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    Nicotinamide derivatives useful as PDE4 inhibitors
    10.
    发明申请
    Nicotinamide derivatives useful as PDE4 inhibitors 失效
    可用作PDE4抑制剂的烟酰胺衍生物

    公开(公告)号：US20050032838A1

    公开(公告)日：2005-02-10

    申请号：US10896315

    申请日：2004-07-20

    Applicant: Simon Bailey ,  Christopher Barber ,  Paul Glossop ,  Donald Middleton

    Inventor： Simon Bailey ,  Christopher Barber ,  Paul Glossop ,  Donald Middleton

    IPC: A61K31/4415 ,  A61K31/4439 ,  A61K31/454 ,  A61P37/00 ,  C07D213/02 ,  C07D213/82 ,  C07D401/12 ,  C07D405/12 ,  C07D41/02

    CPC classification number: C04B35/632 ,  C07D213/82 ,  C07D401/12 ,  C07D405/12

    Abstract: This invention relates to nicotinamide derivatives of formula (I) and to processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions containing, and the uses of such derivatives: wherein R1 is selected from the group consisting of hydrogen, methyl or halo; R7 is attached to the 3- or 4-position of the phenyl ring and is S(O)pR8, R8 is (C1-C4)alkyl optionally substituted by (C3-C6)cycloalkyl; p is 0, 1 or 2; R6 is selected from the group consisting of hydrogen, halo, (C1-C3)alkyl and (C1-C3)alkoxy; m is 0 or 1; L is a (C3-C8)carbocyclic non-aromatic ring; R2 is hydrogen, hydroxy, (C1-C3)alkoxy, (C1-C3)alkyl (optionally substituted by hydroxy or by (C1-C3)alkoxy), CO2R9, NR10R11 or CONR10R11; R3 is hydrogen or (C1-C3)alkyl; R9 is hydrogen or (C1-C3)alkyl; R10 and R11 are each independently hydrogen, or, are selected from the group consisting of: (C1-C6)alkyl optionally substituted by phenyl or a 5- or 6-membered heterocyclic ring incorporating 1 to 3 heteroatom(s) independently selected from N, O and S, which phenyl is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl or (C1-C3)alkoxy and which heterocyclic ring is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl, (C1-C3)alkoxy or oxo; (C3-C8)cycloalkyl; CO((C1-C6)alkyl) optionally substituted by hydroxy, halo, (C3-C8)cycloalkyl, (C1-C3)alkoxy, phenyl or a 5- or 6-membered heterocyclic ring incorporating 1 to 3 heteroatom(s) independently selected from N, O and S, which phenyl is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl or (C1-C3)alkoxy and which heterocyclic ring is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl, (C1-C3)alkoxy or oxo; CO(R12), wherein R12 is (C3-C8)cycloalkyl optionally substituted by (C1-C3)alkyl or R12 is phenyl or a 5- or 6-membered heterocyclic ring incorporating 1 to 3 heteroatom(s) independently selected from N, O and S, which phenyl is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl or (C1-C3)alkoxy and which heterocyclic ring is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl, (C1-C3)alkoxy or oxo; and CO2(C1-C3)alkyl); or R10 and R11 are taken together with the N atom to which they are attached to form a 5- or 6-membered lactam.

    Abstract translation: 本发明涉及式（I）的烟酰胺衍生物以及制备用于制备含有此类衍生物的药物组合物的中间体的方法：其中R1选自氢，甲基或 光环; R7连接到苯环的3-或4-位，是S（O）p R 8，R 8是任选被（C 3 -C 6）环烷基取代的（C 1 -C 4）烷基; p为0,1或2; R 6选自氢，卤素，（C 1 -C 3）烷基和（C 1 -C 3）烷氧基; m为0或1; L是（C 3 -C 8）碳环非芳香环; R 2是氢，羟基，（C 1 -C 3）烷氧基，（C 1 -C 3）烷基（任选被羟基或被（C 1 -C 3）烷氧基取代），CO 2 R 9，NR 10 R 11或CONR 10 R 11; R3是氢或（C1-C3）烷基; R9是氢或（C1-C3）烷基; R 10和R 11各自独立地为氢，或选自：任选被苯基取代的（C 1 -C 6）烷基或包含1至3个独立地选自N的杂原子的5或6元杂环 ，O和S，该苯基任选被一个或多个选自羟基，卤素，（C 1 -C 3）烷基或（C 1 -C 3）烷氧基的取代基取代，并且该杂环任选被一个或多个选自羟基， 卤代，（C1-C3）烷基，（C1-C3）烷氧基或氧代; （C 3 -C 8）环烷基; 任选被羟基，卤素，（C 3 -C 8）环烷基，（C 1 -C 3）烷氧基，苯基或独立地并入1至3个杂原子的5或6元杂环取代的CO（（C 1 -C 6）烷基） 谢尔

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