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1. 发明授权

US06693201B1 Fluorescent photochromic fulgides, particularly for optical memories 失效
标题翻译：荧光光致变色俘获物，尤其适用于光记忆体
公开(公告)号：US06693201B1
公开(公告)日：2004-02-17
申请号：US09391280
申请日：1999-09-07
申请人： Peter M. Rentzepis , Alexander Dvornikov
发明人： Peter M. Rentzepis , Alexander Dvornikov
IPC分类号： C07D40506
CPC分类号： C07D405/06 , G02B5/23 , G11B7/246 , G11B2007/24624
摘要： Photochromic chemicals consisting essentially of colored fluorescent heterocyclic fulgides are particularly suitable for optical memories. The preferred heterocyclic photochromic fulgides consist essentially of colored 2-indolyfulgides capable of excitation by ultraviolet light to fluoresce. These heterocyclic photochromic fulgides are preferably synthesized by process of (1) condensation of 1,3-dimethyl-(5-substituted)indole-2-carboxaldehyde with diethyl IV iospropylidenesuccinate as a key intermediate; followed by (2) hydrolysis; and (3) intramolecular acid anhydride formation.
摘要翻译：基本上由有色荧光杂环捕捉剂组成的光致变色化学品尤其适用于光学存储器。优选的杂环光致变色捕捉剂基本上由能够通过紫外光激发而发出荧光的有色2-取代残基组成。这些杂环光致变色捕捉剂优选通过以下方法合成：（1）1,3-二甲基 - （5-取代的）吲哚-2-甲醛与作为关键中间体的IV ios-丙二烯基琥珀酸二乙酯的缩合; （2）水解; 和（3）分子内酸酐形成。

2. 发明授权

US06180651B2 Diarylmethylidenefuran derivatives, processes for their preparation and their uses in therapeutics 有权
标题翻译：二芳基亚甲基衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US06180651B2
公开(公告)日：2001-01-30
申请号：US09150388
申请日：1998-09-09
申请人： Eric Nicolai , Jean-Marie Teulon
发明人： Eric Nicolai , Jean-Marie Teulon
IPC分类号： C07D40506
CPC分类号： C07D307/58 , C07D405/06
摘要： The present invention relates to derivatives of the formula the process for their preparation, and to their uses in therapeutics, especially as drugs with anti-inflammatory, analgesic and chemopreventive properties.
摘要翻译：本发明涉及其制备方法的制剂衍生物及其在治疗学中的用途，特别是具有抗炎，止痛和化学预防性能的药物。

3. 发明授权

US06818649B2 Chromenylmethyl pyrimidinediamines as antibacterial agents 失效
标题翻译：色烯基甲基嘧啶二酮作为抗菌剂
公开(公告)号：US06818649B2
公开(公告)日：2004-11-16
申请号：US10258777
申请日：2002-10-28
申请人： Peter Mohr , Philippe Pflieger
发明人： Peter Mohr , Philippe Pflieger
IPC分类号： C07D40506
CPC分类号： C07D405/06 , C07D409/14 , C07D491/10 , C07D493/10 , C07F7/0814
摘要： This invention is concerned with substituted chromene derivatives of the general formula (I) in which R1-R4 are as defined in the specification and claims. The invention further relates to the pharmaceutically acceptable acid addition salts of these compounds, their use as therapeutically active substances; medicaments based on these substances, optionally in combination with sulphonamides, and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula (I) and their pharmaceutically acceptable acid addition salts and intermediates for their manufacture.
摘要翻译：本发明涉及通式（I）的取代的色烯衍生物，其中R 1 -R 4如说明书和权利要求中所定义。本发明还涉及这些化合物的药学上可接受的酸加成盐，它们作为治疗活性物质的用途; 基于这些物质的药物，任选地与磺酰胺组合，以及它们的生产; 使用这些物质作为药物和生产抗菌活性药物; 以及式（I）化合物及其药学上可接受的酸加成盐和其制备中间体的制备。

4. 发明授权

US06436964B1 Piperidine derivatives having effects on serotonin related systems 失效
标题翻译：哌啶衍生物对血清素相关系统有影响
公开(公告)号：US06436964B1
公开(公告)日：2002-08-20
申请号：US09701406
申请日：2000-11-28
申请人： Larry Wayne Hertel , Daniel Timothy Kohlman , Sidney Xi Liang , David Taiwai Wong , Yao-Chang Xu
发明人： Larry Wayne Hertel , Daniel Timothy Kohlman , Sidney Xi Liang , David Taiwai Wong , Yao-Chang Xu
IPC分类号： C07D40506
CPC分类号： C07D401/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention provides the compounds of the following formula: Wherein the variables are as defined in the specification and a method for inhibiting the reuptake of seretonin, antagonizing the 5-HT1A receptor and antagonizing the 5-HT2A receptor which comprises administering to a subject in need of such treatment an effective amount of the compound of above formula.
摘要翻译：本发明提供了下列化合物：其中变量如本说明书中所定义，并且抑制依赖顿因子再摄取的方法，拮抗5-HT 1A受体和拮抗5-HT 2A受体，其包括向受试者施用需要这样的治疗有效量的上式化合物。

5. 发明授权

US06274736B1 Chromatographic enantiomer separation of lactones 失效
标题翻译：内酯色谱对映异构体分离
公开(公告)号：US06274736B1
公开(公告)日：2001-08-14
申请号：US09380332
申请日：1999-09-03
申请人： Walter Lange , Rolf Grosser , Burkhard Köhler , Stefan Michel , Bruno Bömer , Uwe Zweering
发明人： Walter Lange , Rolf Grosser , Burkhard Köhler , Stefan Michel , Bruno Bömer , Uwe Zweering
IPC分类号： C07D40506
CPC分类号： C07D405/06 , C07B2200/07 , C07D309/30 , G01N30/02 , G01N30/48 , B01D15/3833
摘要： The present invention relates to the use of optically active polymers of N-acryloyl-phenylalanine neomenthylamide as such, in crosslinked form and/or in carrier-bonded form as stationary phases for the chromatographic separation of enantiomers of lactones.
摘要翻译：本发明涉及N-丙烯酰基 - 苯丙氨酸新戊酰胺的光学活性聚合物作为固定相的交联形式和/或载体键合形式用于内酯对映异构体的色谱分离。

6. 发明授权

US06689889B2 Chromatographic separation of enantiomers of lactones 失效
标题翻译：内酯对映异构体的色谱分离
公开(公告)号：US06689889B2
公开(公告)日：2004-02-10
申请号：US09757919
申请日：2001-01-10
申请人： Walter Lange , Rolf Grosser , Burkhard Köhler , Stefan Michel , Bruno Bömer , Uwe Zweering
发明人： Walter Lange , Rolf Grosser , Burkhard Köhler , Stefan Michel , Bruno Bömer , Uwe Zweering
IPC分类号： C07D40506
CPC分类号： C07D405/06 , C07B2200/07 , C07D309/30 , G01N30/02 , G01N30/48 , B01D15/3833
摘要： The present invention relates to the use of optically active polymers of N-acryloyl-phenylalanine neomenthylamide as such, in crosslinked form and/or in carrier-bonded form as stationary phases for the chromatographic separation of enantiomers of lactones.
摘要翻译：本发明涉及N-丙烯酰基 - 苯丙氨酸新戊酰胺的光学活性聚合物作为固定相的交联形式和/或载体键合形式用于内酯对映异构体的色谱分离。

7. 发明授权

US06608200B1 Process for the preparation of N-(2,3-Dihydrobenzo[1,4]dioxin-2-carbonyl)piperazine 有权
标题翻译：制备N-（2,3-二氢苯并[1,4]二恶英-2-羰基）哌嗪的方法
公开(公告)号：US06608200B1
公开(公告)日：2003-08-19
申请号：US10266991
申请日：2002-10-07
申请人： Malladi Pardhasaradhi , Gullapalli Kumaraswamy , Arun Kanti Das , Nivedita Jena , Chembumkulam Kamalakshyamma Snehalatha Nair , Mudiganti Naga Venkata Sastry
发明人： Malladi Pardhasaradhi , Gullapalli Kumaraswamy , Arun Kanti Das , Nivedita Jena , Chembumkulam Kamalakshyamma Snehalatha Nair , Mudiganti Naga Venkata Sastry
IPC分类号： C07D40506
CPC分类号： C07D319/20
摘要： Described herein is an improved process for the preparation of N-(2,3-Dihydrobenzo[1,4]dioxin-2-carbonyl)piperazine which includes heating a reaction mixture ethyl of 2,3-dihydrobenzo[1,4]dioxin-2-carboxylate and piperazine. The reaction mixture is then subjected to series of washes and extraction to yield N-(2,3-Dihydrobenzo[1,4]dioxin-2-carbonyl)piperazine having a purity of greater than 99.9%.
摘要翻译：本文描述了制备N-（2,3-二氢苯并[1,4]二恶英-2-羰基）哌嗪的改进方法，其包括加热2,3-二氢苯并[1,4]二恶英 - 2-羧酸乙酯和哌嗪。然后将反应混合物进行一系列洗涤和萃取，得到纯度大于99.9％的N-（2,3-二氢苯并[1,4]二恶英-2-羰基）哌嗪。

8. 发明授权

US06476235B2 Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide 失效
标题翻译：合成5-（4-氟苯基）-1- [2 - （（2R，4R）-4-羟基-6-氧代 - 四氢 - 吡喃-2-基） - 乙基] -2-异丙基-4 - 苯基-1H-吡咯-3-甲酸苯基酰胺
公开(公告)号：US06476235B2
公开(公告)日：2002-11-05
申请号：US10015558
申请日：2001-12-17
申请人： Donald Eugene Butler , Randall Lee DeJong , Jade Douglas Nelson , Michael Gerard Pamment , Timothy Lee Stuk
发明人： Donald Eugene Butler , Randall Lee DeJong , Jade Douglas Nelson , Michael Gerard Pamment , Timothy Lee Stuk
IPC分类号： C07D40506
CPC分类号： C07D295/185 , C07D207/34 , C07D207/416 , C07D405/06
摘要： An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight operations or fewer to the desired product, as well as other valuable intermediates used in the process.
摘要翻译：制备5-（4-氟苯基）-1- [2 - （（2R，4R）-4-羟基-6-氧代 - 四氢 - 吡喃-2-基） - 乙基] -2-异丙基的改进方法描述了通过新的合成的4-苯基-1H-吡咯-3-羧酸苯基酰胺，其中将氰基乙酸甲酯转化为八个或更少的操作至所需产物，以及在该方法中使用的其它有价值的中间体。

9. 发明授权

US06172085B2 Cyclic ether compounds as sodium channel modulators 失效
标题翻译：环状醚化合物作为钠通道调节剂
公开(公告)号：US06172085B2
公开(公告)日：2001-01-09
申请号：US09242067
申请日：1999-02-08
申请人： Shigenori Ohkawa , Tadatoshi Hashimoto , Kohji Fukatsu
发明人： Shigenori Ohkawa , Tadatoshi Hashimoto , Kohji Fukatsu
IPC分类号： C07D40506
CPC分类号： C07D405/06 , C07D307/81 , C07D407/12
摘要： A compound of the formula: wherein R1 and R2 each represents hydrogen, lower alkyl which may be substituted or acyl; R3, R4 and R5 each represents lower alkyl which may be substituted or lower alkoxy which may be substituted or R4 and R5 taken together represent a 5- or 6-membered carbocyclic group; R6 represents lower alkyl; Ar represents an aromatic group which may be substituted; ring A represents a 5- to 8-membered nitrogen-containing heterocyclic ring which may be substituted; X represents lower alkylene which may be substituted; Y represents carbon or nitrogen; Za represents CH2, COCH2, OCH2, SCH2, NHCH2, etc.; Zb represents a bond or a divalent aliphatic hydrocarbon group which may be substituted and may contain O, N or S; and m represents an integer of 1 to 3, or a salt thereof is useful for a pharmaceutical composition for modulating sodium channel.
摘要翻译：下式的化合物：其中R1和R2各自表示氢，可被取代的或低级烷基的酰基; R 3，R 4和R 5各自表示可以被取代的低级烷基或可被取代的低级烷氧基，或者R 4和R 5一起代表5-或6-元碳环基; R6代表低级烷基; Ar表示可以被取代的芳基; 环A表示可以被取代的5至8元含氮杂环; X表示可以被取代的低级亚烷基; Y表示碳或氮; Za表示CH2，COCH2，OCH2，SCH2，NHCH2等; Zb表示可以被取代并可以含有O，N或S的键或二价脂族烃基; m表示1〜3的整数，或其盐可用于调制钠通道的药物组合物。

10. 发明授权

US06613905B1 Chemokine receptor antagonists and methods of use therefor 失效
公开(公告)号：US06613905B1
公开(公告)日：2003-09-02
申请号：US09148823
申请日：1998-09-04
申请人： Jay R. Luly , Yoshisuke Nakasato , Etsuo Ohshima
发明人： Jay R. Luly , Yoshisuke Nakasato , Etsuo Ohshima
IPC分类号： C07D40506
CPC分类号： C07D401/06 , C07D211/46 , C07D211/52 , C07D313/12 , C07D405/06 , C07D409/06 , C07D471/04 , C07D491/04 , C07D495/04
摘要： Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.

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