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81. 发明授权

US08309599B2 Synthesis of FR901464 and analogs with antitumor activity 有权
标题翻译：合成FR901464和具有抗肿瘤活性的类似物
公开(公告)号：US08309599B2
公开(公告)日：2012-11-13
申请号：US12883105
申请日：2010-09-15
申请人： Kazunori Koide , Brian J. Albert , Ananthapadmanabhan Sivaramakrishnan
发明人： Kazunori Koide , Brian J. Albert , Ananthapadmanabhan Sivaramakrishnan
IPC分类号： A61K31/35 , C07D315/00
CPC分类号： C07D493/10 , C07D303/12 , C07D413/14
摘要： The present invention provides novel analogs of FR901464, as well as an improved methodology for preparing FR901464 and its analogs. These compounds display an anti-cancer activity and are candidates for therapies against a number of disease states associated with dysfunctional RNA splicing.
摘要翻译：本发明提供FR901464的新型类似物，以及制备FR901464及其类似物的改进方法。这些化合物显示抗癌活性，并且是针对与功能失调的RNA剪接相关的许多疾病状态的治疗的候选者。

82. 发明申请

US20120149707A1 ALPHA-ARYLMETHOXYACRYLATE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME 失效
标题翻译： ALPHA-ARYLMETHOXYACRYLATE衍生物，其制备方法和含有其的药物组合物
公开(公告)号：US20120149707A1
公开(公告)日：2012-06-14
申请号：US13392024
申请日：2011-04-21
申请人： Se-Won Kim , Jung Ho Kim , Se-Nyum Kim , Dae-Pil Kang , Youn Ho Han , Guo Fan Jin , Dong-Sik Jung , Sung-Ho Park , Ji Min Kim , Jhi Zheng
发明人： Se-Won Kim , Jung Ho Kim , Se-Nyum Kim , Dae-Pil Kang , Youn Ho Han , Guo Fan Jin , Dong-Sik Jung , Sung-Ho Park , Ji Min Kim , Jhi Zheng
IPC分类号： A61K31/24 , C07C69/732 , A61K31/216 , C07C69/738 , C07D211/34 , A61K31/4453 , C07D295/192 , A61K31/5375 , C07D295/155 , A61P35/00 , A61P19/02 , A61P17/06 , A61P27/02 , A61P35/02 , A61P29/00 , C07C229/34
CPC分类号： A61K31/216 , A61K31/24 , A61K31/336 , A61K31/40 , A61K31/415 , A61K31/421 , A61K31/4402 , A61K31/4409 , A61K31/4453 , A61K31/5375 , C07C69/736 , C07C217/20 , C07C251/48 , C07C251/86 , C07C2601/02 , C07C2601/08 , C07D213/30 , C07D231/12 , C07D261/08 , C07D295/088 , C07D295/30 , C07D303/12
摘要： The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.
摘要翻译：本发明涉及α-芳基甲氧基丙烯酸酯衍生物，其制备方法和含有该芳香族甲氧基丙烯酸酯衍生物的药物组合物，α-芳基甲氧基丙烯酸酯衍生物是HIF抑制剂，其在调节与能量代谢相关的基因，血管运动中起重要作用，血管生成和凋亡以及在缺氧条件下细胞的反应，从而可用于预防或治疗诸如癌症，关节炎，牛皮癣，糖尿病性视网膜病变和黄斑变性等疾病。

83. 发明申请

US20100317515A1 Azolylmethyloxiranes, use Thereof and Agents Containing the Same 审中-公开
标题翻译：唑基甲基环氧乙烷，其用途和含有它的药剂
公开(公告)号：US20100317515A1
公开(公告)日：2010-12-16
申请号：US12808793
申请日：2008-12-12
申请人： Jochen Dietz , Thomas Grote , Bernd Mueller , Jan Klaas Lohmann , Jens Renner , Sarah Ulmschneider , Alice Glaettli , Marianna Vrettou
发明人： Jochen Dietz , Thomas Grote , Bernd Mueller , Jan Klaas Lohmann , Jens Renner , Sarah Ulmschneider , Alice Glaettli , Marianna Vrettou
IPC分类号： A01C1/06 , C07D405/06 , C07F9/28 , A01N43/653 , C07D303/36 , C07D303/08 , C07D303/14 , A01P3/00
CPC分类号： A01N43/653 , C07D303/08 , C07D303/12 , C07D303/16 , C07D303/36 , C07D403/06
摘要： The present invention relates to triazolylmethyloxiranes of the formula I in which the variables A, B and D have the meanings described in the claims and the description.
摘要翻译：本发明涉及式I的三唑基甲氧基环烷，其中变量A，B和D具有权利要求书和说明书中描述的含义。

84. 发明申请

US20100168379A1 Epichlorohydrin, manufacturing process and use 有权
标题翻译：表氯醇，制造工艺及用途
公开(公告)号：US20100168379A1
公开(公告)日：2010-07-01
申请号：US12663749
申请日：2008-06-11
申请人： Philippe Krafft , Patrick Gilbeau , Dominique Balthasart , Noel Boulos
发明人： Philippe Krafft , Patrick Gilbeau , Dominique Balthasart , Noel Boulos
IPC分类号： C08G65/24 , C09K3/00 , C07F9/141
CPC分类号： C07D303/12 , C07D301/27 , C07D301/28 , C07F9/65502 , C08G59/00 , C08G59/02
摘要： Product containing epichlorohydrin, wherein the amount of trichloropropane is of less than 0.01 g of trichloropropane per kg of product, a process for manufacturing the product and its use in various applications.
摘要翻译：含有表氯醇的产品，其中三氯丙烷的量小于每千克产品0.01克三氯丙烷，制造该产品的方法及其在各种应用中的应用。

85. 发明申请

US20100130712A1 ADAMANTANE DERIVATIVE, RESIN COMPOSITION USING THE SAME, AND RESIN CURED PRODUCT 审中-公开
标题翻译： ADAMANTANE衍生物，使用该树脂的树脂组合物和树脂固化产品
公开(公告)号：US20100130712A1
公开(公告)日：2010-05-27
申请号：US12594254
申请日：2008-03-31
申请人： Katsuki Ito , Yasunari Okada , Hideki Yamane , Shinobu Yamao
发明人： Katsuki Ito , Yasunari Okada , Hideki Yamane , Shinobu Yamao
IPC分类号： C08F124/00 , C07D205/04
CPC分类号： C07D303/12 , C07D305/06 , C08F220/28 , C08F220/32 , C08G65/105 , C08G65/18 , C08L63/00
摘要： Provided is a cured resin of an adamantane derivative having a specific structure, which has excellent optical properties such as transparency and (long-term) light stability, long-term heat resistance, dielectric constant, and mechanical properties, and which can be utilized suitably in the field of electronic and optical materials.
摘要翻译：提供具有特定结构的金刚烷衍生物的固化树脂，其具有优异的光学性能如透明度和（长期）光稳定性，长期耐热性，介电常数和机械性能，并且可以适当地使用在电子和光学材料领域。

86. 发明申请

US20080096879A1 SYNTHESIS OF FR901464 AND ANALOGS WITH ANTITUMOR ACTIVITY 有权
标题翻译： FR901464和具有抗肿瘤活性的模拟物的合成
公开(公告)号：US20080096879A1
公开(公告)日：2008-04-24
申请号：US11852278
申请日：2007-09-08
申请人： Kazunori KOIDE , Brian Albert , Ananthapadmanabhan Sivaramakrishnan
发明人： Kazunori KOIDE , Brian Albert , Ananthapadmanabhan Sivaramakrishnan
IPC分类号： A61K31/5377 , A61P35/00 , C07D303/02 , C07D413/14 , A61K31/351
CPC分类号： C07D493/10 , C07D303/12 , C07D413/14
摘要： The present invention provides novel analogs of FR901464, as well as an improved methodology for preparing FR901464 and its analogs. These compounds display an anti-cancer activity and are candidates for therapies against a number of disease states associated with dysfunctional RNA splicing.
摘要翻译：本发明提供FR901464的新型类似物，以及制备FR901464及其类似物的改进方法。这些化合物显示抗癌活性，并且是针对与功能失调的RNA剪接相关的许多疾病状态的治疗的候选者。

87. 发明申请

US20080021226A1 Process for total synthesis of pladienolide B and pladienolide D 失效
标题翻译：丙二烯内酯B和普拉二烯内酯D的全合成方法
公开(公告)号：US20080021226A1
公开(公告)日：2008-01-24
申请号：US11580047
申请日：2006-10-13
申请人： Regina Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
发明人： Regina Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
IPC分类号： C07D313/00 , C07D303/02
CPC分类号： C07D493/04 , C07D303/12 , C07D303/14 , C07D313/00 , C07D315/00 , C07D405/12 , C07D407/06 , Y02P20/55
摘要： [Problems to be Solved]To provide an effective process for total synthesis of pladienolide B and pladienolide D having excellent anti-tumor activity and to provide useful intermediates in the above-described process. [Measure for Solving the Problem]A process for producing a compound represented by Formula (11): wherein P1, P7, P8, P9 and R1 are the same as defined below, characterized by including reacting a compound represented by Formula (12): wherein P7 means a hydrogen atom or a protecting group for hydroxy group; R1 means a hydrogen atom or a hydroxy group, with a compound represented by Formula (13): wherein P1 means a hydrogen atom or a protecting group for hydroxy group; P8 means a hydrogen atom, an acetyl group or a protecting group for hydroxy group; P9 means a hydrogen atom or a protecting group for hydroxy group; or P8 and P9 may form together a group represented by a formula: wherein R5 means a phenyl group which may have a substituent, in the presence of a catalyst.
摘要翻译： [待解决的问题]为了提供具有优异的抗肿瘤活性的普拉二烯内酯B和普拉二烯内酯D的全合成的有效方法，并且在上述方法中提供有用的中间体。 [解决问题的措施]制备由式（11）表示的化合物的方法：其中P 1，P 2，P 3，，其中P 9和R 12与下述定义相同，其特征在于包括使由式（12）表示的化合物：其中P 是指氢原子或羟基的保护基; R 1表示氢原子或羟基，与式（13）表示的化合物：其中P 1是氢原子或羟基的保护基; “8”表示氢原子，乙酰基或羟基保护基; “9”表示氢原子或羟基的保护基; 或者P 9和P 9可以一起形成由下式表示的基团：其中R 5表示可以具有取代基的苯基，在催化剂存在下。

88. 发明申请

US20040157805A1 11,12-Oxidoarachidonic acid derivatives and methods of their use in treating dry eye disorders 有权
标题翻译： 11,12-氧化花生四烯酸衍生物及其用于治疗干眼症的方法
公开(公告)号：US20040157805A1
公开(公告)日：2004-08-12
申请号：US10774294
申请日：2004-02-06
发明人： David B. Belanger , Peter G. Klimko
IPC分类号： A61K031/557
CPC分类号： C07D303/22 , A61K31/336 , C07D303/12 , C07D303/38
摘要： 11,12-Oxidoarachidonic acid derivatives and methods of their use for treating dry eye are disclosed.
摘要翻译：公开了11,12-氧化花生四烯酸衍生物及其用于治疗干眼症的方法。

89. 发明授权

US06740193B2 Gem-diesters and epoxidized derivatives thereof 失效
标题翻译： Gem-二酯及其环氧化衍生物
公开(公告)号：US06740193B2
公开(公告)日：2004-05-25
申请号：US10032128
申请日：2001-12-21
申请人： John G. Woods , Jianzhao Wang , Jean M. J. Fréchet
发明人： John G. Woods , Jianzhao Wang , Jean M. J. Fréchet
IPC分类号： C09J16300
CPC分类号： C07D303/12 , Y10T156/1111 , Y10T428/31511
摘要： In accordance with the present invention, there are provided gem-diesters and epoxidized derivatives thereof. When cured, thermosets comprising invention gem-diesters and epoxidized derivatives thereof have thermally and/or chemically labile gem-diester groups interspersed throughout the crosslinked network. Thus, thermosets based on invention gem-diesters and epoxidized derivatives thereof can be easily reworked thermally or chemically by treatment with dilute acidic or basic solutions. Further provided by the present invention are adhesive compositions comprising invention gem-diesters and epoxidized derivatives thereof.
摘要翻译：根据本发明，提供了偕二酯及其环氧化衍生物。当固化时，包含本发明偕二酯和环氧化衍生物的热固性材料具有散布在整个交联网络中的热和/或化学不稳定的偕二酯基团。因此，基于本发明的偕二酯和其环氧化衍生物的热固性材料可以通过用稀酸或碱性溶液处理而易于热或化学地再加工。本发明进一步提供的是含有本发明的偕二酯及其环氧化衍生物的粘合剂组合物。

90. 发明授权

US4209447A Imidazole derivatives and intermediates in their preparation 失效
标题翻译：咪唑衍生物及其制备中间体
公开(公告)号：US4209447A
公开(公告)日：1980-06-24
申请号：US965722
申请日：1978-12-01
申请人： Jan Heeres
发明人： Jan Heeres
IPC分类号： A01N43/50 , C07C29/10 , C07C29/36 , C07C41/30 , C07C43/23 , C07D303/04 , C07D303/08 , C07D303/12 , C07D303/22 , C07D317/14 , C07D317/16 , C07D317/22 , C07D317/24 , C07D317/30 , C07D317/10
CPC分类号： C07D317/30 , A01N43/50 , C07C29/106 , C07C29/36 , C07C41/30 , C07D303/04 , C07D303/08 , C07D303/12 , C07D303/22 , C07D317/14 , C07D317/16 , C07D317/22 , C07D317/24
摘要： Novel 1-(2-Ar-4-R-1,3-dioxolan-2-ylmethyl)imidazoles, useful as antifungal and antibacterial agents.
摘要翻译：新颖的1-（2-Ar-4-R-1,3-二氧戊环-2-基甲基）咪唑，可用作抗真菌剂和抗菌剂。

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