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1. 发明申请

WO0134602A3 PROCESS AND INTERMEDIATES FOR THE PREPARATION OF IMIDAZOLIDINONE ALPHA V INTEGRIN ANTAGONISTS 审中-公开
标题翻译：制备咪达唑酮类药物的方法和中间体V INTEGRIN ANTAGONISTS
公开(公告)号：WO0134602A3
公开(公告)日：2002-01-17
申请号：PCT/US0030361
申请日：2000-11-03
申请人： MERCK & CO INC , JENSEN MARK S , PALUCKI MICHAEL , RIVERA NELO R , WELLS KENNETH M , XIAO YI , WANG YALING , YANG CHUNHUA , YASUDA NOBUYOSHI
发明人： JENSEN MARK S , PALUCKI MICHAEL , RIVERA NELO R , WELLS KENNETH M , XIAO YI , WANG YALING , YANG CHUNHUA , YASUDA NOBUYOSHI
IPC分类号： C07D213/64 , C07D471/04
CPC分类号： C07D213/64 , C07D471/04
摘要： A novel process is provided for the preparation of imidazolidinone alpha v beta 3/ alpha v beta 5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of alpha v beta 3/ alpha v beta 5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.
摘要翻译：提供了一种制备咪唑啉酮αvβ3 /αvβ5整联蛋白拮抗剂的新方法及其中获得的有用的中间体。这些化合物是αvβ3/αvβ5整联蛋白受体的拮抗剂，因此可用于抑制骨吸收和治疗和预防骨质疏松症。还公开了3- {2-氧代-3- [3-（5,6,7,8-四氢 - [1,8]萘啶-2-基） - 丙基]咪唑烷-1-基} -3（S ） - 半水合物形式的（6-甲氧基 - 吡啶-3-基） - 丙酸。

2. 发明申请

WO2004085661A3 PROCESS TO CHIRAL BETA-AMINO ACID DERIVATIVES 审中-公开
标题翻译：酰胺氨基酸衍生物的方法
公开(公告)号：WO2004085661A3
公开(公告)日：2005-03-10
申请号：PCT/US2004008533
申请日：2004-03-19
申请人： MERCK & CO INC , DREHER SPENCER D , IKEMOTO NORIHIRO , NJOLITO EUGENIA , RIVERA NELO R , TELLERS DAVID M , XIAO YI
发明人： DREHER SPENCER D , IKEMOTO NORIHIRO , NJOLITO EUGENIA , RIVERA NELO R , TELLERS DAVID M , XIAO YI
IPC分类号： C07C229/34 , C07D295/185 , C07D487/04 , C07D471/00 , C07C207/00 , C07C229/00 , C07C233/00 , C07C235/00 , C07C237/00 , C07D487/00 , C07D491/00 , C07D495/00
CPC分类号： C07D295/185 , C07B2200/07 , C07C229/34 , C07D487/04
摘要： The present invention relates to a process for the synthesis of chiral beta-amino acid derivatives and in particular to a process for the preparation of enantiomerically enriched beta-amino acid amide inhibitors of dipeptidyl peptidase-IV (DP-IV) which are useful for the treatment of Type 2 diabetes.
摘要翻译：本发明涉及一种合成手性β-氨基酸衍生物的方法，特别涉及制备二肽基肽酶-IV（DP-IV）的对映体富集的β-氨基酸酰胺抑制剂的方法，其可用于治疗2型糖尿病。

3. 发明申请

WO2004087650A2 PROCESS AND INTERMEDIATES FOR THE PREPARATION OF BETA-AMINO ACID AMIDE DIPEPTIDYL PEPTIDASE-IV INHIBITORS 审中-公开
标题翻译：制备β-氨基酸酰胺二磷酸酯酶IV抑制剂的方法和中间体
公开(公告)号：WO2004087650A2
公开(公告)日：2004-10-14
申请号：PCT/US2004008826
申请日：2004-03-23
申请人： MERCK & CO INC , ANGELAUD REMY , ARMSTRONG JOSEPH D III , ASKIN DAVID , BALSELLS JAUME , HANSEN KARL , LEE JAEMOON , MALIGRES PETER E , RIVERA NELO R , XIAO YI , ZHONG YONG-LI
发明人： ANGELAUD REMY , ARMSTRONG JOSEPH D III , ASKIN DAVID , BALSELLS JAUME , HANSEN KARL , LEE JAEMOON , MALIGRES PETER E , RIVERA NELO R , XIAO YI , ZHONG YONG-LI
IPC分类号： C07C229/00 , C07C239/20 , C07D20060101 , C07D205/00 , C07D497/00 , C07D
CPC分类号： C07C239/20 , C07D205/08 , C07D487/04
摘要： A novel process is provided for the preparation of chiral beta-amino acid amide inhibitors of the dipeptidyl peptidase-IV and the useful intermediates obtained therein. The products resulting from the instant process are inhibitors of dipeptidyl peptidase-IV and thereby useful for the treatment of Type 2 diabetes.
摘要翻译：提供了用于制备二肽基肽酶-IV的手性β-氨基酸酰胺抑制剂及其中获得的有用的中间体的新方法。本发明产生的产物是二肽基肽酶-IV的抑制剂，因此可用于治疗2型糖尿病。

5. 发明申请

WO2007120299A2 SIGNAL-ON ARCHITECTURE FOR ELECTRONIC, OLIGONUCLEOTIDE-BASED DETECTORS 审中-公开
标题翻译：用于电子，基于寡核苷酸的检测器的信号建筑
公开(公告)号：WO2007120299A2
公开(公告)日：2007-10-25
申请号：PCT/US2006061358
申请日：2006-11-29
申请人： UNIV CALIFORNIA , XIAO YI , LUBIN ARICA , PLAXCO KEVIN
发明人： XIAO YI , LUBIN ARICA , PLAXCO KEVIN
IPC分类号： C12Q1/68 , C12M1/34
CPC分类号： C12Q1/6825 , G01N27/3277 , C12Q2565/133 , C12Q2563/113 , C12Q2525/205 , C12Q2537/163 , C12Q2537/137 , C12Q2565/525 , C12Q2565/549 , C12Q2565/607
摘要： The invention provides a general "signal-on" architecture for oligonucleotide-based detectors that leads to order of magnitude increases in signal gain and sensitivity as compared to prior art detectors. The detectors of the invention rely on base pairing between two oligonucleotide strands, the sensor strand and the blocker strand. In the 'off position of the detector, i.e., in the absence of target, the blocker strand and sensor strand are base-paired. As shown in FIG. 1, the formation of comparatively rigid, duplex DNA prevents the redox moiety from approaching the electrode surface, thereby suppressing Faradaic currents. When target is added to the system, the target displaces the blocker strand, binds to the sensor strand, liberating the end of the redox-labeled oligonucleotide to produce a flexible element. This, in turn, allows the redox moiety to collide with the electrode surface, producing a readily detectable Faradaic current.
摘要翻译：本发明提供了一种基于寡核苷酸的检测器的通用“信号启动”架构，与现有技术的检测器相比，信号增益和灵敏度的幅度增加了一个数量级。本发明的检测器依赖于两个寡核苷酸链之间的碱基配对，传感器链和阻断链。在检测器的关闭位置，即在没有靶的情况下，阻断链和传感器链是碱基配对的。如图所示。 1，相对刚性的双链DNA的形成防止氧化还原部分接近电极表面，从而抑制法拉第电流。当将靶标加入到系统中时，靶标取代阻断链，结合传感器链，释放氧化还原标记的寡核苷酸的末端以产生柔性元件。这又使得氧化还原部分与电极表面碰撞，产生易于检测的法拉第电流。

6. 发明申请

WO2005073405A3 CATALYTIC POLYNUCLEOTIDE AND ITS USE FOR DETERMINATION OF ANALYTES 审中-公开
标题翻译：催化多核苷酸及其用于测定分析物的用途
公开(公告)号：WO2005073405A3
公开(公告)日：2006-02-16
申请号：PCT/IL2005000097
申请日：2005-01-27
申请人： YISSUM RES DEV CO , WILLNER ITAMAR , XIAO YI , PAVLOV VALERI , GILL RON , NIAZOV TAMARA
发明人： WILLNER ITAMAR , XIAO YI , PAVLOV VALERI , GILL RON , NIAZOV TAMARA
IPC分类号： C12Q1/68 , C12N15/115
CPC分类号： C12N15/115 , C12Q1/6813 , C12Q1/683 , C12Q2521/543 , C12Q2521/331
摘要： A method for the determination of an analyte in a sample, the method comprising: (a) providing a catalytic polynucleotide; (b) contacting the catalytic polynucleotide with the sample so that the catalytic polynucleotide may bind to the analyte; (c) providing assay conditions such that the catalytic polynucleotide produces an optically detectable signal in the presence of the analyte; and (d) detecting the signal, thereby determining the presence of the analyte in the sample. One application of the method is for the detection of telomerase in a biological sample.
摘要翻译：一种用于测定样品中分析物的方法，所述方法包括：（a）提供催化多核苷酸; （b）使催化多核苷酸与样品接触，使得催化多核苷酸可以结合分析物; （c）提供测定条件，使得催化多核苷酸在分析物存在下产生可光学检测的信号; 和（d）检测信号，从而确定样品中分析物的存在。该方法的一个应用是用于检测生物样品中的端粒酶。

7. 发明公开

EP1097151A4 IMPROVED PROCESS FOR SYNTHESIZING CARBAPENEM INTERMEDIATES 审中-公开
标题翻译： VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON CARBAPENEM-ZWISCHENPRODUKTEN
公开(公告)号：EP1097151A4
公开(公告)日：2001-10-24
申请号：EP99932358
申请日：1999-07-09
申请人： MERCK & CO INC
发明人： JENSEN MARK S , YANG CHUNHUA , XIAO YI , WELLS KENNETH M , YASUDA NOBUYOSHI
IPC分类号： C07D477/00 , C07D477/02 , C07D477/06 , C07D477/14
CPC分类号： C07D477/02 , Y02P20/55
摘要： The invention describes an improved process for synthesizing 1-β-methyl-2-hydroxymethyl substituted carbapenems as key intermediates for the synthesis of anti-MRSA carbapenem antibiotics. The synthesis eliminates the use of BU3SnCH2OH and HMPA, which are toxic substances and not amenable to industrial scale production. The novel intermediates are also within the scope of this invention.
摘要翻译：本发明描述了合成1-β-甲基-2-羟甲基取代的碳青霉烯类作为合成抗MRSA碳青霉烯类抗生素的关键中间体的改进方法。该合成消除了使用BU3SnCH2OH和HMPA，它们是有毒物质，不适用于工业规模生产。新型中间体也在本发明的范围内。

8. 发明专利

AT400545T 未知
公开(公告)号：AT400545T
公开(公告)日：2008-07-15
申请号：AT04720790
申请日：2004-03-15
申请人： MERCK & CO INC
发明人： XIAO YI , ARMSTRONG JOSEPH , KRSKA SHANE , NJOLITO EUGENIA , RIVERA NELO , SUN YONGKUI , ROSNER THORSTEN
IPC分类号： C07C209/52 , B01J31/22 , B01J31/24 , C07C227/16 , C07C231/12 , C07C237/20 , C07D487/04 , C07F17/02
摘要： The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.

9. 发明专利

BR0015384A 未知
公开(公告)号：BR0015384A
公开(公告)日：2002-10-08
申请号：BR0015384
申请日：2000-11-03
申请人： MERCK & CO INC
发明人： JENSEN MARK S , PALUCKI MICHAEL , RIVERA NELO R , WELLS KENNETH M , XIAO YI , WANG YALING , YANG CHUNHUA , YASUDA NOBUYOSHI
IPC分类号： C07D213/64 , C07D471/04

10. 发明专利

AU6250799A Process for the synthesis of tin carbapenem intermediates 未知
公开(公告)号：AU6250799A
公开(公告)日：2000-04-03
申请号：AU6250799
申请日：1999-09-10
申请人： MERCK & CO INC
发明人： JENSEN MARK S , YANG CHUNHUA , YASUDA NOBUYOSHI , CONLON DAVID A , XIAO YI
IPC分类号： C07B61/00 , C07F7/22
摘要： The present invention relates to a process for synthesizing novel intermediates of formula III: wherein R1 is a halogen. The intermediate compounds described herein are useful for the preparation of carbapenem compounds.

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