Patents Examined by Brian E McDowell
  • Patent number: 11325895
    Abstract: Provided are type I, III, V and VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl)urea which are useful as bulk pharmaceutical crystals. Also provided are type I, III, V and VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl)urea having excellent TrkA inhibitory effect, medicines and medicinal composition containing these crystals, and a method for producing these crystals.
    Type: Grant
    Filed: September 13, 2018
    Date of Patent: May 10, 2022
    Inventors: Yuji Kawada, Fumihiko Saitoh, Hiroshi Nagasue, Tsutomu Satoh
  • Patent number: 11312724
    Abstract: The present disclosure provides compounds represented by Formula I: wherein R3, A, A1, A2, A3, E, E1, E2, L, Q, Z, and are as defined in the specification, and the pharmaceutically acceptable salts and solvates thereof. Compounds of Formula I are KRAS inhibitors and are thus useful to treat cancer and other diseases.
    Type: Grant
    Filed: March 12, 2021
    Date of Patent: April 26, 2022
    Inventors: Chao Li, Guozhi Tang, Jianyong Chen, Lingling Jiao, Liugen Li
  • Patent number: 11312704
    Abstract: The disclosure provides compounds, such as compounds of Formula II, with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease.
    Type: Grant
    Filed: July 23, 2021
    Date of Patent: April 26, 2022
    Assignee: Pardes Biosciences, Inc.
    Inventors: Lee D. Arnold, Andy Jennings, Walter Keung
  • Patent number: 11311506
    Abstract: Compositions and methods for using cyclopropanated structural analogs of fatty acid biofilm dispersal agents are characterized by superior biofilm dispersion. When used in combination with antimicrobials, these analogs decrease the minimum inhibitory concentration of antimicrobial agents required for eradication of the biofilm and/or treatment of infection. Methods for using these analogs include direct application to a surface, blending with lipid based carriers, or covalent anchoring the molecule to a surface. Typically, the cyclopropanated structural analog has the structure according to formula (I): wherein R1 is a C1-C24 linear or branched alkyl group; or an acid halide or acid anhydride thereof.
    Type: Grant
    Filed: October 31, 2019
    Date of Patent: April 26, 2022
    Inventors: Jessica Amber Jennings, Daniel Lee Baker, Rukhsana Awais, Zoe Harrison, Babatunde Raji
  • Patent number: 11306085
    Abstract: The present invention relates to a method for preparing a pyrimidone heteroaryl derivative and an intermediate of the pyrimidone heteroaryl derivative. Specifically, the pyrimidone heteroaryl derivative of the formula is prepared by changing a starting raw material and an intermediate.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: April 19, 2022
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Junlei Jia, Bing Liu, Xiaohui Gao
  • Patent number: 11292785
    Abstract: Related is a nitrogen-containing benzoheterocycle compound containing a carboxylic acid group as shown in general formula (I), or a stereoisomer or pharmaceutically acceptable salt thereof. The compound has excellent pharmacokinetic properties and extremely remarkable liver targeting properties, and a pharmaceutical composition comprising the same may be used as a CCR antagonist, in particular a CCR2 and/or CCR5 antagonist and can be used in mediated disease, including, but not limited to, nonalcoholic fatty liver disease (NAFLD) or the like.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: April 5, 2022
    Assignee: Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.
    Inventors: Shuai Song, Qiang Tian, Yongyong Wu, Mingliang Zhao, Chaolei Wang, Jiaqiang Cai, Lichun Wang, Jingyi Wang
  • Patent number: 11292716
    Abstract: The present invention discloses a process for the photocatalytic splitting of water using self-assembled metalloporphyrin 2D-sheet of formula (I) to form hydrogen and oxygen.
    Type: Grant
    Filed: April 21, 2020
    Date of Patent: April 5, 2022
    Inventors: Santosh Babu Sukumaran, Ranjeesh Karayamkodath Chandran
  • Patent number: 11286243
    Abstract: The subject matter described herein is directed to Ferroportin inhibitor compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis. The compounds of Formula I and pharmaceutical salts thereof have the following structure: wherein R1, R2, R3, X1, X2, X3, X4, Y1, Y2, and Y3 are as described herein.
    Type: Grant
    Filed: December 12, 2019
    Date of Patent: March 29, 2022
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Qing Xu, Brian Walter Metcalf, Calvin Wesley Yee, Peter Michael Rademacher, Carsten Alt
  • Patent number: 11286248
    Abstract: Disclosed are a compound as shown in formula (I), and an isomer thereof or a pharmaceutically acceptable salt thereof, and involved is the use thereof in the preparation of drugs for treating FGFR-associated diseases.
    Type: Grant
    Filed: February 2, 2019
    Date of Patent: March 29, 2022
    Inventors: Yang Zhang, Zhifei Fu, Miaorong Luo, Zaifang Ren, Dongjie Hu, Jie Li, Jian Li, Shuhui Chen
  • Patent number: 11285135
    Abstract: Provided herein are methods of treating cancer with KRAS G12C inhibitors of Formula I and compositions of the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
    Type: Grant
    Filed: November 5, 2019
    Date of Patent: March 29, 2022
    Assignee: AMGEN INC.
    Inventors: Brian Alan Lanman, Victor J. Cee, Alexander J. Pickrell, Anthony B. Reed, Kevin C. Yang, David John Kopecky, Hui-Ling Wang, Patricia Lopez, Kate Ashton, Shon Booker, Christopher M. Tegley
  • Patent number: 11279688
    Abstract: Described herein are compounds that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Grant
    Filed: January 29, 2020
    Date of Patent: March 22, 2022
    Inventors: Jason D. Brubaker, Joseph L. Kim, Kevin J. Wilson, Douglas Wilson, Lucian V. DiPietro
  • Patent number: 11274106
    Abstract: Herein is described the conversion of deoxynybomycin (DNM), a natural product and DNA gyrase inhibitor with minimal cytotoxicity, into a compound (Formula I) that has anticancer activity. Detailed in vitro and cell culture experiments demonstrate that these compounds inhibit Top2 and also act upon topoisomerase I. Similar approaches are applicable to other classes of gyrase inhibitors and other antibacterial targets for discovery of new anticancer drugs.
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: March 15, 2022
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Andrew P. Riley
  • Patent number: 11266754
    Abstract: Disclosed are chelates resulting from the complexation of bifunctional do2pa derivatives ligands of formula (I), wherein the substituents R1, R1?, R2, R2?, R3, R3?, L1, L1?, L2 and L2? are defined as in the claims, with metallic cations, especially Pb(II) and Bi(III). Also disclosed are bifunctional do2pa derivatives ligands of formula (I), as well as the use of chelates in nuclear medicine and the use of ligands in cations detection or epuration of effluents.
    Type: Grant
    Filed: September 23, 2019
    Date of Patent: March 8, 2022
    Inventors: Fatima Oukhatar, Maryline Beyler, Raphaël Tripier
  • Patent number: 11267802
    Abstract: Provided are a 2, 4-di-(nitrogen containing group) substituted pyrimidine compound represented by a general formula (I), a pharmaceutically acceptable salt and a stereoisomer thereof, a preparation method thereof, and a use thereof in preparation of anti-tumor drugs. The compound having a structural feature shown in the general formula (I) can selectively suppress activity of mutant epidermal growth factor receptors (EGFR), including single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. The compound has a weak suppression effect on wild-type EFGR and a very high selectivity, and thus it has a potential to be used in preparation of drugs for treating EGFR mutant tumors, especially non-small cell lung cancer (NSCLC) comprising a T790M EGFR mutation.
    Type: Grant
    Filed: July 26, 2016
    Date of Patent: March 8, 2022
    Assignee: BEBETTER MED INC.
    Inventors: Xiong Cai, Changgeng Qian, Yunwo Weng, Bin Liu, Yanyan Wang, Mingsheng Lin, Junqi Li, Yuanhui Qing, Huajin You, Shiqing Zhou, Weicai Xue
  • Patent number: 11261193
    Abstract: This invention provides an unexpectedly stable, highly crystalline form of the di-HCl salt of for advantageous therapeutic pharmaceutical efficacy and dosage form stability.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: March 1, 2022
    Assignee: GI Therapeutics, Inc.
    Inventors: Alexander Smith, Hannah S. White, Patricia Andres, Xufeng Sun, Lei Zhu, Petinka I. Vlahova
  • Patent number: 11261185
    Abstract: Compounds of the formula Ia or of the formula Ib in which X, Y, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases such as cancer.
    Type: Grant
    Filed: September 17, 2020
    Date of Patent: March 1, 2022
    Assignee: Merck Patent GmbH
    Inventor: Hans-Peter Buchstaller
  • Patent number: 11261186
    Abstract: Compounds having the chemical formula 1, a method for producing the compounds of chemical formula 1, a pharmaceutical composition comprising same, and use thereof as a GPR120 agonist for prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
    Type: Grant
    Filed: December 23, 2015
    Date of Patent: March 1, 2022
    Assignee: LG CHEM. LTD.
    Inventors: Young Kwan Kim, Sang Yun Park, Hyun Woo Joo, Eun Sil Choi, Seung Yup Paek, Seung Wan Kang, Byung Gyu Kim, Chang Seok Lee, Sung Wook Kim, Sang Dae Lee
  • Patent number: 11261152
    Abstract: The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: March 1, 2022
    Assignees: The Regents of the University of California, The United States Government as Represented by the Department of Veterans Affairs
    Inventors: Matthew Rettig, Michael E. Jung, D. Elshan Nakath G. Ralalage, Jiabin An
  • Patent number: 11253613
    Abstract: Compounds, systems, and methods are provided for the design and assembly of a non-invasive, analyte sensing dressing that includes a sensor and a matrix. The sensor is capable of detecting analytes such as molecular oxygen. The matrix is at least partially permeable to the analyte. In one version of the dressing, the sensor includes a meso-unsubstituted metallated porphyrin that is sensitive towards oxygen. The metallated porphyrin can be excited when illuminated at a first wavelength, followed by emission of phosphorescence at a second wavelength whose intensity can be used as an indicator for oxygen concentration. The metallated porphyrin can be prepared from a phosphorescent meso-unsubstituted porphyrin having the Formula (I): wherein M is a metal, wherein each R is independently an atom or a group of atoms, and wherein at least one R is —O(C)OR?, wherein R? is optionally substituted alkyl.
    Type: Grant
    Filed: February 11, 2020
    Date of Patent: February 22, 2022
    Assignee: The General Hospital Corporation
    Inventors: Conor L. Evans, Gabriela Apiou, Alexander J. Nichols, Emmanouil Rousakis, Zongxi Li
  • Patent number: 11248001
    Abstract: The invention relates to novel heteroaryl compounds of Formula (I) and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cardiovascular diseases, and methods treating sepsis or septic shock, using the novel heterocyclic compounds disclosed herein.
    Type: Grant
    Filed: January 16, 2020
    Date of Patent: February 15, 2022
    Assignee: AstraZeneca AB
    Inventors: Michael H. Serrano-Wu, Mark Chambers, Erica Goldsmith, Jason Tierney, Karamjit Jandu, David Clark, Paul Hinchliffe