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公开(公告)号:US20090274650A1
公开(公告)日:2009-11-05
申请号:US12370175
申请日:2009-02-12
申请人: Michael R. Hale , Roger Tung , Stephen Price , Robin David Wilkes , Wayne Carl Schairer , Ashley Nicholas Jarvis , Andrew Spaltenstein , Eric Steven Furfine , Vicente Samano , Istvan Kaldor , John Franklin Miller , Michael Stephen Brieger , Ronald George Sherrill
发明人: Michael R. Hale , Roger Tung , Stephen Price , Robin David Wilkes , Wayne Carl Schairer , Ashley Nicholas Jarvis , Andrew Spaltenstein , Eric Steven Furfine , Vicente Samano , Istvan Kaldor , John Franklin Miller , Michael Stephen Brieger , Ronald George Sherrill
IPC分类号: A61K31/443 , C07D493/04 , C07D413/12 , C07D317/46 , A61K31/5377 , A61K31/357 , A61K31/34 , A61K31/52 , A61K31/522 , A61K31/496 , A61K31/427 , A61K31/472 , A61K31/513 , A61K31/708 , A61K38/21 , A61K38/20 , A61P31/12 , A61P31/18
CPC分类号: C07D493/04 , A61K31/352 , A61K31/36 , A61K45/06 , C07D317/46 , A61K2300/00
摘要: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
摘要翻译: 本发明涉及一类新型的磺酰胺,它们是天冬氨酰蛋白酶抑制剂。 在一个实施方案中,本发明涉及以特定结构和物理化学特征为特征的新型HIV天冬氨酰蛋白酶抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制HIV-1和HIV-2蛋白酶活性,因此可有利地用作针对HIV-1和HIV-2病毒的抗病毒剂。 本发明还涉及使用本发明化合物抑制HIV天冬氨酰蛋白酶活性的方法和用于筛选抗HIV活性化合物的方法。
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公开(公告)号:US08455497B2
公开(公告)日:2013-06-04
申请号:US12370175
申请日:2009-02-12
申请人: Michael R. Hale , Roger Tung , Stephen Price , Robin David Wilkes , Wayne Carl Schairer , Ashley Nicholas Jarvis , Andrew Spaltenstein , Eric Steven Furfine , Vicente Samano , Istvan Kaldor , John Franklin Miller , Michael Stephen Brieger , Ronald George Sherrill
发明人: Michael R. Hale , Roger Tung , Stephen Price , Robin David Wilkes , Wayne Carl Schairer , Ashley Nicholas Jarvis , Andrew Spaltenstein , Eric Steven Furfine , Vicente Samano , Istvan Kaldor , John Franklin Miller , Michael Stephen Brieger , Ronald George Sherrill
IPC分类号: C07D493/04 , A61K31/34 , A61K31/357 , A61K31/36 , A61P31/18 , C07C311/16 , C07C311/29
CPC分类号: C07D493/04 , A61K31/352 , A61K31/36 , A61K45/06 , C07D317/46 , A61K2300/00
摘要: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
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公开(公告)号:US06878728B1
公开(公告)日:2005-04-12
申请号:US09591464
申请日:2000-06-09
申请人: Michael R. Hale , Roger Tung , Stephen Price , Robin David Wilkes , Wayne Carl Schairer , Ashley Nicholas Jarvis , Andrew Spaltenstein , Eric Steven Furfine , Vicente Samano , Istvan Kaldor , John Franklin Miller , Michael Stephen Brieger
发明人: Michael R. Hale , Roger Tung , Stephen Price , Robin David Wilkes , Wayne Carl Schairer , Ashley Nicholas Jarvis , Andrew Spaltenstein , Eric Steven Furfine , Vicente Samano , Istvan Kaldor , John Franklin Miller , Michael Stephen Brieger
IPC分类号: A61K31/352 , A61K31/36 , A61K45/06 , A61K31/454 , A61K31/422 , C07D413/14 , C07D417/12
CPC分类号: C07D493/04 , A61K31/352 , A61K31/36 , A61K45/06 , C07D277/24 , C07D317/62 , C07D407/12 , A61K2300/00
摘要: The invention provides novel compounds of formula (I) wherein all variables are as defined in the specification, that are useful as inhibitors of aspartyl proteases.
摘要翻译: 本发明提供新的式(I)化合物,其中所有变量如说明书中所定义,可用作天冬氨酰蛋白酶抑制剂。
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公开(公告)号:US20050148548A1
公开(公告)日:2005-07-07
申请号:US10958223
申请日:2004-10-04
申请人: Roger Tung , Michael Hale , Christopher Baker , Eric Furfine , Istvan Kaldor , Wieslaw Kazmierski , Andrew Spaltenstein
发明人: Roger Tung , Michael Hale , Christopher Baker , Eric Furfine , Istvan Kaldor , Wieslaw Kazmierski , Andrew Spaltenstein
IPC分类号: A61K31/18 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/4025 , A61K31/496 , A61K31/66 , A61K31/661 , A61K31/664 , A61K31/7048 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/15 , C07C311/18 , C07C311/37 , C07D277/30 , C07D307/20 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/26 , A61K31/675 , A61K31/443 , A61K31/4709 , A61K31/551
CPC分类号: C07D405/12 , C07C311/18 , C07D307/20 , C07F9/65515 , C07F9/65844 , C07H15/04
摘要: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
摘要翻译: 本发明涉及作为天冬氨酰蛋白酶抑制剂的一类磺酰胺的前药。 在一个实施方案中,本发明涉及HIV天冬氨酰蛋白酶抑制剂的新一类前药,其特征在于有利的水溶性,高口服生物利用度和活性成分的体内易生成。 本发明还涉及包含这些前药的药物组合物。 本发明的前药和药物组合物特别适用于降低药丸负担并增加患者依从性。 本发明还涉及用这些前药和药物组合物治疗哺乳动物的方法。
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公开(公告)号:US09045453B2
公开(公告)日:2015-06-02
申请号:US13107873
申请日:2011-05-13
申请人: Roger Tung
发明人: Roger Tung
IPC分类号: C07D401/00 , C07D401/04
CPC分类号: C07D401/04 , A61K31/454 , A61K45/06 , C07B2200/05
摘要: This invention relates to novel substituted dioxopiperidinyl phthalimide derivatives and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an immunomodulatory agent.
摘要翻译: 本发明涉及新的取代的二氧代哌啶基邻苯二甲酰亚胺衍生物及其药学上可接受的酸加成盐。 本发明还提供包含本发明化合物的组合物以及这些组合物在治疗由免疫调节剂有益治疗的疾病和病症的方法中的用途。
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公开(公告)号:US08541436B2
公开(公告)日:2013-09-24
申请号:US13118935
申请日:2011-05-31
申请人: Roger Tung
发明人: Roger Tung
IPC分类号: A61K31/4748 , C07D221/22
CPC分类号: A61K31/195 , A61K31/4709 , A61K31/485 , A61K31/49 , C07B59/002 , C07D221/28 , C07D471/08
摘要: This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ1 receptor agonist that also has NMDA antagonist activity.
摘要翻译: 本公开涉及新的吗啡喃化合物及其衍生物,其药学上可接受的盐,溶剂合物和水合物。 本公开还提供了包含本公开的化合物的组合物以及该组合物在治疗通过施用也具有NMDA拮抗剂活性的σ1受体激动剂有益治疗的疾病和病症的方法中的用途。
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公开(公告)号:US08450492B2
公开(公告)日:2013-05-28
申请号:US12688466
申请日:2010-01-15
申请人: Roger Tung
发明人: Roger Tung
IPC分类号: C07D211/22
CPC分类号: A61K31/4525 , C07D317/64 , C07D405/12
摘要: The present invention relates to an isotopologue of Compound 1 substituted with deuterium at the methylene carbon of the benzodioxol ring. The isotopologues of this invention selective serotonin reuptake inhibitors (SSRIs) and possess unique biopharmaceutical and metabolic properties compared to Compound 1. They may also be used to accurately determine the concentration of Compound 1 in biological fluids and to determine metabolic patterns of Compound 1 and its isotopologues. The invention further provides compositions comprising these deuterated isotopologues and methods of treating diseases and conditions that are responsive to increased neuronal serotonin transmission, alone and in combination with additional agents.
摘要翻译: 本发明涉及在苯并二氧杂环戊烯的亚甲基碳上被氘取代的化合物1的同位素学。 本发明的同位素学选择性5-羟色胺再摄取抑制剂(SSRIs)并且与化合物1相比具有独特的生物药物和代谢性质。它们还可用于精确测定化合物1在生物流体中的浓度并确定化合物1及其化合物1的代谢模式 同位素学。 本发明还提供包含这些氘代同位素异构体的组合物和治疗对增加的神经元血清素传递起反应的疾病和病症的方法,其单独和与另外的试剂组合。
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公开(公告)号:US08338425B2
公开(公告)日:2012-12-25
申请号:US12331431
申请日:2008-12-09
申请人: Roger Tung
发明人: Roger Tung
IPC分类号: A61K31/497 , C07D403/14
CPC分类号: C07D417/14 , A61K31/506 , A61K45/06 , C07D417/12
摘要: This invention relates to novel 2-{6-[4-(2-hydroxy-ethyl)-piperazin-1-yl]-2-methyl-pyrimidin-4-ylamino}-thiazole-5-carboxylic acid (2-chloro-6-methyl-phenyl)-amide derivatives, and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by the inhibition of kinases including Src-kinase and Bcr-Abl kinase.
摘要翻译: 本发明涉及新的2- {6- [4-(2-羟基 - 乙基) - 哌嗪-1-基] -2-甲基 - 嘧啶-4-基氨基} - 噻唑-5-羧酸(2-氯 - 6-甲基 - 苯基) - 酰胺衍生物及其药学上可接受的酸加成盐。 本发明还提供包含本发明化合物的组合物和这些组合物在治疗通过抑制包括Src-激酶和Bcr-Abl激酶的激酶有益治疗的疾病和病症的方法中的用途。
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公开(公告)号:US20120149709A1
公开(公告)日:2012-06-14
申请号:US13256787
申请日:2010-03-16
申请人: Julie F. Liu , Roger Tung , Scott L. Harbeson
发明人: Julie F. Liu , Roger Tung , Scott L. Harbeson
IPC分类号: A61K31/498 , A01N43/90 , A01P15/00 , A61P33/12 , A61P33/10 , C07D471/04 , A61P33/06
CPC分类号: C07D471/04 , A61K31/4184 , A61K31/4985 , A61K45/06 , Y02A50/411 , Y02A50/423 , A61K2300/00
摘要: This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
摘要翻译: 本发明涉及吡嗪并异喹啉衍生物的新化合物及其药学上可接受的盐。 更具体地,本发明涉及作为吡喹酮衍生物的新型吡嗪异喹啉衍生物。 本发明还提供包含一种或多种本发明化合物和载体的组合物,以及所述化合物和组合物在治疗通过施用抗栓剂如吡喹酮有益治疗的疾病和病症的方法中的用途。
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公开(公告)号:US20110300132A1
公开(公告)日:2011-12-08
申请号:US12986135
申请日:2011-01-06
申请人: Roger Tung , Adam Morgan
发明人: Roger Tung , Adam Morgan
IPC分类号: A61K39/395 , A61K31/675 , A61P35/02 , A61K33/24 , A61P35/00 , C07F9/09 , A61K38/22
CPC分类号: C07F9/65586
摘要: This invention relates to prodrugs of 4-aminoquinazoline compounds, and to pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER2.
摘要翻译: 本发明涉及4-氨基喹唑啉化合物的前药及其药学上可接受的盐。 本发明还提供了包含本发明化合物的组合物和这些组合物在治疗通过施用EGFR和HER2的抑制剂有益治疗的疾病和病症的方法中的用途。
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