THIENO[2,3-c]QUINOLIN-4-ONE DERIVATIVES, USEFUL IN TREATMENT OF ERK-DEPENDENT DISEASE Russian patent published in 2016 - IPC C07D495/04 A61K31/4743 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, namely to thieno[2,3-c]quinolin-4-one derivatives of general formula or to their pharmaceutically acceptable salts, where R¹ is selected from the group, consisting of hydrogen, halogen, C₁-C₆alkyl, C₂-C₆alkenyl and C₂-C₆alkinyl; R² is selected from the group, consisting of hydrogen and halogen; R³ is selected from the group, consisting of hydrogen, hydroxyl, C₁-C₆alkoxy, cyano, -OCOR¹⁰³, where R¹⁰³ represents C₁-C₆ alkyl, and -OCOOR¹⁰⁴, where R¹⁰⁴ represents C₁-C₆ alkyl; and R⁴ is selected from the group, consisting of C₂-C_6alkenyl, C₆-C₁₀ aryl, indanyl, heteroaryl and 3-8-membered heterocycloalkyl, and R⁴ is optionally substituted with substituent A; where substituent A is independently selected from the group, consisting of hydroxyl; halogen; C₁-C₆ alkyl, optionally substituted with substituent B; C₃-C₆cycloalkyl, optionally substituted with cyano or C₁-C₆alkyl, substituted with -NR³¹R³², where R³¹ and R³²represent hydrogen; -NR²¹R²², where each R²¹ and R²² independently represents hydrogen; C₁-C₆alkyl; -SO₂NR²³R²⁴, where each R²³ and R²⁴ independently represents hydrogen; C₁-C₆alkyl, optionally substituted with halogen; -NHSO₂(C₁-C₆alkyl); 6-membered heterocycloalkyl, selected from piperazinyl or piperadinyl, substituted with -NR³⁹R⁴⁰, in which each R³⁹ and R⁴⁰ independently represents hydrogen, C₁-C₆alkyl or C₁-C₆alkylsulphonyl; -COR¹², where R¹² represents C₁-C₆alkyl; where substituent B is independently selected from the group, consisting of hydroxyl; cyano; C_3-5cycloalkyl; 5-6-membered heterocycloalkyl, selected from pyrrolidinyl or piperidinyl, optionally substituted with hydroxyl, amino, C₁-C₆aminoalkyl or C₁-C₆alkyl, substituted with C₂-C₄alkyloxycarbonylamino; -NR⁵¹R⁵², where each R⁵¹ and R⁵² independently represents hydrogen; C₁-C₆alkyl, C₁-C₆ alkylsulphonyl or C₅cycloalkyl; -SO₂NR¹⁰⁶R¹⁰⁷, where R¹⁰⁶ and R¹⁰⁷ represent hydrogen; where R⁵ represents hydrogen; and where represents structure -S-CR⁷=CR⁶-, where R⁶ represents hydrogen; where R⁷ is selected from the group, consisting of hydrogen;halogen; C₁-C₆ alkyl. Invention also relates to pharmaceutical composition and ERK inhibitor, based on formula I compound, method for treatment of ERK-dependent disease, and application of formula I compound.

EFFECT: novel thieno[2,3-c]quinolin-4-one derivatives, suitable for treatment of ERK-associated diseases, including cancer, have been obtained.

12 cl, 5 tbl, 1313 ex