New 2,3-Dihydro-1H-pyrrolo[3,2-b]pyridine Derivatives as Sigma Ligands

A compound of formula (I):

• or a corresponding salt, a co-crystal, or a prodrug thereof, or a corresponding solvate thereof, wherein
• R1 is selected from the group consisting of hydrogen, halogen, unsubstituted or substituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
• R2 is selected from the group consisting of hydrogen, halogen, unsubstituted or substituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
• R3 is selected from the group consisting of hydrogen, halogen, unsubstituted or substituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted heterocyclyl, CN and OR3′, wherein R3′ is unsubstituted or substituted C1-6 alkyl or hydrogen;
• R4 is selected from the group consisting of hydrogen, halogen, unsubstituted or substituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted heterocyclyl and CN;
• A is a linear or cyclic amine selected from the group consisting of:
• wherein
• X is a N-containing heterocyclyl wherein said heterocyclyl is a saturated heterocyclyl;
• Y is a N-containing heterocyclyl, wherein said heterocyclyl is a saturated heterocyclyl containing 1 to 2 nitrogen atoms;
• Z is a C4-6-cycloalkyl or a N-containing heterocyclyl wherein said heterocyclyl is a saturated heterocyclyl;
• m is 0, 1 or 2;
• n is 0, 1 or 2;
• p is 0, 1 or 2;
• q is 0, 1 or 2;
• r is 0, 1 or 2;
• R5 is selected from the group consisting of substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkylheterocyclyl;
• R5′ is selected from the group consisting of hydrogen and substituted or unsubstituted C1-6 alkyl;
• R5″ and R5′″ are independently selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
• alternatively, R5″ and R5′″ may form, together with the nitrogen atom to which they are attached, a substituted or unsubstituted N-containing heterocyclyl;
• and
• R5iv is selected from the group consisting of hydrogen, halogen and OR6, wherein R6 is substituted or unsubstituted C1-6 alkyl or a hydrogen.

The compound according to claim 1, wherein said compound is selected from the group consisting of:

• N-(1-Benzylpiperidin-4-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(2-(dimethylamino)-2-phenylethyl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(2-(dimethylamino)-2-phenylethyl)-3,3-dimethyl-5-(trifluoromethyl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(2-(dimethylamino)-2-phenylethyl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(2-(dimethylamino)-2-phenylethyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(2-(dimethylamino)-2-phenylethyl)-5-methyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• 3,3,5-trimethyl-N-(2-phenyl-2-(pyrrolidin-1-yl)ethyl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(2-(dimethylamino)-2-phenylethyl)-N,3,3,5-tetramethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(2-(diethylamino)-2-phenylethyl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (4-benzylpiperazin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-(benzyl(methyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone
• (S)—N-(2-(dimethylamino)-3-phenylpropyl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(2-(dimethylamino)-2-(4-methoxyphenyl)ethyl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)-6-chloro-N-(2-(dimethylamino)-2-phenylethyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)-5-cyano-N-(2-(dimethylamino)-2-phenylethyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(2-(dimethylamino)-2-phenylethyl)-6-fluoro-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(2-(dimethylamino)-2-phenylethyl)-5-methoxy-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(1-benzylpyrrolidin-3-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(2-(dimethylamino)-2-(2-fluorophenyl)ethyl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(2-(dimethylamino)-2-phenylethyl)-6-fluoro-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (S)—N-(1-benzylpyrrolidin-3-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(1-(4-fluorobenzyl)piperidin-4-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(1-(3-cyanobenzyl)piperidin-4-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(1-(4-cyanobenzyl)piperidin-4-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(1-isopentylpiperidin-4-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(1-(3-fluorobenzyl)piperidin-4-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• 3,3,5-trimethyl-N-(1-phenethylpiperidin-4-yl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(1-(2-ethoxyethyl)piperidin-4-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (4-(benzyl(methyl)amino)piperidin-1-yl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• N-(1-benzylpiperidin-4-yl)-5-cyano-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(1-benzylpiperidin-4-yl)-6-fluoro-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(1-benzylpiperidin-4-yl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(2-(dimethylamino)-2-(4-fluorophenyl)ethyl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(2-(dimethylamino)-2-(3-fluorophenyl)ethyl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(2-(dimethylamino)-2-(3-methoxyphenyl)ethyl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• ((3 aR,6aS)-5-benzylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (7-benzyl-2,7-diazaspiro[4.4]nonan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (2-benzyl-2,8-diazaspiro[4.5]decan-8-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (S)-(3-(benzyl(methyl)amino)pyrrolidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• 1-(4-(benzyl(methyl)amino)piperidine-1-carbonyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-5-carbonitrile;
• N-(1-isobutylpiperidin-4-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• 3,3,5-trimethyl-N-(1-((tetrahydro-2H-pyran-4-yl)methyl)piperidin-4-yl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)-(3-(benzyl(methyl)amino)pyrrolidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• N-(1-(3,4-difluorobenzyl)piperidin-4-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• 5-(((1-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)piperidin-4-yl)(methyl)amino)methyl)-2-fluorobenzonitrile;
• N-(1-(3,4-difluorobenzyl)piperidin-4-yl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(1-(3-fluorobenzyl)piperidin-4-yl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-(1-(4-fluorobenzyl)piperidin-4-yl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (4-(benzyl(methyl)amino)piperidin-1-yl)(5-methyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-(methyl(phenethyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-(benzyl(methyl)amino)piperidin-1-yl)(2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(4-(methyl(phenethyl)amino)piperidin-1-yl)methanone;
• (S)-(2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(3-(methyl(phenethyl)amino)piperidin-1-yl)methanone;
• (S)-(3-(methyl(phenethyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• N-(1-(3-chlorobenzyl)piperidin-4-yl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (4-(methyl(3-(methylsulfonyl)benzyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (9-benzyl-3,9-diazaspiro [5.5]undecan-3-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-((4-methoxybenzyl)(methyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-((3-methoxybenzyl)(methyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• 2-fluoro-5-((methyl(1-(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)piperidin-4-yl)amino)methyl)benzonitrile;
• (S)-(3-(benzyl(methyl)amino)piperidin-1-yl)(2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (S)-(2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(3-(methyl(phenethyl)amino)pyrrolidin-1-yl)methanone;
• N,N-dimethyl-3-((methyl(1-(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)piperidin-4-yl)amino)methyl)benzamide;
• (S)-(2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(3-(isopentyl(methyl)amino)piperidin-1-yl)methanone;
• (4-(methyl((tetrahydro-2H-pyran-4-yl)methyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-((benzyl(methyl)amino)methyl)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-(isopentyl(methyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-((4-(dimethylamino)benzyl)(methyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• N-((1-benzylpiperidin-4-yl)methyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• 3,3-dimethyl-N-((1-phenethylpiperidin-4-yl)methyl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-((1r,4r)-4-(benzyl(methyl)amino)cyclohexyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• N-((1s,4s)-4-(benzyl(methyl)amino)cyclohexyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (4-(methyl(pyridin-2-ylmethyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-(methyl(pyridin-3-ylmethyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-(methyl(pyridin-4-ylmethyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• 3-(((1-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)piperidin-4-yl)(methyl)amino)methyl)-5-fluorobenzonitrile;
• 3-(((1-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)piperidin-4-yl)(methyl)amino)methyl)-4-fluorobenzonitrile;
• N-((1r,4r)-4-(benzyl(methyl)amino)cyclohexyl)-N,3,3-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (4-((3,4-Difluorobenzyl)(methyl)amino)piperidin-1-yl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (8-benzyl-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (6-benzyl-2,6-diazaspiro[3.3]heptan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• N-((1-benzylazetidin-3-yl)methyl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• 3-(((1-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)piperidin-4-yl)(methyl)amino)methyl)benzonitrile;
• 4-(((1-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)piperidin-4-yl)(methyl)amino)methyl)benzonitrile;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(4-((3-fluorobenzyl)(methyl)amino)piperidin-1-yl)methanone;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(4-(4-fluorobenzyl)(methyl)amino)piperidin-1-yl)methanone;
• 4-(((1-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)piperidin-4-yl)(methyl)amino)methyl)-2-fluorobenzonitrile;
• N-(1-benzylazetidin-3-yl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (8-benzyl-2,8-diazaspiro[4.5]decan-2-yl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• 3-((2-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-2,8-diazaspiro[4.5]decan-8-yl)methyl)benzonitrile;
• (8-phenethyl-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• 3-((2-(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-2,8-diazaspiro[4.5]decan-8-yl)methyl)benzonitrile;
• (2-benzyl-2,7-diazaspiro[3.5]nonan-7-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (8-(pyridin-2-ylmethyl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (8-(3-methoxybenzyl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (8-(1-phenylethyl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (S)-(2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(3-(phenethylamino)pyrrolidin-1-yl)methanone;
• (8-(pyridin-3-ylmethyl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (8-(pyridin-4-ylmethyl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (8-isopentyl-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (S)-(2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(3-(phenethylamino)piperidin-1-yl)methanone;
• (8-(3-(methylsulfonyl)benzyl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (8-(4-methoxybenzyl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• N-(7-benzyl-7-azaspiro[3.5]nonan-2-yl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (8-((tetrahydro-2H-pyran-4-yl)methyl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• N-((1-isopentylpiperidin-4-yl)methyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• 2-fluoro-5-((2-(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-2,8-diazaspiro[4.5]decan-8-yl)methyl)benzonitrile;
• (8-(2-(tetrahydro-2H-pyran-4-yl)ethyl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• N-((1-(3,3-Dimethylbutyl)piperidin-4-yl)methyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (8-(tetrahydro-2H-pyran-4-yl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (S)-3,3,5-Trimethyl-N-(2-(methylamino)-2-phenylethyl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)-3,3,5-trimethyl-N-(2-(methylamino)-2-phenylethyl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (R)—N-(2-(ethylamino)-2-phenylethyl)-3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxamide;
• (4-((4-Fluorobenzyl)(methyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-(benzylamino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (4-((3-fluorobenzyl)(methyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• 4-((methyl(1-(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)piperidin-4-yl)amino)methyl)benzonitrile;
• 3-((methyl(1-(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)piperidin-4-yl)amino)methyl)benzonitrile;
• (4-(isobutyl(methyl)amino)piperidin-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone
• (3-(Isopentylamino)azepan-1-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (S)-(2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(3-(isopentylamino)azepan-1-yl)methanone;
• (S)-(2,3-Dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(3-(isopentyl(methyl)amino)azepan-1-yl)methanone;
• (1-Benzylpiperidin-4-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((3S,4S)-1-benzyl-4-methylpyrrolidin-3-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((3R,4R)-1-benzyl-4-methylpyrrolidin-3-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1s,4s)-4-(benzyl(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1s,4s)-4-(benzyl(methyl)amino)cyclohexyl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(Benzylamino)cyclohexyl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone dihydrochloride;
• ((1r,4r)-4-(benzylamino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone dihydrochloride;
• 2-(1-Benzylpiperidin-4-yl)-1-(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)ethanone;
• (1-benzylazetidin-3-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (1-benzylazetidin-3-yl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (1-(4-fluorobenzyl)azetidin-3-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,3r)-3-(benzylamino)cyclobutyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (1-(3-fluorobenzyl)azetidin-3-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1s,3s)-3-(benzylamino)cyclobutyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,3r)-3-(Benzyl(methyl)amino)cyclobutyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(benzyl(methyl)amino)cyclohexyl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1s,3s)-3-(benzyl(methyl)amino)cyclobutyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(benzyl(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(8-(2-fluorobenzyl)-2,8-diazaspiro[4.5]decan-2-yl)methanone;
• 4-((2-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-2,8-diazaspiro[4.5]decan-8-yl)methyl)-2-fluorobenzonitrile;
• 5-((2-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-2,8-diazaspiro[4.5]decan-8-yl)methyl)-2-fluorobenzonitrile;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(8-((tetrahydro-2H-pyran-4-yl)methyl)-2,8-diazaspiro[4.5]decan-2-yl)methanone;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(9-(2-fluorobenzyl)-3,9-diazaspiro [5 0.5]undecan-3-yl)methanone;
• 4-((9-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-3,9-diazaspiro [5 0.5]undecan-3-yl)methyl)-2-fluorobenzonitrile;
• 5-((9-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-3,9-diazaspiro [5 0.5]undecan-3-yl)methyl)-2-fluorobenzonitrile;
• (8-(2,5-difluorobenzyl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(8-(4-fluorobenzyl)-2,8-diazaspiro[4.5]decan-2-yl)methanone;
• (8-(2,6-difluorobenzyl)-2,8-diazaspiro[4.5]decan-2-yl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• 4-((2-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-2,8-diazaspiro[4.5]decan-8-yl)methyl)benzonitrile;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(8-(3-fluorobenzyl)-2,8-diazaspiro[4.5]decan-2-yl)methanone;
• 3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(8-(3-fluoropyridin-2-yl)methyl)-2,8-diazaspiro[4.5]decan-2-yl)methanone;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(8-(5-fluoropyridin-2-yl)methyl)-2,8-diazaspiro[4.5]decan-2-yl)methanone;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(8-((6-(trifluoromethyl)pyridin-3-yl)methyl)-2,8-diazaspiro[4.5]decan-2-yl)methanone;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(8-(2-(tetrahydro-2H-pyran-4-yl)ethyl)-2,8-diazaspiro[4.5]decan-2-yl)methanone;
• 4-((2-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-2,8-diazaspiro[4.5]decan-8-yl)methyl)-3-fluorobenzonitrile;
• 5-((2-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-2,8-diazaspiro[4.5]decan-8-yl)methyl)-2,4-difluorobenzonitrile;
• (7-benzyl-2,7-diazaspiro[3.5]nonan-2-yl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (9-(2-fluorobenzyl)-3,9-diazaspiro[5.5]undecan-3-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (9-((tetrahydro-2H-pyran-4-yl)methyl)-3,9-diazaspiro[5.5]undecan-3-yl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• 2-fluoro-5-((9-(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-3,9-diazaspiro[5.5]undecan-3-yl)methyl)benzonitrile;
• 2-fluoro-44(9-(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-3,9-diazaspiro[5.5]undecan-3-yl)methyl)benzonitrile;
• (9-(2,5-difluorobenzyl)-3,9-diazaspiro[5.5]undecan-3-yl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• 4-((9-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-3,9-diazaspiro[5.5]undecan-3-yl)methyl)-3-fluorobenzonitrile;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)(9-((tetrahydro-2H-pyran-4-yl)methyl)-3,9-diazaspiro[5.5]undecan-3-yl)methanone;
• 5-((9-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)-3,9-diazaspiro[5.5]undecan-3-yl)methyl)-2,4-difluorobenzonitrile;
• ((1r,4r)-4-(3,5-difluorobenzyl)(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(3-fluorobenzyl)(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(3,4-difluorobenzyl)(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(2,6-difluorobenzyl)(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(2,4-difluorobenzyl)(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-((2,5-difluorobenzyl)(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-((2,3-difluorobenzyl)(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• (3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)((1 r,4r)-4-((2-fluorobenzyl)(methyl)amino)cyclohexyl)methanone;
• ((1r,4r)-4-((2,5-difluorobenzyl)(methyl)amino)cyclohexyl)(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(methyl((2-(trifluoromethyl)pyridin-4-yl)methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(((3-fluoropyridin-2-yl)methyl)(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(((5-fluoropyridin-2-yl)methyl)(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• 2-fluoro-4-((methyl((1 r,4r)-4-(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)cyclohexyl)amino)methyl)benzonitrile;
• 2-fluoro-5-((methyl((1 r,4r)-4-(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carbonyl)cyclohexyl)amino)methyl)benzonitrile;
• ((1r,4r)-4-((4-fluorobenzyl)(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-((2-fluorobenzyl)(methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(methyl((6-(trifluoromethyl)pyridin-3-yl)methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(methyl((tetrahydro-2H-pyran-4-yl)methyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(benzyl(methyl)amino)cyclohexyl)(3,3-dimethyl-5-(trifluoromethyl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• ((1r,4r)-4-(benzyl(methyl)amino)cyclohexyl)(6-fluoro-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone;
• and
• ((1r,4r)-4-((2-fluorobenzyl)amino)cyclohexyl)(3,3,5-trimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)methanone.

A process for producing a compound of formula (I):

• said process comprising treating a compound of formula (II)
• with an amine compound A in the presence of a carbonyl source under conditions sufficient to produce the compound of formula (I),
• wherein
• R1 is selected from the group consisting of hydrogen, halogen, unsubstituted or substituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
• R2 is selected from the group consisting of hydrogen, halogen, unsubstituted or substituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
• R3 is selected from the group consisting of hydrogen, halogen, unsubstituted or substituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted heterocyclyl, CN and OR3′, wherein R3′ is unsubstituted or substituted C1-6 alkyl or hydrogen;
• R4 is selected from the group consisting of hydrogen, halogen, unsubstituted or substituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted heterocyclyl and CN;
• A is a linear or cyclic amine compound selected from the group consisting of:
• wherein
• X is a N-containing heterocyclyl wherein said heterocyclyl is a saturated heterocyclyl;
• Y is a N-containing heterocyclyl, wherein said heterocyclyl is a saturated heterocyclyl containing 1 to 2 nitrogen atoms;
• Z is a N-containing heterocyclyl wherein said heterocyclyl is a saturated heterocyclyl;
• m is 0, 1 or 2;
• n is 0, 1 or 2;
• p is 0, 1 or 2;
• q is 0, 1 or 2;
• r is 0, 1 or 2;
• R5 is selected from the group consisting of substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkylheterocyclyl;
• R5′ is selected from the group consisting of hydrogen and substituted or unsubstituted C1-6 alkyl;
• R5″ and R5′″ are independently selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
• alternatively, R5″ and R5′″ may form, together with the nitrogen atom to which they are attached, a substituted or unsubstituted N-containing heterocyclyl;
• and
• R5iv is selected from the group consisting of hydrogen, halogen and OR6, wherein R6 is substituted or unsubstituted C1-6 alkyl or a hydrogen.