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    N-substituted azaheterocyclic compounds
    1.
    发明授权
    N-substituted azaheterocyclic compounds 失效
    N-取代的氮杂环化合物

    公开(公告)号：US06187770B1

    公开(公告)日：2001-02-13

    申请号：US09267302

    申请日：1999-03-15

    申请人： Tine Krogh Jørgensen ,  Rolf Hohlweg ,  Knud Erik Andersen ,  Uffe Bang Olsen ,  Zdenék Polivka ,  Karel Sindelar

    发明人： Tine Krogh Jørgensen ,  Rolf Hohlweg ,  Knud Erik Andersen ,  Uffe Bang Olsen ,  Zdenék Polivka ,  Karel Sindelar

    IPC分类号： A61K31395

    CPC分类号： C07D513/04

    摘要： The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Z, R1, R2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation, as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

    摘要翻译： 本发明涉及通式为X，Z，R 1，R 2和r的新的N-取代的氮杂杂环化合物，如本说明书的详细部分所定义，或其盐，其制备方法，含有它们的组合物 ，以及它们用于临床治疗疼痛，痛觉过敏和/或炎性病症，其中C纤维通过引发神经源性疼痛或炎症而发挥病理生理学作用，以及它们用于治疗由分泌物引起或与分泌有关的适应症 和胰岛素拮抗肽的循环，例如 非胰岛素依赖性糖尿病（NIDDM）和衰老相关性肥胖。

    Heterocyclic compounds
    2.
    发明授权
    Heterocyclic compounds 失效
    杂环化合物

    公开(公告)号：US06214816B1

    公开(公告)日：2001-04-10

    申请号：US09266236

    申请日：1999-03-10

    申请人： Rolf Hohlweg ,  Tine Krogh Jørgensen ,  Knud Erik Andersen ,  Uffe Bang Olsen ,  Zdenék Polivka ,  Karel Sindelar

    发明人： Rolf Hohlweg ,  Tine Krogh Jørgensen ,  Knud Erik Andersen ,  Uffe Bang Olsen ,  Zdenék Polivka ,  Karel Sindelar

    IPC分类号： C07D40106

    CPC分类号： C07D403/06 ,  C07D413/06

    摘要： The compounds are N-substituted azaheterocyclic compounds of formula I wherein R1 and R2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C1-6-alkyl or C1-6-alkoxy; and Y is >N—CH2— wherein only the underscored atom participates in the ring system; and X is —C(R6R7)—, —CH2CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —CH2—(C═O)—, —(C═O)—CH2—, —CH2CH2CH2—, —CH═CH—, CH(R10)CH2—, —CH2CH(R10) or —(C═O)— wherein R6 and R7 independently are hydrogen or C1-6-alkyl and wherein R10 is C1-6-alkyl or phenyl; and r is 0, 1 or 2; and Z is selected from wherein A is —CH2—, —O—, —S— or —N(R5)— wherein R5 is H or C1-6-alkyl; and R3 is —(CH2)pCOR4 wherein p is 1, 2, 3 or 4 and R4 is OH, NH2, NHOH or C1-6-alkoxy; or a pharmaceutically acceptable salt thereof. These compounds are useful for treating painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation. They are also useful for treating indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g., non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

    摘要翻译： 化合物是式I的N-取代的氮杂环化合物，其中R1和R2独立地是氢，卤素，三氟甲基，羟基，C1-6烷基或C1-6-烷氧基; 并且Y是> N-CH 2 - ，其中只有下划线原子参与环系; 并且X是-C（R 6 R 7） - ， - CH 2 CH 2 - ， - CH = CH-CH 2 - ， - CH 2 -CH = CH-， - CH 2 - （C = O） - ， - （C = O） -CH 2 CH 2 CH 2 - ， - CH = CH-，CH（R 10）CH 2 - ， - CH 2 CH（R 10）或 - （C = O） - 其中R 6和R 7独立地是氢或C 1-6 - 烷基，其中R 10是C 1-6 - 烷基或苯基; 和r为0,1或2; 并且Z选自其中A是-CH 2 - ， - O - ， - S-或-N（R 5） - ，其中R 5是H或C 1-6 - 烷基; 并且R 3是 - （CH 2）p COR 4，其中p是1,2,3或4，并且R 4是OH，NH 2，NHOH或C 1-6 - 烷氧基; 或其药学上可接受的盐。 这些化合物可用于治疗C型纤维通过引起神经源性疼痛或炎症而发挥病理生理学作用的疼痛，痛觉过敏和/或炎性病症。 它们还可用于治疗由胰岛素拮抗肽（例如非胰岛素依赖性糖尿病（NIDDM））和老龄化相关性肥胖症分泌和循环引起或与之相关的适应症。

    Heterocyclic compounds
    3.
    发明授权
    Heterocyclic compounds 失效
    杂环化合物

    公开(公告)号：US06391890B1

    公开(公告)日：2002-05-21

    申请号：US09535216

    申请日：2000-03-27

    申请人： Tine Krogh Jørgensen ,  Knud Erik Andersen ,  Rolf Hohlweg ,  Uffe Bang Olsen ,  Erik Fischer ,  Zdenek Polivka ,  Kaler Sindelar

    发明人： Tine Krogh Jørgensen ,  Knud Erik Andersen ,  Rolf Hohlweg ,  Uffe Bang Olsen ,  Erik Fischer ,  Zdenek Polivka ,  Kaler Sindelar

    IPC分类号： A61K31445

    CPC分类号： C07D295/15 ,  C07D211/70 ,  C07D409/04 ,  C07D409/14

    摘要： The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, R1, R2 and m are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation, as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

    摘要翻译： 本发明涉及X，Y，Z，R 1，R 2和m一般形式的新的N-取代的氮杂杂环化合物，如本说明书的详细部分或其盐，其制备方法，组合物 并且用于临床治疗疼痛，痛觉过敏和/或炎症性疾病，其中C-纤维通过引发神经源性疼痛或炎症而发挥病理生理学作用，以及它们用于治疗由...引起的或与之相关的适应症 胰岛素拮抗肽的分泌和循环，例如 非胰岛素依赖性糖尿病（NIDDM）和衰老相关性肥胖。