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11. 发明授权

US5869509A Diphenyl oxadiazolones as potassium channel modulators 失效
标题翻译：二苯基恶二唑酮作为钾通道调节剂
公开(公告)号：US5869509A
公开(公告)日：1999-02-09
申请号：US902684
申请日：1997-07-30
申请人： Jeffrey L. Romine , Scott W. Martin , Piyasena Hewawasam , Nicholas A. Meanwell , Valentin K. Gribkoff , John E. Starrett, Jr.
发明人： Jeffrey L. Romine , Scott W. Martin , Piyasena Hewawasam , Nicholas A. Meanwell , Valentin K. Gribkoff , John E. Starrett, Jr.
IPC分类号： C07D271/02 , A61K31/4164 , A61K31/4166 , A61K31/4196 , A61K31/4245 , A61P9/10 , A61P25/00 , A61P25/08 , A61P43/00 , C07D233/32 , C07D233/54 , C07D233/64 , C07D233/70 , C07D233/74 , C07D233/76 , C07D235/12 , C07D249/08 , C07D249/12 , C07D249/14 , C07D263/58 , C07D271/10 , C07D271/113 , C07D413/10 , A61K31/42 , A61K31/425 , C07D271/06
CPC分类号： C07D263/58 , C07D233/64 , C07D233/70 , C07D233/76 , C07D235/12 , C07D249/12 , C07D249/14 , C07D271/113 , C07D413/10
摘要： Novel compounds of Formula 1 are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels: ##STR1## wherein "Het" is one of a select group of heterocyclic moieties; Z is independently for each occurrence selected from O or S; R.sup.a, R.sup.b and R.sup.c each are independently selected from hydrogen, halogen, OH, CF.sub.3, ##STR2## provided R.sup.c is not hydrogen; and when R.sup.a and R.sup.b are hydrogen, R.sup.c may be a heterocyclic moiety selected from the group consisting of imidazol-1-yl, morpholinomethyl, N-methylimidazol- 2-yl, and pyridinyl; R.sup.d and R.sup.e each are independently selected from hydrogen, halogen, CF.sub.3, NO.sub.2 or imidazol-1-yl; m, n and p each are independently selected from an integer of O or 1; and R.sup.f and R.sup.g each are independently hydrogen; C.sub.1-4 alkyl; or R.sup.f and R.sup.g, taken together with the nitrogen atom to which they are attached, is a heterocyclic moiety selected from the group consisting of N-methylpiperazine, morpholine, thiomorpholine, N-benzylpiperazine and imidazolinone.
摘要翻译：式1的新型化合物可用于治疗对大电导钙激活钾通道的开放剂起反应的病症：其中“Het”是选择性杂环部分组之一; Z独立地选自O或S; Ra，Rb和Rc各自独立地选自氢，卤素，OH，CF 3，提供的R c不是氢; 当R a和R b为氢时，R c可以是选自咪唑-1-基，吗啉代甲基，N-甲基咪唑-2-基和吡啶基的杂环部分。 Rd和Re各自独立地选自氢，卤素，CF 3，NO 2或咪唑-1-基; m，n和p各自独立地选自O或1的整数; Rf和Rg各自独立地为氢; C 1-4烷基; 或R f和R g与它们所连接的氮原子一起是选自N-甲基哌嗪，吗啉，硫代吗啉，N-苄基哌嗪和咪唑啉酮的杂环部分。

12. 发明授权

US5158958A Imidazo[4,5-b]quinolinyl oxy alkyl sulfonyl piperidine derivatives 失效
标题翻译：咪唑并[4,5-b]喹啉基氧基烷基磺酰基哌啶衍生物
公开(公告)号：US5158958A
公开(公告)日：1992-10-27
申请号：US863278
申请日：1992-04-03
申请人： Piyasena Hewawasam , Nicholas A. Meanwell
发明人： Piyasena Hewawasam , Nicholas A. Meanwell
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A novel series of 1,3-dihydro-2H-imidazo [4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## wherein R.sup.1 is H, or C.sub.1 -C.sub.4 lower alkyl;R.sup.2 is H, or (CH.sub.2).sub.m R.sup.3 ;R.sup.3 is tetrahydro-2H-pyranyl, C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, or substituted or unsubstituted phenyl in which the substituents are halogen, alkoxy, or trifluoromethyl;m is an integer of 1-3; and n is an integer of 1-5; or pharmaceutically acceptable salt thereof.the compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.
摘要翻译：具有增强的水溶性生物利用度和代谢稳定性的新一系列1,3-二氢-2H-咪唑并[4,5-b]喹啉-2-酮公开在式I的化合物中，其中R 1是H或C1- C4低级烷基; R2是H或（CH2）mR3; R3是四氢-2H-吡喃基，C1-C8烷基，C4-C8环烷基或取代或未取代的苯基，其中取代基是卤素，烷氧基或三氟甲基; m为1-3的整数; n为1-5的整数; 或其药学上可接受的盐。该化合物可用作人富血小板血浆中ADP诱导的血小板聚集抑制剂。

13. 发明授权

US07485633B2 Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors 有权
标题翻译：环丙基稠合吲哚并苯并氮平HCV NS5B抑制剂
公开(公告)号：US07485633B2
公开(公告)日：2009-02-03
申请号：US11684710
申请日：2007-03-12
申请人： Nicholas A. Meanwell , Robert G. Gentles , Min Ding , John A. Bender , John F. Kadow , Piyasena Hewawasam , Thomas W. Hudyma , Xiaofan Zheng
发明人： Nicholas A. Meanwell , Robert G. Gentles , Min Ding , John A. Bender , John F. Kadow , Piyasena Hewawasam , Thomas W. Hudyma , Xiaofan Zheng
IPC分类号： A61K31/55 , A61P31/00 , C07D223/14
CPC分类号： C07D487/04
摘要： The invention encompasses compounds of Formula I, pharmaceutically acceptable salts thereof, compositions, and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
摘要翻译：本发明包括式I的化合物，其药学上可接受的盐，组合物和使用该化合物的方法。该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

14. 发明授权

US5348960A Imidazo[4,5-b]quinolinyl oxy alkyl tetrazolyl piperidine derivatives 失效
标题翻译：咪唑并[4,5-b]喹啉基氧基烷基四唑基哌啶衍生物
公开(公告)号：US5348960A
公开(公告)日：1994-09-20
申请号：US114262
申请日：1993-08-30
申请人： Piyasena Hewawasam , Nicholas A. Meanwell
发明人： Piyasena Hewawasam , Nicholas A. Meanwell
IPC分类号： C07D471/04 , A61K31/445
CPC分类号： C07D471/04
摘要： A series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## wherein R.sup.1 is H, or C.sub.1 -C.sub.4 lower alkyl;R.sup.2 is H, or (CH.sub.2).sub.m R.sup.3 ;R.sup.3 is tetrahydro-2H-pyranyl, C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, or substituted or unsubstituted phenyl, wherein the substituents are halogen, alkoxy, or trifluoromethyl;m is an integer of 1-3; andn is an integer of 1-5;or pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.
摘要翻译：具有增强的水溶性生物利用度和代谢稳定性的一系列1,3-二氢-2H-咪唑并[4,5-b]喹啉-2-酮公开在式I的图像中，其中R1是H或C1-C4 低级烷基 R2是H或（CH2）mR3; R3是四氢-2H-吡喃基，C1-C8烷基，C4-C8环烷基或取代或未取代的苯基，其中取代基是卤素，烷氧基或三氟甲基; m为1-3的整数; n为1-5的整数; 或其药学上可接受的盐。该化合物可用作富含人血小板的血浆中ADP诱导的血小板聚集的抑制剂。

15. 发明授权

US5208237A 7-oxypropylsulfonamido-imidazo[4,5-b]quinolin-2-ones 失效
标题翻译： 7-氧代丙基磺酰氨基 - 咪唑并[4,5-b]喹啉-2-酮
公开(公告)号：US5208237A
公开(公告)日：1993-05-04
申请号：US862879
申请日：1992-04-03
申请人： Piyasena Hewawasam , Nicholas A. Meanwell
发明人： Piyasena Hewawasam , Nicholas A. Meanwell
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A novel series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## wherein R.sup.1 is H, or C.sub.1 -C.sub.4 lower alkyl;R.sup.2 is H, (CH.sub.2).sub.m R.sup.3 ; benzoxazol-2yl, or benzothiazol2-yl;R.sup.3 is C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, or substituted or unsubstituted phenyl, wherein the substituents are halogen, alkoxy or trifluoromethyl;m is an integer of 1-3; andn is an integer of 1-5;or pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.
摘要翻译：具有增强的水溶性生物利用度和代谢稳定性的新一系列1,3-二氢-2H-咪唑并[4,5-b]喹啉-2-酮公开在式I的化合物中，其中R 1是H或C1- C4低级烷基; R2是H，（CH2）mR3; 苯并恶唑-2-基或苯并噻唑-2-基; R3是C1-C8烷基，C4-C8环烷基或取代或未取代的苯基，其中取代基是卤素，烷氧基或三氟甲基; m为1-3的整数; n为1-5的整数; 或其药学上可接受的盐。该化合物可用作富含人血小板的血浆中ADP诱导的血小板聚集的抑制剂。

16. 发明申请

US20120232099A1 Compounds for the Treatment of Hepatitis C 有权
标题翻译：用于治疗丙型肝炎的化合物
公开(公告)号：US20120232099A1
公开(公告)日：2012-09-13
申请号：US13470727
申请日：2012-05-14
申请人： Richard Pracitto , John F. Kadow , John A. Bender , Brett R. Beno , Katherine A. Grant-Young , Ying Han , Piyasena Hewawasam , Andrew Nickel , Kyle E. Parcella , Kap-Sun Yeung , Louis S. Chupak
发明人： Richard Pracitto , John F. Kadow , John A. Bender , Brett R. Beno , Katherine A. Grant-Young , Ying Han , Piyasena Hewawasam , Andrew Nickel , Kyle E. Parcella , Kap-Sun Yeung , Louis S. Chupak
IPC分类号： A61K31/4355 , A61K31/506 , A61P31/04 , C07D491/048
CPC分类号： C07D471/04 , C07D209/42 , C07D333/68 , C07D491/048
摘要： The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
摘要翻译：本公开提供式I，II，III，IV和V的化合物，包括它们的盐，以及使用该化合物的组合物和方法。该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

17. 发明授权

US08048887B2 Compounds for the treatment of hepatitis C 有权
公开(公告)号：US08048887B2
公开(公告)日：2011-11-01
申请号：US12554193
申请日：2009-09-04
申请人： Kap-Sun Yeung , Kyle E. Parcella , John A. Bender , Brett R. Beno , Katharine A. Grant-Young , Ying Han , Piyasena Hewawasam , John F. Kadow , Andrew Nickel
发明人： Kap-Sun Yeung , Kyle E. Parcella , John A. Bender , Brett R. Beno , Katharine A. Grant-Young , Ying Han , Piyasena Hewawasam , John F. Kadow , Andrew Nickel
IPC分类号： A61K31/506 , C07D405/02
CPC分类号： C07D307/84 , C07D405/04 , C07D405/10 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12 , C07D453/00 , C07D491/10
摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

18. 发明申请

US20110256099A1 Compounds for the Treatment of Hepatitis C 有权
标题翻译：用于治疗丙型肝炎的化合物
公开(公告)号：US20110256099A1
公开(公告)日：2011-10-20
申请号：US13166926
申请日：2011-06-23
申请人： Kap-Sun Yeung , Kyle E. Parcella , John A. Bender , Brett R. Beno , Katharine A. Grant-Young , Ying Han , Piyasena Hewawasam , John F. Kadow , Andrew Nickel
发明人： Kap-Sun Yeung , Kyle E. Parcella , John A. Bender , Brett R. Beno , Katharine A. Grant-Young , Ying Han , Piyasena Hewawasam , John F. Kadow , Andrew Nickel
IPC分类号： A61K38/21 , A61P31/14
CPC分类号： A61K31/506 , A61K45/06 , C07D307/84 , C07D405/04 , C07D405/10 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12 , C07D453/00 , C07D491/10
摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
摘要翻译：本公开提供式I化合物，包括其盐，以及使用该化合物的组合物和方法。该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

19. 发明申请

US20090162318A1 Cyclopropyl Fused Indolobenzazepine HCV NS5B Inhibitors 审中-公开
标题翻译：环丙基稠合吲哚扎嗪氮芥HCV NS5B抑制剂
公开(公告)号：US20090162318A1
公开(公告)日：2009-06-25
申请号：US12392620
申请日：2009-02-25
申请人： John A. Bender , Min Ding , Robert G. Gentles , Piyasena Hewawasam
发明人： John A. Bender , Min Ding , Robert G. Gentles , Piyasena Hewawasam
IPC分类号： A61K38/20 , A61K31/55 , A61K31/397 , A61P31/12 , A61K38/21
CPC分类号： C07D487/08 , A61K31/55 , A61K45/06 , C07D471/08 , C07D487/04 , C07D519/00
摘要： The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
摘要翻译：本发明包括式I化合物以及使用该化合物的组合物和方法。该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

20. 发明授权

US07547690B2 Compounds for the treatment of Hepatitis C 有权
标题翻译：用于治疗丙型肝炎的化合物
公开(公告)号：US07547690B2
公开(公告)日：2009-06-16
申请号：US12039239
申请日：2008-02-28
申请人： Robert G. Gentles , Xiaofan Zheng , Min Ding , Yong Tu , Ying Han , Piyasena Hewawasam , John F. Kadow , John A. Bender , Kap-Sun Yeung , Katharine A. Grant-Young , Thomas W. Hudyma
发明人： Robert G. Gentles , Xiaofan Zheng , Min Ding , Yong Tu , Ying Han , Piyasena Hewawasam , John F. Kadow , John A. Bender , Kap-Sun Yeung , Katharine A. Grant-Young , Thomas W. Hudyma
IPC分类号： A61P31/00 , A61K31/55 , C07D223/14
CPC分类号： C07D519/00 , C07D487/04
摘要： The invention encompasses compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
摘要翻译：本发明包括式I化合物，包括药学上可接受的盐，以及使用这些化合物的组合物和方法。该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

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