Abstract: The present invention provides novel compounds having the general formula: wherein R1, R2, A and X are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
December 20, 2018
Date of Patent:
January 18, 2022
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Zhanling Cheng, Xingchun Han, Min Jiang, Song Yang
Abstract: Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
Type:
Grant
Filed:
September 7, 2018
Date of Patent:
June 22, 2021
Assignee:
PHASEBIO PHARMACEUTICALS, INC.
Inventors:
Steven Sparks, Christopher M. Yates, Sammy R. Shaver, William J. Hoekstra
Abstract: Disclosed are a class of coumarin-like cyclic compounds as MEK inhibitors and pharmaceutical compositions comprising the compounds, and the use of same in the preparation of a drug for treating MEK-related diseases. Particularly disclosed are compounds as shown in formula (I) and pharmaceutically acceptable salts thereof or tautomers thereof.
Abstract: RNA polymerase I (Pol I) is a dedicated polymerase for the transcription of the 47S ribosomal RNA precursor subsequently processed into the mature 5.8S, 18S and 28S ribosomal RNAs and assembled into ribosomes in the nucleolus. Pol I activity is commonly deregulated in human cancers. Based on the discovery of lead molecule BMH-21, a series of pyridoquinazolinecarboxamides were synthesized as inhibitors of Pol I and activators of the destruction of RPA194, the Pol I large catalytic subunit protein. The present invention identifies a set of bioactive compounds, including purified stereoisomers, that potently cause RPA194 degradation that function in a tightly constrained chemical space. Pharmaceutical compositions comprising these compounds and their uses in cancer and other Pol I related diseases is also provided.
Type:
Grant
Filed:
March 20, 2015
Date of Patent:
May 11, 2021
Assignee:
The Johns Hopkins University and Lieber Institute, Inc.
Inventors:
Marikki Laiho, Laureen Colis, James C. Barrow, Glen Ernst, Sara Sanders
Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an E3 ubiquitin ligase and on the other end a moiety which binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Type:
Grant
Filed:
December 22, 2017
Date of Patent:
May 4, 2021
Assignees:
ARVINAS OPERATIONS, INC., YALE UNIVERSITY
Inventors:
Andrew P. Crew, Kurt Zimmermann, Jing Wang, Craig M. Crews, Saul Jaime-Figueroa, George Burslem
Abstract: Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.
Type:
Grant
Filed:
May 11, 2017
Date of Patent:
April 20, 2021
Assignees:
Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Medshine Discovery Inc.
Abstract: Described herein are crystalline forms of a compound of formula (III?), including toluene solvates of TATD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane.
Type:
Grant
Filed:
March 4, 2019
Date of Patent:
March 9, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Kristos Adrian Moshos, Valdas Jurkauskas, Giovanni Fogliato, Manuel Scanu, You Seok Hwang
Abstract: This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula I, II or any of Compounds 100-128 or any of those in Tables 2 or 3) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.
Type:
Grant
Filed:
December 26, 2019
Date of Patent:
February 16, 2021
Assignee:
Alkermes, Inc.
Inventors:
Martin R. Jefson, John A. Lowe, III, Fabian Dey, Andreas Bergmann, Andreas Schoop, Nathan Oliver Fuller
Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
Type:
Grant
Filed:
October 17, 2017
Date of Patent:
February 2, 2021
Assignee:
Northwestern University
Inventors:
M. Amin Khan, Joseph R. Moskal, Paul Wood
Abstract: The present invention relates to novel forms of ethyl ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alaninate, pharmaceutical formulations, and therapeutic uses thereof in treating viral infections (e.g., an HIV infection).
Type:
Grant
Filed:
July 30, 2018
Date of Patent:
December 1, 2020
Assignee:
Gilead Sciences, Inc.
Inventors:
Olga Viktorovna Lapina, Bing Shi, Silas Wang
Abstract: The present invention relates to a novel naphtho class of compounds as Stat3 pathway inhibitors and as cancer stem cell inhibitors; to methods of using such compounds to treat cancer; to methods of using such compounds to treat disorders in a mammal related to aberrent Stat3 pathway activity; to pharmaceutical compositions containing such compounds.
Type:
Grant
Filed:
October 16, 2018
Date of Patent:
December 1, 2020
Assignee:
Sumitomo Dainippon Pharma Oncology, Inc.
Inventors:
Zhiwei Jiang, Chiang Jia Li, Wei Li, David Leggett
Abstract: The present invention provides mito-honokiol compounds, pharmaceutical compositions thereof, and methods of using the mito-honokiol compounds in the treatment of cancer.
Type:
Grant
Filed:
June 10, 2016
Date of Patent:
November 17, 2020
Assignees:
The Medical College of Wisconsin, Inc., Aix-Marseille Universite
Inventors:
Balaraman Kalyanaraman, Jacek Michal Zielonka, Micael J. Hardy, Oliver Ouari, Ming You
Abstract: The present invention relates to an improved process for the preparation of Valacyclovir or pharmaceutically acceptable salts thereof, which comprises reaction of amine-protected Valacyclovir or its salt with deprotecting agent in a continuous flow reactor.
Abstract: The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
Type:
Grant
Filed:
July 5, 2016
Date of Patent:
November 3, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Amjad Ali, Xianhai Huang, Yeon-Hee Lim, Rongze Kuang, Heping Wu, Rajan Anand, Younong Yu, Edward Metzger, Michael Man-Chu Lo, Pauline C. Ting, Andrew W. Stamford, Paul Tempest
Abstract: The present invention relates to compounds which have been discovered to be potent ligands (inhibitors) of human GLUT5 (glucose transporter type 5), a facilitative glucose transporter that transports fructose, and their use as ligands assays which can uncover additional ligands of GLUT5, having the potential for being used as drugs. In addition, the present invention is directed to compounds, chemical compositions and methods for treating disease states and conditions which are mediated through GLUT5, including such disease states and conditions as GLUT5 deficiency syndrome, diabetes (type I and II), cancer, metabolic diseases including metabolic syndrome and fatty liver disease, among others.
Type:
Grant
Filed:
June 10, 2016
Date of Patent:
November 3, 2020
Inventors:
Tudor I. Oprea, Cristian George Bologa, Oleg Ursu, Jun-Yong Choe, Cristina Iancu
Abstract: The present application relates to securinine or norsecurinine analogues that, when administered to immature myeloid cells, promote differentiation of these cells to mature cells that do not readily proliferate. Therefore, the agents are useful in the treatment of myeloid disorders including myeloproliferative disorders, acute myeloid leukemia, and autoimmune diseases. The agents may also be used as a myeloablative agent in conjunction with a bone marrow transplant or stem cell therapy.
Abstract: Provided are certain compounds or pharmaceutically acceptable salts thereof which can inhibit kinase activity of Bruton's tyrosine kinase (BTK) and may be useful for the treatment of diseases like cancer, immunological disease and inflammation.
Abstract: The present invention relates to: an organic compound represented by Chemical Formula 1; a composition for an organic optoelectronic diode containing the organic compound; and an organic optoelectronic diode to which the organic compound or the composition is applied. In Chemical Formula 1, Z, R1 to R11, and n1 to n4 are the same as those defined in the specification.
Type:
Grant
Filed:
November 18, 2015
Date of Patent:
September 22, 2020
Assignee:
SAMSUNG SDI CO., LTD.
Inventors:
Sujin Han, Dong Min Kang, Soohyun Min, Eun Sun Yu, Byoungkwan Lee, Hanill Lee, Sung-Hyun Jung, Ho Kuk Jung
Abstract: The present application provides a compound of Formula (I) as an inhibitor against wild-type EGFR and/or mutant EGFR, which may be used for treating human non-small cell lung cancer individually or in combination with other therapeutic agent(s). The compound of Formula (I) of the present application may be used for treating patients of drug-resistant human non-small cell lung cancer harboring wild-type EGFR and/or EGFR T790M mutation and/or EGFR L858R mutation and/or EGFR delE746_A750 mutation.
Type:
Grant
Filed:
December 27, 2016
Date of Patent:
September 22, 2020
Assignee:
PRECEDO PHARMACEUTICALS CO., LTD.
Inventors:
Qingsong Liu, Jing Liu, Xixiang Li, Aoli Wang, Hong Wu, Kailin Yu, Chen Hu, Wenchao Wang, Cheng Chen, Fengming Zou, Ziping Qi, Li Wang, Beilei Wang
Abstract: The present invention provides a compound of general formula (I) (wherein, R1, X, p and q are as described in the present description and claims), or a pharmacologically acceptable salt thereof, and a pharmaceutical composition containing that compound.