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11. 发明授权

US09499545B2 Piperidinone carboxamide azaindane CGRP receptor antagonists 有权
公开(公告)号：US09499545B2
公开(公告)日：2016-11-22
申请号：US14485259
申请日：2014-09-12
申请人： Merck Sharp & Dohme Corp.
发明人： Ian M. Bell , Mark E. Fraley , Steven N. Gallicchio , Anthony Ginnetti , Helen J. Mitchell , Daniel V. Paone , Donnette D. Staas , Cheng Wang , C. Blair Zartman
IPC分类号： A01N43/42 , A61K31/44 , C07D211/00 , C07D213/00 , C07D215/00 , C07D217/00 , C07D219/00 , C07D221/00 , C07D471/20 , A61K31/435 , C07D471/10
CPC分类号： A61K31/4545 , A61K31/435 , A61K31/438 , C07D471/10 , C07D471/20
摘要： The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

12. 发明授权

US08541343B2 Chemical compounds and their use as pesticides 失效
标题翻译：化学化合物及其作为农药的用途
公开(公告)号：US08541343B2
公开(公告)日：2013-09-24
申请号：US13513627
申请日：2010-11-29
申请人： Thomas Pitterna , Michel Muehlebach , Jurgen Harry Schaetzer
发明人： Thomas Pitterna , Michel Muehlebach , Jurgen Harry Schaetzer
IPC分类号： A01N57/00 , A01N43/36 , A01N43/40 , A01N47/28 , A01N43/42 , A01N43/38 , A61K31/44 , A61K31/40 , C07D215/00 , C07D217/00 , C07D219/00 , C07D221/00 , C07D491/00
CPC分类号： C07D471/10 , A01N43/90 , C07D211/98
摘要： Compounds of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.
摘要翻译：式（I）化合物，其中取代基如权利要求1中所定义，可用作农药。

13. 发明申请

US20110281907A1 COMPOSITIONS AND METHODS FOR INHIBITION OF HEPATOCYTE GROWTH FACTOR RECEPTOR C-MET SIGNALING 失效
标题翻译：抑制肝细胞生长因子受体C-MET信号的组合物和方法
公开(公告)号：US20110281907A1
公开(公告)日：2011-11-17
申请号：US12935646
申请日：2009-03-31
申请人： Donald P. Bottaro , Megan Peach , Marc Nicklaus , Nelly Tan
发明人： Donald P. Bottaro , Megan Peach , Marc Nicklaus , Nelly Tan
IPC分类号： A61K31/473 , A61P35/00 , C07D219/00 , C07D311/82 , A61K31/352
CPC分类号： C07D213/90 , C07D213/85 , C07D239/22 , C07D311/86
摘要： Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met obtained by virtual screening, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided. Formula (I)
摘要翻译：提供了通过虚拟筛选获得的受体酪氨酸激酶c-Met抑制剂的衍生物和类似物，含有c-Met抑制剂的衍生物和类似物的药物组合物。提供了制备c-Met抑制剂的衍生物和类似物的方法及其使用方法。式（I）

14. 发明授权

US07785904B2 High quantum yield acridinium compounds and their uses in improving assay sensitivity 有权
标题翻译：高量子产率吖啶鎓化合物及其在提高测定灵敏度方面的应用
公开(公告)号：US07785904B2
公开(公告)日：2010-08-31
申请号：US11764924
申请日：2007-06-19
申请人： Anand Natrajan , Qingping Jiang , David Sharpe , James Costello
发明人： Anand Natrajan , Qingping Jiang , David Sharpe , James Costello
IPC分类号： G01N33/533 , G01N21/76 , G01N33/53 , C07D219/00
CPC分类号： G01N33/533 , B82Y15/00 , C07D219/04 , C07D219/06 , G01N33/542 , G01N33/582 , G01N33/588 , Y10S435/968 , Y10S436/80 , Y10S436/805
摘要： The present invention relates to hydrophilic, high quantum yield acridinium compounds. It has been discovered that the placement of electron-donating groups in the acridinium ring system increases the amount of light that is emitted by the corresponding acridinium compound when its chemiluminescence is triggered by alkaline peroxide. More specifically, it has been found that the placement of one or two hydrophilic, alkoxy groups at the C-2 and/or C-7 position of the acridinium ring system of acridinium compounds increases their quantum yield and enhances the aqueous solubility of these compounds. The present hydrophilic, high quantum yield, acridinium compounds are useful chemiluminescent labels for improving the sensitivity of immunoassays.
摘要翻译：本发明涉及亲水性高量子产率吖啶鎓化合物。已经发现，当其化学发光由碱性过氧化物触发时，电子给体基团在吖啶环体系中的放置增加了相应的吖啶鎓化合物发射的光的量。更具体地，已经发现，在吖啶鎓化合物的吖啶环体系的C-2和/或C-7位置上放置一个或两个亲水性烷氧基增加其量子产率并增强这些化合物的水溶性。本发明的亲水性，高量子产率的吖啶化合物是有用的化学发光标记，用于提高免疫测定的灵敏度。

15. 发明授权

US07781229B2 Ultra-sensitive chemiluminescent substrates for enzymes and their conjugates 有权
标题翻译：用于酶及其共轭物的超敏感化学发光底物
公开(公告)号：US07781229B2
公开(公告)日：2010-08-24
申请号：US11578601
申请日：2005-04-14
申请人： Brij Pal Giri , Dinesh Dagli , Pritam Singh
发明人： Brij Pal Giri , Dinesh Dagli , Pritam Singh
IPC分类号： G01N33/534 , G01N33/533 , C07D219/00
CPC分类号： C07D405/12 , C07H15/24 , C07H15/26 , C09B15/00 , C12Q1/00 , G01N21/76 , G01N33/531 , G01N33/533 , Y10S436/80 , Y10T436/142222 , Y10T436/143333 , Y10T436/20
摘要： New chemiluminescent compounds, stable in aqueous buffers, for use in biological assaying include acridanebased compounds and (1,2)-dioxetanes. Among the new acridanebased compounds are water-soluble acridanes, enhancer coupled acridanes, bis and trisacridanes as well as acridane-(1,2)-dioxetanes. Among the new (1,2)-dioxetanes are electron deficient group-containing dioxetanes and tethered bis-1,2-dioxetanes. The (1,2)-dioxetanes are useful as substrates for various enzymes. The acridanes can be admixed with an oxidizing agent. An aqueous buffer and, optionally, a stabilizer to form a substrate or reagent formulation useful for assaying, inter alia, HRP.
摘要翻译：在水性缓冲液中稳定的用于生物测定的新化学发光化合物包括吖啶基化合物和（1,2） - 二氧杂环丁烷。在新的吖啶系化合物中有水溶性吖啶，增强剂偶联吖啶，双和三吖啶以及吖啶 - （1,2） - 二氧杂环丁烷。新的（1,2） - 二氧杂环丁烷是含有电子缺乏基团的二氧杂环丁烷和连接的双-1,2-二氧杂环丁烷。（1,2） - 二氧杂环己烷可用作各种酶的底物。吖啶可与氧化剂混合。水性缓冲液和任选的稳定剂，以形成用于特别测定HRP的底物或试剂制剂。

16. 发明授权

US07579448B2 Purification of microbial cell fermentation homogenates 失效
标题翻译：纯化微生物细胞发酵匀浆
公开(公告)号：US07579448B2
公开(公告)日：2009-08-25
申请号：US11609529
申请日：2006-12-12
申请人： Philip M. Lester , Josefine Persson
发明人： Philip M. Lester , Josefine Persson
IPC分类号： C12P21/02 , C07D219/00 , A61K39/395
CPC分类号： C12P21/02
摘要： A method for purifying a desired heterologous polypeptide from microbial fermentation broth or homogenate in which it is produced and solubilized is described. This method involves adding to the broth or homogenate an effective amount of a solution of 6,9-diamino-2-ethoxyacridine lactate (ethacridine lactate) to precipitate host cell impurities under conditions wherein the majority of polypeptide remains soluble, and separating the desired polypeptide from the broth or homogenate. The broth or homogenate containing the ethacridine lactate and polypeptide is also disclosed.
摘要翻译：描述了从其产生和溶解的微生物发酵液或匀浆中纯化所需异源多肽的方法。该方法包括加入肉汤或匀浆有效量的6,9-二氨基-2-乙氧基吖啶乳酸盐（ethacridine lactate）溶液，以沉淀宿主细胞杂质，其中大部分多肽保持可溶性，并分离所需多肽从肉汤或匀浆。还公开了含有乙胺丁胺乳酸盐和多肽的肉汤或匀浆物。

17. 发明授权

US07498323B2 Spiro-piperidine compounds and medicinal use thereof 失效
标题翻译：螺哌啶化合物及其医药用途
公开(公告)号：US07498323B2
公开(公告)日：2009-03-03
申请号：US10553596
申请日：2004-04-16
申请人： Rena Nishizawa , Yoshikazu Takaoka , Hiromu Habashita , Shiro Shibayama , Masaya Kokubo
发明人： Rena Nishizawa , Yoshikazu Takaoka , Hiromu Habashita , Shiro Shibayama , Masaya Kokubo
IPC分类号： A01N43/62 , A01N43/58 , A01N43/60 , A01N43/42 , A61K31/55 , A61K31/50 , A61K31/495 , A61K31/44 , C07D471/04 , C07D471/22 , C07D487/00 , C07D491/00 , C07D495/00 , C07D215/00 , C07D217/00 , C07D219/00 , C07D221/00 , C07D237/00 , C07D239/00 , C07D241/00
CPC分类号： C07D471/10 , A61K31/438
摘要： The present invention relates to a spiro-piperidine compound represented by formula (I): wherein R1 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s); and ring A represents a 5- to 8-membered cyclic group which may have a substituent(s), a salt thereof, an N-oxide thereof, a quaternary ammonium salt thereof or a solvate thereof, or a prodrug thereof. The compounds represented by formula (I) have chemokine antagonistic action, so that they are useful for prevention and/or treatment of various inflammatory diseases, immune diseases such as autoimmune diseases or allergic diseases, or HIV infection.
摘要翻译：本发明涉及由式（I）表示的螺哌啶化合物：其中R1表示氢，可具有取代基的脂族烃基或可具有取代基的环状基团; 环A表示可具有取代基的5至8元环基，其盐，其N-氧化物，其季铵盐或其溶剂合物或其前药。由式（I）表示的化合物具有趋化因子拮抗作用，因此它们可用于预防和/或治疗各种炎性疾病，免疫疾病如自身免疫性疾病或过敏性疾病或HIV感染。

18. 发明申请

US20080185555A1 Acene-based organic semiconductor materials and methods of preparing and using the same 有权
标题翻译：基于乙烯的有机半导体材料及其制备和使用方法
公开(公告)号：US20080185555A1
公开(公告)日：2008-08-07
申请号：US11986017
申请日：2007-11-19
申请人： Antonio Facchetti , Tobin J. Marks , Zhiming M. Wang
发明人： Antonio Facchetti , Tobin J. Marks , Zhiming M. Wang
IPC分类号： C07D241/46 , C07D209/56 , C07F9/02 , C07C49/105 , C09K3/00 , C07C13/48 , C07D219/00 , C07D221/06
CPC分类号： H01L51/0053 , C09B5/62 , H01L51/0545 , H01L51/424 , H01L51/5012 , Y02E10/549 , Y02P70/521
摘要： Acene-based compounds that can be used to prepare n-type semiconductor materials are provided with processes for preparing the same. Composites and electronic devices including n-type semiconductor materials prepared from these compounds also are provided.
摘要翻译：可用于制备n型半导体材料的基于乙烯的化合物具有制备它们的方法。还提供了包括由这些化合物制备的n型半导体材料的复合材料和电子器件。

19. 发明申请

US20080139788A1 ACRIDONE DERIVATIVES AS LABELS FOR FLUORESCENCE DETECTION OF TARGET MATERIALS 有权
公开(公告)号：US20080139788A1
公开(公告)日：2008-06-12
申请号：US11943628
申请日：2007-11-21
申请人： JOHN ANTHONY SMITH , RICHARD MARTIN WEST
发明人： JOHN ANTHONY SMITH , RICHARD MARTIN WEST
IPC分类号： C07H21/00 , C07D401/12 , C07D219/00 , C07K14/765
CPC分类号： G01N33/582 , C09B15/00
摘要： Disclosed are new acridone dye derivatives having characteristic fluorescence lifetimes. Also disclosed are methods for labelling target biological materials employing the acridone dyes and use of the labelled materials in biological assays. The acridone derivatives have the following structure: in which Z1 and Z2 represent the atoms necessary to complete one ring, two fused ring, or three fused ring aromatic or heteroaromatic systems, each ring having five or six atoms selected from carbon atoms and optionally no more than two atoms selected from oxygen, nitrogen and sulphur; R2, R3, R4 and R5 are selected from hydrogen, halogen, amide, hydroxyl, cyano, nitro, mono- or di-nitro-substituted benzyl, amino, mono- or di-C1-C4 alkyl-substituted amino, sulphydryl, carbonyl, carboxyl, C1-C6 alkoxy, acrylate, vinyl, styryl, aryl, heteroaryl, C1-C20 alkyl, aralkyl, sulphonate, sulphonic acid, quaternary ammonium, the group -E-F and the group —(CH2—)nY; R1 is selected from hydrogen, mono- or di-nitro-substituted benzyl, C1-C20 alkyl, aralkyl, the group -E-F and the group —(CH2—)nY; where E is a spacer group, F is a target bonding group; Y is selected from sulphonate, sulphate, phosphonate, phosphate, quaternary ammonium and carboxyl; and n is an integer from 1 to 6. The invention also relates to a set of different fluorescent acridone dye derivatives, each dye having a different fluorescence lifetime, the set of dyes being particularly useful for multiparameter analysis.

20. 发明授权

US07332354B2 Compounds for chemiluminescense procedures 失效
标题翻译：化学发光法的化合物
公开(公告)号：US07332354B2
公开(公告)日：2008-02-19
申请号：US10479320
申请日：2002-05-28
申请人： Dieter Heindl , Rupert Herrmann , Hans-Peter Josel , Erasmus Huber , Ursula Klause
发明人： Dieter Heindl , Rupert Herrmann , Hans-Peter Josel , Erasmus Huber , Ursula Klause
IPC分类号： G01N33/532 , G01N33/533 , C12P7/40 , C07D219/00 , C07D277/62
CPC分类号： C07D401/12 , C07D219/06 , C07D417/04 , C07D417/14 , C12Q1/28 , G01N33/533 , G01N33/582 , Y10S435/968 , Y10S436/80 , Y10S436/904
摘要： The present invention relates to a chemical compound comprising a light emitting moiety precursor and a precursor of a leaving group, bound to each other by an amide or by an ester bond and characterized in that the leaving group precursor upon oxidation is converted into the leaving group. The invention also relates to compounds additionally comprising a coupling group to the use of such compounds for labeling of biomolecules and more generally to the use of such compounds in chemiluminescence detection procedures.
摘要翻译：本发明涉及包含发光部分前体和离去基团的前体的化合物，其通过酰胺或酯键彼此结合，并且其特征在于，离去基团前体在氧化时转化为离去基团。本发明还涉及另外包含使用这种化合物的偶联基团用于标记生物分子的化合物，更一般地，在化学发光检测程序中使用这些化合物。

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