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51. 发明申请

WO2006135715A1 BENZTROPINAMINE ANALOGS AS DOPAMINE UPTAKE INHIBITORS 审中-公开
标题翻译：苯并吡喃胺类似物作为多巴胺摄取抑制剂
公开(公告)号：WO2006135715A1
公开(公告)日：2006-12-21
申请号：PCT/US2006/022401
申请日：2006-06-07
申请人： GOVERNMENT OF THE UNITED STATES OF AMERICA, REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , NEWMAN, Amy Hauck , GRUNDT, Peter , KATZ, Jonathan L.
发明人： NEWMAN, Amy Hauck , GRUNDT, Peter , KATZ, Jonathan L.
IPC分类号： A61K31/439 , C07D451/04 , A61P25/30
CPC分类号： C07D451/04
摘要： Disclosed are benztropinamine analogs having the formula I (I) in which E is NR 1 , S, or CH 2 ; B is NR 4 , O, or CH 2 ; m = 1 to 5; n = 1 to 3; Ar is a C 5 -C 20 monocyclic aryl group or a C 10 -C 20 bicyclic aryl group or a heteroaryl group having 2 to 6 carbon atoms and one or more heteroatoms selected from the group consisting of N, O, S, and any combination thereof; and bond "a" can be of α, β, or α/β configuration, wherein R 1 to R 5 are as described in the specification; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions and use thereof, e.g., in treating mental disorders.
摘要翻译：公开了具有式I（I）的苯并丙胺类似物，其中E是NR 1，S或CH 2; B是NR 4，O或CH 2; m = 1〜5; n = 1〜3; Ar是C 5 -C 20 20单环芳基或C 10-20 -C 20双环芳基或具有2至6个碳原子的杂芳基和一个或多个选自N，O，S的杂原子及其任何组合; 并且键“a”可以是ß或a /β构型，其中R 1至R 5是如说明书中所述; 或其药学上可接受的盐或溶剂化物; 药物组合物及其用途，例如治疗精神障碍。

52. 发明申请

WO2006036288A2 METHOD FOR MONITORING EARLY TREATMENT RESPONSE 审中-公开
标题翻译：用于监测早期治疗反应的方法
公开(公告)号：WO2006036288A2
公开(公告)日：2006-04-06
申请号：PCT/US2005/027060
申请日：2005-07-29
申请人： RECEPTOMON, LLC , NORFRAY, Joseph F
发明人： NORFRAY, Joseph F
IPC分类号： A61B5/05
CPC分类号： A61B5/055 , A61B5/4833 , G01N24/08 , G01R33/465 , G06F19/00 , G06F19/3456 , G06F19/3481
摘要： Disclosed is a method for monitoring early treatment response of a cancer treatment comprising measuring by magnetic resonance spectroscopy (MRS), for example, proton MRS, the amount of Choline present in the cancerous tissue before and after treatment; the treatment comprises administration of a cell surface receptor inhibitor, for example, an EGFR inhibitor, whereby a decrease in the amount of Choline after treatment is indicative of a positive response. The decrease in the amount of Choline represents the decrease in the internal cell membrane as a result of down regulation of the organelles and their secretory granules and their transport vesicles. Disclosed also is a method for determining effectiveness of a cell surface receptor inhibitor in the treatment of cancer. Further, the present invention provides for a method for monitoring protein translation in an animal having a cancerous tissue by MRS.
摘要翻译：公开了一种用于监测癌症治疗的早期治疗反应的方法，包括通过磁共振光谱（MRS）测量例如质子MRS，治疗前后癌组织中存在的胆碱的量; 治疗包括施用细胞表面受体抑制剂例如EGFR抑制剂，由此治疗后胆碱量的减少表示阳性反应。由于细胞器及其分泌颗粒及其运输囊泡的下调，胆碱的量的减少代表内细胞膜的减少。还公开了一种确定细胞表面受体抑制剂治疗癌症的有效性的方法。此外，本发明提供了通过MRS具有癌组织的动物监测蛋白质翻译的方法。

53. 发明申请

WO2021127133A1 N-(3-AMINO-3-OXOPROPYL)-2-[(1-METHYL-4-NITRO-1H-IMIDAZOL-5-YL)THIO]BENZAMIDE AND ITS USE FOR TREATING HIV INFECTION 审中-公开
公开(公告)号：WO2021127133A1
公开(公告)日：2021-06-24
申请号：PCT/US2020/065537
申请日：2020-12-17
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
发明人： APPELLA, Daniel H. , NIKOLAYEVSKIY, Herman , ROBELLO, Marco , SCERBA, Michael T.
IPC分类号： A61K31/4174 , A61K31/427 , A61K31/47 , A61K31/513 , A61K31/52 , A61K31/5365 , A61K31/635 , A61K31/675 , A61K45/06 , A61P31/18
摘要： Disclosed is a compound of formula (I): for treating or preventing a human immunodeficiency virus (HIV) infection in a mammal, for inhibiting or preventing maturation of an immature human immunodeficiency virus (HIV) to a mature HIV, and for preventing or inhibiting a human immunodeficiency virus (HIV) infection in a mammal having at least one HIV viral particle on a surface thereof.

54. 发明申请

WO2019241641A2 CANCER TREATMENT METHODS 审中-公开
公开(公告)号：WO2019241641A2
公开(公告)日：2019-12-19
申请号：PCT/US2019/037204
申请日：2019-06-14
申请人： THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , COLD SPRING HARBOR LABORATORY , LE GRICE, Stuart, F., J. , SPECTOR, David, L. , XU, Wenbo , ABULWERDI, Fardokht, A.
发明人： LE GRICE, Stuart, F., J. , SPECTOR, David, L. , XU, Wenbo , ABULWERDI, Fardokht, A.
IPC分类号： A61K31/4168 , A61K31/4184 , A61K31/454 , A61K31/517 , A61K31/5377 , A61P35/00 , A61P35/04 , C12Q1/6886
摘要： Disclosed are methods of treating cancer in a patient in need thereof, wherein the cancer has upregulation of MALAT1, comprising administering to the patient an effective amount of a compound of formula (I) or (II), a tautomer thereof, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or any combination thereof: in which R 1 , R 2 , R 3 , R 4 , R 5 , X, and m are as described herein. Also provided are methods of inhibiting branching morphogenesis in a tumor organoid cell culture comprising contacting the cell culture with a compound of formula (I) or (II), a tautomer thereof, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or any combination thereof, in which formulas (I), (II), R 1 , R 2 , R 3 , R 4 , R 5 , X, and m are as described herein.

55. 发明申请

WO2019217957A1 QUINOLINE COMPOUNDS AND THEIR PREPARATION AND USE AS ANTIMALARIAL AGENTS 审中-公开
公开(公告)号：WO2019217957A1
公开(公告)日：2019-11-14
申请号：PCT/US2019/031987
申请日：2019-05-13
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , THE HENRY M. JACKSON FOUNDATION FOR THE ADVANCEMENT OF MILITARY MEDICINE, INC.
发明人： LUO, Zhiji , SHAH, Pranav , SANDERSON, Philip E. , HUANG, Xiuli , ZHENG, Wei , HUANG, Wenwei , LI, Hao , SUN, Wei , LU, Xiao , XU, Xin , WILLIAMSON, Kim C. , TAWA, Gregory J.
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4353 , A61K31/4375 , A61P33/02
摘要： Disclosed are compounds of formula (I) wherein R 1 , R 2 , R 3 , A, and B are as defined herein, and a method of preparing such compounds. Also disclosed are pharmaceutical compositions containing the compound of formula (I) and a method of blocking transmission of a Plasmodium parasite and a method of treating or preventing malaria by killing or arresting the growth of Plasmodium organisms in a mammal, wherein the Plasmodium organisms are in a liver stage, an asexual stage, or gametocytes, comprising administering to an animal an effective amount of a compound of formula (I).

56. 发明申请

WO2019108665A1 AUTOPHAGY MODULATORS FOR USE IN TREATING CANCER 审中-公开
公开(公告)号：WO2019108665A1
公开(公告)日：2019-06-06
申请号：PCT/US2018/062866
申请日：2018-11-28
申请人： DEPAMPHILIS, Melvin L. , SHARMA, Gaurav , MARUGAN, Juan Jose , FERRER, Marc , THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , ROY, Ajit
发明人： DEPAMPHILIS, Melvin L. , SHARMA, Gaurav , MARUGAN, Juan Jose , FERRER, Marc , ROY, Ajit
IPC分类号： A61K31/506 , A61K31/53 , A61K31/5377 , A61P35/00
CPC分类号： A61K31/506 , A61K31/53 , A61K31/5377 , A61P35/00
摘要： Disclosed is method for treating cancer in a mammal, comprising administering to a mammal in need thereof a compound of the formula: wherein R1, R2, and R3 are as defined herein, wherein the cancer is an autophagy dependent cancer, in an amount sufficient to induce autophagy in the cell and cause the death of cancer cells. Also disclosed is a method for selectively killing cancer cells in a patient afflicted with cancer, comprising administering to the mammal, wherein the cancer cells are autophagy dependent cancer cells, in an amount sufficient to induce autophagy in the cells and cause the death of the cancer cells.

57. 发明申请

WO2015192077A1 HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：杂环化合物及其使用方法
公开(公告)号：WO2015192077A1
公开(公告)日：2015-12-17
申请号：PCT/US2015/035658
申请日：2015-06-12
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , UNIVERSITY OF KANSAS
发明人： LIANG, Tsanyang , HU, Zongyi , MARUGAN, Juan Jose , SOUTHALL, Noel Terrence , HE, Shanshan , HU, Xin , XIAO, Jingbo , FERRER, Marc , ZHENG, Wei , FRANKOWSKI, Kevin J. , SCHOENEN, Frank J. , LI, Kelin
IPC分类号： C07D413/14 , C07D471/08 , A61K31/553 , A61P31/14
CPC分类号： C07D413/06 , A61K31/4178 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/7056 , A61K31/7068 , A61K38/07 , A61K38/13 , A61K38/212 , C07D413/14 , C07D417/14 , C07D471/08 , Y02A50/385
摘要： Disclosed are compounds of formula (I), formula (II), and formula (III): wherein Ar, R 1 , A, and X are as defined in the specification. These compounds are antiviral agents and are contemplated for use in the treatment of viral infections, for example, hepatitis C. These compounds are also contemplated for use in treating or preventing cancers.
摘要翻译：公开了式（I），式（II）和式（III）的化合物：其中Ar，R 1，A和X如说明书中所定义。这些化合物是抗病毒剂，并且被考虑用于治疗病毒感染，例如丙型肝炎。这些化合物也被考虑用于治疗或预防癌症。

58. 发明申请

WO2015191707A2 NANOPARTICULATE COMPLEX OF NICOTINE AND CERIUM OXIDE AND USE THEREOF 审中-公开
标题翻译：尼古丁和氧化铈的纳米复合物及其用途
公开(公告)号：WO2015191707A2
公开(公告)日：2015-12-17
申请号：PCT/US2015/035099
申请日：2015-06-10
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
发明人： IMAM, Syed
IPC分类号： A61K9/51
CPC分类号： A61K9/5052 , A61K9/5031 , A61K9/5115 , A61K9/5169 , A61K31/465 , A61K33/24 , A61K47/593 , A61K47/6415 , A61K47/6921
摘要： Disclosed are particles comprising a complex of nicotine and cerium oxide and a biodegradable coating comprising agglutinin. Also disclosed is a method of treating or preventing neurodegenerative or neurological disorders in a mammal in need thereof, comprising administering to the mammal a therapeutically effective amount of the particles.
摘要翻译：公开了包含尼古丁和氧化铈的复合物和包含凝集素的可生物降解的涂层的颗粒。还公开了一种在有需要的哺乳动物中治疗或预防神经变性或神经障碍的方法，包括向哺乳动物施用治疗有效量的颗粒。

59. 发明申请

WO2015120140A1 AZA-EPOXY-GUAIANE DERIVATIVES AND TREATMENT OF CANCER 审中-公开
标题翻译： AZA-EPOXY-GUAIANE衍生物和治疗癌症
公开(公告)号：WO2015120140A1
公开(公告)日：2015-08-13
申请号：PCT/US2015/014601
申请日：2015-02-05
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , UNIVERSITY OF HAWAII
发明人： CHAIN, William J. , BEUTLER, John A. , FASH, David , FIGG, William D. , LI, Zhenwu , PEER, Cody John , RAMOS, Joe William , SULZMAIER, Florian J.
IPC分类号： C07D493/08 , A61K31/352 , A61P35/00 , A61P3/00 , A61P31/00 , A61P9/00
CPC分类号： C07D493/08 , A61K9/0053 , A61K31/352 , A61K45/06
摘要： Disclosed is a compound of formula (I) or formula (II): (Formulas should be inserted here) wherein R 1 -R 6 are as defined herein. Also disclosed are a pharmaceutical composition comprising such a compound and a method of treating or preventing cancer in a mammal in need thereof, comprising administering to the mammal a compound of formula (I) or formula (II).
摘要翻译：公开了式（I）或式（II）的化合物：式中R 1 -R 6如本文所定义。还公开了包含这种化合物和在有需要的哺乳动物中治疗或预防癌症的方法的药物组合物，其包括向哺乳动物施用式（I）或式（II）的化合物。

60. 发明申请

WO2014014978A1 NITRIC OXIDE-RELEASING DIAZENIUMDIOLATED POLYVINYLPYRROLIDONE-BASED POLYMERS, AND COMPOSITIONS, MEDICAL DEVICES, AND USES THEREOF 审中-公开
标题翻译：氮氧化物释放二氮杂萘基聚吡咯烷酮聚合物及其组合物，医疗器械及其用途
公开(公告)号：WO2014014978A1
公开(公告)日：2014-01-23
申请号：PCT/US2013/050793
申请日：2013-07-17
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
发明人： HRABIE, Joseph A. , KEEFER, Larry K.
IPC分类号： C08F26/10 , C08F226/10 , A61K8/81 , A61B5/00
CPC分类号： C08F226/10 , A61K31/79
摘要： Disclosed is a nitric oxide-releasing polyvinylpyrrolidone-based polymer derived from N -vinylpyrrolidone monomer and at least one nitric oxide releasing N 2 O 2 - group, in which the N 2 O 2 - group is attached to a 2 pyrrolidinone group or a group derived therefrom in the N -vinylpyrrolidone monomer, and the polymer is optionally in combination with a substrate. The NO-releasing polymer can be part of a medical device or pharmaceutical composition and is useful for treating a biological disorder, such as healing a wound, restenosis, and/or promoting angiogenesis.
摘要翻译：公开了一种衍生自N-乙烯基吡咯烷酮单体的一氧化氮释放型聚乙烯吡咯烷酮系聚合物和至少一种释放N2O2 - 的一氧化氮，其中N 2 O 2 - 基团连接到2个吡咯烷酮基或其衍生自N- 乙烯基吡咯烷酮单体，并且聚合物任选地与底物组合。释放NO的聚合物可以是医疗装置或药物组合物的一部分，并且可用于治疗生物学障碍，例如愈合伤口，再狭窄和/或促进血管生成。

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