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    AMINOPYRIMIDINYL COMPOUNDS AS JAK INHIBITORS
    3.
    发明授权
    AMINOPYRIMIDINYL COMPOUNDS AS JAK INHIBITORS 有权

    公开(公告)号：EP3183247B9

    公开(公告)日：2018-07-25

    申请号：EP15766627.2

    申请日：2015-08-07

    申请人： Pfizer Inc.

    发明人： FENSOME, Andrew ,  GOPALSAMY, Ariamala ,  GERSTENBERGER, Brian S. ,  EFREMOV, Ivan Viktorovich ,  WAN, Zhao-Kui ,  PIERCE, Betsy ,  TELLIEZ, Jean-Baptiste ,  TRUJILLO, John I ,  ZHANG, Liying ,  XING, Li ,  SAIAH, Eddine

    IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  C07D487/08 ,  C07D519/00 ,  A61K31/506 ,  A61P35/00 ,  A61P37/00

    CPC分类号： A61K31/55 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/08 ,  C07D519/00

    摘要： A compound having the structure: or a pharmaceutically acceptable salt thereof, wherein X is N or CR, where R is hydrogen, deuterium, C1-C4 alkyl, C1-C4 alkoxy, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, amino, alkylamino, dialkylamino, CF3, or hydroxyl; A is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0—, and —(CRaRb)q—, where R0 is H or C1-C4 alkyl, and Ra and Rb are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, etc.; A′ is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0′, —NR0′(C═O)—, and —(CRa′Rb′)q—, where R0′ is H or C1-C4 alkyl, and Ra′ and Rb′ are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, heteroaryl(C1-C6 alkyl), and heterocyclic(C1-C6 alkyl); Z is —(CH2)h— or a bond, where one or more methylene units are optionally substituted by one or more C1-C3 alkyl, CN, OH, methoxy, or halo, and where said alkyl may be substituted by one or more fluorine atoms; R1 and R1′ are independently selected from the group consisting of hydrogen, deuterium, C1-C4 alkyl, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, etc., wherein said alkyl, aryl, cycloalkyl, heterocyclic, or heteroaryl is further optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, halo, CN, C1-C4 alkylamino, C3-C6 cycloalkyl, etc.; R2 is selected from the group consisting of hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, halo, and cyano, where said alkyl may be substituted by one or more fluorine atoms; R3 is selected from the group consisting of hydrogen, deuterium, and amino; R4 is monocyclic or bicyclic aryl or monocyclic or bicyclic heteroaryl wherein said aryl or heteroaryl is optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, heterocycloalkyl, halo, C3-C6 cycloalkyl, etc., where said alkyl, cycloalkyl, alkoxy, or heterocycloalkyl may be substituted by one or more C1-C6 alkyl, halo, CN, OH, alkoxy, amino, —CO2H, —(CO)NH2, —(CO)NH(C1-C6 alkyl), or —(CO)N(C1-C6 alkyl)2, and where said alkyl may be further substituted by one or more fluorine atoms; R5 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 alkoxy, and hydroxyl; h is 1, 2 or 3; j and k are independently 0, 1, 2, or 3; m and n are independently 0, 1 or 2; and, q is 0, 1 or 2. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.

    AMINOPYRIMIDINYL COMPOUNDS AS JAK INHIBITORS
    4.
    发明公开
    AMINOPYRIMIDINYL COMPOUNDS AS JAK INHIBITORS 有权
    作为JAK抑制剂的氨基嘧啶基化合物

    公开(公告)号：EP3183247A1

    公开(公告)日：2017-06-28

    申请号：EP15766627.2

    申请日：2015-08-07

    申请人： Pfizer Inc.

    发明人： FENSOME, Andrew ,  GOPALSAMY, Ariamala ,  GERSTENBERGER, Brian S. ,  EFREMOV, Ivan Viktorovich ,  WAN, Zhao-Kui ,  PIERCE, Betsy ,  TELLIEZ, Jean-Baptiste ,  TRUJILLO, John I ,  ZHANG, Liying ,  XING, Li ,  SAIAH, Eddine

    IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  C07D487/08 ,  C07D519/00 ,  A61K31/506 ,  A61P35/00 ,  A61P37/00

    CPC分类号： A61K31/55 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/08 ,  C07D519/00

    摘要： or a pharmaceutically acceptable salt thereof, wherein X is N or CR, where R is hydrogen, deuterium, C1-C4 alkyl, C1-C4 alkoxy, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, amino, alkylamino, dialkylamino, CF3, or hydroxyl; A is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0—, and —(CRaRb)q—, where R0 is H or C1-C4 alkyl, and Ra and Rb are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, etc.; A′ is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0′, —NR0′(C═O)—, and —(CRa′Rb′)q—, where R0′ is H or C1-C4 alkyl, and Ra′ and Rb′ are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, heteroaryl(C1-C6 alkyl), and heterocyclic(C1-C6 alkyl); Z is —(CH2)h— or a bond, where one or more methylene units are optionally substituted by one or more C1-C3 alkyl, CN, OH, methoxy, or halo, and where said alkyl may be substituted by one or more fluorine atoms; R1 and R1′ are independently selected from the group consisting of hydrogen, deuterium, C1-C4 alkyl, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, etc., wherein said alkyl, aryl, cycloalkyl, heterocyclic, or heteroaryl is further optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, halo, CN, C1-C4 alkylamino, C3-C6 cycloalkyl, etc.; R2 is selected from the group consisting of hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, halo, and cyano, where said alkyl may be substituted by one or more fluorine atoms; R3 is selected from the group consisting of hydrogen, deuterium, and amino; R4 is monocyclic or bicyclic aryl or monocyclic or bicyclic heteroaryl wherein said aryl or heteroaryl is optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, heterocycloalkyl, halo, C3-C6 cycloalkyl, etc., where said alkyl, cycloalkyl, alkoxy, or heterocycloalkyl may be substituted by one or more C1-C6 alkyl, halo, CN, OH, alkoxy, amino, —CO2H, —(CO)NH2, —(CO)NH(C1-C6 alkyl), or —(CO)N(C1-C6 alkyl)2, and where said alkyl may be further substituted by one or more fluorine atoms; R5 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 alkoxy, and hydroxyl; h is 1, 2 or 3; j and k are independently 0, 1, 2, or 3; m and n are independently 0, 1 or 2; and, q is 0, 1 or 2. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.

    摘要翻译： 具有以下结构的化合物或其药学上可接受的盐，其中X是N或CR，其中R是氢，氘，C 1 -C 4烷基，C 1 -C 4烷氧基，C 3 -C 6环烷基，芳基，杂芳基， C6烷基），CN，氨基，烷基氨基，二烷基氨基，CF3或羟基; A选自键，C = O，-SO 2 - ， - （C = O）NR 0 - 和 - （CR a R b）q - ，其中R 0为H或C 1 -C 4烷基，并且R a和R b 氘，C1-C6烷基，C3-C6环烷基，芳基，芳基（C1-C6烷基），杂芳基，（C1-C6烷基）杂芳基等。 A'选自键，C = O，-SO 2 - ， - （C = O）NR 0'，-NR 0'（C = O） - 和 - （CR a'R b'）q-组成的组， 其中R 0'为H或C 1 -C 4烷基，并且R a'和R b'独立地为氢，氘，C 1 -C 6烷基，C 3 -C 6环烷基，芳基，芳基（C 1 -C 6烷基） ）杂芳基，杂芳基（C 1 -C 6烷基）和杂环（C 1 -C 6烷基）; Z为 - （CH 2）h - 或键，其中一个或多个亚甲基单元任选被一个或多个C 1 -C 3烷基，CN，OH，甲氧基或卤素取代，并且其中所述烷基可被一个或多个 氟原子; R1和R1'独立地选自氢，氘，C1-C4烷基，C3-C6环烷基，芳基，杂芳基，芳基（C1-C6烷基），CN等，其中所述烷基，芳基，环烷基 杂环或杂芳基进一步任选被一个或多个选自C 1 -C 6烷基，卤素，CN，C 1 -C 4烷基氨基，C 3 -C 6环烷基等的取代基取代; R 2选自氢，氘，C 1 -C 6烷基，C 3 -C 6环烷基，卤素和氰基，其中所述烷基可以被一个或多个氟原子取代; R3选自氢，氘和氨基; R 4是单环或双环芳基或单环或双环杂芳基，其中所述芳基或杂芳基任选被一个或多个选自C 1 -C 6烷基，杂环烷基，卤代，C 3 -C 6环烷基等的取代基取代，其中所述烷基 （CO）NH（C 1 -C 6烷基）， - （C 1 -C 6烷基）， - 或 - （CO）N（C 1 -C 6烷基）2，并且其中所述烷基可以进一步被一个或多个氟原子取代; R5独立地选自氢，C1-C6烷基，C1-C6烷氧基和羟基; h是1,2或3; j和k独立地为0,1,2或3; m和n独立地为0,1或2; 并且q是0,1或2.还提供了作为Janus激酶抑制剂和含有本发明化合物和其他治疗剂组合的药物组合物的治疗方法。

    PYRAZOLO[1,5-A]PYRAZIN-4-YL DERIVATIVES AS JAK-INHIBITORS
    10.
    发明公开
    PYRAZOLO[1,5-A]PYRAZIN-4-YL DERIVATIVES AS JAK-INHIBITORS 审中-公开

    公开(公告)号：EP3419978A1

    公开(公告)日：2019-01-02

    申请号：EP17705705.6

    申请日：2017-02-10

    申请人： Pfizer Inc.

    发明人： BROWN, Matthew Frank ,  DERMENCI, Alpay ,  FENSOME, Andrew ,  GERSTENBERGER, Brian Stephen ,  HAYWARD, Matthew Merrill ,  OWEN, Dafydd Rhys ,  WRIGHT, Stephen Wayne ,  XING, Li Huang ,  YANG, Xiaojing

    IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P37/02 ,  A61P29/00 ,  A61P25/28

    摘要： or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A, A′ and A″ are independently O, C═O, C—R′ or N—R″, where R′ and R″ may independently be H, amino, —NR7COR6, COR6, —CONR7R8, C1-C6 alkyl, or hydroxy(C1-C6 alkyl), and R″ may be present or absent, and is present where the rules of valency permit, and where not more than one of A, A′ and A″ is O or C═O; R0 and R are independently H, Br, Cl, F, or C1-C6 alkyl; R1 is H, C1-C6 alkyl, or hydroxy(C1-C6 alkyl); R2 is selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, hydroxy(C1-C6 alkyl), phenyl(C1-C6 alkyl), formyl, heteroaryl, heterocyclic, —COR6, —OCOR6, —COOR6, —NR7COR6, —CONR7R8, and —(CH2)n—W, where W is cyano, hydroxy, C3-C8 cycloalkyl, —SO2NR7R8, and —SO2—R9, where R9 is C1-C6 alkyl, C3-C8 cycloalkyl, heteroaryl, or heterocyclic; wherein each of said alkyl, cycloalkyl, heterocyclic, or heteroaryl may be unsubstituted or substituted by halo, cyano, hydroxy, or C1-C6 alkyl; X is C—R3 or N, where R3 may be H or C1-C6 alkyl; R4 and R5 are independently H, amino, C1-C6 alkyl, or hydroxy(C1-C6 alkyl); R6, R7 and R8 are each independently H, C1-C6 alkyl, C1-C4 alkoxy(C1-C6 alkyl), or C3-C8 cycloalkyl, said C1-C6 alkyl is optionally substituted by halo, CN or hydroxy; or, R7 and R8 together with the atom bonded thereto form a 5- or 6-membered ring, said ring being optionally substituted by halo, hydroxy, CN, or C1-C6 alkyl; and, n is 0, 1, 2 or 3. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.