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1. 发明授权

US08980837B2 Inhibitors of IAP 有权
标题翻译： IAP抑制剂
公开(公告)号：US08980837B2
公开(公告)日：2015-03-17
申请号：US13356556
申请日：2012-01-23
申请人： Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
发明人： Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
IPC分类号： A61K38/06 , A61K31/55 , A61K31/42 , A61K31/433 , A61K31/4436 , A61K31/426 , A61K31/415 , A61K31/381 , A61P35/04 , A61K31/4245 , A61K31/41 , A61K31/506 , C07D417/14 , C12N5/09 , A61K38/17 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07D513/04 , C07K5/062 , C07K5/083 , C07K5/08 , C07K7/06
CPC分类号： C07D417/14 , A61K31/55 , A61K38/177 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07D513/04 , C07K5/06026 , C07K5/0806 , C07K5/0827 , C07K7/06 , C12N5/0693
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4′, R5, R5′, R6 and R6′ are as described herein.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中化合物具有通式I：其中X，Y，A，R 1，R 2，R 3，R 4，R 4'，R 5，R 5'，R 6和 R6'如本文所述。

2. 发明授权

US08394795B2 Pyrazole [3, 4-B] pyridine Raf inhibitors 失效
标题翻译：吡唑[3,4-B]吡啶Raf抑制剂
公开(公告)号：US08394795B2
公开(公告)日：2013-03-12
申请号：US12920050
申请日：2009-02-27
申请人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jason De Meese , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , Paul Lunghofer , David Moreno , Brad Newhouse , Li Ren , Jeongbeob Seo , Hongqi Tian , Steven Mark Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
发明人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jason De Meese , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , Paul Lunghofer , David Moreno , Brad Newhouse , Li Ren , Jeongbeob Seo , Hongqi Tian , Steven Mark Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
IPC分类号： A61K31/535 , A61K31/44 , C07D413/14 , C07D471/04
CPC分类号： C07D471/04 , C07C311/08
摘要： Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
摘要翻译：式I化合物可用于抑制Raf激酶。公开了使用式I化合物和立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

3. 发明授权

US08338452B2 Raf inhibitor compounds and methods of use thereof 失效
标题翻译： Raf抑制剂化合物及其使用方法
公开(公告)号：US08338452B2
公开(公告)日：2012-12-25
申请号：US12920045
申请日：2009-02-27
申请人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , David Moreno , Brad Newhouse , Li Ren , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
发明人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , David Moreno , Brad Newhouse , Li Ren , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02 , C07D491/02
CPC分类号： C07D471/04 , C07C311/08
摘要： Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
摘要翻译：式（I）的化合物可用于抑制Raf激酶。公开了使用式（I）化合物及其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

4. 发明授权

US08119678B2 Compounds, compositions and methods 有权
公开(公告)号：US08119678B2
公开(公告)日：2012-02-21
申请号：US13075076
申请日：2011-03-29
申请人： Andrew McDonald , Gustave Bergnes , Bainian Feng , David J. Morgans, Jr. , Steven David Knight , Kenneth A. Newlander , Dashyant Dhanak , Christopher A. Brook
发明人： Andrew McDonald , Gustave Bergnes , Bainian Feng , David J. Morgans, Jr. , Steven David Knight , Kenneth A. Newlander , Dashyant Dhanak , Christopher A. Brook
IPC分类号： A61K31/4164
CPC分类号： C07D405/06 , C07D311/22 , C07D311/36 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

5. 发明授权

US07763628B2 Methods and compositions utilizing quinazolinones 失效
标题翻译：使用喹唑啉酮的方法和组合物
公开(公告)号：US07763628B2
公开(公告)日：2010-07-27
申请号：US11788039
申请日：2007-04-17
申请人： Jeffrey T. Finer , Gustav E Bergnes , Whitney W. Smith , John C. Chabala , Bainian Feng
发明人： Jeffrey T. Finer , Gustav E Bergnes , Whitney W. Smith , John C. Chabala , Bainian Feng
IPC分类号： A61K31/517 , C07D239/72
CPC分类号： C07D239/90 , C07D239/91
摘要： Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.
摘要翻译：公开了式1a，1b，1c和1d的喹唑啉酮。它们可用于治疗与KSP驱动蛋白活性相关的细胞增殖性疾病和病症。

6. 发明申请

US20100063073A1 Methods and Compositions Utilizing Quinazolinones 有权
标题翻译：使用喹唑啉酮的方法和组合
公开(公告)号：US20100063073A1
公开(公告)日：2010-03-11
申请号：US12547390
申请日：2009-08-25
申请人： Jeffrey T. Finer , Gustave Bergnes , Whitney W. Smith , John C. Chabala , Bainian Feng
发明人： Jeffrey T. Finer , Gustave Bergnes , Whitney W. Smith , John C. Chabala , Bainian Feng
IPC分类号： A61K31/517 , A61P35/00
CPC分类号： C07D239/90 , C07D239/91
摘要： Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.
摘要翻译：公开了式1a，1b，1c和1d的喹唑啉酮。它们可用于治疗与KSP驱动蛋白活性相关的细胞增殖性疾病和病症。

7. 发明授权

US07605164B2 Compositions and methods for treating heart failure 有权
标题翻译：治疗心力衰竭的组合物和方法
公开(公告)号：US07605164B2
公开(公告)日：2009-10-20
申请号：US11353252
申请日：2006-02-14
申请人： Fady Malik , Adam Lewis Tomasi , Bainian Feng , Erica Anne Kraynack , Kathleen A. Elias , Pu-Ping Lu , Whitney Walter Smith , Xiangping Qian , David J. Morgans, Jr.
发明人： Fady Malik , Adam Lewis Tomasi , Bainian Feng , Erica Anne Kraynack , Kathleen A. Elias , Pu-Ping Lu , Whitney Walter Smith , Xiangping Qian , David J. Morgans, Jr.
IPC分类号： A61K31/497 , A61K31/381 , A61K31/4409 , A61K31/4406 , A61K31/4402 , A61K31/42 , A61P9/04 , C07D401/10 , C07D403/10 , C07D213/643 , C07D213/65 , C07D213/68 , C07D261/18 , C07D333/22
CPC分类号： C07D401/12 , A61K31/4412 , A61K31/444 , A61K31/513 , C07D213/65 , C07D261/18 , C07D333/38 , C07D409/12 , C07D413/12
摘要： Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
摘要翻译：某些取代的苯甲酰胺衍生物选择性地调节心脏肌节，例如通过增强心肌肌球蛋白，并且可用于治疗包括充血性心力衰竭的收缩性心力衰竭。

8. 发明授权

US07375078B2 Heterocyclic self-immolative linkers and conjugates 有权
标题翻译：杂环自我消失的接头和共轭体
公开(公告)号：US07375078B2
公开(公告)日：2008-05-20
申请号：US11064785
申请日：2005-02-22
申请人： Bainian Feng
发明人： Bainian Feng
IPC分类号： A61K38/00
CPC分类号： C07D277/46 , A61K38/00 , A61K47/65 , C07D417/12 , C07K5/06052
摘要： The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form.
摘要翻译：本发明提供了可用于将药物部分与配体连接的杂环连接体化合物。化合物还包括药物 - 配体缀合物，其包含能够靶向所选细胞群体的配体，以及通过杂环连接体部分与配体连接的药物。连接体部分包含肽序列，其是细胞内酶的底物，例如组织蛋白酶，其在酰胺键处切割肽。该肽还含有连接药物和蛋白质肽序列的自分离部分。通过细胞内酶切割肽序列后，自我脱除部分自身从药物部分切割，使得药物部分处于未衍生的和活性的形式。

9. 发明申请

US20070299052A1 Inhibitors of IAP 审中-公开
公开(公告)号：US20070299052A1
公开(公告)日：2007-12-27
申请号：US11739030
申请日：2007-04-23
申请人： Frederick Cohen , Kurt Deshayes , Wayne Fairbrother , Bainian Feng , John Flygare , Lewis Gazzard , Vickie Tsui
发明人： Frederick Cohen , Kurt Deshayes , Wayne Fairbrother , Bainian Feng , John Flygare , Lewis Gazzard , Vickie Tsui
IPC分类号： A61K31/55 , A61K31/351 , A61K31/40 , A61K31/41 , A61P35/00 , C07D207/30 , C07D223/14 , C07D277/02 , C07D309/02 , C12N9/00 , C12N5/00 , C07D285/06 , C07D231/02 , C07D221/00 , A61P43/00 , A61K31/415 , A61K31/426 , A61K31/445
CPC分类号： C07D417/14 , A61K31/55 , A61K38/177 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07D513/04 , C07K5/06026 , C07K5/0806 , C07K5/0827 , C07K7/06 , C12N5/0693
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4′, R5, R5′, R6 and R6′ are as described herein.

10. 发明申请

US20050187232A1 Methods and compositions utilizing quinazolinones 有权
标题翻译：使用喹唑啉酮的方法和组合物
公开(公告)号：US20050187232A1
公开(公告)日：2005-08-25
申请号：US11084787
申请日：2005-03-21
申请人： Jeffrey Finer , Gustave Bergnes , Whitney Smith , John Chabala , Bainian Feng
发明人： Jeffrey Finer , Gustave Bergnes , Whitney Smith , John Chabala , Bainian Feng
IPC分类号： C07D239/90 , C07D239/91 , A61K31/517
CPC分类号： C07D239/90 , C07D239/91
摘要： Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.
摘要翻译：公开了式1a，1b，1c和1d的喹唑啉酮。它们可用于治疗与KSP驱动蛋白活性相关的细胞增殖性疾病和病症。

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