发明名称 Modulators of calcium release-activated calcium channel
摘要 Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
申请公布号 US8921364(B2) 申请公布日期 2014.12.30
申请号 US201213722523 申请日期 2012.12.20
申请人 Rhizen Pharmaceuticals SA 发明人 Muthuppalaniappan Meyyappan;Viswanadha Srikant;Merikapudi Gayatri Swaroop;Vakkalanka Swaroop Kumar V. S.
分类号 C07D231/12;C07D417/10;C07D401/14;C07D403/04;C07D403/12;C07D413/12;C07D417/12;C07D417/14;C07D403/14;C07D413/10;C07D401/04;C07D403/10;C07D413/14;C07D207/327;C07D401/12;C07D401/10 主分类号 C07D231/12
代理机构 Blank Rome LLP 代理人 Blank Rome LLP
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.
地址 La Chaux-de-Fonds CH