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71. 发明申请

US20180207628A1 OXALIC ACID MONOAMIDE LIGAND, AND USES THEREOF IN COUPLING REACTION OF COPPER-CATALYZED ARYL HALOGEN SUBSTITUTE 审中-公开
公开(公告)号：US20180207628A1
公开(公告)日：2018-07-26
申请号：US15746646
申请日：2016-04-15
申请人： Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
发明人： Dawei Ma , Wei Zhou , Mengyang Fan , Haibo Wu , Junli Yin , Shanghua Xia
IPC分类号： B01J31/22 , C07B41/02 , C07B43/04 , C07B45/06 , C07C233/56 , C07C231/14 , C07D317/58 , C07D307/52 , C07D307/81 , C07D333/20 , C07D207/335 , C07D213/40 , C07D317/28 , C07D207/14 , C07D307/22 , C07D295/00 , C07D207/06 , C07D495/04 , C07D239/42 , C07D241/20 , C07D213/89 , C07D215/38 , C07D217/22 , C07D317/66 , C07D335/16 , C07D277/64 , C07D295/135 , C07D277/66 , C07D215/40 , C07D241/42 , C07D471/04 , C07D213/73 , C07D207/325 , C07D263/56 , C07D213/65 , C07D295/096 , C07D317/64 , C07D215/20 , C07D241/18 , C07D209/86 , C07D231/12 , C07D233/60 , C07C209/10 , C07C209/08 , C07C213/02 , C07C221/00 , C07C41/26 , C07C319/20 , C07C45/64 , C07C253/30 , C07C213/08 , C07C319/14 , C07C231/12 , C07C315/04
CPC分类号： B01J31/2243 , B01J31/22 , B01J2231/4283 , B01J2231/4288 , B01J2231/4294 , B01J2531/16 , C07B41/02 , C07B43/04 , C07B45/06 , C07C41/26 , C07C45/64 , C07C209/08 , C07C209/10 , C07C213/02 , C07C213/08 , C07C221/00 , C07C231/02 , C07C231/12 , C07C231/14 , C07C233/56 , C07C253/30 , C07C315/04 , C07C319/14 , C07C319/20 , C07D207/06 , C07D207/14 , C07D207/27 , C07D207/325 , C07D207/335 , C07D209/08 , C07D209/86 , C07D211/72 , C07D213/40 , C07D213/65 , C07D213/73 , C07D213/74 , C07D213/89 , C07D215/20 , C07D215/38 , C07D215/40 , C07D217/22 , C07D223/12 , C07D223/22 , C07D231/12 , C07D233/60 , C07D239/42 , C07D239/545 , C07D241/18 , C07D241/20 , C07D241/42 , C07D263/56 , C07D277/64 , C07D277/66 , C07D295/00 , C07D295/096 , C07D295/135 , C07D307/22 , C07D307/52 , C07D307/81 , C07D317/28 , C07D317/58 , C07D317/64 , C07D317/66 , C07D333/20 , C07D333/36 , C07D333/54 , C07D333/58 , C07D335/16 , C07D471/04 , C07D495/04
摘要： The present invention provides oxalic amide ligands and uses thereof in copper-catalyzed coupling reaction of aryl halides. Specifically, the present invention provides a use of a compound represented by formula I, wherein definitions of each group are described in the specification. The compound represented by formula I can be used as a ligand in copper-catalyzed coupling reaction of aryl halides for the formation of C—N, C—O and C—S bonds.

72. 发明授权

US09931315B2 Method of selectively inhibiting Ras-mediated tumor growth in humans 有权
公开(公告)号：US09931315B2
公开(公告)日：2018-04-03
申请号：US15056202
申请日：2016-02-29
申请人： ADT PHARMACEUTICALS, INC.
发明人： Gary A. Piazza , Xi Chen , Adam B. Keeton , Michael R. Boyd
IPC分类号： A61K31/341 , C07D307/52 , C07C235/34 , C07D213/75 , C07D207/14 , C07D213/40 , C07D207/335 , C07C311/29 , A61K31/165 , A61K31/216 , A61K31/401 , A61K31/421 , A61K31/4402 , A61K31/4406 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/167 , A61K31/40 , A61K45/06 , G01N33/574
CPC分类号： C07D317/64 , A61K31/165 , A61K31/167 , A61K31/216 , A61K31/341 , A61K31/36 , A61K31/40 , A61K31/401 , A61K31/421 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/445 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K45/06 , A61K2300/00 , C07C233/58 , C07C235/32 , C07C235/34 , C07C237/20 , C07C311/29 , C07C2601/02 , C07C2602/08 , C07D207/14 , C07D207/335 , C07D207/337 , C07D211/56 , C07D213/24 , C07D213/40 , C07D213/75 , C07D235/30 , C07D307/38 , C07D307/52 , C07D307/54 , C07D405/12 , G01N33/5748 , A61K2800/00
摘要： Disclosed are compounds, for example, a compound of formula I, wherein R, R0, R1-R8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition for example, cancer, mediated by the ras gene.

73. 发明授权

US09386767B2 Derivatives of dillapiol and related monolignans and use thereof 有权
标题翻译：狄拉波醇及相关单宁族的衍生物及其用途
公开(公告)号：US09386767B2
公开(公告)日：2016-07-12
申请号：US13469870
申请日：2012-05-11
申请人： John Thor Arnason , Tony Durst , Brian Foster
发明人： John Thor Arnason , Tony Durst , Brian Foster
IPC分类号： A01N43/30 , C07D317/54 , A01N53/00 , C07D317/64 , C07D317/68
CPC分类号： A01N43/30 , C07D317/54 , C07D317/64 , C07D317/68 , A01N2300/00 , A01N53/00
摘要： Derivatives of dillapiol, sesamol and related monolignans having the following general formula: These compounds have synergistic properties, inhibit cytochrome P450 enzymes such as human CYP3A4, and can be used as pesticide synergists or pharmaco-enhancers. Accordingly, methods for increasing the efficacy and/or bioavailability of a pharmaceutically active agent and for increasing the potency of a pesticide are described, as are synergistic pesticidal and pharmaceutical compositions.
摘要翻译：狄拉波酚，芝麻酚和相关单宁酸衍生物具有以下通式：这些化合物具有协同作用，抑制细胞色素P450酶如人CYP3A4，可用作农药增效剂或药物增强剂。因此，描述了用于提高药物活性剂的功效和/或生物利用度并提高农药效力的方法，协同杀虫剂和药物组合物也是如此。

74. 发明申请

US20150158809A9 METHOD OF MAKING 1-(ACYLOXY)-ALKYL CARBAMATE COMPOUNDS 审中-公开
标题翻译：制备1-（氰基） - 烷基碳酸酯化合物的方法
公开(公告)号：US20150158809A9
公开(公告)日：2015-06-11
申请号：US14189555
申请日：2014-02-25
申请人： XENOPORT, INC.
发明人： Huan Wang , Peng Liu , Qunying Dai , Hao Yin , Stephen P. Raillard
IPC分类号： C07C69/96 , C07C255/57 , C07C269/00
CPC分类号： C07C69/96 , C07C68/06 , C07C235/46 , C07C235/60 , C07C255/55 , C07C255/57 , C07C269/00 , C07C269/04 , C07C317/22 , C07C2601/14 , C07D317/64 , C07D319/18 , C07C271/22
摘要： Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
摘要翻译：提供了制备含胺药物的氨基甲酸酯前药的方法。还提供了可用于合成氨基甲酸酯前药的碳酸酯。

75. 发明授权

US08791156B2 Polyacetylene compound, an extract containing the same and application thereof 有权
标题翻译：聚乙炔化合物，含有该聚乙炔化合物的提取物及其应用
公开(公告)号：US08791156B2
公开(公告)日：2014-07-29
申请号：US13323057
申请日：2011-12-12
申请人： Sheng-Yang Wang , Ting-Yu Lin , Chieh-Yin Chen , Shih-Chang Chien , Wen-Wei Hsiao , Fang-Hua Chu , Wen-Hsiung Li , Jei-Fu Shaw , Chin-Chung Lin
发明人： Sheng-Yang Wang , Ting-Yu Lin , Chieh-Yin Chen , Shih-Chang Chien , Wen-Wei Hsiao , Fang-Hua Chu , Wen-Hsiung Li , Jei-Fu Shaw , Chin-Chung Lin
IPC分类号： A61K31/36 , C07D317/64
CPC分类号： A61K31/36 , C07D317/64
摘要： A polyacetylenes and application thereof. The polyacetylenes is isolated from an extract of the sporophores of Antrodia Cinnamomea and has a function of inhibiting the production of nitric oxide. Therefore, the polyacetylenes can be used for preparing a pharmaceutical composition for anti-inflammation. The present invention also teaches the representative metabolites of the sporophores of Antrodia Cinnamomea, which can be used to evaluate the quality thereof.
摘要翻译：聚乙炔及其应用。聚氧乙烯从番木瓜抗孢子虫的提取物中分离，具有抑制一氧化氮生成的功能。因此，聚乙炔可用于制备用于抗炎的药物组合物。本发明还教导了可以用于评价其品质的Antrodia Cinnamomea孢子的代表性代谢物。

76. 发明授权

US08716499B2 Benzenoid compounds of antrodia cinnamomea, preparation and analysis method thereof 有权
标题翻译：桂皮酚的苯并噻吩类化合物，其制备及分析方法
公开(公告)号：US08716499B2
公开(公告)日：2014-05-06
申请号：US13346300
申请日：2012-01-09
申请人： Yang-Chang Wu , Fang-Rong Chang , Mei-Chin Lu , Ying-Chi Du , Tung-Ying Wu , Yu-Ming Hsu
发明人： Yang-Chang Wu , Fang-Rong Chang , Mei-Chin Lu , Ying-Chi Du , Tung-Ying Wu , Yu-Ming Hsu
IPC分类号： C07D317/48
CPC分类号： C07D317/64 , C07C41/38 , G01N2030/8813 , C07C43/215
摘要： Disclosed are a method for preparing an n-hexane extract of the fruiting body of Antrodia cinnamomea (AC), wherein the fruiting body of AC is sequentially extracted with the ethanol solution and the n-hexane solution to obtain the n-hexane extract containing at least one benzenoid compound. The amounts of 4,7-dimethoxy-5-(3-methylbut-3-en-1-ynyl)-6-methyl-1,3-benzodioxole, 4,7-dimethoxy-5-methyl-1,3-benzodioxole, antrocamphine A and the combination thereof in the at least one benzenoid compound are determined using chromatography, NMR and HPLC. In addition, the present invention is applicable on detecting the amounts of benzenoid compounds in the AC healthcare food/drug or the fruiting body of AC, and thus owns the industrial values.
摘要翻译：本发明提供了一种用于制备仙人掌（AC）子实体的正己烷提取物的方法，其中AC的子实体依次用乙醇溶液和正己烷溶液萃取，得到含有至少一种苯类化合物。 4,7-二甲氧基-5-（3-甲基丁-3-烯-1-炔基）-6-甲基-1,3-苯并间二氧杂环戊烯，4,7-二甲氧基-5-甲基-1,3-苯并间二氧杂环戊烯，抗阿奇霉素A及其在至少一种苯类化合物中的组合使用色谱法，NMR和HPLC测定。此外，本发明可应用于检测AC保健食品/药物或AC的子实体中的苯类化合物的量，因此具有工业价值。

77. 发明授权

US08710096B2 Detection and use of low molecular-weight modulators of the cold-menthol receptor TRPM8 有权
标题翻译：检测和使用低分子量的冷 - 薄荷醇受体TRPM8的调节剂
公开(公告)号：US08710096B2
公开(公告)日：2014-04-29
申请号：US13060323
申请日：2009-08-26
申请人： Thomas Subkowski , Claus Bollschweiler , Jens Wittenberg , Michael Krohn , Holger Zinke
发明人： Thomas Subkowski , Claus Bollschweiler , Jens Wittenberg , Michael Krohn , Holger Zinke
IPC分类号： A61K31/00 , A61Q11/00
CPC分类号： C07D495/22 , A23L27/88 , A61K8/42 , A61K8/49 , A61K8/4926 , A61K8/4946 , A61K8/4953 , A61K8/4973 , A61K8/69 , A61K31/00 , A61K2800/244 , A61K2800/78 , A61Q5/02 , A61Q11/00 , A61Q17/02 , A61Q17/04 , A61Q19/004 , C07C275/28 , C07D211/14 , C07D233/84 , C07D241/44 , C07D317/64 , C07D401/04 , C07D401/12 , C07D409/12 , C07D495/20
摘要： The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.
摘要翻译：本发明涉及冷薄荷醇受体TRPM8的新型调节剂，涉及使用所述调节剂调节TRPM8受体的方法; 使用调制器诱导感冒; 以及使用所述调制器产生的物体和装置。

78. 发明申请

US20140018390A1 DEUTERATED BENZO[D][1,3]-DIOXOL DERIVATIVES 审中-公开
标题翻译： DEUTERATED BENZO [D] [1,3] -DIOXOL DERIVATIVES
公开(公告)号：US20140018390A1
公开(公告)日：2014-01-16
申请号：US13901651
申请日：2013-05-24
申请人： Roger D. Tung
发明人： Roger D. Tung
IPC分类号： C07D405/12
CPC分类号： A61K31/4525 , C07D317/64 , C07D405/12
摘要： The present invention relates to an isotopologue of Compound 1 substituted with deuterium at the methylene carbon of the benzodioxol ring. The isotopologues of this invention selective serotonin reuptake inhibitors (SSRIs) and possess unique biopharmaceutical and metabolic properties compared to Compound 1. They may also be used to accurately determine the concentration of Compound 1 in biological fluids and to determine metabolic patterns of Compound 1 and its isotopologues. The invention further provides compositions comprising these deuterated isotopologues and methods of treating diseases and conditions that are responsive to increased neuronal serotonin transmission, alone and in combination with additional agents.
摘要翻译：本发明涉及在苯并二氧杂环戊烯的亚甲基碳上被氘取代的化合物1的同位素学。本发明的同位素学选择性5-羟色胺再摄取抑制剂（SSRIs）并且与化合物1相比具有独特的生物药物和代谢性质。它们还可用于精确测定化合物1在生物流体中的浓度并确定化合物1及其化合物1的代谢模式同位素学。本发明还提供包含这些氘代同位素异构体的组合物和治疗对增加的神经元血清素传递起反应的疾病和病症的方法，其单独和与另外的试剂组合。

79. 发明授权

US08614345B2 Hydrogenation of esters or carbonyl groups with tetradentate amino/imino-thioether based ruthenium complexes 有权
标题翻译：用四齿氨基/亚氨基 - 硫醚基钌配合物氢化酯或羰基
公开(公告)号：US08614345B2
公开(公告)日：2013-12-24
申请号：US13996847
申请日：2011-12-19
申请人： Francesco Santoro , Lionel Saudan , Michel Alfred Joseph Saudan , Sylvia Joyeuse Adélaïde Ada Saudan
发明人： Francesco Santoro , Lionel Saudan , Christophe Saudan
IPC分类号： C07F15/00 , C07C29/141 , C07C29/145 , C07D317/54
CPC分类号： C07C37/56 , C07B2200/07 , C07C29/145 , C07C323/32 , C07C323/45 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07C2602/32 , C07D307/58 , C07D317/64 , C07F15/0053 , C07C33/22 , C07C35/36 , C07C33/20 , C07C33/14 , C07C31/125 , C07C33/30 , C07C35/06 , C07C35/23 , C07C35/08 , C07C33/18 , C07C33/34 , C07C33/02 , C07C33/12 , C07C33/025
摘要： The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of specific ruthenium catalysts, or pre-catalysts, in hydrogenation processes for the reduction of ketones and/or aldehydes into the corresponding alcohol respectively. Said catalysts are ruthenium complexes comprising a tetradentate ligand (L4) coordinating the ruthenium with: —two nitrogen atoms, each in the form of a primary or secondary amine (i.e. a NH2 or NH group) or N-alkyl imine functional groups (i.e. a C═N group), and —two sulfur atoms, each in the form of thioether functional groups.
摘要翻译：本发明涉及催化氢化领域，更具体地说，涉及在用于将酮和/或醛分别还原成相应的醇的氢化方法中使用特定的钌催化剂或预催化剂。所述催化剂是包含四配位配位体（L4）的钌络合物，所述四齿配位体（L4）将钌配位为： - 两个氮原子，每个氮原子为伯胺或仲胺（即NH 2或NH基）或N-烷基亚胺官能团 C = N基团）和两个硫原子，各自为硫醚官能团的形式。

80. 发明授权

US08450492B2 Deuterated benzo[D][1,3]-dioxol derivatives 有权
标题翻译：氘代苯并[D] [1,3] - 二氧杂环戊烯衍生物
公开(公告)号：US08450492B2
公开(公告)日：2013-05-28
申请号：US12688466
申请日：2010-01-15
申请人： Roger Tung
发明人： Roger Tung
IPC分类号： C07D211/22
CPC分类号： A61K31/4525 , C07D317/64 , C07D405/12
摘要： The present invention relates to an isotopologue of Compound 1 substituted with deuterium at the methylene carbon of the benzodioxol ring. The isotopologues of this invention selective serotonin reuptake inhibitors (SSRIs) and possess unique biopharmaceutical and metabolic properties compared to Compound 1. They may also be used to accurately determine the concentration of Compound 1 in biological fluids and to determine metabolic patterns of Compound 1 and its isotopologues. The invention further provides compositions comprising these deuterated isotopologues and methods of treating diseases and conditions that are responsive to increased neuronal serotonin transmission, alone and in combination with additional agents.
摘要翻译：本发明涉及在苯并二氧杂环戊烯的亚甲基碳上被氘取代的化合物1的同位素学。本发明的同位素学选择性5-羟色胺再摄取抑制剂（SSRIs）并且与化合物1相比具有独特的生物药物和代谢性质。它们还可用于精确测定化合物1在生物流体中的浓度并确定化合物1及其化合物1的代谢模式同位素学。本发明还提供包含这些氘代同位素异构体的组合物和治疗对增加的神经元血清素传递起反应的疾病和病症的方法，其单独和与另外的试剂组合。

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