公开(公告)号：US07994194B2

公开(公告)日：2011-08-09

申请号：US12283620

申请日：2008-09-12

申请人： Scott L. Harbeson

发明人： Scott L. Harbeson

IPC分类号： C07D215/38 ,  A61K31/04

CPC分类号： C07D215/56

摘要： This invention relates to novel compounds that are 4-oxoquinoline derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel 4-oxoquinoline derivatives that are derivatives of elvitegravir. This invention also provides pyrogen-free 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 HIV integrase inhibitor, such as elvitegravir.

摘要翻译： 本发明涉及作为4-氧代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elvitegravir衍生物的新型4-氧代喹啉衍生物。 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整合酶抑制剂如elvitegravir有益治疗的疾病和病症的方法中的用途 。

公开(公告)号：US07943620B2

公开(公告)日：2011-05-17

申请号：US12075107

申请日：2008-03-07

申请人： Scott L. Harbeson ,  Craig Masse

发明人： Scott L. Harbeson ,  Craig Masse

IPC分类号： A61K31/497 ,  C07D241/04 ,  C07D295/00

CPC分类号： C07D295/15

摘要： This invention relates to novel compounds that partially inhibit fatty acid oxidation and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel compounds that are derivatives of ranolazine. This invention also provides compositions comprising one or more compound 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 partial fatty acid oxidation inhibitors, such as ranolazine.

摘要翻译： 本发明涉及部分抑制脂肪酸氧化的新化合物及其药学上可接受的盐。 更具体地，本发明涉及作为雷诺嗪衍生物的新化合物。 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，以及所公开的化合物和组合物在治疗通过部分脂肪酸氧化抑制剂如雷洛嗪有益治疗的疾病和病症的方法中的用途。

公开(公告)号：US07820666B2

公开(公告)日：2010-10-26

申请号：US12116475

申请日：2008-05-07

申请人： Scott L. Harbeson

发明人： Scott L. Harbeson

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00 ,  C07D495/00 ,  C07D497/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： This invention relates to novel substituted tetrahydrotriazolopyrazines and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates 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 enzyme inhibitor of dipeptidyl-peptidase IV (DPP-IV).

摘要翻译： 本发明涉及新型取代的四氢三唑并吡嗪及其衍生物，其药学上可接受的盐，溶剂化物和水合物。 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二肽基肽酶IV（DPP-IV）的酶抑制剂有益治疗的疾病和病症的方法中的用途。

公开(公告)号：US20090163371A1

公开(公告)日：2009-06-25

申请号：US11915533

申请日：2006-05-31

申请人： Andrew M. Stern ,  Scott L. Harbeson ,  Edward M. Driggers ,  Kerry L. Spear

发明人： Andrew M. Stern ,  Scott L. Harbeson ,  Edward M. Driggers ,  Kerry L. Spear

IPC分类号： C40B30/04 ,  C12Q1/68

CPC分类号： C12Q1/6804 ,  C12Q2563/179

摘要： The invention provides methods for compound and lead generation and discovery. In particular, the present invention provides a method for generating compounds and for selecting compounds that bind to a target. The present invention provides a way by which anchors (e.g., weak binders) and anchor-scaffold conjugates can be evolved into new generations of compounds having improved target binding and other desired pharmaceutical properties through control of both synthetic input and selection criteria.

摘要翻译： 本发明提供了化合物和引物产生和发现的方法。 特别地，本发明提供了一种产生化合物和选择与靶标结合的化合物的方法。 本发明提供了通过控制合成输入和选择标准，锚（例如，弱粘合剂）和锚 - 支架共轭物可以通过其改进的靶结合和其它期望的药物性质而演变成新一代化合物的方式。

公开(公告)号：US20090137457A1

公开(公告)日：2009-05-28

申请号：US12286903

申请日：2008-10-02

申请人： Scott L. Harbeson

发明人： Scott L. Harbeson

IPC分类号： A61K38/28 ,  C07D401/04 ,  A61K31/506 ,  C12N5/02

CPC分类号： C07D401/04

摘要： This invention relates to novel compounds that are pyrimidinedione derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrimidinedione derivatives that are derivatives of alogliptin. This invention also provides compositions comprising one or more compounds of this invention and a carrier, and the use of the disclosed compound and compositions in methods of treating diseases and conditions that are beneficially treated by administering a dipeptidyl peptidase IV (DPP4) inhibitor.

摘要翻译： 本发明涉及嘧啶二酮衍生物及其药学上可接受的盐的新化合物。 更具体地，本发明涉及作为脱镁蛋白衍生物的新型嘧啶二酮衍生物。 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，以及所公开的化合物和组合物在治疗通过施用二肽基肽酶IV（DPP4）抑制剂有益治疗的疾病和病症的方法中的用途。

公开(公告)号：US08592487B2

公开(公告)日：2013-11-26

申请号：US12387327

申请日：2009-04-28

申请人： Scott L. Harbeson

发明人： Scott L. Harbeson

IPC分类号： A61K31/34 ,  A01N43/08 ,  C07D493/00 ,  C01B4/00

CPC分类号： C07B59/002 ,  C07D493/04

摘要： This invention relates to novel compounds that are hydroxyethylamino sulfonamide derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel hydroxyethylamino sulfonamide derivatives that are derivatives of darunavir. 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 a human immunodeficiency virus (HIV) protease inhibitor, such as darunavir.

公开(公告)号：US20130012430A1

公开(公告)日：2013-01-10

申请号：US13534531

申请日：2012-06-27

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： A61K38/07 ,  C07K7/06 ,  A61P31/14 ,  C07K5/083 ,  A61K38/06 ,  C07K5/103 ,  A61K38/08

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：US20120270934A1

公开(公告)日：2012-10-25

申请号：US13381419

申请日：2010-07-02

申请人： Craig E. Masse ,  Scott L. Harbeson ,  Roger D. Tung

发明人： Craig E. Masse ,  Scott L. Harbeson ,  Roger D. Tung

IPC分类号： A61K31/5578 ,  C07D317/40 ,  A61K31/5585 ,  A61P9/00 ,  C07C69/73 ,  A61P9/12 ,  A61P13/12 ,  A61P35/00 ,  C07C69/732 ,  C07C311/51

CPC分类号： C07C69/734 ,  C07B2200/05 ,  C07B2200/07 ,  C07C59/46 ,  C07C69/732 ,  C07C311/51 ,  C07C2601/14 ,  C07C2602/22 ,  C07D317/34 ,  C07D319/06

摘要： This invention relates to novel prostacyclin derivatives and acceptable 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 prostacyclin, and in particular those diseases and conditions beneficially treated by dilators of systemic and pulmonary arterial vascular beds or by platelet aggregation inhibitors.

摘要翻译： 本发明涉及新型前列环素衍生物及其可接受的盐。 本发明还提供了包含本发明化合物和这些组合物在治疗由前列环素有益治疗的疾病和病症的方法中的用途，特别是那些通过全身和肺动脉血管床的扩张器或血小板有利地治疗的疾病和病症 聚集抑制剂。

公开(公告)号：US08158805B2

公开(公告)日：2012-04-17

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： A61K31/44 ,  C07D213/00

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.

公开(公告)号：US20110313004A1

公开(公告)日：2011-12-22

申请号：US13132784

申请日：2009-12-03

申请人： Scott L. Harbeson

发明人： Scott L. Harbeson

IPC分类号： A61K31/4412 ,  A61P11/00 ,  A61P25/00 ,  A61P13/12 ,  A61P9/00 ,  A61P17/02 ,  A61P25/28 ,  A61P1/16 ,  A61P15/00 ,  A61P35/00 ,  A61P37/06 ,  A61P17/00 ,  C07D213/64 ,  A61P43/00

CPC分类号： C07D213/64 ,  A61K31/4412 ,  C07B59/002

摘要： This invention relates to novel substituted pyridinones, their deuterium-modified derivatives 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 a TNF (tumor necrosis factor) alpha production inhibitor/TGF (transforming growth factor) beta inhibitor.

摘要翻译： 本发明涉及新的取代的吡啶酮，它们的氘改性衍生物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TNF（肿瘤坏死因子）α产生抑制剂/ TGF（转化生长因子）β抑制剂有益治疗的疾病和病症的方法中的用途。