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1. 发明授权

US4945160A Preparation of certain 7-substituted quinolones 失效
标题翻译：某些7-取代喹诺酮的制备
公开(公告)号：US4945160A
公开(公告)日：1990-07-31
申请号：US275149
申请日：1988-11-22
申请人： John S. Kiely , Lawrence E. Lesheski , Mel C. Schroeder
发明人： John S. Kiely , Lawrence E. Lesheski , Mel C. Schroeder
IPC分类号： C07D215/56 , C07D401/04 , C07D471/04 , C07D471/06 , C07D498/06 , C07D513/06
CPC分类号： C07D401/04 , C07D215/56 , C07D471/04 , C07D471/06 , C07D513/06
摘要： Novel processes for the coupling of alkyl, alkenyl, alkynyl, or aryl groups to the seven position of quinolines and naphthyridines is disclosed. Novel intermediates and final compounds having antibacterial activity are also described as well as the formulations for the same use.
摘要翻译：公开了将烷基，烯基，炔基或芳基偶联到喹啉和萘啶的7位上的新方法。还描述了具有抗菌活性的新型中间体和最终化合物以及相同用途的制剂。

2. 发明授权

US5461165A Individual stereoisomers of intermediates of 7-[3-(1-aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones as antibacterial agents 失效
标题翻译： 7- [3-（1-氨基烷基）-1-吡咯烷基] - 喹诺酮和萘啶酮作为抗菌剂的中间体的单独立体异构体
公开(公告)号：US5461165A
公开(公告)日：1995-10-24
申请号：US221146
申请日：1994-03-30
申请人： John M. Domagala , John S. Kiely , Mel C. Schroeder
发明人： John M. Domagala , John S. Kiely , Mel C. Schroeder
IPC分类号： C07D207/09 , C07D207/26 , C07D401/04 , C07D471/04
CPC分类号： C07D207/26 , C07D207/09 , C07D401/04 , C07D471/04
摘要： Individual stereoisomers of 7-[3-(1-aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones are described, their therapeutic advantages as antibacterial agents, as well as a novel method for the preparation and isolation of such stereoisomers.
摘要翻译：描述了7- [3-（1-氨基烷基）-1-吡咯烷基] - 喹诺酮和萘啶酮的单个立体异构体，它们作为抗菌剂的治疗优点，以及制备和分离这些立体异构体的新方法。

3. 发明授权

US5702672A Apparatus and method for multiple simultaneous synthesis 失效
标题翻译：多种同步合成的装置和方法
公开(公告)号：US5702672A
公开(公告)日：1997-12-30
申请号：US540512
申请日：1995-10-10
申请人： Sheila H. H. DeWitt , Michael Kell , Michael R. Pavia , John S. Kiely , Mel C. Schroeder , Charles J. Stankovic , Steven Ware
发明人： Sheila H. H. DeWitt , Michael Kell , Michael R. Pavia , John S. Kiely , Mel C. Schroeder , Charles J. Stankovic , Steven Ware
IPC分类号： B01J19/00 , C07K1/04 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , B01J8/00 , C07K17/00 , C12M1/00
CPC分类号： C07K1/047 , B01J19/0046 , C07K1/045 , B01J2219/00283 , B01J2219/00308 , B01J2219/0031 , B01J2219/00373 , B01J2219/00416 , B01J2219/00423 , B01J2219/00454 , B01J2219/00493 , B01J2219/00495 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00689 , B01J2219/00695 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14
摘要： An apparatus for multiple, simultaneous synthesis of compounds which consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold.
摘要翻译：一种用于多次同时合成化合物的装置，其包括：具有多个孔的储存器块; 多个反应管，通常为气体分散管，在其下端具有过滤器; 具有多个孔的保持器块; 以及可以具有允许引入/维护受控环境的端口的歧管。歧管顶壁具有孔和具有相同孔的可拆卸板。该装置由适应加热，冷却，搅拌或腐蚀性试剂的材料构成。垫片放在组件之间。提供杆或夹具用于将部件固定在一起。设备操作涉及将过滤器放置在储存器块井中的反应管的下端，并且通过保持器的上端阻挡孔并进入歧管。

4. 发明授权

US5582801A Apparatus for multiple simultaneous synthesis 失效
标题翻译：多次同时合成的装置
公开(公告)号：US5582801A
公开(公告)日：1996-12-10
申请号：US463545
申请日：1995-06-05
申请人： Sheila H. H. DeWitt , John S. Kiely , Michael R. Pavia , Mel C. Schroeder , Charles J. Stankovic
发明人： Sheila H. H. DeWitt , John S. Kiely , Michael R. Pavia , Mel C. Schroeder , Charles J. Stankovic
IPC分类号： B01J19/00 , C07B61/00 , C07C275/28 , C07K1/04 , C07K5/062 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , B01J8/00 , C07K17/00 , C12M1/00
CPC分类号： C07K1/047 , B01J19/0046 , C07K1/045 , B01J2219/00283 , B01J2219/00308 , B01J2219/0031 , B01J2219/00373 , B01J2219/00416 , B01J2219/00423 , B01J2219/00454 , B01J2219/00493 , B01J2219/00495 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00689 , B01J2219/00695 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14
摘要： An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. The apparatus can be adapted to manual, semiautomatic or fully automatic performance. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.
摘要翻译：提供合适的位置用于多次同时合成化合物的装置和方法。该装置包括：具有多个井的储存器块; 多个反应管，通常为气体分散管，在其下端具有过滤器; 具有多个孔的保持器块; 以及可以具有允许引入/维护受控环境的端口的歧管。歧管顶壁具有孔和具有相同孔的可拆卸板。该装置由适应加热，冷却，搅拌或腐蚀性试剂的材料构成。垫片放在组件之间。提供杆或夹具用于将部件固定在一起。设备操作涉及将过滤器放置在储存器块井中的反应管的下端，并且通过保持器的上端阻挡孔并进入歧管。该装置提供超过1mg每种产品的结构知识和对每种化合物的控制。该装置可以适应于手动，半自动或全自动的性能。使用该装置，一系列构建块共价连接到固体支持物上。然后通过共价添加其他不同的构建块或化学修饰一些现有功能来修改这些构建块，直到实现倒数第二个结构。然后通过另一种化学反应将固体支持物从该固体支持物中裂解成孔内的溶液，得到新合成的单独化合物的阵列，其在反应后修饰（如果需要）适于测试活性。

5. 发明授权

US5714127A System for multiple simultaneous synthesis 失效
标题翻译：多个同步合成系统
公开(公告)号：US5714127A
公开(公告)日：1998-02-03
申请号：US475559
申请日：1995-06-07
申请人： Sheila H. H. DeWitt , John S. Kiely , Michael R. Pavia , Mel C. Schroeder , Charles J. Stankovic
发明人： Sheila H. H. DeWitt , John S. Kiely , Michael R. Pavia , Mel C. Schroeder , Charles J. Stankovic
IPC分类号： B01J19/00 , C07K1/04 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , B01J8/00 , C07K17/00 , C12M1/00
CPC分类号： C07K1/045 , B01J19/0046 , C07K1/047 , B01J2219/00283 , B01J2219/00308 , B01J2219/0031 , B01J2219/00373 , B01J2219/00416 , B01J2219/00423 , B01J2219/00454 , B01J2219/00493 , B01J2219/00495 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00689 , B01J2219/00695 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14
摘要： A system for the multiple, simultaneous synthesis of compounds preferably uses a reaction apparatus comprising a reservoir rack having a plurality of reaction wells, a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends, a holder block, having a plurality of apertures, and a manifold, which has ports to allow introduction/maintenance of a controlled environment. The manifold top wall has a plurality of apertures in axial alignment with the reaction tubes and a gasket which allows penetration by a needle in order to dispense and aspirate materials from the reaction tubes. Sealing members, such as gaskets, are placed between the holder block, manifold and reservoir rack and the components are releasably fastened together. A robotic sample processor is used to automate the synthesis process using the reaction apparatus.
摘要翻译：用于多次同时合成化合物的系统优选使用包括具有多个反应孔的储器架的反应装置，多个反应管，通常为气体分散管，在其下端具有过滤器，保持器块，具有多个孔和歧管，其具有允许引入/维持受控环境的端口。歧管顶壁具有与反应管轴向对准的多个孔，以及允许针穿透以便从反应管分配和吸出材料的垫圈。诸如垫圈的密封件被放置在保持器块，歧管和贮存器架之间，并且部件可释放地紧固在一起。使用机器人样品处理器来使用反应装置使合成过程自动化。

6. 发明授权

US5593642A Apparatus for multiple simultaneous synthesis 失效
标题翻译：多次同时合成的装置
公开(公告)号：US5593642A
公开(公告)日：1997-01-14
申请号：US461475
申请日：1995-06-05
申请人： Sheila H. H. DeWitt , John S. Kiely , Michael R. Pavia , Mel C. Schroeder , Charles J. Stankovic
发明人： Sheila H. H. DeWitt , John S. Kiely , Michael R. Pavia , Mel C. Schroeder , Charles J. Stankovic
IPC分类号： B01J19/00 , C07B61/00 , C07C275/28 , C07K1/04 , C07K5/062 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , B01J8/00 , C07K17/00 , C12M1/00
CPC分类号： C07K1/047 , B01J19/0046 , C07K1/045 , B01J2219/00283 , B01J2219/00308 , B01J2219/0031 , B01J2219/00373 , B01J2219/00416 , B01J2219/00423 , B01J2219/00454 , B01J2219/00493 , B01J2219/00495 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00689 , B01J2219/00695 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14
摘要： An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which my have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. The apparatus can be adapted to manual, semiautomatic or fully automatic performance. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.
摘要翻译：提供合适的位置用于多次同时合成化合物的装置和方法。该装置包括：具有多个井的储存器块; 多个反应管，通常为气体分散管，在其下端具有过滤器; 具有多个孔的保持器块; 和一个多方面，我有端口允许引入/维护受控环境。歧管顶壁具有孔和具有相同孔的可拆卸板。该装置由适应加热，冷却，搅拌或腐蚀性试剂的材料构成。垫片放在组件之间。提供杆或夹具用于将部件固定在一起。设备操作涉及将过滤器放置在储存器块井中的反应管的下端，并且通过保持器的上端阻挡孔并进入歧管。该装置提供超过1mg每种产品的结构知识和对每种化合物的控制。该装置可以适应于手动，半自动或全自动的性能。使用该装置，一系列构建块共价连接到固体支持物上。然后通过共价添加其他不同的构建块或化学修饰一些现有功能来修改这些构建块，直到实现倒数第二个结构。然后通过另一种化学反应将固体支持物从该固体支持物中裂解成孔内的溶液，得到新合成的单独化合物的阵列，其在反应后修饰（如果需要）适于测试活性。

7. 发明授权

US5563155A Individual stereosiomers of 7-[3-(aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones as antibacterial agents 失效
标题翻译： 7- [3-（氨基烷基）-1-吡咯烷基] - 喹诺酮和萘啶酮的单体立体异构体作为抗菌剂
公开(公告)号：US5563155A
公开(公告)日：1996-10-08
申请号：US434433
申请日：1995-05-03
申请人： John M. Domagala , John S. Kiely , Mel C. Schroeder
发明人： John M. Domagala , John S. Kiely , Mel C. Schroeder
IPC分类号： C07D207/09 , C07D207/26 , C07D401/04 , C07D471/04 , A61K31/47 , C07D215/56
CPC分类号： C07D207/26 , C07D207/09 , C07D401/04 , C07D471/04
摘要： Individual stereoisomers of 7-[3-(1-aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones are described, their therapeutic advantages as antibacterial agents, as well as a novel method for the preparation and isolation of such stereoisomers.
摘要翻译：描述了7- [3-（1-氨基烷基）-1-吡咯烷基] - 喹诺酮和萘啶酮的单个立体异构体，它们作为抗菌剂的治疗优点，以及制备和分离这些立体异构体的新方法。

8. 发明授权

US5344940A Intermediates for individual stereoisomers of 7-[3-(aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones 失效
标题翻译： 7- [3-（氨基烷基）-1-吡咯烷基] - 喹诺酮类和萘啶酮类单体立体异构体的中间体
公开(公告)号：US5344940A
公开(公告)日：1994-09-06
申请号：US84044
申请日：1993-06-28
申请人： John M. Domagala , John S. Kiely , Mel C. Schroeder
发明人： John M. Domagala , John S. Kiely , Mel C. Schroeder
IPC分类号： C07D207/09 , C07D207/26 , C07D401/04 , C07D471/04 , C07D207/12
CPC分类号： C07D207/26 , C07D207/09 , C07D401/04 , C07D471/04
摘要： Individual stereoisomers of 7-[3-(1-aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones are described, their therapeutic advantages as antibacterial agents, as well as a novel method for the preparation and isolation of such stereoisomers.
摘要翻译：描述了7- [3-（1-氨基烷基）-1-吡咯烷基] - 喹诺酮和萘啶酮的单个立体异构体，它们作为抗菌剂的治疗优点，以及制备和分离这些立体异构体的新方法。

9. 发明授权

US5258528A Individual stereoisomers of pyrrolidine methanamines substituted on the ring nitrogen by a 1-phenylethyl group 失效
标题翻译：通过1-苯基乙基在环氮上取代的吡咯烷甲胺的单个立体异构体
公开(公告)号：US5258528A
公开(公告)日：1993-11-02
申请号：US966651
申请日：1992-10-26
申请人： John M. Domagala , John S. Kiely , Mel C. Schroeder
发明人： John M. Domagala , John S. Kiely , Mel C. Schroeder
IPC分类号： C07D207/09 , C07D207/26 , C07D401/04 , C07D471/04
CPC分类号： C07D207/26 , C07D207/09 , C07D401/04 , C07D471/04
摘要： Individual stereoisomers of 7-[3-(1-aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones are described, their therapeutic advantages as antibacterial agents, as well as a novel method for the preparation and isolation of such stereoisomers.
摘要翻译：描述了7- [3-（1-氨基烷基）-1-吡咯烷基] - 喹诺酮和萘啶酮的单个立体异构体，它们作为抗菌剂的治疗优点，以及制备和分离这些立体异构体的新方法。

10. 发明授权

US5567391A Apparatus for multiple simultaneous synthesis 失效
公开(公告)号：US5567391A
公开(公告)日：1996-10-22
申请号：US464161
申请日：1995-06-05
申请人： Sheila H. H. DeWitt , John S. Kiely , Michael R. Pavia , Mel C. Schroeder , Charles J. Stankovic
发明人： Sheila H. H. DeWitt , John S. Kiely , Michael R. Pavia , Mel C. Schroeder , Charles J. Stankovic
IPC分类号： B01J19/00 , C07K1/04 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , B01J8/00 , C07K17/00 , C12M1/00
CPC分类号： C07K1/047 , B01J19/0046 , C07K1/045 , B01J2219/00283 , B01J2219/00308 , B01J2219/0031 , B01J2219/00373 , B01J2219/00416 , B01J2219/00423 , B01J2219/00454 , B01J2219/00493 , B01J2219/00495 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00689 , B01J2219/00695 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14
摘要： An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. The apparatus can be adapted to manual, semiautomatic or fully automatic performance. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.

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