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1. 发明申请

US20180037539A1 COMPOSITIONS FOR THE TREATMENT OF KIDNEY AND/OR LIVER DISEASE 审中-公开
公开(公告)号：US20180037539A1
公开(公告)日：2018-02-08
申请号：US15558155
申请日：2016-03-18
申请人： VECTUS BIOSYSTEMS LIMITED
发明人： Karen Annette DUGGAN
IPC分类号： C07C235/34 , C07H15/203 , C07D231/12 , C07D333/24 , C07C237/20 , C07D213/56
CPC分类号： C07C235/34 , C07C237/20 , C07D207/327 , C07D213/56 , C07D231/12 , C07D239/26 , C07D261/08 , C07D277/30 , C07D307/54 , C07D333/24 , C07H15/203
摘要： The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of kidney and/or liver disease.

2. 发明授权

US09796640B2 Method for producing optically active carboxylic acid ester 有权
公开(公告)号：US09796640B2
公开(公告)日：2017-10-24
申请号：US15115764
申请日：2015-02-02
申请人： TOKYO UNIVERSITY OF SCIENCE FOUNDATION
发明人： Isamu Shiina
IPC分类号： C07B53/00 , C07C269/06 , C07D235/06 , C07D403/06 , C07D471/04 , C07D263/58 , C07D207/27 , C07C271/22 , C07B55/00 , C07D207/327 , C07D207/333 , C07D207/416 , C07D209/08 , C07D209/12 , C07D209/34 , C07D209/38 , C07D513/04 , C07D209/48 , C07D209/86 , C07D207/34
CPC分类号： C07B53/00 , C07B55/00 , C07B2200/07 , C07C269/06 , C07D207/27 , C07D207/327 , C07D207/333 , C07D207/34 , C07D207/416 , C07D209/08 , C07D209/12 , C07D209/34 , C07D209/38 , C07D209/48 , C07D209/86 , C07D235/06 , C07D263/58 , C07D403/06 , C07D471/04 , C07D513/04 , C07C271/22
摘要： Provided is a method for producing an optically active carboxylic acid ester at a high yield and with high enantioselectivity using dynamic kinetic resolution, said optically active carboxylic acid ester having an α-nitrogen substituent. This method for producing an optically active carboxylic acid ester includes a step in which racemic carboxylic acid represented by formula (a) and a specific alcohol or phenol derivative are reacted in a polar solvent having a dipole moment of at least 3.5 in the presence of an acid anhydride and an asymmetric catalyst, one enantiomer of the racemic carboxylic acid is selectively esterified, and the other enantiomer is racemized. In formula (a), Ra1 represents a nitrogen-containing heteroaromatic ring group bonded to an assymetric carbon via a nitrogen atom constituting a ring, and Ra2 is an organic group.

3. 发明授权

US09758514B2 Modulators of calcium release-activated calcium channel 有权
公开(公告)号：US09758514B2
公开(公告)日：2017-09-12
申请号：US14539470
申请日：2014-11-12
申请人： Rhizen Pharmaceuticals SA
发明人： Meyyappan Muthuppalaniappan , Srikant Viswanadha , Gayatri S. Merikapudi , Swaroop K. Vakkalanka
IPC分类号： C07D417/10 , C07D401/10 , C07D401/12 , C07D403/10 , A61K45/06 , A61K31/427 , A61K31/422 , A61K31/415 , A61K31/433 , A61K31/5377 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D207/327 , C07D413/10 , A61K31/4439 , A61K31/455 , A61K31/496 , A61K31/506 , C07D207/337 , C07D295/195 , C12N5/078
CPC分类号： C07D417/10 , A61K31/415 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/455 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D207/327 , C07D207/337 , C07D231/12 , C07D295/195 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C12N5/0634 , C12N2500/46 , Y02A50/422
摘要： Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.

4. 发明申请

US20170128434A1 NOVEL ESTROGEN RECEPTOR LIGANDS 审中-公开
公开(公告)号：US20170128434A1
公开(公告)日：2017-05-11
申请号：US15407497
申请日：2017-01-17
申请人： Karo Pharma AB
发明人： Aiping Cheng , Neeraj Garg , Lars Krüger , Joakim Löfstedt , Eva Koch , Konrad Koehler , Lars Hagberg , Daniel Nöteberg
IPC分类号： A61K31/472 , A61K31/42 , A61K31/155 , A61K31/165 , A61K31/341 , A61K31/47 , A61K31/343 , A61K31/416 , A61K31/4418 , A61K31/402 , A61K31/415 , A61K31/44 , A61K31/404 , A61K31/365 , A61K31/277 , A61K31/4192 , A61K31/381
CPC分类号： A61K31/472 , A61K31/155 , A61K31/165 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/365 , A61K31/381 , A61K31/402 , A61K31/404 , A61K31/415 , A61K31/416 , A61K31/4192 , A61K31/42 , A61K31/44 , A61K31/4418 , A61K31/47 , C07C209/68 , C07C251/48 , C07D207/327 , C07D213/58 , C07D215/12 , C07D215/14 , C07D217/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D235/16 , C07D261/08 , C07D277/30 , C07D277/34 , C07D295/155 , C07D307/54 , C07D307/68 , C07D307/87 , C07D317/60 , C07D333/20 , C07D333/24 , C07D409/10 , C07D413/10 , C07C211/65
摘要： Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.

5. 发明申请

US20170008820A1 METHOD FOR PRODUCING OPTICALLY ACTIVE CARBOXYLIC ACID ESTER 有权
标题翻译：生产光活性羧酸酯的方法
公开(公告)号：US20170008820A1
公开(公告)日：2017-01-12
申请号：US15115764
申请日：2015-02-02
申请人： TOKYO UNIVERSITY OF SCIENCE FOUNDATION
发明人： Isamu SHIINA
IPC分类号： C07B53/00 , C07C269/06 , C07D209/48 , C07D209/34 , C07D209/38 , C07B55/00 , C07D207/327 , C07D209/08 , C07D235/06 , C07D209/86 , C07D207/34 , C07D263/58 , C07D207/27
CPC分类号： C07B53/00 , C07B55/00 , C07B2200/07 , C07C269/06 , C07D207/27 , C07D207/327 , C07D207/333 , C07D207/34 , C07D207/416 , C07D209/08 , C07D209/12 , C07D209/34 , C07D209/38 , C07D209/48 , C07D209/86 , C07D235/06 , C07D263/58 , C07D403/06 , C07D471/04 , C07D513/04 , C07C271/22
摘要： Provided is a method for producing an optically active carboxylic acid ester at a high yield and with high enantioselectivity using dynamic kinetic resolution, said optically active carboxylic acid ester having an α-nitrogen substituent. This method for producing an optically active carboxylic acid ester includes a step in which racemic carboxylic acid represented by formula (a) and a specific alcohol or phenol derivative are reacted in a polar solvent having a dipole moment of at least 3.5 in the presence of an acid anhydride and an asymmetric catalyst, one enantiomer of the racemic carboxylic acid is selectively esterified, and the other enantiomer is racemized. In formula (a), Ra1 represents a nitrogen-containing heteroaromatic ring group bonded to an assymetric carbon via a nitrogen atom constituting a ring, and Ra2 is an organic group.
摘要翻译：提供了一种使用动态动力学拆分制备光学活性羧酸酯的高产率和高对映体选择性的方法，所述光学活性羧酸酯具有α-氮取代基。该光学活性羧酸酯的制造方法包括使式（a）表示的外消旋羧酸和特定的醇或苯酚衍生物在偶极矩为3.5以下的极性溶剂中，在酸酐和不对称催化剂，外消旋羧酸的一种对映异构体被选择性酯化，另一种对映体被外消旋化。在式（a）中，Ra 1表示通过构成环的氮原子键合到比例碳上的含氮杂芳环，Ra2是有机基。

6. 发明授权

US09498466B2 Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents 有权
公开(公告)号：US09498466B2
公开(公告)日：2016-11-22
申请号：US14922928
申请日：2015-10-26
申请人： Nivalis Therapeutics, Inc.
发明人： Jan Wasley , Gary J. Rosenthal , Xicheng Sun , Sarah Strong , Jian Qiu
IPC分类号： A61K31/4178 , A61K31/4025 , A61K31/40 , C07D207/327 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/14 , C07D207/337 , A61K31/402
CPC分类号： A61K31/4178 , A61K31/40 , A61K31/402 , A61K31/4025 , C07D207/327 , C07D207/337 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/14
摘要： The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

7. 发明申请

US20160244407A1 ARYLOYL(OXY OR AMINO)PENTAFLUOROSULFANYLBENZENE COMPOUND, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PRODRUGS THEREOF 有权
标题翻译：芳香族（OXY或AMINO）PENTAFLUOROSULFANYLENZENE化合物，药物接受盐及其制剂
公开(公告)号：US20160244407A1
公开(公告)日：2016-08-25
申请号：US15032015
申请日：2014-11-04
申请人： UBE INDUSTRIES, LTD.
发明人： Shigeyoshi NISHINO , Hidetaka SHIMA , Hiroyuki ODA , Tetsuro SHIMANO
IPC分类号： C07C381/00 , C07D307/68 , C07D213/81 , C07D213/82 , C07D239/34 , C07D239/28 , C07D311/16 , C07D233/90 , C07D241/24 , C07D207/327 , C07D263/34 , C07D207/34 , C07D231/12 , C07D231/14 , C07D333/38 , C07D237/24 , C07D277/56 , C07D317/60
CPC分类号： C07C381/00 , A61K31/167 , A61K31/216 , A61K31/36 , C07D207/327 , C07D207/34 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/14 , C07D233/90 , C07D237/24 , C07D239/28 , C07D239/34 , C07D241/24 , C07D263/34 , C07D277/56 , C07D307/68 , C07D311/16 , C07D317/60 , C07D333/38
摘要： An aryloyl(oxy or amino)pentafluorosulfanylbenzene compound having pharmacological action. The aryloyl(oxy or amino)pentafluorosulfanylbenzene compound is represented by general formula (A-I), a pharmaceutically acceptable salt thereof, and a prodrug thereof, wherein all of parameters represent the same meanings as defined in the specification.
摘要翻译：具有药理作用的芳基（氧基或氨基）五氟硫烷基苯化合物。芳氧基（氧基或氨基）五氟硫烷基苯化合物由通式（A-I）表示，其药学上可接受的盐及其前药，其中所有参数表示与说明书中所定义的相同含义。

8. 发明授权

US08946682B2 Donor-acceptor fluorene scaffolds: a process and uses thereof 有权
标题翻译：供体受体芴支架：其过程和用途
公开(公告)号：US08946682B2
公开(公告)日：2015-02-03
申请号：US12894428
申请日：2010-09-30
申请人： Atul Goel , Sumit Chaurasia , Vijay Kumar , Sundar Manoharan , R. S. Anand
发明人： Atul Goel , Sumit Chaurasia , Vijay Kumar , Sundar Manoharan , R. S. Anand
IPC分类号： H01L29/08 , C07D295/155 , C07D207/327 , C07D211/14 , C07D307/54 , C07D333/24 , H01L51/00
CPC分类号： C07D295/155 , C07D207/327 , C07D211/14 , C07D307/54 , C07D333/24 , H01L51/0058 , Y02E10/549 , Y02P70/521
摘要： The present invention relates to novel donor-acceptor fluorene compounds, which can be used as for the fabrication of electroluminescent devices, and a process of preparing said novel compounds. More particularly, the present invention relates to amine donor and nitrile/ester acceptor fluorenes, fluorenones their π-conjugated systems and related compounds, processes for preparing the said compounds including oxidation of fluorenes to corresponding fluorenones and their use in preparing organic electronic devices such as organic light emitting diodes (OLEDs), photovoltaic/solar cell, Field effect transistors and other useful electroluminescent devices. The compounds are prepared by reacting 2H-pyran-2-ones in isolated or rigid conformations with cyclic ketones containing methylene carbonyl moiety in the presence of a base in an organic solvent. The present invention also relates to a new concept and approach to overcome the problem of ‘Green emission defect’ in 9-unsubstituted fluorene-based organic light emitting diodes which occurs due to the conversion of fluorenes to fluorenones that show emission mainly in green-yellow region. In the present invention we have placed donor-acceptor substituents in such a way that donor-acceptor fluorenones show emission in the blue region (instead of green-yellow region) thus improving the blue color purity and overcoming the problem of green emission defect.
摘要翻译：本发明涉及可用于制造电致发光器件的新型供体 - 受体芴化合物，以及制备所述新型化合物的方法。更具体地，本发明涉及胺供体和腈/酯受体芴，芴酮及其共轭体系和相关化合物，制备所述化合物的方法，包括将芴氧化成相应的芴酮及其在制备有机电子器件中的用途，作为有机发光二极管（OLED），光伏/太阳能电池，场效应晶体管等有用的电致发光器件。通过在有机溶剂中的碱存在下，将分离或刚性构象中的2H-吡喃-2-酮与含有亚甲基羰基部分的环酮反应制备化合物。本发明还涉及克服9-未取代的基于芴的有机发光二极管中由于将芴转化为芴酮而发生的“绿色发光缺陷”的新概念和方法，其显示主要以绿黄色地区。在本发明中，我们以供体 - 受体芴酮在蓝色区域（而不是绿 - 黄色区域）中显示发射的方式放置了供体 - 受体取代基，从而提高了蓝色纯度并克服了绿色发光缺陷的问题。

9. 发明授权

US08778628B2 Arylalkylamine compound and process for preparing the same 有权
标题翻译：芳烷基胺化合物及其制备方法
公开(公告)号：US08778628B2
公开(公告)日：2014-07-15
申请号：US13919829
申请日：2013-06-17
申请人： Mitsubishi Tanabe Pharma Corporation
发明人： Hiroshi Miyazaki , Junko Okabe , Kosuke Yasuda , Iwao Takamuro , Osamu Sakurai , Tetsuya Yanagida , Yutaka Hisada
IPC分类号： C07D205/04 , C07D207/14 , C07D207/16 , C07D207/27 , C07D207/327 , C07D207/335 , C07D207/34 , C07D211/56 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D405/12 , C07D409/06 , C07D409/12 , C07D417/04 , C07D417/06
CPC分类号： C07D207/14 , C07D205/04 , C07D207/16 , C07D207/27 , C07D207/327 , C07D207/335 , C07D207/34 , C07D211/56 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D405/12 , C07D409/06 , C07D409/12 , C07D417/04 , C07D417/06 , C07H17/02
摘要： An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
摘要翻译：芳基烷基胺化合物由下式[I-e]表示或其药学上可接受的盐。

10. 发明申请

US20140194425A1 Novel Pyrrole Inhibitors of S-Nitrosoglutathione Reductase as Therapeutic Agents 有权
公开(公告)号：US20140194425A1
公开(公告)日：2014-07-10
申请号：US14204849
申请日：2014-03-11
申请人： N30 Pharmaceuticals, Inc.
发明人： Jan Wasley , Gary J. Rosenthal , Xicheng Sun , Sarah Strong , Jian Qiu
IPC分类号： C07D207/337 , C07D401/14 , C07D401/04 , C07D417/04 , C07D413/10 , C07D417/14 , C07D409/04 , C07D409/14 , C07D405/04 , C07D405/12 , C07D403/14 , C07D403/04 , C07D403/10
CPC分类号： A61K31/4178 , A61K31/40 , A61K31/402 , A61K31/4025 , C07D207/327 , C07D207/337 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/14
摘要： The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

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