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81. 发明授权

US07868014B2 1-(hetero)aryl-3-amino-pyrrolidine derivatives for use as mGluR3 antagonists 有权
标题翻译：用作mGluR3拮抗剂的1-（杂）芳基-3-氨基 - 吡咯烷衍生物
公开(公告)号：US07868014B2
公开(公告)日：2011-01-11
申请号：US11576960
申请日：2005-10-13
申请人： Thomas Charles Britton , Veronique Dehlinger , Colin Peter Dell , Bruce Anthony Dressman , Jason Kenneth Myers , Eric Samuel Nisenbaum
发明人： Thomas Charles Britton , Veronique Dehlinger , Colin Peter Dell , Bruce Anthony Dressman , Jason Kenneth Myers , Eric Samuel Nisenbaum
IPC分类号： C07D401/04 , C07D409/04 , A61K31/506
CPC分类号： C07D417/14 , C07C45/41 , C07D207/14 , C07D401/04 , C07D403/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/04 , C07C47/55
摘要： The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.
摘要翻译：本发明涉及可用于治疗与mGluR3受体如抑郁症，精神分裂症和偏头痛相关的病症的式（I）化合物，其药物组合物及其使用方法。

82. 发明申请

US20100312017A1 METHOD FOR THE PRODUCTION OF AROMATIC CARBONYL COMPOUNDS 失效
标题翻译：生产芳香碳化合物的方法
公开(公告)号：US20100312017A1
公开(公告)日：2010-12-09
申请号：US12733445
申请日：2008-09-02
申请人： Klaus Forstinger , Thomas Sommer , Daniel Decker , Andreas Martin , Angela Köckritz , Michael Kant , Alexander Hofmann
发明人： Klaus Forstinger , Thomas Sommer , Daniel Decker , Andreas Martin , Angela Köckritz , Michael Kant , Alexander Hofmann
IPC分类号： C07C45/28
CPC分类号： C07B41/06 , C07C45/28 , C07C47/55
摘要： The invention relates to a method for the production of an aromatic carbonyl compound by the oxidation of a methyl group or methylene group bonded to the aromatic group in which the aromatic substance is reacted in the presence of an oxidising agent and a sulphoxide, a sulphoxide being selected for the oxidation of a specific aromatic substance whose ionisation potential, in terms of magnitude, differs from the ionisation potential of the aromatic substance to be oxidised by a maximum of ±0.25 eV.
摘要翻译：本发明涉及一种芳族羰基化合物的制备方法，该方法是通过氧化与芳族基团结合的甲基或亚甲基，其中芳族物质在氧化剂和亚砜存在下反应，亚砜为选择用于氧化特定芳族物质，其电离电位（以量级计）与待氧化的芳族物质的电离电位不同于最大±0.25eV。

83. 发明授权

US07790931B2 Process for preparing tetrafluorobenzene carbaldehyde alkyl acetal 失效
标题翻译：制备四氟苯甲醛烷基缩醛的方法
公开(公告)号：US07790931B2
公开(公告)日：2010-09-07
申请号：US11993302
申请日：2006-06-12
申请人： Haruhiko Ikeda , Hideo Miyata , Katsutoshi Ohno , Katsuro Urakawa
发明人： Haruhiko Ikeda , Hideo Miyata , Katsutoshi Ohno , Katsuro Urakawa
IPC分类号： C07C45/42 , C07C43/307
CPC分类号： C07C41/50 , C07C45/44 , C07C45/515 , C07C47/55 , C07C43/313
摘要： A process for preparing tetrafluorobenzene carbaldehyde alkyl acetal represented by the following formula (II), comprising reducing tetrafluorocyanobenzene represented by the following formula (I) with a metal catalyst containing a platinum group metal in the presence of an alkyl alcohol represented by R—OH (R is an alkyl group of 1 to 4 carbon atoms) and an acid; (I) wherein m is 1 or 2, n is 0 or 1, and m+n is 2, (II) wherein m and n are the same as those in the formula (I), and R is an alkyl group of 1 to 4 carbon atoms.
摘要翻译：一种制备由下式（II）表示的四氟苯甲醛烷基缩醛的方法，包括在由R-OH表示的烷基醇存在下，用含有铂族金属的金属催化剂还原由下式（I）表示的四氟代氰基苯 R是1至4个碳原子的烷基）和酸; （I）其中m为1或2，n为0或1，m + n为2，（II）其中m和n与式（I）中的相同，R为烷基1 至4个碳原子。

84. 发明申请

US20100040550A1 RADIOLABELLING METHODS 失效
标题翻译：放射性方法
公开(公告)号：US20100040550A1
公开(公告)日：2010-02-18
申请号：US12305253
申请日：2007-06-20
申请人： Matthias Eberhard Glaser , Erik Arstad
发明人： Matthias Eberhard Glaser , Erik Arstad
IPC分类号： A61K49/04 , C12N15/74 , A61K49/00 , A61P35/00
CPC分类号： C07K1/1077 , A61K51/0453 , A61K51/088 , C07B59/008 , C07C17/093 , C07C45/63 , C07D261/08 , C07K1/13 , C07C21/22 , C07C47/55
摘要： The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I): with a compound of formula (II) or, a compound of formula (III): with a compound of formula (IV): in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.
摘要翻译：本发明涉及放射性诊断和放射治疗剂，包括用放射性核素标记的生物活性载体。它还涉及标记载体的方法和试剂，所述载体包括式（I）化合物与式（II）化合物或式（III）化合物与式（IV）化合物的反应：）：在Cu（I）催化剂存在下。所得到的标记的缀合物可用作诊断剂，例如作为放射性药物更具体地用于正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）或放射治疗。

85. 发明申请

US20080287441A1 ALPHA-(TRIFLUOROMETHYL-SUBSTITUTED ARYLOXY, ARYLAMINO, ARYLTHIO OR ARYLMETHYL)-TRIFLUOROMETHYL-SUBSTITUTED PHENYLACETIC ACIDS AND DERIVATIVES AS ANTIDIABETIC AGENTS 审中-公开
标题翻译： ALPHA-（三氟甲磺酸取代的芳基，亚氨基，芳基或芳基甲基） - 三氟甲基取代的苯甲酸和衍生物作为抗菌剂
公开(公告)号：US20080287441A1
公开(公告)日：2008-11-20
申请号：US12107691
申请日：2008-04-22
申请人： Zuchun Zhao , Xin Chen , Jianchao Wang , Hongbin Sun , Jack Shih-Chieh Liang
发明人： Zuchun Zhao , Xin Chen , Jianchao Wang , Hongbin Sun , Jack Shih-Chieh Liang
IPC分类号： A61K31/5377 , C07C63/72 , A61K31/192 , C07D211/94 , A61K31/44 , C07C69/76 , C07D257/04 , A61K31/24 , C07C47/00 , A61K31/11 , C07D413/12
CPC分类号： C07C47/277 , C07B2200/07 , C07C43/23 , C07C45/41 , C07C45/44 , C07C47/55 , C07C51/09 , C07C59/68 , C07C69/007 , C07C69/736 , C07C205/26 , C07C205/37 , C07C205/38 , C07C229/36 , C07C233/18 , C07C323/62 , C07D213/64 , C07D257/04
摘要： Compounds having a formula: or a pharmaceutically acceptable salt or prodrug thereof, are provided, and are useful for the treatment of metabolic disorders.
摘要翻译：提供具有式：或其药学上可接受的盐或前药的化合物，并且可用于治疗代谢性疾病。

86. 发明授权

US07342138B2 Process for producing aromatic aldehyde 有权
标题翻译：芳香醛生产工艺
公开(公告)号：US07342138B2
公开(公告)日：2008-03-11
申请号：US10569469
申请日：2003-08-27
申请人： Kentaro Kawazoe
发明人： Kentaro Kawazoe
IPC分类号： C07C45/29 , C07C45/37
CPC分类号： C07C201/12 , C07C45/30 , C07C47/546 , C07C47/544 , C07C47/54 , C07C47/575 , C07C47/55 , C07C205/44
摘要： A process for producing an aromatic aldehyde compound represented by a general formula (3): (wherein R′ and n are as defined below), which comprises reacting a benzyl compound represented by a general formula (1): (wherein R may represents hydrogen atom, n represents an integer of 1 to 6, and R′ may be the same or different and represent a hydrogen atom or an alkyl gorup, an alkyl group or a phenyl group which may have a substituent) with an oxy-compound of bromine represented by the formula (2): MBrOm (2) (wherein M represents a hydrogen atom or a metal atom, and m represents an integer of 1 to 3) in the presence of an acid catalyst. According to this method, an aromatic aldehyde compound can be produced in high selectivity by a simple operation without using an expensive catalyst or transition metal.
摘要翻译：一种制备由通式（3）表示的芳族醛化合物的方法：（其中R'和n如下所定义），其包括使通式（1）表示的苄基化合物：其中R可以表示氢原子，n表示1〜6的整数，R'可以相同或不同，表示氢原子或烷基，可以具有取代基的烷基或苯基）与溴的氧化合物由公式（2）表示：<？in-line-formula description =“In-line Formulas”end =“lead”？> MBrO （2）<？in-line-formula description （式中，M表示氢原子或金属原子，m表示1〜3的整数）在酸催化剂的存在下进行。根据该方法，通过简单的操作可以高选择性地制备芳族醛化合物，而不使用昂贵的催化剂或过渡金属。

87. 发明申请

US20080051596A1 6-(poly-substituted aryl)-4-aminopicolinates and their use as herbicides 审中-公开
公开(公告)号：US20080051596A1
公开(公告)日：2008-02-28
申请号：US11906973
申请日：2007-10-04
申请人： Terry Balko , John Daeuble , Paul Schmitzer , Carla Yerkes , Thomas Siddall
发明人： Terry Balko , John Daeuble , Paul Schmitzer , Carla Yerkes , Thomas Siddall
IPC分类号： C07C25/24 , C07C211/45 , C07C255/50 , C07C33/46 , C07C381/00 , C07C43/192 , C07C47/14
CPC分类号： C07D213/79 , A01N43/40 , C07C25/13 , C07C39/26 , C07C39/27 , C07C43/225 , C07C47/55 , C07C47/575 , C07C49/80 , C07C211/52 , C07C217/84 , C07C233/25 , C07C233/65 , C07C255/50 , C07C255/54 , C07C323/09 , C07F1/02 , C07F1/08 , C07F3/00 , C07F3/02 , C07F5/025 , C07F7/2208 , A01N25/32
摘要： 4-Aminopicolinic acids having tri- and tetra-substituted aryl substituents in the 6-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.

88. 发明申请

US20080045734A1 6-(poly-substituted aryl)-4-aminopicolinates and their use as herbicides 有权
标题翻译： 6-（多取代芳基）-4-氨基吡啶甲酸盐及其作为除草剂的用途
公开(公告)号：US20080045734A1
公开(公告)日：2008-02-21
申请号：US11906972
申请日：2007-10-04
申请人： Terry Balko , John Daeuble , Paul Schmitzer , Carla Yerkes , Thomas Siddall
发明人： Terry Balko , John Daeuble , Paul Schmitzer , Carla Yerkes , Thomas Siddall
IPC分类号： C07F5/02 , C07F1/08 , C07F7/22
CPC分类号： C07D213/79 , A01N43/40 , C07C25/13 , C07C39/26 , C07C39/27 , C07C43/225 , C07C47/55 , C07C47/575 , C07C49/80 , C07C211/52 , C07C217/84 , C07C233/25 , C07C233/65 , C07C255/50 , C07C255/54 , C07C323/09 , C07F1/02 , C07F1/08 , C07F3/00 , C07F3/02 , C07F5/025 , C07F7/2208 , A01N25/32
摘要： 4-Aminopicolinic acids having tri- and tetra-substituted aryl substituents in the 6-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.
摘要翻译：在6-位上具有三取代和四取代的芳基取代基的4-氨基吡啶甲酸及其胺和酸衍生物是表现出广谱杂草控制的有效除草剂。

89. 发明申请

US20060241300A1 Phosphazenium salt mixtures containing hexakis(amino)diphosphazenium, tetrakis(amino)-phosphonium and polyaminophosphazenium salts 审中-公开
公开(公告)号：US20060241300A1
公开(公告)日：2006-10-26
申请号：US10546502
申请日：2004-02-11
申请人： Thomas Wessel , Daniel Decker , Thomas Sommer , Hagen Huenig , Reinhard Schwesinger
发明人： Thomas Wessel , Daniel Decker , Thomas Sommer , Hagen Huenig , Reinhard Schwesinger
IPC分类号： B01J31/00 , C07F9/02
CPC分类号： B01J31/0268 , B01J31/0239 , B01J31/0265 , B01J2231/40 , C07B39/00 , C07C17/208 , C07C45/63 , C07F9/572 , C07F9/59 , C07C47/55
摘要： The invention relates to mixtures containing 5 to 99.5 wt. % of a compound of formula (I), 95 to 0.5 wt. % of a compound of formula (II) and a maximum of 10 wt. % of one of several compounds of general formula (III a), wherein A1-A32 which are independent from each other are equal or different and represent a straight-chained or branched alkyl or alkenyl having 1-12 carbon atoms, cycloalkyl having 48 carbon atoms, an aryl having 6-12 carbon atoms, an aralkyl having 7-12 carbon atoms, or A1-A2, A3-A4, A5-A6 etc. -A31-A32 which are independent from each other and are equal or different and are connected together directly or via O or N-A33 to a ring having 3-7 ring members, A33 represents an alkyl having 1-4 carbon atoms. X1 and/or X2 and/or X3 which are independent from each other represent a radical of formula (III b), or the radical X1 and/or X2 and/or X3 as well as a straight-chained or branched alkyl or alkenyl having 1-12 carbon atoms, cycloalkyl having 4-8 carbon atoms represent an aryl having 6-12 carbon atoms, an aralkyl having 7-12 carbon atoms, or respectively the radicals which are disposed on an identically bound nitrogen atom, e.g. A1 and A2, A3 and A4, A5 and A6 etc. -A31 and A32 which are independent from each other are equal or different and are connected together directly or via O or N-A33 to a ring having 3-7 ring members and A33 represents an alkyl having 1-4 carbon atoms and B− represents a single-valent organic or inorganic acid radical or the equivalent of a multi-valent acid radical. The mixtures can be used as catalysts and co-catalysts for phase transfer reactions, nucleophilic substitution reactions or halogen-fluoro-exchange reactions.

90. 发明申请

US20060235073A1 Diamino-functional chalcones 失效
标题翻译：二氨基功能查尔酮
公开(公告)号：US20060235073A1
公开(公告)日：2006-10-19
申请号：US10514821
申请日：2003-05-19
申请人： Simon Nielsen , Kristian Schønning , Hasse Kromann , Thomas Boesen , Mogens Larsen
发明人： Simon Nielsen , Kristian Schønning , Hasse Kromann , Thomas Boesen , Mogens Larsen
IPC分类号： A61K31/277 , A61K31/165 , A61K31/137 , C07C255/50 , C07C225/02
CPC分类号： C07C233/36 , C07C45/00 , C07C45/44 , C07C47/277 , C07C47/55 , C07C47/575 , C07C49/813 , C07C217/22 , C07C225/16 , C07C225/22 , C07C233/33 , C07C237/04 , C07C255/56 , C07C311/21 , C07C323/32 , C07D213/65 , C07D295/088 , C07D295/112 , C07D295/185 , C07D307/79 , C07D309/12 , C07D317/66
摘要： The invention provides novel diamino-functionalised chalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic and bacteriostatic agents.
摘要翻译：本发明提供新的二氨基官能化查耳酮衍生物及其类似物。还公开了将化合物或其组合物用于药物活性剂，特别是抗细菌和寄生虫感染的用途。本发明还涉及用于检测对例如细菌，寄生虫，真菌和蠕虫的抑制作用的方法。本发明的查尔酮携带氨基取代基并表现出增强的生物效应以及改善的代谢和物理化学性质，使得该化合物可用作药物物质，特别是作为抗寄生虫和抑菌剂。

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