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1. 发明授权

US06562854B2 Compositions comprising a substituted benzimidazole useful for treating immunomediated inflammatory disorders 失效
公开(公告)号：US06562854B2
公开(公告)日：2003-05-13
申请号：US09874412
申请日：2001-06-04
申请人： Timothy J. Church , Neil Scott Cutshall , Anthony R. Gangloff , Thomas E. Jenkins , Martin S. Linsell , Joane Litvak , Kenneth D. Rice , Jeffrey R. Spencer , Vivian R. Wang
发明人： Timothy J. Church , Neil Scott Cutshall , Anthony R. Gangloff , Thomas E. Jenkins , Martin S. Linsell , Joane Litvak , Kenneth D. Rice , Jeffrey R. Spencer , Vivian R. Wang
IPC分类号： A61K314184
CPC分类号： C07D231/12 , A61F5/445 , C07D233/56 , C07D235/20 , C07D249/08 , C07D401/14 , C07D403/14 , C07D413/06 , C07D413/14 , C07D471/04 , C07F7/0812
摘要： Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.

2. 发明授权

US6150379A Compounds and compositions as anticoagulants 失效
标题翻译：化合物和组合物作为抗凝剂
公开(公告)号：US6150379A
公开(公告)日：2000-11-21
申请号：US193202
申请日：1998-11-17
申请人： Paul R. Fatheree , Thomas E. Jenkins , Martin S. Linsell , Sean G. Trapp , Erik J. Verner , Wendy B. Young
发明人： Paul R. Fatheree , Thomas E. Jenkins , Martin S. Linsell , Sean G. Trapp , Erik J. Verner , Wendy B. Young
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/04 , C07D471/04 , A61K31/4184 , A61K31/4439 , C07D235/18
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/04 , C07D471/04
摘要： The present invention relates to novel biheterocyclic derivatives which are factor Xa inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.
摘要翻译：本发明涉及作为因子Xa抑制剂的新型双杂环衍生物; 其药学上可接受的盐和N-氧化物; 它们作为治疗剂的用途及其制备方法。

3. 发明授权

US06518242B1 Derivatives of glycopeptide antibacterial agents 有权
标题翻译：糖肽抗菌剂的衍生物
公开(公告)号：US06518242B1
公开(公告)日：2003-02-11
申请号：US09253670
申请日：1999-02-19
申请人： Qi-Qi Chen , John H. Griffin , Thomas E. Jenkins , J. Kevin Judice , Martin S. Linsell , Michael R. Leadbetter
发明人： Qi-Qi Chen , John H. Griffin , Thomas E. Jenkins , J. Kevin Judice , Martin S. Linsell , Michael R. Leadbetter
IPC分类号： A61K3812
CPC分类号： C07K9/008 , A61K38/00
摘要： Novel antibacterial agents that act as multibinding agents are disclosed. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of binding to a transglycosylase enzyme substrate thereby modulating the biological processes/functions thereof.
摘要翻译：公开了作为多结合剂的新型抗菌剂。本发明的化合物包含共价连接的2-10个配体，每个所述配体能够结合转糖基酶底物，从而调节其生物学过程/功能。

4. 发明授权

US06576791B1 Local anesthetic compounds and uses 有权
公开(公告)号：US06576791B1
公开(公告)日：2003-06-10
申请号：US09647802
申请日：2000-10-03
申请人： Sabine M. Axt , Timothy J. Church , Witold N. Hruzewicz , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , J. Kevin Judice
发明人： Sabine M. Axt , Timothy J. Church , Witold N. Hruzewicz , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , J. Kevin Judice
IPC分类号： C07C23305
CPC分类号： C07C237/34 , C07C237/04 , C07D211/60 , C07D273/00
摘要： Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.

5. 发明授权

US06495681B1 Local anesthetic compounds and uses 有权
标题翻译：局部麻醉剂及其用途
公开(公告)号：US06495681B1
公开(公告)日：2002-12-17
申请号：US09690019
申请日：2000-10-17
申请人： Sabine M. Axt , Timothy J. Church , Witold Hruzewicz , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , J. Kevin Judice
发明人： Sabine M. Axt , Timothy J. Church , Witold Hruzewicz , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , J. Kevin Judice
IPC分类号： C07D27308
CPC分类号： C07C237/34 , C07C237/04 , C07D211/60 , C07D273/00
摘要： Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.
摘要翻译：公开了新的化合物，药物组合物和方法用于产生长时间的局部麻醉。本发明的化合物是包含共价连接到连接体或连接体的2至10个配体的多结合化合物，每个配体能够结合电压门控Na +通道中的配体结合位点以调节其生物学过程/功能。

6. 发明授权

US06462034B1 Local anesthetic compounds and uses 有权
公开(公告)号：US06462034B1
公开(公告)日：2002-10-08
申请号：US09411331
申请日：1999-10-01
申请人： Sabine M. Axt , Timothy J. Church , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , J. Kevin Judice , Huiwei Wu , Witold Hruzewicz
发明人： Sabine M. Axt , Timothy J. Church , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , J. Kevin Judice , Huiwei Wu , Witold Hruzewicz
IPC分类号： A61K4372
CPC分类号： C07C237/04 , C07C237/34 , C07D211/60 , C07D273/00
摘要： Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.

7. 发明授权

US06355637B1 Local anesthetic compounds 有权
标题翻译：局部麻醉化合物
公开(公告)号：US06355637B1
公开(公告)日：2002-03-12
申请号：US09671626
申请日：2000-09-28
申请人： Sabine M. Axt , Timothy J. Church , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , Huiwei Wu
发明人： Sabine M. Axt , Timothy J. Church , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , Huiwei Wu
IPC分类号： C07D41306
CPC分类号： C07D273/00 , C07D239/90 , C07D413/06 , C07D413/14
摘要： This invention provides novel quinazolinone compounds and pharmaceutically acceptable salts thereof, which are useful as local anesthetics. This invention also provides pharmaceutical compositions containing such compounds; methods for producing local anesthesia in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.
摘要翻译：本发明提供了可用作局部麻醉剂的新颖的喹唑啉酮化合物及其药学上可接受的盐。本发明还提供含有这些化合物的药物组合物; 使用这种化合物在哺乳动物中产生局部麻醉的方法; 以及可用于制备这些化合物的方法和中间体。

8. 发明授权

US06436919B1 Local anesthetic compounds 有权
标题翻译：局部麻醉化合物
公开(公告)号：US06436919B1
公开(公告)日：2002-08-20
申请号：US09671630
申请日：2000-09-28
申请人： Sabine M. Axt , Timothy J. Church , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , Huiwei Wu
发明人： Sabine M. Axt , Timothy J. Church , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , Huiwei Wu
IPC分类号： C07D41306
CPC分类号： C07D273/00 , C07D239/90 , C07D413/06 , C07D413/14
摘要： This invention is directed to novel local anesthetic compounds, pharmaceutical compositions containing these compounds, methods of use and methods of preparing these compounds. In one embodiment, the compounds are of the following formula: wherein: R1 and R2 are independently selected from the group consisting of hydrogen, alkyl, halo, cyano, hydroxy, alkoxy, amino, monosubstituted or disubstituted amino, carboxy, and alkoxycarbonyl; R5 and R6 are independently selected from the group consisting of hydrogen and alkyl; R7 is alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, or substituted heterocycle; R8 and R9 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl and NRaRb-where Ra and Rb are alkyl; and Ar is selected from the group consisting of aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, substituted heterocycle, cycloalkyl and substituted cycloalkyl; or a pharmaceutically acceptable salt thereof. The compounds find use as local anesthetics.
摘要翻译：本发明涉及新的局部麻醉剂化合物，含有这些化合物的药物组合物，使用方法和制备这些化合物的方法。在一个实施方案中，所述化合物具有下式：其中：R 1和R 2独立地选自氢，烷基，卤素，氰基，羟基，烷氧基，氨基，单取代或二取代的氨基，羧基和烷氧基羰基; R5和R6独立地选自氢和烷基; R 7是烷基，取代的烷基，芳基，取代的芳基，杂芳基，取代的杂芳基，杂环或取代的杂环; R 8和R 9独立地选自氢，烷基，取代的烷基和NR a R b，其中R a和R b是烷基; 并且Ar选自芳基，取代的芳基，杂芳基，取代的杂芳基，杂环，取代的杂环，环烷基和取代的环烷基; 或其药学上可接受的盐。该化合物可用作局部麻醉剂。

9. 发明授权

US06420354B1 Sodium channel drugs and uses 有权
公开(公告)号：US06420354B1
公开(公告)日：2002-07-16
申请号：US09458107
申请日：1999-12-08
申请人： Daniel Marquess , Seok-Ki Choi , David T. Beattie , John H. Griffin , Scott Armstrong , Timothy J. Church , Thomas E. Jenkins
发明人： Daniel Marquess , Seok-Ki Choi , David T. Beattie , John H. Griffin , Scott Armstrong , Timothy J. Church , Thomas E. Jenkins
IPC分类号： C07D24502
CPC分类号： C07D239/48 , A61K47/55 , A61K47/65 , G01N33/6872 , G01N2500/04
摘要： The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Na+ channel, thereby modulating the biological activities thereof.

10. 发明授权

US06337423B1 Local anesthetic compounds and uses 有权
公开(公告)号：US06337423B1
公开(公告)日：2002-01-08
申请号：US09285054
申请日：1999-04-02
申请人： Sabine M. Axt , Timothy J. Church , Witold Hruzewicz , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , J. Kevin Judice
发明人： Sabine M. Axt , Timothy J. Church , Witold Hruzewicz , John R. Jacobsen , Thomas E. Jenkins , Yu-Hua Ji , J. Kevin Judice
IPC分类号： C07C23305
CPC分类号： C07C237/34 , C07C237/04 , C07D211/60 , C07D273/00
摘要： Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.

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