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1. 发明授权

US11180518B2 Phenyl-heterocycle-phenyl derivatives for use in the treatment or prevention of melanoma 有权
公开(公告)号：US11180518B2
公开(公告)日：2021-11-23
申请号：US16612717
申请日：2018-05-11
申请人： MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V. , LUDWIG-MAXIMILIANS-UNIVERSITÄT MÜNCHEN
发明人： Dorothea Becker , Thomas M. Jovin , Christian Griesinger , Andrei Leonov , Sergey Ryazanov , Armin Giese , Tiago F. Outeiro , Diana F. Lazaro , Michael P. Schön , Margarete Schön
IPC分类号： C07F9/6503 , A61P35/00 , C07D231/12 , C07D261/08 , C07D271/06 , C07D403/10 , C07D405/10 , C07D413/10 , A61K31/675 , A61K31/4155 , A61K31/415
摘要： The present invention relates to a compound represented by the formula (E) which is useful for treating or preventing melanoma.

2. 发明申请

US20210002233A1 PKM2 MODULATORS AND METHODS FOR THEIR USE 有权
公开(公告)号：US20210002233A1
公开(公告)日：2021-01-07
申请号：US16930254
申请日：2020-07-15
申请人： SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC.
发明人： Koc-Kan HO , Yong XU , Michael David SAUNDERS , Xiaohui LIU , Scott Albert PEARCE , Kevin Bret WRIGHT , Jason Marc FOULKS , Kenneth Mark PARNELL , Steven Brian KANNER , David Lee VOLLMER , Jihua LIU
IPC分类号： C07D231/14 , C07D231/38 , C07F9/6503 , C07D403/12 , C07D401/14 , C07D405/14 , C07D231/16 , C07D401/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , A61P11/00 , A61P43/00 , A61P35/00 , A61K31/4155
摘要： Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

3. 发明申请

US20200109120A1 PKM2 MODULATORS AND METHODS FOR THEIR USE 审中-公开
公开(公告)号：US20200109120A1
公开(公告)日：2020-04-09
申请号：US16584912
申请日：2019-09-26
申请人： TOLERO PHARMACEUTICALS, INC.
发明人： Koc-Kan HO , Yong XU , Michael David SAUNDERS , Xiaohui LIU , Scott Albert PEARCE , Kevin Bret WRIGHT , Jason Marc FOULKS , Kenneth Mark PARNELL , Steven Brian KANNER , David Lee VOLLMER , Jihua LIU
IPC分类号： C07D231/14 , C07D231/38 , C07F9/6503 , C07D403/12 , C07D401/14 , C07D405/14 , C07D231/16 , C07D401/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

4. 发明授权

US10207996B2 PKM2 modulators and methods for their use 有权
公开(公告)号：US10207996B2
公开(公告)日：2019-02-19
申请号：US15183581
申请日：2016-06-15
申请人： Tolero Pharmaceuticals, Inc.
发明人： Koc-Kan Ho , Yong Xu , Michael David Saunders , Xiaohui Liu , Scott Albert Pearce , Kevin Bret Wright , Jason Marc Foulks , Kenneth Mark Parnell , Steven Brian Kanner , David Lee Vollmer , Jihua Liu
IPC分类号： C07D231/14 , C07D231/16 , C07D231/38 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07F9/6503 , A61K31/455
摘要： Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

5. 发明申请

US20170229670A1 COPPER (I) PYRAZOLATE DIMERS FOR ELECTROLUMINESCENT DEVICES 审中-公开
公开(公告)号：US20170229670A1
公开(公告)日：2017-08-10
申请号：US15515176
申请日：2015-10-06
申请人： Dow Global Technologies LLC
发明人： David S. Laitar , Thomas P. Clark , Aaron A. Rachford , Sukrit Mukhopadhyay , Timothy S. De Vries , David D. Devore
IPC分类号： H01L51/50 , C09K11/06 , C07F9/655 , C07F9/6503 , H01L51/00 , C07F9/50
CPC分类号： H01L51/5016 , C07F9/5045 , C07F9/65031 , C07F9/65522 , C09K11/06 , C09K2211/1007 , C09K2211/1044 , C09K2211/1088 , C09K2211/188 , H01L51/009 , H01L51/0091
摘要： The invention provides compositions comprising copper(I) pyrazolate dimer compounds for use in OLEDs applications. The inventive compositions can be used to generate visible light colors or a color blend in electronic devices.

6. 发明授权

US09518040B2 GDF-8 inhibitors 有权
标题翻译： GDF-8抑制剂
公开(公告)号：US09518040B2
公开(公告)日：2016-12-13
申请号：US14833689
申请日：2015-08-24
申请人： Rigel Pharmaceuticals, Inc.
发明人： Somasekhar Bhamidipati , Marina Gelman , Pingyu Ding , Rajinder Singh , Jeffrey Clough , Todd Kinsella , Donald Payan
IPC分类号： C07D405/04 , C07D487/04 , C07D453/02 , C07D417/14 , C07D401/04 , C07F9/6503 , C07D417/04 , C07D471/04 , C07D405/14 , C07D401/14 , C07D213/26 , C07D498/04 , C07D413/04 , C07D513/04
CPC分类号： C07D401/04 , C07D213/26 , C07D401/14 , C07D405/04 , C07D405/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07F9/65038
摘要： Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.

7. 发明授权

US09273074B2 Formylpyrrole-based heterocycles for nucleic acid attachment to supports 有权
标题翻译：用于核酸附着于载体的甲酰基吡咯基杂环
公开(公告)号：US09273074B2
公开(公告)日：2016-03-01
申请号：US14512181
申请日：2014-10-10
申请人： Illumina, Inc.
发明人： Ryan Christopher Smith , Randall Smith , Xiaodong Zhao
IPC分类号： C07F9/6503 , C07F9/6506 , A61K31/675 , C07F9/572 , C07H21/00
CPC分类号： C07F9/5728 , A61K31/675 , C07F9/65031 , C07F9/6506 , C07H21/00
摘要： A compound has Formula I: A, B, C, D, W, X, Y, and Z are independently selected from hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 alkoxy, aryl, aldehyde, protected aldehyde, CH, N, O, S, null, and bond; Q is selected from aldehyde, protected aldehyde, and null, at least one of A, B, C, D, W, X, Y, Z, or Q is an aldehyde or protected aldehyde; the bonds between each of A-B, B-C, C-D, W-X, X-Y, and Y-Z are selected from single bond, double bond, triple bond, and no bond; L is a linker selected from a C1-C12 alkyl, aralkyl, and aryl, any of which is optionally substituted; one or more methylene unit (CH2) of the C1-C12 alkyl is optionally replaced by any combination of oxygen, carbonyl(C═O), and NH; and R1 and R2 are independently selected from —NR3R4, halogen, C1-C8 alkoxy, aralkoxy, alkenyloxy, alkynyloxy, and OCH2CH2CN; R3 and R4 are independently a C1-C4, straight chain or branched alkyl group.
摘要翻译：化合物具有式I：A，B，C，D，W，X，Y和Z独立地选自氢，任选取代的C 1 -C 6烷基，任选取代的C 1 -C 6烷氧基，芳基，醛，被保护的醛，CH ，N，O，S，无效和键; Q选自醛，被保护的醛，无效，A，B，C，D，W，X，Y，Z或Q中的至少一个是醛或被保护的醛; A-B，B-C，C-D，W-X，X-Y和Y-Z各自之间的键选自单键，双键，三键和无键; L是选自C 1 -C 12烷基，芳烷基和芳基，其中任何一个任选被取代的连接体; C1-C12烷基的一个或多个亚甲基单元（CH2）任选被氧，羰基（C = O）和NH的任何组合取代; 并且R 1和R 2独立地选自-NR 3 R 4，卤素，C 1 -C 8烷氧基，芳烷氧基，烯氧基，炔氧基和OCH 2 CH 2 CN; R 3和R 4独立地为C 1 -C 4直链或支链烷基。

8. 发明申请

US20160043332A1 MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES 审中-公开
标题翻译：有机电致发光器件材料
公开(公告)号：US20160043332A1
公开(公告)日：2016-02-11
申请号：US14456282
申请日：2014-08-11
申请人： Merck Patent GmbH
发明人： Harmut Yersin , Uwe Monkowius , Rafal Czerwieniec , Jiangbo Yu
IPC分类号： H01L51/00 , C07F9/6503
CPC分类号： H01L51/0091 , C07F9/5045 , C07F15/0033 , C07F15/0086 , H01L51/0037 , H01L51/0081 , H01L51/5016 , H01L2251/5384 , Y02E10/549 , Y02P70/521
摘要： The invention relates to mononuclear neutral copper(I) complexes with a bidentate ligand which is bonded via nitrogen and two phosphine or arsine ligands, to the use thereof for the production of electronic components, and to electronic devices comprising these complexes.
摘要翻译：本发明涉及与通过氮和两个膦或胂配体结合的双齿配体的单核中性铜（I）络合物，其用于生产电子元件的电子装置以及包含这些络合物的电子器件。

9. 发明授权

US09139604B2 Antiviral phosphonate analogs 有权
标题翻译：抗病毒膦酸酯类似物
公开(公告)号：US09139604B2
公开(公告)日：2015-09-22
申请号：US14309790
申请日：2014-06-19
申请人： Gilead Sciences, Inc.
发明人： Constantine G. Boojamra , Carina E. Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Maria Fardis , Haolun Jin , Ralph Hirschmann , Alan X. Huang , Choung U. Kim , Thorsten A. Kirschberg , Christopher P. Lee , William A. Lee , Richard L. Mackman , David Y. Markevitch , David A. Oare , Vidya K. Prasad , Hyung-Jung Pyun , Adrian S. Ray , Rosemarie O'Shea , Sundaramoorthi Swaminathan , William J. Watkins , Jennifer R. Zhang
IPC分类号： A61K31/44 , C07F9/6561 , A61K31/662 , A61K31/7072 , A61K31/7076 , A61K47/48 , C07D205/04 , C07D211/58 , C07D409/06 , C07D409/14 , C07D413/14 , C07D475/00 , C07F9/40 , C07F9/572 , C07F9/58 , C07F9/60 , C07F9/6503 , C07F9/6509 , C07F9/653 , C07F9/6539 , C07F9/655 , C07F9/6553 , C07H15/00 , C07H17/00 , C07H21/00 , C07H19/056 , C07H19/10 , C07H19/20
CPC分类号： C07F9/65616 , A61K31/662 , A61K31/7072 , A61K31/7076 , A61K47/548 , C07D205/04 , C07D211/58 , C07D409/06 , C07D409/14 , C07D413/14 , C07D475/00 , C07F9/4075 , C07F9/5728 , C07F9/58 , C07F9/60 , C07F9/65031 , C07F9/650905 , C07F9/653 , C07F9/6539 , C07F9/65515 , C07F9/655354 , C07F9/6561 , C07H15/00 , C07H17/00 , C07H19/056 , C07H19/10 , C07H19/20 , C07H21/00 , Y02A50/393 , Y02A50/465
摘要： The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译：本发明涉及具有抗病毒活性的磷取代的化合物，含有这些化合物的组合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

10. 发明授权

US09127028B2 Substrates for chromogenic detection and methods of use in detection assays and kits 有权
标题翻译：用于显色检测的底物和用于检测测定和试剂盒的方法
公开(公告)号：US09127028B2
公开(公告)日：2015-09-08
申请号：US13809354
申请日：2011-08-12
申请人： Brian Daniel Kelly , Christopher Bieniarz , Hiro Nitta , Fabien Gaire
发明人： Brian Daniel Kelly , Christopher Bieniarz , Hiro Nitta , Fabien Gaire
IPC分类号： C07F9/12 , C12Q1/70 , C07F9/6503 , G01N21/78
CPC分类号： C07F9/65031 , G01N21/78
摘要： Embodiments of substrates and processes for chromogenic detection, and in particular pyrazolyl dihydrogen phosphate compounds, are disclosed.
摘要翻译：公开了用于显色检测的底物和方法，特别是吡唑基二氢磷酸酯化合物的实施方案。

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