INDOL-3-YL-CARBONYL-PIPERADINE-BENZIMIDAZOLE DERIVATIVES AS V1A RECEPTOR ANTAGONISTS Russian patent published in 2011 - IPC C07D403/12 C07D413/14 A61K31/422 A61P25/24 A61P9/04 A61P9/12 A61P1/16 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of general formula (I) , where the dotted line is either absent or denotes a double bond; R¹ denotes H or C_1-6-alkyl, possibly substituted with a CN group, or denotes a phenyl or sulphonyl phenyl, substituted with one or more B groups, or denotes -(CH₂)_m-R^a, where R^a denotes: NRⁱRⁱⁱ, C_3-6-cycloalkyl, 6-member heterocycloalkyl, which denotes a univalent saturated group which contains one nitrogen heteroatom, the rest are carbon atoms, aryl, which can be substituted with one or more B groups, or denotes -(CH₂)_n-(CO)-R^b or -(CH₂)_n-(SO₂)-R^b, where R^b denotes: NRⁱRⁱⁱ, 5-6-member heterocycloalkyl, which denotes a univalent saturated group containing one or more heteroatoms selected from nitrogen, oxygen, the rest are carbon atoms, aryl or 5- or 6-member heteroaryl, which denotes an aromatic ring containing two heteroatoms as ring members, the said heteroatoms selected from N or O, the rest are carbon atoms; which can possibly be substituted with one or more B groups, R² denotes one or more H, halo, C_1-6-alkyl, C_1-6-alkoxy, R³ denotes H or-(CO)-R^c, where R^c denotes: C_1-6-alkyl, 5-member heterocycloalkyl, which denotes a univalent saturated group containing one nitrogen heteroatom, the rest are carbon atoms possibly substituted with C_1-6-alkyl, or denotes C_1-6-alkyl; R⁴ denotes H; R⁵ denotes H, C_1-6-alkyl, -(CH₂)_m-NRⁱRⁱⁱ, -(CH₂)_n-(CO)-R^b, where R^b denotes NRⁱRⁱⁱ or a 6-member heterocycloalkyl which denotes a univalent saturated group which contains one nitrogen heteroatom, the rest are carbon atoms, when the dotted line is absent or is absent when the dotted line denotes a double bond; R⁶ is absent, when the dotted line denotes a double bond; R⁷ denotes Cl or NR^eR^f, where R^e and R^f denotes H or C_1-6-alkyl, or R^e and R^f together with the nitrogen atom to which they are bonded form a 6-member heterocycloalkyl which denotes a univalent saturated group containing one or two heteroatoms selected from nitrogen, oxygen, the rest are carbon atoms; which can be substituted with C_1-6-alkyl, or R⁶ and R⁷ together form a C=O group, when the dotted line is absent; B denotes halogen, C_1-6-alkoxy, (CRⁱⁱⁱR^iv)n-phenyl; Rⁱ and Rⁱⁱ denote H, C_1-6-alkyl -C(O)-C_1-6-alkyl; Rⁱⁱⁱ and R^iv denote C_1-6-alkyl; m equals to 1 or 2, n equals 0 or 1; as well as to pharmaceutically acceptable salts thereof. The invention also relates to a pharmaceutical composition, as well as to use of compounds of formula (I), (I-a) or (1-b).

EFFECT: obtaining novel biologically active compounds having activity on V1a receptor.

12 cl, 48 ex