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81. 发明申请

WO2019210223A1 ANTICANCER INDENES, INDANES, AZAINDENES, AZAINDANES, PHARMACEUTICAL COMPOSITIONS AND USES 审中-公开
公开(公告)号：WO2019210223A1
公开(公告)日：2019-10-31
申请号：PCT/US2019/029430
申请日：2019-04-26
申请人： ADT PHARMACEUTICALS, LLC
发明人： BOYD, Michael , CHEN, Xi
IPC分类号： A61K31/192 , A61K31/4035 , A61K31/435 , A61K31/437 , A61K31/661 , A61K31/69 , A61P35/00
摘要： Disclosed are compounds for medical uses, for example, compounds of formula (Ia), wherein A 1 , A 2, A 3 , A 4 , A 5 , A 6 , A 7 , R 6 , R 7 and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

82. 发明申请

WO2017100500A1 VESICLE CONTAINING METALLIC NANOPARTICLE AND METHOD FOR PRODUCTION THEREOF 审中-公开
标题翻译：含有金属纳米粒子的微粒及其生产方法
公开(公告)号：WO2017100500A1
公开(公告)日：2017-06-15
申请号：PCT/US2016/065708
申请日：2016-12-09
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
发明人： CHEN, Xiaoyuan , SONG, Jibin
IPC分类号： A61K9/127 , A61K41/00 , B01F17/00
CPC分类号： A61K9/1272 , A61K9/5115 , A61K41/0052 , A61K49/225 , A61K51/1244 , B01J13/12
摘要： Disclosed is a method of producing a vesicle containing a metallic nanoparticle that is covalently bound to at least one hydrophilic polymer and at least one hydrophobic polymer, wherein the method involves dispersing the polymer-bound metallic nanoparticle in an organic solvent, adding an aqueous solution containing a dispersing aid to form a mixed solution, sonicating the mixed solution to form an emulsion; and removing the organic solvent from the emulsion until the vesicle forms. Using this method, the formed vesicle has a diameter of 20-150 nm, which is useful for a method of conducting photothermal therapy (PTT) for killing cells, such as cancer cells.
摘要翻译：公开了一种制备含有与至少一种亲水性聚合物和至少一种疏水性聚合物共价结合的金属纳米粒子的囊泡的方法，其中所述方法包括将聚合物结合的金属纳米粒子分散在加入含有分散助剂的水溶液以形成混合溶液，对混合溶液进行超声波处理以形成乳液; 并从乳液中除去有机溶剂直至形成囊泡。使用该方法，形成的囊泡具有20-150nm的直径，这对于进行光热疗法（PTT）杀死细胞如癌细胞的方法是有用的。

83. 发明申请

WO2016204988A1 AUTOPHAGY MODULATORS FOR TREATING NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：用于治疗神经病变疾病的自动调节器
公开(公告)号：WO2016204988A1
公开(公告)日：2016-12-22
申请号：PCT/US2016/035830
申请日：2016-06-03
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
发明人： DEPAMPHILIS, Melvin Louis , PARSONS, Lori N.
IPC分类号： A61K31/5377 , A61K31/53 , A61K31/506 , A61P25/00 , A61P25/16 , A61P25/28
CPC分类号： A61K31/53 , A61K31/506 , A61K31/5377
摘要： Disclosed is a method of decreasing an amount of protein aggregate in a cell comprising contacting the cell with a compound of the formula (I): wherein R 1 , R 2 , and R 3 are as defined herein, in an amount sufficient to induce autophagy in the cell and cause the degradation of the protein aggregate within the cell. Also disclosed is a method of treating or preventing a condition, syndrome, or disease in a mammal in need thereof, wherein the condition, syndrome, or disease is selected from Huntington's disease, Alzheimer's disease, Parkinson's disease, Hutchinson-Gilford progeria syndrome, Niemann-Pick type C disease, spinobulbar muscular atrophy (Kennedy disease), dentatorubral-pallidoluysian atrophy (Haw-River syndrome), spinocerebellar ataxia type 1, spinocerebellar ataxia type 2, spinocerebellar ataxia type 3, spinocerebellar ataxia type 6, and spinocerebellar ataxia type 7, comprising administering to the mammal the compound.
摘要翻译：公开了减少细胞中蛋白质聚集体的量的方法，包括使细胞与式（I）化合物（其中R 1，R 2和R 3如本文所定义）以足以诱导细胞自噬的量接触并导致细胞内蛋白质聚集体的降解。还公开了治疗或预防有需要的哺乳动物的病症，综合征或疾病的方法，其中所述病症，综合征或疾病选自亨廷顿舞蹈病，阿尔茨海默氏病，帕金森氏病，哈奇森 - 吉尔福德原始综合征，尼曼柯氏C型疾病，棘皮肌肉萎缩（肯尼迪病），牙弓 - 苍白球萎缩症（Haw-River综合征），1型脊髓小脑性共济失调，2型脊髓小脑共济失调，3型脊髓小脑共济失调，6型脊髓小脑共济失调和7型脊髓小脑共济失调包括向哺乳动物施用该化合物。

84. 发明申请

WO2016100546A1 METHOD OF TREATING OR PREVENTING RAS-MEDIATED DISEASES 审中-公开
标题翻译：治疗或预防RAS介导的疾病的方法
公开(公告)号：WO2016100546A1
公开(公告)日：2016-06-23
申请号：PCT/US2015/066154
申请日：2015-12-16
申请人： ADT PHARMACEUTICALS, INC.
发明人： PIAZZA, Gary A , CHEN, Xi , KEETON, Adam B , BOYD, Michael R
IPC分类号： A61K31/165 , A61K31/216 , A61K31/401 , A61K31/421 , A61K31/4402 , A61K31/4406 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61P35/00
CPC分类号： A61K31/341 , A61K31/165 , A61K31/167 , A61K31/216 , A61K31/40 , A61K31/401 , A61K31/421 , A61K31/4402 , A61K31/4406 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07C235/34 , C07C311/29 , C07D207/14 , C07D207/335 , C07D213/40 , C07D213/75 , C07D307/52 , G01N33/5748 , A61K2800/00
摘要： Disclosed are compounds, for example, a compound of formula I, wherein R, R 0 , R 1 -R 8 , 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.
摘要翻译：公开了化合物，例如式I化合物，其中R，R 0，R 1 -R 8，n，X，Y，Y'和E如本文所述，含有这些化合物的药物组合物，以及治疗或预防的方法由ras基因介导的疾病或病症，例如癌症。

85. 发明申请

WO2015080940A1 A3 ADENOSINE RECEPTOR AGONISTS 审中-公开
标题翻译： A3腺苷受体激动剂
公开(公告)号：WO2015080940A1
公开(公告)日：2015-06-04
申请号：PCT/US2014/066609
申请日：2014-11-20
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , SAINT LOUIS UNIVERSITY
发明人： JACOBSON, Kenneth A. , TOSH, Dilip K. , SALVEMINI, Daniela
IPC分类号： C07D473/00 , C07D473/34 , A61K31/52 , A61P29/00
CPC分类号： C07D473/34 , C07D473/00 , C07F15/02
摘要： Disclosed are compounds of the formula (I) and (II) which are A 3 adenosine receptor agonists, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X, Y, Z, R 2 -R 6 , and R 103 -R 106 are as defined in the specification. These compounds are selective to the A 3 receptor, and are contemplated for use in the treatment or prevention of a number of diseases or conditions, for example, neuropathic pain.
摘要翻译：公开了作为A3腺苷受体激动剂的式（I）和（II）的化合物，包含这些化合物的药物组合物和这些化合物的使用方法，其中X，Y，Z，R 2 -R 6和R 103-R 106 如说明书中所定义。这些化合物对A3受体是选择性的，并且被考虑用于治疗或预防许多疾病或病症，例如神经性疼痛。

86. 发明申请

WO2015035003A1 THIOETHER PRODRUG COMPOSITIONS AS ANTI-HIV AND ANTI-RETROVIRAL AGENTS 审中-公开
标题翻译：作为抗HIV和抗逆转录病毒药物的抗生素组合物
公开(公告)号：WO2015035003A1
公开(公告)日：2015-03-12
申请号：PCT/US2014/054019
申请日：2014-09-04
申请人： THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
发明人： APPELLA, Daniel , KUMAR, Pankaj , SHANK, Nathaniel , HASSINK, Matthew David
IPC分类号： C07C323/62 , A61K31/166 , A61P31/14
CPC分类号： C07C323/62
摘要： Disclosed are inhibitors of retroviral growth of formula (I), that are useful in treatment of retroviral infections such as HIV. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, a method for inactivating a virus, a method for dissociating a metal ion from a zinc finger-containing protein method, and a method for inhibiting the transmission of a virus, wherein R is hydrogen or a linear or branched alkyl.
摘要翻译：公开了式（I）的逆转录病毒生长抑制剂，其可用于治疗逆转录病毒感染如HIV。还公开了包含药学上可接受的载体和本发明的至少一种化合物或盐的组合物，用于灭活病毒的方法，从含锌指蛋白质的蛋白质方法中分离金属离子的方法，以及抑制病毒的传播，其中R是氢或直链或支链烷基。

87. 发明申请

WO2013036743A1 IMAGING AGENTS FOR IMAGING PROTEASE ACTIVITY AND USES THEREOF 审中-公开
标题翻译：成像剂用于成像蛋白酶活性及其用途
公开(公告)号：WO2013036743A1
公开(公告)日：2013-03-14
申请号：PCT/US2012/054121
申请日：2012-09-07
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , CHEN, Xiaoyuan , LEE, Seulki , ZHU, Lei
发明人： CHEN, Xiaoyuan , LEE, Seulki , ZHU, Lei
IPC分类号： A61K47/48 , A61K49/00
CPC分类号： A61K49/0032 , A61K47/65 , A61K49/0054 , A61K49/0056 , A61N5/062
摘要： Disclosed are imaging agents having the following Formula I: (I); wherein F is a near infrared fluorophore, S is an enzymatically cleavable oligopeptide, Q is a fluorescence quencher molecule, and M is a moiety selected from the group consisting of PEG or derivative thereof and a targeting ligand, and wherein F, Q and M are linked to separate amino acids of the enzymatically cleavable oligopeptide. Compositions comprising such compounds, as well as methods of use, methods of identifying a cell or a population of cells in vivo expressing a protease of interest, and methods of treating a disease through imaging are also disclosed.
摘要翻译：公开了具有以下式I的成像剂：（I）; 其中F是近红外荧光团，S是可酶促切割的寡肽，Q是荧光猝灭剂分子，M是选自PEG或其衍生物和靶向配体的部分，其中F，Q和M是与酶切割的寡肽的分离的氨基酸连接。还公开了包含这些化合物的组合物，以及使用方法，鉴定体内表达感兴趣的蛋白酶的细胞或细胞群体的方法，以及通过成像治疗疾病的方法。

88. 发明申请

WO2012148889A1 INHIBITORS OF HUMAN APURINIC/APYRIMIDINIC ENDONUCLEASE 1 审中-公开
标题翻译：人类APURINIC / APYRIMIDINIC内切酶的抑制剂1
公开(公告)号：WO2012148889A1
公开(公告)日：2012-11-01
申请号：PCT/US2012/034755
申请日：2012-04-24
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , MALONEY, David J. , BANTUKALLU, Ganesha Rai , JADHAV, Ajit , WILSON III, David M. , SIMEONOV, Anton
发明人： MALONEY, David J. , BANTUKALLU, Ganesha Rai , JADHAV, Ajit , WILSON III, David M. , SIMEONOV, Anton
IPC分类号： C07D495/04 , A61K31/55 , A61K31/428 , A61P35/00
CPC分类号： C07D495/04
摘要： Disclosed are inhibitors of human APE1, for example, of formula (I), wherein A, B, X, R 2 , and R 3 are as defined herein, that are useful in treating an APE1 mediated disease or disorder, e.g., cancer. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of treating cancer in a mammal and a method of potentiating treatment of cancer.
摘要翻译：公开了人APE1的抑制剂，例如式（I）的化合物，其中A，B，X，R 2和R 3如本文所定义，其可用于治疗APE1介导的疾病或病症，例如癌症。还公开了包含药学上合适的载体和本发明的至少一种化合物，治疗哺乳动物的癌症的方法和增强癌症治疗的方法的组合物。

89. 发明申请

WO2012138530A1 2'-O-AMINOOXYMETHYL NUCLEOSIDE DERIVATIVES FOR USE IN THE SYNTHESIS AND MODIFICATION OF NUCLEOSIDES, NUCLEOTIDES AND OLIGONUCLEOTIDES 审中-公开
标题翻译：用于合成和修饰核苷酸，核苷酸和寡核苷酸的2'-O-氨基甲基甲基衍生物
公开(公告)号：WO2012138530A1
公开(公告)日：2012-10-11
申请号：PCT/US2012/031107
申请日：2012-03-29
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , BEAUCAGE, Serge L. , CIESLAK, Jacek
发明人： BEAUCAGE, Serge L. , CIESLAK, Jacek
IPC分类号： C07H19/02
CPC分类号： C07H19/16 , C07H1/00 , C07H19/048 , C07H19/06 , C07H23/00 , Y02P20/55
摘要： Disclosed are O -protected compounds of the formula (I):wherein B is an optionally protected nucleobase, and R 1 -R 3 are as described herein, a method of preparing such compounds, and a method of preparing oligonucleotides such as RNA starting from such compounds. The O -protected compounds have one or more advantages, for example, the 2'- O -protected compound is stable during the various reaction steps involved in oligonucleotide synthesis; the protecting group can be easily removed after the synthesis of the oligonucleotide, for example, by reaction with tetrabutylammonium fluoride; and/or the O -protected groups do not generate DNA/RNA alkylating side products, which have been reported during removal of 2'- O -(2-cyanoethyl)oxymethyl or 2'- O -[2-(4-tolylsulfonyl)ethoxymethyl groups under similar conditions.
摘要翻译：公开了式（I）的O-保护的化合物：其中B是任选保护的核碱基，并且R 1 -R 3如本文所述，制备此类化合物的方法，以及从这些化合物开始制备寡核苷酸例如RNA的方法。 O保护的化合物具有一个或多个优点，例如，2'-O-保护的化合物在涉及寡核苷酸合成的各种反应步骤期间是稳定的; 在寡核苷酸的合成之后，可以容易地除去保护基，例如通过与四丁基氟化铵反应; 和/或O-保护基团不产生DNA / RNA烷基化副产物，其在除去2'-O-（2-氰基乙基）氧基甲基或2'-O- [2-（4-甲苯磺酰基）乙氧基甲基。

90. 发明申请

WO2012094334A1 ONE-STEP 18F LABELING OF BIOLOGICAL SUBSTRATES AND USES OF 18F LABELED BIOLOGICAL SUBSTRATES 审中-公开
标题翻译：生物基质的一步18F标记和18F标记生物基质的使用
公开(公告)号：WO2012094334A1
公开(公告)日：2012-07-12
申请号：PCT/US2012/020098
申请日：2012-01-03
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , CHEN, Xiaoyuan , JACOBSON WEISS, Orit
发明人： CHEN, Xiaoyuan , JACOBSON WEISS, Orit
IPC分类号： C07B59/00 , C07D259/00
CPC分类号： C07B59/008 , C07D259/00
摘要： Disclosed is a rapid one-step 18 F radiolabeling method for biological substrates that contain a specific arene group activated for nucleophilic aromatic substitution with 18 F. The method involves reacting a biological substrate having at least one 4-nitro-3-trifluorobenzamide moiety covalently bonded thereto with a 18 F anion in the presence of a cryptand. The method of the present invention has one or more advantages: significantly shortens reaction and overall synthesis time; requires low amount of precursor; and provides acceptable yields of high specific activity product. Also disclosed are methods of identifying a cell or population of cells expressing a protein or peptide of interest and methods for diagnosing a disease in a subject. Further disclosed are 18 F labeled compounds of formula (I): wherein X, n, R 1 , R 2 , and R 3 are as described herein.
摘要翻译：公开了一种用于生物底物的快速一步18F放射性标记方法，其包含用18F活化的亲核芳香取代的特定芳族基团。该方法包括使具有至少一个共价键合的4-硝基-3-三氟苯甲酰胺部分的生物底物与18F阴离子在穴状物存在下反应。本发明的方法具有一个或多个优点：显着缩短反应和总合成时间; 需要少量的前体; 并提供可接受的高比活性产品的产率。还公开了鉴定表达感兴趣的蛋白质或肽的细胞或细胞群的方法以及用于诊断受试者中的疾病的方法。进一步公开的是18F标记的式（I）化合物：其中X，n，R 1，R 2和R 3如本文所述。

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