公开(公告)号：US20230201360A1

公开(公告)日：2023-06-29

申请号：US18077484

申请日：2022-12-08

申请人： RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITY

发明人： Jae Hyung PARK ,  Wooram UM ,  Hyeyeon JOO

IPC分类号： A61K47/54 ,  A61K35/745 ,  A61K35/747 ,  A61P1/14

CPC分类号： A61K47/555 ,  A61K35/745 ,  A61K35/747 ,  A61P1/14

摘要： The present disclosure relates to a composition and a kit for colonization of external probiotics in the gut through bioorthogonal click chemistry. The composition or kit for colonization of external probiotics in the gut according to the present disclosure has the effects of overcoming colonization resistance, which is the limitation of existing external probiotics caused by physical discharge and indigenous bacteria, by linking surface-modified external probiotics to the intestinal mucosa into which a bioorthogonal functional group has been introduced, and beneficially changing the intestinal environment by long-term colonization of various external probiotics, such as lactic acid bacteria, bifidobacteria, and yeast. Accordingly, the present disclosure is expected to be effectively used for the development of various medicines and functional foods using probiotics.

公开(公告)号：US20190247523A1

公开(公告)日：2019-08-15

申请号：US16276169

申请日：2019-02-14

申请人： Boston Scientific Scimed, Inc.

发明人： Joseph Thomas Delaney, JR. ,  Douglas Dean Pagoria ,  Douglas Pennington ,  Paul Sorajja

IPC分类号： A61K49/10

CPC分类号： A61K49/10 ,  A61F2/01 ,  A61K47/555 ,  A61K49/103

摘要： A functional gadolinium contrast agent comprising a gadolinium cation and a ligand secured to the gadolinium cation is disclosed, the ligand comprising a reactive group capable of bonding to a capture substrate. A method of removing gadolinium contrast agents from a patient is disclosed, the method comprising providing a gadolinium contrast agent containing a reactive group; providing a capture substrate for insertion into a patient's bloodstream; administering the gadolinium contrast agent to the patient; conducting a magnetic resonance imaging procedure; and sequestering the gadolinium contrast agent on the capture substrate. A system for removing gadolinium contrast agents is also disclosed.

公开(公告)号：US20190192436A1

公开(公告)日：2019-06-27

申请号：US16234044

申请日：2018-12-27

申请人： Washington University

发明人： Gregory M. Lanza ,  Dipanjan Pan

IPC分类号： A61K9/14 ,  A61K41/00 ,  A61K33/24 ,  A61K31/336 ,  A61K9/127 ,  A61K47/54 ,  A61K9/00 ,  A61K9/107 ,  A61K31/337

CPC分类号： A61K9/145 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/10 ,  A61K9/1075 ,  A61K9/1271 ,  A61K31/336 ,  A61K31/337 ,  A61K33/24 ,  A61K41/0071 ,  A61K47/555 ,  A61K47/6907 ,  Y10S977/773 ,  Y10S977/906

摘要： The present invention encompasses prodrug compositions, nanoparticles comprising one or more prodrugs, and methods of use thereof.

公开(公告)号：US20180147288A1

公开(公告)日：2018-05-31

申请号：US15576226

申请日：2016-06-16

申请人： The Regents of the University of California

发明人： Peter V. Robinson ,  Cheng-Ting Tsai ,  Carolyn R. Bertozzi

IPC分类号： A61K47/54 ,  A61P35/00 ,  A61P29/00 ,  A61P31/00 ,  A61K47/64 ,  C12N15/115

CPC分类号： A61K47/545 ,  A61K47/555 ,  A61K47/643 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  C12N15/115

摘要： Pharmaceutical compositions are provided for extending the serum half-life of a therapeutic agent. The composition may include a strained alkyne-labeled therapeutic agent. Also provided is a strained alkyne-carrier protein adduct including a vinyl thioether-linkage to a cysteine residue of the carrier protein. Methods of chemoselectively modifying a carrier protein are provided, that include conjugating a cysteine residue of a carrier protein with a cyclooctyne-labeled cargo agent to produce a vinyl thioether-linked conjugate. Also provided is a method of increasing the in vivo half-life of a bioactive agent including administering a strained alkyne-labeled bioactive agent to a subject.

公开(公告)号：US09931408B2

公开(公告)日：2018-04-03

申请号：US14117655

申请日：2012-05-16

申请人： Marc Stefan Robillard ,  Hendricus Marie Janssen ,  Wolter Ten Hoeve ,  Ronny Mathieu Versteegen ,  Raffaella Rossin

发明人： Marc Stefan Robillard ,  Hendricus Marie Janssen ,  Wolter Ten Hoeve ,  Ronny Mathieu Versteegen ,  Raffaella Rossin

IPC分类号： C07D257/08 ,  C07D237/26 ,  A61K31/435 ,  A61K31/502 ,  C07C13/263 ,  C07C33/16 ,  A61K31/045 ,  A61K47/48 ,  B82Y5/00 ,  A61K31/704 ,  A61K38/05 ,  A61K39/395 ,  A61K47/22

CPC分类号： A61K47/6803 ,  A61K31/435 ,  A61K31/444 ,  A61K31/704 ,  A61K38/05 ,  A61K39/3955 ,  A61K39/39558 ,  A61K47/22 ,  A61K47/545 ,  A61K47/555 ,  A61K47/558 ,  A61K47/6897 ,  B82Y5/00 ,  C07C33/16 ,  C07D237/26 ,  C07D257/08 ,  Y02A50/471

摘要： The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.

公开(公告)号：US09801943B2

公开(公告)日：2017-10-31

申请号：US13774247

申请日：2013-02-22

申请人： KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

发明人： Kwang Meyung Kim ,  Ick Chan Kwon ,  Kuiwon Choi ,  Heebeom Koo ,  Sang-min Lee ,  Inchan Youn

IPC分类号： A61K47/26 ,  A61K47/34 ,  A61K47/48 ,  A61K49/00

CPC分类号： A61K47/26 ,  A61K47/34 ,  A61K47/549 ,  A61K47/555 ,  A61K47/6911 ,  A61K49/0032 ,  A61K49/0052

摘要： The present disclosure relates to a method for in vivo targeting of a nanoparticle via bioorthogonal copper-free click chemistry, more particularly to a method for in vivo targeting of a nanoparticle, including: injecting a precursor capable of being metabolically engineered in vivo when injected into a living system and having a first bioorthogonal functional group into the living system; and injecting a nanoparticle having a second bioorthogonal functional group which can perform a bioorthogonal copper-free click reaction with the first bioorthogonal functional group attached thereto into the living system.In accordance with the present disclosure, accumulation of nanoparticles at a target site in a living system can be increased remarkably and the biodistribution of the nanoparticles can be controlled since the nanoparticles bound to a cell surface are taken up into the cell with time.

公开(公告)号：US20170216460A1

公开(公告)日：2017-08-03

申请号：US15169493

申请日：2016-05-31

申请人： KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

发明人： Kwangmeyung KIM ,  Ju Hee RYU ,  Ick Chan KWON ,  Man Kyu SHIM ,  Hong Yeol YOON

IPC分类号： A61K49/00 ,  G01N33/58 ,  G01N33/574 ,  C07K9/00

CPC分类号： A61K49/0056 ,  A61K47/555 ,  A61K49/0032 ,  A61K49/0052 ,  C07K5/1016 ,  C07K5/1019 ,  C07K9/001 ,  G01N33/57496 ,  G01N33/581 ,  G01N2333/96466

摘要： The present disclosure relates to a glycopeptide targeting cancer cells and a contrast agent kit containing the same. The glycopeptide is one wherein an azide reporting monosaccharide is bound to a substrate peptide. As the substrate peptide is specifically cleaved by cathepsin B in cancer cells, an azide reporting monosaccharide is expressed onto the cell surface via metabolic glycoengineering, thereby providing a target for action as a contrast agent. Accordingly, because the azide is exposed to the cell surface only by cathepsin B, as it is specifically expressed in cancer cells, in particular in metastatic cancer cells, while it is limitedly expressed in normal cells and is hardly excreted out the cells, the cancer cells can be selectively imaged by an azide-specific contrast agent.

公开(公告)号：US20170143840A1

公开(公告)日：2017-05-25

申请号：US15233283

申请日：2016-11-23

申请人： KONINKLIJKE PHILIPS N.V.

发明人： Marc Stefan Robillard ,  Hendricus Marie Janssen ,  Wolter Ten Hoeve ,  Ronny Mathieu Versteegen

IPC分类号： A61K39/00 ,  A61K31/704 ,  A61K31/444 ,  A61K31/435

CPC分类号： A61K47/6803 ,  A61K31/435 ,  A61K31/444 ,  A61K31/704 ,  A61K38/05 ,  A61K39/3955 ,  A61K39/39558 ,  A61K47/22 ,  A61K47/545 ,  A61K47/555 ,  A61K47/558 ,  A61K47/6897 ,  B82Y5/00 ,  C07C33/16 ,  C07D237/26 ,  C07D257/08 ,  Y02A50/471

摘要： The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.

公开(公告)号：US09585963B2

公开(公告)日：2017-03-07

申请号：US14692526

申请日：2015-04-21

申请人： Signature Therapeutics, Inc.

发明人： Thomas E. Jenkins ,  Craig O. Husfeld ,  Julie D. Seroogy ,  Jonathan W. Wray

IPC分类号： A61K31/74 ,  A61K47/48 ,  A61K9/51 ,  A61K31/485 ,  C07D489/02 ,  C07D489/08 ,  C12Q1/37 ,  G01N33/50 ,  G01N33/94

CPC分类号： A61K47/48023 ,  A61K9/51 ,  A61K31/485 ,  A61K47/4813 ,  A61K47/48246 ,  A61K47/54 ,  A61K47/555 ,  A61K47/64 ,  C07D489/02 ,  C07D489/08 ,  C12Q1/37 ,  G01N33/5088 ,  G01N33/9486 ,  G01N2333/976 ,  G01N2500/00

摘要： Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an opioid prodrug that provides enzymatically-controlled release of an opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the opioid from the opioid prodrug so as to attenuate enzymatic cleavage of the opioid prodrug.

摘要翻译： 提供了药物组合物及其使用方法，其中药物组合物包含提供阿片样物质的酶控释放的阿片样前体药物和与介导阿片样物质的酶控释放的酶相互作用的酶抑制剂 来自阿片样前药，以减轻阿片样物质前药的酶切。

公开(公告)号：US20170049903A1

公开(公告)日：2017-02-23

申请号：US15222669

申请日：2016-07-28

申请人： California Institute of Technology ,  Calando Pharmaceuticals, Inc.

发明人： Suzie Hwang Pun ,  Hector Gonzalez ,  Mark E. Davis ,  Nathalie C. Bellocq ,  Jianjun Cheng

IPC分类号： A61K47/48 ,  A61K38/44 ,  A61K48/00 ,  C08G65/333

CPC分类号： A61K48/0041 ,  A61K38/44 ,  A61K47/555 ,  A61K47/6949 ,  A61K47/6951 ,  B82Y5/00 ,  C08B37/0012 ,  C08B37/0015 ,  C08G65/33396 ,  C08G65/48 ,  C08G2650/04 ,  C08G2650/38 ,  C12N15/87 ,  C12Y113/12007

摘要： The invention provides a composition containing particulate composite of a polymer and a therapeutic agent. The composition also contains a complexing agent. The polymer interacts with the complexing agent in a host-guest or a guest-host interaction to form an inclusion complex. A therapeutic composition of the invention may be used to deliver the therapeutic agent and to treat various disorders. Both the polymer of the particulate composite and the complexing agent may be used to introduce functionality into the therapeutic composition. The invention also relates to a method of preparing a composition. The method combines a therapeutic agent, a polymer having host or guest functionality, and a complexing agent having guest or host functionality to form the therapeutic composition. The complexing agent forms an inclusion complex with the polymer. The invention also relates to a method of delivering a therapeutic agent. According to the method, a therapeutically effective amount of a therapeutic composition of the invention is administered to a mammal (e.g. person or animal) in recognized need of the therapeutic. Also disclosed are compounds having the formula:

摘要翻译： 本发明提供了含有聚合物和治疗剂的颗粒复合物的组合物。 该组合物还含有络合剂。 聚合物与宿主客体或客体 - 宿主相互作用中的络合剂相互作用以形成包合物。 本发明的治疗组合物可用于递送治疗剂并治疗各种疾病。 颗粒复合材料的聚合物和络合剂都可用于将功能性引入治疗组合物中。 本发明还涉及制备组合物的方法。 该方法结合治疗剂，具有宿主或客体功能的聚合物和具有客体或宿主功能的络合剂以形成治疗组合物。 络合剂与聚合物形成包合络合物。 本发明还涉及递送治疗剂的方法。 根据该方法，将治疗有效量的本发明的治疗组合物在公认的治疗需要中给予哺乳动物（例如人或动物）。 还公开了具有下式的化合物：