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1. 发明申请

US20180265524A1 SMALL MOLECULES FOR THE MODULATION OF MCL-1 AND METHODS OF MODULATING CELL DEATH, CELL DIVISION, CELL DIFFERENTIATION AND METHODS OF TREATING DISORDERS 审中-公开
公开(公告)号：US20180265524A1
公开(公告)日：2018-09-20
申请号：US15968384
申请日：2018-05-01
申请人： Dana-Farber Cancer Institute, Inc.
发明人： Loren D. Walensky , Michelle L. Stewart , Nicole Cohen
IPC分类号： C07D513/04 , C07D417/04 , C07D403/08 , C07D409/14 , C07D409/06 , C07D405/14 , C07D409/12 , C07D279/06 , C07D413/06 , C07D401/12 , C07D277/34 , C07D403/06 , C07D307/54 , C07D249/12 , C07D413/14 , C07D405/12 , C07D327/04 , C07D239/60 , C07C311/20 , C07C337/08 , C07C251/84 , C07C335/16 , C07C251/20 , C07D403/04 , C07D417/14
CPC分类号： C07D513/04 , C07C251/20 , C07C251/84 , C07C311/20 , C07C335/16 , C07C337/08 , C07C2602/10 , C07D239/60 , C07D249/12 , C07D277/34 , C07D279/06 , C07D307/54 , C07D327/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14
摘要： This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.

2. 发明授权

US10011632B2 PSMA imaging agents 有权
公开(公告)号：US10011632B2
公开(公告)日：2018-07-03
申请号：US14917127
申请日：2012-08-21
申请人： Eric Wang , Hartmuth C. Kolb , Anna Katrin Szardenings , Changhui Liu , Joseph C. Walsh , Gang Chen , Anjana Sinha , Dhanalakshmi Kasi , Chul Yu , Umesh B. Gangadharmath , Wei Zhang , Tieming Zhao , Vani P. Mocharla
发明人： Eric Wang , Hartmuth C. Kolb , Anna Katrin Szardenings , Changhui Liu , Joseph C. Walsh , Gang Chen , Anjana Sinha , Dhanalakshmi Kasi , Chul Yu , Umesh B. Gangadharmath , Wei Zhang , Tieming Zhao , Vani P. Mocharla
IPC分类号： C07K5/02 , A61K51/04 , C07D249/06 , C07D249/04 , A61K51/08 , C07K5/062 , C07K5/072 , C07D403/12 , C07D213/81 , C07D213/82 , C07D233/78 , C07D233/96 , C07D401/12 , C07D403/06 , C07D405/12 , C07D239/60 , C07D251/30 , C07D263/34 , C07D207/16 , C07D277/56 , C07D209/48 , A61K38/00
CPC分类号： C07K5/0215 , A61K38/00 , A61K51/0402 , A61K51/0453 , A61K51/0497 , A61K51/088 , C07D207/16 , C07D209/48 , C07D213/81 , C07D213/82 , C07D233/78 , C07D233/96 , C07D239/60 , C07D249/04 , C07D249/06 , C07D251/30 , C07D263/34 , C07D277/56 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07K5/06026 , C07K5/06113
摘要： Compounds for targeting and agents for imaging, Prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

3. 发明申请

US20150315211A1 SMALL MOLECULES FOR THE MODULATION OF MCL-1 AND METHODS OF MODULATING CELL DEATH, CELL DIVISION, CELL DIFFERENTIATION AND METHODS OF TREATING DISORDERS 有权
标题翻译：用于调节MCL-1的小分子和调节细胞死亡，细胞分裂，细胞分化和治疗疾病的方法的方法
公开(公告)号：US20150315211A1
公开(公告)日：2015-11-05
申请号：US14705764
申请日：2015-05-06
申请人： Dana-Farber Cancer Institute, Inc.
发明人： Loren D. Walensky , Michelle L. Stewart , Nicole Cohen
IPC分类号： C07D513/04 , C07D409/12 , C07C311/20 , C07D409/14 , C07D401/12 , C07D413/14 , C07D405/14 , C07D417/14 , C07D307/54 , C07D405/12 , C07D409/06 , C07D413/06 , C07D279/06 , C07D327/04 , C07D239/60 , C07D403/06 , C07D277/34 , C07D417/04 , C07C337/08 , C07D249/12
CPC分类号： C07D513/04 , C07C251/20 , C07C251/84 , C07C311/20 , C07C335/16 , C07C337/08 , C07C2602/10 , C07D239/60 , C07D249/12 , C07D277/34 , C07D279/06 , C07D307/54 , C07D327/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14
摘要： This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.
摘要翻译：本发明涉及以高亲和性和选择性选择性结合生存蛋白MCL-1的化合物，含有这些化合物的药物组合物以及用于调节MCL-1活性和用于治疗过度增殖性疾病，血管生成障碍，细胞的这些化合物或组合物的用途循环调节障碍，自噬调节障碍，炎性疾病和/或感染性疾病和/或用于增强细胞移植和/或伤口修复，作为唯一的试剂或与其它活性成分组合。

4. 发明授权

US08877766B2 Neuroprotective multifunctional antioxidants and their monofunctional analogs 有权
标题翻译：神经保护多功能抗氧化剂及其单功能类似物
公开(公告)号：US08877766B2
公开(公告)日：2014-11-04
申请号：US13769247
申请日：2013-02-15
申请人： Peter F. Kador
发明人： Peter F. Kador
IPC分类号： C07D401/04 , C07D239/60 , A61K31/505 , C07D239/52 , C07D403/04 , C07D239/47 , C07D239/42
CPC分类号： C07D403/04 , C07D239/42 , C07D239/47 , C07D239/52 , C07D239/60 , C07D401/04
摘要： The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or —OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and —O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.
摘要翻译：神经保护性多功能抗氧化剂是含有2-二乙酰氨基-5-羟基嘧啶部分的化合物，其具有以下结构式：其中R1是CH2或C2H4; R2是H或-OR4，其中R4是H或芳基; R3a和R3b独立地选自H和-O-烷基。抗氧化剂是口服生物可利用的金属减弱多功能抗氧化剂，可以独立减弱过渡金属以及清道夫自由基。多功能抗氧化剂通过独立地螯合金属（如Fe，Cu或Zn）和清除不同来源产生的自由基的能力是神经保护性的，并且有益于治疗各种神经障碍，例如阿尔茨海默病，帕金森病，ALS，创伤性脑损伤，眼部疾病如白内障，青光眼，年龄相关性黄斑变性和其他视网膜变性，以及用于减少糖尿病并发症的进展。

5. 发明授权

US08710491B2 Forming agent for gate insulating film of thin film transistor 有权
标题翻译：薄膜晶体管栅绝缘膜成型剂
公开(公告)号：US08710491B2
公开(公告)日：2014-04-29
申请号：US13131807
申请日：2009-11-26
申请人： Shinichi Maeda , Takahiro Kishioka
发明人： Shinichi Maeda , Takahiro Kishioka
IPC分类号： H01L29/08 , H01L35/24 , H01L51/00 , H01L31/062 , H01L27/146
CPC分类号： H01L51/052 , C07D239/60 , C07D403/06 , H01L21/02118 , H01L21/02282 , H01L21/28194 , H01L21/312 , H01L51/0541 , H01L51/0545
摘要： It is an object to provide a novel forming agent for a gate insulating film that not only provides high insulating properties for the gate insulating film but also takes account of the electric characteristics of a thin film transistor element. A forming agent for a gate insulating film of a thin film transistor characterized by comprising an oligomer compound or a polymer compound including a structural unit containing a pyrimidinetrione ring having a hydroxyalkyl-containing group as a substituent on a nitrogen atom; a gate insulating film formed by the forming agent; and a thin film transistor.
摘要翻译：本发明的目的是提供一种用于栅极绝缘膜的新型成形剂，其不仅为栅极绝缘膜提供高绝缘性，而且还考虑了薄膜晶体管元件的电特性。一种薄膜晶体管的栅极绝缘膜的成型剂，其特征在于包含低聚物化合物或包含含有在氮原子上具有含羟基烷基的基团作为取代基的嘧啶四酮环的结构单元的高分子化合物; 由形成剂形成的栅极绝缘膜; 和薄膜晶体管。

6. 发明授权

US08557834B2 Prolyl hydroxylase inhibitors 有权
标题翻译：脯氨酰羟化酶抑制剂
公开(公告)号：US08557834B2
公开(公告)日：2013-10-15
申请号：US13667634
申请日：2012-11-02
申请人： GlaxoSmithKline LLC
发明人： Duke M. Fitch , Antony N. Shaw , Kenneth Wiggall
IPC分类号： C07D239/54 , A61K31/515
CPC分类号： C07D239/60 , A61K31/515 , C07D239/22 , C07D239/54 , C07D239/62 , C07D401/04 , C07D405/04 , C07D405/10 , C07D409/04 , C07D409/10 , C07D413/06 , C07D413/10 , C07D417/10
摘要： The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
摘要翻译：本文描述的本发明涉及作为HIF脯氨酰羟化酶的拮抗剂的式（I）的某些嘧啶四酮N-取代的甘氨酸衍生物，并且可用于治疗受益于该酶的抑制的疾病，贫血是一个示例。

7. 发明申请

US20120276651A1 FLUORESCENT NANOPROBE FOR DETECTING HYDROGEN PEROXIDE AND FABRICATION METHOD THEREOF 有权
标题翻译：用于检测过氧化氢的荧光纳米微粒及其制备方法
公开(公告)号：US20120276651A1
公开(公告)日：2012-11-01
申请号：US13362183
申请日：2012-01-31
申请人： Sehoon KIM , Ick Chan Kwon , Jai Kyeong Kim , Chang-Keun Lim , Jeongyun Heo
发明人： Sehoon KIM , Ick Chan Kwon , Jai Kyeong Kim , Chang-Keun Lim , Jeongyun Heo
IPC分类号： G01N21/64 , C07C65/05 , C07C255/53 , C07C309/73 , C07C69/732 , C07C49/248 , C07C49/573 , C07D403/10 , C07C69/88 , C07C255/57
CPC分类号： C07D239/60 , C07C39/373 , C07C47/565 , C07C49/248 , C07C49/747 , C07C69/732 , C07C69/94 , C07C255/36 , C07C255/40 , C07C255/41 , C07C309/73 , C07C317/46 , C07C2602/08 , C07D403/10 , Y10T436/206664
摘要： The present disclosure relates to a sulfonated benzene compound emitting fluorescence by reaction with hydrogen peroxide, aqueous-dispersed fluorescent nanoprobes applicable for real-time detection of hydrogen peroxide, and a fluorescent nanoprobe fabrication method. The fluorescent nanoprobe contains the following sulfonated benzene compound and water.
摘要翻译：本公开内容涉及通过与过氧化氢反应发射荧光的磺化苯化合物，适用于过氧化氢的实时检测的水分散荧光纳米探针和荧光纳米探针制造方法。荧光纳米探针含有以下磺化苯化合物和水。

8. 发明申请

US20120059163A1 Non-linear opticaly active molecules, their synthesis, and use 审中-公开
标题翻译：非线性光学活性分子，它们的合成和用途
公开(公告)号：US20120059163A1
公开(公告)日：2012-03-08
申请号：US13290518
申请日：2011-11-07
申请人： Vincent D. McGinniss , Steven M. Risser , Elizabeth Drotleff , Edward Jiang , Kevin B. Spahr
发明人： Vincent D. McGinniss , Steven M. Risser , Elizabeth Drotleff , Edward Jiang , Kevin B. Spahr
IPC分类号： C07D417/04 , C07D261/12 , C07D231/44 , C07C15/12 , C07C255/42 , C07C229/44 , C07C211/45 , C07C15/18 , C07D239/60 , C07D231/08
CPC分类号： C07D231/08 , C07C13/28 , C07C15/52 , C07C211/45 , C07C255/31 , C07C255/42 , C07C271/28 , C07C2601/06 , C07D231/44 , C07D239/60 , C07D261/12 , C07D417/04
摘要： In one aspect, the present invention provides a hyperpolarizable organic chromophore. The chromophore is a nonlinear optically active compound that includes a π-donor conjugated to a π-acceptor through a π-electron conjugated bridge. In other aspects of the invention, donor structures and acceptor structures are provided. In another aspect of the invention, a chromophore-containing polymer is provided. In one embodiment, the chromophore is physically incorporated into the polymer to provide a composite. In another embodiment, the chromophore is covalently bonded to the polymer, either as a side chain polymer or through crosslinking into the polymer. In other aspects, the present invention also provides a method for making the chromophore, a method for making the chromophore-containing polymer, and methods for using the chromophore and chromophore-containing polymer.
摘要翻译：一方面，本发明提供了一种超极化有机发色团。发色团是一种非线性光学活性化合物，其包括通过电解质共轭桥缀合至受体的受体。在本发明的其它方面，提供了供体结构和受体结构。在本发明的另一方面，提供含发色团的聚合物。在一个实施方案中，发色团物理地掺入聚合物中以提供复合物。在另一个实施方案中，发色团与聚合物共价结合，作为侧链聚合物或通过交联进入聚合物。在其它方面，本发明还提供了一种制备发色团的方法，一种制备含发色团的聚合物的方法，以及使用含发色团和含发色团的聚合物的方法。

9. 发明申请

US20110263623A1 PROCESS FOR PREPARATION OF BOSENTAN 审中-公开
标题翻译： BOSENTAN的制备方法
公开(公告)号：US20110263623A1
公开(公告)日：2011-10-27
申请号：US13058285
申请日：2009-08-07
申请人： Kaushilk Sata , Bipin Pandey
发明人： Kaushilk Sata , Bipin Pandey
IPC分类号： A61K31/513 , A61P9/12 , C07D403/04
CPC分类号： C07D239/69 , C07D239/60
摘要： The present invention provides improved processes for preparing Bosentan. The present invention provides novel intermediates like 4,6-dihydroxy-5-(2-methoxy phenoxy)[2,2′]bipyrimidine of formula (II) and N-(6-Chloro-5-(2-ethoxyphenoxy)[2,2′-bipyrimidinyl]-4-t-butyl benzenesulfonamide cesium salt and process for preparation thereof. The invention also disclosed novel polymorphic form of the intermediates.
摘要翻译：本发明提供了制备波生坦的改进方法。本发明提供新的中间体如式（II）的4,6-二羟基-5-（2-甲氧基苯氧基）[2,2']联嘧啶和N-（6-氯-5-（2-乙氧基苯氧基）[2 ，2'-联嘧啶基] -4-叔丁基苯磺酰胺铯盐及其制备方法，本发明还公开了中间体的新型多晶型物。

10. 发明申请

US20110076276A1 Novel HIV reverse transcriptase inhibitors 有权
标题翻译：新型HIV逆转录酶抑制剂
公开(公告)号：US20110076276A1
公开(公告)日：2011-03-31
申请号：US12215450
申请日：2008-06-26
申请人： Hongyan Guo , Choung U. Kim , Ill Y. Lee , Michael L. Mitchell , Gerry Rhodes , Jong C. Son , Lianhong Xu
发明人： Hongyan Guo , Choung U. Kim , Ill Y. Lee , Michael L. Mitchell , Gerry Rhodes , Jong C. Son , Lianhong Xu
IPC分类号： A61K39/395 , C07D239/24 , A61K31/505 , A61K31/496 , A61K31/536 , A61K31/551 , A61P31/18 , A61K31/7072 , A61K31/7064 , A61K31/7076 , A61K31/66 , A61K38/16
CPC分类号： A61K31/513 , A61K31/496 , A61K31/536 , A61K31/551 , A61K31/66 , A61K31/7048 , A61K31/7072 , A61K31/708 , A61K39/39558 , A61K45/06 , C07D239/54 , C07D239/545 , C07D239/553 , C07D239/60 , C07D401/04 , C07D403/04
摘要： The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物，酯和/或膦酸盐，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法。

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