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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：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：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：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：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：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：US09040547B2
公开(公告)日：2015-05-26
申请号：US13617035
申请日：2012-09-14
申请人： Hengmiao Cheng , Theodore Otto Johnson, Jr. , John Charles Kath , Kevin Kun-Chin Liu , Elizabeth Ann Lunney , Asako Nagata , Sajiv Krishnan Nair , Simon Paul Planken , Scott Channing Sutton
发明人： Hengmiao Cheng , Theodore Otto Johnson, Jr. , John Charles Kath , Kevin Kun-Chin Liu , Elizabeth Ann Lunney , Asako Nagata , Sajiv Krishnan Nair , Simon Paul Planken , Scott Channing Sutton
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/52 , C07D473/16 , C07D487/04
CPC分类号： C07D487/04 , C07D473/18 , C07D519/00
摘要： The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中Q，T，V，W，X，Y，Z，环A，R1，R2，R3，R4，R5，R5a，R6，R7 ，R 8，R 9，R 10，R 11，R 12，R 13，R 14，R 15，R 16，R 17和m如本文所定义。 有新的吡咯并嘧啶和嘌呤衍生物可用于哺乳动物治疗异常细胞生长，如癌症。 另外的实施方案涉及含有化合物的药物组合物和使用化合物和组合物治疗哺乳动物异常细胞生长的方法。
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公开(公告)号：US20130079324A1
公开(公告)日：2013-03-28
申请号：US13617035
申请日：2012-09-14
申请人： Hengmiao Cheng , Theodore Otto Johnson, JR. , John Charles Kath , Kevin Kun-Chin Liu , Elizabeth Ann Lunney , Asako Nagata , Sajiv Krishnan Nair , Simon Paul Planken , Scott Channing Sutton
发明人： Hengmiao Cheng , Theodore Otto Johnson, JR. , John Charles Kath , Kevin Kun-Chin Liu , Elizabeth Ann Lunney , Asako Nagata , Sajiv Krishnan Nair , Simon Paul Planken , Scott Channing Sutton
IPC分类号： A61K31/519 , C07D473/18 , A61P35/00 , A61K31/5377 , C07D498/10 , A61K31/5386 , C07D487/04 , A61K31/52
CPC分类号： C07D487/04 , C07D473/18 , C07D519/00
摘要： The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
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9.发明授权Sulfonamide substituted aspartic acid interleukin-1.beta. converting enzyme inhibitors 失效磺酰胺取代的天冬氨酸白细胞介素-1β转换酶抑制剂
公开(公告)号：US6083981A
公开(公告)日：2000-07-04
申请号：US284425
申请日：1999-04-09
申请人： Hamish John Allen , Kenneth Dale Brady , William Glen Harter , Elizabeth Ann Lunney , Mark Stephen Plummer , Tomi Sawyer , Aurash Shahripour , Nigel Walker
发明人： Hamish John Allen , Kenneth Dale Brady , William Glen Harter , Elizabeth Ann Lunney , Mark Stephen Plummer , Tomi Sawyer , Aurash Shahripour , Nigel Walker
IPC分类号： A61K31/192 , A61K31/341 , A61P1/00 , A61P7/08 , A61P19/02 , A61P25/28 , A61P31/04 , C07C311/19 , C07C311/29 , C07C311/46 , C07C323/67 , C07D307/12 , C07D307/40
CPC分类号： C07D307/12 , C07C311/19 , C07C311/29 , C07C311/46 , C07C323/67 , C07C2101/14 , C07C2102/10
摘要： The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula I, II, or III. ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock reperfusion injury, Alzheimer's disease, and shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.
摘要翻译： PCT No.PCT / US97 / 18406 Sec。 371日期1999年4月9日第 102（e）1999年4月9日PCT 1997年10月9日PCT公布。 公开号WO98 / 16504 日期：1998年04月23日本发明涉及具有式I，II或III的白细胞介素-1β转换酶抑制剂的化合物。 本发明还涉及治疗中风，炎性疾病，败血性休克再灌注损伤，阿尔茨海默氏病和志贺氏菌病的方法，以及含有作为白细胞介素-1β转换酶抑制剂的化合物的药学上可接受的组合物。
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