主权项 |
1. A compound of formulaor a tautomer, prodrug, N-oxide, pharmaceutically acceptable ester or pharmaceutically acceptable salt thereof, wherein
Ring Hy representsoptionally substituted with R′″;
R1 and R2 are the same or different and are independently selected from CH3, CH2F, CHF2, CF3, substituted or unsubstituted C(3-5)cycloalkyl, CH2—ORa, CH2—NRaRb, CN and COOH with the proviso that; a) both R1 and R2 at the same time do not represent CF3, b) both R1 and R2 at the same time do not represent CH3, c) when R1 is CF3 then R2 is not CH3 and d) when R1 is CH3 then R2 is not CF3; Ring Ar represents: L1 and L2 together represent —NH—C(═O)—; A is absent; R′ and R″ are the same or different and are independently selected from hydrogen, hydroxy, cyano, halogen, —ORa, —COORa, —S(═O)q—Ra, —NRaRb, —C(═X)—Ra, substituted or unsubstituted C(1-6) alkyl group, substituted or unsubstituted C(1-6) alkenyl, substituted or unsubstituted C(1-6) alkynyl, and substituted or unsubstituted C(3-5) cycloalkyl, or R′ and R″ may be joined to form a substituted or unsubstituted saturated or unsaturated 3-6 member ring, which may optionally include one or more heteroatoms which may be same or different and are selected from O, NRa and S; R′″ is selected from hydrogen, hydroxy, cyano, halogen, —ORa, —COORa, —S(═O)q—Ra, —NRaRb, —C(═X)—Ra, substituted or unsubstituted C(1-6) alkyl group, substituted or unsubstituted C(1-6) alkenyl, substituted or unsubstituted C(1-6) alkynyl, and substituted or unsubstituted C(3-5)cycloalkyl each occurrence of X is independently selected from O, S and —NRa; Cy is selected from monocyclic substituted or unsubstituted cycloalkyl group, and monocyclic substituted or unsubstituted aryl; each occurrence of Ra and Rb are the same or different and are independently selected from hydrogen, nitro, hydroxy, cyano, halogen, —ORc, —S(═O)q—Rc, —NRcRd, —C(═Y)—Rc, —CRcRd—C(═Y)—Rc, —CRcRd—Y—CRcRd—, —C(═Y)—NRcRd—, —NRRd—C(═Y)—NRcRd—, —S(═O)q—NRcRd—, —NRcRd—S(═O)q—NRcRd—, —NRcRd—NRcRd—, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylakyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocylyl, substituted or unsubstituted heterocyclylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, and substituted or unsubstituted heteroarylalkyl, or when Ra and Rb are directly bound to the same atom, they may be joined to form a substituted or unsubstituted saturated or unsaturated 3-10 member ring, which may optionally include one or more heteroatoms which may be the same or different and are selected from O, NRc and S; each occurrence of Rc and Rd may be same or different and are independently selected from hydrogen, nitro, hydroxy, cyano, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylakyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted heterocyclylalkyl, or when two Rc and/or Rd substitutents are directly bound to the same atom, they may be joined to form a substituted or unsubstituted saturated or unsaturated 3-10 member ring, which may optionally include one or more heteroatoms which are the same or different and are selected from O, NH and S; each occurrence of Y is selected from O, S and —NRa; and each occurrence of q independently represents 0, 1 or 2. |