Substituted thiazolo-pyridine compounds as malt1 inhibitors

A compound of the general formula (I), a tautomer thereof, a stereoisomer thereof, a polymorph thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof,

• wherein,
• R1 is selected from hydrogen, halogen, cyano, substituted or unsubstituted alkyl, and cycloalkyl;
• R2 is selected from—
• a) alkyl or alkyl substituted with 1 to 4 substituents independently selected from oxo (═O), halogen, cyano, cycloalkyl, substituted or unsubstituted aryl, heteroaryl, substituted or unsubstituted heterocyclyl, —OR4, —C(═O)OH, —SO2(alkyl), —C(═O)O(alkyl), —NR5R5a, —NR5C(═O)R6, †C(═O)R6, and †C(═O)NR5R5a,
• b) cycloalkyl or cycloalkyl substituted with 1 to 4 substituents independently selected from halogen, cyano, substituted or unsubstituted alkyl, —OR4, —C(═O)OH, —C(═O)O(alkyl), C(═O)R6, and C(═O)NR5R5a,
• c) cycloalkenyl,
• d) cyano,
• e) substituted or unsubstituted aryl,
• f) substituted or unsubstituted heteroaryl,
• g) heterocyclyl or heterocyclyl substituted on either ring carbon atom or a ring nitrogen atom and when it is substituted on ring carbon atom it is substituted with 1 to 4 substituents independently selected from oxo (═O), halogen, cyano, substituted or unsubstituted alkyl, cycloalkyl, —OR4, —C(═O)OH, —C(═O)O-alkyl, —C(═O)NR5N5a, —N(H)C(═O)(alkyl), —N(H)R5, and —N(alkyl)2, and when the heterocycle group is substituted on a ring nitrogen, it is substituted with substituents independently selected from alkyl, cycloalkyl, aryl, heteroaryl, —SO2(alkyl), C(═O)R6, C(═O)O(alkyl), —C(═O)N(H)R5, and —C(═O)N(alkyl)R5, and
• h) —NRaRb, wherein, Ra and Rb are independent selected from hydrogen, cycloalkyl, and alkyl or alkyl substituted with 1 to 4 substituents independently selected from oxo (═O), halogen, cycloalkyl, —OR4, and substituted or unsubstituted aryl;
• R3 is selected from—
• a) heteroaryl or heteroaryl substituted with 1 to 4 substituents selected from halogen, cyano, —COOR4b, —OR4a, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, nitro, —SO2alkyl, —SO2NH(alkyl), —SO2NH2, —SO2NH(CF3), —SO2N(alkyl)2, —NHSO2(alkyl), —COR6, —CON(H)OH, —CONR5R5a, —N(R5)COR5a, and —NR5R5a,
• b) aryl or aryl substituted with 1 to 4 substituents selected from halogen, cyano, —COOR4b, —OR4a, substituted or unsubstituted alkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, nitro, —SO2alkyl, —SO2NH(alkyl), —SO2NH2, —SO2NH(CF3), —SO2N(alkyl)2, —NHSO2(alkyl), —COR6, —CONR5R5a, —CO(NH)OH, —N(R5)COR5a, —NR5R5a, and heteroaryl or heteroaryl substituted with 1 to 4 substituents selected from substituted or unsubstituted alkyl,
• c) heterocyclyl or heterocyclyl substituted with 1 to 4 substituents selected from oxo (═O) and substituted or unsubstituted alkyl, and
• d)
• wherein, X is halogen and ring A is a heterocyclic ring containing heteroatom(s) selected from S, O, and N, which is optionally substituted with an oxo (═O) group;
• R4 is selected from hydrogen, cycloalkyl, and substituted or unsubstituted alkyl;
• R4a is selected from
• a) hydrogen, alkyl, and cycloalkyl, and
• b) alkyl substituted with 1 to 4 substituents independently selected from halogen, —O-alkyl, —NR5R5a, and substituted or unsubstituted heterocyclyl;
• R4b is selected from hydrogen and alkyl;
• R5 and R5a are each independently selected from
• a) hydrogen, alkyl, and cycloalkyl,
• b) alkyl substituted with O-alkyl, NH2, and —CONH2,
• c) heteroaryl, and
• d) heterocyclyl substituted with alkyl;
• and
• R6 is selected from alkyl, heterocyclyl, and cycloalkyl;
• when an alkyl group is substituted, it is substituted with 1 to 4 substituents independently selected from oxo (═O), halogen, cyano, cycloalkyl, aryl, heteroaryl, heterocyclyl, —OR7, —C(═O)OH, —C(═O)O(alkyl), —NR8R8a, —NR8C(═O)R9, and C(═O)NR8R8a;
• when the aryl group is substituted, it is substituted with 1 to 4 substituents independently selected from halogen, nitro, cyano, alkyl, perhaloalkyl, cycloalkyl, heterocyclyl, heteroaryl, —OR7, —NR8R8a, —NR8C(═O)R9, C(═O)R9, C(═O)NR8R8a, —SO2-alkyl, —C(═O)OH, —C(═O)O-alkyl, and haloalkyl;
• when the heteroaryl group is substituted, it is substituted with 1 to 4 substituents independently selected from halogen, nitro, cyano, alkyl, haloalkyl, perhaloalkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, —OR7, —NR8R8a, —NR7C(═O)R9, C(═O)R9, C(═O)NR8R8a, —SO2-alkyl, —C(═O)OH, and —C(═O)O-alkyl;
• when the heterocycle group is substituted, it is substituted either on a ring carbon atom or on a ring hetero atom, and when it is substituted on a ring carbon atom, it is substituted with 1 to 4 substituents independently selected from oxo (═O), halogen, cyano, alkyl, cycloalkyl, perhaloalkyl, —OR7, C(═O)NR8R8a, —C(═O)OH, —C(═O)O-alkyl, —N(H)C(═O)(alkyl), —N(H)R8, and —N(alkyl)2;
• and when the heterocycle group is substituted on a ring nitrogen, it is substituted with substituents independently selected from alkyl, cycloalkyl, aryl, heteroaryl, —SO2(alkyl), C(═O)R9, and —C(═O)O(alkyl);
• when the heterocycle group is substituted on a ring sulfur, it is substituted with 1 or 2 oxo (═O) group(s);
• R7 is selected from hydrogen, alkyl, perhaloalkyl, and cycloalkyl;
• R8 and R8a are each independently selected from hydrogen, alkyl, and cycloalkyl;
• and
• R9 is selected from alkyl and cycloalkyl.