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1. 发明授权

US07951803B2 8-heteroarylpurine MNK2 inhibitors for treating metabolic disorders 有权
标题翻译：用于治疗代谢紊乱的8-杂芳基嘌呤MNK2抑制剂
公开(公告)号：US07951803B2
公开(公告)日：2011-05-31
申请号：US11684262
申请日：2007-03-09
申请人： Andrew G. Cole , Marc-Raleigh Brescia , Joan J. Zhang , Zahid Hussain , David J. Diller , Axel Metzger , Gulzar Ahmed , Ian Henderson
发明人： Andrew G. Cole , Marc-Raleigh Brescia , Joan J. Zhang , Zahid Hussain , David J. Diller , Axel Metzger , Gulzar Ahmed , Ian Henderson
IPC分类号： C07D473/32 , A61K31/52 , A61P3/10 , A61P3/04 , A61P19/02 , C07D409/12 , C07D239/26 , C07D239/28
CPC分类号： C07D473/32
摘要： Compounds of the formula wherein R1 represents optionally substituted C1-C10 alkyl, aryl or heteroaryl, and R3 represents alkoxy-substituted aryl or optionally substituted heteroaryl, are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.
摘要翻译：公开了下式的化合物，其中R 1表示任选取代的C 1 -C 10烷基，芳基或杂芳基，R 3表示烷氧基取代的芳基或任选取代的杂芳基，被公开为Mnk2抑制剂，其可用于治疗和预防代谢性疾病如肥胖症和糖尿病。

2. 发明申请

US20110230480A1 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：US20110230480A1
公开(公告)日：2011-09-22
申请号：US13118166
申请日：2011-05-27
申请人： Andrew G. Cole , Marc-Raleigh Brescia , Joan J. Zhang , Zahid Hussain , David J. Diller , Axel Metzger , Gulzar Ahmed , Ian Henderson
发明人： Andrew G. Cole , Marc-Raleigh Brescia , Joan J. Zhang , Zahid Hussain , David J. Diller , Axel Metzger , Gulzar Ahmed , Ian Henderson
IPC分类号： A61K31/52 , A61K31/5377 , A61P25/00 , A61P3/00 , A61P3/04 , A61P3/10 , A61P25/28 , A61P35/00
CPC分类号： C07D473/32
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.
摘要翻译：公开的化合物作为可用于治疗和预防代谢性疾病如肥胖症和糖尿病的Mnk2抑制剂。

3. 发明授权

US08044040B2 N-heterocyclic inhibitors of TNF-alpha expression 有权
标题翻译： TNF-α表达的N-杂环抑制剂
公开(公告)号：US08044040B2
公开(公告)日：2011-10-25
申请号：US11778219
申请日：2007-07-16
申请人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
发明人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
IPC分类号： C07D239/48 , A61K31/505
CPC分类号： C07D239/48 , C07D213/85 , C07D239/47 , C07D239/50 , C07D401/12 , C07D403/12
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.
摘要翻译：公开了通过抑制p38激酶阻断细胞因子产生的N-杂环化合物。在一个实施方案中，本发明化合物由式（I）表示：还公开了使用本发明化合物治疗与p38激酶活性不适或TNF-α表达相关的病症的生产方法，药物组合物和方法。

4. 发明申请

US20080015185A1 N-HETEROCYCLIC INHIBITORS OF TNF-ALPHA EXPRESSION 有权
标题翻译： TNF-ALPHA表达的N-杂环化合物抑制剂
公开(公告)号：US20080015185A1
公开(公告)日：2008-01-17
申请号：US11778219
申请日：2007-07-16
申请人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
发明人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
IPC分类号： A61K31/513 , A61K31/55 , A61P29/00 , C07D239/50
CPC分类号： C07D239/48 , C07D213/85 , C07D239/47 , C07D239/50 , C07D401/12 , C07D403/12
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.
摘要翻译：公开了通过抑制p38激酶阻断细胞因子产生的N-杂环化合物。在一个实施方案中，本发明的化合物由式（I）表示：还公开了使用本发明的化合物来治疗与不适当p38激酶活性或TNF-α表达相关的病症的生产方法，药物组合物和方法。

5. 发明授权

US07253174B2 N-heterocyclic inhibitors of TNF-α expression 有权
标题翻译： TNF-α表达的N-杂环抑制剂
公开(公告)号：US07253174B2
公开(公告)日：2007-08-07
申请号：US11485075
申请日：2006-07-12
申请人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
发明人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
IPC分类号： C07D239/48 , A61K31/505
CPC分类号： C07D239/48 , C07D213/85 , C07D239/47 , C07D239/50 , C07D401/12 , C07D403/12
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.
摘要翻译：公开了通过抑制p38激酶阻断细胞因子产生的N-杂环化合物。在一个实施方案中，本发明的化合物由式（I）表示：还公开了使用本发明的化合物来治疗与不适当p38激酶活性或TNF-α表达相关的病症的生产方法，药物组合物和方法。

6. 发明授权

US07065453B1 Molecular docking technique for screening of combinatorial libraries 有权
标题翻译：用于筛选组合文库的分子对接技术
公开(公告)号：US07065453B1
公开(公告)日：2006-06-20
申请号：US09595096
申请日：2000-06-15
申请人： David J. Diller , Kenneth M. Merz, Jr.
发明人： David J. Diller , Kenneth M. Merz, Jr.
IPC分类号： G06G7/48 , G06N7/06
CPC分类号： C07K1/047
摘要： A high-throughput molecular docking facility is presented for screening combinatorial libraries to identify binding ligands and ultimately pharmaceutical compounds. The facility employs a pre-docking conformational search to generate multiple solution conformations of a ligand. The molecular docking facility includes: generating a binding site image of the protein, the binding site image having multiple hot spots; matching hot spots of 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 protein in a ligand-protein 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 protein fixed.
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。该设施采用预对接构建搜索以产生配体的多个溶液构象。分子对接设备包括：产生蛋白质的结合位点图像，结合位点图像具有多个热点; 将结合位点图像的热点与配体的多个溶液构象的至少一个溶液构象中的原子匹配，以获得在配体 - 蛋白质复合物形成中相对于蛋白质的至少一个配体位置; 并优化至少一个配体位置，同时允许配体的翻译，取向和可旋转的键发生变化，同时保持蛋白质固定。

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