Indoles, 1H-indazoles, 1,2-benzisoxazoles, 1,2-benzoisothiazoles, and preparation and uses thereof

A pharmaceutical composition comprising a pharmaceutically acceptable carrier and at least one compound according to

• wherein
• X9 to X12 are each, independently, CH or CR3;
• C═B is C═O, C═S, or CH2;
• Y is O or S;
• A3 is
• wherein when A3 is of the following formula, m is 2 or 3, Y is O, and B is O, then at least one of X9 to X12 is CR3 in which R3 is other than H, CH3, halogen, NO2 or NH2, or R10 is other than H, CH3, or C2H5
• R3 is H,
• C1-6-alkyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, OH, alkoxy having 1 to 4 carbon atoms NR13R14, SH, SR13, SOR13, C3-8-cycloalkyl, SO2R13, SO2NR13R14, Ar, Het, or combinations thereof,
• C2-6-alkenyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, OH, alkoxy having 1 to 4 carbon atoms, NR13R14, SH, SR13, SOR13, C3-8-cycloalkyl, SO2R13, SO2NR13R14, Ar, Het, or combinations thereof,
• C2-6-alkynyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, OH, alkoxy having 1 to 4 carbon atoms, NR13R14, SH, SR13, SOR13, C3-8-cycloalkyl, SO2R13, SO2NR13R14, Si(R15)3Ar, Het, or combinations thereof,
• C3-8-cycloalkyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, OH, alkoxy having 1 to 4 carbon atoms, NR13R14, SH, SR13, SOR13, unsubstituted C3-8-cycloalkyl, SO2R13, SO2NR13R14, Ar, Het, or combinations thereof,
• halogen,
• CN, NO2, NR13R14, SH, SR13, SOR13, SO2R13, SO2NR13R14, NR13SO2R14, CONR13R14, CSNR13R14, COOR13, NR13COR14, NR13CSR14, NR13CONR13R14, NR13CSNR13R14, NR13COOR14, NR13CSOR14, OCONR13R14, OCSNR13R14,
• Ar,
• Het, or
• R16O—;
• R6 to R12 are each, independently,
• H,
• C1-4-alkyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, alkoxy having 1 to 4 carbon atoms, Ar, or combinations thereof,
• C3-6-alkenyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, alkoxy having 1 to 4 carbon atoms, Ar, or combinations thereof,
• C3-6-alkynyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, alkoxy having 1 to 4 carbon atoms, Ar, or combinations thereof,
• cycloalkyl having 3 to 10 carbon atoms, which is unsubstituted or substituted one or more times by halogen, hydroxy, oxo, cyano, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, or combinations thereof,
• cycloalkylalkyl having 4 to 16 carbon atoms, which is unsubstituted or substituted in the cycloalkyl portion and/or the alkyl portion one or more times by halogen, oxo, cyano, hydroxy, C1-4-alkyl, C1-4-alkoxy or combinations thereof,
• Ar-alkyl, or
• Het-alkyl;
• R13 and R14 are each independently
• H,
• Ar,
• Ar-alkyl,
• Het,
• C1-4-alkyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, OH, alkoxy having 1 to 4 carbon atoms, monoalkylamino, dialkylamino, C3-8-cycloalkyl, or combinations thereof,
• cycloalkyl having 3 to 10 carbon atoms, which is unsubstituted or substituted one or more times by halogen, hydroxy, oxo, cyano, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, or combinations thereof,
• C3-6-alkenyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, alkoxy having 1 to 4 carbon atoms, Ar, or combinations thereof, or
• C3-6-alkynyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, alkoxy having 1 to 4 carbon atoms, Ar or combinations thereof;
• R15 is C1-6-alkyl;
• R16 is H,
• C1-6-alkyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, OH, alkoxy having 1 to 4 carbon atoms, NR13R14, SH, SR13, SOR13, C3-8-cycloalkyl, SO2R13, SO2NR13R14, Ar, Het, or combinations thereof,
• C3-6-alkenyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, OH, alkoxy having 1 to 4 carbon atoms, NR13R14, SH, SR13, SOR13, C3-8-cycloalkyl, SO2R13, SO2NR13R14, Ar, Het, or combinations thereof,
• C3-6-alkynyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, OH, alkoxy having 1 to 4 carbon atoms, NR13R14, SH, SR13, SOR13, C3-8-cycloalkyl, SO2R13, SO2NR13R14, Ar, Het, or combinations thereof,
• C3-8-cycloalkyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, OH, alkoxy having 1 to 4 carbon atoms, NR13R14, SH, SR13, SOR13, unsubstituted C3-8-cycloalkyl, SO2R13, SO2NR13R14, Ar, Het, or combinations thereof,
• C4-8-cycloalkylalkyl which is unsubstituted or substituted one or more times by F, Cl, Br, I, CN, OH, alkoxy having 1 to 4 carbon atoms, NR13R14, SH, SR13, SOR13, unsubstituted C3-8-cycloalkyl, SO2R13, SO2NR13R14, Ar, Het, or combinations thereof,
• Ar, or
• Het;
• m is 1, 2 or 3;
• o is 1 or 2;
• Ar is an aryl group containing 6 to 10 carbon atoms which is unsubstituted or substituted one or more times by
• alkyl having 1 to 8 carbon atoms,
• alkoxy having 1 to 8 carbon atoms,
• halogen,
• amino,
• cyano,
• hydroxyl,
• nitro,
• halogenated alkyl having 1 to 8 carbon atoms,
• halogenated alkoxy having 1 to 8 carbon atoms,
• hydroxyalkyl having 1 to 8 carbon atoms,
• hydroxyalkoxy having 2 to 8 carbon atoms,
• alkenyloxy having 3 to 8 carbon atoms,
• monoalkylamino having 1 to 8 carbon atoms,
• dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms,
• carboxy,
• alkoxycarbonyl,
• alkylaminocarbonyl,
• acylamido,
• acyloxy,
• alkylthio having 1 to 8 carbon atoms,
• alkylsulphinyl having 1 to 8 carbon atoms,
• alkylsulphonyl having 1 to 8 carbon atoms,
• sulfo,
• sulfonylamino,
• Het,
• cycloalkylamino wherein the cycloalkyl group has 3 to 7 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio,
• aryloxy wherein the aryl portion contains 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio,
• arylthio wherein the aryl portion contains 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio,
• cycloalkyloxy wherein the cycloalkyl group has 3 to 7 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio, or
• combinations thereof;
• Ar-alkyl is an aryl-alkylene group wherein the alkylene portion contains 1 to 4 carbon atoms and is unsubstituted or substituted one or more times by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio, and the aryl portion is Ar as defined above;
• and
• 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
• alkyl having 1 to 8 carbon atoms,
• alkoxy having 1 to 8 carbon atoms,
• halogen,
• amino,
• cyano,
• hydroxyl,
• nitro,
• halogenated alkyl having 1 to 8 carbon atoms,
• halogenated alkoxy having 1 to 8 carbon atoms,
• hydroxyalkyl having 1 to 8 carbon atoms,
• hydroxyalkoxy having 2 to 8 carbon atoms,
• alkenyloxy having 3 to 8 carbon atoms,
• monoalkylamino having 1 to 8 carbon atoms,
• dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms,
• carboxy,
• alkoxycarbonyl,
• alkoxycarbonylmethyl,
• alkylaminocarbonyl,
• acylamido,
• acyloxy,
• alkylthio having 1 to 8 carbon atoms,
• alkylsulphinyl having 1 to 8 carbon atoms,
• alkylsulphonyl having 1 to 8 carbon atoms,
• sulfo,
• oxo,
• sulfonylamino,
• cycloalkylamino wherein the cycloalkyl group has 3 to 7 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio,
• aryl containing 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio,
• aryl-alkylene group wherein the aryl portion contains 6 to 10 carbon atoms and the alkylene portion contains 1 to 4 carbon atoms and is unsubstituted or substituted one or more times by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio,
• aryloxy wherein the aryl portion contains 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio,
• arylthio wherein the aryl portion contains 6 to 10 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio,
• cycloalkyloxy wherein the cycloalkyl group has 3 to 7 carbon atoms and is optionally substituted by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio,
• 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, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio,
• heterocyclic-alkyl group, in which the heterocyclic portion 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 the alkyl portion is an alkylene group containing 1-4 carbon atoms, wherein said heterocyclic-alkyl group is unsubstituted or substituted one or more times by halogen, alkyl having 1 to 8 carbon atoms, halogenated alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 4 carbon atoms, amino, monoalkylamino wherein the alkyl portion has 1 to 8 carbon atoms, dialkylamino wherein the alkyl portions each have 1 to 8 carbon atoms, COR16, CSR16, cyano, hydroxyl, nitro, oxo, or thio, or
• combinations thereof;
• and
• Het-alkyl is a Het-alkylene group wherein the alkylene portion contains 1 to 4 carbon atoms, and the Het portion is Het as defined above;
• or
• a pharmaceutically acceptable salt thereof.