Patents Examined by Laura L. Stockton
  • 4,5,6-trisubstituted indazole derivatives, and preparation method and pharmaceutical use thereof
    Patent number: 11104664
    Abstract: Provided are 4,5,6-tri-substituted indazoles derivatives, a preparation method therefor, and a use thereof in medicines. Specifically, provided are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates, or prodrugs thereof, a preparation method therefor, and a use thereof.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: August 31, 2021
    Inventors: Jianbiao Peng, Yang Liu, Lixiao Wang, Zhihua Fang, Zonglei Fei, Xi Chen, Jiong Lan
  • Pyrazole derivative
    Patent number: 11104648
    Abstract: A pyrazole derivative having the following formula stru-1: The pyrazole derivative is used for prevention and control of pests.
    Type: Grant
    Filed: May 22, 2018
    Date of Patent: August 31, 2021
    Assignees: ZHEJIANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., SINOCHEM LANTIAN CO., LTD.
    Inventors: Tianming Xu, Jiahua Xing, Liangkun Zhong, Dongsong Hu, Youchang Wei, Hongying Huang, Jiping Yu, Weili Peng
  • Dimers of covalent NFKB inhibitors
    Patent number: 11104684
    Abstract: Provided herein are compounds and methods for modulating the NF?B pathway. More particularly, provided are inhibitors of the NF?B pathway and the uses of such inhibitors in regulating diseases and disorders, e.g., to treat cancer, autoimmune diseases, inflammatory diseases, diabetes, cardiovascular diseases, or neurological diseases.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: August 31, 2021
    Assignee: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA
    Inventors: Amarnath Natarajan, Sandeep Rana
  • Ku inhibitors and their use
    Patent number: 11098033
    Abstract: The present disclosure relates to certain compounds having binding affinity for Ku, and uses thereof. Specifically, the present disclosure relates to the use of Ku inhibitors as described herein in site-specific genome engineering technologies, including but not limited to CRISPR/Cas9, Zinc finger nuclease (ZFN), Transcription activator-like effector nuclease (TALEN), and meganuclease. The present disclosure also relates to kits useful for site-specific genome engineering that include at least one compound as described herein.
    Type: Grant
    Filed: May 24, 2017
    Date of Patent: August 24, 2021
    Assignee: Indiana University Research and Technology Corporation
    Inventors: John J Turchi, Navnath Gavande, Pamela S. Vandervere-Carozza
  • Amine prodrugs of pharmaceutical compounds
    Patent number: 11083711
    Abstract: Disclose are amine prodrugs and methods of synthesis thereof. In particular, the amine prodrug comprises a drug molecule and at least one or more prodrug appendage moieties and the method for synthesis the amine prodrug comprises a step of coupling the drug molecule and at least one or more prodrug appendage moieties. Also disclosed are exemplary riluzole prodrugs and methods of synthesis thereof.
    Type: Grant
    Filed: August 19, 2019
    Date of Patent: August 10, 2021
    Assignee: Biohaven Therapeutics Ltd.
    Inventor: Anthony Marfat
  • Prodrugs of fumarates and their use in treating various diseases
    Patent number: 11083703
    Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
    Type: Grant
    Filed: February 14, 2020
    Date of Patent: August 10, 2021
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Deuterated benzimidazole compound and medical use thereof
    Patent number: 11066372
    Abstract: The present invention relates to a medicament for treating or preventing a disease involving Na channel, for example, neuropathic pain, nociceptive pain, inflammatory pain, small-fiber neuropathy, erythromelalgia, paroxysmal extreme pain disorder, dysuria, or multiple sclerosis, comprising a compound of formula (I) wherein R1a, R1b, R1c, and R1d are hydrogen, halogen, cyano, C1-4 alkyl, C1-4 alkoxy, etc., provided that at least one of R1a, R1b, R1c and R1d is the above C6-10 aryl, C6-10 aryloxy, etc., R2 and R3 are hydrogen, C1-6 alkyl, C3-10 cycloalkyl, etc., R4 is hydrogen, C1-6 alkyl, C3-7 cycloalkyl, etc., m is 0, 1, or 2, L is CR7R8, R7 and R8 are hydrogen, hydroxy group, C1-4 alkyl, C1-4 alkoxy, etc., or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 14, 2018
    Date of Patent: July 20, 2021
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Toshio Kanai, Kohei Iwamoto
  • Substituted cyanopyrrolidines with activity as DUB inhibitors
    Patent number: 11059809
    Abstract: The present invention relates to a class of substituted-cyanopyrrolidines of formula (Ia), (Ib), and (Ic), with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30), having utility in a variety of therapeutic areas including cancer and conditions involving mitochondrial dysfunction (Ia).
    Type: Grant
    Filed: June 19, 2018
    Date of Patent: July 13, 2021
    Assignee: MISSION THERAPEUTICS LIMITED
    Inventors: Martin Lee Stockley, Mark Ian Kemp
  • Compound and method for producing same
    Patent number: 11046655
    Abstract: A compound represented by the formula (1) is provided: wherein A1 represents an oxygen atom, a sulfur atom, —NR5— or —PR5—; at least one A1 is —NR5— or —PR5—; R1 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an alkoxy group, a cycloalkoxy group, an aryloxy group, an alkylsulfenyl group, a cycloalkylsulfenyl group, an arylsulfenyl group or a disubstituted amino group; R2 and R3 represent an alkyl group, a cycloalkyl group, an aryl group, an alkoxy group, a cycloalkoxy group, an aryloxy group, an alkylsulfenyl group, a cycloalkylsulfenyl group, an arylsulfenyl group, a monovalent heterocyclic group, a halogen atom or a disubstituted amino group; R4 represents a hydrogen atom, —C(R6)3, —OR7, —N(R7)2 or —Si(R7)3; m represents an integer of 0 to 3; and n represents an integer of 0 to 4.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: June 29, 2021
    Assignees: SUMITOMO CHEMICAL COMPANY, LIMITED, CAMBRIDGE DISPLAY TECHNOLOGY LIMITED
    Inventors: Satoshi Kobayashi, Takayuki Iijima, Nobuhiko Akino, Sheena Zuberi
  • Derivatives of porphyrins, their process of preparation and their use for treating viral infections
    Patent number: 11046704
    Abstract: The present invention concerns metallated porphyrin derivatives as ligands of G-quadruplex and their novel use as anti-viral agents.
    Type: Grant
    Filed: January 14, 2020
    Date of Patent: June 29, 2021
    Assignees: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITÉDE BORDEAUX
    Inventors: Samir Amrane, Marie-Aline Andreola, Geneviève Pratviel, Jean-Louis Mergny
  • Benzimidazole-proline derivatives
    Patent number: 11040966
    Abstract: The present invention relates to compounds of the formula (II) wherein Ar1, R1, R2, R3, R4a, R4b and (R5)n are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (II), and especially to their use as orexin receptor antagonists.
    Type: Grant
    Filed: May 7, 2019
    Date of Patent: June 22, 2021
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Christoph Boss, Christine Brotschi, Markus Gude, Bibia Heidmann, Thierry Sifferlen, Jodi Williams
  • Isoxazole analogs as FXR agonists and methods of use thereof
    Patent number: 11034684
    Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.
    Type: Grant
    Filed: September 13, 2019
    Date of Patent: June 15, 2021
    Assignee: ENANTA PHARMACEUTICALS, INC.
    Inventors: Jun Ma, Guoqiang Wang, Bin Wang, Xuechao Xing, Ruichao Shen, Jing He, Yat Sun Or
  • Anti-inflammatory and antitumor 2-oxothiazoles and 2-oxothiophenes compounds
    Patent number: 11034666
    Abstract: A compound of formula (I) wherein X is O, C?O or S; Y is N or CH; R2 and R4 are each independently H, —(CH2)pCOOH, —(CH2)pCON(R5)2 or —(CH2)pCOOC1-6alkyl; or R2 and R4 together form a 6-membered phenyl ring fused to the five membered ring; each R1 is independently selected from H, halo (e.g. fluoro or chloro), C6-10aryl, C7-12arylalkyl, C2-12 alkenyl; OC1-12 alkyl, OC2-12 alkenyl or a C1-12 alkyl group; each R5 is H or C1-6 alkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g. a salt thereof.
    Type: Grant
    Filed: October 25, 2019
    Date of Patent: June 15, 2021
    Assignee: Avexxin AS
    Inventors: Berit Johansen, Marcel Sandberg, Inger-Reidun Aukrust, George Kokotos, Efrosini Barbayianni
  • 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives as dihydroorotate oxygenase inhibitors
    Patent number: 11028054
    Abstract: The present invention provides 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives as dihydroorotate oxygenase inhibitor compounds of formula (I), which may be therapeutically useful as DHODH inhibitors, in which R1 to R3 and ‘m’ have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomer thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting DHODH. The present invention also provides methods for synthesizing 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives of formula (I). The present invention also provides pharmaceutical formulations comprising at least one of the DHODH inhibitor compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.
    Type: Grant
    Filed: February 23, 2018
    Date of Patent: June 8, 2021
    Assignee: Merck Patent GmbH
    Inventors: Siva Sanjeeva Rao Thunuguntla, Subramanya Hosahalli, Sunil Kumar Panigrahi, Matthias Schwarz, Michael Arit
  • Butylphthalide-telmisartan hybrids, preparation method and application thereof
    Patent number: 11028073
    Abstract: The invention discloses a butylphthalide-telmisartan heterocomplex, a preparation method and an application thereof. The invention specifically relates to an optically active ring-opening butylphthalide-telmisartan heterocomplex shown in formula I or a pharmaceutically acceptable salt or ester thereof, a preparation method thereof, a pharmaceutical composition containing the compounds, and a pharmaceutical application thereof, particularly application in prevention and treatment of neuroinflammation-related diseases, including ischemic stroke, Alzheimer's disease, brain trauma, Parkinson's disease, multiple sclerosis, depression and so on.
    Type: Grant
    Filed: January 4, 2018
    Date of Patent: June 8, 2021
    Assignee: GUANGDONG LONGFU MEDICINE CO., LTD.
    Inventors: Zhangjian Huang, Tao Pang, Cunfang Wang, Wenbin Zeng, Jinxiang Deng, Weijie Wu, Tingyu Huang
  • 2,6-disubstituted-9-cyclopentyl-9H-purines, use thereof as medicaments, and pharmaceutical compositions
    Patent number: 11028087
    Abstract: The present invention relates to novel 2,6-disubstituted-9-cyclopentyl-9H-purines of general formula I, capable of inhibiting the activity of kinases such as FLT3, CDKs and PDGFRs in cancer and other related proliferative diseases. The invention further includes pharmaceutical compositions containing the 2,6-disubstituted-9-cyclopentyl-9H-purines. Compounds of the present invention can be used as active ingredients of a pharmaceutical compositions for treating acute myeloid leukemia (AML).
    Type: Grant
    Filed: March 19, 2018
    Date of Patent: June 8, 2021
    Assignee: UNIVERZITA PALACKEHO V OLOMOUCI
    Inventors: Tomas Gucky, Eva Reznickova, Radek Jorda, Vladimir Krystof, Miroslav Strnad, Tereza Radosova Muchova, Vladimir Divoky
  • Spiro-lactam and bis-spiro-lactam NMDA receptor modulators and uses thereof
    Patent number: 11028095
    Abstract: Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: August 1, 2017
    Date of Patent: June 8, 2021
    Assignee: Aptinyx Inc.
    Inventor: M. Amin Khan
  • Compounds for treating proliferative diseases
    Patent number: 11028055
    Abstract: The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating and/or preventing proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: June 8, 2021
    Assignees: Children's Medical Center Corporation, Beth Israel Deaconess Medical Center, Inc.
    Inventors: Bruce R. Zetter, Lijun Sun
  • IRE1 small molecule inhibitors
    Patent number: 11021466
    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: August 16, 2019
    Date of Patent: June 1, 2021
    Assignee: Cornell University
    Inventors: Joseph P. Vacca, Dansu Li, Sarah Bettigole
  • Azetidine derivative
    Patent number: 11014943
    Abstract: Disclosed in the present application are a compound represented by formula (I), or a pharmaceutically acceptable salt, a tautomer thereof, a stereoisomer thereof, or a geometrical isomer thereof, and uses thereof in the preparation of drugs for treating or preventing multiple myeloma.
    Type: Grant
    Filed: February 28, 2018
    Date of Patent: May 25, 2021
    Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP GO., LTD.
    Inventors: Jian Xiong, Cheng Xie, Kevin X Chen, Xiongbin Xu, Xuejin Zhang, Zhen Gong, Jian Li, Shuhui Chen, Aiming Zhang, Zhulian Jiang, Xiquan Zhang, Xin Tian