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1. 发明授权

US09802951B2 Biologically active taxane analogs and methods of treatment by oral administration 有权
公开(公告)号：US09802951B2
公开(公告)日：2017-10-31
申请号：US13950316
申请日：2013-07-25
申请人： Tapestry Pharmaceuticals, Inc.
发明人： James D. McChesney , Gilles H. Tapolsky , David Lloyd Emerson , John Marshall , Michael Kurman , Manuel R. Modiano
IPC分类号： A61K31/35 , A61K31/335 , C07D309/00 , C07D407/00 , A61K39/395 , A61K31/357 , A61K31/495 , A61K45/06 , C07D493/06
CPC分类号： C07D493/06 , A61K31/357 , A61K31/495 , A61K39/3955 , A61K45/06
摘要： The present invention relates to a novel chemical compound for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.

2. 发明授权

US09522932B2 Phosphonate nucleosides useful as active ingredients in pharmaceutical compositions for the treatment of viral infections, and intermediates for their production 有权
标题翻译：可用作用于治疗病毒感染的药物组合物中的活性成分的膦酸核苷和用于其生产的中间体
公开(公告)号：US09522932B2
公开(公告)日：2016-12-20
申请号：US14867208
申请日：2015-09-28
申请人： K.U. Leuven Research & Development
发明人： Piet Herdewijn , Christophe Pannecouque , Tongfei Wu , Erik De Clercq
IPC分类号： C07H23/00 , C07H19/04 , C07H19/20 , C07H19/10 , C07H3/00 , C07H11/00 , C07H15/00 , C07H17/00 , C07D311/00 , C07D493/00 , C07D305/00 , C07D309/00 , C07H19/00 , C07H19/06 , C07H19/16 , C07H1/00 , C07F7/08 , C07H15/04 , C07H17/02 , C07D313/00 , C07D319/00 , C07D321/00 , C07D323/00 , C07D325/00 , C07D407/00 , C07D323/04 , C07F7/02
CPC分类号： C07H19/20 , C07F7/0812 , C07H1/00 , C07H15/04 , C07H17/02 , C07H19/00 , C07H19/06 , C07H19/10 , C07H19/16
摘要： The invention is directed to a process for the preparation of substituted threonolactone and substituted threose compounds which are intermediates in the synthesis of phosphonate nucleosides being useful antiviral agents.
摘要翻译：本发明涉及一种制备取代的苏氨酸内酯和取代的苏糖化合物的方法，其是合成膦酸酯核苷的中间体是有用的抗病毒剂。

3. 发明授权

US09133150B2 O-nitro compounds and pharmaceutical compositions including same 有权
标题翻译： O-硝基化合物和包含它们的药物组合物
公开(公告)号：US09133150B2
公开(公告)日：2015-09-15
申请号：US13951720
申请日：2013-07-26
申请人： Orbital ATK, Inc.
发明人： Mark D. Bednarski , Susan Knox , Louis F. Cannizzo , Kirstin F. Warner , Robert B. Wardle , Stephen P. Velarde , Shoucheng Ning
IPC分类号： C07D307/02 , C07D305/00 , C07D407/00 , C07D493/00 , A01N43/02 , A61K31/335 , C07D303/22 , A61K31/21 , A61K31/336 , A61K31/38 , A61K31/395 , A61K45/06
CPC分类号： C07D303/22 , A61K31/21 , A61K31/336 , A61K31/38 , A61K31/395 , A61K45/06
摘要： The present invention provides O-nitro compounds, pharmaceutical compositions of O-nitro compounds and methods of using O-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.
摘要翻译：本发明提供O-硝基化合物，O-硝基化合物的药物组合物和使用O-硝基化合物和/或其药物组合物的方法来治疗或预防以异常细胞增殖为特征的疾病或病症，例如癌症，炎症，心血管疾病和自身免疫性疾病。

4. 发明授权

US08916330B2 Chemically amplified photoresist composition and method for forming resist pattern 有权
标题翻译：化学扩增的光致抗蚀剂组合物和形成抗蚀剂图案的方法
公开(公告)号：US08916330B2
公开(公告)日：2014-12-23
申请号：US12821850
申请日：2010-06-23
申请人： Koji Ichikawa , Takashi Hiraoka
发明人： Koji Ichikawa , Takashi Hiraoka
IPC分类号： G03F7/004 , G03F7/40 , C07C321/00 , C07D407/00
CPC分类号： G03F7/0397 , C08F220/18 , C08F220/20 , C08F2220/303 , G03F7/0045 , G03F7/0046 , G03F7/2041
摘要： The present invention provides a resist composition giving a resist pattern excellent in CD uniformity and focus margin. A chemically amplified photoresist composition comprises a resin (A) and an acid generator (B), and the resin (A) contains, as a part or an entirety thereof, a copolymer (A1) which is obtained by polymerizing at least: a (meth)acrylic monomer (a1) having C5-20 alicyclic hydrocarbon group which becomes soluble in an aqueous alkali solution by the action of an acid; a (meth)acrylic monomer (a2) having a hydroxy group-containing adamantyl group; and a (meth)acrylic monomer (a3) having a lactone ring, and the copolymer (A1) has a weight-average molecular weight of 2500 or more and 5000 or less, and a content of the copolymer (A1) is not less than 50 parts by mass with respect to 100 parts by mass of the resin (A).
摘要翻译：本发明提供了具有优异的CD均匀性和聚焦余量的抗蚀剂图案的抗蚀剂组合物。化学放大型光致抗蚀剂组合物包含树脂（A）和酸产生剂（B），树脂（A）的一部分或全部含有共聚物（A1），其通过至少聚合得到：（甲基）丙烯酸单体（a1），其具有通过酸的作用变得可溶于碱性水溶液的C5-20脂环族烃基; 具有含羟基金刚烷基的（甲基）丙烯酸系单体（a2）和具有内酯环的（甲基）丙烯酸系单体（a3），共聚物（A1）的重均分子量为2500以上且5000以下，共聚物（A1）的含量为相对于100质量份树脂（A）为50质量份。

5. 发明授权

US08883824B2 3-(4-aminophenyl)-2-furancarboxylic acid derivative and pharmaceutically acceptable salt thereof 有权
标题翻译： 3-（4-氨基苯基）-2-呋喃甲酸衍生物及其药学上可接受的盐
公开(公告)号：US08883824B2
公开(公告)日：2014-11-11
申请号：US13320204
申请日：2010-05-12
申请人： Akihito Fujii , Kazumi Niidome , Chiaki Migihashi , Toshiyuki Kamei , Takafumi Matsumoto , Tomoyuki Hirata
发明人： Akihito Fujii , Kazumi Niidome , Chiaki Migihashi , Toshiyuki Kamei , Takafumi Matsumoto , Tomoyuki Hirata
IPC分类号： A61K31/34 , A61K31/381 , C07D307/46 , C07D407/00 , C07D307/68 , A61K31/343 , C07D307/79 , C07D333/58 , A61K31/341 , A61K31/357 , A61K31/427 , C07D407/12 , C07D409/12 , C07D417/12
CPC分类号： C07D307/68 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/381 , A61K31/427 , C07D307/46 , C07D307/79 , C07D333/58 , C07D407/12 , C07D409/12 , C07D417/12
摘要： Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is 1: a C3-8 cycloalkyl C1-4 alkyl group, 2: a C7-14 aralkyl group, in which the aryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, (b) C1-4 alkyl, which is optionally substituted with 1 to 3 fluorine atoms, (c) C1-4 alkoxy, which is optionally substituted with 1 to 3 fluorine atoms, and (d) C1-4 alkylcarbonyl, which is optionally substituted with C1-4 alkoxy, 3: a five-to ten-membered heteroaryl-C1-4 alkyl group, in which the heteroaryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, and (b) C1-4 alkyl, or 4: a C6-10 aryl C2-6 alkenyl group; and R2 is a cyano group or a nitro group.
摘要翻译：公开了由式（I）表示的化合物或其药学上可接受的盐：其中R 1为1：C 3-8环烷基C 1-4烷基，2为C 7-14芳烷基，其中芳基部分为任选的用相同或不同的1至3个选自以下的基团取代：（a）卤素，（b）任选被1至3个氟原子取代的C 1-4烷基，（c）C 1-4烷氧基，其中任选被1至3个氟原子取代，和（d）任选被C 1-4烷氧基取代的C 1-4烷基羰基，3：五至十元杂芳基-C 1-4烷基，其中杂芳基其部分任选被相同或不同的1至3个选自以下的基团取代：（a）卤素和（b）C 1-4烷基或4：C 6-10芳基C 2-6烯基; R2为氰基或硝基。

6. 发明授权

US08785669B2 Taxane compounds, compositions and methods 有权
标题翻译：紫杉烷化合物，组合物和方法
公开(公告)号：US08785669B2
公开(公告)日：2014-07-22
申请号：US13170830
申请日：2011-06-28
申请人： John K. Thottathil , Raymond P. Warrell, Jr.
发明人： John K. Thottathil , Raymond P. Warrell, Jr.
IPC分类号： C07D205/08 , C07D407/00 , C07D305/14 , C07D407/02
CPC分类号： C07D493/08 , C07D205/08 , C07D305/14 , C07D401/04 , C07D407/02
摘要： The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.
摘要翻译：本发明提供了一种制备口服可用的五环紫杉烷化合物的方法，以及可用于其制备的中间体。

7. 发明授权

US08658811B2 Process for the preparation of docetaxel, its intermediates, and methods for preparation thereof 有权
标题翻译：多西他赛制剂的制备方法，其中间体及其制备方法
公开(公告)号：US08658811B2
公开(公告)日：2014-02-25
申请号：US12741714
申请日：2009-05-22
申请人： Xin Shen , Huaxing Zhan , Jidong Yang , Xiao He , Fuxing Lin , Shaohong Wu
发明人： Xin Shen , Huaxing Zhan , Jidong Yang , Xiao He , Fuxing Lin , Shaohong Wu
IPC分类号： C07D407/00 , C07D493/00
CPC分类号： C07D305/14 , C07C269/04 , C07C269/06 , C07C271/22 , Y02P20/55
摘要： Described is a process for preparing docetaxel 1, including the following steps: a) hydroxyl acylation reaction of compound 2 and 3 to obtain compound 4; b) deprotection group R1 of the hydroxyl group of compound 4 obtained from step a to prepare compound 5; c) removing one tert-butoxycarbonyl of compound 5 obtained from step b to prepare compound 6; d) removing one acetyl of compound 6 obtained from step c to prepare compound 1; wherein, R1 represents tert-butyl dimethyl silyl, triethylsilyl, ethoxyethyl, tetrahydropyranyl, trichloroethoxycarbonyl or methoxymethyl, Boc is tert-butoxycarbonyl, Ac is acetyl, and Ph is phenyl. Also disclosed are intermediates of docetaxel and methods for preparation thereof.
摘要翻译：描述了制备多西紫杉醇1的方法，包括以下步骤：a）化合物2和3的羟基酰化反应得到化合物4; b）由步骤a获得的化合物4的羟基的脱保护基团R1，以制备化合物5; c）除去由步骤b获得的化合物5的一个叔丁氧基羰基，制备化合物6; d）除去由步骤c获得的化合物6的一个乙酰基，制备化合物1; 其中，R1表示叔丁基二甲基甲硅烷基，三乙基甲硅烷基，乙氧基乙基，四氢吡喃基，三氯乙氧基羰基或甲氧基甲基，Boc是叔丁氧基羰基，Ac是乙酰基，Ph是苯基。还公开了多西他赛的中间体及其制备方法。

8. 发明授权

US08629197B2 Chemically patterned hydrogels, manufacture and use thereof 失效
标题翻译：化学图案化水凝胶，其制造和使用
公开(公告)号：US08629197B2
公开(公告)日：2014-01-14
申请号：US12082002
申请日：2008-04-07
申请人： Molly Shoichet , Jordan Wosnick , Ryan Wylie
发明人： Molly Shoichet , Jordan Wosnick , Ryan Wylie
IPC分类号： C08F2/46 , C08J3/28 , G01N33/52 , C07D407/00
CPC分类号： C07D311/16 , C08J3/28 , C08K5/205 , C08K5/3725 , Y02P20/55
摘要： A chemically patterned modified hydrogel formed from a modified hydrogel is provided. The hydrogel is conjugated with a multiphoton photocleavable molecule. The molecule has a multiphoton-labile protective group and a protected group. The protective group is cleavable upon multiphoton excitation to deprotect the protected group, without substantial polymerization of the hydrogel. The chemically patterned modified hydrogel is formed by exposing the modified hydrogel to multiphoton excitation to deprotect a portion of the protected groups.
摘要翻译：提供由改性水凝胶形成的化学图案化的改性水凝胶。水凝胶与多光子可透光分子结合。该分子具有多光子不稳定保护基团和受保护基团。保护基团可以在多光子激发下切割，以使保护基团脱保护，而不会使水凝胶基本上聚合。化学图案化的改性水凝胶通过将改性水凝胶暴露于多光子激发以使一部分受保护基团脱保护而形成。

9. 发明授权

US08552056B2 Biologically active taxane analogs and methods of treatment by oral administration 有权
标题翻译：生物活性紫杉烷类似物和口服治疗方法
公开(公告)号：US08552056B2
公开(公告)日：2013-10-08
申请号：US13620852
申请日：2012-09-15
申请人： James D. McChesney , Gilles Tapolsky , David E. Emerson , John Marshall , Tauseef Ahmed , Allen Cohn , Michael Kurman , Manuel Modiano
发明人： James D. McChesney , Gilles Tapolsky , David E. Emerson , John Marshall , Tauseef Ahmed , Allen Cohn , Michael Kurman , Manuel Modiano
IPC分类号： A61K31/335 , A61K31/44 , C07D407/00 , C07D309/00
CPC分类号： C07D493/06 , A61K31/357 , A61K31/495 , A61K39/3955 , A61K45/06
摘要： The present invention relates to a novel chemical compound of formula S-(1): for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.
摘要翻译：本发明涉及式S-（1）的新型化合物：用于治疗癌症的组合物，含有所述化合物的组合物，制备方法和与其它治疗剂的组合。

10. 发明授权

US08354265B2 Chemicals promoting the growth of N-acylhomoserine lactone-degrading bacteria 有权
标题翻译：促进N-酰基高丝氨酸内酯降解细菌生长的化学物质
公开(公告)号：US08354265B2
公开(公告)日：2013-01-15
申请号：US12523095
申请日：2008-01-18
申请人： Denis Faure , Amélie Cirou , Yves Dessaux
发明人： Denis Faure , Amélie Cirou , Yves Dessaux
IPC分类号： C12N1/20 , C05F11/08 , C07D307/02 , C07D407/00
CPC分类号： A01N63/00 , A01N43/08 , A01N2300/00
摘要： The present invention concerns the field of bacterial biocontrol. More precisely, the invention relates to the identification of chemicals which promote the growth of bacteria inactivating NAHL, such as gamma-caprolactone (GCL) and 4-heptanolide (HTN) and their use in soil additives.
摘要翻译：本发明涉及细菌生物防治领域。更确切地说，本发明涉及促进NAHL灭活细菌生长的化学物质，如γ-己内酯（GCL）和4-庚内酯（HTN）及其在土壤添加剂中的应用。

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