发明名称 Imidazo[1,2-<i>b</i>]pyridazine and imidazo[4,5-<i>b</i>]pyridine derivatives as JAK inhibitors
摘要 New imidazo[1,2-b]pyridazine and imidazo[4,5-b]pyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).;
申请公布号 US9133200(B2) 申请公布日期 2015.09.15
申请号 US201113988798 申请日期 2011.11.24
申请人 Almirall, S.A. 发明人 Gonzalez Rodriguez Jacob;Vidal Juan Bernat;Vidal Gispert Laura;Bach Taña Jordi
分类号 C07D487/04;A61K9/20;A61K9/48;A61K31/437;A61K31/5025;A61K45/06;C07D471/04 主分类号 C07D487/04
代理机构 Finnegan, Henderson, Farabow, Garrett & Dunner 代理人 Finnegan, Henderson, Farabow, Garrett & Dunner
主权项 1. A compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof: wherein: m is 0, 1, 2, or 3; X is chosen from a nitrogen atom and a —CR7 group; Y is a —CR7 group; G1 is a carbon atom; G2 is a nitrogen atom; R1 and R2 are independently chosen from a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, a linear or branched C1-C6 alkyl group, a C1-C4 haloalkyl group, a C1-C4 hydroxyalkyl group, a C3-C10 cycloalkyl group, a C3-C10 cycloalkenyl group, a monocyclic or polycyclic C5-C14 aryl group, a 5- to 14-membered heteroaryl group containing at least one heteroatom chosen from O, S and N, a 5- to 14-membered heterocyclyl group containing at least one heteroatom chosen from O, S and N, wherein the alkyl, haloalkyl, hydroxyalkyl, cycloalkyl, cycloalkenyl, aryl, heteroaryl, and heterocyclyl groups are unsubstituted or substituted by one or more substituents chosen from a halogen atom, a cyano group, a linear or branched C1-C6 alkyl group, a C1-C4 haloalkyl group, a C1-C4 hydroxyalkyl group, a C1-C4 alkylsulfonyl group, a C3-C7 cycloalkyl group, a phenyl group, a pyridyl group, a pyrimidinyl group, and a piperidyl group; or R1 and R2 are independently chosen from a —(CH2)0-2OR9 group, a —O—(CH2)1-2OR9 group, and a —NR8R9 group; R3 is chosen from a hydrogen atom, a halogen atom, a cyano group, a linear or branched C1-C6 alkyl group, a C1-C4 haloalkyl group, a C1-C4 hydroxyalkyl group, a C3-C10 cycloalkyl group, a C3-C10 cycloalkenyl group, a monocyclic or polycyclic C5-C14 aryl group, a 5- to 14-membered heteroaryl group containing at least one heteroatom chosen from O, S and N, and a 5- to 14-membered heterocyclyl group containing at least one heteroatom chosen from O, S and N, wherein the alkyl, haloalkyl, hydroxyalkyl, cycloalkyl, cycloalkenyl, aryl, heteroaryl, and heterocyclyl groups are unsubstituted or substituted by one or more substituents chosen from a halogen atom, a cyano group, a linear or branched C1-C6 alkyl group, a C1-C4 haloalkyl group, a C1-C4 hydroxyalkyl group, a C3-C7 cycloalkyl group, a phenyl group, a pyridyl group, a pyrimidinyl group, a piperidyl group, a —(CH2)0-2OR9 group, a —NR8R9 group,a —C(O)—(CH2)0-2—R6 group, a —C(O)(CH2)0-2—NR6R9 group,a —S(O)2(CH2)0-2R9 group, and a —S(O)2(CH2)0-2NR8R9 group; R4 is chosen from a hydrogen atom, a C1-C4 haloalkyl group, a C1-C4 hydroxyalkyl group, and a linear or branched C1-C6 alkyl group, said alkyl group is unsubstituted or substituted by one or more substituents chosen from a cyano group, a C3-C7 cycloalkyl group, a phenyl group, a pyridyl group, a pyrimidinyl group, and a piperidyl group; R5 and R6 are independently chosen from a hydrogen atom, a C1-C4 haloalkyl group, a C1-C4 hydroxyalkyl group, and a linear or branched C1-C6 alkyl group, said alkyl group is unsubstituted or substituted by one or more substituents chosen from a cyano group, a C3-C7 cycloalkyl group, a phenyl group, a pyridyl group, a pyrimidinyl group, and a piperidyl group; R7 is chosen from a hydrogen atom, a halogen atom, a cyano group, a linear or branched C1-C6 alkyl group, a C1-C4 haloalkyl group, a C1-C4 hydroxyalkyl group, a C3-C10 cycloalkyl group, a C3-C10 cycloalkenyl group, a monocyclic or polycyclic C5-C14 aryl group, a 5- to 14-membered heteroaryl group containing at least one heteroatom chosen from O, S and N, and a 5- to 14-membered heterocyclyl group containing at least one heteroatom chosen from O, S and N, wherein the alkyl, haloalkyl, hydroxyalkyl, cycloalkyl, cycloalkenyl, aryl, heteroaryl, and heterocyclyl groups are unsubstituted or substituted by one or more substituents chosen from a halogen atom, a cyano group, a linear or branched C1-C6 alkyl group, a C1-C4 haloalkyl group, a C1-C4 hydroxyalkyl group, a C3-C7 cycloalkyl, a phenyl group, a pyridyl group, a pyrimidinyl group, and a piperidyl group; R8 is chosen from a hydrogen atom, a cyano group, a C1-C4 haloalkyl group, a C1-C4 hydroxyalkyl group or a linear or branched C1-C6 alkyl group, said alkyl group is unsubstituted or substituted by one or more substituents chosen from a cyano group, a C3-C7 cycloalkyl group, a phenyl group, a pyridyl group, a pyridinyl group, and a piperidyl group; R9 is chosen from a hydrogen atom, a C1-C4 haloalkyl group, a C1-C4 hydroxyalkyl group or a linear or branched C1-C6 alkyl group, said alkyl group is unsubstituted or substituted by one or more substituents chosen from a cyano group, a C3-C7 cycloalkyl group, a phenyl group, a pyridyl group, a pyrimidinyl group, and a piperidyl group.
地址 Barcelona ES