公开(公告)号：US08314141B2

公开(公告)日：2012-11-20

申请号：US12031486

申请日：2008-02-14

申请人： Roger D. Tung ,  Scott L. Harbeson ,  David D. Deininger ,  Mark A. Murcko ,  Govinda R. Bhisetti ,  Luc J. Farmer

发明人： Roger D. Tung ,  Scott L. Harbeson ,  David D. Deininger ,  Mark A. Murcko ,  Govinda R. Bhisetti ,  Luc J. Farmer

IPC分类号： A61K31/40

CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/1024 ,  C07K5/1027 ,  C07K7/02

摘要： The present invention relates to Formula (II) compounds having the structure as well as to their use in methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases.

摘要翻译： 本发明涉及具有结构的式（II）化合物及其在抑制蛋白酶，特别是丝氨酸蛋白酶，更具体地HCV NS3蛋白酶的方法和药物组合物中的用途。

公开(公告)号：US08263601B2

公开(公告)日：2012-09-11

申请号：US12874783

申请日：2010-09-02

申请人： Roger D. Tung ,  Julie F. Liu ,  Scott L. Harbeson

发明人： Roger D. Tung ,  Julie F. Liu ,  Scott L. Harbeson

IPC分类号： C07D473/10 ,  A61K31/522 ,  A61P1/16 ,  A61P13/12 ,  A61P25/02 ,  A61P3/10 ,  C07B59/00

CPC分类号： A61K31/522 ,  C07D473/06

摘要： This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. In particular, this invention relates to novel substituted xanthine derivatives that are derivatives of a pentoxifylline metabolite. 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 for which pentoxifylline and related compounds are beneficial. The compounds of the invention are represented by one of the following structural formulas: wherein the values of R1, R2, Y1 and Y2 are described herein.

摘要翻译： 本发明涉及作为取代黄嘌呤衍生物的新化合物及其药学上可接受的盐。 特别地，本发明涉及作为己酮可可碱代谢物的衍生物的新的取代黄嘌呤衍生物。 本发明还提供了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己酮可可碱和相关化合物有益的疾病和病症的方法中的用途。 本发明的化合物由以下结构式之一表示：其中R1，R2，Y1和Y2的值在本文中描述。

公开(公告)号：US20110065711A1

公开(公告)日：2011-03-17

申请号：US12820570

申请日：2010-06-22

申请人： Scott L. Harbeson ,  Roger D. Tung ,  Julie F. Liu

发明人： Scott L. Harbeson ,  Roger D. Tung ,  Julie F. Liu

IPC分类号： A61K31/5025 ,  C07D487/04 ,  A61P25/00 ,  A61P29/00 ,  A61P19/02

CPC分类号： C07D487/04 ,  A61K31/5025 ,  A61K45/06

摘要： This invention relates to novel substituted triazolo-pyridazines and 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 an α1-GABAA receptor antagonist or an α2- and/or an α3-GABAA receptor partial agonist.

摘要翻译： 本发明涉及新的取代三唑并 - 哒嗪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α1-GABA A受体拮抗剂或α2-和/或α3-GABA A受体部分激动剂有益治疗的疾病和病症的方法中的用途 。

公开(公告)号：US20110059995A1

公开(公告)日：2011-03-10

申请号：US12874049

申请日：2010-09-01

申请人： Roger D. Tung ,  Julie F. Liu ,  Scott L. Harbeson

发明人： Roger D. Tung ,  Julie F. Liu ,  Scott L. Harbeson

IPC分类号： A61K31/522 ,  C07D473/04 ,  A61P3/10 ,  A61P1/16 ,  A61P13/12 ,  A61P27/02 ,  A61P31/18

CPC分类号： C07D473/04 ,  C07D473/06

摘要： This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. 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 for which pentoxifylline and related compounds are beneficial.

公开(公告)号：US20090239886A1

公开(公告)日：2009-09-24

申请号：US12380579

申请日：2009-02-27

申请人： Roger D. Tung ,  Julie F. Liu ,  Scott L. Harbeson

发明人： Roger D. Tung ,  Julie F. Liu ,  Scott L. Harbeson

IPC分类号： A61K31/522 ,  C07D473/04 ,  A61P13/12

CPC分类号： C07D473/10 ,  C07B2200/05 ,  C07B2200/07 ,  C07D473/04

摘要： This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. 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 for which pentoxifylline and related compounds are beneficial.

摘要翻译： 本发明涉及作为取代黄嘌呤衍生物的新化合物及其药学上可接受的盐。 例如，本发明涉及作为己酮可可碱衍生物的新型取代黄嘌呤衍生物。 本发明还提供了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己酮可可碱和相关化合物有益的疾病和病症的方法中的用途。

公开(公告)号：US06617309B2

公开(公告)日：2003-09-09

申请号：US09875390

申请日：2001-06-06

申请人： Roger D Tung ,  Scott L. Harbeson ,  David D. Deininger ,  Mark A. Murcko ,  Govinda R. Bhisetti ,  Luc J. Farmer

发明人： Roger D Tung ,  Scott L. Harbeson ,  David D. Deininger ,  Mark A. Murcko ,  Govinda R. Bhisetti ,  Luc J. Farmer

IPC分类号： A61K31497

CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/1024 ,  C07K5/1027 ,  C07K7/02

摘要： The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

公开(公告)号：US08952016B2

公开(公告)日：2015-02-10

申请号：US12874049

申请日：2010-09-01

申请人： Roger D. Tung ,  Julie F. Liu ,  Scott L. Harbeson

发明人： Roger D. Tung ,  Julie F. Liu ,  Scott L. Harbeson

IPC分类号： A61K31/522 ,  C07D473/04 ,  C07D473/06

CPC分类号： C07D473/04 ,  C07D473/06

摘要： This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. The compound of the invention are represented by one of the following structural formulas: The variables for these structural formulas are described herein. 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 for which pentoxifylline and related compounds are beneficial.

摘要翻译： 本发明涉及作为取代黄嘌呤衍生物的新化合物及其药学上可接受的盐。 例如，本发明涉及作为己酮可可碱衍生物的新型取代黄嘌呤衍生物。 本发明的化合物由以下结构式之一表示：这些结构式的变量在本文中描述。 本发明还提供了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己酮可可碱和相关化合物有益的疾病和病症的方法中的用途。

公开(公告)号：US20120165288A1

公开(公告)日：2012-06-28

申请号：US13411089

申请日：2012-03-02

申请人： Scott L. Harbeson ,  Roger D. Tung

发明人： Scott L. Harbeson ,  Roger D. Tung

IPC分类号： A61K31/4418 ,  A61K31/536 ,  A61K31/522 ,  A61P31/18 ,  A61K31/675 ,  A61K31/52 ,  A61K31/7072 ,  C07D213/56 ,  A61K31/506

CPC分类号： C07D213/42 ,  C07F9/58

摘要： This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.

摘要翻译： 本发明涉及作为氮杂肽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HIV蛋白酶抑制剂阿扎那韦硫酸盐的衍生物的新型氮杂肽化合物。 本发明还提供了包含一种或多种本发明化合物和载体的无热原组合物，以及所公开的化合物和组合物在治疗通过施用HIV蛋白酶抑制剂治疗的疾病和病症的方法中的用途。 本发明还涉及一种或多种所公开的化合物在涉及阿扎那韦的分析研究中作为试剂的用途。

公开(公告)号：US20110077255A1

公开(公告)日：2011-03-31

申请号：US12874783

申请日：2010-09-02

申请人： Roger D. Tung ,  Julie F. Liu ,  Scott L. Harbeson

发明人： Roger D. Tung ,  Julie F. Liu ,  Scott L. Harbeson

IPC分类号： A61K31/522 ,  C07D473/16 ,  A61P3/10 ,  A61P3/04 ,  A61P3/06 ,  A61P7/06 ,  A61P27/02 ,  A61P11/00

CPC分类号： A61K31/522 ,  C07D473/06

摘要： This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. 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 for which pentoxifylline and related compounds are beneficial.

摘要翻译： 本发明涉及作为取代黄嘌呤衍生物的新化合物及其药学上可接受的盐。 例如，本发明涉及作为己酮可可碱衍生物的新型取代黄嘌呤衍生物。 本发明还提供了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己酮可可碱和相关化合物有益的疾病和病症的方法中的用途。

公开(公告)号：US20110009355A1

公开(公告)日：2011-01-13

申请号：US12755184

申请日：2010-04-06

申请人： Scott L. Harbeson ,  Roger D. Tung

发明人： Scott L. Harbeson ,  Roger D. Tung

IPC分类号： A61K31/708 ,  C07D213/56 ,  A61K31/4418 ,  C07F9/06 ,  A61K31/675 ,  A61K31/536 ,  A61K31/472 ,  A61K31/505 ,  A61P31/18

CPC分类号： C07D213/42 ,  C07F9/58

摘要： This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.

摘要翻译： 本发明涉及作为氮杂肽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HIV蛋白酶抑制剂阿扎那韦硫酸盐的衍生物的新型氮杂肽化合物。 本发明还提供了包含一种或多种本发明化合物和载体的无热原组合物，以及所公开的化合物和组合物在治疗通过施用HIV蛋白酶抑制剂治疗的疾病和病症的方法中的用途。 本发明还涉及一种或多种所公开的化合物在涉及阿扎那韦的分析研究中作为试剂的用途。