Abstract: The present invention relates to a medicament for treating neuropsychiatric diseases, comprising a compound of Formula (1): or a pharmaceutically acceptable salt thereof, as an active ingredient.
Type:
Grant
Filed:
February 10, 2020
Date of Patent:
August 18, 2020
Assignee:
SUMITOMO DAINIPPON PHARMA CO., LTD.
Inventors:
Hidefumi Yoshinaga, Yohei Ikuma, Junya Ikeda, Satoshi Adachi, Harunobu Mitsunuma, Yoshinori Aihara, Jeremy Besnard, Andrew Simon Bell
Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
Type:
Grant
Filed:
November 8, 2018
Date of Patent:
August 18, 2020
Assignee:
Cornell University
Inventors:
Joseph P. Vacca, Dansu Li, Sarah Bettigole
Abstract: Disclosed in the present invention is a type of novel ?-lactamase inhibitors, and specifically disclosed are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
June 2, 2017
Date of Patent:
August 11, 2020
Assignee:
QILU PHARMACEUTICAL CO., LTD.
Inventors:
Boyu Hu, Charles Z. Ding, Zhigang Huang, Ruibin Lin, Minliang Xiao, Jinsheng Xie, Shuhui Chen, Cheng Li
Abstract: The present invention relates to compounds of the formula I or II: (I) (II) processes for their preparation and their use as pharmaceutical agents or compositions in the treatment, of neurological disorders.
Type:
Grant
Filed:
May 10, 2019
Date of Patent:
August 11, 2020
Assignee:
Prana Biotechnology Limited
Inventors:
Penelope Jane Huggins, Jack Gordon Parsons, Kevin Jeffrey Barnham, Elisabeth Colette Louise Gautier, Antony Vincent Robinson
Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the 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 effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
Type:
Grant
Filed:
March 18, 2016
Date of Patent:
August 4, 2020
Assignees:
ARVINAS OPERATIONS, INC., YALE UNIVERSITY
Inventors:
Andrew P. Crew, Craig M. Crews, Xin Chen, Hanqing Dong, Caterina Ferraro, Yimin Qian, Kam Siu, Jing Wang, Meizhong Jin, Michael Berlin, Kurt Zimmermann, Lawrence Snyder
Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of 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, or the constitutive activation 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:
July 28, 2020
Assignees:
ARVINAS OPERATIONS, INC., YALE UNIVERSITY
Inventors:
Andrew P. Crew, Keith R. Hornberger, Jing Wang, Hanqing Dong, Yimin Qian, Craig M. Crews, Saul Jaime-Figueroa
Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VI). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.
Type:
Grant
Filed:
February 13, 2019
Date of Patent:
July 28, 2020
Assignee:
IMMUNOGEN, INC.
Inventors:
Ravi V. J. Chari, Michael Louis Miller, Manami Shizuka
Abstract: The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.
Type:
Grant
Filed:
September 26, 2017
Date of Patent:
July 14, 2020
Assignees:
Rhode Island Hospital, Midwestern University
Inventors:
Jack R. Wands, Suzanne De La Monte, Arihiro Aihara, Mark Jon Olsen, John-Michael Thomas
Abstract: The present disclosure provides a novel polymorph of an intermediate useful in the preparation of palbociclib. The polymorph has enhanced properties that influence process ability of the intermediate and synthesis of palbociclib.
Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R13, Ra, Rb, A and n are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring a pro-apoptotic agent.
Type:
Grant
Filed:
January 15, 2019
Date of Patent:
July 14, 2020
Assignees:
LES LABORATORIES SERVIER, VERNALIS (R&d) LTD
Inventors:
Zoltán Szlávik, András Kotschy, Maïa Chanrion, Didier Demarles, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, Szabolcs Sipos, Attila Paczal, Balázs Bálint
Abstract: Compositions and methods for inhibits the binding of GTP to oncogenic mutant KRas are disclosed. These compositions may be used in method to treat a subject with cancer. In particular, the compositions may be used to treat cancers involving overactive Ras signaling.
Type:
Grant
Filed:
August 14, 2019
Date of Patent:
July 14, 2020
Assignees:
H. Lee Moffitt Cancer Center and Research Institute, Inc., Torrey Pines Institute for Molecular Studies
Inventors:
Said M. Sebti, Yangmei Li, Richard A. Houghten
Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.
Type:
Grant
Filed:
March 4, 2019
Date of Patent:
July 7, 2020
Assignee:
ALFASIGMA S.P.A.
Inventors:
Giuseppe Claudio Viscomi, Manuela Campana, Donatella Confortini, Maria Barbanti, Dario Braga
Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.
Type:
Grant
Filed:
May 13, 2019
Date of Patent:
July 7, 2020
Assignee:
Gilead Sciences, Inc.
Inventors:
Hang Chu, Juan A. Guerrero, Anna E. Hurtley, Tae H. Hwang, Lan Jiang, Darryl Kato, Tetsuya Kobayashi, John E. Knox, Scott E. Lazerwith, Xiaofen Li, David W. Lin, Jonathan W. Medley, Michael L. Mitchell, Devan Naduthambi, Zachary Newby, Neil H. Squires, Vickie H. Tsui, Chandrasekar Venkataramani, William J. Watkins, Hong Yang
Abstract: Amorphous rifaximin, methods of making it, and pharmaceutical compositions containing it. Also described are methods of converting amorphous rifaximin to crystalline rifaximin and vice versa.
Abstract: The invention provides compounds of formula I: and pharmaceutically acceptable salts thereof where R1 is a substituted or unsubstituted phenyl or a fused bicyclic comprising a substituted or unsubstituted phenyl. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
Type:
Grant
Filed:
February 7, 2019
Date of Patent:
June 30, 2020
Assignee:
Genentech, Inc.
Inventors:
Vishal Verma, Matthew Volgraf, Baihua Hu
Abstract: The present invention relates to compounds of formula (I) and formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R5-R6 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
Type:
Grant
Filed:
November 21, 2018
Date of Patent:
June 30, 2020
Assignees:
GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
Inventors:
Patrick Cyr, Sarah Bronner, F. Anthony Romero, Steven Magnuson, Vickie Hsiao-Wei Tsui, John Wai, Kwong Wah Lai, Fei Wang
Abstract: The invention relates to a xanthine derivative defined by chemical formula I or a salt thereof, its use as a medicament, especially for use in the treatment of serotonin-related diseases or disorders, and a pharmaceutical preparation comprising the xanthine derivative. The novel xanthine compounds are capable of inhibiting tryptophan hydroxylases (TPH) involved in the biosynthesis of serotonin and are effective in influencing the serotonin level in the body.
Type:
Grant
Filed:
July 27, 2017
Date of Patent:
June 16, 2020
Assignees:
MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN, FORSCHUNGSVERBUND BERLIN E.V.
Inventors:
Michael Bader, Edgar Specker, Susann Matthes, Anja Schütz, Keven Mallow, Maik Grohmann, Marc Nazaré
Abstract: The present invention is directed to inhibitors of the interaction of menin with MLL and MLL fusion proteins, pharmaceutical compositions containing the same, and their use in the treatment of cancer and other diseases mediated by the menin-MLL interaction.
Type:
Grant
Filed:
June 8, 2017
Date of Patent:
June 16, 2020
Assignee:
VITAE PHARMACEUTICALS, LLC
Inventors:
Salvacion Cacatian, David A. Claremon, Lawrence Wayne Dillard, Chengguo Dong, Yi Fan, Lanqi Jia, Stephen D. Lotesta, Andrew Marcus, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Jing Yuan, Yajun Zheng, Linghang Zhuang, Stephan D. Parent, Travis L. Houston
Abstract: Among the various aspects of the present disclosure is the provision of a compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof. Provided are imaging agents for imaging S1P1 and S1P1 associated diseases, disorders, and conditions. Also provided are therapeutic compositions and methods for the treatment of S1P1 associated diseases, disorders, and conditions.
Type:
Grant
Filed:
July 2, 2018
Date of Patent:
June 9, 2020
Assignee:
Washington University
Inventors:
Zhude Tu, Adam Rosenberg, Hui Liu, Junbin Han