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1. 发明公开

EP2496928A1 METHOD FOR DETERMINING POLYCYCLIC AROMATIC HYDROCARBON CONTAMINANT CONCENTRATION 审中-公开
标题翻译：方法用于确定污染物的浓度在多环芳香族烃的FORM
公开(公告)号：EP2496928A1
公开(公告)日：2012-09-12
申请号：EP10768238.7
申请日：2010-10-21
申请人： Universität für Bodenkultur Wien , Janik, Leslie Joseph
发明人： JANIK, Leslie Joseph , LOIBNER, Andreas Paul , KATTNER, Juergen , EDELMANN, Eva
IPC分类号： G01N21/35 , G01N21/93 , G01N21/27 , G01N21/31
CPC分类号： G01N21/3563 , G01N21/274 , G01N21/314 , G01N21/3504 , G01N21/3577 , G01N21/359 , G01N21/552 , G01N21/93 , G01N2021/3133 , G01N2021/3155 , G01N2021/3595 , G01N2201/1293
摘要： Method for determining polycyclic aromatic hydrocarbon (PAH) concentration in a solid state sample. The method includes exposing the sample to diffuse reflectance infrared spectroscopy, recording at least one spectroscopic parameter of infrared diffuse reflection of the sample, which is a signal obtained at one or more frequencies within a range of frequencies (+/−10 cm−1) selected from the group consisting of 3000-3100 cm−1, 740, 777, 814, 842, 1430, 1510, 1600, 4055-4056, 4642-4646, 5924, and 5951-5953 cm−1, and performing data analysis by correlating the at least one spectroscopic parameter with variables of a trained multivariate calibration model related to PAH concentrations, thereby determining PAH concentrations in the sample.

2. 发明申请

WO2011051166A1 METHOD FOR DETERMINING POLYCYCLIC AROMATIC HYDROCARBON CONTAMINANT CONCENTRATION 审中-公开
标题翻译：多环芳烃污染物浓度测定方法
公开(公告)号：WO2011051166A1
公开(公告)日：2011-05-05
申请号：PCT/EP2010/065911
申请日：2010-10-21
申请人： UNIVERSITÄT FÜR BODENKULTUR WIEN , JANIK, Leslie Joseph , LOIBNER, Andreas Paul , KATTNER, Juergen , EDELMANN, Eva
发明人： JANIK, Leslie Joseph , LOIBNER, Andreas Paul , KATTNER, Juergen , EDELMANN, Eva
IPC分类号： G01N21/35 , G01N21/93 , G01N21/27 , G01N21/31
CPC分类号： G01N21/3563 , G01N21/274 , G01N21/314 , G01N21/3504 , G01N21/3577 , G01N21/359 , G01N21/552 , G01N21/93 , G01N2021/3133 , G01N2021/3155 , G01N2021/3595 , G01N2201/1293
摘要： The invention refers to the use of a device for determining PAH concentration in a solid state sample, which device comprises a) means for exposing the sample to diffuse reflectance infrared spectroscopy, b) detecting means for recording at least one spectroscopic parameter of infrared diffuse reflection of said sample, which is a signal obtained at one or more frequencies within a range of frequencies (+/- 10 cm -1 ) selected from the group consisting of 3000-3100 cm -1 , 740, 777, 814, 842, 1430, 1510, 1600, 4055- 4056, 4642-4646, 5924, and 5951-5953 cm -1 , and c) computing means for performing data analysis by correlating the at least one spectroscopic parameter with variables of a trained multivariate calibration model related to PAH concentrations, thereby obtaining prediction of PAH concentrations in the sample, and a method of determining a PAH concentration by diffuse reflectance infrared spectroscopy.
摘要翻译：本发明涉及用于测定固体样品中PAH浓度的装置，该装置包括：a）将样品暴露于漫反射红外光谱的装置，b）用于记录红外漫反射的至少一个光谱参数的检测装置所述样本是在选自3000-3100cm -1，740,777,814,842,1430的频率（+/- 10cm -1）范围内的一个或多个频率处获得的信号，1510,1600,4055-40546,4642-4646,5924和5951-5953cm-1，以及c）用于通过将所述至少一个光谱参数与经训练的多变量校准模型的变量相关联来执行数据分析的计算装置 PAH浓度，从而获得样品中PAH浓度的预测，以及通过漫反射红外光谱法测定PAH浓度的方法。

3. 发明申请

WO2006134341A1 THERAPEUTIC AGENTS 审中-公开
标题翻译：治疗药剂
公开(公告)号：WO2006134341A1
公开(公告)日：2006-12-21
申请号：PCT/GB2006/002156
申请日：2006-06-13
申请人： MERCK SHARP & DOHME LIMITED , BLACKABY, Wesley, Peter , HUSCROFT, Ian, Thomas , KEOWN, Linda, Elizabeth , LEWIS, Richard, Thomas , RAUBO, Piotr, Antoni , STREET, Leslie, Joseph , THOMSON, Christopher, George , THOMSON, Joanne
发明人： BLACKABY, Wesley, Peter , HUSCROFT, Ian, Thomas , KEOWN, Linda, Elizabeth , LEWIS, Richard, Thomas , RAUBO, Piotr, Antoni , STREET, Leslie, Joseph , THOMSON, Christopher, George , THOMSON, Joanne
IPC分类号： C07C317/32 , C07D249/04 , C07D211/26 , C07D207/09 , A61K31/16 , A61K31/4192 , A61K31/435 , A61K31/40 , A61P25/18
CPC分类号： C07D249/04 , C07C317/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/08 , C07D207/09 , C07D211/26 , C07D211/28 , C07D211/60 , C07D213/40 , C07D249/12 , C07D295/067 , C07D309/04 , C07D401/12
摘要： A compound of the formula (I): wherein R 1 ,R 2 ,R 3 , R 4 ,Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are their use in medicine, for example in the treatment of schizophrenia.
摘要翻译：式（I）的化合物：其中R 1，R 2，R 3，R 4， Ar，A，n和m在本文中定义，公开为GlyT1抑制剂; 还公开了含有式（I）化合物的药物组合物，它们在医学中的用途，例如在精神分裂症的治疗中。

4. 发明申请

WO2003093273A1 IMIDAZO-TRIAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：咪达唑啶衍生物作为GABA受体的配体
公开(公告)号：WO2003093273A1
公开(公告)日：2003-11-13
申请号：PCT/GB2003/001957
申请日：2003-05-01
申请人： MERCK SHARP & DOHME LIMITED , CHAMBERS, Mark, Stuart , GOODACRE, Simon, Charles , HALLETT, David, James , MAXEY, Robert, James , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
发明人： CHAMBERS, Mark, Stuart , GOODACRE, Simon, Charles , HALLETT, David, James , MAXEY, Robert, James , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A class of imidazo[1,2 b ][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABA A receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类由任选取代的五元或六元杂芳环在7-位取代的咪唑并[1,2b] [1,2,4]三嗪衍生物是GABA 受体的选择性配体，特别是对α2和/或α3和/或α5亚基具有良好亲和力，因此在治疗和/或预防中枢神经系统的不良状况（包括焦虑，惊厥和认知障碍）方面是有益的。

5. 发明申请

WO2003093272A1 IMIDAZO-TRIAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：咪达唑啶衍生物作为GABA受体的配体
公开(公告)号：WO2003093272A1
公开(公告)日：2003-11-13
申请号：PCT/GB2003/001888
申请日：2003-05-01
申请人： MERCK SHARP & DOHME LIMITED , BETTATI, Michela , CHAMBERS, Mark, Stuart , GOODACRE, Simon, Charles , HALLETT, David, James , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
发明人： BETTATI, Michela , CHAMBERS, Mark, Stuart , GOODACRE, Simon, Charles , HALLETT, David, James , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A class of 7-phenylimidazo[1,2- b ][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a -NH- linkage, and substituted on the phenyl ring by one or two further substituents as defined herein, being selective ligands for GABA A receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类7-苯基咪唑并[1,2-b] [1,2,4]三嗪衍生物，其在苯环的间位被任选取代的被氧原子连接或桥连的芳基或杂芳基取代或-NH-键，并且在苯环上被如本文所定义的一个或两个另外的取代基取代，是GABA A受体的选择性配体，特别是对α2和/或α3和/或其α5亚基具有良好的亲和力。因此在治疗和/或预防中枢神经系统的不利条件方面有益，包括焦虑，抽搐和认知障碍。

6. 发明申请

WO2003018546A2 TRICYCLIC PYRIDIN-2-ONE ANALOGUES AS LIGANDS FOR GABA-A RECEPTORS 审中-公开
标题翻译：作为GABA-A受体配体的三聚吡啶-2-酮类似物
公开(公告)号：WO2003018546A2
公开(公告)日：2003-03-06
申请号：PCT/GB2002/003703
申请日：2002-08-12
申请人： MERCK SHARP & DOHME LIMITED , BOURRAIN, Sylvie , GOODACRE, Simon, Charles , HALLETT, David, James , LEWIS, Richard, Thomas , ROWLEY, Michael , STERNFELD, Francine , STREET, Leslie, Joseph
发明人： BOURRAIN, Sylvie , GOODACRE, Simon, Charles , HALLETT, David, James , LEWIS, Richard, Thomas , ROWLEY, Michael , STERNFELD, Francine , STREET, Leslie, Joseph
IPC分类号： C07D
CPC分类号： C07D471/14
摘要： A class of selectively substituted fused tricyclic compounds based on a substituted pyridinone moiety are potent and functionally selective ligands for the α2/α3 subunit of the human GABA-A receptor and are thereby effective in the treatment of anxiety.
摘要翻译：一类基于取代的吡啶酮部分的选择性取代的稠合三环化合物是人类GABA-A受体的α2/α3亚基的有效和功能选择性配体，因此有效治疗焦虑症。

7. 发明申请

WO0012505A3 TRIAZOLOPYRIDAZINE DERIVATIVES FOR TREATING ANXIETY AND ENHANCING COGNITION 审中-公开
标题翻译：用于治疗厌食症和增强感觉的三唑吡啶衍生物
公开(公告)号：WO0012505A3
公开(公告)日：2000-06-08
申请号：PCT/GB9902737
申请日：1999-08-20
申请人： MERCK SHARP & DOHME , LADDUWAHETTY TAMARA , MERCHANT KEVIN JOHN , STERNFELD FRANCINE , STREET LESLIE JOSEPH
发明人： MERCHANT KEVIN JOHN , STERNFELD FRANCINE , STREET LESLIE JOSEPH
IPC分类号： A61K31/5025 , A61P25/22 , A61P25/28 , C07D487/04 , A61K31/4985
CPC分类号： C07D487/04
摘要： A compound of formula (I), or a salt or prodrug thereof wherein: Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl, di(C1-6)alkylamino or C6-12 bicycloalkyl, any of which groups may be optionally substituted; R represents an optionally substituted five-membered heteroaromatic ring selected from pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or R represents an optionally substituted six-membered heteroaromatic ring selected from pyridine, pyrazine, pyrimidine and pyridazine; and R represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alkyl, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.
摘要翻译：式（I）化合物或其盐或前药，其中：Z表示C 1-6烷基，C 3-7环烷基，C 4-7环烯基，芳基，C 3-7杂环烷基，杂芳基，二（C 1-6）烷基氨基或 C 6-12双环烷基，其任何基团可以任选被取代; R 1表示选自吡咯，恶唑，噻唑，异恶唑，异噻唑，咪唑，吡唑，恶二唑，噻二唑，三唑和四唑的任选取代的五元杂芳环; 或R 1表示任选取代的六元杂芳环，其选自吡啶，吡嗪，嘧啶和哒嗪; 并且R 2表示氰基（C 1-6）烷基，羟基（C 1-6）烷基，C 3-7环烷基（C 1-6）烷基，炔丙基，C 3-7杂环烷基羰基（C 1-6）烷基， 6）烷基或杂芳基（C 1-6）烷基，其中任何基团可任选被取代; 其用于治疗焦虑症和包含它的药物组合物; 还公开了可用于增强认知的化合物的亚类，例如阿尔茨海默氏病。

8. 发明申请

WO1998003504A1 AMINOCYCLOHEXANE DERIVATIVES AS 5-HT RECEPTOR AGONISTS 审中-公开
标题翻译：氨基胆碱衍生物作为5-HT受体激动剂
公开(公告)号：WO1998003504A1
公开(公告)日：1998-01-29
申请号：PCT/GB1997001897
申请日：1997-07-15
申请人： MERCK SHARP & DOHME LIMITED , MACLEOD, Angus, Murray , SHOWELL, Graham, Andrew , STREET, Leslie, Joseph
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D403/04
CPC分类号： C07D231/12 , C07D209/14 , C07D233/56 , C07D249/08
摘要： A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D alpha receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT1D alpha receptor subtype relative to the 5-HT1D beta subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
摘要翻译：一类取代的氨基环己烷衍生物是5-HT1样受体的选择性激动剂，它是人5-HT1Dα受体亚型的有效激动剂，同时对5-HT1Dα受体亚型具有至少10倍的选择性亲和力 5-HT1D beta亚型; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

9. 发明申请

WO1993023396A1 FUSED IMIDAZOLE AND TRIAZOLE DERIVATIVES AS 5-HT1 RECEPTOR AGONISTS 审中-公开
标题翻译：作为5-HT1受体激动剂的咪唑并噻唑衍生物
公开(公告)号：WO1993023396A1
公开(公告)日：1993-11-25
申请号：PCT/GB1993000936
申请日：1993-05-06
申请人： MERCK SHARP & DOHME LIMITED , STREET, Leslie, Joseph
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D473/00
摘要： Compounds of formula (I) wherein Q represents the residue of a six-membered aromatic or heteroaromatic nucleus containing zero, one or two nitrogen atoms; V represents nitrogen or C-A ; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula (a); U represents nitrogen or C-R ; B represents oxygen, sulphur or N-R ; R represents -CH2.CHR .NR R or a group of formula (i), (ii), (iii) or (iv); are selective agonists of 5-HT1-like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
摘要翻译：式（I）的化合物，其中Q表示含有零个，一个或两个氮原子的六元芳族或杂芳族核的残基; V表示氮或C-A 2; E表示含有1至4个碳原子的键或直链或支链亚烷基链; F表示式（a）的基团。 U表示氮或C-R 2; B表示氧，硫或N-R 3; R 1表示-CH 2 CHR 4，R 6 R 7或式（i），（ii），（iii）或（iv）的基团。是5-HT1样受体的选择性激动剂，因此可用于治疗临床状况，特别是偏头痛和相关疾病，其中指出了这些受体的选择性激动剂。

10. 发明申请

WO2011035391A1 METHOD OF CONTAMINANT PREDICTION 审中-公开
标题翻译：污染物预测方法
公开(公告)号：WO2011035391A1
公开(公告)日：2011-03-31
申请号：PCT/AU2010/001261
申请日：2010-09-24
申请人： COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ORGANISATION , FORRESTER, Sean, Thomas , JANIK, Leslie, Joseph , McLAUGHLIN, Michael, John
发明人： FORRESTER, Sean, Thomas , JANIK, Leslie, Joseph , McLAUGHLIN, Michael, John
IPC分类号： G01N21/35 , G01N21/47 , G01N33/24
CPC分类号： G01N21/359 , G01N21/3563 , G01N33/241 , G01N2201/129
摘要： Disclosed is a method of selectively predicting hydrocarbon concentration in a sample of unknown hydrocarbon concentration (the unknown sample). The method comprises the steps of: (i) separately subjecting two or more samples of known hydrocarbon concentration to infrared (IR) radiation; (ii) separately detecting an IR signal from the samples of known hydrocarbon concentration; (iii) analysing the IR signals using a multivariate chemometric technique to produce a training data set; (iv) generating a predictive model for hydrocarbon concentration based on the training data set; (v) subjecting the unknown sample to infrared (IR) radiation; (vi) detecting an IR signal from the unknown sample; (vii) applying the predictive model to the IR signal from the unknown sample; and thereafter (viii) selectively predicting hydrocarbon concentration in the unknown sample. Also disclosed is a method for generating a model to selectively predict hydrocarbon concentration in a sample of unknown hydrocarbon concentration and a software program for selectively predicting hydrocarbon concentration from inputted IR signal data of an unknown sample.
摘要翻译：公开了选择性地预测未知烃浓度的样品中的烃浓度的方法（未知样品）。该方法包括以下步骤：（i）将已知烃浓度的两个或多个样品分别经受红外（IR）辐射; （ii）从已知烃浓度的样品中分别检测IR信号; （iii）使用多变量化学计量技术分析IR信号以产生训练数据集; （iv）基于训练数据集生成烃浓度预测模型; （v）使未知样品经受红外（IR）辐射; （vi）检测来自未知样品的IR信号; （vii）将预测模型应用于来自未知样本的IR信号; （viii）有选择地预测未知样品中的烃浓度。还公开了一种生成用于选择性地预测未知烃浓度的样品中的烃浓度的模型的方法和用于从未知样品的输入的IR信号数据中选择性地预测烃浓度的软件程序。

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