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    Spirocyclic-6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines
    6.
    发明授权
    Spirocyclic-6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines 失效
    控制炎症细胞因子的螺环-6,7-二氢-5H-吡唑并[1,2-a]吡唑-1-酮

    公开(公告)号：US06566357B1

    公开(公告)日：2003-05-20

    申请号：US10246499

    申请日：2002-09-18

    申请人： Matthew John Laufersweiler ,  Michael Philip Clark ,  Jane Far-Jine Djung ,  Adam Golebiowski ,  Todd Andrew Brugel ,  Biswanath De

    发明人： Matthew John Laufersweiler ,  Michael Philip Clark ,  Jane Far-Jine Djung ,  Adam Golebiowski ,  Todd Andrew Brugel ,  Biswanath De

    IPC分类号： C07D40104

    CPC分类号： C07D487/04 ,  C07D491/20 ,  C07D495/20

    摘要： The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; two R2 units on the same carbon atom are taken together to form a spirocyclic ring having from 4 to 7 atoms, the balance of the R2 units are independently selected from the group consisting of: a) hydrogen; b) —O(CH2)jR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —CH2)jCON(R10)2; and g) two R2 units can be taken together to form a carbonyl unit; R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 units can be take together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; j is an index from 0 to 5; the index n is from 3 to 5.

    摘要翻译： 本发明涉及能够防止炎性细胞因子细胞外释放的化合物，所述化合物包括所有对映异构体和非对映体形式及其药学上可接受的盐，具有下式：其中R包括醚或胺; R 1是：a）取代或 未取代的芳基; 环）取代或未取代的杂芳基;同一碳原子上的两个R2单元一起形成具有4至7个原子的螺环，其余的R2单元独立地选自：a）氢; b ） - （CH2）jR8; c） - （CH2）jNR9aR9b; d） - （CH2）jCO2R10; e） - （CH2）jOCO2R10f）-CH2）jCON（R10）2; 和g）两个R2单元可以一起取代形成羰基单元; R8，R9a，R9b和R10各自独立地为氢，C1-C4烷基及其混合物; R9a和R9b可以一起形成包含3至7个原子的碳环或杂环; 两个R 10单元可以一起形成包含3至7个原子的碳环或杂环; j是从0到5的索引; 索引n为3到5。

    Bicyclic pyrazolone cytokine inhibitors
    8.
    发明授权
    Bicyclic pyrazolone cytokine inhibitors 失效
    双环吡唑啉酮细胞因子抑制剂

    公开(公告)号：US07482356B2

    公开(公告)日：2009-01-27

    申请号：US10983114

    申请日：2004-11-05

    申请人： Michael Philip Clark ,  Steven Karl Laughlin ,  Adam Golebiowski ,  Todd Andrew Brugel ,  Mark Sabat

    发明人： Michael Philip Clark ,  Steven Karl Laughlin ,  Adam Golebiowski ,  Todd Andrew Brugel ,  Mark Sabat

    IPC分类号： C07D487/04 ,  A61K31/4162

    CPC分类号： C07D487/04

    摘要： The present invention relates to 6,7-dihydro-5H-pyrazolo[1,2α]pyrazol-1-ones which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 6,7-dihydro-5H-pyrazolo[1,2α]pyrazol-1-ones and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.

    摘要翻译： 本发明涉及抑制炎性细胞因子细胞外释放的6,7-二氢-5H-吡唑并[1,2α]吡唑-1-酮，所述细胞因子负责一种或多种人或更高级哺乳动物疾病状态。 本发明还涉及包含所述6,7-二氢-5H-吡唑并[1,2α]吡唑-1-酮的组合物以及用于预防，减轻或以其他方式控制酶的方法，所述酶被理解为负责 这里描述了疾病状态。