NITROGEN-CONTAINING HETEROARYL COMPOUNDS AND USE THEREOF IN INCREASING ENDOGENOUS ERYTHROPOIETIN Russian patent published in 2010 - IPC C07D217/22 C07D401/12 C07D401/04 A61K31/47 A61K31/4725 A61P9/10 A61P25/28 

FIELD: chemistry.

SUBSTANCE: novel isoquinoline derivatives are described by general formula I, where q equals zero; p equals zero or one; R^a is -COOH or WR⁸; under the condition that, if R^a is -COOH, then p equals zero, and if R^a is -WR⁸, then p equals one; W is selected from an oxygen atom and -NR⁹-, where R⁹ is selected from a group consisting of a hydrogen atom, acyl and alkyl; and R⁸ is selected from a group consisting of a hydrogen atom and alkyl; R¹ is selected from a group consisting of a hydrogen atom, alkyl, alkyl substituted with one group selected from alkoxy and dialkylamino, a halogen atom, heteroaryl containing up to six carbon atoms, one of which is nitrogen, aminoacyl, aryl, aryl substituted with alkyl, and -XR⁶, where X is an oxygen atom, -S(O)_n- or -NR⁷, where n equals zero, one or two, R⁶ is selected from a group consisting of alkyl, aryl, aryl substituted with one group selected from a halogen atom, alkoxy, alkylcarbonylamino and alkylsulfonamide, heteroaryl, containing up to six carbon atoms, one of which is nitrogen, and R⁷ is a hydrogen atom or aryl; R² and R³ are independently selected from a group consisting of a hydrogen atom, amino, amino substituted with alkoxy-substituted phenylsulfonyl, alkyl, alkyl substituted with up to three times by a halogen atom, aryl, halogen atom -NR⁶C(O)NR⁶R⁶, and -XR⁶, where X is an oxygen atom or -S(O)_n-, where n equals zero, one or two, each of the substitutes R⁶ is independently selected from a group consisting of hydrogen, alkyl, alkyl substituted with aryl, aryl , aryl substituted with one or two groups selected from a halogen atom, alkyl, alkyl substituted with up to three times by a halogen, alkoxy, alkoxy substituted with up to three times by a halogen, aryloxy substituted with a halogen, nitro, alkylsulfonamide, arylsulfonamide and alkyl-substituted arylsulfonamide, cycloalkyl, heteroaryl, containing up to six carbon atoms, one of which is nitrogen, under the condition that if X is -SO₂-, R⁶ cannot be a hydrogen atom; or R² and R³ together with carbon atoms to which they are bonded, are bonded with formation of an aryl group; R⁴ and R⁵ are independently selected from a hydrogen atom or aryl; R is selected from a group which includes a hydrogen atom, deuterium and methyl; R' is selected from a group consisting of a hydrogen atom, deuterium, alkyl or alkyl substituted with one group selected from hydroxyl, amino, carboxyl, aryl, aryl substituted with one hydroxyl and heteroaryl, containing up to five carbon atoms, two of which can be nitrogen; on the other hand, R and R' and the carbon atom to which they are bonded can be bonded with formation of cycloalkyl; R" is formed from a hydrogen atom and alkyl, or R" together with R' and the nitrogen atom to which they are bonded can be bonded with formation of a heterocyclic group containing up to six carbon atoms, one of which is nitrogen; R'" is selected from a group consisting of hydroxyl, alkoxy, alkoxy substituted with aryl, acyloxy, aryl, -S(O)_n-R¹⁰, where R¹⁰ is hydrogen, and n is zero; or its pharmaceutically acceptable salts, esters or amides; under the condition that restrictive conditions given in paragraph 1 of the formula of invention are met. The invention also relates to specific produced and described compounds, a pharmaceutical composition based on compounds with general formula I, a method of treating, preventing and pretreatment using said pharmaceutical composition, a method of inhibiting activity of hydrolase enzyme, based on taking an effective amount of a formula I compound, a composition for preventing and pretreatment, based on formula I compound and erythropoietin.

EFFECT: new isoquinoline derivatives have useful biological properties.

53 cl, 4 tbl, 253 ex