Patents Examined by Timothy R Rozof
  • Patent number: 10927077
    Abstract: Disclosed is a process for preparing an intermediate of anti-tumor drug niraparib and an intermediate thereof. The present invention discloses a process for preparing compound f, which comprises conducting a cyclization reaction of compound e in a solvent and in the presence of a base to give compound f. The process of the present invention does not involve the steps of catalytic reduction or catalytic coupling reaction of precious metals and chiral separation, which has advantages such as low equipment requirements, simple operation, favorable industrial production, avoiding waste liquid containing heavy metals and phosphorus, low cost and high product ee value.
    Type: Grant
    Filed: October 12, 2018
    Date of Patent: February 23, 2021
    Assignee: ZAI LAB (SHANGHAI) CO., LTD.
    Inventor: Tianhao Wang
  • Patent number: 10927078
    Abstract: Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.
    Type: Grant
    Filed: June 27, 2018
    Date of Patent: February 23, 2021
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Martha Alicia De La Rosa, Wieslaw Mieczyslaw Kazmierski, Yoshiaki Washio
  • Patent number: 10913753
    Abstract: The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula: where R1, R2, R3, R4, R5, R5?, R6, R7, X, m, and n are described herein.
    Type: Grant
    Filed: February 13, 2017
    Date of Patent: February 9, 2021
    Assignee: VALO EARLY DISCOVERY, INC.
    Inventors: David Joseph Guerin, Kenneth W. Bair, Justin A. Caravella, Stephanos Ioannidis, Jr., David R. Lancia, Jr., Hongbin Li, Steven Mischke, Pui Yee Ng, David Richard, Shawn E. R. Schiller, Tatiana Shelekhin, Zhongguo Wang
  • Patent number: 10913749
    Abstract: The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
    Type: Grant
    Filed: April 18, 2019
    Date of Patent: February 9, 2021
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Francis G. Fang, Dae-Shik Kim, Hyeong-Wook Choi, Charles E. Chase
  • Patent number: 10906924
    Abstract: Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.
    Type: Grant
    Filed: June 27, 2018
    Date of Patent: February 2, 2021
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Martha Alicia De La Rosa, Hongfeng Deng, Ghotas Evindar, Wieslaw Mieczyslaw Kazmierski, John Franklin Miller, Vicente Samano, Yoshiaki Washio, Bing Xia
  • Patent number: 10906875
    Abstract: The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): comprising treating a compound of Formula (I): with a transition metal catalyst and under alkylation conditions as valence and stability permit.
    Type: Grant
    Filed: May 31, 2019
    Date of Patent: February 2, 2021
    Assignee: California Institute of Technology
    Inventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
  • Patent number: 10899713
    Abstract: The present invention relates to an improved process for the preparation of quinolone based compounds of general formula (I) using intermediate compound of general formula (XII). Invention also provides an improved process for the preparation of compound of formula (I-a) using intermediate compound of formula (XII-a) and some novel impurities generated during process. Compounds prepared using this process can be used to treat anemia.
    Type: Grant
    Filed: May 24, 2019
    Date of Patent: January 26, 2021
    Assignee: CADILA HEALTHCARE LIMITED
    Inventors: Ranjit C. Desai, Rajiv Sharma, Vrajesh Pandya, Kalpesh Shah, Sunil Patel, Rakesh Chauhan, Ranjeet Nair, Vivek Joshi, Manoj Patel, Mrigendra Shukla
  • Patent number: 10889611
    Abstract: Disclosed herein are novel sialyltransferase inhibitors, and compositions and methods for treating diseases and/or conditions associated with the activation of sialyltransferase, such as a cancer, an immune disease or an inflammatory disease.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: January 12, 2021
    Assignee: Academia Sinica
    Inventors: Wen-Shan Li, Wen-Chun Hung, Chia-Ning Shen
  • Patent number: 10889575
    Abstract: The invention belongs to the field of medicine and chemical industry and relates to a 4,4-diphenylpiperidine compound or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same and uses thereof. In particular, the invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, and to a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof. In the present invention, the compound or pharmaceutically acceptable salt thereof and the pharmaceutical composition have significant activity in blocking an N-type calcium channel, and have good pharmacokinetic properties, can effectively relieve pain, and have a potential as a new medicament for prevention or treatment of pain, stroke, cerebral ischemia, alcohol addiction, alcoholism, kidney disease, addictive disorder caused by analgesic or tolerance disorder caused by analgesic.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: January 12, 2021
    Assignee: Academy of Military Medical Sciences
    Inventors: Cheng Zhang, Haoshan Wang, Guoxing Dong, Ning Wu, Shuzhuo Zhang, Xiaomei Zhuang, Chong Pang, Juan Wang, Rifang Yang, Jianquan Zheng, Jin Li, Liuhong Yun
  • Patent number: 10889569
    Abstract: A condensed ring group azacyclobutyl triazole derivative, a preparation method therefor and use thereof in medicine are provided. In particular, a condensed ring group azacyclobutyl triazole derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, use thereof as a therapeutic agent, in particular as an oxytocin antagonist, and for treating or preventing a disease or a condition that is known or can exhibit a beneficial effect of inhibiting oxytocin are provided. The definition for each substituent in general formula (I) is the same as that in the description.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: January 12, 2021
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Xin Li, Wei He, Bin Wang, Zhigao Zhang, Feng He, Weikang Tao
  • Patent number: 10889585
    Abstract: The present invention relates generally to glutaminase inhibitors of Formula I, Formula II, or Formula III, as well as pharmaceutical compounds containing them and methods of their use.
    Type: Grant
    Filed: January 6, 2020
    Date of Patent: January 12, 2021
    Assignees: CORNELL UNIVERSITY, ITHACA COLLEGE
    Inventors: Richard Cerione, Kristin Cerione, Clint Stalnecker, Scott Ulrich
  • Patent number: 10889548
    Abstract: The invention provides therapeutic compositions that contain an inhibitor of dihydroorotate dehydrogenase (DHODH) and promote sustained elevation of dihydroorotate (DHO) levels in a patient. The compositions are useful for treating disorders associated with unregulated DHODH activity, such as acute myeloid leukemia. The invention also provides methods of determining therapeutically effective doses of compositions that contain a DHODH inhibitor. The invention further provides methods of synthesis of 2-(2?-halo-1-1?-biphenyl-4-yl)-quinoline carboxylic acids, which are useful as DHODH inhibitors.
    Type: Grant
    Filed: March 26, 2019
    Date of Patent: January 12, 2021
    Assignee: Clear Creek Bio, Inc.
    Inventors: Vikram S. Kumar, David P. Hesson, Ping Huang, Mo Jia, Xianjun You
  • Patent number: 10889562
    Abstract: Aspects of the present disclosure include prodrugs of compounds that activate Nrf2. Such prodrugs find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these prodrugs, methods of using these prodrugs in the treatment of various diseases and disorders, processes for preparing these prodrugs and intermediates useful in these processes.
    Type: Grant
    Filed: August 12, 2020
    Date of Patent: January 12, 2021
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Jiaxin Yu, Beth Fernandez, Gary Park, Ihab Darwish
  • Patent number: 10889556
    Abstract: There are provided inter alia metalloenzyme inhibitors, such as inhibitors of influenza A RNA dependent RNA polymerase PA subunit endonuclease, and methods of synthesis and use of the same.
    Type: Grant
    Filed: September 7, 2018
    Date of Patent: January 12, 2021
    Assignee: The Regents of the University of California
    Inventors: Seth M. Cohen, Cy V. Credille, David T. Puerta
  • Patent number: 10881653
    Abstract: There is provided compounds of formula (I), or pharmaceutically-acceptable salts thereof, wherein X, Y, Z, R1 and R2 have meanings provided in the description, which compounds are useful in the treatment of cancers.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: January 5, 2021
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Elias Set Jenö Arnér, William Chester Stafford, Nathan Patrick Coussens, Diane Karen Luci, David Joseph Maloney, Anton Simeonov, Ajit Jadhav, Thomas S. Dexheimer
  • Patent number: 10882856
    Abstract: Disclosed herein are 5 or 8-substituted imidazo [1, 5-a] pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo [1, 5-a] pyridines, processes for the preparation thereof and the use thereof in therapy. Disclosed herein are certain 5 or 8-substituted imidazo [1, 5-a] pyridines that can be useful for inhibiting indoleamine 2, 3-dioxygenase and/or tryptophane 2, 3-dioxygenase and for treating diseases or disorders mediated thereby.
    Type: Grant
    Filed: September 23, 2017
    Date of Patent: January 5, 2021
    Assignee: BEIGENE, LTD.
    Inventors: Hexiang Wang, Yunhang Guo, Bo Ren, Zhiwei Wang, Guoliang Zhang, Changyou Zhou
  • Patent number: 10874633
    Abstract: This disclosure provides methods and pharmaceutical compositions for reducing or eliminating cardiotoxicity, particularly cardiotoxicity induced by a cancer treatment or other therapy. In some cases, the methods and compositions prevent or reduce cardiotoxicity caused by anthracycline treatment. The methods provided herein often comprise administering a protective agent such as myricetin, tricetin, robinetin, ficetin, vitexin, quercetin, dihydrorobinetin, kaempferol, 7,3?,4?,5?-tetrahydroxyflavone, and myricitrin in conjunction with the administration of a cancer drug or other treatment. They may comprise administering a protective agent in combination with dexrazoxane. The compositions provided herein include co-formulations of a protective agent with a different protective agent or with a cancer treatment (e.g., anthracycline drug).
    Type: Grant
    Filed: January 8, 2020
    Date of Patent: December 29, 2020
    Assignees: Auransa Inc., SCT II LLC
    Inventors: Christopher G. Armstrong, Kevin J. Kim, Lisa Maria Lucia Pham, Eunhye Park, Zhong Zhong, Guanyi Huang, Joseph C. Wu, Sidney Paul Elmer, Viwat Visuthikraisee, Eithon Michael G. Cadag, Thomas Bernard Freeman, Pek Yee Lum
  • Patent number: 10875838
    Abstract: This application is directed to a compound of Formula II Also disclosed is a process for preparing a compound of Formula II comprising using the compounds of Formulae IV and V Also disclosed is a method for preparing a compound of Formula I comprising contacting a compound of Formula II with a compound of a compound of Formula VI wherein A1, A2 A3, R1, R2, R3a, R3b, R4, B1, B2 and B3, are as defined in the disclosure.
    Type: Grant
    Filed: March 16, 2018
    Date of Patent: December 29, 2020
    Assignee: FMC Corporation
    Inventors: Yuzhong Chen, Rafael Shapiro
  • Patent number: 10864201
    Abstract: The present invention encompasses compounds of the formula I which are suitable for the treatment of diseases related to Vanin, and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.
    Type: Grant
    Filed: August 26, 2019
    Date of Patent: December 15, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Cédrickx Godbout, Martin Thomas Fleck, Hannes Fiepko Koolman
  • Patent number: 10865200
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the specification, or a salt thereof.
    Type: Grant
    Filed: December 4, 2018
    Date of Patent: December 15, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masami Yamada, Shinkichi Suzuki, Takahiro Sugimoto, Minoru Nakamura, Hiroki Sakamoto, Makoto Kamata