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1. 发明授权

US10618922B2 Biaryl ligands, methods of making biaryl ligands, and methods of use thereof 有权
公开(公告)号：US10618922B2
公开(公告)日：2020-04-14
申请号：US15927505
申请日：2018-03-21
申请人： University of Florida Research Foundation, Inc.
发明人： Aaron Aponick , Flavio S. P. Cardoso
IPC分类号： C07F7/02 , C07F9/6506 , C07D233/20 , B01J31/24 , C07C209/22 , C07C213/02 , C07D211/74 , C07F7/08
CPC分类号： C07F9/6506 , B01J31/2447 , C07C209/22 , C07C213/02 , C07D211/74 , C07D233/20 , C07F7/083 , B01J2231/766
摘要： Embodiments of the present disclosure provide for biaryl ligands (also referred to herein as “biaryl compound”), biaryl complexes, methods of making biaryl compounds, methods of making single enantiomers of these biaryl compounds, methods of use (e.g., catalysis), and the like.

2. 发明申请

US20180319743A1 TETRALIN AND INDANE DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：US20180319743A1
公开(公告)日：2018-11-08
申请号：US16033169
申请日：2018-07-11
申请人： Roche Palo Alto LLC
发明人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
IPC分类号： C07C317/32 , C07D233/58 , C07D277/82 , C07D239/42 , C07D239/14 , C07D235/06 , C07D233/90 , C07D233/88 , C07D233/84 , C07D233/64 , C07D233/54 , C07D233/48 , C07D233/34 , C07D233/20 , C07D231/18 , C07D209/30 , C07D207/36 , C07D207/34 , C07D207/325 , C07D207/16 , C07C317/44 , C07D233/44
CPC分类号： C07C317/32 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07D207/16 , C07D207/325 , C07D207/34 , C07D207/36 , C07D209/30 , C07D231/18 , C07D233/20 , C07D233/34 , C07D233/44 , C07D233/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D239/14 , C07D239/42 , C07D277/82
摘要： The applicaton discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, R1R5, R6 and R7 are as defined herein.

3. 发明授权

US09815793B2 Articles and methods comprising persistent carbenes and related compositions 有权
公开(公告)号：US09815793B2
公开(公告)日：2017-11-14
申请号：US15171998
申请日：2016-06-02
申请人： Massachusetts Institute of Technology
发明人： Jeremiah A. Johnson , Aleksandr V. Zhukhovitskiy
IPC分类号： C07D233/20 , C07D233/06 , C07D403/10 , C08F292/00 , C07D403/14
CPC分类号： C07D233/20 , C07D233/06 , C07D403/10 , C07D403/14 , C08F292/00
摘要： Articles and methods comprising persistent carbenes are provided, as well as related compositions. In some embodiments, a persistent carbene may be associated with a portion of a substrate (e.g., at least a portion of a surface on the substrate). In certain embodiments, the association of persistent carbene with the substrate may be used to affect certain properties of substrate (e.g., surface chemistry, stability). In some cases, a persistent carbene may be functionalized after association with a portion of a substrate. In some embodiments, a persistent carbene and at least one secondary compound may be associated with a portion of a substrate. Articles and methods of the present invention may be useful for applications involving electronics, sensing, microfabrication, nanotechnology, biomimetic, and drug delivery, amongst others.

4. 发明授权

US09309203B2 Malignant and non-malignant disease treatment with Ras antagonists 有权
标题翻译：恶性和非恶性疾病治疗与Ras拮抗剂
公开(公告)号：US09309203B2
公开(公告)日：2016-04-12
申请号：US14350303
申请日：2012-10-05
申请人： PISCES THERAPEUTICS, LLC
发明人： James H. Wikel , Michael J. Brownstein
IPC分类号： C07D233/20 , A61K31/41 , C07D239/06 , C07D257/04 , C07D285/06 , C07D333/38 , C07D333/40
CPC分类号： C07D239/06 , C07D233/20 , C07D257/04 , C07D285/06 , C07D333/38 , C07D333/40
摘要： The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition. The present disclosure also describes a method for inhibiting such Ras-induced or mediated cellular processes. The method entails administering a Ras antagonist in an amount effective to inhibit such cellular processes.
摘要翻译：本公开描述了用于治疗由Ras诱导或介导的细胞过程（包括细胞增殖，分化，凋亡，衰老和存活）引起的病症的新的抑制剂或拮抗剂。这些细胞过程可能与非恶性或恶性疾病，病症或病理状况相关。本公开还描述了抑制这种Ras诱导或介导的细胞过程的方法。该方法需要以有效抑制这种细胞过程的量施用Ras拮抗剂。

5. 发明申请

US20150126563A1 SMALL MOLECULE INHIBITORS OF THE PLECKSTRIN HOMOLOGY DOMAIN AND METHODS FOR USING SAME 有权
标题翻译：蛤K IN IN Y AME AME AME AME AME AME AME AME AME AME AME AME AME AME AME AME AME AME
公开(公告)号：US20150126563A1
公开(公告)日：2015-05-07
申请号：US14589360
申请日：2015-01-05
申请人： Board of Regents, The University of Texas System , Arizona Board of Regents on Behalf of the University of Arizona
发明人： Daruka MAHADEVAN , Emmanuelle J. MEUILLET , Eugene A. MASH, JR. , Vijay M. GOKHALE , Garth POWIS , Shuxing ZHANG
IPC分类号： A61K31/433
CPC分类号： A61K31/433 , C07C59/90 , C07C65/40 , C07C233/75 , C07C235/64 , C07C237/42 , C07C271/22 , C07C311/21 , C07C317/14 , C07C317/18 , C07C317/28 , C07C317/44 , C07C323/65 , C07D213/50 , C07D213/643 , C07D213/74 , C07D213/76 , C07D231/06 , C07D231/12 , C07D231/20 , C07D231/38 , C07D231/42 , C07D233/20 , C07D233/26 , C07D233/64 , C07D237/08 , C07D237/18 , C07D239/26 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/52 , C07D261/08 , C07D261/20 , C07D263/32 , C07D263/42 , C07D263/56 , C07D271/10 , C07D271/113 , C07D277/52 , C07D277/64 , C07D285/12 , C07D285/125 , C07D285/135 , C07D295/135 , C07D295/192 , C07D295/26 , C07D333/38 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/06 , C07D417/06 , C07D417/10 , C07D417/12 , C07F9/65583
摘要： Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.
摘要翻译：本文描述了Pleckstrin同源结构域结合化合物，包括这些化合物的药物组合物及其使用方法。

6. 发明申请

US20140275555A1 ARTICLES AND METHODS COMPRISING PERSISTENT CARBENES AND RELATED COMPOSITIONS 有权
标题翻译：包含耐久性碳和相关组合物的文章和方法
公开(公告)号：US20140275555A1
公开(公告)日：2014-09-18
申请号：US14210187
申请日：2014-03-13
申请人： Massachusetts Institute of Technology
发明人： Jeremiah A. Johnson , Aleksandr V. Zhukhovitskiy
IPC分类号： C07D233/20 , C07D403/10 , C07D403/14
CPC分类号： C07D233/20 , C07D233/06 , C07D403/10 , C07D403/14 , C08F292/00
摘要： Articles and methods comprising persistent carbenes are provided, as well as related compositions. In some embodiments, a persistent carbene may be associated with a portion of a substrate (e.g., at least a portion of a surface on the substrate). In certain embodiments, the association of persistent carbene with the substrate may be used to affect certain properties of substrate (e.g., surface chemistry, stability). In some cases, a persistent carbene may be functionalized after association with a portion of a substrate. In some embodiments, a persistent carbene and at least one secondary compound may be associated with a portion of a substrate. Articles and methods of the present invention may be useful for applications involving electronics, sensing, microfabrication, nanotechnology, biomimetic, and drug delivery, amongst others.
摘要翻译：提供了包含持续卡宾的制品和方法以及相关组合物。在一些实施方案中，持久卡宾可以与基底的一部分（例如，基底上的表面的至少一部分）相关联。在某些实施方案中，持久卡宾与底物的缔合可用于影响底物的某些性质（例如，表面化学，稳定性）。在一些情况下，持续卡宾可以在与一部分底物缔合后进行官能化。在一些实施方案中，持久卡宾和至少一种次级化合物可与底物的一部分缔合。本发明的制品和方法可用于涉及电子学，感测，微细加工，纳米技术，仿制和药物递送等应用。

7. 发明申请

US20130281709A1 PROCESS FOR PRODUCING ALPHA-HYDROXYKETONE COMPOUND 审中-公开
标题翻译：生产α-羟基酮酮化合物的方法
公开(公告)号：US20130281709A1
公开(公告)日：2013-10-24
申请号：US13979441
申请日：2012-01-27
申请人： Koji Hagiya
发明人： Koji Hagiya
IPC分类号： C07C319/20 , C07D233/20
CPC分类号： C07C319/20 , B01J31/0239 , B01J31/0244 , B01J2231/342 , C07C45/72 , C07C45/75 , C07D233/06 , C07D233/20 , C07C323/22 , C07C49/17 , C07C49/82
摘要： An object of the present invention is to produce an α-hydroxyketone compound easily and effectively. Provided is a process for producing an α-hydroxyketone compound comprising a stirring step of stirring one or more aldehyde compounds or polymers thereof in the presence of a base and an imidazolinium salt represented by the formula (1): wherein R1 and R2 each independently represent a hydrogen atom, an alkyl group optionally having a substituent or an aryl group optionally having a substituent, or R1 and R2 are bound to each other to form a ring together with carbon atoms to which they bind, R3 and R4 each independently represent an aryl group having one or more electron withdrawing groups, and X− represents an anion.
摘要翻译：本发明的目的是容易且有效地制备α-羟基酮化合物。提供一种制备α-羟基酮化合物的方法，其包括在碱和式（1）表示的咪唑啉鎓盐存在下搅拌一种或多种醛化合物或其聚合物的搅拌步骤：其中R1和R2各自独立地表示氢原子，任选具有取代基的烷基或任选具有取代基的芳基，或R 1和R 2彼此结合形成环，与它们所键合的碳原子一起形成环，R 3和R 4各自独立地表示芳基基团，具有一个或多个吸电子基团，X-表示阴离子。

8. 发明申请

US20120071506A1 METHODS FOR TREATING CNS DISORDERS WITH BICYCLO-SUBSTITUTED 2-IMIDAZOLINE AND 2-IMIDAZOLES 审中-公开
标题翻译：用双相取代的2-咪唑啉和2-咪唑烷处理CNS病症的方法
公开(公告)号：US20120071506A1
公开(公告)日：2012-03-22
申请号：US13303465
申请日：2011-11-23
申请人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
发明人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
IPC分类号： A61K31/4709 , A61K31/4178 , C07D401/04 , C07D401/06 , C07D405/04 , C07D233/60 , C07D233/58 , C07D233/20 , A61P25/20 , C07D233/06 , C07D233/24 , C07D405/06 , C07D233/22 , A61P25/24 , A61P25/22 , A61P25/18 , A61P25/00 , A61P25/16 , A61P25/28 , A61P25/08 , A61P25/06 , A61P9/12 , A61P25/30 , A61P3/00 , A61P3/10 , A61P3/04 , A61P3/06 , A61P43/00 , A61P9/00 , A61K31/4164
CPC分类号： C07D233/56 , A61K31/4166 , A61K31/4174 , A61K31/4709 , C07D233/06 , C07D233/20 , C07D233/22 , C07D233/64 , C07D401/04 , C07D401/06 , C07D405/04
摘要： The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification, and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms. The invention also relates to novel compounds of formula I, compositions containing them, and methods for their preparation.
摘要翻译：本发明涉及一种治疗选自抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，应激相关障碍，精神病性精神分裂症，神经性疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢紊乱，如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管其包括向个体施用治疗有效量的式I化合物，其中R 1，R 2，Q，W，X，Y，m和n如说明书中所定义，以及它们的药学活性盐，外消旋混合物，对映体，光学异构体和互变异构体。本发明还涉及式I的新化合物，含有它们的组合物及其制备方法。

9. 发明授权

US07741493B2 Heterocyclic compounds as P2X7 ion channel blockers 失效
标题翻译：杂环化合物作为P2X7离子通道阻断剂
公开(公告)号：US07741493B2
公开(公告)日：2010-06-22
申请号：US11947442
申请日：2007-11-29
申请人： Patrick Shum , Alexandre Gross , Liang Ma , Daniel G. McGarry , Gregory H. Merriman , David Rampe , Garth Ringheim , Jeffrey Stephen Sabol , Francis A. Volz
发明人： Patrick Shum , Alexandre Gross , Liang Ma , Daniel G. McGarry , Gregory H. Merriman , David Rampe , Garth Ringheim , Jeffrey Stephen Sabol , Francis A. Volz
IPC分类号： A61K31/4184 , C07D235/02
CPC分类号： C07D401/04 , C07D233/20 , C07D233/22 , C07D233/24 , C07D233/42 , C07D233/46 , C07D233/48 , C07D235/30 , C07D401/06 , C07D405/06 , C07D405/12 , C07D409/10
摘要： The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.
摘要翻译：本发明涉及式II的新一系列4,5-二苯基-2-氨基-4,5-二氢咪唑衍生物：其中R，R 1，R 2，R 3，R 4，R 5，X和Y为本文定义。本发明还涉及制备这些化合物的方法。本发明的化合物是P2X7离子通道阻断剂，因此可用作药剂，特别是用于治疗和/或预防各种具有炎症成分的疾病，包括炎性肠病，类风湿性关节炎和与中枢相关的疾病状况神经系统，如中风，阿尔茨海默病等

10. 发明申请

US20080293751A1 Tetralin and indane derivatives and uses thereof 有权
标题翻译：四氢萘啶和茚满衍生物及其用途
公开(公告)号：US20080293751A1
公开(公告)日：2008-11-27
申请号：US11985459
申请日：2007-11-15
申请人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
发明人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
IPC分类号： A61K31/505 , C07C211/01 , C07C257/00 , C07C279/02 , A61K31/155 , C07D235/04 , C07C275/04 , C07C311/01 , A61P25/00 , A61K31/18 , A61K31/17 , A61K31/4184 , A61K31/135 , C07D233/54 , A61K31/4164 , C07D239/24
CPC分类号： C07C317/32 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07D207/16 , C07D207/325 , C07D207/34 , C07D207/36 , C07D209/30 , C07D231/18 , C07D233/20 , C07D233/34 , C07D233/44 , C07D233/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D239/14 , C07D239/42 , C07D277/82
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
摘要翻译：式I化合物或其药学上可接受的盐，其中m，p，q，Ar，R 1和R 2如本文所定义。还提供了制备方法，组合物和使用式I化合物的方法。

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