Use of selective potassium channel openers
OwnerJeppe Sturisinventor
Life of this patent
Estimating the term…
Abstract
The present invention relates to a use of SUR1/Kir6.2 selective potassium channel openers for the preparation of a pharmaceutical composition for the prevention or the treatment of diabetes, and for the treatment of hyperinsulinaemia and hyperandrogenism in women with Polycystic Ovary Syndrome (PCOS) as well as a pharmaceutical composition for use in the prevention or the treatment of diabetes, and in the treatment of hyperinsulinaemia and hyperandrogenism in women with Polycystic Ovary Syndrome.
Claims26
A use of SUR1/Kir6.2 selective potassium channel openers for the preparation of a pharmaceutical composition for the treatment or the prevention of diabetes and for the treatment of hyperinsulinemia and hyperandrogenism in women with Polycystic Ovary Syndrome.
A use of a compound of the general formula (I):
- 6
- wherein
- B represents >NR5 or >CR5R6, wherein R5 and R6 independently are hydrogen;
- hydroxy;
- C1-6-alkoxy;
- or C1-6-alkyl, C3-6-cycloalkyl, C2-6-alkenyl or C2-6-alkynyl optionally mono- or poly substituted with halogen;
- or R5 and R4 together represent one of the bonds in a double bond between the atoms 2 and 3 of formula (I);
- D represents —S(═O)2— or —S(═O)—;
- or
- D-B represents —S(═O)(R7)═N—
- wherein R7 is C1-6-alkyl;
- or aryl or heteroaryl optionally mono- or poly substituted with halogen, hydroxy, C1-6-alkoxy, aryloxy, arylalkoxy, nitro, amino, C1-6-monoalkyl- or dialkylamino, cyano, acyl, or C1-6-alkoxycarbonyl;
- R1 is hydrogen;
- hydroxy;
- C1-6-alkoxy;
- or C1-6-alkyl, C3-6-cycloalkyl, C2-6-alkenyl or C2-4-alkynyl optionally mono- or poly substituted with halogen and R4 is hydrogen;
- or R4 together with R5 represent one of the bonds in a double bond between the atoms 2 and 3 of formula (I);
- or R1 together with R4 represent one of the bonds in a double bond between the atoms 3 and 4 of formula (I);
- R2 is hydrogen;
- hydroxy;
- C1-6-alkoxy;
- or C1-6-alkyl, C3-6-cycloalkyl, C2-6-alkenyl or C2-6-alkynyl optionally mono- or poly substituted with halogen;
- R3 is R8;
- —OR8;
- —C(═X)R8;
- —NR8R9;
- bicycloalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl optionally mono- or poly substituted with halogen, hydroxy, C1-6-alkoxy, aryloxy, arylalkoxy, nitro, amino, C1-6-monoalkyl- or dialkylamino, cyano, oxo, acyl or C1-6-alkoxycarbonyl;
- or aryl substituted with C1-6-alkyl;
- wherein R8 is hydrogen;
- C3-6-cycloalkyl or (C3-6-cycloalkyl)C1-6-alkyl, the C3-6-cycloalkyl group optionally being mono- or poly substituted with C1-6-alkyl, halogen, hydroxy or C1-6-alkoxy;
- a 3-6 membered saturated ring system comprising one or more nitrogen, oxygen or sulfur atoms;
- or straight or branched C1-18-alkyl optionally mono- or poly substituted with halogen, hydroxy, C1-6-alkoxy, C1-6-alkylthio, C3-6-cycloalkyl, aryl, aryloxy, arylalkoxy, nitro, amino, C1-6-monoalkyl- or dialkylamino, cyano, oxo, formyl, acyl, carboxy, C1-6-alkoxycarbonyl, or carbamoyl;
- X is O or S;
- R9 is hydrogen;
- C1-6alkyl;
- C2-4-alkenyl;
- C3-6-cycloalkyl optionally mono- or poly substituted with C1-6-alkyl, halogen, hydroxy or C1-6-alkoxy;
- or
- R8 and R9 together with the nitrogen atom form a 3-12 membered mono- or bicyclic system, in which one or more of the carbon atoms may be exchanged with nitrogen, oxygen or sulfur, each of these ring systems optionally being mono- or poly substituted with halogen, C1-6-alkyl, hydroxy, C1-6-alkoxy, C1-6alkoxy-C1-6-alkyl, nitro, amino, cyano, trifluoromethyl, C1-6-monoalkyl- or dialkylamino, oxo;
- or
- R3 is
- 7
- wherein n, m, p independently are 0, 1, 2, 3 and R10 is hydrogen;
- hydroxy;
- C1-6alkoxy;
- C3-6-cycloalkyl optionally mono- or poly substituted with C1-6-alkyl, halogen, hydroxy or C1-6-alkoxy;
- C1-6-alkyl, C2-4-alkenyl or C2-6-alkynyl optionally mono- or poly substituted with halogen;
- or
- R2 and R3 together with the nitrogen atom forms a 3-12 membered mono- or bicyclic system, in which one or more of the carbon atoms may be exchanged with nitrogen, oxygen or sulfur, each of these ring systems optionally being mono- or poly substituted with halogen, C1-6-alkyl, hydroxy, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, nitro, amino, cyano, trifluoromethyl, C1-6-monoalkyl- or dialkylamino or oxo;
- A together with carbon atoms 5 and 6 of formula (I) represents a 5 or 6 membered heterocyclic system comprising one or more nitrogen-, oxygen- or sulfur atoms, the heterocyclic systems optionally being mono- or poly substituted with halogen;
- C1-12-alkyl;
- C3-4-cycloalkyl;
- hydroxy;
- C1-6-alkoxy;
- C1-6-alkoxy-C1-6-alkyl;
- nitro;
- amino;
- cyano;
- cyanomethyl;
- perhalomethyl;
- C1-6-monoalkyl- or dialkylamino;
- sulfamoyl;
- C1-6-alkylthio;
- C1-6-alkylsulfonyl;
- C1-6-alkylsulfinyl;
- C1-6-alkylcarbonylamino;
- arylthio, arylsulfinyl, arylsulfonyl, the aryl group optionally being mono- or polysubstituted with C1-6-alkyl, halogen, hydroxy or C1-6-alkoxy;
- C1-6-alkoxycarbonyl;
- C1-6-alkoxycarbonyl-C1-6-alkyl;
- carbamyl;
- carbamyl-methyl;
- C1-6-monoalkyl- or dialkylaminocarbonyl;
- C1-6-monoalkyl- or dialkylaminothiocarbonyl;
- ureido;
- C1-6-monoalkyl- or dialkylaminocarbonylamino, thioureido;
- C1-6-monoalkyl- or dialkylaminothiocarbonyl-amino;
- C1-6-monoalkyl- or dialkylaminosulfonyl;
- carboxy;
- carboxy-C1-6-alkyl;
- acyl;
- aryl, arylalkyl, aryloxy, the aryl group optionally being mono- or polysubstituted with C1-6-alkyl, halogen, hydroxy or C1-6-alkoxy;
- (1,2,4-oxadiazol-5-yl)- or (1,2,4-oxadiazol-3-yl)-C1-6-alkyl the oxadiazolyl group optionally being substituted with C1-6-alkyl or C3-4-cycloalkyl;
- or a 5-6 membered nitrogen containing ring, optionally substituted with phenyl or C1-6-alkyl;
- or a pharmaceutically acceptable salt thereof, for the preparation of a pharmaceutical composition for the treatment or the prevention of diabetes and for the treatment of hyperinsulinaemia and hyperandrogenism in women with Polycystic Ovary Syndrome.
A pharmaceutical composition for use in the treatment or the prevention of diabetes, and for the treatment of hyperinsulinaemia and hyperandrogenism in women with Polycystic Ovary Syndrome, comprising a compound of the formula (I) or (Ia) or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable acid or base, or any optical isomer or mixture of optical isomers including a racemic mixture, or any tautomeric form together with one or more pharmaceutically acceptable carriers or diluents.
A method for treating or preventing diabetes, and for treating hyperinsulinaemia and hyperandrogenism in women with Polycystic Ovary Syndrome comprising administering an effective amount of a compound of the formula (I) or (Ia) to said subject.
Dependencies are inferred from the claim text.