| 主权项 |
1. A compound of formula or a tautomer, prodrug, N-oxide, pharmaceutically acceptable ester or pharmaceutically acceptable salt thereof, wherein
Ring Hy represents optionally 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 andd) when R1 is CH3 then R2 is not CF3;Ring Ar represents: T, U, V and W are the same or different and are independently selected from CR1 and N;Z1, Z2 and Z3 are the same or different and are independently selected from CRa, CRaRb, O, S and —NRa, with the proviso that at least one of Z1, Z2 and Z3 represents O, S or —NRa;L1 and L2 together represent —NH—C(═X)—, —NH—S(═O)q—, —C(═X)NH—, or—S(═O)qNH— or —NH—CR′R″—;A is absent or selected from —(CR′R″)—, O, S(═O)q, C(═X) and —NRa;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 a bicyclic ring selected from substituted or unsubstituted cycloalkyl group, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl;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—, —NRcRd—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; andeach occurrence of q independently represents 0, 1 or 2; with Proviso (e) that the compound of formula (I) is not:
N-[4-[5-cyclopropyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-1-methyl-3-(trifluoromethyl)-1H-Thieno[2,3-c]pyrazole-5-carboxamide or N-[4-[5-cyclopropyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-Pyrazolo[1,5-a]pyrimidine-2-carboxamide. |
