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1. 发明申请

US20110230464A1 PURINE DERIVATIVES USEFUL AS P13 KINASE INHIBITORS 审中-公开
标题翻译：嘌呤衍生物作为P13激酶抑制剂有用
公开(公告)号：US20110230464A1
公开(公告)日：2011-09-22
申请号：US12739437
申请日：2008-10-27
申请人： Paul Goldsmith , Timothy Colin Hancox , Nei Anthony Pegg , Janusz Josef Kulagowski , Alan John Nadin , Stephen Price
发明人： Paul Goldsmith , Timothy Colin Hancox , Nei Anthony Pegg , Janusz Josef Kulagowski , Alan John Nadin , Stephen Price
IPC分类号： A61K31/5377 , C07D473/34 , C07D487/04 , C07D498/04 , A61K31/5383 , A61K31/541 , A61P35/00 , A61P37/00 , A61P9/00 , A61P29/00 , A61P3/00 , A61P5/00 , A61P25/00 , A61P31/12
CPC分类号： C07D473/34 , C07D471/10 , C07D498/04 , C07D498/08 , C07D498/10 , C07D519/00
摘要： This invention provides a compound which is a purine of formula (Ia) or (Ib): and the pharmaceutically acceptable salts thereof that are inhibitors of PI3K and a selective for the p110δ isoform, which is a class Ia PI3 kinase, over other class Ia PI3 kinases and over class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：本发明提供一种化合物，其为式（Ia）或（Ib）的嘌呤：及其药学上可接受的盐，其为PI3K的抑制剂，并且对于与其它Ia类相比为Ia类PI3激酶的p110δ同种型 PI3激酶和1b类激酶。该化合物可用于治疗与PI3激酶相关的异常细胞生长，功能或行为引起的疾病和障碍，例如癌症免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍。

2. 发明申请

US20060193776A1 Screening methods employing zebrafish and the blood brain barrier 审中-公开
标题翻译：使用斑马鱼和血脑屏障的筛选方法
公开(公告)号：US20060193776A1
公开(公告)日：2006-08-31
申请号：US10566888
申请日：2005-02-17
申请人： Paul Goldsmith , Angeleen Fleming
发明人： Paul Goldsmith , Angeleen Fleming
IPC分类号： A61K49/00
CPC分类号： G01N33/5088
摘要： Use of fish, in particular zebrafish, in screening for substances with an ophthalmological effect or biological effect on the brain or central nervous system and/or effect on a disease or disorder of the brain or central nervous system. Based on identification and characterisation of the blood brain barrier.
摘要翻译：使用鱼类，特别是斑马鱼，筛选具有眼睛作用或对脑或中枢神经系统的生物学作用的物质和/或对脑或中枢神经系统的疾病或病症的影响。基于血脑屏障的识别和表征。

3. 发明申请

US20060150259A1 Model of bone disease amenable to high-throughput screening 审中-公开
标题翻译：骨病模型适合高通量筛查
公开(公告)号：US20060150259A1
公开(公告)日：2006-07-06
申请号：US10544001
申请日：2004-01-28
申请人： Paul Goldsmith , Angeleen Fleming
发明人： Paul Goldsmith , Angeleen Fleming
IPC分类号： A61K49/00 , A01K67/027
CPC分类号： G01N33/6893 , G01N33/5088 , G01N33/6887 , G01N2500/10 , G01N2800/108
摘要： Model fish and use thereof for screening for agents and genetic suppressors to treat bone disease or disorders, especially in zebrafish. Induction of a disease state and visualization of the skeleton in living zebrafish. Visualization of the skeleton in vivo facilitates screening for compounds that can be used in treatment of bone disease or genetic mutations that rescue or suppress the disease phenotype.
摘要翻译：模型鱼及其用于筛选用于治疗骨疾病或遗传抑制剂的药剂和遗传抑制剂，特别是在斑马鱼中。感染斑马鱼的疾病状态和骨骼的可视化。骨骼在体内的可视化有助于筛选可用于治疗骨疾病的化合物或挽救或抑制疾病表型的遗传突变。

4. 发明授权

US08399690B2 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene compounds 有权
标题翻译： 4,5-二氢-6-氧杂-3-硫杂-1-氮杂 - 苯并[e]薁化合物
公开(公告)号：US08399690B2
公开(公告)日：2013-03-19
申请号：US13018068
申请日：2011-01-31
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： C07D313/00 , C07D333/00
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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和II的苯并吡喃和苯并辛菌素化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症由脂质激酶介导。公开了使用式I和II的化合物在体外，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。

5. 发明申请

US20050015823A1 Screening methods employing fish model assessment of vision 审中-公开
标题翻译：使用鱼模型评估视力的筛选方法
公开(公告)号：US20050015823A1
公开(公告)日：2005-01-20
申请号：US10497023
申请日：2002-12-02
申请人： Paul Goldsmith
发明人： Paul Goldsmith
IPC分类号： A01K67/027 , C12N15/09 , C12N15/85 , C12Q1/68 , G01N33/15 , G01N33/50
CPC分类号： C12N15/8509 , A01K67/0275 , A01K2217/05 , A01K2217/20 , A01K2227/105 , A01K2227/40 , A01K2267/0306 , A01K2267/0318 , A01K2267/0356 , A01K2267/0393
摘要： Screening Methods Employing Fish Model Assessment of Vision Fish such as zebrafish are provided and used in a suppressor screen or other screen to identify a gene or test substance that affects activity or effect of a second gene provided transgenically that affects vision of the fish, or a treatment of the fish that affects vision. Vision of model fish is compared with vision of mutated or treated fish, allowing for identification of genes and test substances with therapeutic application.
摘要翻译：筛选方法采用鱼类模型评估视力提供斑马鱼等鱼类，并在抑制筛网或其他筛选中使用，以鉴定影响转基因而影响鱼类视力的第二基因的活性或作用的基因或试验物质，或治疗影响视力的鱼类。模型鱼的愿景与突变或处理的鱼的视力进行比较，允许用治疗应用鉴定基因和测试物质。

6. 发明授权

US5113387A Three laser optical disk drive system 失效
标题翻译：三激光光盘驱动系统
公开(公告)号：US5113387A
公开(公告)日：1992-05-12
申请号：US449002
申请日：1989-12-12
申请人： Paul Goldsmith , William R. A. Ziegler
发明人： Paul Goldsmith , William R. A. Ziegler
IPC分类号： G11B7/00 , G11B7/004 , G11B7/0045 , G11B7/0055 , G11B7/095 , G11B7/127 , G11B7/13 , G11B7/24 , G11B7/30
CPC分类号： G11B7/127 , G11B7/004 , G11B7/13 , G11B7/24
摘要： An erasable optical disk drive system is disclosed which utilizes an electron trapping media coated on the disk surface to store data in the form of light energy and which utilizes three laser beams, each having a wavelength range distinct from each other as well as distinct from the wavelength range of the emission produced by the impingement of the read laser onto the electron trapping media. Data is written onto the disk, which is contained in a light-tight contamination-free environment, using a visible light laser beam. Data is read from the disk and the disk is erased by using a near infrared light laser beam. The focus and tracking functions of the disk drive system are accomplished by using a laser beam having yet another range of wavelengths, which are greater than those of the visible light laser beam and those of the photon emission from the electron trapping optical memory media, but less than those of the read/erase laser.
摘要翻译：公开了一种可擦除光盘驱动系统，其利用涂覆在盘表面上的电子捕获介质以光能的形式存储数据，并且利用三个激光束，每个激光束具有彼此不同的波长范围，通过将读取的激光撞击到电子俘获介质上产生的发射的波长范围。使用可见光激光束将数据写入包含在不透光的环境中的光盘上。从磁盘读取数据，并通过使用近红外光激光束擦除磁盘。磁盘驱动系统的聚焦和跟踪功能是通过使用具有大于可见光激光束的另一波长范围的激光束和来自电子捕获光存储介质的光子发射的激光束来实现的，但是小于读取/擦除激光器的数量。

7. 发明申请

US20120316213A1 COMBINATION OF ALPHA-2 RECEPTOR AGONIST (CLONIDIN) AND ANTI-MUSCARINIC AGENT (OXYBUTYNIN) FOR THE TREATMENT OF SIALORRHOEA 失效
标题翻译： ALPHA-2受体激动剂（CLONIDINE）和抗精神病药（OXYBUTYNIN）的组合用于治疗腹泻
公开(公告)号：US20120316213A1
公开(公告)日：2012-12-13
申请号：US13593173
申请日：2012-08-23
申请人： Alan Geoffrey Roach , Paul Goldsmith
发明人： Alan Geoffrey Roach , Paul Goldsmith
IPC分类号： A61K31/4168 , A61P7/00
CPC分类号： A61K31/216 , A61K9/0053 , A61K9/006 , A61K31/415 , A61K45/06 , A61K2300/00
摘要： An alpha2 adrenoreceptor agonist eg. clonidine, brimonidine, monoxidine, lofexidine is useful for the treatment of siaiorrhoea, administered by the paraungual, sublingual or buccal route. The patient to be treated is also given an anti-muscarinic agent eg. oxybutynin, glycopyrrolate, ipratropium.
摘要翻译： α2肾上腺素受体激动剂，例如可乐定，溴莫尼定，单恶唑，洛非昔定可用于治疗由腹膜，舌下或口腔途径给药的双侧眼。待治疗的患者也被给予抗毒蕈碱剂，例如。奥昔布宁，格隆溴铵，异丙托铵。

8. 发明授权

US07928248B2 Benzopyran and benzoxepin PI3K inhibitor compounds and methods of use 有权
标题翻译：苯并吡喃和苯并辛菌素PI3K抑制剂化合物及其使用方法
公开(公告)号：US07928248B2
公开(公告)日：2011-04-19
申请号：US12414403
申请日：2009-03-30
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： C07D333/00
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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和II的苯并吡喃和苯并辛菌素化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症由脂质激酶介导。公开了使用式I和II的化合物在体外，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。

9. 发明申请

US20100298282A1 Treatment of Ocular Conditions and the Side-Effects of Glucocorticoids 审中-公开
标题翻译：治疗眼病和副作用糖皮质激素
公开(公告)号：US20100298282A1
公开(公告)日：2010-11-25
申请号：US12161413
申请日：2007-01-19
申请人： Alan Geoffrey Roach , Paul Goldsmith , Ruth Margaret Barrett
发明人： Alan Geoffrey Roach , Paul Goldsmith , Ruth Margaret Barrett
IPC分类号： A61K31/575 , A61P27/06 , A61P27/12 , A61P9/12 , A61P27/02
CPC分类号： A61K31/56 , A61K31/00
摘要： A compound having glucocorticoid receptor (GR) antagonist activity and a clogP value of less than 5 is useful for the treatment of an ocular condition. Further, a compound having glucocorticoid receptor (GR) antagonist activity is useful, for the treatment of a patient exhibiting side-effects of the administration of a glucocorticosteroid, e.g. wherein the glucocorticosteroid and said compound are administered by different routes.
摘要翻译：具有糖皮质激素受体（GR）拮抗剂活性和小于5的clogP值的化合物可用于治疗眼部病症。此外，具有糖皮质激素受体（GR）拮抗剂活性的化合物可用于治疗显示给予糖皮质激素的副作用的患者，例如，其中所述糖皮质激素和所述化合物通过不同途径施用。

10. 发明申请

US20060115895A1 Fish disease models and uses thereof 审中-公开
标题翻译：鱼病模型及其用途
公开(公告)号：US20060115895A1
公开(公告)日：2006-06-01
申请号：US10537258
申请日：2003-12-01
申请人： Paul Goldsmith , Angeleen Fleming , Andrew McGlashan Richards , Derek Jones , William Harris
发明人： Paul Goldsmith , Angeleen Fleming , Andrew McGlashan Richards , Derek Jones , William Harris
IPC分类号： C12N5/00 , C12N5/02
CPC分类号： C12N15/8509 , A01K67/0275 , A01K2207/15 , A01K2217/00 , A01K2217/05 , A01K2227/40 , A01K2267/03 , C12N2830/008
摘要： Generation and use of disease models, for instance in assays to identify and investigate genes and substances involved in disease and disease treatment, identification and use of drug targets. In particular, the present invention relates to generation and use of disease models in fish such as zebrafish. Gradable phenotypes may be generated in fish, allowing for degree of correction or alteration of an activity or effect of a treatment, gene or mutation to be assayed. Competing stimuli may be applied to fish in screens assaying for ability to affect an activity or effect of a treatment, gene or mutation. Example include any combination of an addictive drug, a visual stimulus, an audible startle stimulus, a temperature gradient, an electric shock, an aversive compound, a threatening shape or a dark area.
摘要翻译：疾病模型的生成和使用，例如用于鉴定和调查涉及疾病和疾病治疗的基因和物质的鉴定和使用的测定中。特别地，本发明涉及鱼类如斑马鱼中疾病模型的产生和使用。可能在鱼中产生可梯度表型，允许修正程度或改变待测定的活性或作用，基因或突变。竞争刺激可以在筛选测定影响治疗，基因或突变的活性或作用的能力的筛选中应用于鱼。示例包括成瘾药物，视觉刺激，可听惊厥刺激，温度梯度，电击，厌恶化合物，威胁形状或黑暗区域的任何组合。

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