Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof

A compound according to Formulas I, II, III, or IV:

• wherein
• A is
• X is O or S;
• X1 to X4 are each, independently, N, CH, CR1, or C—, wherein C— represents the point of attachment of group A to the remainder of the structure of formulas (I), (II), (III) or (IV);
• R′ is H, alkyl having 1 to 4 carbon atoms, halogenated alkyl having 1 to 4 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, or cycloalkylalkyl having 4 to 7 carbon atoms;
• R1 is H, F, Cl, Br, I, OH, CN, nitro, NH2, COH, NR6R7, carboxy, CONR6R7, NR2COR8, NR2COOR8, NR2CSR8, NR2CONR2R9, NR2CSNR2R9, NR2SO2R10, NR2CONR6R7, NR2CSNR6R7, NR2R9, SO2R10, SOR10, —O—(C1-6-alkyl-O)1-2—C1-6-alkyl, NR2—C1-6-alkyl-NR6R7, NR2—C1-6-alkyl-CONR6R7, NR2—CO—C1-6-alkyl-Ar, NR2—C1-6-alkyl-CO—O—R2, NR2—C1-6-alkyl-NR2(CO—O—R2), —C1-6-alkyl-NR2, —O—C1-6-alkyl-NR6R7, alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 2 to 6 carbon atoms, alkynyl having 2 to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms which is unsubstituted or substituted by HCO—, C1-6-alkoxy, NR6R7, CO—NR6R7, C2-6-alkoxycarbonyl, —CO—R10, or combinations thereof, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, alkoxy having 1 to 4 carbon atoms, cycloalkoxy having 3 to 7 carbon atoms, cycloalkylalkoxy having 4 to 7 carbon atoms, alkylthio having 1 to 4 carbon atoms, fluorinated alkoxy having 1 to 4 carbon atoms, hydroxyalkyl having 1 to 4 carbon atoms, fluorinated hydroxyalkyl having 1 to 4 carbon atoms, hydroxyalkoxy having 2 to 4 carbon atoms, fluorinated hydroxyalkoxy having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, alkoxycarbonyl having 2 to 6 carbon atoms, Ar, Het, OAr, OHet, Carbo-O, Ar—C1-6-alkyl-O—, Het-C1-6-alkyl-O—, Het-CO-Het-, Het-C1-6-alkyl-NR2—, or Ar—C1-6-alkyl-Het-O—;
• or
• R1 is of one of the following formulas
• two R1 can together form a 5-membered fused ring structure containing at least one N atom;
• R2 is alkyl having 2 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, fluorinated C1-4-alkyl-CO—, C3-7-cycloalkyl-CO—, C1-4-alkyl-NH—CO—, C3-7-cycloalkyl-NH—CO—, Het, Ar—C1-4-alkyl-, Ar—C1-4-alkyl CO—, Ar—C1-4-alkyl SO2—, C1-4-alkyl-O—C1-4 alkyl-, or Ar—C1-4-alkyl-NH—CO—;
• R6 and R7 are each, independently, H, alkyl having 1 to 4 carbon atoms, alkoxyalkyl having 2 to 8 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, or cycloalkylalkyl having 4 to 7 carbon atoms, or R6 and R7 together are an alkylene group containing 4-6 carbon atoms which forms a ring with the N atom;
• R8 is H, alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3 to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 1 to 4 carbon atoms, fluorinated hydroxyalkyl having 1 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, Ar, or Het;
• R9 is alkyl having 1 to 4 carbon atoms, Ar, Ar-alkyl wherein the alkyl portion has 1 to 4 carbon atoms, or Het;
• R10 is alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3 to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 2 to 4 carbon atoms, fluorinated hydroxyalkyl having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, NR6R7, NR2R8, Ar, or Het;
• Ar is an aryl group having 6 to 10 carbon atoms which is unsubstituted or substituted one or more times by alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, halogen, dialkylamino wherein the alkyl portions each have 1 to 8 C atoms, amino, cyano, hydroxyl, nitro, halogenated alkyl having 1 to 8 C atoms, halogenated alkoxy having 1 to 8 C atoms, hydroxyalkyl having 1 to 8 C atoms, hydroxyalkoxy having 2 to 8 C atoms, alkenyloxy having 3 to 8 C atoms, alkylthio having 1 to 8 C atoms, alkylsulphinyl having 1 to 8 C atoms, alkylsulphonyl having 1 to 8 C atoms, monoalkylamino having 1 to 8 C atoms, cycloalkylamino wherein the cycloalkyl group has 3 to 7 C atoms and is optionally substituted by alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, hydroxyl, amino, monoalkylamino having 1 to 4 carbon atoms, dialklyamino in which each alkyl group has 1 to 4 carbon atoms, or combinations thereof, aryloxy wherein the aryl portion has 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, arylthio wherein the aryl portion has 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, cycloalkyloxy wherein the cycloalkyl group has 3 to 7 C atoms and is optionally substituted by alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, hydroxyl, amino, monoalkylamino having 1 to 4 carbon atoms, dialklyamino in which each alkyl group has 1 to 4 carbon atoms, or combinations thereof, sulfo, sulfonylamino, acylamido, acyloxy or combinations thereof;
• Het is a heterocyclic group, which is fully saturated, partially saturated or fully unsaturated, having 5 to 10 ring atoms in which at least 1 ring atom is a N, O or S atom, which is unsubstituted or substituted one or more times by halogen, aryl having 6 to 10 carbon atoms which is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, cycloalkyl having 3 to 7 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, halogenated alkoxy having 1 to 8 C atoms, cycloalkoxy having 3 to 7 carbon atoms, cycloalkylalkoxy having 4 to 7 carbon atoms, alkoxyalkyl having 2 to 8 carbon atoms, alkyl(halogenated alkyl)amino wherein each alkyl group has 1 to 8 C atoms, di(halogenated alkyl)amino wherein each alkyl group has 1 to 8 C atoms, (halogenated alkyl)amino having 1 to 8 C atoms, cyano, halogenated alkyl having 1 to 8 carbon atoms, nitro, oxo, OH, alkoxycarbonylalkyl having 3 to 8 carbon atoms, amino, monoalkylamino having 1 to 8 C atoms, dialkylamino wherein each alkyl group has 1 to 8 C atoms, SO2R11, —CXR11, piperidinylethyl or combinations thereof;
• Carbo is a partially unsaturated carbocyclic group having 5 to 14 carbon atoms, which is unsubstituted or substituted one or more times by halogen, alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, hydroxy, nitro, cyano, oxo, or combinations thereof;
• and
• R11 is alkyl having 1 to 4 carbon atoms, halogenated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3 to 6 carbon atoms, wherein the alkyl, halogenated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 2 to 4 carbon atoms, fluorinated hydroxyalkyl having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, or Ar;
• and pharmaceutically acceptable salts or solvates or N-oxides thereof, or solvates of pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts or solvates of N-oxides thereof,
• wherein said compound can also be in the form of a polymorph,
• wherein if said compound exhibits chirality it can be in the form of a mixture of enantiomers or a mixture of diastereomers, or can be in the form of a single enantiomer or a single diastereomer, and
• with the proviso that:
• A has at least one R1 substituent that is Het other than thiazolyl.

A compound according to Formulas I, II, III, or IV:

• wherein
• A is
• X is O or S;
• X1 to X4 are each, independently, N, CH, CR1, or C—, wherein C— represents the point of attachment of group A to the remainder of the structure of formulas (I), (II), (III) or (IV);
• R′ is H, alkyl having 1 to 4 carbon atoms, halogenated alkyl having 1 to 4 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, or cycloalkylalkyl having 4 to 7 carbon atoms;
• R1 is H, F, Cl, Br, I, OH, CN, nitro, NH2, COH, NR6R7, carboxy, CONR6R7, NR2COR8, NR2COOR8, NR2CSR8, NR2CONR2R9, NR2CSNR2R9, NR2SO2R10, NR2CONR6R7, NR2CSNR6R7, NR2R9, SO2R10, SOR10, —O—(C1-6-alkyl-O)1-2—C1-6-alkyl, NR2—C1-6-alkyl-NR6R7, NR2—C1-6-alkyl-CONR6R7, NR2—CO—C1-6-alkyl-Ar, NR2—C1-6alkyl-CO——R2, NR2—C1-6-alkyl-NR2(CO—O—R2), —C1-6-alkyl-NR2, —O—C1-6-alkyl-NR6R7, alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 2 to 6 carbon atoms, alkynyl having 2 to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms which is unsubstituted or substituted by HCO—, C1-6-alkoxy, NR6R7, CO—NR6R7, C2-6-alkoxycarbonyl, —CO—R10, or combinations thereof, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, alkoxy having 1 to 4 carbon atoms, cycloalkoxy having 3 to 7 carbon atoms, cycloalkylalkoxy having 4 to 7 carbon atoms, alkylthio having 1 to 4 carbon atoms, fluorinated alkoxy having 1 to 4 carbon atoms, hydroxyalkyl having 1 to 4 carbon atoms, fluorinated hydroxyalkyl having 1 to 4 carbon atoms, hydroxyalkoxy having 2 to 4 carbon atoms, fluorinated hydroxyalkoxy having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, alkoxycarbonyl having 2 to 6 carbon atoms, Ar, Het, OAr, OHet, Carbo-O, Ar—C1-6-alkyl-O—, Het-C1-6-alkyl-O—, Het-CO-Het-, Het-C1-6-alkyl-NR2—, or Ar—Ci 6-alkyl-Het-O—;
• or
• R1 is of one of the following formulas
• two R1 can together form a 5-membered fused ring structure containing at least one N atom;
• R2 is H, alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, fluorinated C1-4-alkyl-CO—, C3-7-cycloalkyl-CO—, C1-4-alkyl-NH—CO —, C3-7-cycloalkyl-NH—CO—, Het, Ar—C1-4-alkyl-, Ar—C1-4-alkyl-CO—, Ar—C1-4-alkyl-SO2—, C1-4-alkyl-O—C1-4-alkyl-, Ar—C1-4-alkyl-NH—CO—, or Het-NH—CO—;
• R6 and R7 are each, independently, H, alkyl having 1 to 4 carbon atoms, alkoxyalkyl having 2 to 8 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, or cycloalkylalkyl having 4 to 7 carbon atoms, or R6 and R7 together are an alkylene group containing 4-6 carbon atoms which forms a ring with the N atom;
• R8 is H, alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3 to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 1 to 4 carbon atoms, fluorinated hydroxyalkyl having 1 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, Ar, or Het;
• R9 is alkyl having 1 to 4 carbon atoms, Ar, Ar-alkyl wherein the alkyl portion has 1 to 4 carbon atoms, or Het;
• R1° is alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3 to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 2 to 4 carbon atoms, fluorinated hydroxyalkyl having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, NR6R7, NR2R8, Ar, or Het;
• Ar is an aryl group having 6 to 10 carbon atoms which is unsubstituted or substituted one or more times by alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, halogen, dialkylamino wherein the alkyl portions each have 1 to 8 C atoms, amino, cyano, hydroxyl, nitro, halogenated alkyl having 1 to 8 C atoms, halogenated alkoxy having 1 to 8 C atoms, hydroxyalkyl having 1 to 8 C atoms, hydroxyalkoxy having 2 to 8 C atoms, alkenyloxy having 3 to 8 C atoms, alkylthio having 1 to 8 C atoms, alkylsulphinyl having 1 to 8 C atoms, alkylsulphonyl having 1 to 8 C atoms, monoalkylamino having 1 to 8 C atoms, cycloalkylamino wherein the cycloalkyl group has 3 to 7 C atoms and is optionally substituted by alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, hydroxyl, amino, monoalkylamino having 1 to 4 carbon atoms, dialklyamino in which each alkyl group has 1 to 4 carbon atoms, or combinations thereof, aryloxy wherein the aryl portion has 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, arylthio wherein the aryl portion has 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, cycloalkyloxy wherein the cycloalkyl group has 3 to 7 C atoms and is optionally substituted by alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, hydroxyl, amino, monoalkylamino having 1 to 4 carbon atoms, dialklyamino in which each alkyl group has 1 to 4 carbon atoms, or combinations thereof, sulfo, sulfonylamino, acylamido, acyloxy or combinations thereof;
• Het is a heterocyclic group, which is fully saturated, partially saturated or fully unsaturated, having 5 to 10 ring atoms in which at least 1 ring atom is a N, O or S atom, which is unsubstituted or substituted one or more times by halogen, aryl having 6 to 10 carbon atoms which is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, cycloalkyl having 3 to 7 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, halogenated alkoxy having 1 to 8 C atoms, cycloalkoxy having 3 to 7 carbon atoms, cycloalkylalkoxy having 4 to 7 carbon atoms, alkoxyalkyl having 2 to 8 carbon atoms, alkyl(halogenated alkyl)amino wherein each alkyl group has 1 to 8 C atoms, di(halogenated alkyl)amino wherein each alkyl group has 1 to 8 C atoms, (halogenated alkyl)amino having 1 to 8 C atoms, cyano, halogenated alkyl having 1 to 8 carbon atoms, nitro, oxo, OH, alkoxycarbonylalkyl having 3 to 8 carbon atoms, amino, monoalkylamino having 1 to 8 C atoms, dialkylamino wherein each alkyl group has 1 to 8 C atoms, SO2R11, —CXR11, piperidinylethyl or combinations thereof;
• Carbo is a partially unsaturated carbocyclic group having 5 to 14 carbon atoms, which is unsubstituted or substituted one or more times by halogen, alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, hydroxy, nitro, cyano, oxo, or combinations thereof;
• and
• R11 is alkyl having 1 to 4 carbon atoms, halogenated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3 to 6 carbon atoms, wherein the alkyl, halogenated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 2 to 4 carbon atoms, fluorinated hydroxyalkyl having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, or Ar;
• and pharmaceutically acceptable salts or solvates or N-oxides thereof, or solvates of pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts or solvates of N-oxides thereof,
• wherein said compound can also be in the form of a polymorph,
• wherein if said compound exhibits chirality it can be in the form of a mixture of enantiomers or a mixture of diastereomers, or can be in the form of a single enantiomer or a single diastereomer, and
• wherein said compound possess at least one Het group which is fully saturated, partially saturated or fully unsaturated, having 5 to 10 ring atoms in which at least 1 ring atom is a N, O or S atom, and which is substituted, wherein at least one of the substituents is halogenated alkoxy having 1 to 8 C atoms, cycloalkoxy having 3 to 7 carbon atoms, cycloalkylalkoxy having 4 to 7 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, halogenated alkyl having 2 to 8 carbon atoms, alkoxyalkyl having 2 to 8 carbon atoms, alkyl(halogenated alkyl)amino wherein each alkyl group has 1 to 8 C atoms, di(halogenated alkyl)amino wherein each alkyl group has 1 to 8 C atoms, or (halogenated alkyl)amino having 1 to 8 C atoms.

A compound according to Formulas I, II, III, or IV:

• wherein
• A is
• X is O or S;
• X1 to X4 are each, independently, N, CH, CR1, or C—, wherein C— represents the point of attachment of group A to the remainder of the structure of formulas (I), (II), (III) or (IV);
• R′ is H, alkyl having 1 to 4 carbon atoms, halogenated alkyl having 1 to 4 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, or cycloalkylalkyl having 4 to 7 carbon atoms;
• R1 is H, F, Cl, Br, I, OH, CN, nitro, NH2, COH, NR6R7, carboxy, CONR6R7, NR2COR8, NR2COOR8, NR2CSR8, NR2CONR2R9, NR2CSNR2R9, NR2SO2R10, NR2CONR6R7, NR2CSNR6R7, NR2R9, SO2R10, SOR10, —O—(C1-6-alkyl-O)1-2—C1-6-alkyl, NR2—C1-6-alkyl-NR6R7, NR2—C1-6-alkyl-CONR6R7, NR2—CO—C1-6-alkyl-Ar, NR2—C1-6-alkyl-CO—O—R2, NR2—C1-6-alkyl-NR2(CO—O—R2), —C1-6-alkyl-NR2, —O—C1-6-alkyl-NR6R7, alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 2 to 6 carbon atoms, alkynyl having 2 to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms which is unsubstituted or substituted by HCO—, C1-6-alkoxy, NR6R7, CO—NR6R7, C2-6-alkoxycarbonyl, —CO—R10, or combinations thereof, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, alkoxy having 1 to 4 carbon atoms, cycloalkoxy having 3 to 7 carbon atoms, cycloalkylalkoxy having 4 to 7 carbon atoms, alkylthio having 1 to 4 carbon atoms, fluorinated alkoxy having 1 to 4 carbon atoms, hydroxyalkyl having 1 to 4 carbon atoms, fluorinated hydroxyalkyl having 1 to 4 carbon atoms, hydroxyalkoxy having 2 to 4 carbon atoms, fluorinated hydroxyalkoxy having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, alkoxycarbonyl having 2 to 6 carbon atoms, Ar, Het, OAr, OHet, Carbo-O, Ar—C1-6-alkyl-O—, Het-C1-6-alkyl-O—, Het-CO-Het-, Het-C1-6-alkyl-NR2—, or Ar—C1-6-alkyl-Het-O—;
• or
• R1 is of one of the following formulas
• two R1 can together form a 5-membered fused ring structure containing at least one N atom;
• R2 is H, alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, fluorinated C1-4-alkyl-CO—, C3-7-cycloalkyl-CO—, C1-4-alkyl-NH—CO—, C3-7-cycloalkyl-NH—CO—, Het, Ar—C1-4-alkyl-, Ar—C1-4-alkyl—CO—, Ar—C1-4-alkyl-SO2—, C1-4-alkyl-O—C1-4-alkyl-, Ar—C1-4-alkyl-NH—CO—, or Het-NH—CO—;
• R6 and R7 are each, independently, H, alkyl having 1 to 4 carbon atoms, alkoxyalkyl having 2 to 8 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, or cycloalkylalkyl having 4 to 7 carbon atoms, or R6 and R7 together are an alkylene group containing 4-6 carbon atoms which forms a ring with the N atom;
• R8 is H, alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 1 to 4 carbon atoms, fluorinated hydroxyalkyl having 1 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, Ar, or Het;
• R9 is alkyl having 1 to 4 carbon atoms, Ar, Ar-alkyl wherein the alkyl portion has 1 to 4 carbon atoms, or Het;
• R10 is alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3 to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 2 to 4 carbon atoms, fluorinated hydroxyalkyl having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, NR6R7, NR2R8, Ar, or Het;
• Ar is an aryl group having 6 to 10 carbon atoms which is unsubstituted or substituted one or more times by alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, halogen, dialkylamino wherein the alkyl portions each have 1 to 8 C atoms, amino, cyano, hydroxyl, nitro, halogenated alkyl having 1 to 8 C atoms, halogenated alkoxy having 1 to 8 C atoms, hydroxyalkyl having 1 to 8 C atoms, hydroxyalkoxy having 2 to 8 C atoms, alkenyloxy having 3 to 8 C atoms, alkylthio having 1 to 8 C atoms, alkylsulphinyl having 1 to 8 C atoms, alkylsulphonyl having 1 to 8 C atoms, monoalkylamino having 1 to 8 C atoms, cycloalkylamino wherein the cycloalkyl group has 3 to 7 C atoms and is optionally substituted by alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, hydroxyl, amino, monoalkylamino having 1 to 4 carbon atoms, dialklyamino in which each alkyl group has 1 to 4 carbon atoms, or combinations thereof, aryloxy wherein the aryl portion has 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, arylthio wherein the aryl portion has 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, cycloalkyloxy wherein the cycloalkyl group has 3 to 7 C atoms and is optionally substituted by alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, hydroxyl, amino, monoalkylamino having 1 to 4 carbon atoms, dialklyamino in which each alkyl group has 1 to 4 carbon atoms, or combinations thereof, sulfo, sulfonylamino, acylamido, acyloxy or combinations thereof;
• Het is a heterocyclic group, which is fully saturated, partially saturated or fully unsaturated, having 5 to 10 ring atoms in which at least 1 ring atom is a N, O or S atom, which is unsubstituted or substituted one or more times by halogen, aryl having 6 to 10 carbon atoms which is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, cycloalkyl having 3 to 7 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, halogenated alkoxy having 1 to 8 C atoms, cycloalkoxy having 3 to 7 carbon atoms, cycloalkylalkoxy having 4 to 7 carbon atoms, alkoxyalkyl having 2 to 8 carbon atoms, alkyl(halogenated alkyl)amino wherein each alkyl group has 1 to 8 C atoms, di(halogenated alkyl)amino wherein each alkyl group has 1 to 8 C atoms, (halogenated alkyl)amino having 1 to 8 C atoms, cyano, halogenated alkyl having 1 to 8 carbon atoms, nitro, oxo, OH, alkoxycarbonylalkyl having 3 to 8 carbon atoms, amino, monoalkylamino having 1 to 8 C atoms, dialkylamino wherein each alkyl group has 1 to 8 C atoms, SO2R11, —CXR11, piperidinylethyl or combinations thereof;
• Carbo is a partially unsaturated carbocyclic group having 5 to 14 carbon atoms, which is unsubstituted or substituted one or more times by halogen, alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, hydroxy, nitro, cyano, oxo, or combinations thereof;
• and
• R11 is alkyl having 1 to 4 carbon atoms, halogenated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3 to 6 carbon atoms, wherein the alkyl, halogenated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 2 to 4 carbon atoms, fluorinated hydroxyalkyl having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, or Ar;
• and pharmaceutically acceptable salts or solvates or N-oxides thereof, or solvates of pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts or solvates of N-oxides thereof,
• wherein said compound can also be in the form of a polymorph,
• wherein if said compound exhibits chirality it can be in the form of a mixture of enantiomers or a mixture of diastereomers, or can be in the form of a single enantiomer or a single diastereomer, and
• wherein at least one of X1, X2, X3, and X4 is N.

A compound according to Formulas I, II, III, or IV:

• wherein
• A is
• X is O or S;
• X1 to X4 are each, independently, N, CH, CR1, or C—, wherein C— represents the point of attachment of group A to the remainder of the structure of formulas (I), (II), (III) or (IV);
• R′ is H, alkyl having 1 to 4 carbon atoms, halogenated alkyl having 1 to 4 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, or cycloalkylalkyl having 4 to 7 carbon atoms;
• R1 is H, F, Cl, Br, I, OH, CN, nitro, NH2, COH, NR6R7, carboxy, CONR6R7, NR2COR8, NR2COOR8, NR2CSR8, NR2CONR2R9, NR2CSNR2R9, NR2SO2R10, NR2CONR6R7, NR2CSNR6R7, NR2R9, SO2R10, SOR10, —O—(C1-6alkyl-O)1-2—C1-6-alkyl, NR2—C1-6-alkyl-NR6R7, NR2—C1-6-alkyl-CONR6R7, NR2—CO—C1-6-alkyl-Ar, NR2—C1-6-alkyl-CO—O—R2, NR2—C1-6-alkyl-NR2(CO—O—R2), —C1-6-alkyl-NR2, —O—C1-6-alkyl-NR6R7, alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 2 to 6 carbon atoms, alkynyl having 2 to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms which is unsubstituted or substituted by HCO—, C1-6-alkoxy, NR6R7, CO—NR6R7, C2-6-alkoxycarbonyl, —CO—R10, or combinations thereof, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, alkoxy having 1 to 4 carbon atoms, cycloalkoxy having 3 to 7 carbon atoms, cycloalkylalkoxy having 4 to 7 carbon atoms, alkylthio having 1 to 4 carbon atoms, fluorinated alkoxy having 1 to 4 carbon atoms, hydroxyalkyl having 1 to 4 carbon atoms, fluorinated hydroxyalkyl having 1 to 4 carbon atoms, hydroxyalkoxy having 2 to 4 carbon atoms, fluorinated hydroxyalkoxy having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, alkoxycarbonyl having 2 to 6 carbon atoms, Ar, Het, OAr, OHet, Carbo-O, Ar—C1-6-alkyl-O—, Het-C1-6-alkyl-O—, Het-CO-Het-, Het-C1-6-alkyl-NR2—, or Ar—C1-6-alkyl-Het-O—;
• or
• R1 is of one of the following formulas
• two R1 can together form a 5-membered fused ring structure containing at least one N atom;
• R2 is H, alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, fluorinated C1-4-alkyl-CO—, C3-7-cycloalkyl-CO—, C1-4-alkyl-NH—CO—, C3-7-cycloalkyl-NH—CO—, Het, Ar—C1-4-alkyl-, Ar—C1-4-alkyl-CO—, Ar—C1-4-alkyl-SO2—, C1-4-alkyl-O—C1-4-alkyl-, Ar—C1-4-alkyl-NH—CO—, or Het-NH—CO—;
• R6 and R7 are each, independently, H, alkyl having 1 to 4 carbon atoms, alkoxyalkyl having 2 to 8 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, or cycloalkylalkyl having 4 to 7 carbon atoms, or R6 and R7 together are an alkylene group containing 4-6 carbon atoms which forms a ring with the N atom;
• R8 is H, alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3 to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 1 to 4 carbon atoms, fluorinated hydroxyalkyl having 1 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, Ar, or Het;
• R9 is alkyl having 1 to 4 carbon atoms, Ar, Ar-alkyl wherein the alkyl portion has 1 to 4 carbon atoms, or Het;
• R10 is alkyl having 1 to 4 carbon atoms, fluorinated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3 to 6 carbon atoms, wherein the alkyl, fluorinated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 2 to 4 carbon atoms, fluorinated hydroxyalkyl having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, NR6R7, NR2R8, Ar, or Het;
• Ar is an aryl group having 6 to 10 carbon atoms which is unsubstituted or substituted one or more times by alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, halogen, dialkylamino wherein the alkyl portions each have 1 to 8 C atoms, amino, cyano, hydroxyl, nitro, halogenated alkyl having 1 to 8 C atoms, halogenated alkoxy having 1 to 8 C atoms, hydroxyalkyl having 1 to 8 C atoms, hydroxyalkoxy having 2 to 8 C atoms, alkenyloxy having 3 to 8 C atoms, alkylthio having 1 to 8 C atoms, alkylsulphinyl having 1 to 8 C atoms, alkylsulphonyl having 1 to 8 C atoms, monoalkylamino having 1 to 8 C atoms, cycloalkylamino wherein the cycloalkyl group has 3 to 7 C atoms and is optionally substituted by alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, hydroxyl, amino, monoalkylamino having 1 to 4 carbon atoms, dialklyamino in which each alkyl group has 1 to 4 carbon atoms, or combinations thereof, aryloxy wherein the aryl portion has 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, arylthio wherein the aryl portion has 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, cycloalkyloxy wherein the cycloalkyl group has 3 to 7 C atoms and is optionally substituted by alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, hydroxyl, amino, monoalkylamino having 1 to 4 carbon atoms, dialklyamino in which each alkyl group has 1 to 4 carbon atoms, or combinations thereof, sulfo, sulfonylamino, acylamido, acyloxy or combinations thereof;
• Het is a heterocyclic group, which is fully saturated, partially saturated or fully unsaturated, having 5 to 10 ring atoms in which at least 1 ring atom is a N, O or S atom, which is unsubstituted or substituted one or more times by halogen, aryl having 6 to 10 carbon atoms which is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, hydroxy, alkoxy having 1 to 8 carbon atoms, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino having 1 to 8 carbon atoms, dialkylamino in which each alkyl group has 1 to 8 carbon atoms, hydroxyalkyl having 1 to 8 carbon atoms, hydroxyalkoxy having 1 to 8 carbon atoms, carboxy, cyano, acyl, alkoxycarbonyl wherein the alkoxy group has 1 to 8 carbon atoms, alkylthio, alkylsulphinyl having 1 to 8 carbon atoms, alkylsulphonyl having 1 to 8 carbon atoms, phenoxy, acyloxy, or combinations thereof, alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, cycloalkyl having 3 to 7 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, halogenated alkoxy having 1 to 8 C atoms, cycloalkoxy having 3 to 7 carbon atoms, cycloalkylalkoxy having 4 to 7 carbon atoms, alkoxyalkyl having 2 to 8 carbon atoms, alkyl(halogenated alkyl)amino wherein each alkyl group has 1 to 8 C atoms, di(halogenated alkyl)amino wherein each alkyl group has 1 to 8 C atoms, (halogenated alkyl)amino having 1 to 8 C atoms, cyano, halogenated alkyl having 1 to 8 carbon atoms, nitro, oxo, OH, alkoxycarbonylalkyl having 3 to 8 carbon atoms, amino, monoalkylamino having 1 to 8 C atoms, dialkylamino wherein each alkyl group has 1 to 8 C atoms, SO2R11, —CXR11, piperidinylethyl or combinations thereof;
• Carbo is a partially unsaturated carbocyclic group having 5 to 14 carbon atoms, which is unsubstituted or substituted one or more times by halogen, alkyl having 1 to 8 C atoms, alkoxy having 1 to 8 C atoms, hydroxy, nitro, cyano, oxo, or combinations thereof;
• and
• R11 is alkyl having 1 to 4 carbon atoms, halogenated alkyl having 1 to 4 carbon atoms, alkenyl having 3 to 6 carbon atoms, alkynyl having 3 to 6 carbon atoms, wherein the alkyl, halogenated alkyl, alkenyl, or alkynyl groups are in each case unsubstituted or substituted by Ar or Het, cycloalkyl having 3 to 7 carbon atoms, cycloalkenyl having 5 to 8 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 6 to 9 carbon atoms, hydroxyalkyl having 2 to 4 carbon atoms, fluorinated hydroxyalkyl having 2 to 4 carbon atoms, monoalkylamino having 1 to 4 carbon atoms, dialkylamino wherein each alkyl group independently has 1 to 4 carbon atoms, or Ar;
• and pharmaceutically acceptable salts, including quaternary ammonium salts, or solvates or N-oxides thereof, or solvates of pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts or solvates of N-oxides thereof,
• wherein said compound can also be in the form of a polymorph, and
• wherein if said compound exhibits chirality it can be in the form of a mixture of enantiomers or a mixture of diastereomers, or can be in the form of a single enantiomer or a single diastereomer;
• with the proviso that the 1-azabicyclo group is in the form of a quaternary ammonium salt of the subformula:
• wherein Z is alkyl having 1 to 4 carbon atoms, halogenated alkyl having 1 to 4 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, or arylalkyl having 7 to 16 carbon atoms, and anion A is iodide, bromide, chloride, triflate, tosylate, or mesylate.

A compound selected from:

• 3) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-5,6-dimethoxy-1H-indazole-3-carboxamide hydroformate,
• 4) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-propyl-6-(1,3-thiazol-2-yl)-1H-indazole-3-carboxamide,
• 5) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-isopropyl-6-(1,3-thiazol-2-yl)-1H-indazole-3-carboxamide,
• 6) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(tetrahydrofuran-3-yloxy)-1H-indazole-3-carboxamide hydroformate,
• 7) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(tetrahydro-2H-pyran-4-yloxy)-1H-indazole-3-carboxamide hydroformate,
• 8) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-[(1-methylpyrrolidin-3-yl)oxy]-1H-indazole-3-carboxamide hydroformate,
• 9) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-4-hydroxy-1H-indazole-3-carboxamide hydroformate,
• 10) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-5-bromo-4-hydroxy-1H-indazole-3-carboxamide hydroformate,
• 11) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-5,7-dibromo-4-hydroxy-1H-indazole-3-carboxamide hydroformate,
• 15) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-ethyl-6-(2-oxopyrrolidin-1-yl)-1H-indazole-3-carboxamide hydroformate,
• 16) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-7-hydroxy-1H-indazole-3-carboxamide hydroformate,
• 17) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-6-methoxy-N-methyl-1H-indazole-3-carboxamide hydroformate,
• 18) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-methyl-6-{[(propylamino)carbonyl]amino}-1H-indazole-3-carboxamide hydroformate,
• 19) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-ethyl-6-methoxy-1H-indazole-3-carboxamide,
• 20) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-1-ethyl-6-methoxy-1H-indazole-3-carboxamide,
• 21) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-(difluoromethyl)-6-methoxy-1H-indazole-3-carboxamide,
• 22) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-(difluoromethyl)-6-(1,3-thiazol-2-yl)-1H-indazole-3-carboxamide,
• 23) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-[(cyclopropylcarbonyl)amino]-1-methyl-1H-indazole-3-carboxamide hydroformate,
• 24) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-[(cyclopropylcarbonyl)amino]-1-(difluoromethyl)-1H-indazole-3-carboxamide hydroformate,
• 25) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-(difluoromethyl)-6-{[(propylamino)carbonyl]amino}-1H-indazole-3-carboxamide hydroformate,
• 26) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-cyclopropyl-6-(1,3-thiazol-2yl)-1H-indazole-3-carboxamide,
• 27) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(1,3-thiazol-2-yl)-1-(3-thienyl)-1H-indazole-3-carboxamide,
• 28) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-N-methyl-6-(1,3-oxazol-2-yl)-1H-indazole-3-carboxamide,
• 29) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-N-methyl-6-(1,3-thiazol-2-yl)-1H-indazole-3-carboxamide,
• 30) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-ethyl-6-(1,3-oxazol-2-yl)-1H-indazole-3-carboxamide,
• 31) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-(cyclopropylmethyl)-6-(1,3-oxazol-2-yl)-1H-indazole-3-carboxamide,
• 32) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(1,3-oxazol-2-yl)-1-propyl-1H-indazole-3-carboxamide,
• 33) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-ethyl-N-methyl-6-(1,3-oxazol-2-yl)-1H-indazole-3-carboxamide,
• 34) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-N-methyl-6-(tetrahydro-2H-pyran-4-yl)-1H-indazole-3-carboxamide,
• 35) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-N-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-indazole-3-carboxamide,
• 36) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-5-(difluoromethoxy)-N-methyl-1H-indazole-3-carboxamide,
• 37) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(difluoromethoxy)-N-methyl-1H-indazole-3-carboxamide,
• 38) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-cyclopropyl-6-[(cyclopropylcarbonyl)amino]-1H-indazole-3-carboxamide,
• 39) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-cyclopropyl-6-{[(propylamino)carbonyl]amino}-1H-indazole-3-carboxamide,
• 40) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-5-methoxy-N-methyl-1H-indazole-3-carboxamide,
• 41) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-[(4S)-4-hydroxy-2-oxopyrrolidin-1-yl]-1H-indazole-3-carboxamide hydroformate,
• 42) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-5-methoxy-N-methyl-1H-indazole-3-carboxamide hydroformate,
• 43) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-5-(difluoromethoxy)-N-methyl-1H-indazole-3-carboxamide hydroformate,
• 44) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(difluoromethoxy)-N-methyl-1H-indazole-3-carboxamide hydroformate,
• 45) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-N-methyl-6-(tetrahydro-2H-pyran-4-yl)-1H-indazole-3-carboxamide hydroformate,
• 46) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-N-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-indazole-3-carboxamide hydroformate,
• 47) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-N-methyl-6-(1,3-thiazol-2-yl)-1H-indazole-3-carboxamide hydroformate,
• 55) N-[(3S)-1-Oxido-1-azabicyclo[2.2.2]oct-3-yl]-5-(trifluoromethoxy)-1H-indazole-3-carboxamide,
• 58) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-[3-(cyclopropylmethoxy)pyrrolidin-1-yl]-1H-indazole-3-carboxamide hydroformate,
• 61) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-6-[3-(cyclopropylmethoxy)pyrrolidin-1-yl]-1H-indazole-3-carboxamide hydroformate, 62) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(3-methoxypyrrolidin-1-yl)-1H-indazole-3-carboxamide hydroformate,
• 63) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(2-oxo-3-propylimidazolidin-1-yl)-1H-indazole-3-carboxamide hydroformate,
• 73) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-1-ethyl-6-(1,3-oxazol-2-yl)-1H-indazole-3-carboxamide hydroformate,
• 74) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-1-ethyl-6-(1,3-oxazol-2-yl)-1H-indazole-3-carboxamide hydrochloride,
• 77) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(2-oxo-3-propylimidazolidin-1-yl)-1H-indazole-3-carboxamide,
• 89) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(4,5-dihydro-1H-imidazol-2-yl)-1H-indazole-3-carboxamide,
• 161) N,N′-di-(3S)-1-Azabicyclo[2.2.2]oct-3-yl-1H-indazole-1,3-dicarboxamide,
• 162) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(1-methyl-4,5-dihydro-1H-imidazol-2-yl)-1H-indazole-3-carboxamide,
• 163) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-(1-methyl-4,5-dihydro-1H-imidazol-2-yl)-1H-indazole-3-carboxamide,
• 164) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-5-[(3S)-3-(cyclopropylmethoxy)pyrrolidin-1-yl]-1H-indazole-3-carboxamide,
• 165) (3S)-1-(Chloromethyl)-3-[(1H-indazol-3-ylcarbonyl)amino]-1-azoniabicyclo[2.2.2]octane chloride,
• 166) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-5-[(3S)-3-methoxypyrrolidin-1-yl]-1H-indazole-3-carboxamide dihydroformate,
• 184) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-cyano-1H-indazole-3-carboxamide,
• 185) 3-[(3S)-1-Azabicyclo[2.2.2]oct-3-ylamino]carbonyl-1H-indazole-6-carboxylic acid hydrochloride,
• 186) N(3)-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-N(6),N(6)-dimethyl-1H-indazole-3,6-dicarboxamide,
• 187) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-[(4-methylpiperazin-1-yl)carbonyl]-1H-indazole-3-carboxamide,
• 188) N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-6-[(3R)-3-methoxypyrrolidin-1-yl]carbonyl-1H-indazole-3-carboxamide,
• 190) N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-5-(tetrahydro-2H-pyran-4-yloxy)-1H-indazole-3 -carboxamide,
• wherein salts listed above can also be in free base form or in the form of another pharmaceutically acceptable salt, and free base forms listed above can also be in the form of a pharmaceutically acceptable salt,
• wherein a compound listed above, in either a free base form or in the form of a pharmaceutically acceptable salt, can also be in the form of a solvate,
• wherein a compound listed above, in either a free base form or in the form of a pharmaceutically acceptable salt, can also be in the form of an N-oxide,
• wherein a compound listed above, in a free base form or solvate or N-oxide thereof, or in the form of a pharmaceutically acceptable salt or solvate thereof, can also be in the form of a polymorph, and
• wherein if the compound exhibits chirality it can be in the form of a mixture of enantiomers or a mixture of diastereomers, or can be in the form of a single enantiomer or a single diastereomer.