Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
Type:
Grant
Filed:
August 21, 2018
Date of Patent:
June 23, 2020
Assignee:
Agios Pharmaceuticals, Inc.
Inventors:
Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
Abstract: The present disclosure relates generally to compounds and pharmaceutical compositions suitable as modulators of hemoglobin, and methods for their use in treating disorders mediated by hemoglobin.
Abstract: The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.
Type:
Grant
Filed:
July 27, 2018
Date of Patent:
June 16, 2020
Assignee:
Ogeda SA
Inventors:
Hamid R. Hoveyda, Guillaume Dutheuil, Graeme Lovat Fraser, Marie-Odile Roy, Mohamed El Bousmaqui, Frederic Batt
Abstract: Compounds for the treatment of hyperglycemia and/or diabetes are provided. The compounds, which inhibit the enzyme dipeptidyl peptidase (DPP-4), are based on the structure where X may be present or absent an may be OH, Ar is an aryl group; and n ranges from 0 to 5.
Type:
Grant
Filed:
November 21, 2019
Date of Patent:
June 16, 2020
Assignee:
KING ABDULAZIZ UNIVERSITY
Inventors:
Abdelsattar M. Omar, Mohamed A. El-Zahabi, Salah G. Atteiah, Ashraf B. Abdel-Naim, Moustafa E. El-Araby
Abstract: Compounds and compositions comprising them are provided. The compounds and compositions are useful for inhibiting transport of heme across membranes in parasitic heme auxotrophic organisms, thereby limiting their growth or killing the parasites.
Type:
Grant
Filed:
January 29, 2019
Date of Patent:
May 26, 2020
Assignees:
University of Maryland, College Park, University of Maryland, Baltimore
Abstract: Compounds for the treatment of hyperglycemia and/or diabetes are provided. The compounds, which inhibit the enzyme dipeptidyl peptidase (DPP-4), are based on the structure where X may be present or absent an may be OH, Ar is an aryl group; and n ranges from 0 to 5.
Type:
Grant
Filed:
March 16, 2020
Date of Patent:
May 19, 2020
Assignee:
KING ABDULAZIZ UNIVERISTY
Inventors:
Abdelsattar M. Omar, Mohamed A. El-Zahabi, Salah G. Atteiah, Ashraf B. Abdel-Naim, Moustafa E. El-Araby
Abstract: The present invention provides a new method for making TH-302 and solid forms thereof. The compound in its solid form is an effective anti-cancer agent and may be used in various pharmaceutical compositions, and are particularly effective for the treatment of cancer. The invention also provides a method for preparing such compounds and forms and for treating cancer in a mammal comprising the step of administering a therapeutically effective amount of a solid form of TH-302 thereof.
Type:
Grant
Filed:
November 16, 2018
Date of Patent:
May 19, 2020
Assignee:
Molecular Templates, Inc.
Inventors:
Jian-Xin Duan, Mark Matteucci, Nipun Davar, Denise Andersen
Abstract: Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. A substituted hydrocarbon is added to water to form a mixture, and a 1-oxa-4-azacyclohexane derivative is then added. The reaction mixture stirred until a solution containing the 1-oxa-4-azonium cyclohexane salt is obtained.
Type:
Grant
Filed:
May 16, 2018
Date of Patent:
May 19, 2020
Inventors:
Christopher P. Nicholas, Mark A. Miller, Melissa M. Galey, Benjamin D. Yuhas, Sesh Prabhakar
Abstract: Provided herein are novel maytansinoid compounds of general formula I. Also provided herein are conjugates comprising the compounds linked to a binding protein via a linker, and conjugating reagents comprising the compounds attached via a linker to at least one functional group capable of reacting with a binding protein. Also provided herein are pharmaceutical compositions comprising the compounds and conjugates, therapeutic methods and uses involving the compounds and conjugates, for example in cancer therapy, and novel synthetic processes.
Type:
Grant
Filed:
September 15, 2017
Date of Patent:
May 19, 2020
Assignee:
POLYTHERICS LIMITED
Inventors:
Nareshkumar Jain, Sanjeevani Ghone, Sean Smith, Ian Glassford, Sylvia J. Degrado, Fu-an Kang, Senzhi Zhao
Abstract: The present invention provides compounds as bacterial topoisomerase inhibitors with antibacterial activity. The present invention also provides pharmaceutical compositions comprising at least one of the compounds and methods of using the compounds and pharmaceutical compositions as antibacterial agents for treating infectious diseases.
Type:
Grant
Filed:
March 4, 2019
Date of Patent:
May 19, 2020
Assignees:
THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES, UNIVERSITY OF HAWAII
Abstract: Provided herein are benzimidazole derivatives, for example, of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
Abstract: The present disclosure is directed to the synthesis and application of undecavertol derivatives having unique and desired flavor and/or fragrant characteristics. The compounds of the present disclosure can be employed alone or incorporated as fragrance or flavor ingredients in fragrance or flavor compositions. The present disclosure is also directed to consumer products comprising such derivatives and/or fragrance or flavor compositions.
Abstract: The present disclosure provides a compound of Formula (I?): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein R1, R2, Rx, X1, n, n1, and q are as defined herein, and methods of making and using same.
Type:
Grant
Filed:
August 5, 2019
Date of Patent:
May 12, 2020
Assignee:
Novartis AG
Inventors:
Rohan Eric John Beckwith, Simone Bonazzi, Artiom Cernijenko, Ritesh Bhanudasji Tichkule, Michael Scott Visser
Abstract: The present disclosure provides a compound of Formula (I?): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein R1, R2, Rx, X1, n, n1, and q are as defined herein, and methods of making and using same.
Type:
Grant
Filed:
August 5, 2019
Date of Patent:
May 5, 2020
Assignee:
Novartis AG
Inventors:
Rohan Eric John Beckwith, Simone Bonazzi, Artiom Cernijenko, Ritesh Bhanudasji Tichkule, Michael Scott Visser
Abstract: Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. A substituted hydrocarbon is added to water to form a mixture, and a 1-oxa-4-azacyclohexane derivative is then added. The reaction mixture stirred until a solution containing the 1-oxa-4-azonium cyclohexane salt is obtained.
Type:
Grant
Filed:
May 16, 2018
Date of Patent:
April 28, 2020
Inventors:
Christopher P. Nicholas, Mark A. Miller, Melissa M. Galey, Benjamin D. Yuhas, Sesh Prabhakar
Abstract: The present invention is directed to certain amides and heterocyclic compounds. The present invention also relates to uses of these compounds to treat several diseases including autoimmune disorders, cardiovascular disorders, inflammation, central nervous system disorders, arterial thrombotic disorders, fibrotic disorders, glaucoma, and neoplastic disorders.
Abstract: A method for producing a compound (4), which comprises allowing a compound (1) to react with hydrogen gas in an inert solvent, in the presence of a specific chiral ligand and a ruthenium catalyst, or in the presence of an asymmetric transition metal complex catalyst previously generated from the chiral ligand and the ruthenium catalyst.
Abstract: The present invention relates to an improved process for the preparation of enzalutamide by conventional synthesis, which avoids utilization of microwave irradiation and noxious reagents. The present invention also relates to an improved process for preparation of 4-isothiocyanato-2-(trifluoromethyl) benzonitrile, which is an intermediate in the synthesis of Enzalutamide.
Abstract: Isoindoline sigma-2 receptor antagonist compounds, pharmaceutical compositions comprising such compounds, and methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology are provided.
Type:
Grant
Filed:
December 21, 2018
Date of Patent:
April 7, 2020
Assignee:
COGNITION THERAPEUTICS, INC.
Inventors:
Gilbert M. Rishton, Susan M. Catalano, Gary C. Look