Patents Examined by Bruck Kifle
  • Patent number: 10751341
    Abstract: The invention provides substituted pyrrolo[1,2-a]pyrimidines and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrrolo[1,2-a]pyrimidines compounds described herein include substituted 2,4-dimethyl-N-phenylpyrrolo[1,2-a]pyrimidine-8-carboxamide compounds and variants thereof.
    Type: Grant
    Filed: June 26, 2019
    Date of Patent: August 25, 2020
    Assignee: Lysosomal Therapeutics Inc.
    Inventors: Renato T. Skerlj, Peter T. Lansbury, Andrew C. Good, Elyse Marie Josee Bourque, Richard B. Silverman, Dimitri Krainc, Jianbin Zheng
  • Patent number: 10751339
    Abstract: The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: August 25, 2020
    Assignees: SUNSHINE LAKE PHARMA CO., LTD., CALITOR SCIENCES, LLC
    Inventors: Ning Xi, Liang Wang, Xuejin Feng, Min Liao
  • Patent number: 10745401
    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
  • Patent number: 10745379
    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
  • Patent number: 10738051
    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
  • Patent number: 10738050
    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
  • Patent number: 10730870
    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
  • Patent number: 10723717
    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
  • Patent number: 10722588
    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
  • Patent number: 10711010
    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
  • Patent number: 10710999
    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.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: July 14, 2020
    Assignee: MYLAN LABORATORIES LIMITED
    Inventors: Mahdeshkumar Gadakar, Dnyandeo Punde, Rajendra Yadav, Yogesh Wakchaure
  • Patent number: 10711014
    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
  • Patent number: 10710995
    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
  • Patent number: 10702505
    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.
    Type: Grant
    Filed: January 17, 2018
    Date of Patent: July 7, 2020
    Assignee: CIPLA Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manjinder Singh Phull, Muruti Ghagare
  • Patent number: 10703733
    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
  • Patent number: 10703763
    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
  • Patent number: 10696655
    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
  • Patent number: 10695348
    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
  • Patent number: 10689325
    Abstract: Processes are described for the preparation of F-benzoxazinorifamycin I: and intermediates for conjugation with an antibody.
    Type: Grant
    Filed: May 17, 2019
    Date of Patent: June 23, 2020
    Assignee: Genentech, Inc.
    Inventors: Stephan Bachmann, Serena Maria Fantasia, Michael Jansen, Stefan Koenig, Xin Linghu, Sebastian Rieth, Nathaniel L. Segraves, Andreas Zogg
  • Patent number: 10683302
    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