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61. 发明申请

US20040014168A1 Reagents and methods for library synthesis and screening 审中-公开
标题翻译：用于图书馆合成和筛选的试剂和方法
公开(公告)号：US20040014168A1
公开(公告)日：2004-01-22
申请号：US10243974
申请日：2002-09-13
申请人： Howard Hughes Medical Institute
发明人： Stuart L. Schreiber , Helen E. Blackwell , Lucy Perez Fernandez , John A. Tallarico
IPC分类号： C12P021/06 , C08G063/48 , C08G063/91
CPC分类号： C07D311/78 , C07B2200/11 , C40B40/00
摘要： The invention provides novel solid supports for the synthesis of compound libraries. The solid supports have the physical capacity to deliver at least 50 nmol of compound and are functionalized with a silicon-containing linker. In one embodiment of the invention the solid support comprises a bead having a diameter of between approximately 400 and 600 nullm functionalized with a silicon-containing linker. According to certain embodiments of the invention the bead is a polystyrene bead. According to certain embodiments of the invention the linker is a diisopropylalkyl-substituted silyl ether. The invention further provides grafted polymeric supports such as lanterns functionalized with a silicon-containing linker. The invention provides methods for screening in which compounds are synthesized on solid supports in a quantity so that a single solid support such as a bead provides a stock solution sufficient to perform hundreds or thousands of biological or chemical assays. The methods include decoding the sequence of chemical reactions used to synthesize the compound by identifying tags incorporated into the compound during synthesis.
摘要翻译：本发明提供用于合成化合物文库的新型固体载体。固体载体具有递送至少50nmol化合物的物理能力，并用含硅连接体官能化。在本发明的一个实施方案中，固体支持物包含直径为约400-600μm的用含硅连接体官能化的珠粒。根据本发明的某些实施方案，珠是聚苯乙烯珠。根据本发明的某些实施方案，连接体是二异丙基烷基取代的甲硅烷基醚。本发明还提供接枝聚合物载体，例如用含硅接头官能化的灯。本发明提供筛选方法，其中化合物在固体支持物上合成，其量使得单个固体支持物如珠提供足以进行数百或数千种生物或化学测定的储备溶液。所述方法包括通过鉴定合成期间掺入到化合物中的标记来解码用于合成化合物的化学反应序列。

62. 发明申请

US20030096117A1 Chromene compound 有权
标题翻译：色烯化合物
公开(公告)号：US20030096117A1
公开(公告)日：2003-05-22
申请号：US09958843
申请日：2001-10-15
发明人： Yuichiro Kawabata , Yasuko Takeda , Junji Momoda , Hironobu Nagoh , Shinobu Izumi
IPC分类号： C07D321/00 , B32B009/04
CPC分类号： G03C1/685 , C07D311/78 , C07D311/94 , C07D311/96 , C07D405/04 , C07D405/10 , C07D409/04 , C07D409/10 , C07D491/04 , C07D491/10 , C07D493/04 , C07D493/10 , C07D495/04 , C07D495/10 , C09K9/02 , C09K2211/1011 , C09K2211/1029 , C09K2211/1033 , C09K2211/1037 , C09K2211/1088 , G03C1/73 , Y10T428/31504
摘要： Novel chromene compounds having various substituents to exhibit a high color-developing sensitivity and a high density even when dispersed in a high-molecular matrix, and exhibiting a large fading rate, less color when deteriorated, and excellent light resistance in the photochromic properties; photochromic materials containing the chromene compounds; and use thereof.
摘要翻译：具有各种取代基的新型色烯化合物即使分散在高分子基质中也具有高的显色灵敏度和高密度，并且表现出大的褪色速率，劣化时的颜色较少，并且光致变色性能具有优异的耐光性; 含有色烯化合物的光致变色材料; 及其用途。

63. 发明授权

US06506322B1 Naphthopyrans annelated in C5-C6 with an indene- or dihydronaphthalene-type carbocycle, and compositions and (co)polymer matrices containing them 有权
标题翻译： Naphthopyrans在C5-C6中用茚或二氢萘型碳环，和包含它们的组合物和（共）聚合物基质）
公开(公告)号：US06506322B1
公开(公告)日：2003-01-14
申请号：US09712058
申请日：2000-11-14
申请人： Olivier Breyne , You-Ping Chan , Patrick Jean
发明人： Olivier Breyne , You-Ping Chan , Patrick Jean
IPC分类号： G02B523
CPC分类号： C07D311/92 , C07D311/78 , C07D311/94
摘要： The present invention relates to novel naphthopyran-type compounds, annelated in position C5-C6 by an indene- or dihydronaphthalene-type carbocycle, which are of the formulae (I) and (II) given below: These compounds (I) and (II) have interesting photochromic properties. The invention also relates to their preparation, to their applications as photochromes, as well as to the compositions and (co)polymer matrices containing them.
摘要翻译：本发明涉及由下式给出的式（I）和（II）的茚或二氢萘型碳环在C5-C6位置上取代的新型萘并吡喃型化合物：这些化合物（I）和（II ）具有有趣的光致变色性质。本发明还涉及它们作为光致变色剂的应用以及含有它们的组合物和（共）聚合物基质）的制备。

64. 发明申请

US20020034761A1 Methods of labelling polynucleotides with dibenzorhodamine dyes 有权
标题翻译：用二苄唑胺染料标记多核苷酸的方法
公开(公告)号：US20020034761A1
公开(公告)日：2002-03-21
申请号：US09969430
申请日：2001-10-02
申请人： The Perkin-Elmer Corporation
发明人： Scott C. Benson , Joe Y.L. Lam , Steven Michael Menchen
IPC分类号： C12Q001/68 , C07D311/94
CPC分类号： C09B11/24 , C07D209/60 , C07D221/10 , C07D311/78 , C07D491/14 , C07D491/147 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/04 , C09B11/02 , C12Q1/6869 , Y10T436/143333 , C12Q2563/107 , C12Q2527/125
摘要： Dibenzorhodamine compounds having the structure 1 are disclosed, including nitrogen- and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure 2 including nitrogen- and aryl-substituted forms thereof, and a second intermediate having the structure 3 including nitrogen- and aryl-substituted forms thereof, where in substituents at positions C-14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylic acid, sulfonic acid, nullCH2OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodamine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.
摘要翻译：公开了具有该结构的二苄氧苯胺类化合物，包括其氮和芳基取代的形式。此外，公开了可用于合成这些化合物的两个中间体，具有包括其氮和芳基取代形式的结构的第一中间体和具有包括其氮和芳基取代形式的结构的第二中间体，其中在单独取代的C-14至C18位选自氢，氯，氟，低级烷基，羧酸，磺酸，-CH 2 OH，烷氧基，苯氧基，连接基团及其取代形式。本发明还包括包含二苄基罗丹胺化合物的能量转移染料，用二苯并呋喃胺化合物标记的核苷，以及使用二苯并呋喃胺化合物的核酸分析方法。

65. 发明申请

US20010024798A1 Biomimetic combinatorial synthesis 审中-公开
标题翻译：仿生组合合成
公开(公告)号：US20010024798A1
公开(公告)日：2001-09-27
申请号：US09838760
申请日：2001-04-19
发明人： Matthew D. Shair , Craig W. Lindsley , Henry E. Pelish , Scott M. Sheehan , Brian C. Goess , Mark E. Layton , Lawrence K. Chan , Chuo Chen , Nicholas J. Westwood
IPC分类号： G01N033/53 , C07D241/04
CPC分类号： C07D311/78 , C07B2200/11 , C40B40/00
摘要： The present invention provides biomimetic compounds and libraries thereof, as well as methods for their production. In general, the inventive method involves the selection of a desired biological synthetic pathway and mimics that synthetic pathway utilizing modern synthetic tools. The structures formed from this method are preferably generated in fewer than four steps. These scaffold structures can then be functionalized to yield biomimetic compounds and libraries of compounds. In preferred embodiments, biomimetic compounds and libraries are generated from an oxidative phenolic coupling reaction. In other particularly preferred embodiments, the compounds and libraries of compounds are generated from cascade reactions to yield bicyclo nulln.3.1null ring systems, medium ring systems, and fused ring systems. In addition to compounds, libraries and methods for their production, the present invention also provides pharmaceutical compositions and methods and kits for determining one or more biological activities of the library members.
摘要翻译：本发明提供仿生化合物及其文库，以及其生产方法。通常，本发明的方法涉及选择期望的生物合成途径，并模仿使用现代合成工具的合成途径。由该方法形成的结构优选地以不到四个步骤生成。然后可以将这些支架结构官能化以产生化合物的仿生化合物和文库。在优选的实施方案中，仿生化合物和文库是由氧化酚偶联反应产生的。在其它特别优选的实施方案中，化合物和化合物文库由级联反应产生，得到双环[n.3.1]环体系，中环体系和稠环体系。除了用于生产的化合物，文库和方法之外，本发明还提供用于确定文库成员的一种或多种生物活性的药物组合物和方法和试剂盒。

66. 发明申请

US20010011139A1 Polynucleotides labeled with dibenzorhodamine dyes 有权
标题翻译：用二苄唑胺染料标记的多核苷酸
公开(公告)号：US20010011139A1
公开(公告)日：2001-08-02
申请号：US09784943
申请日：2001-02-14
申请人： The Perkin-Elmer Corporation
发明人： Scott C. Benson , Joe Y.L. Lam , Steven Michael Menchen
IPC分类号： C07D311/78
CPC分类号： C09B11/24 , C07D209/60 , C07D221/10 , C07D311/78 , C07D491/14 , C07D491/147 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/04 , C09B11/02 , C12Q1/6869 , Y10T436/143333 , C12Q2563/107 , C12Q2527/125
摘要： Dibenzorhodamine compounds having the structure 1 are disclosed, including nitogen- and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure 2 including nitrogen- and aryl-substituted forms thereof, and a second intermediate having the structure 3 including nitrogen- and aryl-substituted forms thereof, wherein substituents at positions C-14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylic acid, sulfonic acid, nullCH2OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodamine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.
摘要翻译：公开了具有该结构的二苄唑胺化合物，包括硝基和芳基取代形式。此外，公开了可用于合成这些化合物的两种中间体，具有包括其氮和芳基取代形式的结构的第一中间体和具有其氮和芳基取代形式的结构的第二中间体，其中位置 C-14至C18分别选自氢，氯，氟，低级烷基，羧酸，磺酸，-CH 2 OH，烷氧基，苯氧基，连接基团及其取代形式。本发明还包括包含二苄基罗丹胺化合物的能量转移染料，用二苯并呋喃胺化合物标记的核苷，以及使用二苯并呋喃胺化合物的核酸分析方法。

67. 发明授权

US6133446A Heterocyclic compounds for the treatment of CNS and cardiovascular disorders 失效
标题翻译：用于治疗CNS和心血管病的杂环化合物
公开(公告)号：US6133446A
公开(公告)日：2000-10-17
申请号：US239007
申请日：1999-01-28
申请人： Ruth E. TenBrink , Michael D. Ennis , Chiu-Hong Lin , Robert A. Lahti , Arthur G. Romero , John C. Sih
发明人： Ruth E. TenBrink , Michael D. Ennis , Chiu-Hong Lin , Robert A. Lahti , Arthur G. Romero , John C. Sih
IPC分类号： C07D295/18 , A61K31/35 , A61K31/352 , A61K31/495 , A61P9/06 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D295/08 , C07D295/096 , C07D295/10 , C07D295/14 , C07D295/155 , C07D295/185 , C07D307/87 , C07D307/88 , C07D311/02 , C07D311/76 , C07D311/78 , C07D311/80 , C07D313/08 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07F7/08 , A61K31/445 , C07D409/06
CPC分类号： C07D295/185 , A61K31/495 , C07D295/096 , C07D295/155 , C07D307/87 , C07D307/88 , C07D311/76 , C07D311/78 , C07D313/08 , C07D405/06 , C07D405/12 , C07D405/14 , C07F7/0814 , C07C2102/08 , C07C2102/10
摘要： Novel aromatic bicyclic amines of formula (I) ##STR1## are useful in treating central nervous system disorders and cardiac arrhythmias and cardiac fibrillation.
摘要翻译：式（I）的新型芳族二环胺可用于治疗中枢神经系统疾病和心律失常以及心脏纤维性颤动。

68. 发明授权

US6030951A Chrysomycin derivative compounds and use as antitumor agents 失效
标题翻译：赤霉素衍生物，用作抗肿瘤剂
公开(公告)号：US6030951A
公开(公告)日：2000-02-29
申请号：US308710
申请日：1999-07-08
申请人： Takashi Nakashima , Tadashi Fujii , Kazuya Sakai , Tomohiro Sameshima , Hiroyuki Kumagai , Takeo Yoshioka
发明人： Takashi Nakashima , Tadashi Fujii , Kazuya Sakai , Tomohiro Sameshima , Hiroyuki Kumagai , Takeo Yoshioka
IPC分类号： C07D311/78 , C07D407/04 , C12P17/06 , A61K31/70 , C07H7/04
CPC分类号： C07D407/04 , C07D311/78 , C12P17/06
摘要： Disclosed are the novel C-glycoside compounds Mer-1020dA, Mer-1020dB, Mer-1020dC and Mer-1020dD which have a chromophore group in common with well-known chrysomycins A and B, but can be distinguished from the chrysomycins and the like in that the novel C-glycoside compounds have a sugar residue having a higher degree of oxidation, as well as the compound Mer-1020dE comprising only the chromophore thereof. Among these compounds, the C-glycoside compounds are antibiotics which have low toxicity and can strongly inhibit the growth of solid cancer cells in particular.
摘要翻译： PCT No.PCT / JP97 / 04007 Sec。 371日期：1999年7月8日 102（e）1999年7月8日PCT PCT 1997年11月4日PCT公布。公开号WO98 / 22612 PCT 日期1998年5月28日公开了具有发色团组的新颖的C-糖苷化合物Mer-1020dA，Mer-1020dB，Mer-1020dC和Mer-1020dD，与着名的科莫昔霉素A和B相同，但可以区别于科莫昔霉素因为新型C-糖苷化合物具有较高氧化度的糖残基以及仅包含其发色团的化合物Mer-1020dE。在这些化合物中，C-糖苷化合物是具有低毒性并特别强烈地抑制固体癌细胞生长的抗生素。

69. 发明授权

US5294522A Photochromic compound 失效
标题翻译：光致变色化合物
公开(公告)号：US5294522A
公开(公告)日：1994-03-15
申请号：US025133
申请日：1993-03-02
申请人： Manabu Uchida , Masahiro Irie
发明人： Manabu Uchida , Masahiro Irie
IPC分类号： C07D311/78 , C07D311/92 , G03C1/73 , C07D333/50
CPC分类号： G03C1/73 , C07D311/78 , C07D311/92 , Y10S430/163
摘要： A novel photochromic compound as a photoreactive material making use of photochromism is provided, which compound is expressed by the following formula (1) or (2)): ##STR1## wherein R is alkyl, alkoxy, perfluoroalkyl or cyano; X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5 and X.sub.6 are each H, halogen, alkyl, alkoxy, cyano, alkanoyloxy or alkyloxycarbonyl, or a substituted or unsubstituted benzene ring is formed by condensation between at adjacent groups among X.sub.1 to X.sub.6 ; Y is Y.sub.1 C=CY.sub.2, O, S, SO, SO.sub.2 or NY.sub.3 wherein Y.sub.1 and Y.sub.2 are each as defined in the case of the above X.sub.1 to X.sub.6 and Y.sub.3 is H, alkyl, alkanoyl, alkyloxycarbonyl or aryl; and the symbol refers to occurrence of E- or Z-isomer, and which compound is useful as rewritable optical memory element or photo-display element and also as solar energy-storage material, duplicating material, masking material, optical filter, toys, etc.
摘要翻译：（1）或（2）表示化合物：（*化学结构*）（1）或（*化学结构*）（2））其中R是烷基，烷氧基，全氟烷基或氰基; X 1，X 2，X 3，X 4，X 5和X 6各自为H，卤素，烷基，烷氧基，氰基，烷酰氧基或烷氧基羰基，或者通过X1至X6中的相邻基团之间的缩合形成取代或未取代的苯环; Y是Y1C = CY2，O，S，SO，SO2或NY3，其中Y1和Y2各自如上述X1至X6的定义，Y3为H，烷基，烷酰基，烷氧基羰基或芳基; 符号是指E-或Z-异构体的出现，哪种化合物可用作可重写光存储元件或光显示元件，也可用作太阳能储存材料，复制材料，掩模材料，滤光器，玩具等。

70. 发明授权

US5281620A Compounds having antitumor and antibacterial properties 失效
标题翻译：具有抗肿瘤和抗菌特性的化合物
公开(公告)号：US5281620A
公开(公告)日：1994-01-25
申请号：US912466
申请日：1992-07-13
申请人： William A. Denny , Bruce C. Baguley , Graham J. Atwell , Gordon W. Rewcastle
发明人： William A. Denny , Bruce C. Baguley , Graham J. Atwell , Gordon W. Rewcastle
IPC分类号： C07D311/78 , C07D311/86 , C07D491/04 , A61K31/335
CPC分类号： C07D491/04 , C07D311/78 , C07D311/86
摘要： The novel class of xanthenone-4-acetic acids represented by the general formula (I) ##STR1## where R.sub.1 represents up to two of the groups lower alkyl, halogen, CF.sub.3, CN, NO.sub.2, NH.sub.2, CH.sub.2 COOH, OR.sub.2, OH, NHCOR.sub.2, NHSO.sub.2 R.sub.2, SR.sub.2, SO.sub.2 R.sub.2, CH.sub.2 CONHR.sub.2 or NHR.sub.2 (where R.sub.2 is lower alkyl optionally substituted with hydroxy, amino or methoxy functions), at any of the positions 1-8 which are available, R.sub.1 may also represent the substitution of an aza (--N.dbd.) group for one or two of the methine (--CH.dbd.) groups in the carbocyclic rings and two of R.sub.1 on any two available adjacent positions may also represent the grouping --CH.dbd.CH--CH.dbd.CH-- to form an additional fused benzene ring;and basic addition salts thereof, possess antitumour and antibacterial properties.
摘要翻译：由通式（I）表示的呫吨酮-4-乙酸的新型类别（I）其中R1代表至少两个低级烷基，卤素，CF 3，CN，NO 2，NH 2，CH 2 COOH，OR 2， OH，NHCOR 2，NHSO 2 R 2，SR 2，SO 2 R 2，CH 2 CONHR 2或NHR 2（其中R 2是任选被羟基，氨基或甲氧基官能团取代的低级烷基），在任何可用的位置1-8，R 1还可以代表碳环中的一个或两个次甲基（-CH =）基团和任何两个可用相邻位置上的两个R1中的氮杂（-N =）基团也可以表示组-CH = CH-CH = CH-以形成一个额外的稠合苯环; 及其碱式加成盐，具有抗肿瘤和抗菌的特性。

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