| CPC C07D 403/12 (2013.01) [A61P 35/00 (2018.01); C07D 405/12 (2013.01); C07D 491/048 (2013.01)] | 27 Claims |
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1. A compound of the general formula (I), its tautomeric form, its stereoisomer, its pharmaceutically acceptable salt, its polymorph, or solvate thereof,
 wherein
Ring A is selected from aryl, heteroaryl, and heterocyclyl;
‘- - -’ is either a single bond or double bond;
X and Y are independently selected from CH, CH2, O, and NRc, provided that both X and Y cannot be O at the same time;
R1 is selected from hydrogen and substituted or unsubstituted alkyl;
R2 is selected from hydrogen, halogen, alkyl, and cycloalkyl;
R3 is selected from —OR6, —NRaRb, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, alkyl substituted with substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroaryl, and substituted or unsubstituted heterocyclyl;
R4 is selected from oxo and substituted or unsubstituted alkyl;
R5 is selected from halogen, cyano, —NRcRd, substituted or unsubstituted alkyl, —C(═O) substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; optionally two R5 groups attached to the adjacent carbon atoms forming substituted or unsubstituted heterocycle;
R6 is selected from substituted or unsubstituted alkyl, substituted or unsubstituted heterocyclyl, and alkyl substituted with substituted heterocyclyl;
Ra and Rb are independently selected from hydrogen, substituted or unsubstituted alkyl, and substituted or unsubstituted heterocyclyl;
Rc and Rd are independently selected from hydrogen and alkyl;
m is an integer selected from 0, 1, 2, and 3;
n is an integer selected from 0, 1, 2, 3, and 4;
when an alkyl group is substituted, it is substituted with 1 to 5 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 a cycloalkyl group is substituted, it is substituted with 1 to 4 substituents independently selected from oxo (—O), halogen, alkyl, hydroxyalkyl, cyano, 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, haloalkyl, perhaloalkyl, cycloalkyl, heterocyclyl, heteroaryl, —OR7, —NR8R8a, —NR8C(—O) R9, —C(—O) R9, —C(═O) NR8R8a, —SO2-alkyl, —C(═O) OH, and —C(═O)O-alkyl;
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, haloalkyl, alkoxyalkyl, hydroxyalkyl, 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, haloalkyl, 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.
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