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31. 发明授权

US07186724B2 Heterocyclic substituted carbonyl derivatives and their use as dopamine D3 receptor ligands 失效
标题翻译：杂环取代的羰基衍生物及其作为多巴胺D3受体配体的用途
公开(公告)号：US07186724B2
公开(公告)日：2007-03-06
申请号：US10819037
申请日：2004-04-06
申请人： James A Hendrix , Horst Hemmerle , Matthias Urmann , Gregory M Shutske , Jospeh T Strupczewski , Kenneth J Bordeau , John G Jurcak , Thaddeus Nieduzak , Sharon A Jackson , Paul Angell , James P Carey , George Lee , David Fink , Jean-Fancois Sabuco , Yulin Chiang , Nicola Collar
发明人： James A Hendrix , Horst Hemmerle , Matthias Urmann , Gregory M Shutske , Jospeh T Strupczewski , Kenneth J Bordeau , John G Jurcak , Thaddeus Nieduzak , Sharon A Jackson , Paul Angell , James P Carey , George Lee , David Fink , Jean-Fancois Sabuco , Yulin Chiang , Nicola Collar
IPC分类号： A61K31/496 , C07D409/04 , C07D409/14 , A61K31/4535 , A61K31/454 , C07D403/04
CPC分类号： A61K31/496 , C07D209/08 , C07D213/74 , C07D215/40 , C07D231/12 , C07D233/56 , C07D239/42 , C07D241/04 , C07D241/20 , C07D249/08 , C07D261/20 , C07D295/14 , 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 , C07D498/04
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 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 D3 receptors.
摘要翻译：本发明涉及显示与多巴胺D 3受体的选择性结合的杂环取代的羰基衍生物。另一方面，本发明涉及在需要这种治疗的患者中治疗与多巴胺D 3 N 3受体活性相关的中枢神经系统障碍的方法，包括向所述受试者施用治疗有效量的所述用于缓解这种病症的化合物。可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，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，杜氏综合征和亨廷顿疾病），痴呆，焦虑疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。本发明还涉及制备本文所述化合物的方法以及制备和使用化合物作为多巴胺D 3受体的显像剂的方法。

32. 发明授权

US07071339B2 Process for preparing functionalized γ-butyrolactones from mucohalic acid 失效
标题翻译：从粘酸卤酸制备官能化γ-丁内酯的方法
公开(公告)号：US07071339B2
公开(公告)日：2006-07-04
申请号：US10463612
申请日：2003-06-18
申请人： Daniel Belmont , Ji Zhang
发明人： Daniel Belmont , Ji Zhang
IPC分类号： C07D307/32
CPC分类号： C07D307/30 , C07D307/58 , C07D307/66 , C07D315/00
摘要： A process for preparing functionalized γ-butyrolactones 3 and various biologically active compounds using mucohalic acid 1 and halide 2 in the presence of indium is disclosed, wherein X, Y, R1, R2, and R3 may have any of the meanings defined herein
摘要翻译：公开了一种在铟存在下使用粘稠卤酸1和卤化物2制备官能化的γ-丁内酯3和各种生物活性化合物的方法，其中X，Y，R 1，R 2， / SUB>和R 3可以具有本文定义的任何含义

33. 发明授权

US07012075B2 Cathepsin cysteine protease inhibitors 有权
公开(公告)号：US07012075B2
公开(公告)日：2006-03-14
申请号：US10469430
申请日：2002-03-01
申请人： Petpihoon Prasit , Christopher Ian Bayly , Joel Stephane Robichaud , W. Cameron Black , Eduardo L. Setti , Robert M. Rydzewski , James T. Palmer
发明人： Petpihoon Prasit , Christopher Ian Bayly , Joel Stephane Robichaud , W. Cameron Black , Eduardo L. Setti , Robert M. Rydzewski , James T. Palmer
IPC分类号： A61K31/495 , A61K31/44 , A61K31/275 , C07D413/00 , C07C255/00
CPC分类号： C07D231/12 , C07C255/29 , C07C323/60 , C07C323/61 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/16 , C07D209/42 , C07D211/20 , C07D211/58 , C07D211/60 , C07D215/12 , C07D231/18 , C07D231/38 , C07D233/64 , C07D239/42 , C07D249/12 , C07D257/06 , C07D261/14 , C07D271/08 , C07D275/03 , C07D285/06 , C07D295/096 , C07D295/135 , C07D295/155 , C07D295/205 , C07D307/66 , C07D333/28 , C07D333/36 , C07D333/54 , C07D401/04 , C07D409/10 , C07D417/04 , C07D417/10 , C07D487/08
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

34. 发明申请

US20050179013A1 Hyperpolarizable organic chromophores 失效
标题翻译：超极化有机发色团
公开(公告)号：US20050179013A1
公开(公告)日：2005-08-18
申请号：US11077607
申请日：2005-03-11
申请人： Larry Dalton , Kwan-Yue Jen , Timothy Londergan , William Carlson , Gregory Phelan , Diyun Huang , Daniel Casmier , Todd Ewy , Nicholas Buker
发明人： Larry Dalton , Kwan-Yue Jen , Timothy Londergan , William Carlson , Gregory Phelan , Diyun Huang , Daniel Casmier , Todd Ewy , Nicholas Buker
IPC分类号： C07D307/36 , C07D307/54 , C07D307/56 , C07D307/66 , C07D319/06 , C07D333/24 , C07D409/06 , C07D409/14 , C07D495/04 , C07D519/00 , C07F7/08 , C07F7/10 , C07F7/12 , C09B23/00 , C09B23/01 , C09B23/10 , C09B69/10 , G03C1/00
CPC分类号： C07D307/56 , C07D307/36 , C07D307/54 , C07D307/66 , C07D319/06 , C07D333/24 , C07D409/06 , C07D495/04 , C07F7/0814 , C09B23/0075 , C09B23/105 , C09B69/105
摘要： The present invention provides hyperpolarizable organic chromophores. The chromophores are nonlinear optically active compounds that include a π-donor conjugated to a π-acceptor through a π-electron conjugated bridge. Macromolecular structures including the hyperpolarizable organic chromophores are also provided.
摘要翻译：本发明提供了超极化有机发色团。发色团是非线性光学活性化合物，其包括通过π-电子共轭桥键合到pi受体的π-供体。还提供了包括超极化有机发色团的大分子结构。

35. 发明申请

US20050106414A1 Oligofluorenlylene compounds 失效
标题翻译：低聚芴二烯化合物
公开(公告)号：US20050106414A1
公开(公告)日：2005-05-19
申请号：US10506300
申请日：2003-03-25
申请人： Akihito Saitoh , Mizuho Hiraoka , Koichi Suzuki , Akihiro Senoo , Hiroshi Tanabe , Naoki Yamada , Chika Negishi , Maki Okajima
发明人： Akihito Saitoh , Mizuho Hiraoka , Koichi Suzuki , Akihiro Senoo , Hiroshi Tanabe , Naoki Yamada , Chika Negishi , Maki Okajima
IPC分类号： H01L51/50 , C07C211/61 , C07D213/74 , C07D307/66 , C07D333/36 , C09K11/06 , H01L51/00 , H01L51/30 , H05B33/14
CPC分类号： H01L51/0039 , C07C211/61 , C07C2603/18 , C07C2603/24 , C07C2603/26 , C07D213/74 , C07D307/66 , C07D333/36 , H01L51/0035 , H01L51/0038 , H01L51/005 , H01L51/0053 , H01L51/0058 , H01L51/006 , H01L51/0062 , H01L51/007 , H01L51/0077 , H01L51/0078 , H01L51/0081 , H01L51/0085 , H01L51/50 , Y10S428/917
摘要： The present invention provides an oligofluorenylene compound represented by the general formula below, which enables production of an organic light-emitting device that exhibits an extremely pure luminescent hue and has a light emission of high efficiency, high brightness, and long lifetime.
摘要翻译：本发明提供一种由以下通式表示的低聚芴醇化合物，其能够生产具有极纯度的发光色调并具有高效率，高亮度和长使用寿命的发光的有机发光装置。

36. 发明授权

US06806024B1 Oxime derivatives and the use thereof as photoinitiators 有权
标题翻译：肟衍生物及其作为光引发剂的用途
公开(公告)号：US06806024B1
公开(公告)日：2004-10-19
申请号：US09914433
申请日：2001-08-27
申请人： Hisatoshi Kura , Hitoshi Yamato , Masaki Ohwa , Kurt Dietliker
发明人： Hisatoshi Kura , Hitoshi Yamato , Masaki Ohwa , Kurt Dietliker
IPC分类号： G03F7004
CPC分类号： G03F7/031 , B33Y70/00 , C07C309/66 , C07C309/73 , C07C323/57 , C07C381/00 , C07D307/66 , C07D333/36 , C07D339/08 , C07F9/097 , C07F9/655345 , C08F2/50 , Y10S430/12 , Y10S430/123
摘要： Radically photopolymerizable compositions comprising (a) at least one ethylenically unsaturated photopolymerizable compound; (b) as photoinitiator, at least one compound of formulae (I, II, III, IV, V and/or VI), wherein m is 0 or 1; n is 0, 1, 2 or 3; x is 1 or 2; R1 is inter alia phenyl, naphthyl, anthracyl or phenanthryl, a heteroaryl radical, C2-C12alkenyl, C4-C8cycloalkenyl, or C6-C12bicycloalkenyl; R′1 is inter alia C2-C12alkylene, or phenylene; R2 has one of the meanings of R1 or inter alia is phenyl; y is 1 or 2; R3 if x is 1 inter alia is C1-C18alkylsulfonyl, or phenyl-C1-C3alkylsulfonyl, R3 if x is 2, is for example C2-C12alkylenedisulfonyl; R4 and R5 inter alia are hydrogen, halogen, or C1-C8alkyl; R6, R7, R8 inter alia are hydrogen, R26Y—, or phenyl; R9 inter alia is C5-C8cycloalkyl, or phenyl; A is for example —S—, —O—, or —NR10—; Q is C1-C8-alkylene optionally interrupted by —O—; X is —O— or —NR9—; R10 inter alia is hydrogen, or phenyl; and (c) at least one coinitiator; are especially suitable for the preparation of color filter systems.
摘要翻译：自由基光聚合组合物，其包含（a）至少一种烯属不饱和光聚合化合物; （b）作为光引发剂，至少一种式（I，II，III，IV，V和/或VI）的化合物，其中m为0或1; n为0,1,2或3; x为1或2; R 1特别是苯基，萘基，蒽基或菲基，杂芳基，C 2 -C 12烯基，C 4 -C 8环烯基或C 6 -C 12双环烯基; R'1特别是C 2 -C 12亚烷基或亚苯基; R2具有R 1的含义之一，尤其是苯基; y为1或2; 如果x是1，则R3如果是C 1 -C 18烷基磺酰基，或苯基-C 1 -C 3烷基磺酰基，如果x是2，则R 3是例如C 2 -C 12亚烷基二磺酰基; R4和R5尤其是氢，卤素或C1-C8烷基; R6，R7，R8特别是氢，R26Y-或苯基; R9尤其是C5-C8环烷基或苯基; A是例如-S-，-O-或-NR 10 - ; Q是任选被-O-间隔的C1-C8-亚烷基; X是-O-或-NR 9 - ; R 10尤其是氢或苯基; 和（c）至少一种共引发剂; 特别适用于制备滤色器系统。

37. 发明申请

US20040002539A1 Process for preparing aminoguanidines and alkoxyguanidines as protease inhibitors 有权
标题翻译：制备氨基胍和烷氧基胍作为蛋白酶抑制剂的方法
公开(公告)号：US20040002539A1
公开(公告)日：2004-01-01
申请号：US10419972
申请日：2003-04-22
申请人： 3-Dimensional Pharmaceuticals, Inc.
发明人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan
IPC分类号： C07D317/08 , C07C069/76 , C07C279/10 , A61K031/365
CPC分类号： C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C323/66 , C07C2601/02 , C07C2601/14 , C07D211/96 , C07D213/42 , C07D213/74 , C07D215/36 , C07D217/02 , C07D217/22 , C07D239/42 , C07D295/13 , C07D295/26 , C07D307/66
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: 1 wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula L The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.
摘要翻译：氨基胍和烷氧基胍化合物，包括下式的化合物：其中X是O或NR 9和R 1 -R 4，R 6 -R 9，R 11，R 12，说明书中列出的R a，R b，R c，Y，Z，n和m以及抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐是描述。还描述了制备式L化合物的方法。本发明的新化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。

38. 发明申请

US20030225087A1 N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups, their preparation and their therapeutic uses 失效
标题翻译：含有金属螯合基团的N-烷基-N-苯基羟胺化合物，其制备及其治疗用途
公开(公告)号：US20030225087A1
公开(公告)日：2003-12-04
申请号：US10456024
申请日：2003-06-05
发明人： Eu-Gene Oh , Sung-Bo Ko , Won-Yeob Kim , Kyung-Hwa Kim , Dennis W. Choi , Laura L. Dugan , Tae-Cheon Kang , Jae-Young Koh , Kyung-Mi Kim , In-Jae Shin
IPC分类号： A61K031/53 , A61K031/4965 , A61K031/50 , A61K031/16
CPC分类号： C07D213/75 , C07C239/18 , C07D215/38 , C07D231/42 , C07D233/88 , C07D237/20 , C07D239/42 , C07D241/20 , C07D249/14 , C07D251/42 , C07D257/06 , C07D263/48 , C07D277/46 , C07D307/66 , C07D333/36
摘要： The present invention provides novel N-alkyl-N-phenylhydroxylamine derivatives containing metal chelating groups, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species (ROS) and/or excess Zn ions, in particular stroke, Parkinson's disease and Alzheimer's disease. The compounds of the invention possess similar or superior LPO inhibition activity to the reference compounds of Trolox and Ebselen. While showing lower toxicity, they also effectively inhibit the cerebral neuronal cell death caused by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.
摘要翻译：本发明提供了含有金属螯合基团的新型N-烷基-N-苯基羟胺衍生物及其制备方法，该新化合物用作治疗和/或预防各种医学功能障碍和由活性氧产生的疾病的用途（ ROS）和/或过量的Zn离子，特别是中风，帕金森病和阿尔茨海默病。本发明的化合物对Trolox和依布硒林的参考化合物具有相似或优异的LPO抑制活性。虽然毒性较低，但也有效地抑制由ROS和/或锌离子引起的脑神经元细胞死亡，并显示对缺血性神经元变性的神经保护作用。

39. 发明授权

US06620933B2 Azomethine yellow dye compound 失效
标题翻译：偶氮甲基黄染料化合物
公开(公告)号：US06620933B2
公开(公告)日：2003-09-16
申请号：US10254599
申请日：2002-09-26
申请人： Kiyoshi Takeuchi , Shigeki Uehira
发明人： Kiyoshi Takeuchi , Shigeki Uehira
IPC分类号： C07D23720
CPC分类号： C07D213/75 , C07C251/24 , C07C255/61 , C07C311/08 , C07D239/42 , C07D307/66 , C09B55/002
摘要： A azomethine yellow dye compound of general formula (I): General formula (I) wherein R1 and R2 each independently represent a hydrogen atom or a substituent; R3 represents a substituent; m indicates an integer from 0 to 3; when m is 2 or greater, R3's may be the same or different and may be mutually bonded to form a condensed ring; R3 may be bonded to R1 or R2 to form a condensed ring; R4 represents an aryl group or a heterocyclic group; R5 and R6 each independently represent a hydrogen atom or a substituent; R7 represents a substituent; n indicates an integer from 0 to 4; when n is 2 or greater, R7's may be the same or different and the may be mutually bonded to form a condensed ring; R7 may be bonded to R5 or R6 to form a condensed ring; and R5 and R6 may be bonded to each other to form a ring.
摘要翻译：通式（I）的偶氮甲碱黄染料化合物：通式（I）其中R 1和R 2各自独立地表示氢原子或取代基; R3表示取代基; m表示0〜3的整数，当m为2或更大时，R 3可以相同或不同并且可以相互结合形成稠环; R 3可以与R 1或R 2结合形成稠环; R4表示芳基或杂环基; R5和R6各自独立地表示氢原子或取代基; R7表示取代基; n表示0〜4的整数，当n为2或更大时，R 7可以相同或不同，并且可以相互键合形成稠环; R7可以键合到R5或R6以形成稠环; 并且R 5和R 6可以彼此键合形成环。

40. 发明申请

US20020084446A1 Hyperpolarizable organic chromophores 失效
标题翻译：超极化有机发色团
公开(公告)号：US20020084446A1
公开(公告)日：2002-07-04
申请号：US09912444
申请日：2001-07-24
发明人： Larry R. Dalton , Kwan-Yue Jen , Timothy Londergan , William Brenden Carlson , Gregory Phelan , Diyun Huang , Daniel Casmier , Todd Ewy , Nicholas Buker
IPC分类号： G02B001/04
CPC分类号： C07D307/56 , C07D307/36 , C07D307/54 , C07D307/66 , C07D319/06 , C07D333/24 , C07D409/06 , C07D495/04 , C07F7/0814 , C09B23/0075 , C09B23/105 , C09B69/105
摘要： The present invention provides hyperpolarizable organic chromophores. The chromophores are nonlinear optically active compounds that include a null-donor conjugated to a null-acceptor through a null-electron conjugated bridge. Macromolecular structures including the hyperpolarizable organic chromophores are also provided.
摘要翻译：本发明提供了超极化有机发色团。发色团是非线性光学活性化合物，其包括通过π-电子共轭桥键合到pi受体的π-供体。还提供了包括超极化有机发色团的大分子结构。

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