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    5-Membered heterocyclic compound
    72.
    发明授权
    5-Membered heterocyclic compound 有权
    5元杂环化合物

    公开(公告)号：US08334301B2

    公开(公告)日：2012-12-18

    申请号：US12680184

    申请日：2008-09-24

    Applicant: Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Keizo Hirase

    Inventor： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Keizo Hirase

    IPC: A61K31/415 ,  C07D233/00

    CPC classification number: C07D333/20 ,  C07D231/18 ,  C07D231/38 ,  C07D231/40 ,  C07D231/42 ,  C07D233/24 ,  C07D233/42 ,  C07D333/32 ,  C07D333/34 ,  C07D401/12 ,  C07D403/04 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14

    Abstract: Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like.A compound represented by the formula (I) or a salt thereof: wherein ring A is a saturated or unsaturated 5-membered heterocycle containing, as a ring-constituting atom besides carbon atoms, at least one heteroatom selected from a nitrogen atom, an oxygen atom and a sulfur atom, the ring-constituting atoms X1 and X2 are the same or different and each is C or N, the ring-constituting atoms X3 and X4 are the same or different and each is C, N, O or S (provided that a pyrrole ring wherein X1 is N is excluded from ring A), and when the ring-constituting atom X3 or X4 is C or N, each ring-constituting atom optionally has substituent(s) selected from an optionally substituted alkyl, an acyl, an optionally substituted hydroxy, an optionally substituted mercapto, an optionally substituted amino, a halogen, a cyano and a nitro; R1 and R2 are each a cyclic group optionally having substituent(s); R3 and R4 are each H or alkyl, or R3 and R4 form, together with the adjacent N, an nitrogen-containing heterocycle; and Y is a spacer.

    Abstract translation: 提供具有优异的酸分泌抑制作用的化合物，其表现出抗溃疡活性等。 由式（I）表示的化合物或其盐：其中环A是饱和或不饱和的5元杂环，其含有除碳原子之外的构成环的原子，至少一个选自氮原子，氧原子的杂原子 原子和硫原子，构成环的原子X1和X2相同或不同，分别为C或N，构成成环原子X3和X4相同或不同，分别为C，N，O或S（ 条件是其中X1为N的吡咯环不包括在环A）中，并且当构成环的原子X 3或X 4为C或N时，每个构成环的原子任选具有选自任选取代的烷基， 酰基，任选取代的羟基，任选取代的巯基，任选取代的氨基，卤素，氰基和硝基; R1和R2各自为任选具有取代基的环状基团; R3和R4各自为H或烷基，或R3和R4与相邻的N一起形成含氮杂环; Y是间隔物。

    Process for the preparation of pyrazole derivatives
    75.
    发明授权
    Process for the preparation of pyrazole derivatives 失效
    吡唑衍生物的制备方法

    公开(公告)号：US08288563B2

    公开(公告)日：2012-10-16

    申请号：US13256564

    申请日：2010-03-12

    Applicant: Maximilian Dochnahl ,  Martin Sukopp ,  Alexander Korte

    Inventor： Maximilian Dochnahl ,  Martin Sukopp ,  Alexander Korte

    IPC: C07D231/10

    CPC classification number: C07D231/38

    Abstract: The present invention refers to a process for the preparation of pyrazole derivatives of formula (I) wherein W is nitrogen or CR1, R1, R2, R4 and R5 are each independently selected from hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, R7S(O)n, nitro, cyano, and pentafluorothio; R3 is hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, R7S(O)n, nitro, cyano, pentafluorothio or phenyl which is unsubstituted or substituted by 1 to 5 members of the group consisting of halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, R7S(O)n, nitro, cyano, and pentafluorothio which are the same or different; R7 is C1-C6-alkyl or C1-C6-haloalkyl; and n is 0, 1, or 2; characterized in that hydrazines of formula (II) wherein W, R2, R3, R4, and R5 are as defined for pyrazole derivatives of formula (I), are reacted with a compound of formula (III)

    Abstract translation: 本发明涉及一种制备式（I）的吡唑衍生物的方法，其中W是氮或CR 1，R 1，R 2，R 4和R 5各自独立地选自氢，卤素，C 1 -C 6烷基，C 1 -C 6 卤代烷基，C 1 -C 6 - 烷氧基，C 1 -C 6卤代烷氧基，R 7 S（O）n，硝基，氰基和五氟硫基; R3是氢，卤素，C1-C6-烷基，C1-C6-卤代烷基，C1-C6-烷氧基，C1-C6-卤代烷氧基，R7S（O）n，硝基，氰基，五氟硫基或未被取代或被1 至卤素，C 1 -C 6 - 烷基，C 1 -C 6 - 卤代烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 卤代烷氧基，R 7 S（O）n，硝基，氰基和五氟硫基的5个成员相同 或不同; R7是C1-C6-烷基或C1-C6-卤代烷基; 并且n为0,1或2; 其特征在于其中W，R 2，R 3，R 4和R 5如式（I）的吡唑衍生物所定义的式（II）的肼与式（III）的化合物反应，

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