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1. 发明授权

US6005113A Long wavelength dyes for infrared tracing 失效
标题翻译：用于红外线追踪的长波长染料
公开(公告)号：US6005113A
公开(公告)日：1999-12-21
申请号：US856422
申请日：1997-05-14
申请人： Yexin Wu , Dieter H. Klaubert , Hee Chol Kang , Yu-Zhong Zhang
发明人： Yexin Wu , Dieter H. Klaubert , Hee Chol Kang , Yu-Zhong Zhang
IPC分类号： C09B57/10 , C09K11/06 , C09K3/00 , C09K11/02 , G01N33/546
CPC分类号： C09B57/10 , C09K11/06 , Y10S436/805
摘要： The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron difluoride moiety, forming a fluorescent dibenzopyrrometheneboron difluoride compound ##STR1## that is further substituted by bathochromic substituents that are aryl or heteroaryl moieties further substituted by an additional aryl or heteroaryl, that is itself optionally further substituted by an additional aryl or heteroaryl. These aryl and heteroaryl groups are separated by a covalent bond, or by an ethenyl, butadienyl or hexatrienyl linkage. The dyes of the invention are particularly useful as labels for carriers, particularly polymeric microparticles. The resulting microparticles have a long-wavelength fluorescence emission, and possess utility for tracing flow in biological systems, particularly in tracing blood flow.
摘要翻译：本发明涉及通过两个异吲哚氮结合到二氟化硼部分的1-（异吲哚基）亚甲基 - 异吲哚的取代或未取代的衍生物，形成荧光二苯并吡咯并噻唑二氟化物化合物，其进一步被作为芳基的红移取代基取代或进一步被另外的芳基或杂芳基取代的杂芳基，其本身任选进一步被另外的芳基或杂芳基取代。这些芳基和杂芳基通过共价键或乙烯基，丁二烯基或己三烯基键分离。本发明的染料特别可用作载体，特别是聚合物微粒的标签。所得微粒具有长波长荧光发射，并且具有用于追踪生物系统中的流动的效用，特别是在追踪血流中。

2. 发明授权

US4504660A Process for the production of 2,6-diaminobenzonitrile derivatives 失效
标题翻译： 2,6-二氨基苄腈衍生物的制备方法
公开(公告)号：US4504660A
公开(公告)日：1985-03-12
申请号：US395520
申请日：1982-07-06
申请人： Dieter H. Klaubert , Stanley C. Bell
发明人： Dieter H. Klaubert , Stanley C. Bell
IPC分类号： C07C255/58 , C07D207/04 , C07D295/12 , C07C121/52
CPC分类号： C07C255/00
摘要： 2,6-Diaminobenzonitriles, useful in the production of N-(2-cyano-3-substituted or unsubstituted amino-phenyl)oxamate and N-(2-cyano-3-substituted or unsubstituted amino-phenyl)tetrazole-5-carboxamide antiallergy and antisecretory agents, are prepared by sequential displacement of the fluoro substituents from 2,6-difluorobenzonitrile with the appropriately substituted amine.
摘要翻译：可用于制备N-（2-氰基-3-取代或未取代的氨基 - 苯基）草酸酯和N-（2-氰基-3-取代或未取代的氨基 - 苯基）四唑-5-甲酰胺的2,6-二氨基苯腈抗过敏和抗分泌剂，通过用适当取代的胺将2,6-二氟苄腈中的氟取代基顺序置换而制备。

3. 发明授权

US4495101A Antiinflammatory 5H-tetrazolo (5,1-c)(1,4)benzodiazepine derivatives 失效
标题翻译：抗炎性5H-四唑（5,1-c）（1,4）苯并二氮杂衍生物
公开(公告)号：US4495101A
公开(公告)日：1985-01-22
申请号：US489655
申请日：1983-04-28
申请人： Dieter H. Klaubert , Stanley C. Bell , Thomas W. Pattison , Richard W. Rees
发明人： Dieter H. Klaubert , Stanley C. Bell , Thomas W. Pattison , Richard W. Rees
IPC分类号： C07D257/04 , C07D487/04 , C07D403/00
CPC分类号： C07D257/04 , C07D487/04
摘要： The compounds of the formula ##STR1## in which R is hydrogen, halogen, alkyl, alkoxy, hydroxyl, nitro or cyano; andR.sup.2 is .dbd.O, .dbd.S, H.sub.2, --SCH.sub.3, or an amino group; with the proviso that when R is chloro in 8-position, R.sup.2 must be other than oxygen or sulfur; or a pharmaceutically acceptable salt thereof.
摘要翻译：其中R为氢，卤素，烷基，烷氧基，羟基，硝基或氰基的式“IMAGE”的化合物; 并且R 2为= O，= S，H 2，-SCH 3或氨基; 条件是当R 8为8-位时，R 2必须不同于氧或硫; 或其药学上可接受的盐。

4. 发明授权

US4316037A N-Benzyl and N-substituted benzyl tetrazole-5-carboxylic acids and the preparation thereof 失效
标题翻译： N-苄基和N-取代的苄基四唑-5-羧酸及其制备
公开(公告)号：US4316037A
公开(公告)日：1982-02-16
申请号：US761149
申请日：1977-01-21
申请人： John H. Sellstedt , Dieter H. Klaubert
发明人： John H. Sellstedt , Dieter H. Klaubert
IPC分类号： C07D257/04 , C07D257/02
CPC分类号： C07D257/04
摘要： N-Protected-tetrazole-5-carboxylic acid derivatives of the formula: ##STR1## in which R is --OM, halo or lower alkoxy wherein M is hydrogen, an alkali metal or an alkaline earth metal; andR.sub.1 is phenyl, 4-methoxyphenyl, 2,4-dimethoxyphenyl or 2,4,6-trimethoxyphenyl,are produced by addition of R.sub.1 --CH.sub.2 --N.sub.3 to a lower alkyl cyanoformate followed by saponification, optional acidification, and conversion to the carbonyl halide. The N-protected tetrazole-5-carbonylhalides are intermediates for the production of anti-allergic agents.
摘要翻译：其中R为-OM，卤素或低级烷氧基，其中M为氢，碱金属或碱土金属的N-保护的四唑-5-羧酸衍生物。 R1为苯基，4-甲氧基苯基，2,4-二甲氧基苯基或2,4,6-三甲氧基苯基，是通过将R1-CH2-N3加成到氰基甲酸低级烷基酯中进行皂化，任选酸化，并转化成羰基卤化物。 N-保护的四唑-5-羰基卤化物是用于生产抗过敏剂的中间体。

5. 发明授权

US4054591A 2-Cyano-3-or 4-(substituted amino)oxanilic acid derivatives 失效
标题翻译： 2-氰基-3-或4-（取代的氨基）恶烷酸衍生物
公开(公告)号：US4054591A
公开(公告)日：1977-10-18
申请号：US710481
申请日：1976-08-04
申请人： Dieter H. Klaubert , John H. Sellstedt , Charles J. Guinosso
发明人： Dieter H. Klaubert , John H. Sellstedt , Charles J. Guinosso
IPC分类号： C07D265/26 , C07D295/155 , C07C121/78
CPC分类号： C07D295/155 , C07D265/26
摘要： The 2-cyano-3-or 4-(substituted amino)oxanilic acid derivatives of the formula: ##STR1## in which the group ##STR2## appears in the designated 3- or 4- position and R is -H; an alkali metal; .sup.+ NH.sub.4 ; alkyl of 1 to 6 carbon atoms, inclusive; aralkyl of 7 or 8 carbon atoms; or cycloalkyl of 5 or 6 carbon atoms;R.sup.1 is --H or alkyl of 1 to 9 carbon atoms;R.sup.2 is --H, alkyl of 1 to 9 carbon atoms or cycloalkyl of 3 to 6 carbon atoms;R.sup.1 and R.sup.2, together, with the nitrogen atom to which they are attached, are aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, 4-lower alkyl-piperazinyl, morpholino or thiomorpholino; and pharmaceutically acceptable acid addition salts thereof are anti-allergic agents.
摘要翻译：下式的2-氰基-3-或4-（取代氨基）草氨酸衍生物：其中基团出现在指定的3-或4-位，R为-H; 碱金属; + NH4; 含1-6个碳原子的烷基; 7或8个碳原子的芳烷基; 或5或6个碳原子的环烷基; R1是-H或1至9个碳原子的烷基; R2为-H，1〜9个碳原子的烷基或3〜6个碳原子的环烷基; R 1和R 2与它们所连接的氮原子一起是氮丙啶基，氮杂环丁烷基，吡咯烷基，哌啶基，哌嗪基，4-低级烷基 - 哌嗪基，吗啉代或硫代吗啉代; 及其药学上可接受的酸加成盐是抗过敏剂。

6. 发明授权

US4013647A Morpholine containing tetrazole-5-carboxamide derivatives 失效
标题翻译：含有四唑-5-羧酰胺衍生物的吗啉
公开(公告)号：US4013647A
公开(公告)日：1977-03-22
申请号：US669570
申请日：1976-03-23
申请人： John H. Sellstedt , Dieter H. Klaubert
发明人： John H. Sellstedt , Dieter H. Klaubert
IPC分类号： A61K31/41 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/505 , A61K31/535 , A61K31/54 , C07D213/75 , C07D247/00 , C07D257/04 , C07D277/46 , C07D295/12 , C07D401/12 , C07D403/12 , C07D417/12 , C07D413/02
CPC分类号： C07D417/12 , A61K31/41 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/505 , A61K31/535 , A61K31/54 , C07D213/75 , C07D247/00 , C07D257/04 , C07D277/46 , C07D295/12 , C07D401/12 , C07D403/12 , Y10S514/826
摘要： Anti-allergic agents of N-aromatic 1H-(or 2H) tetrazole-5-carboxamide derivation present the following formulae: ##STR1## in which R.sup.1 is --CN or --CONH.sub.2 ;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, polyhalo(lower)alkyl, lower alkyl carbonyl or carb(lower)alkoxy;X is --CH.sub.2 --, ##STR2## where R.sup.3 is lower alkyl and R.sup.4 is hydrogen or lower alkyl;Or a pharmaceutically acceptable salt thereof.
摘要翻译： N-芳香族1H-（或2H）四唑-5-甲酰胺衍生物的抗过敏剂呈现以下分子式：其中R 1为-CN或-CONH 2; R 2是氢，低级烷基，低级烷氧基，卤素，多卤代（低级）烷基，低级烷基羰基或碳（低级）烷氧基; X是-CH 2 - ，其中R 3是低级烷基，R 4是氢或低级烷基; 或其药学上可接受的盐。

7. 发明授权

US09487520B2 Coelenterazine derivatives and methods of using same 有权
标题翻译： Coelenterazine衍生物及其使用方法
公开(公告)号：US09487520B2
公开(公告)日：2016-11-08
申请号：US13287519
申请日：2011-11-02
申请人： Dieter H. Klaubert , Poncho Meisenheimer , James Unch , Wenhui Zhou
发明人： Dieter H. Klaubert , Poncho Meisenheimer , James Unch , Wenhui Zhou
IPC分类号： C07D487/04 , C07H17/02 , C12Q1/66
CPC分类号： C07D487/04 , C07H17/02 , C12Q1/66
摘要： The invention provides coelenterazine derivatives which are substrates for a non-luminescent enzyme and a pro-substrate for a luminescent enzyme. The invention also provides a method of using the derivatives. The derivatives are of Formula II:

8. 发明授权

US08809529B2 Imidazo[1,2-α]pyrazine derivatives 有权
标题翻译：咪唑并[1,2-α]吡嗪衍生物
公开(公告)号：US08809529B2
公开(公告)日：2014-08-19
申请号：US13287992
申请日：2011-11-02
申请人： Dieter H. Klaubert , Poncho Meisenheimer , James Unch
发明人： Dieter H. Klaubert , Poncho Meisenheimer , James Unch
IPC分类号： C07D495/00
CPC分类号： C12Q1/66 , A01K2217/072 , C07D487/04 , C12N9/0004 , C12N9/0069 , C12N15/52 , C12N2009/02 , C12Y113/12005 , C12Y113/12007
摘要： The present invention provides, among other things, imidazo[1,2-α]pyrazine derivatives according for Formula (Ia) or Formula (Ib). The derivatives are useful in any method which other coelenterazines have been used. For example, the derivatives may be used in a bioluminogenic method to detect the presence of certain compounds or molecules.
摘要翻译：本发明尤其提供根据式（Ia）或式（Ib）的咪唑并[1,2-α]吡嗪衍生物。这些衍生物可用于已经使用其它肠胃蛋白酶的任何方法。例如，衍生物可用于生物发光法以检测某些化合物或分子的存在。

9. 发明授权

US6162931A Fluorinated xanthene derivatives 失效
标题翻译：氟化呫吨衍生物
公开(公告)号：US6162931A
公开(公告)日：2000-12-19
申请号：US631202
申请日：1996-04-12
申请人： Kyle R. Gee , Martin Poot , Dieter H. Klaubert , Wei-Chuan Sun , Richard P. Haugland , Fei Mao
发明人： Kyle R. Gee , Martin Poot , Dieter H. Klaubert , Wei-Chuan Sun , Richard P. Haugland , Fei Mao
IPC分类号： G01N33/48 , C07B61/00 , C07C37/00 , C07C37/055 , C07C39/27 , C07C205/26 , C07C205/37 , C07C209/36 , C07C213/00 , C07C217/82 , C07C245/20 , C07D311/82 , C07D493/10 , C07F9/6561 , C07K1/13 , C07K16/18 , C09B11/00 , C09B11/24 , C09B11/28 , G01N1/30 , G01N21/76 , C07D311/78 , C07D311/88 , C07D471/00
CPC分类号： C09B11/00 , C07C37/055 , C07C41/18 , C07C201/08 , C07C201/12 , C07C205/26 , C07C205/37 , C07C209/10 , C07C213/02 , C07C213/08 , C07C245/20 , C07D311/82 , C09B11/24 , G01N1/30 , Y10S430/116 , Y10S430/126 , C07C39/245 , C07C211/52 , C07C217/84 , C07C215/76 , C07C43/225
摘要： The family of dyes of the invention are fluoresceins and rhodols that are directly substituted on one or more aromatic carbons by fluorine. These fluorine-substituted fluorescent dyes possess greater photostability and have lower sensitivity to pH changes in the physiological range of 6-8 than do non-fluorinated dyes, exhibit less quenching when conjugated to a substance, and possess additional advantages. The dyes of the invention are useful as detectable tracers and for preparing conjugates of organic and inorganic substances.
摘要翻译：本发明的染料族是在一个或多个芳族碳上被氟直接取代的荧光素和二醇。这些氟取代的荧光染料具有更高的光稳定性，并且对于6-8生理范围内的pH变化的敏感性低于非氟化染料，当与物质缀合时表现出较少的淬灭，并且具有额外的优点。本发明的染料可用作可检测的示踪剂并用于制备有机和无机物质的共轭物。

10. 发明授权

US5773469A Diaryl antimicrobial agents 失效
标题翻译：二芳基抗菌剂
公开(公告)号：US5773469A
公开(公告)日：1998-06-30
申请号：US665653
申请日：1996-06-18
申请人： Ramesh M. Kanojia , James P. Demers , Dennis J. Hlasta , Sigmond G. Johnson , Dieter H. Klaubert
发明人： Ramesh M. Kanojia , James P. Demers , Dennis J. Hlasta , Sigmond G. Johnson , Dieter H. Klaubert
IPC分类号： A61K31/137 , A61K31/155 , A61K31/404 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/4465 , C07C43/225 , C07C217/58 , C07C217/60 , C07C217/62 , C07C271/16 , C07C279/08 , C07C279/24 , C07D209/48 , C07D211/70 , C07D213/30 , C07D213/38 , A61K31/135 , C07C217/02 , C07C321/28
CPC分类号： C07D209/48 , A61K31/137 , A61K31/155 , A61K31/404 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/4465 , C07C217/58 , C07C217/60 , C07C217/62 , C07C271/16 , C07C279/08 , C07C279/24 , C07C43/225 , C07D211/70 , C07D213/30 , C07D213/38 , C07B2200/09 , C07C2102/10 , C07C2103/18
摘要： The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.
摘要翻译：本发明涉及以下通式的二芳基抗微生物化合物：其中G，EL，J，q，m，X，Ar，W，p，n和A如本文所述，含有该化合物的药物组合物，其生产及其在治疗细菌感染中的应用。

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