公开(公告)号：US10047135B2

公开(公告)日：2018-08-14

申请号：US14622217

申请日：2015-02-13

申请人： STC.UNM

发明人： Yubin Miao

IPC分类号： A61K51/00 ,  A61M36/14 ,  C07K14/68 ,  A61K51/08 ,  A61K45/06 ,  C07K7/54 ,  A61K38/00

摘要： The present invention is directed to novel non-invasive diagnostic tools/compounds to image cancers, especially, melanoma, including metastatic melanoma in vivo. The present compounds exhibit enhanced uptake in cancerous cells and tissue and decreased renal uptake in kidney, evidencing favorable pharmacokinetics of compounds of the present invention. The compounds according to the present invention represent an advance in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention are also useful for initiating therapy for melanoma as well as monitor patients' response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.

公开(公告)号：US10039844B2

公开(公告)日：2018-08-07

申请号：US14956431

申请日：2015-12-02

申请人： The Board of Trustees of the Leland Stanford Junior University

发明人： Timothy Witney ,  Michelle L. James ,  Sanjiv S. Gambhir

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K51/04 ,  C07D295/26 ,  G01N33/574 ,  G01N33/60

摘要： A novel pyruvate kinase M2 (PKM2)-specific activator, [11C]DASA-23 and derivatives thereof, and methods for their rapid synthesis are provided. The probes are particularly useful in methods for the non-invasive positron emission tomography (PET) detection and imaging of PKM2 expression in subcutaneous and orthotopic tumors. [11C]DASA-23 cell uptake correlates with PKM2 protein expression in cultured tumor cells and orthotopic tumors are delineated from the surrounding normal brain tissue in vivo.

公开(公告)号：US10016521B2

公开(公告)日：2018-07-10

申请号：US15002690

申请日：2016-01-21

申请人： Bailing Cloud Biomedical Technologies Innovation

发明人： Bailing Hsu

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K51/08 ,  A61K51/06 ,  C07K1/13

CPC分类号： A61K51/082 ,  A61K51/065 ,  A61K51/088 ,  C07K1/13

摘要： The disclosure is related to a chemical structure, a preparation and an imaging method of a tumor imaging tracer, especially to a SPECT radionuclide-labeled trimeric cyclic RGD peptide: 99mTc-4P-RGD3which functions as a ligand to be combined with integrin αvβ3 receptor in tumor for tumor imaging. The preparation includes linking HYNIC-OSu with 4P-RGD3 to form HYNIC-4P-RGD3 and then chelating HYNIC with 99mTc to create 99mTc-4P-RGD3Animal biodistribution and imaging experiments reveal higher uptake in tumor and lower uptake in normal organs, therefore the disclosure can improve image quality, Through animal metabolic experiments, the original form of 99mTc-4P-RGD3 can be still excreted without the evidence of further metabolites in urine and feces. According to the disclosure, the tumor imaging tracer 99mTc-4P-RGD; combined with the integrin αvβ3 solves the issue of high background uptake in normal organs, such that radio-labeled SPECT imaging tracers are more suitable for animal whole-body tumor evaluation.

公开(公告)号：US09901604B2

公开(公告)日：2018-02-27

申请号：US15017376

申请日：2016-02-05

申请人： Crestovo Holdings LLC

发明人： Thomas Julius Borody

IPC分类号： A61K45/00 ,  A01N63/00 ,  A61M36/14 ,  A61K9/16 ,  A61K9/50 ,  A61K35/742 ,  A61K35/74 ,  A61K38/48 ,  A61K35/741 ,  A61K35/744 ,  A61K35/747 ,  A61K36/062 ,  A61K45/06 ,  A61K38/14 ,  A61K31/341 ,  A61K31/41 ,  A61K31/495 ,  A61K31/7034 ,  A23L2/52 ,  A61K35/745 ,  A61K35/38 ,  A61K35/24 ,  A61K9/00 ,  A23C9/123 ,  A61K9/48 ,  A23C9/13 ,  A23L33/135 ,  A23C9/127 ,  A61K9/19 ,  A61K35/37 ,  A61K31/545 ,  A61K39/00 ,  A61K35/76 ,  A61K31/43 ,  A61K38/00 ,  A61K31/7048 ,  A61K39/39 ,  A61K51/12 ,  A61K35/00

CPC分类号： A61K35/742 ,  A23C9/123 ,  A23C9/127 ,  A23C9/13 ,  A23L2/52 ,  A23L33/135 ,  A23V2002/00 ,  A61K9/0031 ,  A61K9/0053 ,  A61K9/19 ,  A61K9/48 ,  A61K9/4891 ,  A61K9/50 ,  A61K9/5005 ,  A61K9/5078 ,  A61K31/341 ,  A61K31/41 ,  A61K31/43 ,  A61K31/495 ,  A61K31/545 ,  A61K31/7034 ,  A61K31/7048 ,  A61K35/24 ,  A61K35/37 ,  A61K35/38 ,  A61K35/74 ,  A61K35/741 ,  A61K35/744 ,  A61K35/745 ,  A61K35/747 ,  A61K35/76 ,  A61K36/062 ,  A61K38/00 ,  A61K38/14 ,  A61K38/4893 ,  A61K39/00 ,  A61K39/39 ,  A61K45/06 ,  A61K51/1217 ,  A61K2035/115 ,  C12N2795/00032 ,  Y02A50/401 ,  Y02A50/469 ,  Y02A50/473 ,  A61K2300/00

摘要： The present invention relates to pharmaceutical compositions suitable for the treatment of chronic diseases associated with the presence of abnormal or an abnormal distribution of microflora in the gastrointestinal tract of a mammalian host, which compositions comprise viable non-pathogenic or attenuated pathogenic Clostridia. The compositions further comprise one or more additional viable non-pathogenic or attenuated pathogenic microorganisms selected from the group consisting of Bacteroides, Eubacteria, Fusobacteria, Propionibacteria, Lactobacilli, anaerobic cocci, Ruminococcus, E. coli, Gemmiger, Desulfomonas, Peptostreptococcus, and fungi. The present invention also provides pharmaceutical compositions suitable for the treatment of the same chronic diseases comprising viable non-pathogenic or attenuated pathogenic Escherichia coli, at least one strain of viable non-pathogenic or attenuated pathogenic Bacteroides and at least one strain of viable non-pathogenic or attenuated pathogenic microorganism.

公开(公告)号：US09849201B2

公开(公告)日：2017-12-26

申请号：US14270061

申请日：2014-05-05

申请人： The Washington University

发明人： Gregory M Lanza ,  Samuel A. Achilefu ,  Grace Hufang Cui

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K51/08 ,  C07K7/06 ,  A61K49/00 ,  A61K49/08 ,  A61K49/12 ,  A61K49/14 ,  A61K51/06

CPC分类号： A61K51/088 ,  A61K49/0002 ,  A61K49/0032 ,  A61K49/0054 ,  A61K49/0056 ,  A61K49/085 ,  A61K49/124 ,  A61K49/14 ,  A61K51/065 ,  C07K7/06

摘要： The present disclosure provides peptide constructs for diagnostic imaging and therapeutic applications, using pegylated peptides which exhibit specific binding for a target molecule of interest, such as a biomarker of a disease or disorder.

公开(公告)号：US09833520B2

公开(公告)日：2017-12-05

申请号：US13952576

申请日：2013-07-26

申请人： The Methodist Hospital Research Institute

发明人： King Chuen Li ,  Zheng Li ,  Feng Li

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K49/00 ,  A61K47/48 ,  A61K51/04 ,  A61K45/06 ,  C07D403/14 ,  C07D239/14 ,  A61K9/127 ,  A61K9/51 ,  A61K31/505 ,  A61K31/506 ,  A61K47/60 ,  A61K47/55

CPC分类号： A61K49/0021 ,  A61K9/127 ,  A61K9/51 ,  A61K31/505 ,  A61K31/506 ,  A61K45/06 ,  A61K47/55 ,  A61K47/60 ,  A61K49/0052 ,  A61K51/0459 ,  C07D239/14 ,  C07D403/14

摘要： Disclosed are multivalent, integrin-receptor antagonists that are useful in a variety of therapeutic, prophylactic, and/or diagnostic imaging modalities. In illustrative embodiments, such compounds have been prepared and utilized in the imaging, detection, localization, and/or quantitation of one or more samples of biological interest. Similarly, these compounds, as well as formulations comprising them, find utility in the prevention, treatment, and/or amelioration of one or more symptoms of a disease, abnormal condition, dysfunction, etc., including, for example proliferative diseases such as cancer in affected animals. In certain embodiments, fluorescently- or radio-labeled-non-peptidic, multivalent integrin αvβ3 compounds are provided. Compositions including such compounds have been shown to have utility in detecting, localizing, quantitating, and/or imaging integrin αvβ3 receptor-expressing cells, including, for example, cancer cells in vitro, in vivo, and/or in situ.

公开(公告)号：US09795692B2

公开(公告)日：2017-10-24

申请号：US14296721

申请日：2014-06-05

申请人： SYSTEM OF SYSTEMS ANALYTICS, INC.

发明人： Giora Feuerstein ,  Richard Cliff

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K49/00 ,  G01N33/68 ,  A61B5/00 ,  A61B3/12

CPC分类号： A61K49/0056 ,  A61B3/12 ,  A61B5/4088 ,  A61K49/0021 ,  A61K49/006 ,  G01N33/6896 ,  G01N2800/2821

摘要： Described are methods for the detection, in the eye of an individual, of protein aggregates or other misfolded proteins associated with disease using peptide or peptide mimic probes that preferentially associate with the protein aggregates or misfolded proteins, which can be accomplished non-invasively.

公开(公告)号：US09695251B2

公开(公告)日：2017-07-04

申请号：US13566913

申请日：2012-08-03

申请人： Roger Y. Tsien ,  Tao Jiang ,  Elamprakash N. Savariar

发明人： Roger Y. Tsien ,  Tao Jiang ,  Elamprakash N. Savariar

IPC分类号： A61K51/00 ,  A61M36/14 ,  C07K19/00 ,  A61K49/00 ,  A61K41/00 ,  A61K47/48 ,  A61K49/08 ,  A61K49/14 ,  A61K51/08 ,  C07K14/47

CPC分类号： C07K19/00 ,  A61K41/0095 ,  A61K47/64 ,  A61K47/645 ,  A61K47/65 ,  A61K49/0032 ,  A61K49/0043 ,  A61K49/0056 ,  A61K49/085 ,  A61K49/14 ,  A61K49/146 ,  A61K51/088 ,  C07K14/4728

摘要： The invention provides compositions useful as molecular probes. In particular, the invention provides activatable cell penetrating peptides comprising a fluorescence donor and a fluorescence acceptor. Exemplary fluorescence donors and fluorescence acceptors include compounds derived from cyanine. Also provided are ratiometric, multispectral, and excitation lifetime imaging methods for detecting the molecular probes provided herein.

公开(公告)号：US09693957B2

公开(公告)日：2017-07-04

申请号：US14131575

申请日：2012-07-09

申请人： Wenbin Lin ,  Demin Liu ,  Joseph Della Rocca ,  Stephanie A. Kramer ,  Christopher Y. Poon

发明人： Wenbin Lin ,  Demin Liu ,  Joseph Della Rocca ,  Stephanie A. Kramer ,  Christopher Y. Poon

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K9/127 ,  A61K9/14 ,  A61K9/00 ,  A61K9/51 ,  A61K47/48 ,  A61K31/663 ,  A61K31/675 ,  A61K49/00 ,  A61K51/12

CPC分类号： A61K9/127 ,  A61K9/0019 ,  A61K9/14 ,  A61K9/5115 ,  A61K9/5123 ,  A61K9/5146 ,  A61K31/663 ,  A61K31/675 ,  A61K47/6929 ,  A61K49/00 ,  A61K51/1244

摘要： Metal-bisphosphonate nanoparticles are disclosed. Also disclosed are pharmaceutical compositions including the metal-bisphosphonate nanoparticles, methods of preparing the metal-bisphosphonate nanoparticles and materials comprising the nanoparticles, and methods of using the compositions to treat cancer or bone-related disorders (e.g., bone-resorption-related diseases, osteoporosis, Paget's disease, and bone metastases) and as imaging agents.

公开(公告)号：US09688673B2

公开(公告)日：2017-06-27

申请号：US14002964

申请日：2012-03-08

申请人： Caius G. Radu ,  Hsiang-I Liao ,  Nagichettiar Satyamurthy ,  Johannes Czernin ,  Jennifer M. Murphy ,  David A. Nathanson

发明人： Caius G. Radu ,  Hsiang-I Liao ,  Nagichettiar Satyamurthy ,  Johannes Czernin ,  Jennifer M. Murphy ,  David A. Nathanson

IPC分类号： A61K51/00 ,  A61M36/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/426 ,  A61K31/44 ,  A61K31/506 ,  A61K31/513 ,  G01N33/50

CPC分类号： C07D417/12 ,  A61K31/426 ,  A61K31/44 ,  A61K31/506 ,  A61K31/513 ,  C07D417/14 ,  G01N33/5088

摘要： The invention provides compounds that bind to deoxycytidine kinase (dCK) and compositions including pharmaceutically acceptable compositions containing the compounds. The compounds are useful in treating diseases and disorders where dCK activity is implicated such as cancer and immune disorders. The compounds also find use in clinical methodologies including positron emission tomography (PET) imaging.