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31. 发明申请

US20080306096A1 Quinazoline Derivatives, Process for Their Preparation and Their Use as Anti-Cancer Agents 审中-公开
标题翻译：喹唑啉衍生物，其制备方法及其用作抗癌剂
公开(公告)号：US20080306096A1
公开(公告)日：2008-12-11
申请号：US12097965
申请日：2006-12-19
申请人： Brian Aquila , Jayachandran Ezhuthachan , Paul Lyne , Timothy Pontz , Xiaolan Zheng
发明人： Brian Aquila , Jayachandran Ezhuthachan , Paul Lyne , Timothy Pontz , Xiaolan Zheng
IPC分类号： A61K31/517 , A61P35/00 , C07D239/94 , C07D403/12 , C07D405/02 , C07D409/02 , C07D401/02
CPC分类号： C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
摘要翻译：本发明涉及具有B Raf抑制活性的式（I）化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制备用于在温血动物如人中产生抗癌作用的药物中的用途。

32. 发明申请

US20080297035A1 Novel Materials for N-Type Doping of the Electron Transporting Layers in Organic Electronic Devices 有权
标题翻译：用于有机电子器件中电子传输层的N型掺杂的新型材料
公开(公告)号：US20080297035A1
公开(公告)日：2008-12-04
申请号：US12065859
申请日：2006-08-29
申请人： Andreas Kanitz
发明人： Andreas Kanitz
IPC分类号： H01L51/52 , C07D471/02 , C07D409/02
CPC分类号： H01L51/002 , H01L51/006 , H01L51/0061 , H01L51/0068 , H01L51/5052 , Y02B10/10 , Y02E10/549 , Y10S428/917
摘要： The invention pertains to new materials based on donor carbene intermediates for the improvement of electron injection and electron transport in organic electronic components like organic light-emitting diodes (OLED's), organic field effect transistors (OFET's), and components based on organic photovoltaics, in particular organic solar cells.
摘要翻译：本发明涉及用于改善有机电子部件如有机发光二极管（OLED），有机场效应晶体管（OFET）以及基于有机光伏组件的有机电子部件中的电子注入和电子传输的基于供体卡宾中间体的新材料，特定的有机太阳能电池。

33. 发明授权

US07399770B2 Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors 有权
标题翻译：噻吩并亚氨基酸衍生物用作基质金属蛋白酶抑制剂
公开(公告)号：US07399770B2
公开(公告)日：2008-07-15
申请号：US11461189
申请日：2006-07-31
申请人： Manfred Schudok , Hans Matter , Armin Hofmeister , Maxime Lampilas
发明人： Manfred Schudok , Hans Matter , Armin Hofmeister , Maxime Lampilas
IPC分类号： A61K31/4365 , C07D409/02 , C07D495/06
CPC分类号： C07D495/04
摘要： The invention is directed to a compound of the formula I wherein the variables are as defined herein, or a stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a salt thereof. Another aspect of the present invention is directed to a pharmaceutical composition comprising, a pharmaceutically effective amount of one or more compounds of formula I according to claim 1 in admixture with a pharmaceutically acceptable carrier.The invention is also directed to a method for effecting the prophylaxis and therapy of degenerative joint diseases such as osteoarthroses, spondyloses, cartilage loss following joint trauma or a relatively long period of joint immobilization following meniscus or patella injuries or ligament ruptures, diseases of the connective tissue such as collagenoses, periodontal diseases, wound healing disturbances and chronic diseases of the locomotory apparatus such as inflammatory, immunological or metabolism-associated acute and chronic arthritides, arthropathies, myalgias and disturbances of bone metabolism, for the treatment of ulceration, atheroscleroses and stenoses, and for the treatment of inflammations, cancer diseases, tumor metastasis formation, cachexia, anorexia, cardiac insufficiency and septic shock or for the prophylaxis of myocardial and cerebral infarctions, in a patient in need thereof, comprising administering to the patient a pharmaceutically effective amount of the compound of formula I according to claim 1, or a pharmaceutically acceptable salt, solvate or prodrug thereof.Furthermore the invention is directed to a method for preparing a compound of formula I.
摘要翻译：本发明涉及式I化合物，其中变量如本文所定义，或其立体异构形式，立体异构体形式的任何比例的混合物或其盐。本发明的另一方面涉及一种药物组合物，其包含药学有效量的一种或多种根据权利要求1的式I化合物与药学上可接受的载体的混合物。本发明还涉及一种用于预防和治疗退行性关节疾病如骨关节炎，椎关节强硬，关节创伤后的软骨损失或半月板或髌骨损伤或韧带断裂后相对较长的关节固定的方法，连接性疾病诸如胶原蛋白，牙周病，伤口愈合障碍和诸如炎症，免疫学或代谢相关的急性和慢性关节炎的关节病，关节病，肌痛和骨骼代谢紊乱的运动器官的组织，用于治疗溃疡，动脉粥样硬化和狭窄，并且用于在有需要的患者中治疗炎症，癌症疾病，肿瘤转移形成，恶病质，厌食症，心脏功能不全和败血性休克或用于预防心肌和脑梗死，包括向患者施用药学有效量的compou 根据权利要求1的式I的或其药学上可接受的盐，溶剂合物或前药。此外，本发明涉及制备式I化合物的方法。

34. 发明申请

US20080146797A1 PROCESS FOR SYNTHESIZING HETEROCYCLIC COMPOUNDS 有权
标题翻译：合成杂环化合物的方法
公开(公告)号：US20080146797A1
公开(公告)日：2008-06-19
申请号：US12026746
申请日：2008-02-06
申请人： Uwe HEINELT , Hans-Jochen LANG
发明人： Uwe HEINELT , Hans-Jochen LANG
IPC分类号： C07D265/06 , C07D233/06 , C07D277/08 , C07D235/04 , C07D263/52 , C07D235/02 , C07D409/02
CPC分类号： C07D413/12 , C07D233/50 , C07D235/30 , C07D263/28 , C07D263/58 , C07D265/08 , C07D265/12 , C07D265/18 , C07D277/18 , C07D409/12 , C07D495/04
摘要： The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine or formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.
摘要翻译：本发明提供了用于合成式I的杂环化合物的方案1中所示的方法。在该方法中，式II的异硫氰酸酯最初与伯胺或式III反应，得到式IV的硫脲。随后，使用碱和磺酰氯将式IV的硫脲转化成相应的式I的杂环。

35. 发明授权

US07385067B2 Process for the preparation of compounds having a CF2O bridge 失效
标题翻译：制备具有CF2O桥的化合物的方法
公开(公告)号：US07385067B2
公开(公告)日：2008-06-10
申请号：US11445167
申请日：2006-06-02
申请人： Peer Kirsch , Andreas Taugerbeck , Alexander Hahn
发明人： Peer Kirsch , Andreas Taugerbeck , Alexander Hahn
IPC分类号： C07D321/00 , C07D339/06 , C07D339/08 , C07D409/02 , C07D317/72 , C07D493/10 , C07C25/24
CPC分类号： C07D317/72 , C07B41/04 , C07C45/59 , C07C45/60 , C07C49/753 , C07D319/14 , C07D321/10 , C07D339/08 , C07D409/06 , C09K19/3066 , C09K19/42 , C09K19/588 , C09K2019/3408 , C09K2019/3425 , C09K2019/3433 , C09K2019/3438
摘要： The invention relates to a process for the preparation of compounds containing at least one —CF2—O— bridge in the molecule, in which a) an acid is added onto at least one ketene dithioketal, b) the resultant bis(alkylthio)carbenium salt is reacted with at least one compound having at least one hydroxyl group in the presence of a base, c) and subsequently, preferably in situ, the resultant dithioorthoester is subjected to oxidative fluorodesulfurisation using a fluorinating agent and an oxidant to give the compound containing at least one —CF2—O— bridge in the molecule.
摘要翻译：本发明涉及在分子中制备含有至少一个-CF 2 -O-O-桥的化合物的方法，其中a）将酸加入到至少一种烯酮二硫酮缩酮上，b）所得的双（烷硫基）咔唑盐与至少一种具有至少一个羟基的化合物在碱的存在下反应，c）然后优选原位，所得的二硫代外酯使用氟化剂进行氧化氟脱硫，氧化剂在分子中得到含有至少一个-CF 2 -O-O-桥的化合物。

36. 发明申请

US20070208045A1 SUBSTITUTED-(QUINAZOLINYL)PHENYL THIOPHENYL-SULFONYLUREAS, METHODS FOR MAKING AND INTERMEDIATES THEREOF 审中-公开
标题翻译：取代 - （喹喔啉基）苯基噻吩磺酰亚胺，其制备方法及其中间体
公开(公告)号：US20070208045A1
公开(公告)日：2007-09-06
申请号：US11556518
申请日：2006-11-03
申请人： Robert Scarborough , Carroll Scarborough , Anjali Pandey , Mukund Mehrotra , Michael Cruskie , David White , George Yiannikouros
发明人： Robert Scarborough , Carroll Scarborough , Anjali Pandey , Mukund Mehrotra , Michael Cruskie , David White , George Yiannikouros
IPC分类号： A61K31/517 , C07D409/02
CPC分类号： C07D409/12
摘要： The present invention provides sulfonylurea compounds of formula (VIII) and pharmaceutically acceptable derivatives thereof and a process for making thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention also provides a method for inhibition platelet ADP receptor and preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (VIII) or a pharmaceutically acceptable salt or forms thereof.
摘要翻译：本发明提供式（VIII）的磺酰脲化合物及其药学上可接受的衍生物及其制备方法。各种形式的化合物是有效的血小板ADP受体抑制剂，可用于各种药物组合物中，并且特别有效预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病。本发明还提供了可用于该方法的中间体化合物，以及通过该方法生产的最终产物及其盐或前药。本发明还提供了抑制血小板ADP受体并预防或治疗哺乳动物血栓形成和血栓形成相关病症的方法，包括施用治疗有效量的式（Ⅷ）化合物或其药学上可接受的盐或其形式的步骤。

37. 发明申请

US20070179180A1 Novel m3 muscarinic acetylcholine receptor antagonists 审中-公开
标题翻译：新型m3毒蕈碱乙酰胆碱受体拮抗剂
公开(公告)号：US20070179180A1
公开(公告)日：2007-08-02
申请号：US10581229
申请日：2004-12-03
申请人： Jakob Busch-Petersen , Jian Jin , Michael Palovich , Wei Fu
发明人： Jakob Busch-Petersen , Jian Jin , Michael Palovich , Wei Fu
IPC分类号： A61K31/4709 , A61K31/454 , A61K31/4545 , A61K31/453 , A61K31/452 , C07D409/02 , C07D405/02 , C07D403/02 , C07D401/02
CPC分类号： C07D211/56 , C07D215/36 , C07D263/46 , C07D277/44 , C07D317/46 , C07D333/34 , C07D401/12 , C07D405/06 , C07D409/02 , C07D409/14 , C07D413/12 , C07D417/14
摘要： Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.
摘要翻译：提供毒蕈碱性乙酰胆碱受体拮抗剂及其使用方法。

38. 发明申请

US20070161701A1 4-oxo-4,5-dihydro-furan-2-carboxylic acid derivatives and methods of treatment of metabolic-related disorders thereof 失效
标题翻译： 4-氧代-4,5-二氢呋喃-2-羧酸衍生物及其代谢相关病症的治疗方法
公开(公告)号：US20070161701A1
公开(公告)日：2007-07-12
申请号：US11602551
申请日：2006-11-21
申请人： Jae-Kyu Jung , Graeme Semple , Benjamin Johnson
发明人： Jae-Kyu Jung , Graeme Semple , Benjamin Johnson
IPC分类号： A61K31/381 , A61K31/34 , C07D409/02 , C07D307/02
CPC分类号： C07D307/68 , C07D405/04 , C07D409/04 , C07D409/10
摘要： System for selecting a colour shade comprising a very small number of colour display cards with mixed shades of two or more colours. The system comprises means for selecting one shade among mixed shades, means for presenting the selected mixed shade as well as means for specifying the selected mixed shade for making paint in the desired colour tone.
摘要翻译：用于选择颜色的系统，其包括具有两种或更多种颜色的混合色调的非常少量的彩色显示卡。该系统包括用于选择混合色调中的一个色调的装置，用于呈现所选择的混合色调的装置以及用于指定所选择的混合色调以用于制作所需色调的油漆的装置。

39. 发明申请

US20070161650A1 Novel thiophene derivatives which are HM74A agonists 失效
标题翻译： HM74A激动剂的新型噻吩衍生物
公开(公告)号：US20070161650A1
公开(公告)日：2007-07-12
申请号：US11638220
申请日：2006-12-13
申请人： Henrietta Dehmlow , Uwe Grether , Nicole Kratochwil , Robert Narquizian , Constantinos Panousis
发明人： Henrietta Dehmlow , Uwe Grether , Nicole Kratochwil , Robert Narquizian , Constantinos Panousis
IPC分类号： A61K31/497 , A61K31/513 , A61K31/4436 , A61K31/381 , C07D409/02
CPC分类号： C07D409/12 , C07D333/38
摘要： The invention is concerned with novel substituted thiophene derivatives of formula (I) wherein R1 to R8, X, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新的取代噻吩衍生物，其中R 1至R 8，X，m和n如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物是HM74A激动剂，可用作药物。

40. 发明申请

US20070112009A1 1-N-phenyl-amino-1h-imidazole derivatives and pharmaceutical compositions containing them 失效
标题翻译： 1-N-苯基 - 氨基-1h-咪唑衍生物和含有它们的药物组合物
公开(公告)号：US20070112009A1
公开(公告)日：2007-05-17
申请号：US10582778
申请日：2004-12-15
申请人： Jean Lafay , Benoit Rondot , Paule Bonnet , Thierry Clerc , Jaqueline Shields , Igor Duc , Eric Duranti , Francois Puccio , Christian Blot , Philippe Maillos
发明人： Jean Lafay , Benoit Rondot , Paule Bonnet , Thierry Clerc , Jaqueline Shields , Igor Duc , Eric Duranti , Francois Puccio , Christian Blot , Philippe Maillos
IPC分类号： A61K31/513 , A61K31/497 , A61K31/4152 , A61K31/501 , A61K31/4439 , C07D409/02 , C07D403/02
CPC分类号： C07D233/54 , C07D409/12 , C07D419/12
摘要： The invention relates to the compounds of formula (I): in which R1, R2, R3, R4, Q and Z are as defined in the specification. The invention also relates to the pharmaceutical compositions containing these compounds.
摘要翻译：本发明涉及式（I）化合物：其中R 1，R 2，R 3，R 4， / SUB，Q和Z如说明书中所定义。本发明还涉及含有这些化合物的药物组合物。

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