Abstract: Disclosed are anthranilic amide derivatives having the formula. Compositions are disclosed that include the anthranilic amide derivatives and the use of the anthranilic amide derivatives for the manufacture of a medicament. Further disclosed are methods of inhibiting or treating cancer, inhibiting or reversing an epithelial to mesenchymal cellular transition, and/or inhibiting MEK1/2 and/or MEK 5 enzymatic activity in a subject by administering to the subject an effective amount of a disclosed anthranilic amide derivative.
Type:
Grant
Filed:
September 11, 2014
Date of Patent:
October 11, 2022
Assignees:
THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND, DUQUESNE UNIVERSITY OF THE HOLY GHOST
Inventors:
Suravi Chakrabarty, Patrick T. Flaherty, Darlene Monlish, Jane E. Cavanaugh, Matthew E. Burow, Steven Elliott, Van T. Hoang
Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.
Abstract: The present invention discloses a compound comprising the formula: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CH2, and optionally comprising a pharmaceutically acceptable salt, hydrate, or solvate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt, hydrate, or solvate thereof.
Abstract: The present disclosure relates to lead ion sensors for testing, detecting and analyzing particle-containing samples for gunshot residue. The lead ion sensors include a fluorophore itself or a combination of a fluorophore and matrix material. The particle-containing samples are contacted with the lead ion sensors. Due to a presence of Pb2+ ions in a sample, a fluorescence emission is visually observed and a correlation of a presence of gunshot residue can be made. In addition, the fluorescence emission intensity can be assessed to obtain information relating to the GSR sample. Further, there is provided a device for conducting on-site testing, detecting and analyzing of particle-containing samples for gunshot residue.
Type:
Application
Filed:
July 31, 2015
Publication date:
June 1, 2017
Applicant:
DUQUESNE UNIVERSITY OF THE HOLY GHOST
Inventors:
Partha Basu, Antoinette Peterson, John Thomas
Abstract: This invention provides substituted pyrimidine compounds having the formula: wherein X is absent, CH2, S, or O, and R is an alkyl group having from one to ten carbon atoms, and optionally salts, hydrates, or solvates thereof, that are useful in treating a patient having a disease or cancer. The compounds of this invention are useful as multi-enzyme antifolates selectively targeting the folate receptor (FR). Further, a method of making 5- and 6-substituted cyclopenta[d]pyrimidine for nonclassical and classical antifolates as TS and DHFR inhibitors is provided.
Abstract: The invention generally relates to compounds having structure I: wherein x represents alkyl, aryl or het-aryl, each of y independently represents hydrogen or halogen and z represents hydrogen or alkyl. Further, said compounds are inhibitors of MEK 1, 2 and 5. Furthermore, the invention includes methods of making said compounds, compositions including said compounds and uses for inhibiting MEK 1, 2 and 5.
Type:
Application
Filed:
December 19, 2016
Publication date:
April 6, 2017
Applicant:
DUQUESNE UNIVERSITY OF THE HOLY GHOST
Inventors:
SURAVI CHAKRABARTY, DARLENE MONLISH, PATRICK FLAHERTY, JANE E. CAVANAUGH, SNEHA POTDAR
Abstract: The invention generally relates to compounds having structure I: wherein x represents alkyl, aryl or het-aryl, each of y independently represents hydrogen or halogen and z represents hydrogen or alkyl. Further, said compounds are inhibitors of MEK 1, 2 and 5. Furthermore, the invention includes methods of making said compounds, compositions including said compounds and uses for inhibiting MEK 1, 2 and 5.
Type:
Grant
Filed:
November 15, 2013
Date of Patent:
January 31, 2017
Assignee:
Duquesne University of the Holy Ghost
Inventors:
Suravi Chakrabarty, Darlene Monlish, Patrick Flaherty, Jane E. Cavanaugh, Sneha Potdar
Abstract: Pyrrolo[2,3-d]pyrimidine derivatives, and pharmaceutical acceptable salts thereof, useful in therapeutically treating patients with cancer are disclosed. These compounds selectively target folate receptors (FR) of cancerous tumor cells and inhibit purine synthesis and hence, DNA synthesis.
Type:
Application
Filed:
September 29, 2016
Publication date:
January 19, 2017
Applicants:
DUQUESNE UNIVERSITY OF THE HOLY GHOST, WAYNE STATE UNIVERSITY
Abstract: Pyrrolo[2,3-d]pyrimidine derivatives, and pharmaceutical acceptable salts thereof, useful in therapeutically treating patients with cancer are disclosed. These compounds selectively target folate receptors (FR) of cancerous tumor cells and inhibit purine synthesis and hence, DNA synthesis.
Type:
Grant
Filed:
February 9, 2015
Date of Patent:
November 1, 2016
Assignees:
Duquesne University of the Holy Ghost, Wayne State University
Abstract: This invention relates to novel isonitriles, including arylthio isonitriles, and methods for their preparation. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions.
Type:
Grant
Filed:
February 20, 2015
Date of Patent:
November 1, 2016
Assignee:
Duquesne University of the Holy Ghost
Inventors:
Fraser Fergusson Fleming, Jesus Armando Lujan-Montelongo
Abstract: A method for treating cancer tumors, particularly ovarian cancer tumors, is described, where fused cyclic pyrimidine having a cancer treating ability is selectively delivered to an FR expressing cancerous tumor.
Type:
Grant
Filed:
January 8, 2015
Date of Patent:
September 20, 2016
Assignees:
Duquesne University of the Holy Ghost, Wayne State University
Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
Abstract: Pyrrolo[2,3-d]pyrimidine derivatives, and pharmaceutical acceptable salts thereof, useful in therapeutically treating patients with cancer are disclosed. These compounds selectively target folate receptors (FR) of cancerous tumor cells and inhibit purine synthesis and hence, DNA synthesis.
Abstract: The invention relates to non-fluorescent or low-fluorescent compounds for contact with mercury ions to produce fluorescent compounds as a detector for mercury. The fluorescence produced by the contact of the non-fluorescent or low-fluorescent compounds with mercury ions has an intensity greater than the intensity produced by the contact of the non-fluorescent or low-fluorescent compounds with other metals. The fluorescent compounds may be used as sensors/detectors for mercury ions in various samples. Methods for detecting and calculating the concentration of mercury ions in samples are also disclosed.
Type:
Application
Filed:
October 1, 2014
Publication date:
April 7, 2016
Applicant:
DUQUESNE UNIVERSITY OF THE HOLY GHOST
Inventors:
Partha BASU, Igor PIMKOV, Kristine DEIBLER
Abstract: The present invention relates to substituted pterin compounds, their synthesis and use. In particular, the present invention relates to a new precursor compound and its analogs for synthesizing a new substituted pterin compound and its analogs. These new compounds are particularly suitable for treating molybdenum cofactor deficiency.
Abstract: This invention relates to novel isonitriles, including arylsulfonyl isonitriles, and methods for their synthesis. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions.
Type:
Application
Filed:
February 20, 2015
Publication date:
August 27, 2015
Applicant:
DUQUESNE UNIVERSITY OF THE HOLY GHOST
Inventors:
FRASER FERGUSSON FLEMING, Jesus Armando Lujan-Montelongo
Abstract: This invention relates to novel isonitriles, including arylthio isonitriles, and methods for their preparation. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions.
Type:
Application
Filed:
February 20, 2015
Publication date:
August 27, 2015
Applicant:
DUQUESNE UNIVERSITY OF THE HOLY GHOST
Inventors:
FRASER FERGUSSON FLEMING, Jesus Armando Lujan-Montelongo