Indazoles, benzothiazoles, benzoisothiazoles, benzoisoxazoles, pyrazolopyridines, isothiazolopyridines, preparing and using them

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to organic chemistry, namely new compounds of formula , wherein A represents residues of formulae

, , , X represents O; X1-X4 represents N, CH, CR1 or C-, X9-X12 represents N, CH, CR4 or C-, X13-X16 represents N, CH, CR or C-, wherein C represents an attachment point of the group A to a residue of the structure of formula (I); R' represents H or alkyl; R represents alkoxy, or Het; R1 represents F, CI, Br, I, OH, CN, carboxy, CONR6R7, NR2COR8, NR2COOR8, alkoxy, fluorinated alkoxy, Ar, Het or OHet; or R1 represents one of the following formulas: wherein n is equal to 2 and m is equal to 3; R2 represents H, alkyl, fluorinated alkyl, cycloalkyl, Het or Het-NH-CO-; R4 represents F, Cl, Br, I, OH, alkoxy, cycloalkoxy, Het or OHet; or R4 represents one of the following formulae: , wherein n is equal to 2 and t is equal to 3; each R6 and R7 independently represents alkyl, or cycloalkyl, or R6 and R7 together represent alkylene group containing 5-6 carbon atoms which forms a cycle with N atoms; R8 represent alkyl, or cycloalkylalkyl; R9 represents alkyl; Ar represents aryl group; Het represents heterocyclic group which is completely saturated, particularly saturated or completely unsaturated containing 5 to 10 ring atoms in which at least 1 ring atom represents N, O or S atom which is unsubstituted or substituted once or several times by the substituted specified in cl. 1; and their pharmaceutically acceptable salts or solvates or N-oxides, or solvates of their pharmaceutically acceptable salts, or solvates of N-oxides of their pharmaceutically acceptable salts wherein said compound can be presented in the form of a polymorph, wherein if said compound shows chirality, it can be presented in the form of a mixture of enanthiomers or a mixture of diastereoisomers, or can be presented in the form of single enanthiomer or single diastereoisomer; and wherein at least one of the groups R, R1 or R4 represents Het or OHet, wherein the group Het is specified in each case in substituted or unsubstituted azabicyclooctyl, oxaazabicycloheptyl, diazabicycloheptyl, diazabicyclononyl, diazabicyclooctyl, pyrazolyl, dihydroimidazolyl, 1,4-diazepanyl, hezahydropyrrolopyrazinyl and octahydropyrrolopyridinyl. Also the invention refers to other compounds of formula (I), to specific compounds, to a pharmaceutical composition based on the compound of formula (I), to a method of selective activation/stimulation of α-7 nicotinic receptors, to application of the compound of formula (I) for making the drug.

EFFECT: there are produced new compounds showing effective biological properties.

53 cl, 1 tbl

 

The text descriptions are given in facsimile form.

1. The compound of formula I:

where And is a

or
X represents O;
X1-X4each independently represents N, CH, CR1or C, where C represents the point of joining the group And to the rest of the structure of formula (I);
X9-X12each independently represents N, CH, CR4or C, where C represents the point of joining the group And to the rest of the structure of formula (I);
X13-X16each independently represents N, CH, CR or C-, where C represents the point of joining the group And to the rest of the structure of formula (I);
R' represents H or alkyl containing from 1 to 4 carbon atoms;
R represents an alkoxy containing from 1 to 4 carbon atoms, or Het;
R1represents F, Cl, Br, I, IT, CN, carboxy, CONR6R7, NR2COR8, NR2COOR8, alkoxy containing from 1 to 4 carbon atoms, fluorinated alkoxy containing from 1 to 4 carbon atoms, Ar, Het or OHet; or
R1represents one of the following formulas:
or
where n equals 2 and m equals 3;
R2represents H, alkyl containing from 1 to 4 atoms ug is erode, fluorinated alkyl containing from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, Het or Het-NH-CO-;
R4represents F, Cl, Br, I, HE, alkoxy containing from 1 to 4 carbon atoms, cycloalkane containing from 3 to 7 carbon atoms, Het or OHet; or
R4represents one of the following formulas:
or
where n equals 2 and m equals 3;
R6and R7each independently represents alkyl containing from 1 to 4 carbon atoms, or cycloalkyl containing from 3 to 7 carbon atoms, or R6and R7together represent alkylenes group containing 5-6 carbon atoms, which forms a cycle with N atom;
R8represents alkyl containing from 1 to 4 carbon atoms, or cycloalkenyl containing from 4 to 7 carbon atoms;
R9represents alkyl containing from 1 to 4 carbon atoms;
AG represents an aryl group containing from 6 to 10 carbon atoms;
Het represents a heterocyclic group which is fully saturated, partially saturated or fully unsaturated, containing from 5 to 10 atoms in the ring, in which at least 1 atom in the ring is an atom of N, O or S, which is unsubstituted or substituted one or more times by alkyl containing 1 to 8 carbon atoms, alkoxy containing from 1 to 8 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, halogenated alkoxy containing from 1 to 8 carbon atoms, cycloalkane containing from 3 to 7 carbon atoms, halogenated alkyl containing from 1 to 8 carbon atoms, oxo, HE, amino, monoalkylamines containing from 1 to 8 carbon atoms, dialkylamino, where each alkyl group contains from 1 to 8 carbon atoms, or-CXR11;
R11represents alkyl containing from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, or cycloalkenyl containing from 4 to 7 carbon atoms;
and their pharmaceutically acceptable salt, or solvate, or N-oxide, or solvate their pharmaceutically acceptable salt, or a solvate of N-oxides, their pharmaceutically acceptable salts,
where the specified connection may also be in the form of polymorph,
where, if the specified connection exhibits chirality it can be in the form of mixtures of enantiomers or mixtures of diastereomers, or can be in the form of a single enantiomer or a single diastereoisomer; and
where at least one of the groups R, R1or R4represents Het or OHet, where the group Het is selected in each instance from a substituted or unsubstituted azabicycloalkanes, kaasamistavadele, disalicylate, Diisobutylene, diazabicyclo, pyrazolyl, dihydroimidazole, 1,4-diazepine, hexahydrotriazine and octahydrophenanthrene.

2. The compound according to claim 1, where at least one of the groups R, R1or R4represents 1-azabicyclo[2.2.2]Oct-3-yloxy, 2-oxa-5-azabicyclo[2.2.1]heptyl, diazabicyclo (for example, 2,5-diazabicyclo [2.2.1]hept-2-yl, 5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl, triptorelin-2,5-diazabicyclo[2.2.1]hept-2-yl, 5-(cyclopropanecarbonyl)-2,5-diazabicyclo[2.2.1]hept-2-yl, 1,4-diazabicyclo[3.2.2]non-4-yl, 5-methyl-2,5-diazabicyclo[2.2.2]Oct-2-yl, 8-methyl-3,8-diazabicyclo[3.2.1]Oct-3-yl, pyrazolyl, dihydroimidazole, 1,4-diazepan-1-yl, 4-methyl-1,4-diazepan-1-yl, hexahydropyrazino[1,2-a]pyrazin-2(1H)-yl or 1-(cyclopropanecarbonyl)-octahydro-6N-pyrrolo [3,4-b] pyridine-6-yl.

3. The compound according to claim 1, where at least one of the groups R, R1or R3represents a substituted or unsubstituted disalicylate or oxazaborolidine.

4. The compound according to claim 3, where at least one of the groups R, R1or R4represents a 2,5-diazabicyclo[2.2.1]hept-2-yl, methyl-2,5-diazabicyclo[2.2.1]hept-2-yl, triptorelin-2,5-diazabicyclo[2.2.1]hept-2-yl or 2-oxa-5-azabicyclo[2.2.1]hept-5-yl.

5. The compound of formula I:

where And is a

or

X represents O;
X1-X4each independently represents N, CH, CR1or C, where C represents the point of joining the group And to the rest of the structure of formula (I);
X9-X12each independently represents N, CH, CR or C-, where C represents the point of joining the group And to the rest of the structure of formula (I);
R' represents H or alkyl containing from 1 to 4 carbon atoms;
R1represents F, Cl, Br, I, IT, CN, alkoxy containing from 1 to 4 carbon atoms, fluorinated alkoxy containing from 1 to 4 carbon atoms, Ar, Het or OHet; or
R1represents one of the following formulas:
or
where n equals 2 and m equals 3;
R2represents H, alkyl containing from 1 to 4 carbon atoms, fluorinated alkyl containing from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, Het or Het-NH-CO-;
R4represents F, Cl, Br, I, HE, alkoxy containing from 1 to 4 carbon atoms, cycloalkane containing from 3 to 7 carbon atoms, Het or OHet; or
R4represents one of the following formulas:
or
where n equals 2 and m equals 3; R6and R7each independently represents H, alkyl containing from 1 to 4 carbon atoms, or cycloalkyl containing from 3 to 7 carbon atoms, or R6and R7together represent alkylenes group containing 5-6 carbon atoms which forms a ring with the N atom;
R9represents alkyl containing from 1 to 4 carbon atoms;
AG represents an aryl group containing from 6 to 10 carbon atoms;
Het represents a heterocyclic group which is fully saturated, partially saturated or fully unsaturated, containing from 5 to 10 atoms in the ring, in which at least 1 atom in the ring is an atom of N, O or S, which is unsubstituted or substituted one or more times by alkyl containing 1 to 8 carbon atoms, alkoxy containing from 1 to 8 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, halogenated alkoxy containing from 1 to 8 carbon atoms, cycloalkane containing from 3 to 7 carbon atoms, cycloalkenes containing from 4 to 7 carbon atoms, alkoxyalkyl containing from 2 to 8 carbon atoms, alkyl(halogenated alkyl)amino, where each alkyl group contains from 1 to 8 carbon atoms, halogenated alkyl containing them from 1 to 8 carbon atoms, oxo, HE monoalkylamines containing from 1 to 8 carbon atoms, dialkylamino, where each alkyl group contains from 1 to 8 carbon atoms, or-CXR11;
R11represents alkyl containing from 1 to 4 carbon atoms, or cycloalkyl containing from 3 to 7 carbon atoms, or cycloalkenyl containing from 4 to 7 carbon atoms;
and their pharmaceutically acceptable salt, or solvate, or N-oxide, or solvate their pharmaceutically acceptable salts, or pharmaceutically acceptable salt or solvate, N-oxide,
where the specified connection may also be in the form of polymorph,
where, if the specified connection exhibits chirality it can be in the form of mixtures of enantiomers or mixtures of diastereomers, or can be in the form of a single enantiomer or a single diastereoisomer, and
provided that:
And represents the formula (a) and contains at least one substituent R1that is a Het, non-thiazolyl, and R2represents alkyl containing from 2 to 4 carbon atoms, fluorinated alkyl containing from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, or Het; or
And represents the formula (C) and contains at least one substituent R4that performance, which provides imidazolyl, pyrrolyl, pyrazolyl,1-8alkylphenolic, oxazaborolidine, diazabicyclo,1-8alkyldiethanolamine, halogenated C1-8alkyldiethanolamine, piperidinyl or pyrrolidinyl, substituted hydroxy, halogenated alkoxy, cycloalkylation, monoalkylamines-(C1-8alkyl-NH-), dialkylamino-((C1-8alkyl)2-N-), alkoxyalkyl or alkyl(fluorinated alkyl)amino.

6. The compound of formula I:

where And is a

or
X represents O;
X1-X4each independently represents N, CH, CR1or C, where C represents the point of joining the group And to the rest of the structure of formula (I);
X9-X12each independently represents N, CH, CR4or C, where C represents the point of joining the group And to the rest of the structure of formula (I);
X13-X16each independently represents N, CH, CR or C-, where C represents the point of joining the group And to the rest of the structure of formula (I);
R' represents H or alkyl containing from 1 to 4 carbon atoms;
R represents an alkoxy containing from 1 to 4 carbon atoms, or Het;
R1represents F, Cl, Br, I, IT, CN, carboxy, CONR6 R7, NR2COR8, NR2CONR6R7, alkoxy containing from 1 to 4 carbon atoms, fluorinated alkoxy containing from 1 to 4 carbon atoms, Ar, Het or OHet; or
R1represents one of the following formulas:
or
where n equals 2 and m equals 3;
R2represents H, alkyl containing from 1 to 4 carbon atoms, fluorinated alkyl containing from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, Het or Het-NH-CO-;
R4represents F, Cl, Br, I, HE, alkoxy containing from 1 to 4 carbon atoms, cycloalkane containing from 3 to 7 carbon atoms, Het or OHet; or
R4represents one of the following formulas:
or
where n equals 2 and m equals 3;
R6and R7each independently represents H, alkyl containing from 1 to 4 carbon atoms, or cycloalkyl containing from 3 to 7 carbon atoms, or R6and R7together represent alkylenes group containing 5-6 carbon atoms which forms a ring with the N atom;
R8represents alkyl containing from 1 to 4 carbon atoms;
R9represents alkyl containing from 1 to 4 carbon atoms;
AG before the hat is aryl group, containing from 6 to 10 carbon atoms;
Het represents a heterocyclic group which is fully saturated, partially saturated or fully unsaturated, containing from 5 to 10 atoms in the ring, in which at least 1 atom in the ring is an atom of N, O or S, which is unsubstituted or substituted one or more times by alkyl containing 1 to 8 carbon atoms, alkoxy containing from 1 to 8 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, halogenated alkoxy containing from 1 to 8 carbon atoms, cycloalkane containing from 3 to 7 carbon atoms, cycloalkenes containing from 4 to 7 carbon atoms, alkoxyalkyl containing from 2 to 8 carbon atoms, alkyl(halogenated alkyl)amino, where each alkyl group contains from 1 to 8 carbon atoms, halogenated alkyl containing from 1 to 8 carbon atoms, oxo, HE monoalkylamines containing from 1 to 8 carbon atoms, dialkylamino, where each alkyl group contains from 1 to 8 carbon atoms, or-R11;
R11represents alkyl containing from 1 to 4 carbon atoms, or cycloalkenyl containing from 4 to 7 carbon atoms;
and their pharmaceutically acceptable salt, or solvate, or N-oxide, or solvate their Pharma is efticiency acceptable salts, or a pharmaceutically acceptable salt, or their solvate, N-oxide,
where the specified connection may also be in the form of polymorph,
where, if the specified connection exhibits chirality it can be in the form of mixtures of enantiomers or mixtures of diastereomers, or can be in the form of a single enantiomer or a single diastereoisomer, and
where the specified compound contains at least one group Het, which is fully saturated, partially saturated or fully unsaturated, containing from 5 to 10 atoms in the ring, in which at least 1 atom in the ring is an atom of N, O or S and which is substituted, where at least one of the substituents represents a halogenated alkoxy containing from 1 to 8 carbon atoms, cycloalkane containing from 3 to 7 carbon atoms, cycloalkenes containing from 4 to 7 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, halogenated alkyl containing from 2 to 8 carbon atoms, alkoxyalkyl containing from 2 to 8 carbon atoms, or alkyl(halogenated alkyl)amino, where each alkyl group contains from 1 to 8 carbon atoms.

7. The connection according to claim 6, where the specified compound contains at least one group Het, which is fully saturated, partially saturated or fully n is saturated, containing from 5 to 10 atoms in the ring, in which at least 1 atom in the ring is an atom of N, O or S and which is substituted, where at least one of the substituents represents a halogenated alkoxy containing from 1 to 8 carbon atoms, cycloalkenes containing from 4 to 7 carbon atoms, or halogenated alkyl containing from 2 to 8 carbon atoms.

8. The connection according to claim 6 or 7, where R2represents H, alkyl containing from 1 to 4 carbon atoms, or fluorinated alkyl containing from 1 to 4 carbon atoms.

9. The compound of formula I:

where And is a

or

X represents O;
X1-X4each independently represents N, CH, CR1or C, where C represents the point of joining the group And to the rest of the structure of formula (I);
X9-X12each independently represents N, CH, CR4or C, where C represents the point of joining the group And to the rest of the structure of formula (I);
R' represents H or alkyl containing from 1 to 4 carbon atoms;
R is alkoxy containing from 1 to 4 carbon atoms, or Het,
R1represents F, Cl, Br, I., HE, CN, carboxy, CONR6R7, NR2COR8, NR2ONR6, R 4, alkoxy containing from 1 to 4 carbon atoms, fluorinated alkoxy containing from 1 to 4 carbon atoms, Ar, Het or OHet; or
R1represents one of the following formulas:
or
where n equals 2 and m equals 3;
R2represents H, alkyl containing from 1 to 4 carbon atoms, fluorinated alkyl containing from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, Het or Het-NH-CO-;
R4represents F, Cl, Br, I, HE, alkoxy containing from 1 to 4 carbon atoms, cycloalkane containing from 3 to 7 carbon atoms, Het or OHet; or
R4represents one of the following formulas:
or
where n equals 2 and m equals 3;
R6and R7each independently represents H, alkyl containing from 1 to 4 carbon atoms, or cycloalkyl containing from 3 to 7 carbon atoms, or R6and R7together represent alkylenes group containing 5-6 carbon atoms which forms a ring with the N atom;
R8represents alkyl containing from 1 to 4 carbon atoms, or cycloalkenyl containing from 4 to 7 carbon atoms;
R9represents alkyl containing from 1 to 4 carbon atoms;
the r represents an aryl group, containing from 6 to 10 carbon atoms;
Het represents a heterocyclic group which is fully saturated, partially saturated or fully unsaturated, containing from 5 to 10 atoms in the ring, in which at least 1 atom in the ring is an atom of N, O or S, which is unsubstituted or substituted one or more times by alkyl containing 1 to 8 carbon atoms, alkoxy containing from 1 to 8 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, halogenated alkoxy containing from 1 to 8 carbon atoms, cycloalkane containing from 3 to 7 carbon atoms, cycloalkenes containing from 4 to 7 carbon atoms, alkoxyalkyl containing from 2 to 8 carbon atoms, alkyl(halogenated alkyl)amino, where each alkyl group contains from 1 to 8 carbon atoms, halogenated alkyl containing from 1 to 8 carbon atoms, oxo, HE monoalkylamines containing from 1 to 8 carbon atoms, dialkylamino, where each alkyl group contains from 1 to 8 carbon atoms, or-CXR11;
R11represents alkyl containing from 1 to 4 carbon atoms, or cycloalkenyl containing from 4 to 7 carbon atoms;
and their pharmaceutically acceptable salt, or solvate, or N-oxide, or solvate their formats whitesky acceptable salts, or a pharmaceutically acceptable salt, or their solvate, N-oxide,
where the specified connection may also be in the form of polymorph,
where, if the specified connection exhibits chirality it can be in the form of mixtures of enantiomers or mixtures of diastereomers, or can be in the form of a single enantiomer or a single diastereoisomer, and
where at least one of X1X2X3and X4represents N; or at least one of X9X10X11and X12represents N.

10. The connection according to claim 9, where R2represents H, alkyl containing from 1 to 4 carbon atoms, or fluorinated alkyl containing from 1 to 4 carbon atoms.

11. The connection according to claim 9 or 10, where
at least one of X1X2X3and X4represents N, and 1 or 2 of the remaining X1-X4represent CR1; or
at least one of X9X10X11and X12represents N, and 1 or 2 of the remaining X9-X12represent CR4.

12. The compound according to any one of claims 1 to 11, where a represents podporou (a) and attached to the remainder of the compound at the 3-, 4 - or 7-position.

13. The compound according to any one of claims 1 to 11, where a represents podporou (s) and attached to the remainder of the compound at the 3-, 4 - or 7-position.

14. The compound according to any one of claims 1 to 4, and 6-8, where a represents podporou (d) and attached to the remainder of the compound at the 3-, 4 - or 7-position.

15. The connection section 12, where a is attached to the remainder of the compound at the 3-position.

16. The connection indicated in paragraph 13, where And attached to the remainder of the compound at the 3-position.

17. The connection 14, where And attached to the remainder of the compound at the 3-position.

18. The compound of formula I:

where And is a

or

X represents O;
X1-X4each independently represents N, CH, CR1or C, where C represents the point of joining the group And to the rest of the structure of formula (I);
X9-X12each independently represents N, CH, CR4or C, where C represents the point of joining the group And to the rest of the structure of formula (I);
R' represents H or alkyl containing from 1 to 4 carbon atoms;
R represents an alkoxy containing from 1 to 4 carbon atoms, or Het;
R1represents F, Cl, Br, I, IT, CN, carboxy, CONR6R7, NR2COR8, NR2CONR6R7, alkoxy containing from 1 to 4 carbon atoms, fluorinated alkoxy containing from 1 to 4 carbon atoms, Ar, Het or OHet; or
R1represents one of sleduushemu:
or
where n equals 2 and m equals 3;
R2represents H, alkyl containing from 1 to 4 carbon atoms, fluorinated alkyl containing from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, Het or Het-NH-CO-;
R4represents F, Cl, Br, I, HE, alkoxy containing from 1 to 4 carbon atoms, cycloalkane containing from 3 to 7 carbon atoms, Het or OHet; or
R4represents one of the following formulas:
or
where n equals 2 and m equals 3;
R6and R7each independently represents H, alkyl containing from 1 to 4 carbon atoms, or cycloalkyl containing from 3 to 7 carbon atoms, or R6and R7together form alkylenes group containing 5-6 carbon atoms which forms a ring with the N atom;
R8represents alkyl containing from 1 to 4 carbon atoms, or cycloalkenyl containing from 4 to 7 carbon atoms;
R9represents alkyl containing from 1 to 4 carbon atoms;
AG represents an aryl group containing from 6 to 10 carbon atoms;
Het represents a heterocyclic group which is fully saturated, partially saturated or floor is awn unsaturated, containing from 5 to 10 atoms in the ring, in which at least 1 atom in the ring is an atom of N, O or S, which is unsubstituted or substituted one or more times by alkyl containing 1 to 8 carbon atoms, alkoxy containing from 1 to 8 carbon atoms, cycloalkyl containing from 3 to 7 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, halogenated alkoxy containing from 1 to 8 carbon atoms, cycloalkane containing from 3 to 7 carbon atoms, cycloalkenes containing from 4 to 7 carbon atoms, alkoxyalkyl containing from 2 to 8 carbon atoms, alkyl(halogenated alkyl)amino, where each alkyl group contains from 1 to 8 carbon atoms, halogenated alkyl containing from 1 to 8 carbon atoms, oxo, HE monoalkylamines containing from 1 to 8 carbon atoms, dialkylamino, where each alkyl group contains from 1 to 8 carbon atoms, or-R11;
R11represents alkyl containing from 1 to 4 carbon atoms, or cycloalkenyl containing from 4 to 7 carbon atoms;
and their pharmaceutically acceptable salts, including Quaternary ammonium salt, or solvate, or N-oxide, or solvate their pharmaceutically acceptable salts, or pharmaceutically acceptable salt, or their solvate, N-oxide,
where the specified connection can also on titsa in the form of polymorph, and
where, if the specified connection exhibits chirality it can be in the form of mixtures of enantiomers or mixtures of diastereomers, or can be in the form of a single enantiomer or a single diastereoisomer;
provided that 1-azabicyclo is in the form of Quaternary ammonium salts podhorany:

where Z represents alkyl containing from 1 to 4 carbon atoms, halogenated alkyl containing from 1 to 4 carbon atoms, cycloalkenyl containing from 4 to 7 carbon atoms, or arylalkyl containing from 7 to 16 carbon atoms, and an anion And is an iodide, bromide, chloride, triflate, tosylate or mesilate.

19. Connection p, where group a represents the formula (a) or (C).

20. The connection according to claim 19, where X1-X4each represents CH or CR1or X9-X12each represents CH or CR4.

21. The compound according to any one of claims 1 to 20, where R' represents H or CH3.

22. A compound selected from the following compounds:
1) (3S)-3-({[6-(cyclopropylmethoxy)-1,2-benzisothiazol-3-yl]carbonyl}amino)-1-(cyclopropylmethyl)-1-azoniabicyclo[2.2.2]octabrain or formate,
2) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
3) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5,6-dimmock and-1H-indazol-3-carboxamide,
4) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-propyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
5) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-isopropyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
6) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(tetrahydrofuran-3-yloxy)-1H-indazol-3-carboxamide,
7) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(tetrahydro-2H-Piran-4-yloxy)-1H-indazol-3-carboxamide,
8) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1-methylpyrrolidine-3-yl)oxy]-1H-indazol-3-carboxamide,
9) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-4-hydroxy-1H-indazol-3-carboxamide,
10) hydroformed N-[(3S)-1-azabicyclo[2,2 .2]Oct-3-yl]-5-bromo-4-hydroxy-1H-indazol-3-carboxamid,
11) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5,7-dibromo-4-hydroxy-1H-indazol-3-carboxamide,
12) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-hydroxy-1,2-benzisothiazol-3-carboxamide,
13) (3S)-3-{[(5-hydroxy-1,2-benzisothiazol-3-yl)carbonyl]amino}-1-methyl-1-azoniabicyclo[2.2.2]attenuated or formate,
14) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-FuelMAX)-1,2-benzisothiazol-3-carboxamide,
15) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-(2-oxopyrrolidin-1-yl)-1H-indazol-3-carboxamide,
16) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-hydroxy-1H-indazol-3-carboxamide,
17) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-N-methyl-1H-indazol-3-carboxamide,
18) HYDROFORM is N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-methyl-6-{[(propylamino)carbonyl]amino}-1H-indazol-3-carboxamide,
19) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-methoxy-1H-indazol-3-carboxamid,
20) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-methoxy-1H-indazol-3-carboxamid,
21) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-(deformity)-6-methoxy-1H-indazol-3-carboxamid,
22) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-(deformity)-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
23) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(cyclopropanecarbonyl)amino]-1-methyl-1H-indazol-3-carboxamide,
24) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(cyclopropanecarbonyl)amino]-1-(deformity)-1H-indazol-3-carboxamide,
25) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-(deformity)-6-{[(propylamino)carbonyl]amino}-1H-indazol-3-carboxamide,
26) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-cyclopropyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
27) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,3-thiazol-2-yl)-1-(3-thienyl)-1H-indazol-3-carboxamid,
28) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamid,
29) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
30) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamid,
31) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-(cyclopropylmethyl)-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamid,
32) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,3-oxazol-2-yl)-1-propyl-1H-indazol-3-carboxamid,
33) N - [(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-1H-methyl-6-(1,3-oxazol-2-yl-1H-indazol-3-carboxamid,
34) N-[(3S)-1-azabicyclo[2.2.2]-Oct-3-yl]-N-methyl-6-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamid,
35) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-5-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamid,
36) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-(deformedarse)-N-methyl-1H-indazol-3-carboxamid,
37) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(deformedarse)-N-methyl-1H-indazol-3-carboxamid,
38) N-[(3S)-1-azabicyclo [2.2.2] Oct-3-yl]-1-cyclopropyl-6-[(cyclopropanecarbonyl)amino]-1H-indazol-3-carboxamid,
39) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-cyclopropyl-6-{[(propylamino)carbonyl]amino}-1H-indazol-3-carboxamid,
40) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-methoxy-N-methyl-1H-indazol-3-carboxamid,
41) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(4S)-4-hydroxy-2-oxopyrrolidin-1-yl]-1H-indazol-3-carboxamide,
42) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-methoxy-N-methyl-1H-indazol-3-carboxamide,
43) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-(deformedarse)-N-methyl-1H-indazol-3-carboxamide,
44) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-deformedarse)-N-methyl-1H-indazol-3-carboxamide,
45) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamide,
46) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamide,
47) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-Carbo is samida,
48) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-N-methyl-1,2-benzisothiazol-3-carboxamide,
49) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
50) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-hydroxy-1,2-benzisothiazol-3-carboxamide,
51) of the hydrochloride of N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-1,2-benzisothiazol-3-carboxamide,
52) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-1,2-benzisothiazol-3-carboxamide,
53) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-methoxy-1,2-benzisothiazol-3-carboxamide,
54) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(2-oxo-3-propylimidazolium-1-yl)-1,2-benzisothiazol-3-carboxamide,
55) N-[(3S)-1-oxido-1-azabicyclo[2.2.2]Oct-3-yl]-5-(triptoreline)-1H-indazol-3-carboxamid,
56) 6-methoxy-N - [(3S)-1-oxido-1-azabicyclo[2.2.2]Oct-3-yl]-1,2-benzisothiazol-3-carboxamide,
57) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-fluoro-1H-pyrazolo[3,4-b]pyridine-3-carboxamide,
58) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(cyclopropylmethoxy)pyrrolidin-1-yl]-1H-indazol-3-carboxamide,
59) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1H-pyrazolo[4,3-C]pyridine-3-carboxamide,
60) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1H-pyrazolo[3,4-C] pyridine-3-carboxamide,
61) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(cyclopropylmethoxy)pyrrolidin-1-yl]-1H-indazol-3-carboxamide,
62) hydroformed N-[(3R)-1-and bicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-1H-indazol-3-carboxamide,
63) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(2-oxo-3-propylimidazolium-1-yl)-1H-indazol-3-carboxamide,
64) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-pyrrolidin-1-yl-1,2-benzisothiazol-3-carboxamide,
65) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-methyl-2-oxopyrrolidin-1-yl)-1,2-benzisothiazol-3-carboxamide,
66) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1H-pyrrol-1-yl)-1,2-benzisothiazol-3-carboxamide,
67) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethyl-2-Oxymetazoline-1-yl)-1,2-benzisothiazol-3-carboxamide,
68) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(cyclopropylmethoxy)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
69) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-1,2-benzisoxazol-3-carboxamide,
70) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-(3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
71) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-1,2-benzisoxazol-3-carboxamide,
72) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
73) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamide,
74) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamide,
75) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
76) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
77) N-[(3S)-1-asabis the CLO[2.2.2]Oct-3-yl]-6-(2-oxo-3-propylimidazolium-1-yl)-1H-indazol-3-carboxamid,
78) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-hydroxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
79) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(deformedarse)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
80) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1H-imidazol-1-yl)-1,2-benzisothiazol-3-carboxamide,
81) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1H-pyrazole-1-yl)-1,2-benzisothiazol-3-carboxamide,
82) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-methyl-1H-pyrazole-1-yl)-1,2-benzisothiazol-3-carboxamide,
83) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(5-methyl-1H-pyrazole-1-yl)-1,2-benzisothiazol-3-carboxamide,
84) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
85) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
86) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-1,2-benzisoxazol-3-carboxamide,
87) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-7-fluoro-1,2-benzisothiazol-3-carboxamide,
88)] N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-phenyl-1H-pyrazolo[3,4-b]pyridine-3-carboxamide,
89) N-(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(4,5-dihydro-1H-imidazol-2-yl)-1H-indazol-3-carboxamid,
90) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(dimethylamino)pyrrolidin-1-yl]-1H-pyrazolo[3,4-b]pyridine-3-carboxamide,
91) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(dimethylamino)pyrrolidin-1-yl]-1H-pyrazolo[3,4-b]pyridine-3-carboxamide,
92) N-[(3R)-1-azabicyclo[2.2.]Oct-3-yl]-7-fluoro-6-(3-ethoxypyrrolidine the-1-yl)-1,2-benzisothiazol-3-carboxamide,
93) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-fluoro-6-(3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
94) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
95) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
96) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
97) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]hept-5-yl]-1,2-benzisothiazol-3-carboxamide,
98) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
99) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
100) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
101) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3R)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
102) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3S)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
103) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
104) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]hept-5-yl]-1,2-benzisothiazol-3-carboxamide,
105) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
106) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct--yl]isothiazole[5,4-b]pyridine-3-carboxamide,
107) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]isothiazole[5,4-b]pyridine-3-carboxamide,
108) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisoxazol-3-carboxamide,
109) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisoxazol-3-carboxamide,
110) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
111) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
112) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
113) hydroformed N-[(3S)-1-azabicyclo[2.2,2]Oct-3-yl]-7-[(3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
114) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-fluoro-6-methoxy-1,2-benzisothiazol-3-carboxamide,
115) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-7-fluoro-6-methoxy-1,2-benzisothiazol-3-carboxamide,
116) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
117) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(15,45)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
118) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
119) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
120) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(methylaminopropyl-1-yl]-1,2-benzisothiazol-3-carboxamide,
121) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(methylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
122) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-(2,2,2-triptorelin)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
123) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-{3-[methyl(2,2,2-triptorelin)amino]pyrrolidin-1-yl}-1,2-benzisothiazol-3-carboxamide,
124) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-{3-[methyl(2,2,2-triptorelin)amino]pyrrolidin-1-yl}-1,2-benzisothiazol-3-carboxamide,
125) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(methoxymethyl)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
126) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(methoxymethyl)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
127) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
128) N(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
129) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[4-(dimethylamino)piperidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
130) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[4-(dimethylamino)piperidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
131) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(2-oxo-3-propylimidazolium-1-yl)-1,2-benzisothiazol-3-carboxamide,
132) dihydrofolate N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
133) dihydrofolate N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-[(S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
134) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
135) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
136) dihydrofolate N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,4-diazabicyclo[3.2.2]non-4-yl)-1,2-benzisothiazol-3-carboxamide,
137) dihydrofolate N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,4-diazabicyclo[3.2.2]non-4-yl)-1,2-benzisothiazol-3-carboxamide,
138) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-pyrrolidin-1-yl-1,2-benzisothiazol-3-carboxamide,
139) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(4-methylpiperazin-1-yl)-1,2-benzisothiazol-3-carboxamide,
140)] N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(4-methylpiperazin-1-yl)-1,2-benzisothiazol-3-carboxamide,
141) N-[(3R)-1-azabicyclo [2.2.2]Oct-3-yl]-6-(4-methyl-1,4-diazepan-1-yl)-1,2-benzisothiazol-3-carboxamide,
142) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(4-methyl-1,4-diazepan-1-yl)-1,2-benzisothiazol-3-carboxamide,
143) N-[(3R-)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(hexahydropyrazino[1,2-a]pyrazin-2(1H)-yl)-1,2-benzisothiazol-3-carboxamide,
144) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(hexahydropyrazino[1,2-a]pyrazin-2(1H)-yl)-1,2-benzisothiazol-3-carboxamide,
145) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(5-methyl-2,5-diazabicyclo[2.2.2]Oct-2-yl)-1,2-benzisothiazol-3-carboxamide,
146) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(5-methyl-2,5-diazabicyclo[2.2.2]Oct-2-yl)-1,2-benzisothiazol-3-carboxamide,
147) N-[(3R)-1-azabicyclo[2.2.2]OK the-3-yl]-6-(8-methyl-3,8-diazabicyclo[3.2.1]Oct-3-yl)-1,2-benzisothiazol-3-carboxamide,
148) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(8-methyl-3,8-diazabicyclo[3.2.1]Oct-3-yl)-1,2-benzisothiazol-3-carboxamide,
149) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-cyclopropyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
150) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-cyclopropyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
151) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-(cyclopropylmethyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
152) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-(cyclopropylmethyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
153) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-(4-methyl-1,4-diazepan-1-yl)-1,2-benzisothiazol-3-carboxamide,
154) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
155)] N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
156) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-[(3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
157) N-(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1-methylpyrrolidine-3-yl)oxy]-1,2-benzisothiazol-3-carboxamide,
158) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1-methylpyrrolidine-3-yl)oxy]-1,2-benzisothiazol-3-carboxamide,
159) N-(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1-azabicyclo[2.2.2]Oct-3-yloxy)-1,2-benzisothiazol-3-carboxamide,
160) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1-azabicyclo[2.2.2]Oct-3-yloxy)-1,2-benzisothiazol-3-carboxym the d,
161) N,N'-di-(3S)-1-azabicyclo[2.2.2]Oct-3-yl-1H-indazol-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-indazol-3-carboxamid,
163) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1-methyl-4,5-dihydro-1H-imidazol-2-yl)-1H-indazol-3-carboxamid,
164) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-[(3S)-3-(cyclopropylmethoxy)pyrrolidin-1-yl]-1H-indazol-3-carboxamid,
165) chloride (3S)-1-(chloromethyl)-3-[(1H-indazol-3-ylcarbonyl)amino]-1-azoniabicyclo[2.2.2]octane
166) dihydrofolate N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-[(3S)-3-ethoxypyrrolidine-1-yl]-1H-indazol-3-carboxamide,
167) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-floristical[5,4-b]pyridine-3-carboxamide,
168) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-methylpiperazin-1-yl)-1,2-benzisothiazol-3-carboxamide,
169) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(octahydro-6N-pyrrolo[3,4-b]pyridine-6-yl)-1,2-benzisothiazol-3-carboxamide,
170) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(octahydro-6N-pyrrolo[3,4-b]pyridine-6-yl)-1,2-benzisothiazol-3-carboxamide,
171) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-piperazine-1-yl-1,2-benzisothiazol-3-carboxamide,
172) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-piperazine-1-yl-1,2-benzisothiazol-3-carboxamide,
173) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,4-diazepan-1-yl)-1,2-benzisothiazol-3-carboxamide,
174) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,4-diazepan-1-yl)-1,2-benzisothiazol-3-carboxamide,
175) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(2-methylpiperazin-1-yl)-1,2-benzisothiazol-carboxamid,
176) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(2-methylpiperazin-1-yl)-1,2-benzisothiazol-3-carboxamide,
177) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[4-(cyclopropanecarbonyl)piperazine-1-yl]-1,2-benzisothiazol-3-carboxamide,
178)] N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl)-6-[4-(cyclopropanecarbonyl)piperazine-1-yl]-1,2-benzisothiazol-3-carboxamide,
179) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[1-(cyclopropanecarbonyl)octahydro-6N-pyrrolo[3,4-b]pyridine-6-yl]-1,2-benzisothiazol-3-carboxamide,
180) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[1-(cyclopropanecarbonyl)octahydro-6N-pyrrolo[3,4-b]pyridine-6-yl]-1,2-benzisothiazol-3-carboxamide,
181) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-(cyclopropanecarbonyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
182) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-(cyclopropanecarbonyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
183) N-[(3R)1-azabicyclo[2.2.2]Oct-3-yl]-6-(3,4-dimethylpiperazine-1-yl)-1,2-benzisothiazol-3-carboxamide,
184) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-cyano-1H-indazol-3-carboxamid,
185) hydrochloride 3-[(3S)-1-azabicyclo[2.2.2]Oct-3-ylamino]carbonyl-1H-indazol-6-carboxylic acid,
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-indazol-3-carboxamid,
188) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-ethoxypyrrolidine-1-yl] carbonyl-1H-indazol-3-carboxamid,
189)N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxyethanol[5,4-b]pyridine-3-carboxamide and
190) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-(tetrahydro-2H-Piran-4-yloxy)-1H-indazol-3-carboxamid,
where the above salts can also be in the form of free bases or in the form of another pharmaceutically acceptable salt, and the above form of the free bases can also be in the form of a pharmaceutically acceptable salt,
where the above compound in free base form or in the form of pharmaceutically acceptable salts may also be in the form of MES,
where the above compound in free base form or in the form of pharmaceutically acceptable salts may also be in the form of N-oxide,
where the above compound in free base form, or MES, or N-oxide or in the form of pharmaceutically acceptable salts, or its MES, also can be in the form of polymorph, and
where, if the specified connection exhibits chirality it can be in the form of mixtures of enantiomers or mixtures of diastereomers, or can be in the form of a single enantiomer or a single diastereoisomer.

23. Connection p.22, where the specified connection is selected from the following compounds:
2) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
3) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5,6-dimethoxy-1H-indazol-3-carboxamide,
5) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-isopropyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
6) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(tetrahydrofuran-3-yloxy)-1H-indazol-3-carboxamide,
7) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(tetrahydro-2H-Piran-4-yloxy)-1H-indazol-3-carboxamide,
8) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1-methylpyrrolidine-3-yl)oxy]-1H-indazol-3-carboxamide,
9) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-4-hydroxy-1H-indazol-3-carboxamide,
10) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-bromo-4-hydroxy-1H-indazol-3-carboxamide,
11) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5,7-dibromo-4-hydroxy-1H-indazol-3-carboxamide,
12) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-hydroxy-1,2-benzisothiazol-3-carboxamide,
13) (3S)-3-{[(5-hydroxy-1,2-benzisothiazol-3-yl)carbonyl]amino}-1-methyl-1-azoniabicyclo[2.2.2]octane iodide or formate,
14) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-FuelMAX)-1,2-benzisothiazol-3-carboxamide,
15) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-(2-oxopyrrolidin-1-yl)-1H-indazol-3-carboxamide,
16) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-hydroxy-1H-indazol-3-carboxamide,
17) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-N-methyl-1H-indazol-3-carboxamide,
18) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-methyl-6-{[(propylamino)carbonyl]amino}-1H-indiso the-3-carboxamide,
19) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-methoxy-1H-indazol-3-carboxamid,
20) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-methoxy-1H-indazol-3-carboxamid,
21) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-(deformity)-6-methoxy-1H-indazol-3-carboxamid,
22) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-(deformity)-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
23) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(cyclopropanecarbonyl)amino]-1-methyl-1H-indazol-3-carboxamide,
24) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(cyclopropanecarbonyl)amino]-1-(deformity)-1H-indazol-3-carboxamide,
25) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-(deformity)-6-{[(propylamino)carbonyl]amino}-1H-indazol-3-carboxamide,
26) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-cyclopropyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
27) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,3-thiazol-2-yl)-1-(3-thienyl)-1H-indazol-3-carboxamid,
28) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamid,
29) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
30) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamid,
31) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-(cyclopropylmethyl)-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamid,
32) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,3-oxazol-2-yl)-1-propyl-1H-indazol-3-carboxamid,
33) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-N-methyl-6-(1,3-oxazol-2-yl)1H-indazol-3-carboxamid,
34) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamid,
35) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-5-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamid,
36) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-(deformedarse)-N-methyl-1H-indazol-3-carboxamid,
37) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(deformedarse)-N-methyl-1H-indazol-3-carboxamid,
38) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-cyclopropyl-6-[(cyclopropanecarbonyl)amino]-1H-indazol-3-carboxamid,
39) N[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-cyclopropyl-6-{[(propylamino)carbonyl]amino}-1H-indazol-3-carboxamid,
40) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-methoxy-N-methyl-1H-indazol-3-carboxamid,
41) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(4S)-4-hydroxy-2-oxopyrrolidin-1-yl]-1H-indazol-3-carboxamide,
42) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-methoxy-N-methyl-1H-indazol-3-carboxamide,
43) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-(deformedarse)-N-methyl-1H-indazol-3-carboxamide,
44) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(deformedarse)-N-methyl-1H-indazol-3-carboxamide,
45) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamide,
46) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-5-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamide,
47) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carbox the amide,
48) hydroformed N-[(3R)-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-N-methyl-1,2-benzisothiazol-3-carboxamide,
49) of the hydrochloride of N-[(3S)-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
50) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-hydroxy-1,2-benzisothiazol-3-carboxamide,
51) of the hydrochloride of N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-1,2-benzisothiazol-3-carboxamide,
52) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-1,2-benzisothiazol-3-carboxamide,
53) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-methoxy-1,2-benzisothiazol-3-carboxamide,
54) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-oxo-3-propylimidazolium-1-yl)-1,2-benzisothiazol-3-carboxamide,
55) N-[(3S)-1-oxido-1-azabicyclo[2.2.2]Oct-3-yl]-5-(triptoreline)-1H-indazol-3-carboxamide and
56) 6-methoxy-N-[(3S)-1-oxido-1-azabicyclo[2.2.2]Oct-3-yl]-1,2-benzisothiazol-3-carboxamide,
where the above salts can also be in the form of free bases or in the form of another pharmaceutically acceptable salt, and the above form of the free bases can also be in the form of a pharmaceutically acceptable salt,
where the above compound in free base form or in the form of pharmaceutically acceptable salts may also be in the form of MES,
where the above compound in free base form or in the form of a pharmaceutically acceptable with the and may also be in the form of N-oxide,
where the above compound in free base form, or MES or N-oxide or in the form of pharmaceutically acceptable salts, or its MES, also can be in the form of polymorph, and
where, if the specified connection exhibits chirality it can be in the form of mixtures of enantiomers or mixtures of diastereomers, or can be in the form of a single enantiomer or a single diastereoisomer.

24. Connection p.22, where the specified connection is selected from the following compounds:
2) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
3) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5,6-dimethoxy-1H-indazol-3-carboxamide,
4) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-propyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
5) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-isopropyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
6) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(tetrahydrofuran-3-yloxy)-1H-indazol-3-carboxamide,
7) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(tetrahydro-2H-Piran-4-yloxy)-1H-indazol-3-carboxamide,
8) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1-methylpyrrolidine-3-yl)oxy]-1H-indazol-3-carboxamide,
9) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-4-hydroxy-1H-indazol-3-carboxamide,
10) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-bromo-4-hydroxy-1H-indazol-3-carbox the IDA,
11) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5,7-dibromo-4-hydroxy-1H-indazol-3-carboxamide,
12) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-hydroxy-1,2-benzisothiazol-3-carboxamide,
13) (3S)-3-{[(5-hydroxy-1,2-benzisothiazol-3-yl)carbonyl]amino}-1-methyl-1-azoniabicyclo[2.2.2]octane iodide or formate,
14) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-FuelMAX)-1,2-benzisothiazol-3-carboxamide,
15) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-(2-oxopyrrolidin-1-yl)-1H-indazol-3-carboxamide,
16) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-hydroxy-1H-indazol-3-carboxamide,
17) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-N-methyl-1H-indazol-3-carboxamide,
18) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-methyl-6-{[(propylamino)carbonyl]amino}-1H-indazol-3-carboxamide,
19) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-methoxy-1H-indazol-3-carboxamid,
20) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-methoxy-1H-indazol-3-carboxamid,
21) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-(deformity)-6-methoxy-1H-indazol-3-carboxamid,
22) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-(deformity)-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
23) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(cyclopropanecarbonyl)amino]-1-methyl-1H-indazol-3-carboxamide,
24) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(cyclopropanecarbonyl)amino]-1-(deformity)-1H-indazol-3-carboxamide
25) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-deformity)-6-{[(propylamino)carbonyl]amino}-1H-indazol-3-carboxamide,
26) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-cyclopropyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
27) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,3-thiazol-2-yl)-1-(3-thienyl)-1H-indazol-3-carboxamid,
28) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamid,
29) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamid,
30) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamid,
31) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-(cyclopropylmethyl)-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamid,
32) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,3-oxazol-2-yl)-1-propyl-1H-indazol-3-carboxamid,
33) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-N-methyl-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamid,
34) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamid,
35) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-5-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamid,
36) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-(deformedarse)-N-methyl-1H-indazol-3-carboxamid,
37) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(deformedarse)-N-methyl-1H-indazol-3-carboxamid,
38) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-cyclopropyl-6-[(cyclopropanecarbonyl)amino]-1H-indazol-3-carboxamid,
39) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-cyclopropyl-6-{[(propylamino)carbonyl]am is but}-1H-indazol-3-carboxamid,
40) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-methoxy-N-methyl-1H-indazol-3-carboxamid,
41) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(4S)-4-hydroxy-2-oxopyrrolidin-1-yl]-1H-indazol-3-carboxamide,
42) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-methoxy-N-methyl-1H-indazol-3-carboxamide,
43) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-(deformedarse)-N-methyl-1H-indazol-3-carboxamide,
44) hydroformed N-[(3R-)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(deformedarse)-N-methyl-1H-indazol-3-carboxamide,
45) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamide,
46) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-5-(tetrahydro-2H-Piran-4-yl)-1H-indazol-3-carboxamide,
47) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-(1,3-thiazol-2-yl)-1H-indazol-3-carboxamide,
48) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-N-methyl-1,2-benzisothiazol-carboxamide,
49) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
50) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-hydroxy-1,2-benzisothiazol-3-carboxamide,
where the above salts can also be in the form of free bases or in the form of another pharmaceutically acceptable salt, and the above form of the free bases can also be in the form of a pharmaceutically acceptable salt,
where the above is Obedinenie in free base form or in the form of pharmaceutically acceptable salts may also be in the form of MES,
where the above compound in free base form or in the form of pharmaceutically acceptable salts may also be in the form of N-oxide,
where the above compound in free base form, or MES, or N-oxide or in the form of pharmaceutically acceptable salts, or its MES may also be in the form of polymorph, and
where, if the specified connection exhibits chirality it can be in the form of mixtures of enantiomers or mixtures of diastereomers, or can be in the form of a single enantiomer or a single diastereoisomer.

25. Connection p.22, where the specified connection is selected from the following compounds:
57) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-fluoro-1H-pyrazolo[3,4-b]pyridine-3-carboxamide,
58) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(cyclopropylmethoxy)pyrrolidin-1-yl]-1H-indazol-3-carboxamide,
59) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1H-pyrazolo[4,3-C]pyridine-3-carboxamide,
60) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1H-pyrazolo[3,4-C]pyridine-3-carboxamide,
61) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(cyclopropylmethoxy)pyrrolidin-1-yl]-1H-indazol-3-carboxamide,
62) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-1H-indazol-3-carboxamide,
63) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(2-oxo-3-propylimidazolium-1-yl)-1H-indiso the-3-carboxamide,
64) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-pyrrolidin-1-yl-1,2-benzisothiazol-3-carboxamide,
65) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-methyl-2-oxopyrrolidin-1-yl)-1,2-benzisothiazol-3-carboxamide,
66) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1H-pyrrol-1-yl)-1,2-benzisothiazol-3-carboxamide,
67) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethyl-2-Oxymetazoline-1-yl)-1,2-benzisothiazol-3-carboxamide,
68) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(cyclopropylmethoxy)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
69) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-1,2-benzisoxazol-3-carboxamide,
70) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-(3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
71) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-1,2-benzisoxazol-3-carboxamide,
72) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
73) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamide,
74) of the hydrochloride of N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-1-ethyl-6-(1,3-oxazol-2-yl)-1H-indazol-3-carboxamide,
75) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
76) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
77) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(2-oxo-3-propylimidazolium-1-yl)-1H-indazol-3-carboxamid,
78) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl-6-(3-hydroxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
79) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(deformedarse)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
80) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1H-imidazol-1-yl)-1,2-benzisothiazol-3-carboxamide,
81) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1H-pyrazole-1-yl)-1,2-benzisothiazol-3-carboxamide,
82) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-methyl-1H-pyrazole-1-yl)-1,2-benzisothiazol-3-carboxamide,
83) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(5-methyl-1H-pyrazole-1-yl)-1,2-benzisothiazol-3-carboxamide,
84) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
85) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
86) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxy-1,2-benzisoxazol-3-carboxamide,
87) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-ethoxypyrrolidine-1-yl)-7-fluoro-1,2-benzisothiazol-3-carboxamide,
88) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-phenyl-1H-pyrazolo[3,4-b]pyridine-3-carboxamide,
89) N-(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(4,5-dihydro-1H-imidazol-2-yl)-1H-indazol-3-carboxamid,
90) N-[(3S)-1-azabicyclo[2.2.2]Oct-CIL]-6-[3-(dimethylamino)pyrrolidin-1-yl]-1H-pyrazolo[3,4-b]pyridine-3-carboxamide,
91) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(dimethylamino)pyrrolidin-1-yl]-1H-pyrazolo[3,4-b]pyridine-3-carboxamide,
92) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-7-fluoro-6-(3-ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamide,
93) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-fluoro-6-(3-detoxify ridin-1-yl)-1,2-benzisothiazol-3-carboxamide,
94) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
95) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
96) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
97) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]hept-5-yl]-1,2-benzisothiazol-3-carboxamide,
98) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
99) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
100) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
101) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3R)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
102) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3S)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
103) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
104) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]hept-5-yl]-1,2-benzisothiazol-3-carboxamide,
105) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
106) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]isothiazole[5,4-b]pyridine-3-carboxamide,
107) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]isotis the lo[5,4-b]pyridine-3-carboxamide,
108) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisoxazol-3-carboxamide,
109) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisoxazol-3-carboxamide,
110) hydroformed N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3R-)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
111) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
112) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
113) hydroformed N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-[(3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
114) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-7-fluoro-6-methoxy-1,2-benzisothiazol-3-carboxamide,
115) N-(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-7-fluoro-6-methoxy-1,2-benzisothiazol-3-carboxamide,
116) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
117) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
118) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
119) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
120) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(methylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
121) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(who ethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
122) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-(2,2,2-triptorelin)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
123) N-(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-{3-[methyl(2,2,2-triptorelin)amino]pyrrolidin-1-yl}-1,2-benzisothiazol-3-carboxamide,
124) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-{3-[methyl(2,2,2-triptorelin)amino]pyrrolidin-1-yl}-1,2-benzisothiazol-3-carboxamide,
125) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(methoxymethyl)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
126) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(methoxymethyl)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
127) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
128) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide,
129) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[4-(dimethylamino)piperidine-1-yl]-1,2-benzisothiazol-3-carboxamide and
130) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[4-dimethylamino)piperidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
where the above salts can also be in the form of free bases or in the form of another pharmaceutically acceptable salt, and the above form of the free bases can also be in the form of a pharmaceutically acceptable salt,
where the above compound in free base form or in the form of pharmaceutically acceptable salts may also be in the form of the e MES,
where the above compound in free base form or in the form of pharmaceutically acceptable salts may also be in the form of N-oxide,
where the above compound in free base form, or MES, or N-oxide or in the form of pharmaceutically acceptable salts, or its MES, also can be in the form of polymorph, and
where, if the specified connection exhibits chirality it can be in the form of mixtures of enantiomers or mixtures of diastereomers, or can be in the form of a single enantiomer or a single diastereoisomer.

26. Connection p.22, where the connection specified is a
(131) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(2-oxo-3-propylimidazolium-1-yl)-1,2-benzisothiazol-3-carboxamide and its pharmaceutically acceptable salts,
where the above salts can also be in the form of free bases or in the form of another pharmaceutically acceptable salt, and the above form of the free bases can also be in the form of a pharmaceutically acceptable salt,
where the above compound in free base form or in the form of pharmaceutically acceptable salts may also be in the form of MES,
where the above compound in free base form or in the form of pharmaceutically acceptable salts may also be in the form of N-is XID,
where the above compound in free base form, or MES, or N-oxide or in the form of pharmaceutically acceptable salts, or its MES, also can be in the form of polymorph, and
where, if the specified connection exhibits chirality it can be in the form of mixtures of enantiomers or mixtures of diastereomers, or can be in the form of a single enantiomer or a single diastereoisomer.

27. Connection p.22, where the specified connection is selected from the following compounds:
1) (3S)-3-({[6-(cyclopropylmethoxy)-1,2-benzisothiazol-3-yl]carbonyl}amino)-1-(cyclopropylmethyl)-1-azoniabicyclo[2.2.2]octabrain or formate,
132) dihydrofolate N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
133) dihydrofolate N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-N-methyl-6-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
134) N-(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
135) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
136) dihydrofolate N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,4-diazabicyclo[3.2.2]non-4-yl)-1,2-benzisothiazol-3-carboxamide,
137) dihydrofolate-N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,4-diazabicyclo[3.2.2]non-4-yl)-1,2-basisat the azole-3-carboxamide,
138) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-pyrrolidin-1-yl-1,2-benzisothiazol-3-carboxamide,
139) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(4-methylpiperazin-1-yl)-1,2-benzisothiazol-3-carboxamide,
140) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(4-methylpiperazin-1-yl)-1,2-benzisothiazol-3-carboxamide,
141) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(4-methyl-1,4-diazepan-1-yl)-1,2-benzisothiazol-3-carboxamide,
142) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(4-methyl-1,4-diazepan-1-yl)-1,2-benzisothiazol-3-carboxamide,
143) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(hexahydropyrazino[1,2-a]pyrazin-2(1H)-yl)-1,2-benzisothiazol-3-carboxamide,
144) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(hexahydropyrazino[1,2-a]pyrazin-2(1H)-yl)-1,2-benzisothiazol-3-carboxamide,
145) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(5-methyl-2,5-diazabicyclo[2.2.2]Oct-2-yl)-1,2-benzisothiazol-3-carboxamide,
146) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(5-methyl-2,5-diazabicyclo[2.2.2]Oct-2-yl)-1,2-benzisothiazol-3-carboxamide,
147) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(8-methyl-3,8-diazabicyclo[3.2.1]Oct-3-yl)-1,2-benzisothiazol-3-carboxamide,
148) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(8-methyl-3,8-diazabicyclo[3.2.1]Oct-3-yl)-1,2-benzisothiazol-3-carboxamide,
149) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-cyclopropyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
150) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-cyclopropyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
151) N-(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1,4S)-5-(cyclopropylmethyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
152) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-(cyclopropylmethyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
153) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-(4-methyl-1,4-diazepan-1-yl)-1,2-benzisothiazol-3-carboxamide,
154) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
155) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-[(3R)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
156) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-[(3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide,
157) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1-methylpyrrolidine-3-yl)oxy]-1,2-benzisothiazol-3-carboxamide,
158) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1-methylpyrrolidine-3-yl)oxy]-1,2-benzisothiazol-3-carboxamide,
159) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1-azabicyclo[2.2.2]Oct-3-yloxy)-1,2-benzisothiazol-3-carboxamide,
160) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1-azabicyclo[2.2.2]Oct-3-yloxy)-1,2-benzisothiazol-3-carboxamide,
161) N,N'-di-(3S)-1-azabicyclo[2.2.2]Oct-3-yl-1H-indazol-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-indazol-3-carboxamid,
163) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1-methyl-4,5-dihydro-1H-imidazol-2-yl)-1H-indazol-3-carboxamid,
164) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-[(3S)-3-(cyclopropylmethoxy)pyrrolidin-1-yl]-1H-indazol-3-carboxamid,
165) chloride (3S)-1-(chloromethyl)-3-[(1H-indazol-3-ylcarbonyl)amino]-1-azoniabicyclo[2.2.2]octane
166 dihydrofolate N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-5-[(3S)-3-ethoxypyrrolidine-1-yl]-1H-indazol-3-carboxamide,
167) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-floristical[5,4-b]pyridine-3-carboxamide,
168) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3-methylpiperazin-1-yl)-1,2-benzisothiazol-3-carboxamide,
169) N-[(3R)-1-azabicyclo [2.2.2] Oct-3-yl]-6-(octahydro-6N-pyrrolo[3,4-b]pyridine-6-yl)-1,2-benzisothiazol-3-carboxamide,
170) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(octahydro-6N-pyrrolo[3,4-b]pyridine-6-yl)-1,2-benzisothiazol-3-carboxamide,
171) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-piperazine-1-yl-1,2-benzisothiazol-3-carboxamide,
172) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-piperazine-1-yl-1,2-benzisothiazol-3-carboxamide,
173) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,4-diazepan-1-yl)-1,2-benzisothiazol-3-carboxamide,
174) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(1,4-diazepan-1-yl)-1,2-benzisothiazol-3-carboxamide,
175) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(2-methylpiperazin-1-yl)-1,2-benzisothiazol-3-carboxamide,
176) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methylpiperazin-1-yl)-1,2-benzisothiazol-3-carboxamide,
177) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[4-(cyclopropanecarbonyl)piperazine-1-yl]-1,2-benzisothiazol-3-carboxamide,
178) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[4-(cyclopropanecarbonyl)piperazine-1-yl]-1,2-benzisothiazol-3-carboxamide,
179) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[1-(cyclopropanecarbonyl)octahydro-6N-pyrrolo[3,4-b]pyridine-6-yl]-1,2-benzisothiazol-3-carboxamide,
180) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[1-(cyclopropanecarbonyl)octahydro-6N-pyrrolo[3,4-b]pyridine-6-yl]-1,2-basisat the azole-3-carboxamide,
181) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-(cyclopropanecarbonyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
182) N-(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(1S,4S)-5-(cyclopropanecarbonyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-1,2-benzisothiazol-3-carboxamide,
183) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3,4-dimethylpiperazine-1-yl)-1,2-benzisothiazol-3-carboxamide,
184) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-cyano-1H-indazol-3-carboxamid,
185) hydrochloride 3-[(3S)-1-azabicyclo[2.2.2]Oct-3-ylamino]carbonyl-1H-indazol-6-carboxylic acid,
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-indazol-3-carboxamid,
188) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[(3R)-3-ethoxypyrrolidine-1-yl] carbonyl-1H-indazol-3-carboxamid,
189) N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-methoxyethanol[5,4-b]pyridine-3-carboxamide and
190) N-[(3R)-1-azabicyclo[2.2.2]Oct-3-yl]-5-(tetrahydro-2H-Piran-4-yloxy)-1H-indazol-3-carboxamid,
where the above salts can also be in the form of free bases or in the form of another pharmaceutically acceptable salt, and the above form of the free bases can also be in the form of a pharmaceutically acceptable salt,
where the above compound in free base form or in the form of pharmaceutically acceptable salts may also be in formetanate,
where the above compound in free base form or in the form of pharmaceutically acceptable salts may also be in the form of N-oxide,
where the above compound in free base form, or MES, or N-oxide or in the form of pharmaceutically acceptable salts, or its MES, also can be in the form of polymorph, and
where, if the specified connection exhibits chirality it can be in the form of mixtures of enantiomers or mixtures of diastereomers, or can be in the form of a single enantiomer or a single diastereoisomer.

28. Connection p.22, where the specified connection is a N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-pyrrolidin-1-yl-1,2-benzisothiazol-3-carboxamide or its pharmaceutically acceptable salt.

29. Connection p.22, where the specified connection is a N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3S)-3-hydroxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide or its pharmaceutically acceptable salt.

30. Connection p.22, where the specified connection is a N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3S)-3-ethoxypyrrolidine-1-yl]-1,2-benzisothiazol-3-carboxamide or its pharmaceutically acceptable salt.

31. Connection p.22, where the specified connection is a N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-(3 ethoxypyrrolidine-1-yl)-1,2-benzisothiazol-3-carboxamid Il is its pharmaceutically acceptable salt.

32. Connection p.22, where the specified connection is a N-[(3S)-1-azabicyclo[2.2.2]Oct-3-yl]-6-[3-(deformedarse)pyrrolidin-1-yl]-1,2-benzisothiazol-3-carboxamide or its pharmaceutically acceptable salt.

33. Pharmaceutical composition for the selective activation/stimulation of the α-7 nicotinic receptors containing the compound according to any one of claims 1 to 32, and a pharmaceutically acceptable carrier.

34. Process for the selective activation/stimulation of the α-7 nicotinic receptors in a patient in which such activation/stimulation has a therapeutic effect, comprising the administration to a patient in need this, compounds according to any one of claims 1 to 32 in an effective amount.

35. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment of psychotic diseases, neurodegenerative diseases, including dysfunction of the cholinergic system, and/or the memory status, and/or attenuation of cognitive perception.

36. Use p, where the specified drug is intended for treatment of schizophrenia, anxiety, mania, depression, Huntington's, Alzheimer's, disease Taurus Levi, amyotrophic lateral sclerosis, memory impairment, loss of memory, deficits of learning, attention deficit and/or hyperactivity disorders attention deficit.

37 the Use of compounds according to any one of claims 1 to 32 for receiving the medicinal product, designed for treatment of a patient suffering from dementia and/or another condition with memory loss.

38. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment of memory impairment caused by Alzheimer's disease, age-related mild cognitive disorder, schizophrenia, Parkinson's disease, Huntington's disease, a disease of Peak disease of Creutzfeldt-Jakob disease, depression, aging, head trauma, stroke, CNS hypoxia, cerebral aging system, multi-infarct dementia, HIV, and/or cardiovascular disease.

39. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment and/or prophylaxis of dementia in Alzheimer's disease patients.

40. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment of alcohol dependence or provide antinociceptive therapy.

41. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended to ensure neurotoxity against damage caused by stroke and ischemia, caused by the glutamate excitotoxicity.

42. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the ecene nicotine addiction, pain, disturbances of circadian rhythm, obesity and/or diabetes.

43. Method of inducing Smoking cessation in a patient comprising the administration to a patient compounds according to any one of claims 1 to 32 in an effective amount.

44. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment of moderate cognitive disorder (MCI), vascular dementia (VaD), age-related cognitive disorders (AACD), amnesia associated with open heart surgery, cardiac arrest, General anesthesia, lack of memory from early exposure to anesthetic agents, cognitive disorders caused by sleep deprivation, chronic fatigue syndrome, narcolepsy, dementia associated with AIDS, cognitive disorders associated with epilepsy, down syndrome, dementia associated with alcoholism, memory impairment caused by drugs dependence, dementia Puglistica syndrome (Boxer), or dementia in animals.

45. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment of memory loss.

46. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment of memory disorders.

47. The application of § 46, where the specified memory disorder caused by reduced activity and nicotinic acetylcholine receptor.

48. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment or prevention of a disease or condition caused by the dysfunction of the transmission nicotinic acetylcholine receptor.

49. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment or prevention of a disease or condition caused by the violation or improper functioning of nicotinic acetylcholine receptors.

50. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment or prevention of a disease or condition caused by the suppression of the transmission of the nicotinic acetylcholine receptor.

51. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment or prevention of a disease or condition caused by a deficiency of cholinergic synapses.

52. The way to protect neurons from a patient from neurotoxicity induced by activation of α7nACh receptors, comprising the administration to a patient compounds according to any one of claims 1 to 32 in an effective amount.

53. The use of compounds according to any one of claims 1 to 32 for obtaining a medicinal product intended for the treatment or prevention of neurodegenerative disorders by which ingibirovaniya binding peptides β with α7nACh receptors.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: present application describes substituted bicyclic beta-lactams of formula I: which are class A and class C β-lactamase inhibitors wherein X, R1 and R2 are specified in the application, as well as a method for producing them. The compounds of formula I and their pharmaceutically acceptable salts are applicable for preparing a pharmaceutical composition and for producing a drug. The declared compounds are applicable for treating bacterial infections, optionally in a combination with a β-lactam antibiotic. Particularly, the compounds may be used with such β-lactam antibiotics, as e.g. imipenem, piperacillin or ceftazidime to control microorganisms resistant to β -lactam antibiotics due to the presence of β-lactamases.

EFFECT: preparing the composition for treating bacterial infections.

28 cl, 117 ex, 3 tbl, 3 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formulae

and ,

which can be used to inhibit lipid kinase, including PI3K, and treat lipid kinase-mediated disorders. Values of radicals are given in claim 1.

EFFECT: improved properties of the compound.

11 cl, 2 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formulae and including their stereoisomers, as well as pharmaceutically acceptable salt, where X denotes O or S; R1 is selected from H, F, CI, Br, I, CN, -CR14R15-NR16R17, -CR14R15-NHR10, -(CR14R15)NR10R11, -(CR14R15)nNR12C(=Y)R10, -(CR14R15)nNR12S(O)2R10, -(CR14R15)mOR10, -(CR14R15)nS(O)2R10, -C(OR10)R11R14, -C(R14)=CR18R19, -C(=Y)OR10, -C(=Y)NR10R11, -C(=Y)NR12OR10, -C(=O)NR12S(O)2R10, -C(=O)NR12(CR14R15)mNR10R11, -NHR12, -NR12C(=Y)R10, -S(O)2R10, -S(O)2NR10R11, C2-C12 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C4 carbocyclyl, piperidinyl, thiopyranyl, phenyl or C5-C6 heteroaryl; R2 is selected from H, C2-C12 alkyl and thiazolyl; R3 denotes a condensed bicyclic heteroaryl selected from indazole, indole, benzoimidazole, pyrrolopyridine, imidazopyridine and quinoline; R10, R11 and R12 independently denote H, C2-C12 alkyl, C3 carbocyclyl, heterocyclyl selected from pyrrolidine, morpholine and piperazine, phenyl or heteroaryl selected from pyrazole, pyridine, benzothiophene; or R10 and R11 together with a nitrogen atom with which they are bonded possibly form a saturated C3-C6 heterocyclic ring, possibly containing one additional ring atom selected from N or O, where said heterocyclic ring is possibly substituted with one or more groups independently selected from oxo, (CH2)mOR10, NR10R11, SO2R10, C(=O)R10, NR12S(O)R11, C(=Y)NR10R11, C1-C12 alkyl and heterocyclyl selected from pyrrolidine; R14 and R15 are independently selected from H or C1-C12 alkyl; R16 and R17 independently denote H or phenyl; R18 and R19 together with a carbon atom with which they are bonded form a C3-C20 heterocyclic ring, where said alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, phenyl, heteroaryl, piperidinyl and condensed bicyclic heteroaryl possibly substituted with one or more groups independently selected from F, CI, Br, I, CF3, -C(=Y)R10, -C(=Y)OR10, oxo, R10, -C(=Y)NR10R11, -(CR14R15)nNR10R11, -NR10R11, -NR12C(=Y)R10, -NR12C(=Y)NR10R11, -NR12SO2R10, OR10, SR10, -S(O)2R10, -S(O)2NR10R11, possibly substituted with carbocyclyl, selected from cyclopropyl, possibly substituted heterocyclyl selected from piperazine, possibly substituted with alkyl and alkylsulphonyl, pyrrolidine, morpholine, piperdine, possibly substituted CH3, phenyl and possibly substituted heteroaryl selected from imidazole and triazole; Y denotes O; m equals 0, 1 or 2; n equals 1 and t equals 2. The invention also relates to a pharmaceutical composition which modulates lipid kinase activity, based on said compounds.

EFFECT: obtaining novel compounds and a composition based on said compounds, which can be used to treat lipid kinase-mediated diseases, for example, cancer.

48 cl, 2 tbl, 372 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula where R1 is selected from H, F, CI, Br, CF3, C1-C6 alkoxy and OH; R2 is selected from H and C1-C6 alkyl; n equals 1-5; m equals 0 or 1; and Y is selected from CH2, NR3, (NR3R4)+X-, O and S; R3 and R4 are independently selected from H and C1-C4 alkyl; and X- is selected from pharmaceutically acceptable anions. The invention also relates to a method of producing said compound and to an antiviral pharmaceutical composition based on said compound of formula (I).

EFFECT: obtaining novel compounds and a composition based on said compounds, which can be used in medicine to treat a viral diseases such as herpes.

19 cl, 2 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: described is a compound of general formula: [1], where R1 denotes an optionally substituted C2-C12 alkyl, aryl or heterocyclic group which can be a mono- or bicyclic 5-11-member radical, where the heteroatoms can be nitrogen, oxygen or sulphur; X1 denotes C2-C4 an alkylene group; X2 denotes a bond; X3 denotes a group of general formula NR3 or CR4R5NR3 (where R3 denotes a hydrogen atom, optionally substituted lower alkyl group or imino-protective group) and R4 and R5 are identical or different, and each denotes a hydrogen atom or a lower alkyl group or bond; X4 denotes a lower alkylene or lower alkenylene or lower alkynylene group, which can be substituted with one or more oxo groups or a bond; X5 denotes a sulphur atom or bond; Y1 denotes an optionally substituted divalent 4-, 5- or 6-member alicyclic hydrocarbon residue or an optionally subsituted divalent 5- or 6-member alicyclic amine residue, where the heteroatoms can be nitrogen or oxygen; Z1, Z2, Z3, Z4, Z5 and Z6 are identical or different, and each denotes a nitrogen atom or a group of general formula CR7 (where R7 denotes a hydrogen atom, a halogen atom, a hydroxyl group, a cyano group, an optionally substituted amino group, or an amino group substituted with one or more C1-6 alkyl groups, a lower alkyl group, a cycloalkyl, a lower alkoxy group or a monocyclic 5-member heterocyclic group which can be substituted with one or more halogen atoms, where the heteroatoms can be nitrogen, acid or sulphur or a group of general formula Q1CO2R10 (where R10 denotes a carboxyl-protective group and Q1 denotes a lower alkenylene group), provided that at least one of Z3, Z4, Z5 and Z6 denotes a nitrogen atom, or salt thereof. The invention also describes an antimicrobial agent based on said compound.

EFFECT: novel compounds which can be used as antimicrobial agents are obtained and described.

25 cl, 176 ex, 6 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a novel crystalline form of vinflunine ditartrate, production method thereof and use thereof in therapy, especially for cancer pathology treatment.

EFFECT: high stability and wide variety of galenic forms.

8 cl, 3 ex, 5 dwg

FIELD: medicine.

SUBSTANCE: invention refers to a compound presented by formula (1), to its salt or hydrate where in formula R1 represents a methylene group, R2 represents a phenyl group which can contain a substitute(s), or a heterocyclic group which can contain a substitute(s), the cycle A represents a 6- or 7-members cycle (where cycle-making atoms of the cycle A different from a sulfur atom in position 6 are carbon atoms), and R3 represents a hydrogen atom, or 1-3 equal or different substitutes used to substitute the cycle A where the possible substitutes are specified in clause 1 of the patent claim. Also, the invention refers to a pharmaceutical composition exhibiting an anticancer activity, on the basis of the compound presented by formula (1).

EFFECT: there are produced new compounds and pharmaceutical composition on their basis which can find application in medicine for cancer treatment.

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compounds (la) of formula applied as tyrosine kinase c-Met inhibitors. , where: LA is selected from ,

or ; RA is selected from:

or each RA2 and RA6 represents hydrogen; RA3 represents RAr; or RA3, RA4 and carbon atoms whereto attached form 6-members aryl, optionally substituted, in the amount up to 4 by independent groups RAr, or a 5-6-members heterocyclyl or heteroaryl ring containing at least one O, N or S atom; R represents -OH; RA5 represents hydrogen or RAr; LB represents a covalent bond or -N(R*)-; RB represents halogen, NH2 or C1-8aliphatic group, optionally substituted by R; a 6-10-members aryl ring; a 3-7-members carbocyclyl ring, a 5-10-members heteroaryl ring containing 1-4 heteroatoms independently selected from nitrogen, oxygen and sulphur atoms, where each said aryl or heteroaryl ring is optionally substituted, in the amount up to five by independent groups RAr; R represents halogen, -R°, -SR°, Ph, optionally substituted R° or -C(O)OR°; each RAr is independently selected from halogen, -R°, -OR°, -SR°, Ph, optionally substituted in the amount up to five by independent groups -R°, -CN, -N(R°)2 or -C(O)OR°; or two adjacent groups RAr taken together, represent 1,2-methylenedixy or 1,2-ethylenedixy; each R* represents hydrogen; and each R° represents independently hydrogen, an optionally substituted C1-6aliphatic radical or an unsubstituted 5-6-members heteroaryl or heterocyclic ring containing 1-3 heteroatoms independently selected from nitrogen, oxygen and sulphur atoms.

EFFECT: invention refers to pharmaceutically acceptable compositions containing the compounds under the invention, and methods of application of the compositions in treatment of various proliferative disorders.

10 cl, 4 tbl, 548 ex, 9 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I in which A denotes X denotes O; R denotes H; R1 denotes OH, CN, a nitro group, NH2, NR2CSR8, NR2CONR2R9, NR2C SNR2R9, NR2SO2R10, NR2CONR6R7, NR2CSNR6R7, NR2R9, SO2R10, SOR10, alkyl containing 1-4 carbon atoms, fluorinated alkyl containing 1-4 carbon atoms, alkenyl containing 2-6 carbon atoms, alkynyl containing 2-6 carbon atoms, where each alkyl, fluorinated alkyl, alkenyl or alkynyl group in each case is unsubstituted or substituted with Ar or He, cycloalkenyl containing 5-8 carbon atoms, alkoxy group containing 1-4 carbon atoms, cycloalkoxy group containing 3-7 carbon atoms, cycloalkylalkoxy group containing 4-7 carbon atoms, fluorinated alkoxy group containing 1-4 carbon atoms, fluorinated hydroxyalkyl containing 1-4 carbon atoms, hydroxyalkoxy group containing 2-4 carbon atoms, an ordinary hydroxyalkoxy group containing 2-4 carbon atoms, monoalkylamino group containing 1-4 carbon atoms, dialkylamine group, where each alkyl group independently contains 1-4 carbon atoms, alkoxycarbonyl containing 2-6 carbon atoms, Het or OAr; R2 denotes H, alkyl containing 1-4 carbon atom, cycloalkyl containing 3-7 carbon atoms, and cycloalkyl alkyl containing 4-7 carbon atoms; R6 and R7 independently denote H, alkyl containing 1-4 carbon atoms, cycloalkyl containing 3-7 carbon atoms, or cycloalkylalkyl containing 4-7 carbon atoms, or R6 and R7 together denote an alkylene group containing 4-6 carbon atoms, which forms a ring with an N atom; R8 denotes alkyl containing 1-4 carbon atoms, fluorinated alkyl containing 1-4 carbon atoms, alkenyl containing 3-6 carbon atoms, alkynyl containing 3-6 carbon atoms, where each alkyl, fluorinated alkyl, alkenyl or alkynyl group is unsubstituted or substituted with Ar, cycloalkyl containing 3-7 carbon atoms, or Het; R9 denotes Ar or Het; R10 denotes alkyl containing 1-4 carbon atoms which is unsubstituted or substituted with Ar, or NR6R7; Ar denotes an aryl group containing 6-10 carbon atoms, which is unsubstituted or substituted once or several times with an alkyl containing 1-8 carbon atoms, alkoxy group containing 1-8 carbon atoms, halogen, cyano group or combinations thereof; and Het denotes dihydropyranyl, tetrahydropyranyl, tetrahydrofuranyl, tetrahydrothienyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, isoxazolinyl, thiazolyl, oxazolyl, pyrrolyl, pyrazolyl, imidazolyl, pyridyl, pyrimidinyl, indolyl, quinolinyl, isoquinolinyl or naphthyridinyl, which is unsubstituted or substituted once or several times with halogen, aryl containing 6-10 carbon atoms, which is optionally substituted with alkyl containing 1-8 carbon atoms, alkoxy group containing 1-8 carbon atoms, oxo group, -CXR11 or combinations thereof, or R11 denotes alkyl containing 1-4 carbon atoms which is unsubstituted or substituted with Ar or Het; or pharmaceutically acceptable salts thereof, where formula IA is attached to the rest of the bonding molecule in the 3, 4 or 7 positions. The invention also relates to a pharmaceutical composition and to use of compounds in any of claims 1-37.

EFFECT: obtaining novel biologically active compounds, having nicotinic acetylcholine receptor subtype α7 ligand activity.

59 cl, 316 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula [I-D1] or pharmaceutically acceptable salt thereof,

,

where each symbol is defined in the claim. The invention also relates to pharmaceutical compositions containing said compound and having HCV polymerase inhibiting activity.

EFFECT: disclosed compound exhibits anti-HCV activity, based on HCV polymerase inhibiting activity and is useful as an agent for preventing and treating hepatitis C.

32 cl, 497 tbl, 1129 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula where R1, R2 and R3 are independently selected from a group consisting of hydrogen, halogen and lower alkyl containing 1-6 carbon atoms; R4 denotes a residue given in the claim; R5 denotes hydrogen or methyl; R10 is selected from a group consisting of: (i) hydrogen; (ii) (C1-C10) alkyl; (iii) (C1-C10)alkyl, substituted with one or more substitutes independently selected from a group consisting of -N(CH3)2, morpholinyl, (C1-C4) alkoxy, hydroxyl, -CON(CH3)2 and halogen; (iv) monocyclic (C3-C8) cycloalkyl containing one N heteroatom; (v) 9-methyl-9-azabicyclo[3.3.1]nonane; (vi) phenyl; (vii) phenyl substituted with one or more (C1-C4)alkoxy; R11 is selected from a group consisting of hydrogen and (C1-C10)alkyl; or R10, R11 and a nitrogen atom with which they are bonded, together, form a nitric heterocycle or a substituted nitric heterocycle, such as given in the claim. The invention also relates to a pharmaceutical composition, having serotonin type 3 receptor modulating capacity and a method of treating a disorder which depends on serotonin type 3 receptor modulation.

EFFECT: compounds of formula II as serotonin type 3 receptor modulators.

18 cl, 1 tbl, 159 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to heterocyclic compounds of formula ,

wherein X2 represents residue C-Z-R2 or C-R3, wherein Z represents NH or S; R1 is selected from structures , and R2 and R3 have the values specified in cl.1 of the patent claim, or to their pharmaceutically acceptable salts. The invention also refers to a pharmaceutical composition, a series of specific compounds, application of the declared compounds and to an intermediate compound for preparing the compounds of formula (I).

EFFECT: compounds under the invention have affinity to muscarine receptors and can be used in treating, relieving and preventing diseases and conditions mediated by muscarine receptors.

13 cl, 3 tbl

FIELD: pharmacology.

SUBSTANCE: invention refers to the compound of formula(I) or to is salt where R1 is -H or C1-6 alkyl; R2 is bridged aza-ring chosen out of group including formula and where ring hydrogen atom in bridged aza-ring may be substituted by one or several groups of R22; m, n and p have respective values 1 or 2; r has the value 0 or 1; R21 is C1-6 alkyl, -C1-6 alkyl-O-phenyl or -C1-6 alkyl-phenyl; R22 is C1-6 alkyl-cycloalkyl or -C1-6 alkyl-phenyl; R2 is thienyl, phenyl, pyridyl, pyranzinyl, thiazolyl or pyrazolyl, each of which can be substituted by one or several R31; R31 is the halogen, -OH, -CN, -CF3, C1-6 alkyl or -O-C1-6 alkyl; ring A is the group consisting of thiophene, thiazole, isothiazole, thidiazole, oxazole, isooxazole, cyclohexan, norboran, benzothiophene and 5,6-dihydro-4H-cyclopentathiophene, each of which can be substituted by the group chosen out of the group consisting out of one or several RA1; where RA1 is a halogen, -CN, -NH2, C1-6 alkyl, -O-C1-6 alkyl, CONH2, - HN-C1-6 alkyl, -HN-C1-6 alkyl-O-C1-6 alkyl-phenyl, -HN-C1-6 alkyl-phenyl or -HN-C1-6 alkyl-OH where C1-6 alkyl can be substituted with one or several halogen atoms; V is -NH- or -O-; W is -(CH2)q-; q has the value 0.1 or 2; X is the counteranion and is an ordinary bond; on condition when in case ring A is cyclohexane, R3 is phenyl which can be replaced with one or several R31. The invention also refers to pharmaceutical composition that has antagonistic effect on muscarine receptor M3, on the basis of said compound.

EFFECT: production of new compound and pharmaceutical composition on its basis, which can be applied in the medicine as an active substance for preventive and/or therapeutic drug for treatment of inflammatory diseases such as chronic obstructive pulmonary disease (COPD), asthma and the like.

14 cl, 60 tbl, 15 ex

FIELD: chemistry.

SUBSTANCE: described is a method of producing 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide by reacting 1-azabicyclo[2.2.2]oct-3(R)yl ether of 2-hydroxy-2,2-dithien-2-ylacetic acid and 3-phenoxypropyl bromide, where the reaction takes place in a solvent or mixtures of solvents, having boiling point ranging from 50 to 210°C and selected from a group comprising ketones and cyclic ethers, preferably in acetone, dioxane and tetrahydrofuran.

EFFECT: efficient method of obtaining the compounds.

12 cl, 8 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing (R)- quinuclidin-3-yl 6-((3S,4R)-4-(4-amino-5-chloro-2-methoxybenzamide)-3-methoxypiperidin-1-yl)hexanoate or salt thereof, involving: 1) converting a compound which is 4-amino-3-methoxypiperidine-1-carboxylate to a salt; 2) converting the ethyl 4-amino-3-methoxypiperidine-1-carboxylate salt into ethyl 4-(diphenylamine)-3-methoxypiperidine-1-carboxylate 3) treating ethyl 4-(diphenylamino)-3-methoxypiperidine-1-carboxylate with hydroxide or hydride of an alkali metal to obtain 3-methoxy-N,N-diphenylpiperidine-4-amine 4) obtainijng a chiral salt of the cis-isomer of 3-methoxy-N,N-diphenylpiperidine-4-amine by bringing 3-methoxy-N,N-diphenylpiperidine-4-amine into contact with a chiral splitting agent and extracting the obtained chiral salt of the cis-isomer of 3-methoxy-N,N-diphenylpiperidine-4-amine; optional recrystalisation of product 4; converting product 4 or 5 to a base to obtain product 4 or 5 in form of a free base; 7) bringing product 6 into contact with ethyl 6-bromohexanoate to obtain ethyl 6-((3S,4R)-4-(diphenylamine)-3-methoxypiperidin-1-yl)hexanoate 8) esterification of ethyl 6-((3S,4R)-4-(diphenylamine)-3-methoxypiperidin-1-yl)hexanoate using (R)-quinuclidin-3-ol with a Lewis acid to obtain (R)- quinuclidin-3-yl 6-((3S,4R)-4-(diphenylamine)-3-methoxypiperidin-1-yl)hexanoate 9) removing protection from the 4-amine group of product 8 to obtain (R- quinuclidin-3-yl 6- [(3S,4R)-4-amino-3-methoxypiperidin-1-yl)hexanoate; 10) acylation of product 9 4-amino-5-chloro-2-methoxybenzoic acid to obtain (R)- quinuclidin-3-yl 6-((38,4R)-4-(4-amino-5-chloro-2-methoxybenzamide)-3-methoxypiperidin-1-yl)hexanoate; 11) optional conversion of product 10 into a salt.

EFFECT: method increases output of the end product and reduces content of impurities.

7 cl, 3 ex, 6 tbl, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound of formula I where X1-X4 each independently represent CR1, B represents -C(O)-O- or -C(O)-NH-CH2-, Y represents S or NH, R1 represents H, C1-C4alkoxy, unsubstituted or substituted by once or several times with F, or Het, and Het stands for heterocyclic group, fully saturated, partly saturated or fully unsaturated, containing in cycle 5-10 atoms, of which at least one atom represents N, O or S, unsubstituted or substituted once or several times with C1-C8alkyl, or to its pharmaceutically acceptable salt.

EFFECT: obtaining pharmaceutical composition for selective activation/stimulation of nicotine receptors α7 on the basis of said compound, as well as to their application for treatment of patient, suffering from psychotic disease, neurodegenerative disease, including cholinergic system dysfunction and/or condition of memory failure and/or failure of cognitive abilities.

52 cl, 38 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I in which A denotes X denotes O; R denotes H; R1 denotes OH, CN, a nitro group, NH2, NR2CSR8, NR2CONR2R9, NR2C SNR2R9, NR2SO2R10, NR2CONR6R7, NR2CSNR6R7, NR2R9, SO2R10, SOR10, alkyl containing 1-4 carbon atoms, fluorinated alkyl containing 1-4 carbon atoms, alkenyl containing 2-6 carbon atoms, alkynyl containing 2-6 carbon atoms, where each alkyl, fluorinated alkyl, alkenyl or alkynyl group in each case is unsubstituted or substituted with Ar or He, cycloalkenyl containing 5-8 carbon atoms, alkoxy group containing 1-4 carbon atoms, cycloalkoxy group containing 3-7 carbon atoms, cycloalkylalkoxy group containing 4-7 carbon atoms, fluorinated alkoxy group containing 1-4 carbon atoms, fluorinated hydroxyalkyl containing 1-4 carbon atoms, hydroxyalkoxy group containing 2-4 carbon atoms, an ordinary hydroxyalkoxy group containing 2-4 carbon atoms, monoalkylamino group containing 1-4 carbon atoms, dialkylamine group, where each alkyl group independently contains 1-4 carbon atoms, alkoxycarbonyl containing 2-6 carbon atoms, Het or OAr; R2 denotes H, alkyl containing 1-4 carbon atom, cycloalkyl containing 3-7 carbon atoms, and cycloalkyl alkyl containing 4-7 carbon atoms; R6 and R7 independently denote H, alkyl containing 1-4 carbon atoms, cycloalkyl containing 3-7 carbon atoms, or cycloalkylalkyl containing 4-7 carbon atoms, or R6 and R7 together denote an alkylene group containing 4-6 carbon atoms, which forms a ring with an N atom; R8 denotes alkyl containing 1-4 carbon atoms, fluorinated alkyl containing 1-4 carbon atoms, alkenyl containing 3-6 carbon atoms, alkynyl containing 3-6 carbon atoms, where each alkyl, fluorinated alkyl, alkenyl or alkynyl group is unsubstituted or substituted with Ar, cycloalkyl containing 3-7 carbon atoms, or Het; R9 denotes Ar or Het; R10 denotes alkyl containing 1-4 carbon atoms which is unsubstituted or substituted with Ar, or NR6R7; Ar denotes an aryl group containing 6-10 carbon atoms, which is unsubstituted or substituted once or several times with an alkyl containing 1-8 carbon atoms, alkoxy group containing 1-8 carbon atoms, halogen, cyano group or combinations thereof; and Het denotes dihydropyranyl, tetrahydropyranyl, tetrahydrofuranyl, tetrahydrothienyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, isoxazolinyl, thiazolyl, oxazolyl, pyrrolyl, pyrazolyl, imidazolyl, pyridyl, pyrimidinyl, indolyl, quinolinyl, isoquinolinyl or naphthyridinyl, which is unsubstituted or substituted once or several times with halogen, aryl containing 6-10 carbon atoms, which is optionally substituted with alkyl containing 1-8 carbon atoms, alkoxy group containing 1-8 carbon atoms, oxo group, -CXR11 or combinations thereof, or R11 denotes alkyl containing 1-4 carbon atoms which is unsubstituted or substituted with Ar or Het; or pharmaceutically acceptable salts thereof, where formula IA is attached to the rest of the bonding molecule in the 3, 4 or 7 positions. The invention also relates to a pharmaceutical composition and to use of compounds in any of claims 1-37.

EFFECT: obtaining novel biologically active compounds, having nicotinic acetylcholine receptor subtype α7 ligand activity.

59 cl, 316 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I , in which A denotes hydrogen, B denotes methyl or B is in a trans-position relative oxygen; X denotes CH2; Y denotes a group of formula , , ,

, or ;

, in which the left-hand bond is to an oxygen atom, and the right-hand bond is to the group R; R denotes 5-indolyl; in form of a free base or an acid addition salt. The invention also relates to a pharmaceutical composition, to use of compounds in any of claims 1-7, to a method of preventing and treating psychiatric and neurodegenerative disorders in a person, as well as a method of treating and preventing diseases or pathological condition in which α7 nAChR activation plays a role.

EFFECT: obtaining novel biologically active compounds having α7 nAChR agonist activity.

16 cl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I

in form of a salt, where R1 and R2 each independently denotes phenyl, where one or both R1 and R2 are substituted in one, two or three positions by the following groups: halogen, C1-C8alkyl or C1-C8alkoxy, and R3 is hydroxy, or R1 and R2 each denotes an unsubstituted phenyl, and R is hydrogen, C1-C8alkyl, C1-C8alkoxy or C1-C8alkylthio, or R1 is C3-C8cycloalkyl and R2 is phenyl or a 5-member heterocycle containing at least one heteroatom in the ring selected from a group which includes oxygen and sulphur, and R3 is hydroxy, or -CR1R2R3 denotes 9-hydroxy- 9H-fluoren-9-yl or 9-hydroxy-9H-xanthen-9-yl, and R4 is C1-C8alkyl substituted in one, two or three positions by a -CO-N(R5)R6 group, where R5 is hydrogen and R6 is a 5-member heterocycle containing at least one heteroatom in the ring selected from a group which includes nitrogen and oxygen, optionally substituted with phenyl, or R1 and R2 each denotes an unsubstituted phenyl, and R3 is hydroxy and R4 is C1-C8alkyl substituted in one, two or three positions by a -CO-N(R5)R6 group, where R5 is hydrogen and R6 is 5-methyl-3-isoxazolyl or R1 and R2 each denote unsubstituted phenyl, and R3 is hydroxy and R4 is 1-ethyl substituted in one, two or three positions by a -CO-N(R5)R6 group, where R5 is hydrogen, R6 is a 5-member heterocycle containing at least one heteroatom in the ring selected from a group which includes nitrogen and oxygen, provided that the formula I compound is not (R)-3-(2-hydroxy-2,2-dithiophen-2-ylacetoxy)-1-(pyrazin-2-ylcarbamoylmethy)-1-azoniumbicyclo[2.2.2]octane, (R)-3-(2-hydroxy-2,2-dithiophen-2-ylacetoxy)-1-(isoxazol-3-ylcarbamoylmethyl)-1-azoniumbicyclo [2.2.2]octane bromide or (R)-3-(2-hydroxy-2,2-dithiophen-2-ylacetoxy)-1-(pyrimidin-4-ylcarbamoylmethyl)-1-azoniumbicyclo [2.2.2]octane bromide. The invention also relates to a pharmaceutical composition, to use of compounds in any of claims 1-8, as well as to methods for synthesis of formula I compounds.

EFFECT: obtaining new biologically active compounds which have M3 muscarinic receptor mediated activity.

14 cl, 254 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: compounds can be used to treat diseases mediated by the nicotinic acetylcholine receptor, such as derangement of memory. In general formulae , and A is an indazolyl, benzothiazolyl or isobenzothiazolyl group which corresponds to structural formulae a) to c) respectively or X is O; R1 is H, F, Cl, Br, I, cycloalkyl containing 3-7 carbon atoms, alkoxy which contains 1-4 carbon atoms, fluorinated alkoxy which contains 1-4 carbon atoms, Ar or Het; ; R2 is H; R3 is H; R4 is H, F, Cl, Br, I, cycloalkyl which contains 3-7 carbon atoms, alkoxy which contains 1-4 carbon atoms, fluorinated alkoxy which contains 1-4 carbon atoms, Ar or Het; R5 is H; Ar is an aryl group containing 6 carbon atoms which is unsubstituted or substituted once or several times with halogen; and Het is a 5- or 6-member heteroaromatic group containing a heteroatom in the ring which is selected from N, O and S, or a 6-member saturated heterocyclic group which contains a heteroatom in the ring which is selected from N and O; and their pharmaceutically acceptable salts, where, if the said compound has formula I, the indazolyl group of group A is bonded through its 3rd, 4th or 7th position, the benzothiazole group of group A is bonded through the 4th or 7th position, the isobenzothiazole group of group A is bonded through the 3rd, 4th or 7th position.

EFFECT: obtaining compounds with properties of nicotinic acetylcholine receptor (nAChR) ligands, and pharmaceutical compositions based on the said compounds.

53 cl, 95 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula where R1, R2 and R3 are independently selected from a group consisting of hydrogen, halogen and lower alkyl containing 1-6 carbon atoms; R4 denotes a residue given in the claim; R5 denotes hydrogen or methyl; R10 is selected from a group consisting of: (i) hydrogen; (ii) (C1-C10) alkyl; (iii) (C1-C10)alkyl, substituted with one or more substitutes independently selected from a group consisting of -N(CH3)2, morpholinyl, (C1-C4) alkoxy, hydroxyl, -CON(CH3)2 and halogen; (iv) monocyclic (C3-C8) cycloalkyl containing one N heteroatom; (v) 9-methyl-9-azabicyclo[3.3.1]nonane; (vi) phenyl; (vii) phenyl substituted with one or more (C1-C4)alkoxy; R11 is selected from a group consisting of hydrogen and (C1-C10)alkyl; or R10, R11 and a nitrogen atom with which they are bonded, together, form a nitric heterocycle or a substituted nitric heterocycle, such as given in the claim. The invention also relates to a pharmaceutical composition, having serotonin type 3 receptor modulating capacity and a method of treating a disorder which depends on serotonin type 3 receptor modulation.

EFFECT: compounds of formula II as serotonin type 3 receptor modulators.

18 cl, 1 tbl, 159 ex

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