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1. 发明授权

US07087615B2 6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which provide analgesia 失效
公开(公告)号：US07087615B2
公开(公告)日：2006-08-08
申请号：US10689388
申请日：2003-10-20
申请人： Michael Philip Clark , Matthew John Laufersweiler , Biswanath De , Michael John Janusz
发明人： Michael Philip Clark , Matthew John Laufersweiler , Biswanath De , Michael John Janusz
IPC分类号： A61K31/506 , A61P25/04
CPC分类号： C07D487/04
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; each R2 unit is independently selected from the group consisting of: a) hydrogen; b) —(CH2)jO(CH2)nR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —(CH2)jCON(R10)2; g) —(CH2)jOCON(R10)2; h) two R2 units can be taken together to form a carbonyl unit; i) and mixtures thereof; 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, n is an index from 0 to 5; Z is O, S, NR11, or NOR11; R11 is hydrogen or C1–C4 alkyl.

2. 发明授权

US06821971B2 Fused pyrazolone compounds which inhibit the release of inflammatory cytokines 失效
标题翻译：抑制炎性细胞因子释放的融合的吡唑啉酮化合物
公开(公告)号：US06821971B2
公开(公告)日：2004-11-23
申请号：US10245927
申请日：2002-09-18
申请人： Michael Philip Clark , Matthew John Laufersweiler , Jane Far-Jine Djung , Biswanath De
发明人： Michael Philip Clark , Matthew John Laufersweiler , Jane Far-Jine Djung , Biswanath De
IPC分类号： C07D48704
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; R2a and R2b units are each independently hydrogen, ethers, amines, amides, carboxylates, or said units can form a double bond, a carbonyl, or R2a and R2b can be taken together to form a substituted or unsubstituted ring comprising from 4 to 8 atoms, said ring selected from the group consisting of: i) carbocyclic; ii) heterocyclic; iii) aryl; iv) heteroaryl; v) bicyclic; and vi) heterobicyclic.
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; R 2a和R 2b单元各自独立地为氢，醚，胺，酰胺，羧酸盐或所述单元可以形成双键，羰基或R 2a， 2b）可以一起形成包含4至8个原子的取代或未取代的环，所述环选自：i）碳环; ii）杂环; iii）芳基; iv）杂芳基; v）双环; andvi）杂双环。

3. 发明授权

US06960593B2 6,7-dihydro-5H-pyrazolo[1,2a]pyrazol-1-ones which control inflammatory cytokines 失效
标题翻译： 6,7-二氢-5H-吡唑并[1,2a]吡唑-1-酮，其控制炎性细胞因子
公开(公告)号：US06960593B2
公开(公告)日：2005-11-01
申请号：US10661730
申请日：2003-09-12
申请人： Michael Philip Clark , Matthew John Laufersweiler
发明人： Michael Philip Clark , Matthew John Laufersweiler
IPC分类号： A61P29/00 , C07D487/04 , C07D491/20 , C07D495/20 , A61P19/02 , A61K31/516
CPC分类号： C07D487/04
摘要： The present invention relates to 2-(4-fluorophenyl)-3-(2-phenoxy-pyrimidin-4-yl)-6,7-dihydro-5H-pyrazolo-[1,2-a]pyrazol-1-one, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, having the formula: and pharmaceutical compositions thereof, and methods for controlling the level of one or more inflammation inducing cytokines selected from the group consisting of, interleukin-1 (IL-1), Tumor Necrosis Factor-α(TNF-α), interleukin-6 (IL-6), and interleukin-8 (IL-8), thereby controlling, mediating, or abating disease states affected by the level of extracellular inflammatory cytokines in humans.
摘要翻译：本发明涉及2-（4-氟苯基）-3-（2-苯氧基 - 嘧啶-4-基）-6,7-二氢-5H-吡唑并[1,2-a]吡唑-1-酮，包括具有下式的所有对映异构体和非对映体形式及其药学上可接受的盐：及其药物组合物，以及用于控制一种或多种炎性诱导细胞因子水平的方法，所述细胞因子选自白介素-1（IL-1），肿瘤坏死因子-α（TNF-α），白细胞介素-6（IL-6）和白细胞介素-8（IL-8），从而控制，介导或减轻受到人类细胞外炎症细胞因子水平的影响。

4. 发明授权

US06730668B2 6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines 失效
标题翻译： 6,7-二氢-5H-吡唑并[1,2-a]吡唑-1-酮，其控制炎性细胞因子
公开(公告)号：US06730668B2
公开(公告)日：2004-05-04
申请号：US10246214
申请日：2002-09-18
申请人： Michael Philip Clark , Matthew John Laufersweiler , Jane Far-Jine Djung , Michael George Natchus , Biswanath De
发明人： Michael Philip Clark , Matthew John Laufersweiler , Jane Far-Jine Djung , Michael George Natchus , Biswanath De
IPC分类号： C07D41314
CPC分类号： C07D487/04
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; each R2 unit is independently selected from the group consisting of: a) hydrogen; b) —(CH2)jO(CH2)nR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —(CH2)jCON(R10)2; g) —(CH2)jOCON(R10)2; h) two R2 units can be taken together to form a carbonyl unit; i) and mixtures thereof; 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, n is an index from 0 to 5; Z is O, S, NR11, or NOR11; R11 is hydrogen or C1-C4 alkyl.
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：）取代或未取代的芳基; 环）取代或未取代的杂芳基;每个R 2单元独立地选自：a）氢; b） - （CH 2）j O（CH 2）n R 8; c） - （CH 2）j NR 9 d） - （CH 2）j CO 2 R 10; e） - （CH 2）j CO 2 R 10 f） - （CH 2）j CON（R 10）2; g） - （CH 2） R 10）2; h）两个R 2单元可以一起形成羰基单元; i）及其混合物; R 8，R 9a，R 9b和R 10 各自独立地为氢，C 1 -C 4烷基及其混合物; R 9a和R 9b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为0至5的指数，n为0至5的指数; Z为O，S，NR 11或NOR 11; R 11是氢或C 1 -C 4烷基。

5. 发明授权

US07368455B2 6,7-Dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines 失效
标题翻译： 6,7-二氢-5H-吡唑并[1,2-a]吡唑-1-酮，其控制炎性细胞因子
公开(公告)号：US07368455B2
公开(公告)日：2008-05-06
申请号：US11159662
申请日：2005-06-23
申请人： Michael Philip Clark , Matthew John Laufersweiler
发明人： Michael Philip Clark , Matthew John Laufersweiler
IPC分类号： C07D487/04 , C07D403/04 , A61K31/506 , A61K31/416 , A61P19/02
CPC分类号： C07D487/04
摘要： The present invention relates to 2-(4-fluorophenyl)-3-(2-phenoxy-pyrimidin-4-yl)-6,7-dihydro-5H-pyrazolo-[1,2-a]pyrazol-1-one, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, having the formula: and pharmaceutical compositions thereof, and methods for controlling the level of one or more inflammation inducing cytokines selected from the group consisting of, interleukin-1 (IL-1), Tumor Necrosis Factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-8 (IL-8), thereby controlling, mediating, or abating disease states affected by the level of extracellular inflammatory cytokines in humans.
摘要翻译：本发明涉及2-（4-氟苯基）-3-（2-苯氧基 - 嘧啶-4-基）-6,7-二氢-5H-吡唑并[1,2-a]吡唑-1-酮，包括具有下式的所有对映异构体和非对映体形式及其药学上可接受的盐：及其药物组合物，以及用于控制一种或多种炎性诱导细胞因子水平的方法，所述细胞因子选自白介素-1（IL-1），肿瘤坏死因子-α（TNF-α），白细胞介素-6（IL-6）和白细胞介素-8（IL-8），从而控制，介导或减轻受到人类细胞外炎症细胞因子水平的影响。

6. 发明授权

US06849627B2 6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines 失效
标题翻译： 6,7-二氢-5H-吡唑并[1,2-a]吡唑-1-酮，其控制炎性细胞因子
公开(公告)号：US06849627B2
公开(公告)日：2005-02-01
申请号：US10390216
申请日：2003-03-17
申请人： Michael Philip Clark , Matthew John Laufersweiler , Adam Golebiowski , Mark Sabat , Todd Andrew Brugel
发明人： Michael Philip Clark , Matthew John Laufersweiler , Adam Golebiowski , Mark Sabat , Todd Andrew Brugel
IPC分类号： C07D487/04 , C07D491/20 , C07D495/20 , C07D403/04 , A61K31/501 , C07D403/14
CPC分类号： C07D487/04
摘要： The present invention relates to compounds 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 R1 is substituted aryl; R4 is substituted or unsubstituted aryl or heteroaryl.
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 1是取代的芳基; R 4是取代或未取代的芳基或杂芳基。

7. 发明授权

US06677337B2 1,2-dihydropyrazol-3-ones which controls inflammatory cytokines 失效
标题翻译：控制炎性细胞因子的1,2-二氢吡唑-3-酮
公开(公告)号：US06677337B2
公开(公告)日：2004-01-13
申请号：US10382060
申请日：2003-03-05
申请人： Matthew John Laufersweiler , Cynthia Monesa Crago Clark , Michael Philip Clark , Jane Far-Jine Djung , Biswanath De , Michael George Natchus
发明人： Matthew John Laufersweiler , Cynthia Monesa Crago Clark , Michael Philip Clark , Jane Far-Jine Djung , Biswanath De , Michael George Natchus
IPC分类号： A61K31513
CPC分类号： C07D401/14 , A61K31/505 , C07D403/04 , C07D403/14 , C07D405/14 , C07D407/14 , C07D417/14
摘要： The present invention relates to compounds which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, or enantiomeric and diasteriomeric forms or pharmaceutically acceptable salts thereof, have the formula: wherein R is an ether or amino unit, R1 is substituted phenyl, each R2 and R3 unit is independently selected from the group consisting of: a) hydrogen; and b) substituted or unsubstituted C1-C10 hydrocarbyl selected from the group consisting of: i) C1-C10 linear, branched or cyclic alkyl; ii) C1-C10 aryl; iii) C1-C10 heterocyclic; iv) C1-C10 heteroaryl.
摘要翻译：本发明涉及能够防止炎性细胞因子，所述化合物或对映异构体和非对映体形式或其药学上可接受的盐的细胞外释放的化合物，其具有下式：其中R是醚或氨基单元，R 1是取代的苯基，每个R 2和R 3单元独立地选自：a）氢; 和）b）C 1 -C 10杂环; iv）C 1 -C 10杂芳基。

8. 发明授权

US06566357B1 Spirocyclic-6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines 失效
标题翻译：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。

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