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公开(公告)号：US06380400B1
公开(公告)日：2002-04-30
申请号：US09674381
申请日：2000-10-31
申请人： Victor Fedij , Christopher Andrew Gajda , Brian Keith Huckabee , Brian Stuart Moon , Kenneth Thomas Porter , Denis Martin Sobieray , Timothy Lee Stuk , Bradley Dean Tait , James Norton Wemple
发明人： Victor Fedij , Christopher Andrew Gajda , Brian Keith Huckabee , Brian Stuart Moon , Kenneth Thomas Porter , Denis Martin Sobieray , Timothy Lee Stuk , Bradley Dean Tait , James Norton Wemple
IPC分类号： C07D30932
CPC分类号： C07D309/32 , C07C45/00 , C07C45/513 , C07C45/62 , C07C45/74 , C07C205/45 , C07C205/56 , C07C229/42 , C07C233/33 , C07C233/54 , C07C319/14 , C07C331/12 , C07C333/04 , C07C333/20 , C07C381/04 , C07C47/565 , C07C49/255 , C07C323/29
摘要： The present invention relates to methods of making dihydropyrone HIV inhibitors.
摘要翻译： 本发明涉及制备二氢吡喃酮HIV抑制剂的方法
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公开(公告)号：US06927217B2
公开(公告)日：2005-08-09
申请号：US10271467
申请日：2002-10-16
申请人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Elizabeth Ann Lunney , Alexander Pavlovsky , Vara Prasad Venkata Nagendra Josyula , Bradley Dean Tait
发明人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Elizabeth Ann Lunney , Alexander Pavlovsky , Vara Prasad Venkata Nagendra Josyula , Bradley Dean Tait
IPC分类号： A61P31/12 , A61P31/18 , C07D309/32 , C07D401/06 , A61K31/351 , C07D401/04 , C07D403/04
CPC分类号： C07D309/32
摘要： The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.
摘要翻译： 本发明涉及式I的新型二氢呋喃，其中X是NH或NR 8，其抑制HIV天冬氨酰蛋白酶阻断HIV感染性。 二氢吡喃可用于开发用于治疗病毒感染和疾病（包括AIDS）的治疗。
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公开(公告)号：US06852711B2
公开(公告)日：2005-02-08
申请号：US10299510
申请日：2002-11-19
申请人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Susan Elizabeth Hagen , Michael James Lovdahl , Elizabeth Ann Lunney , Larry James Markoski , Josyula Venkata Nagendra Vara Prasad , Bradley Dean Tait
发明人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Susan Elizabeth Hagen , Michael James Lovdahl , Elizabeth Ann Lunney , Larry James Markoski , Josyula Venkata Nagendra Vara Prasad , Bradley Dean Tait
IPC分类号： C07D233/64 , A61K31/351 , A61K31/381 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61P31/14 , A61P31/18 , C07D207/333 , C07D209/12 , C07D209/30 , C07D213/30 , C07D213/71 , C07D231/12 , C07D235/06 , C07D235/26 , C07D239/26 , C07D239/42 , C07D241/44 , C07D277/20 , C07D277/24 , C07D277/46 , C07D277/82 , C07D307/12 , C07D307/42 , C07D309/32 , C07D333/16 , C07D333/32 , C07D333/62 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/06 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/12 , C07D417/14 , A61K31/33 , A61K31/35 , C07D277/00 , C07D309/00 , C07D315/00
CPC分类号： C07D405/06 , C07D309/32 , C07D405/12 , C07D405/14 , C07D407/06 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
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公开(公告)号：US06512006B1
公开(公告)日：2003-01-28
申请号：US09641260
申请日：2000-08-17
申请人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Elizabeth Ann Lunney , Alexander Pavlovsky , Vara Prasad Venkata Nagendra Josyula , Bradley Dean Tait
发明人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Elizabeth Ann Lunney , Alexander Pavlovsky , Vara Prasad Venkata Nagendra Josyula , Bradley Dean Tait
IPC分类号： C07D30930
CPC分类号： C07D309/32
摘要： The present invention related to novel dihydropyrones possessing 3-position nitrogen atom, which inhabit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections, and diseases, including AIDS.
摘要翻译： 本发明涉及具有3-位氮原子的新型二氢吡喃酮，其存在HIV天冬氨酰蛋白酶阻断HIV感染性。 二氢吡喃酮可用于开发用于治疗病毒感染和包括艾滋病在内的疾病的治疗。
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公开(公告)号：US5834506A
公开(公告)日：1998-11-10
申请号：US883743
申请日：1997-06-27
申请人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Susan Elizabeth Hagen , Harriet Wall Hamilton , Elizabeth Ann Lunney , Larry James Markoski , Josyula Venkata Nagendra Vara Prasad , Bradley Dean Tait
发明人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Susan Elizabeth Hagen , Harriet Wall Hamilton , Elizabeth Ann Lunney , Larry James Markoski , Josyula Venkata Nagendra Vara Prasad , Bradley Dean Tait
IPC分类号： C07D295/22 , A61K31/366 , A61K31/381 , A61K31/4178 , A61K31/4433 , A61K31/453 , A61K31/496 , A61K31/5355 , A61P31/18 , C07C39/26 , C07C43/225 , C07C49/255 , C07C59/48 , C07C59/52 , C07C59/68 , C07C69/734 , C07C69/738 , C07C233/33 , C07C381/04 , C07D233/84 , C07D233/86 , C07D241/04 , C07D295/205 , C07D309/32 , C07D405/04 , C07D405/12 , C07D409/12 , C07F7/08 , C07F7/18 , A61K31/35 , A61K31/415
CPC分类号： C07D295/205 , C07C233/33 , C07C381/04 , C07C59/48 , C07C59/52 , C07C59/68 , C07C69/738 , C07F7/1852 , C07F7/1856
摘要： This invention pertains to improved antiviral activity of 6,6-disubstituted-5,6-dihydropyran-2-ones caused by judicious placement of certain polar substituents at the 3 and/or 6 positions. The same substituents which enhance the cellular activity also diminish cytotoxicity further enhancing the desirable properties of these agents as antivirals.
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公开(公告)号：US06528510B1
公开(公告)日：2003-03-04
申请号：US09674652
申请日：2000-11-02
申请人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Susan Elizabeth Hagen , Michael James Lovdahl , Elizabeth Ann Lunney , Larry James Markoski , Josyula Venkata Nagendra Vara Prasad , Bradley Dean Tait
发明人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Susan Elizabeth Hagen , Michael James Lovdahl , Elizabeth Ann Lunney , Larry James Markoski , Josyula Venkata Nagendra Vara Prasad , Bradley Dean Tait
IPC分类号： A61K31495
CPC分类号： C07D405/06 , C07D309/32 , C07D405/12 , C07D405/14 , C07D407/06 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
摘要翻译： 本发明涉及具有改善的药理学性质的具有栓系杂环的新型二氢吡喃酮，其有效抑制HIV天冬氨酰蛋白酶阻断HIV感染性。 二氢吡喃可用于开发用于治疗病毒感染和疾病（包括AIDS）的治疗。 本发明还涉及合成二氢吡喃的方法和可用于制备最终化合物的中间体。
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公开(公告)号：US6046355A
公开(公告)日：2000-04-04
申请号：US124190
申请日：1998-07-28
申请人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Susan Elizabeth Hagen , Harriet Wall Hamilton , Elizabeth Ann Lunney , Larry James Markoski , Josyula Venkata Nagendra Vara Prasad , Bradley Dean Tait
发明人： Frederick Earl Boyer, Jr. , John Michael Domagala , Edmund Lee Ellsworth , Christopher Andrew Gajda , Susan Elizabeth Hagen , Harriet Wall Hamilton , Elizabeth Ann Lunney , Larry James Markoski , Josyula Venkata Nagendra Vara Prasad , Bradley Dean Tait
IPC分类号： C07D295/22 , A61K31/366 , A61K31/381 , A61K31/4178 , A61K31/4433 , A61K31/453 , A61K31/496 , A61K31/5355 , A61P31/18 , C07C39/26 , C07C43/225 , C07C49/255 , C07C59/48 , C07C59/52 , C07C59/68 , C07C69/734 , C07C69/738 , C07C233/33 , C07C381/04 , C07D233/84 , C07D233/86 , C07D241/04 , C07D295/205 , C07D309/32 , C07D405/04 , C07D405/12 , C07D409/12 , C07F7/08 , C07F7/18 , C07D309/31
CPC分类号： C07D295/205 , C07C233/33 , C07C381/04 , C07C59/48 , C07C59/52 , C07C59/68 , C07C69/738 , C07F7/1852 , C07F7/1856
摘要： This invention pertains to improved antiviral activity of 6,6-disubstituted-5,6-dihydropyran-2-ones caused by judicious placement of certain polar substituents at the 3 and/or 6 positions.The same substituents which enhance the cellular activity also diminish cytotoxicity further enhancing the desirable properties of these agents as antivirals.
摘要翻译： 本发明涉及通过在3和/或6位明智地放置某些极性取代基引起的6,6-二取代-5,6-二氢吡喃-2-酮的改进的抗病毒活性。 增强细胞活性的相同取代基也降低了细胞毒性，从而进一步提高了这些药物作为抗病毒剂的期望性质。
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公开(公告)号：US5972980A
公开(公告)日：1999-10-26
申请号：US295742
申请日：1999-04-20
IPC分类号： A61K31/4184 , A61K31/425 , A61K31/44
CPC分类号： A61K31/4184
摘要： Inhibitors of 15-lipoxygenase (15-LO) are useful to treat and prevent inflammation or atherosclerosis. Preferred inhibitors have a ratio of 5-LO to 15-LO inhibitory activity of at least about 10 or more. Typical 15-LO inhibitors have the formula ##STR1## wherein R.sup.13 is phenyl, 4-chlorophenyl, 4-fluorophenyl, 4-nitrophenyl, 2,5-dichlorophenyl, 2-furanyl, 2-thienyl, 3-pyridyl, or 4-pyridyl.
摘要翻译： PCT No.PCT / US96 / 14242 Sec。 371日期1995年10月5日第 102（e）日期1995年10月5日PCT 1996年9月5日提交15-脂肪氧合酶（15-LO）的抑制剂可用于治疗和预防炎症或动脉粥样硬化。 优选的抑制剂具有至少约10或更高的5-LO与15-LO抑制活性的比率。 典型的15-LO抑制剂具有下式：其中R 13是苯基，4-氯苯基，4-氟苯基，4-硝基苯基，2,5-二氯苯基，2-呋喃基，2-噻吩基，3-吡啶基或4-吡啶基。
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公开(公告)号：US5808062A
公开(公告)日：1998-09-15
申请号：US319768
申请日：1994-10-12
申请人： John Michael Domagala , Edmund Lee Ellsworth , Elizabeth Lunney , Daniel Fred Ortwine , Kimberly Suzanne Para , Josyula Venkata Nagendra Vara Prasad , Tomi Sawyer , Bradley Dean Tait
发明人： John Michael Domagala , Edmund Lee Ellsworth , Elizabeth Lunney , Daniel Fred Ortwine , Kimberly Suzanne Para , Josyula Venkata Nagendra Vara Prasad , Tomi Sawyer , Bradley Dean Tait
IPC分类号： A61K31/365 , A61P31/12 , A61P31/18 , C07D309/38 , C07D335/02 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D413/12 , C07F7/18 , C07D309/30 , C07D417/00 , C07D401/04
CPC分类号： C07D403/06 , C07D309/38 , C07D335/02 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D413/12 , C07F7/1856
摘要： The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.
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公开(公告)号：US5789440A
公开(公告)日：1998-08-04
申请号：US319821
申请日：1994-10-12
IPC分类号： C07C321/26 , C07C323/20 , C07C323/22 , C07D211/86 , C07D309/32 , C07D311/96 , C07D405/04 , C07D405/12 , C07D407/06 , C07D407/12 , A61K31/35 , A61K31/38 , A61K31/40 , A61K31/42 , A61K31/495 , A61K31/54
CPC分类号： C07D405/04 , C07C321/26 , C07C323/20 , C07C323/22 , C07D211/86 , C07D309/32 , C07D311/96 , C07D405/12 , C07D407/06 , C07D407/12 , C07C2101/08 , C07C2101/10 , C07C2101/14 , C07C2101/16
摘要： The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.
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