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2. 发明专利

AU2002316421B2 N-heterocyclic inhibitors of TNF-ALPHA expression 未知
公开(公告)号：AU2002316421B2
公开(公告)日：2008-05-15
申请号：AU2002316421
申请日：2002-06-26
申请人： SQUIBB BRISTOL MYERS CO , PHARMACOPEIA INC
发明人： AHMED GULZAR , DILLER DAVID J , METZGER AXEL , HENDERSON IAN , WROBLESKI STEPHEN T , LEFTHERIS KATERINA , WEN JAMES
IPC分类号： C07D213/85 , A61K31/44 , A61K31/505 , A61K31/506 , A61K31/551 , A61K31/56 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/06 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P29/02 , A61P31/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/48 , C07D239/50 , C07D401/12 , C07D403/12 , C07D403/14 , C07D409/12
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.

3. 发明专利

HU0401711A2 N-HETEROCYCLIC INHIBITORS OF TNF-ALPHA AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：HU0401711A2
公开(公告)日：2004-12-28
申请号：HU0401711
申请日：2002-06-26
申请人： SQUIBB BRISTOL MYERS CO , PHARMACOPEIA
发明人： AHMED GULZAR , METZGER AXEL , WROBLESKI STEPHEN T , HENDERSON IAN , WEN JAMES , DILLER DAVID J , LEFTHERIS KATERINA
IPC分类号： A61K31/44 , A61K31/505 , A61K31/506 , A61K31/551 , A61K31/56 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/06 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P29/02 , A61P31/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D213/85 , C07D239/48 , C07D239/50 , C07D401/12 , C07D403/12 , C07D403/14 , C07D409/12 , C07D239/42
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.

4. 发明专利

CA2451128A1 N-HETEROCYCLIC INHIBITORS OF TNF-ALPHA EXPRESSION 未知
公开(公告)号：CA2451128A1
公开(公告)日：2003-01-09
申请号：CA2451128
申请日：2002-06-26
申请人： SQUIBB BRISTOL MYERS CO
发明人： AHMED GULZAR , METZGER AXEL , DILLER DAVID J , WEN JAMES , WROBLESKI STEPHEN T , LEFTHERIS KATERINA , HENDERSON IAN
IPC分类号： A61K31/44 , A61K31/505 , A61K31/506 , A61K31/551 , A61K31/56 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/06 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P29/02 , A61P31/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D213/85 , C07D239/48 , C07D239/50 , C07D401/12 , C07D403/12 , C07D403/14 , C07D409/12 , C07D239/42
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p3 8 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I). Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriat e p38 kinase activity or TNF-.alpha. expression utilizing compounds of the present invention are also disclosed.

5. 发明申请

WO2007104053A3 8-HETEROARYLPURINE MNK2 INHIBITORS FOR TREATING METABOLIC DISORDERS 审中-公开
标题翻译： 8-HETEROARYLPURINE MNK2用于治疗代谢性疾病的抑制剂
公开(公告)号：WO2007104053A3
公开(公告)日：2007-11-01
申请号：PCT/US2007063699
申请日：2007-03-09
申请人： PHARMACOPEIA INC , COLE ANDREW G , BRESCIA MARC-RALEIGH , ZHANG JOAN J , HUSSAIN ZAHID , DILLER DAVID J , METZGER AXEL , AHMED GULZAR , HENDERSON IAN
发明人： COLE ANDREW G , BRESCIA MARC-RALEIGH , ZHANG JOAN J , HUSSAIN ZAHID , DILLER DAVID J , METZGER AXEL , AHMED GULZAR , HENDERSON IAN
IPC分类号： C07D473/32 , A61K31/52 , A61P3/00
CPC分类号： C07D473/32
摘要： This invention relates to 8-Heteroarylpurine Mnk2 Inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.
摘要翻译：本发明涉及可用于治疗和预防代谢性疾病如肥胖症和糖尿病的8-杂芳基嘌呤Mnk2抑制剂。

6. 发明申请

WO0197098A3 COMPUTATIONAL MOLECULAR DOCKING METHODS FOR ASSESSING COMPLEMENTARITY OF COMBINATORIAL LIBRARIES TO BIOTARGETS 审中-公开
标题翻译：用于评估组合图书馆对生物技术的补充的计算分子锁定方法
公开(公告)号：WO0197098A3
公开(公告)日：2003-08-28
申请号：PCT/US0119318
申请日：2001-06-15
申请人： PHARMACOPEIA INC , DILLER DAVID J , MERZ KENNETH M JR
发明人： DILLER DAVID J , MERZ KENNETH M JR
IPC分类号： G01N33/15 , C07K1/04 , C40B30/02 , G06F19/00 , G06F19/16 , G06F19/18 , G01N33/68 , G06F17/50
CPC分类号： C07K1/047 , C40B30/02 , G06F19/16 , G06F19/706 , G06F19/707
摘要： A high-throughput molecular docking facility is presented for screening combinatorial libraries to identity binding ligands and ultimately pharmaceutical compounds. The facility employs a pre-coking conformational search to generate multiple solution conformations of a ligand. The molecular docking facility includes: generating a binding site image of the target molecule, the binding site image to atoms in at least one solution conformation of the multiple solution conformations of the ligand to obtain at least one ligand position relative to the target molecule in a ligand-target molecule complex formation; and optimizing the at least one ligand position while allowing translation, orientation and rotatable bonds of the ligand to vary, and while holding the target molecule fixed. Docking results are clustered using as a metric the rms deviation between the core of two docked molecules. A library is rated is rated as to complementarity to the target molecule according to the relative number of ligands in the top cluster.
摘要翻译：提出了一种高通量分子对接设备，用于筛选组合文库以鉴定结合配体和最终的药物化合物。该设施采用预焦化构象搜索以产生配体的多个溶液构象。分子对接设备包括：产生靶分子的结合位点图像，以配体的多个溶液构象的至少一个溶液构象中的原子的结合位点图像，以获得相对于靶分子的至少一个配体位置配体 - 靶分子复合体形成; 并优化至少一个配体位置，同时允许配体的翻译，取向和可旋转键发生变化，同时保持靶分子固定。对接结果使用两个对接分子的核心之间的均方根偏差作为度量进行聚类。根据顶部簇中配体的相对数量，对额定分子量的额定值与靶分子互补。

7. 发明专利

EA014907B1 ИНГИБИТОРЫ Mnk2 НА ОСНОВЕ 8-ГЕТЕРОАРИЛПУРИНА ДЛЯ ЛЕЧЕНИЯ МЕТАБОЛИЧЕСКИХ НАРУШЕНИЙ 未知
公开(公告)号：EA014907B1
公开(公告)日：2011-02-28
申请号：EA200801897
申请日：2007-03-09
申请人： PHARMACOPEIA INC
发明人： COLE ANDREW G , BRESCIA MARC-RALEIGH , ZHANG JOAN J , HUSSAIN ZAHID , DILLER DAVID J , METZGER AXEL , AHMED GULZAR , HENDERSON IAN
IPC分类号： C07D473/32 , A61K31/52 , A61P3/00
摘要： Визобретенииописанысоединенияформулыкоторыеявляютсяингибиторами Mnk2 икоторыеможноиспользоватьдлялеченияи профилактикиметаболическихнарушений, такихкакожирениеи диабет.

8. 发明专利

CA2411190A1 MOLECULAR DOCKING METHODS FOR ASSESSING COMPLEMENTARITY OF COMBINATORIAL LIBRARIES TO BIOTARGETS 未知
公开(公告)号：CA2411190A1
公开(公告)日：2001-12-20
申请号：CA2411190
申请日：2001-06-15
申请人： PHARMACOPEIA INC
发明人： DILLER DAVID J , MERZ KENNETH M JR
IPC分类号： G01N33/15 , C07K1/04 , C40B30/02 , G06F19/00 , G06F19/16 , G06F19/18 , G06F17/50
摘要： A high-throughput molecular docking facility is presented for screening combinatorial libraries to identity binding ligands and ultimately pharmaceutical compounds. The facility employs a pre-coking conformational search to generate multiple solution conformations of a ligand. The molecula r docking facility includes: generating a binding site image of the target molecule, the binding site image to atoms in at least one solution conformation of the multiple solution conformations of the ligand to obtain at least one ligand position relative to the target molecule in a ligand-target molecule complex formation; and optimizing the at least one ligand position while allowing translation, orientation and rotatable bonds of the ligand to vary, and while holding the target molecule fixed. Docking results are clustered using as a metric the rms deviation between the core of two docked molecules. A library is rated is rated as to complementarity to the target molecule according to the relative number of ligands in the top cluster.

9. 发明专利

BRPI0709007A2 未知
公开(公告)号：BRPI0709007A2
公开(公告)日：2011-06-21
申请号：BRPI0709007
申请日：2007-03-09
申请人： PHARMACOPEIA INC
发明人： COLE ANDREW G , BRESCIA MARC-RALEIGH , ZHANG JOAN J , HUSSAIN ZAHID , DILLER DAVID J , METZGER AXEL , AHMED GULZAR , HENDERSON IAN
IPC分类号： C07D473/32 , A61K31/52 , A61P3/00
摘要： Compounds of the formula are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.

10. 发明专利

ZA200807715B 9-Heteroarylpurine MNK2 inhibitors for treating metabolic disorders 未知
公开(公告)号：ZA200807715B
公开(公告)日：2009-11-25
申请号：ZA200807715
申请日：2007-03-09
申请人： PHARMACOPEIA INC
发明人： COLE ANDREW G , MARC-RALEIGH BRESCIA , ZHANG JOAN J , ZAHID HUSSAIN , DILLER DAVID J , AXEL METZGER , GULZAR AHMED , IAN HENDERSON
IPC分类号： A61K20100101 , A61P20100101 , C07D20100101
摘要： Compounds of the formula are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.

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