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US 2006/0069100 A1Published application
Variously substituted derivatives of guanidine, and their use as medicines with anti-diabetes and/or anti-obesity activity
AssigneeSigma-Tau Industrie Farmaceutiche Riunite S.p.A.
InventorsFabio Giannessi, Emanuela Tassoni, Maria Tinti, Pompeo Pessotto, Maurizio Botta, Pederico Corelli
Life of this patent
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Abstract
Formula (I) compounds are described where the groups are as identified in the text, and their use as medicines, particularly as anti-diabetes, serum glucose-lowering and anti-obesity agents. Said medicines are useful for the prophylaxis and treatment of diabetes, particularly type 2 diabetes, and its complications, syndrome X, the various forms of insulin resistance, and hyperlipidaemias, as well as for the treatment of obesity.
Claims14
A compound of the formula:
- in which:
- Z is selected from:
- H;
- saturated or unsaturated, straight or branched alkyl, consisting of from 1 to 7 carbon atoms, optionally substituted with alkoxy and halogens;
- aryl or heteroaryl, mono- or bicyclic, containing one or more heteroatoms selected from nitrogen, oxygen and sulphur, optionally substituted with halogens, NO2, OH, alkyls and alkoxy, optionally substituted with halogens;
- arylalkyl or heteroarylalkyl, where the saturated or unsaturated alkyl residue consists of from 1 to 7 carbon atoms, mono- or bicyclic, containing one or more heteroatoms selected from nitrogen, oxygen and sulphur, optionally substituted with halogens, NO2, OH, carboxy, alkyls and alkoxy, optionally substituted with halogens;
- or, together with W, may form a cycle, optionally containing one or more heteroatoms;
- W is equal to H or, together with Z, may form a cycle, optionally containing one or more heteroatoms;
- n=0-10;
- Q is selected from the Z groups listed above;
- X and Y are the same or different and are selected from the Z groups listed above;
- X may be a substituted amino-imino of the formula:
- where Z1 is selected from the Z groups listed above;
- or X is an R—CO group and, with nitrogen, may form a group:
- where R is selected from the Z groups listed above or —OZ or —NZ;
- when n=0, the X—N—Y group is replaced by an H;
- and their pharmacologically acceptable salts, the racemic mixtures, the single enantiomers, stereoisomers and geometric isomers and tautomers,
- with the proviso that the formula (I) compound is not N-(4-aminobutyl)-N′-(γ,γ-dimethylallyl)guanidine methane sulphonate (ST2369) or N-(γ,γ-dimethylallyl)guanidine methane sulphonate (ST 2527).
15 more elements
(canceled)
-12. (canceled)
Dependencies are inferred from the claim text.