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42. 发明授权

US5958929A 6-aryl pyrazolo �3,4-d! pyrimidin-4-ones and compositions and methods of use thereof 失效
标题翻译： 6-芳基吡唑并[3,4-d]嘧啶-4-酮及其组合物及其使用方法
公开(公告)号：US5958929A
公开(公告)日：1999-09-28
申请号：US16572
申请日：1998-01-30
申请人： Edward R. Bacon , Baldev Singh
发明人： Edward R. Bacon , Baldev Singh
IPC分类号： A61K31/505 , A61P9/00 , A61P9/12 , C07D487/04
CPC分类号： C07D487/04
摘要： 6-Aryl pyrazolo�3,4-d!pyrimidin-4-one derivatives, pharmaceutical compositions containing them and methods for effecting c-GMP-phosphodiesterase inhibition and for treating heart failure and/or hypertension.
摘要翻译： 6-芳基吡唑并[3,4-d]嘧啶-4-酮衍生物，含有它们的药物组合物和用于实现c-GMP-磷酸二酯酶抑制和治疗心力衰竭和/或高血压的方法。

43. 发明授权

US5736548A 6-aryl pyrazolo�3,4-D! pyrimidin-4-ones and compositions and method of use thereof 失效
标题翻译： 6-芳基吡唑并[3,4-D]嘧啶-4-酮及其组合物及其使用方法
公开(公告)号：US5736548A
公开(公告)日：1998-04-07
申请号：US788893
申请日：1997-01-22
申请人： Edward R. Bacon , Baldev Singh
发明人： Edward R. Bacon , Baldev Singh
IPC分类号： A61K31/505 , A61P9/00 , A61P9/12 , C07D487/04 , C07D498/04
CPC分类号： C07D487/04
摘要： 6-Aryl pyrazolo�3,4-d!pyrimidin-4-one derivatives, pharmaceutical compositions containing them and methods for effecting c-GMP-phosphodiesterase inhibition and for treating heart failure and/or hypertension.
摘要翻译： 6-芳基吡唑并[3,4-d]嘧啶-4-酮衍生物，含有它们的药物组合物和用于实现c-GMP-磷酸二酯酶抑制和治疗心力衰竭和/或高血压的方法。

44. 发明授权

US5541187A 6-heterocycyclyl pyrazolo[3,4-d]pyrimidin-4-ones and compositions and method of use thereof 失效
标题翻译： 6-杂环基吡唑并[3,4-d]嘧啶-4-酮及其组合物及其使用方法
公开(公告)号：US5541187A
公开(公告)日：1996-07-30
申请号：US159158
申请日：1993-11-30
申请人： Edward R. Bacon , Baldev Singh , George Y. Lesher, deceased
发明人： Edward R. Bacon , Baldev Singh , George Y. Lesher, deceased
IPC分类号： C07D487/04 , C07D519/00 , A61K31/505 , A61K31/535 , C07D213/44 , C07D413/00
CPC分类号： C07D487/04
摘要： Novel 6-heterocyclyl-pyrazolo[3,4-d]pyrimidin-4-ones, useful in treating cardiovascular disease, are prepared by reacting a 5-amino-1H-pyrazole-4-carboxamide with heterocyclyl-carboxaldehyde or by reacting a 5-amino-1H-pyrazole-4-carbonitrile with a heterocyclylcarboxamidine, followed by diazotization and hydrolysis of the resulting 4-amino-6-heterocyclyl-pyrazolo[3,4-d]pyrimidine.
摘要翻译：可用于治疗心血管疾病的新型6-杂环基 - 吡唑并[3,4-d]嘧啶-4-酮通过使5-氨基-1H-吡唑-4-甲酰胺与杂环基甲醛反应或通过使5 - 氨基-1H-吡唑-4-腈与杂环基甲脒反应，然后重氮化并水解所得的4-氨基-6-杂环基 - 吡唑并[3,4-d]嘧啶。

45. 发明授权

US5492687A Compositions of iodophenoxy alkylene ethers and pharmaceutically acceptable clays for visualization of the gastrointestinal tract 失效
标题翻译：碘苯氧基亚烷基醚的组合物和用于胃肠道可视化的药学上可接受的粘土
公开(公告)号：US5492687A
公开(公告)日：1996-02-20
申请号：US237502
申请日：1994-05-03
申请人： Stephen B. Ruddy , Gregory L. McIntire , Mary E. Roberts , Edward R. Bacon
发明人： Stephen B. Ruddy , Gregory L. McIntire , Mary E. Roberts , Edward R. Bacon
IPC分类号： A61K49/04 , C07C43/225
CPC分类号： A61K49/0404 , A61K49/04 , A61K49/0409 , A61K49/0461 , C07C43/225
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodophenoxy alkylene ethers and pharmaceutically acceptable clays in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
摘要翻译：公开了用于口服或逆行检查胃肠道的x射线造影剂组合物，其包含药学上可接受的载体中的碘苯氧基亚烷基醚和药学上可接受的粘土; 以及它们用于胃肠道诊断放射学的方法。

46. 发明授权

US5488133A Iodinated aroyloxy ketones 失效
标题翻译：碘化芳酰基酮
公开(公告)号：US5488133A
公开(公告)日：1996-01-30
申请号：US209181
申请日：1994-03-10
申请人： Baldev Singh , Edward R. Bacon , Shaughnessy Robinson
发明人： Baldev Singh , Edward R. Bacon , Shaughnessy Robinson
IPC分类号： A61K49/04 , C07C233/54 , C07C237/46 , C07D307/33 , C07C229/56
CPC分类号： C07D307/33 , A61K49/0433 , C07C233/54 , C07C2103/74
摘要： Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid; n is an integer from 0 to 20;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy, acylamino, acetamidoalkyl, acetamidoaryl, --COO-alkyl, --COO-aryl, --COO-aralkyl, --CO-alkyl, --CO-aryl, --CO-heterocyclyl, cyano or heterocyclyl;R.sup.5 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, heterocyclyl, or a Z-CO.sub.2 -CR.sup.1 R.sup.2 (CR.sup.3 R.sup.4).sub.n group, wherein Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n are as defined above, m is an integer from 0 to 10, p is an integer from 0 to 10, and m+p.gtoreq.1 are useful as contrast agents in x-ray imaging compositions and methods.
摘要翻译：具有结构式（Ia）或（Ib）的化合物（Ib）其中（Z-COO是碘化芳族酸的残基; n是0至20的整数; R1，R2，R3和R4独立地为H 烷基，氟代烷基，环烷基，芳基，芳烷基，烷氧基，芳氧基，卤素，羟基，酰氨基，乙酰氨基烷基，乙酰氨基芳基，-COO-烷基，-COO-芳基，-COO-芳烷基， -CO-杂环基，氰基或杂环基; R5是H，烷基，氟烷基，环烷基，芳基，芳烷基，烷氧基烷基，杂环基或Z-CO2-CR1R2（CR3R4）n基团，其中Z，R1，R2，R3，R4 和n如上所定义，m是0至10的整数，p是0至10的整数，并且m + p> / = 1可用作x射线成像组合物和方法中的造影剂。

47. 发明授权

US5385721A Compositions of alkylbenzenes and cellulose derivatives for visualization of the gastrointestinal tract 失效
标题翻译：用于胃肠道可视化的烷基苯和纤维素衍生物的组合物
公开(公告)号：US5385721A
公开(公告)日：1995-01-31
申请号：US217138
申请日：1994-03-22
申请人： Edward J. Baker , Kurt A. Josef , Edward R. Bacon , Kimberly G. Estep , Carl R. Illig , Brent D. Douty , John L. Toner , Robert W. Lee
发明人： Edward J. Baker , Kurt A. Josef , Edward R. Bacon , Kimberly G. Estep , Carl R. Illig , Brent D. Douty , John L. Toner , Robert W. Lee
IPC分类号： A61K49/00 , A61K49/04 , C07C17/00 , C07C17/12 , C07C17/26 , C07C25/02 , C07C25/13 , C07C25/24 , C07C33/46 , C07C43/225 , C07C69/65 , C07C69/76 , C07C69/92 , A61K31/715 , A61K31/02
CPC分类号： C07C17/354 , A61K49/04 , A61K49/0404 , A61K49/0409 , A61K49/0433 , C07C17/12 , C07C17/2635 , C07C25/02 , C07C25/24 , C07C69/65
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof ##STR1## wherein R is methyl, ethyl, n-propyl, C.sub.4 -C.sub.25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl; (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H, lower-alkyl, optionally substituted with halo;n is 2-5;m is 2-5;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;in a pharmaceutically acceptable carrier comprising a cellulose derivative.
摘要翻译：公开了用于口服或逆行检查胃肠道的x射线造影剂组合物，其包含下式的x射线产生剂或其药学上可接受的盐，其中R是甲基，乙基，正丙基，C 4 -C 25烷基，环烷基，不饱和烯丙基或卤代低级烷基，其各自可以任选被卤素，氟代低级烷基，芳基，低级烷氧基，羟基，羧基或低级烷氧基羰基取代; （CR 1 R 2）p - （CR 3 = CR 4）m Q或（CR 1 R 2）p -C 3OND C-Q; R 1，R 2，R 3和R 4独立地为H，低级烷基，任选被卤素取代; n为2-5; m为2-5; p为1-10; Q为H，低级烷基，低级烯基，低级炔基，低级亚烷基，芳基或芳基 - 低级烷基; 在包含纤维素衍生物的可药用载体中。

48. 发明授权

US5348727A Compositions of iodophenoxy alkylene ethers for visualization of the gastrointestinal tract 失效
标题翻译：用于可视化胃肠道的碘苯氧基亚烷基醚的组合物
公开(公告)号：US5348727A
公开(公告)日：1994-09-20
申请号：US29485
申请日：1993-03-11
申请人： Edward R. Bacon , Carl R. Illig , Thomas J. Caulfield , Brent D. Douty , Kurt A. Josef
发明人： Edward R. Bacon , Carl R. Illig , Thomas J. Caulfield , Brent D. Douty , Kurt A. Josef
IPC分类号： A61K49/04 , C07C43/225 , C07C43/23 , C07C69/92 , C07C255/54 , A61B5/055 , A61K31/075 , C07C41/00
CPC分类号： A61K49/0404 , A61K49/04 , A61K49/0409 , A61K49/0461 , C07C43/225
摘要： A compound of the formula: ##STR1## wherein Z.dbd.H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, wherein thealkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.dbd.C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p -(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C-Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H, or lower-alkyl, optionally substituted with halo;x is 1-4;n is [1-5]1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, these compounds are useful as X-ray contrast agents or aryl-lower alkyl.
摘要翻译：其中Z = H，卤素，C 1 -C 20烷基，环烷基，低级烷氧基，烷氧基羰基，氰基，其中烷基和环烷基可以被卤素或卤代低级烷基取代; R = C 1 -C 25烷基，环烷基，或低级烷基; 羟基，羧基，低级烷氧基羰基或低级烷氧基 - 羰基氧基（CR 1 R 2）p - （CR 3 = CR 4）m Q或任选被卤素，氟 - 低级 - 烷基，芳基，（CR1R2）pC 3BOND CQ; R 1，R 2，R 3和R 4独立地为H或被卤素取代的低级烷基; x为1-4; n是[1-5] 1-4; m为1-15; p是1-20; Q为H，低级烷基，低级烯基，低级炔基，低级亚烷基，芳基，这些化合物可用作X射线造影剂或芳基 - 低级烷基。

49. 发明授权

US5328404A Method of x-ray imaging using iodinated aromatic propanedioates 失效
标题翻译：使用碘化芳族丙二酸盐的X射线成像方法
公开(公告)号：US5328404A
公开(公告)日：1994-07-12
申请号：US148112
申请日：1993-11-04
申请人： Edward R. Bacon
发明人： Edward R. Bacon
IPC分类号： C07C63/307 , A61K49/04 , C07C69/76 , C07C69/82 , C07C69/83 , C07C233/54 , C07C237/46 , C07C255/20 , C07C309/70 , C07C311/24 , C07C229/40
CPC分类号： C07C69/76 , A61K49/0433 , C07C233/54 , C07C237/46
摘要： Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid;R.sup.1 and R.sup.2 are independently alkyl, fluoroalkyl, cycloalkyl, aryl or aralkyl; andR.sup.3 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, cyano, sulfonate, carboxamido, sulfonamido, CO.sub.2 -alkyl, CO.sub.2 -aryl or CO.sub.2 -aralkyl;are useful as contrast agents in x-ray imaging compositions and methods.
摘要翻译：具有结构的化合物，其中（Z-COO是碘化芳族酸的残基; R1和R2独立地是烷基，氟烷基，环烷基，芳基或芳烷基; R3是H，烷基，氟代烷基，环烷基，芳基，芳烷基，烷氧基，芳氧基，氰基，磺酸酯，甲酰氨基，亚磺酰氨基，CO 2烷基，CO 2 - 芳基或CO 2 - 芳烷基;可用作x射线成像组合物和方法中的造影剂。

50. 发明授权

US5324737A 3-arylcarbonyl-1-(C-attached-N-heteryl)-1H-indoles 失效
标题翻译： 3-芳基羰基-1-（C-连接的N-异基）-1H-吲哚
公开(公告)号：US5324737A
公开(公告)日：1994-06-28
申请号：US807032
申请日：1991-09-26
申请人： Thomas E. D'Ambra , Edward R. Bacon , Malcolm R. Bell , Philip M. Carabateas , Michael A. Eissenstat , Virendra Kumar , John P. Mallamo , Susan J. Ward
发明人： Thomas E. D'Ambra , Edward R. Bacon , Malcolm R. Bell , Philip M. Carabateas , Michael A. Eissenstat , Virendra Kumar , John P. Mallamo , Susan J. Ward
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/545 , A61K31/55 , A61P25/04 , A61P29/00 , C07D209/12 , C07D401/02 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06 , C07D40/06
CPC分类号： C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
摘要： 2-R.sub.2 -R.sub.4 -substitutea-3-R.sub.3 -CO-1-[(C-attached-N-heteryl)(Alk).sub.n ]-1H-indoles useful as analgesic, anti-rheumatic, anti-inflammatory or anti-glaucoma agents.
摘要翻译：可用作镇痛，抗风湿，消炎或抗青光眼的2-R2-R4-替代-3-R3-CO-1 - [（C-连接的N-异基）（Alk）n] 代理商

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