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1. 发明申请

US20090093479A1 ANTI-CANCER AGENTS AND USES THEREOF 审中-公开
标题翻译：抗癌药剂及其用途
公开(公告)号：US20090093479A1
公开(公告)日：2009-04-09
申请号：US12336857
申请日：2008-12-17
申请人： Martha KELLY , Younghee LEE , Bin LIU , Ted FUJIMOTO , Joel FREUNDLICH , Bruce D. DORSEY , Gary A. FLYNN , Arifa HUSAIN
发明人： Martha KELLY , Younghee LEE , Bin LIU , Ted FUJIMOTO , Joel FREUNDLICH , Bruce D. DORSEY , Gary A. FLYNN , Arifa HUSAIN
IPC分类号： A61K31/5377 , C07D401/02 , C07D211/80 , C07D409/02 , C07D401/14 , C07D405/02 , A61K31/497 , A61K31/506 , A61P35/00 , A61K31/422 , A61K31/4709 , A61K31/4439 , A61K31/4436 , A61K31/443 , A61K31/44 , C07D413/02
CPC分类号： C07D209/08 , C07D213/74 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/10
摘要： The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, non-small cell lung and colon.
摘要翻译：本发明涉及新型化合物及其盐，其合成及其作为抗癌剂的用途。化合物包括式I化合物及其溶剂合物，水合物及其药学上可接受的盐，其中A1为N或CR1; A3是N或CR3; A5为N或CR5; R1，R3-R6和L在说明书中定义; n为0或1; 并且X是在环部分中具有6-10个碳的任选取代的芳基，在环部分中具有1-3个氮原子的任选取代的6元杂芳基，任选取代的5元杂芳基具有0 -4个氮原子，并且在环部分中任选具有1个硫原子或1个氧原子，或任选取代的杂芳基，其中6元环稠合到5元环或6元环其中在每种情况下，1,2,3或4个环原子是独立地选自氮，氧和硫的杂原子。它们对广泛的癌症尤其是白血病，非小细胞肺和结肠有效。

2. 发明申请

US20060100416A1 Novel substitution mutant receptors and their use in an nuclear receptor-based inducible gene expression system 有权
标题翻译：新型取代突变体受体及其在基于核受体的诱导型基因表达系统中的应用
公开(公告)号：US20060100416A1
公开(公告)日：2006-05-11
申请号：US10468193
申请日：2002-02-20
申请人： Subba Palli , Mohan Kumar , Dean Cress , Ted Fujimoto
发明人： Subba Palli , Mohan Kumar , Dean Cress , Ted Fujimoto
IPC分类号： A01K67/00 , C07H21/04 , C12P21/06 , C07K14/715
CPC分类号： C12N15/635 , C07K14/70567 , C07K14/721 , C12N7/00 , C12N15/86 , C12N2710/10043 , C12P21/02
摘要： This invention relates to the field of biotechnology or genetic engineering. Specifically, this invention relates to the field of gene expression. More specifically, this invention relates to novel substitution mutant receptors and their use in a Group H nuclear receptor-based inducible gene expression system and methods of modulating the expression of a gene in a host cell for applications such as gene therapy, large scale production of proteins and antibodies, cell-based high throughput screening assays, functional genomics and regulation of traits in transgenic organisms.
摘要翻译：本发明涉及生物技术或遗传工程领域。具体地，本发明涉及基因表达领域。更具体地，本发明涉及新的取代突变体受体及其在基于H核受体的诱导型基因表达系统中的用途以及调节宿主细胞中基因表达的方法，用于基因治疗，大规模生产蛋白质和抗体，基于细胞的高通量筛选测定，功能基因组学和转基因生物体中性状的调节。

3. 发明授权

US4894479A Herbicidal diphenyl ethers 失效
标题翻译：除草二苯醚
公开(公告)号：US4894479A
公开(公告)日：1990-01-16
申请号：US269224
申请日：1981-06-01
申请人： John W. Ashmore , Ted Fujimoto
发明人： John W. Ashmore , Ted Fujimoto
IPC分类号： A01N37/40 , A01N37/44 , A01N37/48 , A01N41/10 , A01N43/34 , A01N47/24 , C07C53/00 , C07C67/00 , C07C231/00 , C07C231/12 , C07C237/06 , C07C239/00 , C07C239/18 , C07C239/22 , C07C253/00 , C07C255/54 , C07C271/06 , C07C313/00 , C07C315/04 , C07C317/46 , C07C323/62
CPC分类号： C07C255/00 , A01N37/48 , A01N47/24
摘要： This invention is directed to diphenyl ethers having in the 3' position a radical of the formula: ##STR1## The products are prepared by reacting a 3'-halocarbonyl compound with an appropriate substituted hydroxyl amine. These compounds and their agronomically acceptable salts and compositions containing these compounds as active ingredients are selective herbicides.
摘要翻译：本发明涉及在3'位置具有下式基团的二苯醚：产物通过使3'-卤代羰基化合物与适当的取代的羟基胺反应制备。这些化合物及其农艺学上可接受的盐和含有这些化合物作为活性成分的组合物是选择性除草剂。

4. 发明申请

US20060270686A1 Anti-cancer agents and uses thereof 失效
标题翻译：抗癌剂及其用途
公开(公告)号：US20060270686A1
公开(公告)日：2006-11-30
申请号：US10928401
申请日：2004-08-30
申请人： Martha Kelly , Younghee Lee , Bin Liu , Ted Fujimoto , Joel Freundlich , Bruce Dorsey , Gary Flynn , Arifa Husain
发明人： Martha Kelly , Younghee Lee , Bin Liu , Ted Fujimoto , Joel Freundlich , Bruce Dorsey , Gary Flynn , Arifa Husain
IPC分类号： A61K31/497 , A61K31/44 , C07D403/02
CPC分类号： C07D209/08 , C07D213/74 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/10
摘要： The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3—R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, non-small cell lung and colon.
摘要翻译：本发明涉及新型化合物及其盐，其合成及其作为抗癌剂的用途。化合物包括式I化合物及其溶剂合物，水合物及其药学上可接受的盐，其中A 1是N或CR 1; N 3或N 3是N或CR 3; A <5>为N或CR 5; 在说明书中定义了R 1，R 3，R 6和L 6; n为0或1; 并且X是在环部分中具有6-10个碳的任选取代的芳基，在环部分中具有1-3个氮原子的任选取代的6元杂芳基，任选取代的5元杂芳基具有0 -4个氮原子，并且在环部分中任选具有1个硫原子或1个氧原子，或任选取代的杂芳基，其中6元环稠合到5元环或6元环其中在每种情况下，1,2,3或4个环原子是独立地选自氮，氧和硫的杂原子。它们对广泛的癌症尤其是白血病，非小细胞肺和结肠有效。

5. 发明申请

US20060167247A1 Urea inhibitors of MAP kinases 失效
标题翻译： MAP激酶的尿素抑制剂
公开(公告)号：US20060167247A1
公开(公告)日：2006-07-27
申请号：US11295638
申请日：2005-12-07
申请人： Enrique Michelotti , Eric Springman , Duyan Nguyen , Rupa Shetty , Younghee Lee , Kristofer Moffett , Jennifer Ludington , Ted Fujimoto , Zenon Konteatis , Bin Liu , Frank Hollinger , Bruce Dorsey
发明人： Enrique Michelotti , Eric Springman , Duyan Nguyen , Rupa Shetty , Younghee Lee , Kristofer Moffett , Jennifer Ludington , Ted Fujimoto , Zenon Konteatis , Bin Liu , Frank Hollinger , Bruce Dorsey
IPC分类号： C07D417/02 , C07D413/02 , C07D409/02
CPC分类号： C07D333/38 , C07D231/40 , C07D243/08 , C07D277/48 , C07D277/56 , C07D295/192 , C07D333/36 , C07D403/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/14 , C07D495/04
摘要： The present invention is directed to a compound having the formula wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.
摘要翻译：本发明涉及具有下式的化合物：其中R 1，R 2，G和Q在本文中定义。本发明的化合物可用作蛋白激酶如MAP激酶，特别是p38激酶的抑制剂。本发明还涉及包含根据上式的化合物的组合物。本文所述的化合物和组合物可用于治疗和预防炎性疾病或疾病。本发明还涉及治疗或预防蛋白激酶介导的病症的方法。

6. 发明申请

US20070300313A1 NOVEL SUBSTITUTION MUTANT RECEPTORS AND THEIR USE IN A NUCLEAR RECEPTOR-BASED INDUCIBLE GENE EXPRESSION SYSTEM 有权
标题翻译：新型替代突变体受体及其在基于受体基因的诱导基因表达系统中的应用
公开(公告)号：US20070300313A1
公开(公告)日：2007-12-27
申请号：US11841529
申请日：2007-08-20
申请人： Subba Palli , Mohan Kumar , Dean Cress , Ted Fujimoto
发明人： Subba Palli , Mohan Kumar , Dean Cress , Ted Fujimoto
IPC分类号： C12N15/87 , A01K67/00 , C07K14/00 , C12N5/06 , C12N15/00 , C12N15/11
CPC分类号： C12N15/635 , C07K14/70567 , C07K14/721 , C12N7/00 , C12N15/86 , C12N2710/10043 , C12P21/02
摘要： This invention relates to the field of biotechnology or genetic engineering. Specifically, this invention relates to the field of gene expression. More specifically, this invention relates to novel substitution mutant receptors and their use in a Group H nuclear receptor-based inducible gene expression system and methods of modulating the expression of a gene in a host cell for applications such as gene therapy, large scale production of proteins and antibodies, cell-based high throughput screening assays, functional genomics and regulation of traits in transgenic organisms.
摘要翻译：本发明涉及生物技术或遗传工程领域。具体地，本发明涉及基因表达领域。更具体地，本发明涉及新的取代突变体受体及其在基于H核受体的诱导型基因表达系统中的用途以及调节宿主细胞中基因表达的方法，用于基因治疗，大规模生产蛋白质和抗体，基于细胞的高通量筛选测定，功能基因组学和转基因生物体中性状的调节。

7. 发明授权

US4306900A Herbicidal nitrodiphenyl ethers 失效
标题翻译：除草硝基二苯醚
公开(公告)号：US4306900A
公开(公告)日：1981-12-22
申请号：US182372
申请日：1980-08-29
申请人： Colin Swithenbank , Ted Fujimoto
发明人： Colin Swithenbank , Ted Fujimoto
IPC分类号： A01N33/22 , A01N35/04 , A01N37/40 , C07C45/71 , C07C205/38 , A01N31/14 , C07C49/84
CPC分类号： C07C205/38 , A01N33/22 , A01N35/04 , A01N37/40 , C07C205/44 , C07C205/45 , C07C255/00 , C07C45/71
摘要： Compounds of the formula ##STR1## wherein X is a hydrogen atom, a halogen atom, a trihalomethyl group, an alkyl group, or a cyano group;Y is a hydrogen atom or a halogen atom;R is CHOHR' or COR'; andR' is hydrogen or (C.sub.1 -C.sub.4)alkyl;and compositions containing these compounds which exhibit herbicidal activity.
摘要翻译：其中X为氢原子，卤素原子，三卤代甲基，烷基或氰基的式“IMAGE”的化合物; Y是氢原子或卤素原子; R是CHOHR'或COR'; 和R'是氢或（C 1 -C 4）烷基; 以及含有这些具有除草活性的化合物的组合物。

8. 发明申请

US20080280891A1 Anti-cancer agents and uses thereof 审中-公开
标题翻译：抗癌剂及其用途
公开(公告)号：US20080280891A1
公开(公告)日：2008-11-13
申请号：US11819494
申请日：2007-06-27
申请人： Martha Kelly , Younghee Lee , Bin Liu , Ted Fujimoto , Joel Freundlich , Bruce D. Dorsey , Gary A. Flynn , Arifa Husain , William R. Moore, Jr.
发明人： Martha Kelly , Younghee Lee , Bin Liu , Ted Fujimoto , Joel Freundlich , Bruce D. Dorsey , Gary A. Flynn , Arifa Husain , William R. Moore, Jr.
IPC分类号： A61K31/541 , A61K31/404 , C07D209/42 , C07D401/02 , C07D417/14 , A61K31/44 , A61P35/00 , A61K31/4439 , A61K31/5377 , C07D413/14
CPC分类号： A61K31/404 , A61K31/44 , A61K31/4439 , A61K31/5377 , A61K31/541 , C07D213/74 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/10 , C07D413/12 , C07D498/04
摘要： The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.
摘要翻译：本发明涉及新型化合物及其盐，其合成及其作为抗癌剂的用途。化合物包括式I化合物及其溶剂合物，水合物及其药学上可接受的盐，其中A 1是N或CR 1; N 3或N 3是N或CR 3; A <5>为N或CR 5; 在说明书中定义了R 1，R 3，R 6和L 6; n为0或1; 并且X是在环部分中具有6-10个碳的任选取代的芳基，在环部分中具有1-3个氮原子的任选取代的6元杂芳基，任选取代的5元杂芳基具有0 -4个氮原子，并且在环部分中任选具有1个硫原子或1个氧原子，或任选取代的杂芳基，其中6元环稠合到5元环或6元环其中在每种情况下，1,2,3或4个环原子是独立地选自氮，氧和硫的杂原子。它们对广泛的癌症尤其是白血病，前列腺，非小细胞肺和结肠有效。它们还可用于治疗增殖性视网膜病变，例如糖尿病性神经病变和黄斑变性。

9. 发明申请

US20050222776A1 Method for fragment preparation 审中-公开
标题翻译：片段制备方法
公开(公告)号：US20050222776A1
公开(公告)日：2005-10-06
申请号：US10813553
申请日：2004-03-31
申请人： Jennifer Ludington , Ted Fujimoto , Frank Hollinger
发明人： Jennifer Ludington , Ted Fujimoto , Frank Hollinger
IPC分类号： G01N33/48 , G01N33/50 , G01N33/68 , G06F19/00
CPC分类号： G01N33/6803 , G16B15/00
摘要： A method for characterizing a molecular fragment to collect data related to the fragment that allows its evaluation for drug discovery purposes. Starting with a two-dimensional model of the fragment, an initial three-dimensional model of the fragment is derived. Conformers of the fragment are identified. The conformers are then clustered, and a representative conformer is selected from each cluster. An ab initio or semi-empirical calculation and analysis is performed on one or more of the selected conformers. Each atom in the selected conformer is then assigned a type. The selected conformer is analyzed to determine if it is structurally symmetric. If so, the three-dimensional model of the fragment is adjusted to reflect the symmetry. The size of the fragment is calculated to allow geometric analysis of how the fragment physically fits with the protein and/or other fragments. The solvation energy of the fragment is calculated. The free energy curve for the fragment is calculated. Derivatization points for the fragment are then determined; a score is then assigned to each derivatization point, reflecting the ease or difficulty in bonding at the derivatization points. The fragment is then assigned a name and categorized. The fragment and its data derived in the above process can then be stored in a database.
摘要翻译：用于表征分子片段以收集与该片段相关的数据的方法，其允许其评估药物发现目的。从片段的二维模型开始，导出片段的初始三维模型。确定片段的构象。然后将构象异构体聚集，并从每个聚类中选择代表性构象。对一个或多个所选构象进行从头或半经验的计算和分析。然后将所选构象异构体中的每个原子分配一个类型。分析所选择的构象异构体以确定其是否在结构上对称。如果是这样，则调整片段的三维模型以反映对称性。计算片段的大小以允许对片段与蛋白质和/或其他片段物理匹配的几何分析。计算片段的溶剂化能。计算片段的自由能曲线。然后确定片段的衍生点; 然后将分数分配给每个衍生化点，反映在衍生化点处的粘合的容易性或难度。然后将该片段分配一个名称并进行分类。然后将上述过程中导出的片段及其数据存储在数据库中。

10. 发明授权

US5290756A 4-trifluoromethyl-4'-nitrodiphenyl ethers 失效
标题翻译： 4-三氟甲基-4'-硝基二苯醚
公开(公告)号：US5290756A
公开(公告)日：1994-03-01
申请号：US386455
申请日：1982-06-08
申请人： Colin Swithenbank , Ted Fujimoto
发明人： Colin Swithenbank , Ted Fujimoto
IPC分类号： C07C205/59 , C07C317/18 , C07C323/12 , C07D277/24 , C07C205/00
CPC分类号： C07C205/59 , C07C317/18 , C07C323/12 , C07D277/24
摘要： Compounds of the formula: ##STR1## wherein X is hydrogen, halo, trihalomethyl, alkyl, nitroor cyano; X.sup.1 is hydrogen, halo, or trihalomethyl; R.sup.1 and R.sup.2 are hydrogen, alkyl phenyl or benzyl; n is 1 to 5, and Z is halo, cyano, nitro, trihalomethyl, methylthio, methylsulfinyl, methylsulfonyl, acetyl, phenyl, or heterocycle, and compositions containing these compounds exhibit herbicidal activity.
摘要翻译：下式的化合物：其中X是氢，卤素，三卤甲基，烷基，硝基或氰基; X1是氢，卤素或三卤甲基; R1和R2是氢，烷基苯基或苄基; n为1至5，Z为卤素，氰基，硝基，三卤甲基，甲硫基，甲基亚磺酰基，甲基磺酰基，乙酰基，苯基或杂环，并且含有这些化合物的组合物显示除草活性。

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