Abstract: Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.
Type:
Grant
Filed:
February 9, 2024
Date of Patent:
August 5, 2025
Assignee:
Incyte Corporation
Inventors:
Qinda Ye, Matthew McCammant, Rocco Policarpo, Artem Shvartsbart, Wenyu Zhu, Jeremy Roach, Gia Hoang, Bin Hu, Gencheng Li, Robert Susick, Padmaja Polam, Fenglei Zhang, Chao Qi, Xiaozhao Wang, Wenqing Yao, Alexander Sokolsky, Haolin Yin, Le Zhao, Peter Carlsen
Abstract: The present invention relates to novel methods and compounds for synthesizing amanitin derivatives. The invention in particular relates to methods for synthesizing (S)-6-hydroxy-tryptophan derivatives which can be used as building blocks for synthesizing amanitin derivatives or amatoxin drug conjugates. The invention further relates to intermediate compounds of said synthesis pathways for use in amanitin derivative and amatoxin drug conjugate synthesis, and to the use of particular catalysts suited for mediating said synthesis pathways.
Type:
Grant
Filed:
December 11, 2019
Date of Patent:
August 5, 2025
Assignee:
Heidelberg Pharma Research GmbH
Inventors:
Werner Simon, Susanne Werner-Simon, Christoph Müller
Abstract: Optionally substituted benzoimidazol-1,2-yl amides, such as compounds of Formula 1 or Formula 2, can be used to treat disorders associated with a Kv7 potassium channel activator. Compositions, medicaments, and dosage forms related to the treatment are also disclosed herein.
Type:
Grant
Filed:
October 20, 2023
Date of Patent:
July 8, 2025
Assignee:
Biohaven Therapeutics Ltd.
Inventors:
Lynn Resnick, George T. Topalov, Justin K. Belardi, James S. Hale, Scott S. Harried, Charles A. Flentge, David A. Mareska
Abstract: This invention relates to a process for producing cyanoacetates using asparagine as a precursor to cyanoacetamide, a staring material to form the cyanoacetates.
Type:
Grant
Filed:
October 18, 2021
Date of Patent:
July 8, 2025
Assignee:
Henkel AG & Co. KGaA
Inventors:
Cormac Duffy, Justine O'Sullivan, Ciara Goff, Umar Farid, Jessica Ramos, Michael Thai Trung King, Isidro Cobo Cardenete, Marisa Phelan, Barry Burns
Abstract: A process reduces the odor of compounds with al least one five-membered cyclic monothiocarbonate group, referred to as monothiocarbonate compounds. The monothiocarbonate compounds are in are liquid phase and are brought into contact with an oxidant.
Type:
Grant
Filed:
August 13, 2020
Date of Patent:
July 8, 2025
Assignee:
BASF SE
Inventors:
Indre Thiel, Thomas Maximilian Wurm, Peter Rudolf
Abstract: Provided are a compound having a 1,2,3,4-tetrahydronaphthalene moiety or pharmaceutically acceptable salt thereof, of Formula 1 a pharmaceutical composition comprising the same and a use thereof, where the compound having a 1,2,3,4-tetrahydronaphthalene moiety or pharmaceutically acceptable salt thereof has an inhibitory activity against glucosylceramide synthase (GCS), and therefore can be usefully applied for preventing or treating various diseases associated with GCS, such as Gaucher disease, Fabry disease, Tay-Sachs disease, Parkinson's disease, etc.
Type:
Grant
Filed:
November 12, 2020
Date of Patent:
June 24, 2025
Assignees:
Yuhan Corporation, Green Cross Corporation
Inventors:
Dong-Hoon Kim, Jae-Eun Joo, Eui-Chul Lee, Tae-Dong Han, Seung-Yub Shin, Sool-Ki Kwon, Young-Gyu Kong, Sang-Ho Ma, Ick-Hwan Son
Abstract: A method of synthesizing indole compounds. The method may include allyllating an indole compound, oxidizing the resulting ?-indolepropene, and reductively aminating the resulting indoleacetaldehyde, providing a tryptamine. The indole compound may be substituted with a functional group on the indole ring or may be unsubstituted indole. The method may include substitution, oxidation or other derivatization of the indole ring of the indole compound, of tryptophan, of the tryptamine, or of intermediates. The method may include oxidizing tryptophan or a ring-substituted tryptophan analogue and reductively aminating the resulting indoleacetaldehyde, providing a tryptamine. The method may be applied in a telescoped approach without isolation of intermediates. The method may be applied to production of indoles, ?-indolepropenes, indole propyl diols, indoleacetaldehydes and tryptamines. Compounds from each of these classes of compounds are also provided herein.
Type:
Grant
Filed:
December 17, 2021
Date of Patent:
June 17, 2025
Assignee:
1280225 B.C. LTD.
Inventors:
Jason Ellis Hein, Corey Sanz, Shao-Kai Chen, Blessing Cao
Abstract: The present invention discloses a class of anti-influenza virus compounds, and the use thereof in the preparation of a drug for treating diseases associated with influenza viruses. In particular, the present invention discloses a compound represented by formula (I) and a pharmaceutically acceptable salt thereof.
Abstract: The present disclosure is directed to salt and solid forms of (R)-1-(5-METHOXY-1H-INDOL-1-YL)-N,N-DIMETHYLPROPAN-2-AMINE and methods of treating neurological disorder and/or a psychiatric disorder in a subject in need thereof.
Abstract: Provided is a process for the preparation of a compound with at least one five-membered cyclic monothiocarbonate group. A compound C1 with at least one halohydrin group is used as starting material. Compound C1 is reacted with phosgene or an alkyl chloroformate to give an adduct C2. The adduct C2 is reacted with a compound that includes anionic sulfur to obtain the compound with at least one five-membered cyclic monothiocarbonate group.
Type:
Grant
Filed:
January 17, 2020
Date of Patent:
April 29, 2025
Assignee:
BASF SE
Inventors:
Peter Rudolf, Indre Thiel, Thomas Maximilian Wurm, Joaquim Henrique Teles, Jan-Dirk Arndt
Abstract: Provided are carbazole-based host compounds containing a 9-membered ring represented by Formula I where the variables are defined herein. Also provided are formulations comprising these carbazole-based hosts compounds. Further provided are OLEDs and related consumer products that utilize these carbazole-based hosts compounds.
Abstract: Provided herein are optionally substituted benzoimidazol-1,2-yl amides, pharmaceutical compositions comprising a therapeutically effective amount of such compounds and a pharmaceutically acceptable excipient, and methods of treating Kv7 associated diseases, such as, epilepsy, amyotrophic lateral sclerosis, various types of pain, hyperexcitability, a dyskinesia, dystonia, mania and tinnitus with such compounds and pharmaceutical compositions.
Type:
Grant
Filed:
June 20, 2023
Date of Patent:
April 29, 2025
Assignee:
Biohaven Therapeutics Ltd.
Inventors:
Michael E. Bozik, Scott S. Harried, Lynn Resnick, George T. Topalov, Justin K. Belardi, Charles A. Flentge, David A. Mareska, James S. Hale
Abstract: Provided herein are therapeutic and/or prophylactic compounds for mitochondrial or oxidative stress diseases such as cancer, amyotropic lateral sclerosis, Creutzfeldt-Jakob disease, Machado-Joseph disease, spinocerebellar ataxia, Huntington disease, Parkinson disease, Alzheimer disease, myocardial infarction, cerebral infarction, diseases related to aging, diabetes, alcoholic liver injury, chronic obstructive pulmonary disease, mitochondrial myopathy, encephalopathy, lactic acidosis, and stroke-like episodes (MELAS), and the like, wherein the compound is represented by formula (1), or reduced forms thereof, or pharmaceutically acceptable salts thereof.
Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
Type:
Grant
Filed:
October 2, 2020
Date of Patent:
April 15, 2025
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jie Chen, Carolyn Diane Dzierba, Junqing Guo, Amy C. Hart, William J. Pitts, Sing-Yuen Sit
Abstract: An amino dithioperacid thioester compound, a preparation method therefor, and use thereof. The structural formula of compound is as shown in formula I: wherein m=1-11, X is a nitrogen-containing aliphatic heterocyclic ring, and a nitrogen atom in the aliphatic heterocyclic ring is connected to a carbon atom of a thiocarbonyl group. The compounds disclosed by the invention are found to be capable of relieving muscular atrophy and lipolysis caused by cancer cachexia through in-vivo and in-vitro experiments. The compounds are also capable of obviously relieving weight and food intake reduction caused by cancer cachexia in animal experiments, so that the carbamo(dithioperoxo)thioates compounds have the effect on resisting cancer cachexia, can be applied to the treatment of cancer cachexia and related diseases, and become one kind of ideal cancer cachexia treatment medicament.
Type:
Grant
Filed:
November 27, 2020
Date of Patent:
April 8, 2025
Assignees:
FUDAN UNIVERSITY, EAST CHINA NORMAL UNIVERSITY
Abstract: The invention relates to pyrazolo-pyridine compounds which inhibit mitogen-activated protein kinase kinase 4 (MKK4) and in particular, selectively inhibit MKK4 over protein kinases JNK1 and MKK7. The compounds are useful for promoting liver regeneration or reducing or preventing hepatocyte death. They are further useful for treating osteoarthritis or rheumatoid arthritis, or CNS-related diseases.
Type:
Grant
Filed:
November 8, 2023
Date of Patent:
April 1, 2025
Assignee:
HEPAREGENIX GMBH
Inventors:
Bent Praefke, Philip Klövekorn, Roland Selig, Wolfgang Albrecht, Stefan Laufer
Abstract: The present disclosure provides compounds for treating a variety of diseases, such as respiratory syncytial virus (RSV), HRV, hMPV, Ebola, Zika, West Nile, Dengue, and HCV.
Type:
Grant
Filed:
July 18, 2023
Date of Patent:
April 1, 2025
Assignee:
Gilead Sciences, Inc.
Inventors:
Gregory F. Chin, Byoung-Kwon Chun, Michael O. Clarke, Bindu Goyal, Hon C. Hui, Petr Jansa, Richard L. Mackman, Dustin S. Siegel, Hai Yang
Abstract: The present disclosure is directed to modulators of SOS1 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.
Type:
Grant
Filed:
October 11, 2022
Date of Patent:
March 25, 2025
Assignee:
Revolution Medicines, Inc.
Inventors:
Adrian L. Gill, Andreas Buckl, Elena S. Koltun, Naing Aay, Arlyn A. Tambo-ong, Severin Thompson, Micah James Gliedt, John E. Knox, James Cregg, Anne V. Edwards, Yang Liu, G. Leslie Burnett