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1. 发明授权

US5378694A Acyl and alkoxy substituted quinolines 失效
标题翻译：酰基和烷氧基取代的喹啉
公开(公告)号：US5378694A
公开(公告)日：1995-01-03
申请号：US983519
申请日：1993-03-01
申请人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles , Stuart B. Rosenblum
发明人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles , Stuart B. Rosenblum
IPC分类号： A61K31/11 , A61K31/12 , A61K31/13 , A61K31/16 , A61K31/18 , A61K31/185 , A61K31/22 , A61K31/235 , A61K31/365 , A61K31/38 , A61K31/382 , A61K31/47 , A61K31/695 , A61P9/12 , A61P31/12 , C07C49/755 , C07C49/757 , C07C225/22 , C07C235/82 , C07C309/59 , C07C311/16 , C07C323/42 , C07C323/62 , C07C323/66 , C07C323/67 , C07D215/22 , C07D215/56 , C07D311/16 , C07D311/18 , C07D335/06 , C07D401/06 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/04 , C07F7/18 , C07F9/12 , C07F9/38 , C07F9/40 , C07F9/60 , C07F9/655 , C07F9/6553
CPC分类号： C07D215/22 , C07D311/16 , C07D401/06 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/04 , C07F7/1856 , C07F9/60
摘要： Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are are represented by compounds of Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 and methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed.Also disclosed are compounds useful as antihypertensive agents and methods of treating hypertension using such compounds. The antihypertensive agents are compounds represented by Formula 1.0 wherein R.sup.4 is selected from the group consisting of alkyl and aminoalkyl. Preferably R.sup.1 is H.
摘要翻译： PCT No.PCT / US91 / 06250 Sec。 371日期1993年3月1日 102（e）1993年3月1日PCT PCT 1991年9月6日PCT公布。出版物WO92 / 04328 日期：1992年3月19日。公开了可用作抗病毒剂的化合物，用于含有DNA的病毒如疱疹病毒。化合物由式1.0化合物：其中药学上可接受的盐和溶剂合物表示。公开了含有由式1.0表示的化合物的药物组合物和使用由式1.0表示的化合物治疗病毒感染的方法。还公开了可用作抗高血压药的化合物和使用这些化合物治疗高血压的方法。抗高血压药是由式1.0表示的化合物，其中R 4选自烷基和氨基烷基。 R1优选为

2. 发明授权

US5179107A Antiviral quinolinone compounds 失效
标题翻译：抗病毒喹啉酮化合物
公开(公告)号：US5179107A
公开(公告)日：1993-01-12
申请号：US811890
申请日：1991-12-19
申请人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles
发明人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles
IPC分类号： C07D215/22 , C07D311/56 , C07D335/06 , C07D401/14 , C07D405/14 , C07D409/14
CPC分类号： C07D215/22 , C07D311/56 , C07D335/06 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Compounds useful as antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are selected from the group consisting of: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating a viral infection using compounds represented by Formula 1.0.A process for making compounds of Formula 1.0 from the appropriate 3-oximino-quinolin-2,4(1H)-dione (Formula 2.5) is also disclosed. The process comprises reductively hydrolyzing an appropriate 3-oximino-quinolin-2,4(1H)-dione (Formula 2.5) in a mixture with a hydrogenation catalyst and an acidic solvent mixture.
摘要翻译：公开了用作抗病毒药物的化合物，其可用于含有病毒的DNA，如疱疹病毒。化合物选自：式1.0（1.0）及其药学上可接受的盐和溶剂合物。公开了含有由式1.0表示的化合物的药物组合物。还公开了使用由式1.0表示的化合物治疗病毒感染的方法。还公开了从适当的3-肟基 - 喹啉-2,4（1H） - 二酮制备式1.0化合物的方法（式2.5）。该方法包括在与氢化催化剂和酸性溶剂混合物的混合物中还原性水解合适的3-肟基 - 喹啉-2,4（1H） - 二酮（式2.5）。

3. 发明授权

US5175151A Antiviral compounds and antihypertensive compounds 失效
标题翻译：抗病毒化合物和抗高血压化合物
公开(公告)号：US5175151A
公开(公告)日：1992-12-29
申请号：US830958
申请日：1992-02-05
申请人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles
发明人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles
IPC分类号： C07D215/22 , C07D215/56 , C07D311/18 , C07F7/18
CPC分类号： C07D215/22 , C07D215/56 , C07D311/18 , C07F7/1856
摘要： Compounds useful as antihypertensive agents, or antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension or a viral infection using compounds represented by Formulas 1.0.Also disclosed is a compound of Structure B ##STR2## useful as an intermediate in producing compounds of Formula 1.0. A process for preparing the compounds of Formula 1.0 is also disclosed. In the process a compound of Structure B ##STR3## is reacted with an alkoxide R.sub.1 O.sup.- M.sup.+ in a solvent comprising the corresponding alcohol R.sub.1 OH of the alkoxide. Optionally, an organic cosolvent may be used with the solvent.
摘要翻译：公开了可用作抗高血压剂的化合物或抗DNA病毒的抗病毒剂如疱疹病毒。化合物由式1.0表示：其中药学上可接受的盐和溶剂合物。公开了含有由式1.0表示的化合物的药物组合物。还公开了使用由式1.0表示的化合物治疗高血压或病毒感染的方法。还公开了可用作制备式1.0化合物的中间体的结构B B的化合物。还公开了制备式1.0化合物的方法。在该方法中，将结构B B的化合物与醇盐R 1 O-M +在包含醇盐的相应醇R 1 OH的溶剂中反应。任选地，有机共溶剂可以与溶剂一起使用。

4. 发明授权

US5412104A Ester and alkoxy substituted benzopyrans 失效
标题翻译：酯和烷氧基取代的苯并吡喃
公开(公告)号：US5412104A
公开(公告)日：1995-05-02
申请号：US30186
申请日：1993-03-01
申请人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles
发明人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles
IPC分类号： A61K31/37 , A61K31/38 , A61K31/382 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/47 , A61K31/66 , A61K31/665 , A61K31/67 , A61K31/675 , A61P9/12 , A61P31/12 , A61P31/22 , C07D215/22 , C07D233/60 , C07D277/04 , C07D311/06 , C07D311/16 , C07D335/06 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/04 , C07D409/12 , C07D417/04 , C07F7/18 , C07F9/60
CPC分类号： C07D215/22 , C07D311/16 , C07D401/06 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/04 , C07F7/1856 , C07F9/60
摘要： Compounds useful as antihypertensive agents and useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed.Also disclosed are methods of treating hypertension using compounds of Formula 1.0 wherein R is selected from the group consisting of H, halogen and --C(O)OR.sup.6 ; and R.sup.1 is selected from the group consisting of --OR.sup.14, --O(CH.sub.2).sub.a C(H).sub.3-i Z.sub.i and --O(CH.sub.2).sub.h N(R.sup.15).sub.2.
摘要翻译： PCT No.PCT / US91 / 06252 Sec。 371日期1993年3月1日 102（e）1993年3月1日PCT PCT 1991年9月6日PCT公布。出版物WO92 / 04327 日期：1992年3月19日。公开了可用作抗高血压剂并可用作抗病毒剂的化合物，其用于含有DNA的病毒如疱疹病毒。化合物由式1.0表示：其中药学上可接受的盐和溶剂合物。公开了含有由式1.0表示的化合物的药物组合物。公开了使用由式1.0表示的化合物治疗病毒感染的方法。还公开了使用式1.0化合物治疗高血压的方法，其中R选自H，卤素和-C（O）OR 6; 并且R 1选自-OR 14，-O（CH 2）a C（H）3 -iZi和-O（CH 2）h N（R 15）2。

5. 发明授权

US5382572A Alkyl and acyl substituted quinolines 失效
标题翻译：烷基和酰基取代的喹啉
公开(公告)号：US5382572A
公开(公告)日：1995-01-17
申请号：US30187
申请日：1993-03-01
申请人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles
发明人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles
IPC分类号： A61K31/12 , A61K31/13 , A61K31/165 , A61K31/18 , A61K31/185 , A61K31/19 , A61K31/22 , A61K31/37 , A61K31/38 , A61K31/382 , A61K31/47 , A61K31/665 , A61K31/67 , A61K31/675 , A61P31/12 , C07C49/755 , C07D215/22 , C07D311/56 , C07D335/06
CPC分类号： C07D215/22 , C07D311/56 , C07D335/06
摘要： Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates; wherein:(A) X is selected from the group consisting of N--R.sup.3, O, S, and C(R.sup.3).sub.2 ;(B) R.sup.3 is selected from H and a range of substituents;(C) R.sup.1 is an etherifying or esterifying group;(D) R.sup.2 is selected from a range of substituents;(E) m is 0 or an integer from 1 to 4; and(F) R.sup.4 and R.sup.5 are the same and are selected from alkyl and acyl groups;together with the pharmaceutically acceptable salts of the compounds of Formula 1.0 that are acidic or basic.Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating a viral infection using compounds represented by Formula 1.0.
摘要翻译： PCT No.PCT / US91 / 06251 Sec。 371日期1993年3月1日 102（e）1993年3月1日PCT PCT 1991年9月6日PCT公布。出版物WO92 / 04326 日期：1992年3月19日。公开了可用作抗病毒剂的化合物，用于含有DNA的病毒如疱疹病毒。化合物由式1.0表示：其药学上可接受的盐和溶剂合物; 其中：（A）X选自N-R3，O，S和C（R3）2; （B）R 3选自H和取代基的范围; （C）R1是醚化或酯化基团; （D）R2选自取代基的范围; （E）m为0或1〜4的整数; 和（F）R 4和R 5相同并且选自烷基和酰基; 以及式1.0化合物的药学上可接受的盐，它们是酸性或碱性的。公开了含有由式1.0表示的化合物的药物组合物。还公开了使用由式1.0表示的化合物治疗病毒感染的方法。

6. 发明授权

US5190956A Certain N-substituted 3-oximino-2,4-dioxoquinolin-2,4-(1H)diones useful for treating viral infections 失效
标题翻译：某些N-取代的3-肟基-2,4-二氧代喹啉-2,4-（1H）二酮可用于治疗病毒感染
公开(公告)号：US5190956A
公开(公告)日：1993-03-02
申请号：US579919
申请日：1990-09-07
申请人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles
发明人： Adriano Afonso , Jay Weinstein , Margaret J. Gentles
IPC分类号： C07D215/22 , C07D215/38 , C07D311/58 , C07D335/06 , C07D401/14 , C07D405/14
CPC分类号： C07D215/22 , C07D215/38 , C07D311/58 , C07D335/06 , C07D401/14 , C07D405/14
摘要： Compounds useful as antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are selected from the group consisting of: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.00 are disclosed. Also disclosed are methods of treating a viral infection using compounds represented by Formula 1.00The compounds of Formula 1.00 are also useful as intermediates to compounds of: ##STR2## Compounds of Formula 1.0 are useful as antiviral agents against the same viruses that the compounds of Formula 1.00 are useful against.
摘要翻译：公开了用作抗病毒药物的化合物，其可用于含有病毒的DNA，如疱疹病毒。化合物选自：式1.00及其药学上可接受的盐和溶剂化物。公开了含有式1.00表示的化合物的药物组合物。还公开了使用式1.00表示的化合物治疗病毒感染的方法。式1.00的化合物也可用作以下化合物的中间体：式1.0的化合物可用作抗化学药剂，其针对相同的病毒，化合物的1.00是有用的。

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