup.9 each independently represent hydrogen, halogen, substituted or unsubstituted alkyl or alkoxy. 8. A method according to claim 7, wherein R.sup.8 and R.sup.9 in (e) each represent hydrogen. 9. A method according to claim 1, of formula (II): ##STR97## or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof and/or a pharmaceutically acceptable solvate thereof, wherein A.sup.1, R.sup.1, R.sup.2, R.sup.3 and n are as defined in relation to formula (I) in claim 1 and R.sup.8 and R.sup.9 are as defined in relation to formula (e) in claim 7. 10. A method according to claim 1, wherein n in the compound of formula (I) represents an integer 2 or 3. 11. A method according to claim 1, wherein R.sup.1 in the compound of formula (I) represents a methyl group. 12. A method according to claim 1 which comprises the administration of a compound selected from the group consisting of: 5-(4-[2-(N-methyl-N-(2-benzothiazolyl)amino)ethoxy]benzyl)-2,4-thiazolidine dione; 5-(4-[2-(N-methyl-N-(2-benzothiazolyl)amino)ethoxy]benzylidene)-2,4-thiazol idinedione; 5-(4-[2-(N-methyl-N-(2-benzoxazolyl)amino)ethoxy]benzyl)-2,4-thiazolidinedi one; 5-(4-[2-(N-methyl-N-(2-benzoxazolyl)amino)ethoxy]benzylidene)-2,4-thiazolid inedione; 5-(4-[2-(N-methyl-N-(2-pyrimidinyl)amino)ethoxy]benzyl)-2,4-thiazolidinedio ne; 5-(4-[2-(N-methyl-N-(2-pyrimidinyl)amino)ethoxy]benzylidene)-2,4-thiazolidi nedione; 5-(4-(2-(N-methyl-N-[2-(4,5-dimethylthiazolyl)]amino) ethoxy]benzyl)-2,4-thiazolidinedione; 5-(4-[2-(N-methyl-N-[2-(4,5-dimethylthiazolyl)]amino) ethoxy]benzylidene)-2,4-thiazolidinedione; 5-(4-[2-(N-methyl-N-(2-thiazolyl)amino)ethoxy]benzyl)-2,4-thiazolidinedione 5-(4-[2-(N-methyl-N-(2-thiazolyl)amino)ethoxy]benzylidene)-2,4-thiazolidine dione; 5-[4-(2-(N-methyl-N-(2-(4-phenylthiazolyl))amino) ethoxy)benzyl]-2,4-thiazolidinedione; 5-(4-[2-(N-methyl-N-(2-(4-phenylthiazolyl))amino) ethoxy]benzylidene)-2,4-thiazolidinedione; 5-(4-[2-(N-methyl-N-[2-(4-phenyl-5-methylthiazolyl)]amino)ethoxy]benzyl)-2, 4-thiazolidinedione; 5-(4-[2-(N-methyl-N-[2-(4-phenyl-5-methylthiazolyl)]amino)ethoxy]benzyliden e)-2,4-thiazolidinedione; 5-(4-[2-(N-methyl-N-[2-(4-methyl-5-phenylthiazolyl)]amino)ethoxy]benzyl)-2, 4-thiazolidinedione; 5-(4-[2-(N-methyl-N-[2-(4-methyl-5-phenylthiazolyl)]amino)ethoxy]benzyliden e)-2,4-thiazolidinedione; 5-(4-[2-(N-methyl-N-[2-(4-methylthiazolyl)]amino)ethoxy]benzyl)-2,4-thiazol idinedione; 5-(4-[2-(N-methyl-N-[2-(4-methylthiazolyl)]amino) ethoxy]benzylidene)-2,4-thiazolidinedione; 5-[4-(2-(N-methyl-N-[2-(5-phenyloxazolyl)]amino) ethoxy)benzyl]-2,4-thiazolidinedione; 5-(4-[2-(N-methyl-N-[2-(5-phenyloxazolyl)]amino) ethoxy]benzylidene)-2,4-thiazolidinedione; 5-(4-[2-(N-methyl-N-[2-(4,5-dimethyloxazolyl)]amino) ethoxy]benzyl)-2,4-thiazolidinedione; 5-(4-[2-(N-methyl-N-[2-(4,5-dimethyloxazolyl)]amino)ethoxy]benzylidene)-2,4 -thiazolidinedione; 5-[4-(2-(2-pyrimidinylamino)ethoxy)benzyl]-2,4-thiazolidinedione; 5-[4-(2-(2-pyrimidinylamino)ethoxy)benzylidene]-2,4-thiazolidinedione; 5-(4-[2-(N-acetyl-N-(2-pyrimidinyl)amino)ethoxy]benzyl)-2,4-thiazolidinedio ne; 5-(4-(2-(N-(2-benzothiazolyl)-N-benzylamino)ethoxy) benzylidene)-2,4-thiazolidinedione; 5-(4-(2-(N-(2-benzothiazolyl)-N-benzylamino)ethoxy) benzyl)-2,4-thiazolidinedione; 5-(4-[3-(N-methyl-N-(2-benzoxazolyl)amino)propoxy]benzyl)-2,4-thiazolidined ione; 5-(4-[3-(N-methyl-N-(2-benzoxazolyl)amino)propoxy]benzylidene)-2,4-thiazoli dinedione; 5-(4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl)-2,4-thiazolidinedione; 5-(4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzylidene)-2,4-thiazolidinedi one; 5-(4-[4-(N-methyl-N-(2-benzoxazolyl)amino)butoxy]benzylidene)-2,4-thiazolid inedione; 5-(4-[4-(N-methyl-N-(2-benzoxazolyl)amino)butoxy]benzyl)-2,4-thiazolidinedi one; 5-(4-[2-(N-(2-benzoxazolyl)amino)ethoxy]benzylidene)-2,4-thiazolidinedione; 5-(4-[2-(N-(2-benzoxazolyl)amino)ethoxy]benzyl)-2,4-thiazolidinedione; and 5-(4-[2-(N-isopropyl-N-(2-benzoxazolyl)amino)ethoxy]benzyl)-2,4-thiazolidin edione; or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof and/or a pharmaceutically acceptable solvate thereof. 13. A method according to claim 1, wherein the compound is 5-(4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl)-2,4-thiazolidinedione. 14. A method according to claim 12, wherein the compound is 5-(4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl)-2,4-thiazolidinedione.