专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明授权

US5696260A Certain cycloalkyl imidazopyrimidines, a new class of gaba brain receptor ligands 失效
标题翻译：某些环烷基咪唑并嘧啶，一类新的gaba脑受体配体
公开(公告)号：US5696260A
公开(公告)日：1997-12-09
申请号：US492806
申请日：1995-06-20
申请人： Kenneth Shaw , Alan Hutchison
发明人： Kenneth Shaw , Alan Hutchison
IPC分类号： A61K31/505 , A61P25/20 , C07D487/04
CPC分类号： C07D487/04
摘要： Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable non-toxic salts thereof wherein: R.sub.9 and Y are substituents as defined herein; and R.sub.a and R.sub.b independently represent halogen, hydroxy, amino, mono or dialkylamino where each alkyl is straight or branched chain alkyl having 1-6 carbon atoms, straight or branched chain lower alkyl having 1-6 chain atoms, or straight or branched chain lower alkoxy having 1-6 carbon atoms, where R.sub.a and R.sub.b each appear at most only once on the phenyl ring which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.
摘要翻译：公开了下式的化合物：其中：R 9和Y是如本文所定义的取代基; 并且R a和R b独立地表示卤素，羟基，氨基，单或二烷基氨基，其中每个烷基是具有1-6个碳原子的直链或支链烷基，具有1-6个链原子的直链或支链低级烷基，或直链或支链低级具有1-6个碳原子的烷氧基，其中R a和R b在苯环上最多仅出现一次，该化合物是GABAa脑受体或其前药的高选择性激动剂，拮抗剂或反向激动剂，并且可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物服用过量，提高警惕性。

12. 发明授权

US5604235A Certain pyrroloquinolinones; a new class of gaba brain receptor ligands 失效
标题翻译：某些吡咯喹啉酮; 一类新的gaba脑受体配体
公开(公告)号：US5604235A
公开(公告)日：1997-02-18
申请号：US367242
申请日：1995-02-27
申请人： Kenneth Shaw , Jun Yuan
发明人： Kenneth Shaw , Jun Yuan
IPC分类号： C07D471/04 , A61K31/395 , C07D487/06
CPC分类号： C07D471/04
摘要： This invention encompasses compounds of formula (I), and pharmaceutically acceptable non-toxic salts thereof wherein X and Y am the same or different and represent oxygen or H.sub.2 with the proviso that not both X and Y are H.sub.2 ; W represents phenyl, thienyl, or pyridyl, each of which may be unsubstituted or mono or disubstituted with organic or inorganic substituents; and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are variables representing organic and inorganic substituents. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorder overdose with benzodiazepine drugs, and enhancement of memory.
摘要翻译： PCT No.PCT / US93 / 04096 Sec。 371日期：1995年2月27日 102（e）日期1995年2月27日PCT提交1993年5月6日PCT公布。第WO94 / 26741号公报（I）本发明包括式（I）化合物及其药学上可接受的无毒盐，其中X和Y相同或不同，代表氧或H 2，条件是不是两者 X和Y是H 2; W代表苯基，噻吩基或吡啶基，它们各自可以是未被取代的或被有机或无机取代基单取代或二取代; 并且R1，R2，R3和R4是表示有机和无机取代基的变量。这些化合物是用于GABAa脑受体或其前药的高度选择性激动剂，拮抗剂或反向激动剂，并且可用于用苯并二氮杂药物过量的焦虑，睡眠和癫痫发作障碍的诊断和治疗以及记忆的增强。

13. 发明授权

US5597920A Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes 失效
标题翻译： Gabaa受体亚型和使用咪唑并喹啉和吡咯并嘧啶结合gabaa受体亚型筛选药物化合物的方法
公开(公告)号：US5597920A
公开(公告)日：1997-01-28
申请号：US876050
申请日：1992-04-30
申请人： Kenneth Shaw , Alan Hutchison , Andrew Thurkauf , John Tallman
发明人： Kenneth Shaw , Alan Hutchison , Andrew Thurkauf , John Tallman
IPC分类号： G01N33/53 , A61K31/495 , A61K31/505 , A61P25/08 , A61P25/20 , A61P25/28 , C07B59/00 , C07D487/04 , G01N33/534 , G01N33/566 , G01N33/94 , C07D487/06 , C07D487/02
CPC分类号： G01N33/9426 , C07B59/002 , G01N33/566 , G01N33/948 , G01N2500/20
摘要： The present invention provides methods for screening drug compounds utilizing compounds of formulas I and II, where formulas I and II are ##STR1## and the pharmaceutically acceptable salts thereof where: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 represent hydrogen, halogen, alkyl or alkoxy substituents;R5 is hydrogen or lower alkyl;X and Y represent hydrogen, halogen, alkyl or alkoxy substituents; andZ is hydrogen or fluorine.The invention also provides tritium or iodine isotope radiolabeled compounds of the formulas I and II radiolabeled with tritium or isotopes of iodine.The invention further provides novel GABAa receptor subtypes which specifically bind to compounds of formulas I or II.The invention also provides GABAa receptor subtypes which are bound in situ to a compound of formula I or II.The compounds provided herein bind selectively to a novel subtype of the GABAa binding site. Selective interaction of ligands at this unique receptor population results in pharmacological specificity which may lead to superior anxiolytics, cognition enhancers, anticonvulsants and sedative hypnotics.
摘要翻译：本发明提供了利用式I和II化合物筛选药物化合物的方法，其中式I和II是其中R 1，R 2，R 3和R 4表示氢，卤素，烷基或烷氧基取代基; R5是氢或低级烷基; X和Y表示氢，卤素，烷基或烷氧基取代基; Z是氢或氟。本发明还提供用氚或碘的同位素放射性标记的式I和II的氚或碘同位素放射性标记的化合物。本发明还提供了与式I或II化合物特异性结合的新型GABAa受体亚型。本发明还提供了与式I或II化合物原位结合的GABAa受体亚型。本文提供的化合物选择性结合GABAa结合位点的新亚型。配体在这种独特的受体群体上的选择性相互作用导致药理学特异性，这可能导致优异的抗焦虑药，认知增强剂，抗惊厥药和镇静催眠药。

14. 发明授权

US5426186A Certain cycloalkyl imidazopyrimidines, a new class of GABA brain receptor ligands 失效
标题翻译：某些环烷基咪唑并嘧啶，一类新的GABA脑受体配体
公开(公告)号：US5426186A
公开(公告)日：1995-06-20
申请号：US30122
申请日：1993-03-03
申请人： Kenneth Shaw , Alan Hutchison
发明人： Kenneth Shaw , Alan Hutchison
IPC分类号： A61K31/505 , A61P25/20 , C07D487/04
CPC分类号： C07D487/04
摘要： This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: n is 0, 1, or 2, X is ##STR2## and R.sub.1, R.sub.2, R.sub.3, W and Y are variables These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.
摘要翻译： PCT No.PCT / US91 / 06174 Sec。 371日期1993年3月3日 102（e）日期1993年3月3日PCT 1991年9月4日PCT。本发明包括下式的化合物：其中n为0,1或2，X为 R1，R2，R3，W和Y是变量这些化合物是用于GABAa脑受体或其前药的高选择性激动剂，拮抗剂或反向激动剂，并且可用于诊断和治疗焦虑，睡眠和癫痫发作，过量服用苯二氮卓类药物，提高警惕性。

15. 发明申请

US20120144762A1 MOBILE TRAINING UNIT 审中-公开
标题翻译：移动培训单位
公开(公告)号：US20120144762A1
公开(公告)日：2012-06-14
申请号：US13139336
申请日：2009-11-19
申请人： Darren Eatock , Fraser Gilmour , Kenneth Shaw , Hugh Anderson
发明人： Darren Eatock , Fraser Gilmour , Kenneth Shaw , Hugh Anderson
IPC分类号： E04H1/00
CPC分类号： G09B19/00
摘要： A mobile training unit including a transportable cargo container having a transport position and at least one training position, the cargo container including: (a) at least one confined working compartment wholly or substantially within the cargo container dimensions; (b) at least one cargo container wall portion movable between a closed transport position and an open training position; (c) at least one door for entry into and exit from the cargo container; and (d) a tower movable between a transport position within the cargo container dimensions, and a training position extending beyond the cargo container. The mobile training unit in its transport position provides a very convenient unit for easy transportation to different locations where training is necessary or desired. This mobile training unit can at least supply facilities to provide training in relation to confined /enclosed spaces, working at height, fall potential and rescue situations.
摘要翻译：一种移动训练单元，包括具有运输位置和至少一个训练位置的可移动货物集装箱，所述货物集装箱包括：（a）完全或基本上在货物集装箱尺寸内的至少一个密闭工作舱; （b）至少一个在封闭的运输位置和开放训练位置之间运动的货物集装箱壁部分; （c）至少一个进入和离开货物集装箱的门; 和（d）可在货物集装箱尺寸内的运输位置和延伸超过货物集装箱的训练位置之间移动的塔架。移动训练单元在运输位置提供了一个非常方便的单位，便于运输到需要或需要进行训练的不同地点。这个移动训练单位至少可以提供设施，提供有限的封闭空间，高空作业，跌倒潜力和救援情况方面的培训。

16. 发明申请

US20110008453A1 Stable Corticosteroid Nanoparticulate Formulations And Methods For The Making And Use Thereof 有权
标题翻译：稳定的皮质类固醇纳米颗粒制剂及其制备和使用方法
公开(公告)号：US20110008453A1
公开(公告)日：2011-01-13
申请号：US12777920
申请日：2010-05-11
申请人： Kenneth Shaw , Mingbao Zhang
发明人： Kenneth Shaw , Mingbao Zhang
IPC分类号： A61K9/14 , A61K31/58 , A61P11/00 , A61P17/04 , A61P27/02
CPC分类号： A61K9/145 , A61K9/007 , A61K9/0073 , A61K9/0075 , A61K9/0078 , A61K9/008 , A61K9/1623 , A61K9/1652 , A61K9/2886 , A61K9/5078 , A61K31/58 , A61K47/14 , A61K47/6949 , B82Y5/00 , C07J71/00 , Y10S977/773 , Y10S977/906
摘要： Disclosed are stable corticosteroid nanoparticulate formulations, methods of making and therapeutic uses thereof.
摘要翻译：公开了稳定的皮质类固醇纳米颗粒制剂，其制备方法及其治疗用途。

17. 发明授权

US07326709B2 Bicyclic and tricyclic heteroaromatic compounds 失效
标题翻译：双环和三环杂芳族化合物
公开(公告)号：US07326709B2
公开(公告)日：2008-02-05
申请号：US11442812
申请日：2006-05-30
申请人： Jun Yuan , Pamela A. Albaugh , Kenneth Shaw , Alan J. Hutchison
发明人： Jun Yuan , Pamela A. Albaugh , Kenneth Shaw , Alan J. Hutchison
IPC分类号： C07D487/04 , A61K31/5025
CPC分类号： C07D217/26 , C07D237/30 , C07D471/04 , C07D487/04 , C07D519/00 , G01N2333/70571
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。这些化合物以高选择性和/或高亲和力结合GABA A A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和用作GABA < 组织样品中的受体。还公开了可用于制备这些化合物的中间体。

18. 发明申请

US20070264268A1 Man2as as Modifiers of the Igfr Pathway and Methods of Use 有权
标题翻译： Man2as作为Igfr途径的修饰剂和使用方法
公开(公告)号：US20070264268A1
公开(公告)日：2007-11-15
申请号：US10587253
申请日：2005-01-27
申请人： Lori Friedman , Helen Francis-Lang , Annette Parks , Kenneth Shaw , HaiGuang Zhang , Timothy Heuer
发明人： Lori Friedman , Helen Francis-Lang , Annette Parks , Kenneth Shaw , HaiGuang Zhang , Timothy Heuer
IPC分类号： A61K39/00 , A61P35/00 , C12N5/06 , C12Q1/02 , C12Q1/34 , C12Q1/68 , G01N33/53 , G01N33/566 , G01N33/574
CPC分类号： C12Q1/34 , G01N2500/00
摘要： Human MIGFR genes are identified as modulators of the IGFR pathway, and thus are therapeutic targets for disorders associated with defective IGFR function. Methods for identifying modulators of IGFR, comprising screening for agents that modulate the activity of MIGFR are provided.
摘要翻译：人MIGFR基因被鉴定为IGFR途径的调节剂，因此是与缺陷性IGFR功能相关的病症的治疗靶点。提供了鉴定IGFR调节剂的方法，包括筛选调节MIGFR活性的药剂。

19. 发明申请

US20050038043A1 Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands 有权
标题翻译：咪唑并 - 嘧啶和三唑并嘧啶：苯并二氮杂受体配体
公开(公告)号：US20050038043A1
公开(公告)日：2005-02-17
申请号：US10898690
申请日：2004-07-23
申请人： Linghong Xie , Bingsong Han , Yuelian Xu , George Maynard , Bertrand Chenard , Kenneth Shaw , Yang Gao
发明人： Linghong Xie , Bingsong Han , Yuelian Xu , George Maynard , Bertrand Chenard , Kenneth Shaw , Yang Gao
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
摘要翻译：提供了式I化合物，以及其制备方法。上述式中的变量Z1，Z2，Z3，R4，R5，R6，R7，R8和Ar定义如下。这样的化合物可用于在体内或体外调节配体与GABA A受体的结合，并且特别可用于治疗人，驯养的伴侣动物和家畜中的各种中枢神经系统（CNS）障碍。本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用，以增强其它CNS剂的作用。还提供了用于治疗这种病症的药物组合物和方法，以及使用这种配体检测GABA A受体的方法（例如受体定位研究）。

20. 发明申请

US20050014939A1 Fused pyrrolecarboxamides: GABA brain receptor ligands 审中-公开
标题翻译：融合的吡咯甲酰胺：GABA脑受体配体
公开(公告)号：US20050014939A1
公开(公告)日：2005-01-20
申请号：US10909022
申请日：2004-07-30
申请人： Pamela Albaugh , Kenneth Shaw , Alan Hutchison
发明人： Pamela Albaugh , Kenneth Shaw , Alan Hutchison
IPC分类号： A61K51/04 , C07D209/42 , C07D209/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D417/14 , C07D471/04 , C07D417/02 , C07D413/02 , C07
CPC分类号： C07D471/04 , A61K51/0419 , A61K51/0446 , A61K51/0453 , A61K51/0455 , A61K51/0459 , A61K51/0463 , C04B35/632 , C07D209/42 , C07D209/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D417/14 , G01N2333/70571
摘要： Substituted pyrrolecarboxamide compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Alzheimer's dementia, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译：公开了取代的吡咯甲酰胺化合物。这些化合物是用于GABA A受体的高选择性激动剂，拮抗剂或反向激动剂或GABA A受体的激动剂，拮抗剂或反向激动剂的前体药物，因此可用于诊断和治疗焦虑，抑郁，阿尔茨海默氏痴呆，睡眠和发作障碍，过量与苯二氮卓类药物和增强记忆。还提供药物组合物，包括包装的药物组合物。本发明的化合物也可用作组织样品中GABA A受体定位的探针。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式