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    PYRAZOLOPYRIDINES AND PYRAZOLOPYRIMIDINES
    2.
    发明公开
    PYRAZOLOPYRIDINES AND PYRAZOLOPYRIMIDINES 审中-公开
    吡唑并吡啶在吡唑并嘧啶中的应用

    公开(公告)号：EP3143021A1

    公开(公告)日：2017-03-22

    申请号：EP15724365.0

    申请日：2015-04-30

    申请人： Pfizer Inc.

    发明人： COE, Jotham Wadsworth ,  DEHNHARDT, Christoph Martin ,  JONES, Peter ,  SABNIS, Yogesh Anil ,  STROHBACH, Joseph Walter ,  WAKENHUT, Florian Michel ,  WHITLOCK, Gavin Alistair

    IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/4162 ,  A61P35/00

    CPC分类号： A61K31/519 ,  A61K31/437 ,  A61K31/4725 ,  C07D471/04 ,  C07D487/04

    摘要： A compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A and A′ are independently C or N, where C may be unsubstituted or substituted by halo or C1-C6 alkyl; R and R0 are independently selected from the group consisting of H, C1-C6 alkyl, hydroxy(C1-C6 alkyl), phenyl(C1-C6 alkyl), and —(CH2)n—W, where W is C3-C8 cycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1-3 N, S and/or O atoms, —SO2—R′, —NHSO2—R′, —NR″SO2—R′ and SR′, where R′ and R″ are independently C1-C6 alkyl or C3-C8 cycloalkyl, etc.; wherein each of said alkyl, cycloalkyl, heterocyclic, phenyl, naphthyl or heteroaryl may be unsubstituted or substituted by phenyl, heteroaryl, etc.; or, R and R0 and the N atom to which they are bonded together form a monocyclic or bicyclic heterocyclic ring which may be unsubstituted or substituted by (a) halo, hydroxy, heteroaryl, C1-C6 alkyl, C1-C6 alkoxy, etc., or (b) —(CH2)n—W, where W is C3-C8 cycloalkyl, phenyl, etc.; R1 is H, halo or cyano; R2 and R2′ are independently H, C1-C6 alkyl, cyano, C1-C6 alkoxy, C1-C6 alkylthio, or C3-C8 cycloalkyl where alkyl, alkoxy, or cycloalkyl is optionally substituted by one or more fluorine atoms; X is a bond, —CO—, —CONH—, —SO2—, —SONH—, or —(CH2)m—; R3 is H, C1-C4 alkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1-3 N atoms, a 5-membered heteroaryl or heterocyclic, etc., or (c) 2 O or S atoms and 0-2 N atoms; wherein each of said phenyl, naphthyl, heteroaryl or heterocyclic is optionally substituted by alkyl, 1 substituent —Y—R4 and/or 1-4 substituents each independently selected from R5; with the proviso that when X is —CO— or —SO2—, R3 is not H; Y is a bond, —(CH2)m— or —O—; R4 is (a) H, C1-C6 alkyl, C3-C8 cycloalkyl, halo, oxo, —OR6, —NR7R8, —SR6, —SOR9, —SO2R9, —COR6, —OCOR6, —OCOR6, —NR6COR6, —CONR7R8, etc.; (b) phenyl or naphthyl, said phenyl and naphthyl being optionally substituted with 1-5 substituents selected from C1-C6 alkyl, C3-C8 cycloalkyl, halo, cyano, —OR6, —NR7R8, etc.; or (c) a 3 to 8-membered saturated or partially unsaturated monocyclic heteroaryl, etc.; R6 is H, C1-C6 alkyl or C3-C8 cycloalkyl, etc.; R7 and R8 are each independently H, C1-C6 alkyl or C3-C8 cycloalkyl or are taken together with the nitrogen atom to which they are attached to form a 4-, 5- or 6-membered saturated heterocyclic ring containing 1-2 nitrogen atoms or 1 nitrogen and 1 oxygen atom, said C1-C6 alkyl is optionally substituted by C3-C8 cycloalkyl, halo, etc., and said heterocyclic ring being optionally substituted by one or more C1-C6 alkyl or C3-C8 cycloalkyl groups; R9 is C1-C6 alkyl or C3-C8 cycloalkyl; and, m and n are independently 0, 1, 2 or 3. The invention also relates to pharmaceutically acceptable salts of these compounds and to pharmaceutically acceptable solvates thereof; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.

    摘要翻译： 或其药学上可接受的盐，或所述化合物或其药学上可接受的盐的药学上可接受的溶剂化物，其中A和A'独立地为C或N，其中C可以是未取代的或被卤素或C 1 -C 6烷基取代; R 1和R 2独立地选自H，C 1 -C 6烷基，羟基（C 1 -C 6烷基），苯基（C 1 -C 6烷基）和 - （CH 2）n-W，其中W是C 3 -C 8环烷基 ，苯基，萘基，含有1-3个N，S和/或O原子的5或6元杂芳基或杂环，-SO 2 -R'，-NHSO 2 -R'，-NR“SO 2 -R'和SR' 其中R'和R“独立地为C 1 -C 6烷基或C 3 -C 8环烷基等; 其中所述烷基，环烷基，杂环，苯基，萘基或杂芳基中的每一个可以是未取代的或被苯基，杂芳基等取代; 或者，R和R 0以及与它们相连的N原子一起形成可被未被取代或被（a）卤素，羟基，杂芳基，C 1 -C 6烷基，C 1 -C 6烷氧基等取代的单环或双环杂环。 ，或（b） - （CH 2）n -W，其中W是C 3 -C 8环烷基，苯基等; R1是H，卤素或氰基; R 2和R 2'独立地为H，C 1 -C 6烷基，氰基，C 1 -C 6烷氧基，C 1 -C 6烷硫基或C 3 -C 8环烷基，其中烷基，烷氧基或环烷基任选被一个或多个氟原子取代; X是键，-CO - ， - CONH - ， - SO 2 - ， - SOH-或 - （CH 2）m - ; R 3是H，C 1 -C 4烷基，苯基，萘基，含有1-3个N原子的5或6元杂芳基或杂环，5元杂芳基或杂环等，或（c）2 O或S原子和 0-2个N原子; 其中所述苯基，萘基，杂芳基或杂环中的每一个任选被烷基，1个取代基-Y-R 4和/或1-4个独立地选自R 5的取代基取代; 条件是当X是-CO - 或-SO 2 - 时，R 3不是H; Y是键， - （CH 2）m - 或-O-; R4是（a）H，C1-C6烷基，C3-C8环烷基，卤素，氧代，-OR6，-NR7R8，-SR6，-SOR9，-SO2R9，-COR6，-OCOR6，-COOR6，-NR6COR6，-CONR7R8 等等 （b）苯基或萘基，所述苯基和萘基任选被1-5个选自C 1 -C 6烷基，C 3 -C 8环烷基，卤素，氰基，-OR 6，-NR 7 R 8等取代基取代; 或（c）3至8元饱和或部分不饱和单环杂芳基等; R6是H，C1-C6烷基或C3-C8环烷基等; R 7和R 8各自独立地为H，C 1 -C 6烷基或C 3 -C 8环烷基，或与它们所连接的氮原子一起形成含有1-2个氮的4-，5-或6-元饱和杂环 原子或1个氮原子和1个氧原子，所述C 1 -C 6烷基任选被C 3 -C 8环烷基，卤素等取代，所述杂环任选被一个或多个C 1 -C 6烷基或C 3 -C 8环烷基取代; R9是C1-C6烷基或C3-C8环烷基; m和n独立地为0,1,2或3.本发明还涉及这些化合物的药学上可接受的盐及其药学上可接受的溶剂合物; 含有这些化合物的组合物; 以及这些化合物在治疗各种疾病，特别是哮喘和COPD中的用途。