Abstract: Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.
Type:
Grant
Filed:
May 9, 2022
Date of Patent:
March 19, 2024
Assignees:
THE JOHNS HOPKINS UNIVERSTY, INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY AS CR V.V.I.
Inventors:
Barbara Slusher, Rana Rais, Marcela Krecmerova, Tomas Tichy, Pavel Majer, Andrej Jancarik
Abstract: The present disclosure relates to 3?3?-cyclic dinucleotides having a carbocyclic nucleotide and derivatives that can modulate the activity of the STING adaptor protein.
Type:
Grant
Filed:
March 4, 2020
Date of Patent:
September 26, 2023
Assignee:
INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.
Inventors:
Gabriel Birkus, Petra Brehova, Milan Dejmek, Radim Nencka, Ondrej Pav, Michal Sala
Abstract: Small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) and their use for treating neurodegenerative diseases, such as, neurodegenerative diseases associated with high levels of ceramide, including, but not limited to Alzheimer's disease (AD), HIV-associated neurocognitive disorder (HAND), multiple sclerosis (MS), and amyotrophic lateral sclerosis (ALS), and, in other aspects, for treating cancer, are provided.
Type:
Grant
Filed:
January 5, 2018
Date of Patent:
August 30, 2022
Assignees:
The Johns Hopkins University, Institute of Organic Chemistry & Biochemistry
Inventors:
Barbara Slusher, Camilo Rojas, Ajit G. Thomas, Radim Nencka, Michal Sala, Hubert Hrebabecky, Norman Haughey
Abstract: The present disclosure relates to 3?3?-cyclic dinucleotides having a carbocyclic nucleotide and derivatives that can modulate the activity of the STING adaptor protein.
Type:
Application
Filed:
March 4, 2020
Publication date:
May 26, 2022
Applicant:
INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I
Inventors:
Gabriel BIRKUS, Petra BREHOVA, Milan DEJMEK, Radim NENCKA, Ondrej PAV, Michal SALA
Abstract: The present disclosure relates to 2?3? cyclic phosphonate dinucleotides of Formula (I), the pharmaceutically acceptable salts, pharmaceutical composition and combinations of the substances and other medicaments or pharmaceuticals. The disclosure also relates to the compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases.
Type:
Application
Filed:
March 4, 2020
Publication date:
May 19, 2022
Applicant:
INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.
Inventors:
Gabriel BIRKUS, Ondrej PAV, Ondrej KOSTOV, Petra BREHOVA, Martin Maxmilian KAISER, Ondrej SIMAK
Abstract: The present disclosure relates to 3?3? cyclic phosphonate dinucleotides of general formula (I), their pharmaceutically acceptable salts, their pharmaceutical composition and combinations of the substances and other medicaments or pharmaceuticals. The disclosure also relates to compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases.
Type:
Application
Filed:
March 4, 2020
Publication date:
May 12, 2022
Applicant:
INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.
Inventors:
Gabriel BIRKUS, Ondrej PAV, Petra BREHOVA, Ondrej SIMAK
Abstract: The present invention relates to 3?3?-cyclic dinucleotides modified with a 3?-phosphonoalkyl bond and derivatives thereof, that can modulate the activity of the STING adaptor protein.
Type:
Grant
Filed:
April 4, 2019
Date of Patent:
April 5, 2022
Assignee:
INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.
Inventors:
Gabriel Birkus, Ondrej Pav, Ivan Rosenberg, Ondrej Simak
Abstract: The present disclosure relates to 2?3? cyclic phosphonate dinucleotides of general formula (J), their pharmaceutically acceptable salts, their pharmaceutical composition and combinations of said substances and other medicaments or pharmaceuticals. The disclosure also relates to the use of said compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. In addition, these substances can be used as adjuvants in vaccines.
Type:
Grant
Filed:
December 19, 2018
Date of Patent:
December 21, 2021
Assignee:
INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.
Inventors:
Gabriel Birkus, Ondrej Pav, Tomas Jandusik, Ivan Rosenberg, Radim Nencka
Abstract: The present disclosure relates to 2?3?-cyclic dinucleotides modified with a 2?- or 3?-phosphonoalkyl bond and derivatives thereof, that can modulate the activity of the STING adaptor protein.
Type:
Grant
Filed:
April 4, 2019
Date of Patent:
October 19, 2021
Assignee:
INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.
Inventors:
Gabriel Birkus, Ondrej Pav, Ivan Rosenberg, Ondrej Simak
Abstract: Provided herein are the 3?3? cyclic phosphonate dinucleotides of general formula J, their pharmaceutically acceptable salts, a pharmaceutical composition containing them and combinations of said substances and other medicaments or pharmaceuticals. The disclosure also relates to the use of said compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. In addition, these substances can be used as adjuvants in vaccines.
Type:
Grant
Filed:
December 19, 2018
Date of Patent:
April 6, 2021
Assignee:
INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.
Inventors:
Gabriel Birkus, Ondrej Pav, Tomas Jandusik, Ivan Rosenberg, Radim Nencka
Abstract: A device for parallel oligomer synthesis having a centrifuge with a plurality of reactor holders configured to retain reactors at an angle and a plurality of siphon based outflow holders are disclosed. A method of parallel solid-based peptide synthesis following the timing protocol of the device and a use of the device for parallel oligomer synthesis are also disclosed.
Type:
Application
Filed:
December 11, 2018
Publication date:
December 10, 2020
Applicants:
THE INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY AV CR, SPYDER INSTITUTE PRAHA S.R.O.
Inventors:
Michal LEBL, Zuzana FLEGELOVA, Pavel PONCAR, Petr MUDRA, Ondrej PACES, Matyas KNOR, Michal BUZEK, Jiri SMRZ, Vit POKORNY, Vaclav PESEK
Abstract: Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.
Type:
Grant
Filed:
January 4, 2019
Date of Patent:
February 4, 2020
Assignees:
Gilead Sciences Inc., Institute of Organic Chemistry and Biochemistry of the AS CR, V.V.I.
Inventors:
Ondrej Baszczynski, Milan Dejmek, Yunfeng Eric Hu, Petr Jansa, Eric Lansdon, Richard L. Mackman, Petr Simon
Abstract: The invention provides compounds of formula I, wherein R1, R2 and R3 have values defined in the specification and a pharmaceutically acceptable salt thereof; or an optical isomer thereof; or a mixture of optical isomers, as well as compositions comprising such compounds and therapeutic methods that utilize such compounds and/or compositions.
Type:
Grant
Filed:
March 8, 2017
Date of Patent:
May 21, 2019
Assignee:
INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.
Inventors:
Aurelie Bourderioux, Michal Hocek, Petr Naus
Abstract: Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.
Type:
Grant
Filed:
June 27, 2017
Date of Patent:
February 19, 2019
Assignees:
Gilead Sciences, Inc., Institute of Organic Chemistry and Biochemistry of the AS CR, V.V.I.
Inventors:
Ondrej Baszczynski, Milan Dejmek, Yunfeng Eric Hu, Petr Jansa, Eric Lansdon, Richard L. Mackman, Petr Simon
Abstract: A hypervalent iodine of formula (I) or formula (II) wherein R is a nucleophile and a method for their production is described. Such compounds can be used for fluoroethylation of compounds carrying a reactive group. A preferred compound carrying a reactive group is cystein in any environment such as peptide targets.
Type:
Grant
Filed:
August 3, 2015
Date of Patent:
August 7, 2018
Assignees:
ETH ZURICH, INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ACADEMY OF SCIENCES OF THE CZECH REPUBLIC, V.V.I
Inventors:
Vaclav Matousek, Petr Beier, Antonio Togni
Abstract: Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.
Type:
Grant
Filed:
August 6, 2015
Date of Patent:
June 5, 2018
Assignees:
THE JOHNS HOPKINS UNIVERSITY, INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY AS CR V.V.I.
Inventors:
Barbara Slusher, Rana Rais, Marcela Krecmerova, Tomas Tichy, Pavel Majer, Andrej Jancarik