Abstract: The inventive compounds are small molecule therapeutics that are potent inhibitors of arginase 1 and arginase 2 activity. The invention also provides pharmaceutical compositions comprising the compounds, and methods for using the compounds for treating or preventing a disease or condition associated with arginase activity.
Type:
Grant
Filed:
December 22, 2021
Date of Patent:
April 28, 2026
Assignee:
Molecure S.A.
Inventors:
Anna Gzik, Jacek Chrzanowski, Bartlomiej Borek, Roman Blaszczyk, Jacek Olczak, Adam Golebiowski, Marcin Mikolaj Grzybowski, Paulina Pomper, Nazan Cemre Güner-Chalimoniuk, Kamil Lisiecki, Damian Kusmirek
Abstract: The inventive compounds are small molecule therapeutics that are potent inhibitors of USP7 activity. The invention also provides pharmaceutical compositions comprising the compounds, and methods for using the compounds for treating or preventing a disease, disorder, or condition associated with USP7 activity.
Type:
Grant
Filed:
December 22, 2022
Date of Patent:
September 2, 2025
Assignee:
Molecure S.A.
Inventors:
Jacek Chrzanowski, Julita Nowicka, Łukasz Joachimiak, Robert Koralewski, Sylwia Olejniczak, Marzena Mazur, Bartlomiej Borek, Anna Gzik, Krzysztof Matyszewski, Sylwia Ciastek-Iskrzycka, Piotr Niedziejko, Angelika Muchowicz, Zbigniew Zasłona, Roman Błaszczyk, Jacek Olczak, Adam Golebiowski
Abstract: Disclosed are assays for screening active compounds interfering with interaction between chitinase-like protein YKL-40 and chitin oligomers, as well as interfering with interaction between chitinase-like protein YKL-40 and heparan sulfate. Moreover, disclosed are active compounds identified by these assays as inhibitors of chitinase-like protein YKL-40, their therapeutic applications, and their use in biosensors measuring the level of chitinase-like protein YKL-40 in biological samples.
Type:
Grant
Filed:
March 3, 2023
Date of Patent:
June 10, 2025
Assignee:
Molecure S.A.
Inventors:
Łukasz Krzemiński, Wojciech Czestkowski, Marzena Mazur, Gleb Andryianau, Sylwia Olejniczak, Michal Czesław Piotrowicz, Robert Koralewski, Elżbieta Pluta, Krzysztof Matyszewski, Michał Kowaiski, Barbara Dymek, Rafał Kozieł, Jacek Olozak, Adam Gołębiowski, Agnieszka Bartoszewicz, Katarzyna Krysztofiak
Abstract: The present invention relates to a process for the synthesis of 5-(4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-1H-1,2,4-triazol-3-amine in two hydrated crystalline forms and in one anhydrous crystalline form. The present invention further relates to methyl (Z)-4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)-N-cyanopiperidine-1-carbimidothioate which is an intermediate in this process.
Type:
Grant
Filed:
July 17, 2023
Date of Patent:
June 3, 2025
Assignee:
Molecure S.A.
Inventors:
Grzegorz Witkowski, Marta Magdycz, Magdalena Tyszkiewicz, Marcin Zakrzewski, Stanisław Pikul
Abstract: The present invention relates to a process for the synthesis of 5-(4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-1H-1,2,4-triazol-3-amine in two hydrated crystalline forms and in one anhydrous crystalline form. The present invention further relates to methyl (Z)-4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)-N-cyanopiperidine-1-carbimidothioate which is an intermediate in this process.
Type:
Grant
Filed:
September 25, 2020
Date of Patent:
September 5, 2023
Assignee:
Molecure S.A.
Inventors:
Grzegorz Witkowski, Marta Magdycz, Magdalena Tyszkiewicz, Marcin Zakrzewski, Stanislaw Pikul
Abstract: Disclosed are amino triazole compounds of formula (I). These compounds are inhibitors of acidic mammalian chitinase and chitotriosidase. Also disclosed are methods of using the compounds to treat asthma reactions caused by allergens, as well as acute and chronic inflammatory diseases, autoimmune diseases, dental diseases, neurologic diseases, metabolic diseases, liver diseases, polycystic ovary syndrome, endometriosis, and cancer.
Type:
Grant
Filed:
July 15, 2020
Date of Patent:
May 2, 2023
Assignee:
Molecure S.A.
Inventors:
Marzena Mazur, Gleb Andryianau, Lukasz Joachimiak, Wojciech Czestkowski, Michal Kowalski, Piotr Niedziejko, Sylwia Olejniczak, Krzysztof Matyszewski, Robert Koralewski, Jacek Olczak, Adam Golebiowski, Agnieszka Bartoszewicz