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1. 发明专利

CA168494A MELTING DEVICE 未知
公开(公告)号：CA168494A
公开(公告)日：1916-03-28
申请号：CA168494D
申请日：1916-01-03
申请人： LEE GEORGE E
发明人： LEE GEORGE E

2. 发明专利

CA2438264A1 HETEROCYCLIC SUBSTITUTED CARBONYL DERIVATIVES AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS 未知
公开(公告)号：CA2438264A1
公开(公告)日：2002-08-29
申请号：CA2438264
申请日：2002-02-15
申请人： CAREY JAMES P , LEE GEORGE E , AVENTIS PHARMA INC
发明人： URMANN MATTHIAS , ANGELL PAUL , BORDEAU KENNETH J , STRUPCZEWSKI JOSEPH T , SHUTSKE GREGORY , NIEDUZAK THADDEUS , JACKSON SHARON ANNE , SABUCO JEAN-FRANCOIS , JURCAK JOHN G , HEMMERLE HORST , COLLAR NICOLA , FINK DAVID M , CHIANG YULIN , HENDRIX JAMES A
IPC分类号： C07D295/14 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/44 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/46 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/535 , A61K31/5377 , A61K31/551 , A61K45/00 , A61K47/14 , A61K47/44 , A61K51/00 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C07D209/08 , C07D211/14 , C07D213/74 , C07D215/40 , C07D231/56 , C07D239/42 , C07D241/04 , C07D241/20 , C07D261/08 , C07D261/20 , C07D295/155 , C07D307/66 , C07D307/68 , C07D307/81 , C07D317/58 , C07D333/58 , C07D333/66 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D451/04 , C07D471/06 , C07D495/04 , C07D498/04 , C07D521/00
摘要： The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of su ch treatment comprising administering to the subject a therapeutically effectiv e amount of said compounds for alleviation of such disorder. The central nervo us system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson s Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington s Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. T he subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D3 receptors.

3. 发明申请

WO0119832A3 THIENOISOXAZOLE PHENOXY UNSUBSTITUTED ETHYL AND PROPYL DERIVATIVES USEFUL AS D4 ANTAGONISTS 审中-公开
标题翻译：噻吩并恶唑苯氧基取代的乙基和用作D4拮抗剂的丙基衍生物
公开(公告)号：WO0119832A3
公开(公告)日：2001-10-04
申请号：PCT/US0024949
申请日：2000-09-13
申请人： AVENTIS PHARMA INC , LEE GEORGE E , AYERS TIMOTHY A , JURCAK JOHN G
发明人： LEE GEORGE E , AYERS TIMOTHY A , JURCAK JOHN G
IPC分类号： A61K31/424 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/55 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/30 , C07D498/04 , A61K31/40 , A61K31/42 , A61K31/44 , A61K31/501
CPC分类号： C07D498/04
摘要： The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
摘要翻译：该化合物属于噻吩并异恶唑苯氧基未取代的乙基和丙基衍生物类，可用作D4拮抗剂。所述化合物可用于治疗由D4受体抑制介导的医学病症。这些病症包括例如注意缺陷多动障碍，强迫症，精神病，药物滥用，物质依赖，帕金森病，帕金森综合征，迟发性硬脑膜炎，吉尔斯德拉图雷特综合征，行为障碍和对立违抗性障碍。本发明的另一方面是提供药物组合物，中间体和制备所述类型的化合物的方法。

4. 发明申请

WO2002066446A1 HETEROCYCLIC SUBSTITUTED CARBONYL DERIVATIVES AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS 审中-公开
标题翻译：杂环取代的羰基衍生物及其作为DOPAMINE D3受体配体的用途
公开(公告)号：WO2002066446A1
公开(公告)日：2002-08-29
申请号：PCT/US2002/004713
申请日：2002-02-15
申请人： AVENTIS PHARMACEUTICALS INC. , CAREY, James, P. , LEE, George, E. , HENDRIX, James, A. , HEMMERLE, Horst , URMANN, Matthias , SHUTSKE, Gregory , STRUPCZEWSKI, Joseph, T. , BORDEAU, Kenneth, J. , JURCAK, John, G. , NIEDUZAK, Thaddeus , JACKSON, Sharon, Anne. , ANGELL, Paul , FINK, David, M. , SABUCO, Jean-Francois , CHIANG, Yulin , COLLAR, Nicola
发明人： HENDRIX, James, A. , HEMMERLE, Horst , URMANN, Matthias , SHUTSKE, Gregory , STRUPCZEWSKI, Joseph, T. , BORDEAU, Kenneth, J. , JURCAK, John, G. , NIEDUZAK, Thaddeus , JACKSON, Sharon, Anne. , ANGELL, Paul , FINK, David, M. , SABUCO, Jean-Francois , CHIANG, Yulin , COLLAR, Nicola
IPC分类号： C07D241/04
CPC分类号： C07D239/42 , A61K31/496 , C07D209/08 , C07D213/74 , C07D215/40 , C07D231/12 , C07D233/56 , C07D241/04 , C07D241/20 , C07D249/08 , C07D261/20 , C07D295/155 , C07D307/66 , C07D307/68 , C07D317/58 , C07D333/58 , C07D333/66 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D471/06 , C07D495/04
摘要： The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D 3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D 3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson s Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington s Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D¿3 receptors.
摘要翻译：本发明涉及显示与多巴胺D3受体的选择性结合的杂环取代的羰基衍生物。另一方面，本发明涉及一种治疗需要这种治疗的患者中与多巴胺D3受体活性相关的中枢神经系统障碍的方法，其包括向受试者施用治疗有效量的所述化合物以减轻这种病症。可以用这些化合物治疗的中枢神经系统疾病包括精神病，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏杜勒氏综合征和亨廷顿疾病），痴呆，焦虑障碍，睡眠障碍，昼夜节律紊乱和情绪障碍。本发明还涉及本文所述化合物的制备方法以及制备和使用化合物作为多巴胺D3受体的显像剂的方法。

5. 发明申请

WO2010107969A1 IMPROVED CHEMICAL SYNTHESIS OF DIAZAINDOLES BY CHICHIBABIN CYCLIZATION 审中-公开
标题翻译：通过CHICHIBABIN循环改进DIAZAINDOLES的化学合成
公开(公告)号：WO2010107969A1
公开(公告)日：2010-09-23
申请号：PCT/US2010/027755
申请日：2010-03-18
申请人： SANOFI-AVENTIS , LEE, George E. , SHRIMP II, Frederick L. , WEIBERTH, Franz J.
发明人： LEE, George E. , SHRIMP II, Frederick L. , WEIBERTH, Franz J.
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02
CPC分类号： C07D487/04
摘要： An improved synthesis method for making diazaindoles using a Chichibabin cyclization is disclosed. In particular, this method is useful for making the compound of Formula I.
摘要翻译：公开了一种利用奇切布宾环化制备二氮茚的改进的合成方法。特别地，该方法可用于制备式I化合物。

6. 发明申请

WO2010107633A1 BELT EXTENDER 审中-公开
标题翻译：皮带扩展器
公开(公告)号：WO2010107633A1
公开(公告)日：2010-09-23
申请号：PCT/US2010/026733
申请日：2010-03-09
申请人： HIGH VALLEY RANCH PROPERTIES, L.L.C. , LEE, George, E. , ERICKSEN, Erik, Philip
发明人： LEE, George, E. , ERICKSEN, Erik, Philip
IPC分类号： A41F9/02
CPC分类号： A41F9/002
摘要： A belt extender for installation on a belt with a removable buckle comprising a main body with a first end and a second end, a metal tab fixedly attached to and extending from a first end of the main body of the belt extender, and a longitudinal slot roughly centrally disposed on the main body of the belt extender. The main body folds over itself at a fold line that extends through the center of the longitudinal slot and is secured in place with snap fasteners to create a folded end. A belt buckle comprising a tongue and a frame is installed on the folded end of the belt extender by sliding the frame of the belt buckle over the second end of the belt extender and inserting the tongue through the longitudinal slot prior to folding.
摘要翻译：一种带状延伸器，用于安装在具有可拆卸带扣的带上的带子延伸器，该带子包括具有第一端和第二端的主体，固定地附接到带延伸器的主体的第一端并从其延伸的金属接头，大致中心地布置在带延伸器的主体上。主体折叠在折叠线上，折线延伸穿过纵向槽的中心，并用紧固件固定就位以产生折叠端。通过将带扣的框架滑动在带延伸器的第二端上并且在折叠之前将舌片插入纵向槽中，将包括舌和框架的带扣安装在带延伸器的折叠端上。

7. 发明申请

WO2010077623A1 INTERMEDIATES AND PROCESSES FOR THE PREPARATION OF FLUOROGLYCOSIDE DERIVATIVES 审中-公开
标题翻译：制备荧光素衍生物的中间体和方法
公开(公告)号：WO2010077623A1
公开(公告)日：2010-07-08
申请号：PCT/US2009/067079
申请日：2009-12-08
申请人： SANOFI-AVENTIS , GESSLER, Simon , GILL, Harpal S. , LEE, George E. , PLETTENBURG, Oliver , PODESCHWA, Michael , POWERS, Matthew R. , ROSSEN, Kai , SHRIMP, II, Frederick L. , SUBOTKOWSKI, Witold , VANASSE, Benoit J. , WEHLAN, Hermut A. , WEIBERTH, Franz J. , YU, Yong , ZHANG, Jiuqing
发明人： GESSLER, Simon , GILL, Harpal S. , LEE, George E. , PLETTENBURG, Oliver , PODESCHWA, Michael , POWERS, Matthew R. , ROSSEN, Kai , SHRIMP, II, Frederick L. , SUBOTKOWSKI, Witold , VANASSE, Benoit J. , WEHLAN, Hermut A. , WEIBERTH, Franz J. , YU, Yong , ZHANG, Jiuqing
IPC分类号： C07D231/20 , C07H5/02 , C07H13/08
CPC分类号： C07D231/20
摘要： The present invention provides processes for producing (2 S ,3 R ,4 R ,5 S ,6 R )-5-fluoro-6- hydroxymethyl-2-[4-(4-methoxy-benzyl)-5-trifluoromethyl-1 H -pyrazol-3-yloxy]- tetrahydro-pyran-3,4-diol or a tautomer or hydrate thereof, of high purity and in a relatively high yield suitable for use on an industrial scale. The present invention is also directed to synthetic intermediates that are useful for the preparation of (2 S ,3 R ,4 R ,5 S ,6 R )-5-fluoro-6-hydroxymethyl-2-[4-(4-methoxy- benzyl)-5-trifluoromethyl-1 H -pyrazol-3-yloxy]-tetrahydro-pyran-3,4-diol or a tautomer or hydrate thereof.
摘要翻译：本发明提供（2S，3R，4R，5S，6R）-5-氟-6-羟甲基-2- [4-（4-甲氧基 - 苄基）-5-三氟甲基-1H-吡唑-3-基] 氧基] - 四氢 - 吡喃-3,4-二醇或其互变异构体或水合物，其具有高纯度和相对高的产率，适用于工业规模。本发明还涉及可用于制备（2S，3R，4R，5S，6R）-5-氟-6-羟甲基-2- [4-（4-甲氧基 - 苄基）-5 - 三氟甲基-1H-吡唑-3-基氧基] - 四氢 - 吡喃-3,4-二醇或其互变异构体或水合物。

8. 发明申请

WO2005035496A1 PROCESS FOR THE PREPARATION OF N-AMINO SUBSTITUTED HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：制备N-氨基取代的杂环化合物的方法
公开(公告)号：WO2005035496A1
公开(公告)日：2005-04-21
申请号：PCT/US2004/032086
申请日：2004-10-01
申请人： AVENTIS PHARMACEUTICALS INC. , WEIBERTH, Franz , LEE, George, E. , HANNA, Reda, G. , DUBBERKE, Silke , UTZ, Roland , MUELLER-LEHAR, Jurgen
发明人： WEIBERTH, Franz , LEE, George, E. , HANNA, Reda, G. , DUBBERKE, Silke , UTZ, Roland , MUELLER-LEHAR, Jurgen
IPC分类号： C07D209/08
CPC分类号： C04B35/632 , C07D209/08 , C07D209/86 , C07D401/04 , C07D401/12
摘要： An improved process for the preparation of N-amino nitrogen heterocyclic compounds is disclosed and claimed. In an ambodiment of this invention, a compound of the formula (VI) is prepared starting from the corresponding indole derivative by way of N-amination and subsequently forming an hydrazone by the reaction with a keto compound in a single step. Further reduction of the hydrazone and subsequent coupling with a pyridine compound affords the compound of formula VI or a suitable salt thereof.
摘要翻译：公开并要求保护制备N-氨基氮杂环化合物的改进方法。在本发明的实施方案中，式（Ⅵ）化合物由相应的吲哚衍生物开始通过N-胺化制备，随后通过在一个步骤中与酮化合物的反应形成腙。腙的进一步还原，随后与吡啶化合物的偶合得到式Ⅵ化合物或其合适的盐。

9. 发明授权

US1057157A Matrix-suspending bar for linotype-machines. 失效
标题翻译：用于LINOTYPE-MACHINES的矩阵悬挂条。
公开(公告)号：US1057157A
公开(公告)日：1913-03-25
申请号：US1911631884
申请日：1911-06-08
申请人： LEE GEORGE E
发明人： LEE GEORGE E
CPC分类号： B41B11/18

10. 发明授权

US2423562A Film cartridge for moving picture cameras 失效
标题翻译：用于移动摄像机的胶片盒
公开(公告)号：US2423562A
公开(公告)日：1947-07-08
申请号：US54155444
申请日：1944-06-22
申请人： LEE GEORGE E
发明人： LEE GEORGE E
IPC分类号： G03B17/26
CPC分类号： G03B17/265

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