-
公开(公告)号:US20140212419A1
公开(公告)日:2014-07-31
申请号:US14182706
申请日:2014-02-18
Inventor: Richard D. DiMARCHI , Arnab DE
IPC: A61K38/28 , A61K39/395
CPC classification number: A61K38/28 , A61K9/0019 , A61K38/26 , A61K39/395 , A61K47/48215 , A61K47/48246 , A61K47/60 , A61K47/64
Abstract: Prodrug formulations of bioactive polypeptides are provided wherein the bioactive polypeptide has been modified by the linkage of a dipeptide to the bioactive polypeptide through an ester linkage. The prodrugs disclosed herein in some embodiments have extended half lives of at least 1.5 hours (e.g., at least 10 hours), and more typically greater than 20 hours and less than 70 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
Abstract translation: 提供生物活性多肽的前药制剂,其中生物活性多肽已经通过二酯与生物活性多肽的连接通过酯键进行了修饰。 在一些实施方案中本文公开的前体药物具有至少1.5小时(例如,至少10小时),更通常大于20小时和小于70小时的半衰期延长,并且在生理条件下通过 由化学不稳定驱动的非酶反应。
-
122.
公开(公告)号:US20130292562A1
公开(公告)日:2013-11-07
申请号:US13844901
申请日:2013-03-16
Inventor: David Edward Clemmer , Michael A. Ewing , Steven M. Zucker , Christopher R. P. Conant
IPC: G01N27/62
CPC classification number: G01N27/622 , H01J49/0031 , H01J49/26
Abstract: An ion mobility spectrometer instrument has a drift tube that is partitioned into a plurality of cascaded drift tube segments. A number of electric field activation sources may each be coupled to one or more of the plurality of drift tube segments. A control circuit is configured to control operation of the number of electric field activation sources in a manner that sequentially applies electric fields to the drift tube segments with a activation duration of at least one of the electric field activation sources different than that of the others to allow only ions having a predefined ion mobility or range of ion mobilities to travel through the drift tube. The drift tube segments may define a linear drift tube or a closed drift tube with a continuous ion travel path.
Abstract translation: 离子迁移谱仪具有漂移管,其被分隔成多个级联漂移管段。 多个电场激活源可以各自耦合到多个漂移管段中的一个或多个。 控制电路被配置为以对于至少一个电场激活源的激活持续时间不同于其他电场激活源的激活持续时间顺序地向漂移管段施加电场的方式来控制电场激活源的数量的操作, 仅允许具有预定离子迁移率或离子迁移率范围的离子穿过漂移管。 漂移管段可以限定具有连续离子行进路径的线性漂移管或闭合漂移管。
-
123.
公开(公告)号:US20250152733A1
公开(公告)日:2025-05-15
申请号:US18837694
申请日:2023-02-08
Inventor: Yan Yu , Jared T. Wiemann , Swagata Bhattacharyya
Abstract: “Two-faced” amphiphilic Janus nanoparticles that have different surface chemistries on two hemispheres. One hemisphere of the Janus nanoparticles is functionalized with a hydrophobic moiety. The other hemisphere of the nanoparticles is functionalized with either a cationic antibiotic or cationic polymer. Janus nanoparticles effectively inhibit the growth of both Gram-negative and Gram-positive bacteria at picomolar concentrations and may be used as a broad-spectrum antibiotic on surfaces or to treat bacterial infections in patients.
-
公开(公告)号:US12115158B2
公开(公告)日:2024-10-15
申请号:US17195166
申请日:2021-03-08
Inventor: Jian-Ting Zhang , Jing-Yuan Liu , Mingji Dai
IPC: A61K31/4985 , A61K31/498 , A61P35/00
CPC classification number: A61K31/4985 , A61K31/498 , A61P35/00
Abstract: Methods for treating various cancers by administering one or more compounds that target the dimeric protein survivin are disclosed. Pharmaceutical compositions containing such compounds are also disclosed, along with general methods of identifying anti-cancer compounds that target oncogenic dimeric proteins. Exemplary compounds that can be used in the disclosed methods of treatment and pharmaceutical compositions have the chemical structures disclosed in the specification.
-
125.
公开(公告)号:US20240315220A1
公开(公告)日:2024-09-26
申请号:US18605786
申请日:2024-03-14
Inventor: Gareth Howell , Michael Sasner , Gregory Carter , Bruce Lamb
IPC: A01K67/0278 , C07K14/705 , C07K14/775 , G01N33/68
CPC classification number: A01K67/0278 , C07K14/70503 , C07K14/775 , G01N33/6896 , A01K2217/056 , A01K2217/072 , A01K2217/15 , A01K2227/105 , A01K2267/0312 , G01N2500/00
Abstract: Genetically modified mice characterized by one or more symptoms or signs associated with expression of human APOE4p and mouse Trem2p and relevant to non-familial late-onset Alzheimer's disease are provided wherein the genome of the mouse includes: 1) a DNA sequence encoding a human APOE4 protein (APOE4p) operably linked to a promoter; and 2) a DNA sequence encoding a mouse Trem2 protein having a mutation p.R47H (Trem2p) operably linked to a promoter, such that the mouse expresses human APOE4p and mouse Trem2p. Methods are provided for screening for a compound for use in the treatment of Alzheimer's disease using such genetically modified mice.
-
公开(公告)号:US20240025890A1
公开(公告)日:2024-01-25
申请号:US18460337
申请日:2023-09-01
Inventor: William W. TURNER , Lee D. ARNOLD , Hans MAAG , Leping LI , Mark G. BURES , Simon Nicolas HAYDAR , Samson FRANCIS
IPC: C07D417/12 , C07D403/12 , A61K45/06 , C07D401/12 , C07D413/12 , C07D417/14 , A61K31/554 , C07D453/02 , C07D471/04 , A61P31/20 , C07D243/38 , C07D267/20 , C07D281/16
CPC classification number: C07D417/12 , C07D403/12 , A61K45/06 , C07D401/12 , C07D413/12 , C07D417/14 , A61K31/554 , C07D453/02 , C07D471/04 , A61P31/20 , C07D243/38 , C07D267/20 , C07D281/16
Abstract: The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
-
公开(公告)号:US11733243B2
公开(公告)日:2023-08-22
申请号:US16818854
申请日:2020-03-13
Inventor: Craig Erickson , Debomoy Lahiri
IPC: A61K31/185 , G01N33/573 , A61K31/16
CPC classification number: G01N33/573 , A61K31/16 , A61K31/185 , G01N2333/4709 , G01N2333/48 , G01N2333/91205 , G01N2500/20 , G01N2800/2814 , G01N2800/52
Abstract: Studies in mouse models of Fragile X and preliminary studies in human youth demonstrate that ERK1/2 is biomarker useful to monitoring the treatment of people diagnosed with ASD. Results reported herein demonstrate that acamprosate has the ability to reduce levels of ERK1/2 activation associated with many of the symptoms of ASD. Accordingly, in addition to its utility as a diagnostic marker for ASD ERK1/2 activation levels can be used to monitor patients treated with acamprosate and to screen potentially therapeutic compounds.
-
公开(公告)号:US11723886B2
公开(公告)日:2023-08-15
申请号:US16968009
申请日:2019-02-07
Inventor: Mark R. Kelley , Timothy W. Corson
IPC: A61K31/165 , A61P27/02 , A61K31/445 , A61K31/45 , A61K31/675 , A61K45/06
CPC classification number: A61K31/165 , A61K31/445 , A61K31/45 , A61K31/675 , A61K45/06 , A61P27/02
Abstract: [[(2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methylidene]-N,N-diethylpentanamide] (APX2009) and (2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronapthalen-2-yl)methylidene]-N-methoxypentanamide] (APX2014) for inhibiting ocular diseases are disclosed herein.
-
129.
公开(公告)号:US20230212276A1
公开(公告)日:2023-07-06
申请号:US18097078
申请日:2023-01-13
Applicant: Indiana University Research and Technology Corporation , THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS
Inventor: Matthias Clauss , Irina Petrache
CPC classification number: C07K16/2866 , A61P11/00 , C07K2317/56 , C07K2317/24
Abstract: The present invention provides methods for diagnosing a patient with emphysema, COPD of lung injury caused by tobacco use by detecting the levels of EMAP II in a sample. Disclosed herein are the hypervariable regions for a rat monoclonal antibody that binds to a form of EMAP II. This disclosure also includes a polypeptide sequence included in EMAP II that is the target for the binding of the antibody to its target protein. This epitope serves as the basis for a humanized antibody that can be used to treat patients that suffer from pathologies that exhibit elevated levels of EMAP II expression.
-
130.
公开(公告)号:US11672811B2
公开(公告)日:2023-06-13
申请号:US16635769
申请日:2018-08-02
Applicant: Indiana University Research and Technology Corporation , University of Rochester , The United States of America As Represented by the Department of Veterans Affairs Office of General
Inventor: Teresita M. Bellido , G. David Roodman , Jesus Delgado-Calle , Robert K. Boeckman , Frank H. Ebetino
IPC: A61K31/664 , A61P35/00 , A61K38/29 , A61K45/06 , C07F9/38
CPC classification number: A61K31/664 , A61K38/29 , A61K45/06 , A61P35/00 , C07F9/3886
Abstract: Various aspects and embodiments disclosed herein relate generally to the modelling, treatment, reducing resistance to the treatment, prevention, and diagnosis of diseases/symptoms induced by multiple myeloma. Embodiments include methods of treating a bone related disease, comprising the steps of: administering to a subject at least one therapeutically effective dose of a compound disclosed herein.
-
-
-
-
-
-
-
-
-