Patents Examined by Timothy R Rozof
  • Patent number: 12221420
    Abstract: The invention provides a process for manufacturing 5-ethyl-4-methyl-N-[4-[(2S) morpholin-2-yl]phenyl]-1H-pyrazole-3-carboxamide (Formula I), or a pharmaceutically acceptable salt thereof, on an industrial scale, comprising a one-pot process for manufacturing 5-ethyl-4-methyl-1H-pyrazole-3-carboxylic acid (1).
    Type: Grant
    Filed: January 7, 2022
    Date of Patent: February 11, 2025
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Spurr, Rene Trussardi
  • Patent number: 12220408
    Abstract: The present disclosure provides methods for the acute treatment of migraine with or without aura, comprising the administration of ubrogepant. In particular, the present disclosure provides methods for the acute treatment of migraine in patients having hepatic impairment; in patients with renal impairment; and in patients concurrently taking CYP3A4 modulators or BCRP and/or P-gp only inhibitors.
    Type: Grant
    Filed: July 18, 2024
    Date of Patent: February 11, 2025
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Mary Ann Johnson, Leonardo R. Allain, W. Mark Eickhoff, Craig B. Ikeda, Chad D. Brown, Francis J. Flanagan, Jr., Rebecca Nofsinger, Melanie J. Marota, Lisa Lupton, Paresh B. Patel, Hanmi Xi, Wei Xu
  • Patent number: 12221425
    Abstract: This disclosure relates to an improved chemical process for making compounds which are CIC-1 chloride channel inhibitors.
    Type: Grant
    Filed: June 19, 2020
    Date of Patent: February 11, 2025
    Assignee: NMD PHARMA A/S
    Inventors: Nicholas Kelly, Michael John McKenzie
  • Patent number: 12221437
    Abstract: The invention relates to bispyranilidenes, dithiobispyranilidenes and diselenobispyranilidene according to formula (I), to the use thereof as light or IR-absorber and to an electronic or optoelectronic component containing at least one compound according to formula (I).
    Type: Grant
    Filed: May 14, 2020
    Date of Patent: February 11, 2025
    Assignee: SENORICS GMBH
    Inventors: Olaf Zeika, Christina Kaiser, Koen Vandewal, Bernhard Siegmund, Johannes Benduhn, Manuel Tropiano
  • Patent number: 12220411
    Abstract: Application of a PTGDS inhibitor in preparation of a drug for treating cataracts is provided. As an effective and selective PTGDS inhibitor, AT-56 competitively inhibits production of PGD2 by occupying a catalytic site of PTGDS. The PTGDS catalyzes synthesis of the PGD2 to cause an oxidative stress injury of human lens epithelial cells, thereby promoting occurrence and development of aging and opacity of a lens. By reducing apoptosis caused by the oxidative stress injury, a degree of the cataracts can be effectively reduced.
    Type: Grant
    Filed: October 8, 2023
    Date of Patent: February 11, 2025
    Assignee: THE EYE HOSPITAL OF WENZHOU MEDICAL UNIVERSITY
    Inventors: Jin Li, Jiasheng Liu, Yitong Xu, Mengchao Zhu, Haisen Sun
  • Patent number: 12215114
    Abstract: Processes for producing diazaspiro lactam compounds and intermediates useful in the processes.
    Type: Grant
    Filed: June 23, 2020
    Date of Patent: February 4, 2025
    Assignee: NAUREX INC.
    Inventors: Danny T. Dinh, William R. Perrault, Khalid Diker
  • Patent number: 12215110
    Abstract: Disclosed is a process for the preparation of certain intermediates, e.g. a process for preparing a compound of formula (I) wherein, R1, R2 and X1 are as defined in the description, and which intermediate and processes are useful in the preparation of a BTK inhibitor, such as ibrutinib.
    Type: Grant
    Filed: May 20, 2020
    Date of Patent: February 4, 2025
    Assignee: Janssen Pharmaceutica NV
    Inventors: Philip James Pye, Andras Horvath, Cheng Yi Chen, Yuanyuan Yuan, Jinxiong Su, Shuo Wang, Simon Albert Wagschal
  • Patent number: 12215064
    Abstract: The present invention relates to compounds of general formula (I), wherein —X is selected from a group consisting of H; C1 to C6, alkyl; halogen (F, Cl, Br or I); Y is selected from a group consisting of nitrogen; N-oxide; Z1, Z2, Zm, wherein m is 1 or 2, are independently selected from the group consisting of —CH2—CH2— and —CH2—CH2—CH2; A, Am, wherein m is 1 or 2, are independently selected from H; —CH2COOH; —CH2C(O)NH2; —CH2P(O)(OH)2, and n is 1 or 2; R1, R2, R3 are independently H; C1 to C6, alkyl; C1 to C6 alkyloxy; C6 to C10 aryloxy; benzyloxy; C1 to C6 alkylthio; C6, to C10 arylthio; F; Cl; Br; I; OH; SH; NH2; C1 to C6, alkylamino; di(C1 to C6, alkyl)amino; C1 to C6 acylamino; di(C1 to C6 acyl) amino; C6 to C10 arylamino; di(C6 to C10 aryl)amino; CN; OH; nitro; COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is independently H or C1 to C10 alkyl or C6, to C10 aryl; and/or neighboring two of R1, R2, R3 together with neighboring two carbon atoms of the aromatic cycle form a six-membered ring, optionally subst
    Type: Grant
    Filed: May 28, 2020
    Date of Patent: February 4, 2025
    Assignee: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.
    Inventor: Miloslav Polasek
  • Patent number: 12202827
    Abstract: The present invention relates to a compound selected from (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine and a pharmaceutically acceptable salt thereof, and in particular to the phosphate salt of (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine, both having preferably an enantiomeric excess of the (R) form higher than or equal to 97%. Furthermore, the present invention relates to pharmaceutical compositions comprising the same, their use as a medicament and in methods of treatment of diseases and disorders in humans including women of child bearing potential and pediatric patients in which aldosterone over-exposure contributes to the deleterious effects of said diseases or disorders, as well as processes for preparing said inventive compounds.
    Type: Grant
    Filed: August 9, 2022
    Date of Patent: January 21, 2025
    Assignee: DAMIAN PHARMA AG
    Inventors: Christoph Schumacher, Walter Fuhrer, Ronald Edward Steele
  • Patent number: 12202803
    Abstract: Compounds capable of, or usable in, inducing death of cancer cells and/or modulating a biological activity of a chemokine e.g., cell migration, and/or treating diseases and disorders associated with a biological activity of a chemokine and/or cell migration, and/or in treating cancer, are provided herein. The compounds are collectively represented by Formulae Ia or Ib: wherein A, B, D, E, G and R1-R5 are as defined in the specification, with one or more of D, E and G, preferably E, is hydroxy.
    Type: Grant
    Filed: September 19, 2023
    Date of Patent: January 21, 2025
    Assignee: AlonBio Ltd.
    Inventors: Amnon Peled, Michal Abraham Karni, Orly Eizenberg
  • Patent number: 12202830
    Abstract: Provided is, for example, a method for producing a morphinan derivative represented by General Formula (II), including the step of: allowing metal sodium and ethylenediamine to act on a morphinan derivative represented by General Formula (I) in presence of an auxiliary solvent. wherein R1 represents a hydrogen atom, or a C1-10 alkyl group, a C3-6 cycloalkyl group, a C2-6 alkenyl group, a C6-10 aryl group, or a heteroaryl group optionally having a substituent, R2 represents an amino protecting group, R3 represents a methoxy group, R4 and R5 represent a hydrogen atom or a hydroxy group, R6 and R7 represent a hydrogen atom or an electron-donating group, wherein R6 and R7 are not simultaneously a hydrogen atom, and X represents O or CH2.
    Type: Grant
    Filed: July 17, 2020
    Date of Patent: January 21, 2025
    Assignee: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Daisuke Saito, Kohei Hayashida
  • Patent number: 12202821
    Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as herbicides.
    Type: Grant
    Filed: May 21, 2020
    Date of Patent: January 21, 2025
    Assignee: SYNGENTA CROP PROTECTION AG
    Inventors: William Guy Whittingham, John Williams, Christopher John Mathews
  • Patent number: 12194030
    Abstract: The present disclosure provides methods for the acute treatment of migraine with or without aura, comprising the administration of ubrogepant. In particular, the present disclosure provides methods for the acute treatment of migraine in patients having hepatic impairment; in patients with renal impairment; and in patients concurrently taking CYP3A4 modulators or BCRP and/or P-gp only inhibitors.
    Type: Grant
    Filed: March 1, 2024
    Date of Patent: January 14, 2025
    Assignee: Allergan Pharmaceuticals International Limited
    Inventors: Joel M. Trugman, Ramesh Boinpally, Abhijeet Jakate, Michelle Finnegan
  • Patent number: 12195476
    Abstract: Provided is a method for synthesizing a compound 2-[(2R,5S)-5-[2-[(R)-1-hydroxyethyl]furo[3,2-b]imidazo[4,5-d]pyridin-1-yl]tetrahydropyran-2-yl]acetonitrile as a selective JAK1/TYK2 kinase inhibitor. The compound is prepared by nucleophilic substitution, palladium on carbon reduction, and cyclization reaction using 7-chloro-6-nitrofuro[3,2-b]pyridine as a starting material. The synthesis method has mild reaction conditions, high product yield, and high purity, and is suitable for industrial production. Further provided are a crystal form of the compound, crystal forma of its salts, and their preparation methods. The crystal form of the compound and the crystal forms of its salts have good physical and chemical properties and are suitable for drug development.
    Type: Grant
    Filed: April 30, 2020
    Date of Patent: January 14, 2025
    Assignee: HANGZHOU HIGHLIGHTLL PHARMACEUTICAL CO., LTD.
    Inventors: Congxin Liang, Laibao Wang, Haihui Liu
  • Patent number: 12195474
    Abstract: A preparation method of zaleplon is provided and belongs to the technical field of pharmaceutical chemistry. The preparation method adopts simple and cheap m-nitrobenzaldehyde and triethylamine as raw materials, and constructs a core structure of zaleplon with high efficiency and high selectivity through a one-pot series reaction without transition metal catalysis, thereby avoiding the formation of isomers, reducing the generation of by-products, increasing the yield of target products and reducing the synthesis cost; and after simple nitro reduction modification, zaleplon is prepared. The method has the advantages of short preparation route, mild reaction conditions and simple operation, so the method is suitable for industrial production.
    Type: Grant
    Filed: January 5, 2022
    Date of Patent: January 14, 2025
    Assignees: Xinxiang Medical College, Anhui University of Technology
    Inventors: Qinghe Gao, Xinya Han, Yongtao Xu, Yingchao Duan, Jieli Lv, Lizhen Fang, Yan Zhang, Jufen Yan, Yingying Li
  • Patent number: 12187663
    Abstract: The invention concerns a compound of Formula (I) or a salt thereof, wherein R1 is H, (C1-C3)alkyl or CF3; R2 is H, (C1-C3)alkyl or CF3; A is CH2COOH, XCH2COOCH2CH3, XCH2COOH, XCH2CH2NH2, where X is nitrogen or oxygen atom; Ar is an aromatic fragment selected from the group consisting of (Ar1), (Ar2) and (Ar3); where R3 is H, —CH3, —CH2CH3 or CH3CO—, R4 is H or —CH3, R5 is H or —CH3, and R6 is H or —CH3. The compounds of Formula (I) can be used in the treatment of diseases modulated by thyroid hormone receptor-beta (TRb or TR?).
    Type: Grant
    Filed: March 10, 2020
    Date of Patent: January 7, 2025
    Assignee: INTERNATIONAL SOCIETY FOR DRUG DEVELOPMENT S.R.L.
    Inventors: Guido Puricelli, Simona Rapposelli, Grazia Chiellini, Amedeo Columbano, Andrea Perra, Massimiliano Runfola, Sheraz Gul
  • Patent number: 12187712
    Abstract: Provided are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, Y1, Y2, L1, and G1 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 25, 2019
    Date of Patent: January 7, 2025
    Assignee: CYTOKINETICS, INC.
    Inventors: Bradley P. Morgan, Mark Vanderwal, Chihyuan Chuang
  • Patent number: 12187723
    Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: May 7, 2020
    Date of Patent: January 7, 2025
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, Laxman Pasunoori, Sreekantha Ratna Kumar, Srinivasan Kunchithapatham Duraisamy, Pitani Veera Venkata Srinivas, Vikram Bhogadi, Subramanya Hegde
  • Patent number: 12187694
    Abstract: Provided herein are inhibitors of SLC26A3, which is an anion (Cl?, HCO3?, oxalate) exchanger expressed in intestinal epithelial cells. SLC26A3 inhibitors have potential utility for treatment of constipation including chronic idiopathic constipation (CIC), opioid-induced constipation (OIC), constipation-predominant irritable bowel syndrome (IBS-C), cystic fibrosis-associated constipation, meconium ileus, distal intestinal obstruction syndrome, calcium oxalate kidney stone disease, enteric hyperoxaluria and primary hyperoxalurias.
    Type: Grant
    Filed: January 18, 2023
    Date of Patent: January 7, 2025
    Assignee: The Regents of the University of California
    Inventors: Alan S. Verkman, Onur Cil, Peter M. Haggie
  • Patent number: 12180194
    Abstract: The present invention relates to a multi-aziridine compound having: a) from 2 to 6 of the following structural units (A): whereby R?, R?, R1, R2, R3 and R4 are as defined herein m is an integer from 1 to 6; b) one or more linking chains wherein each one of these linking chains links two of the structural units A; and c) a molecular weight in the range from 600 Daltons to 5000 Daltons. The multi-aziridine compound can be used for example for crosslinking of for example carboxylic acid functional polymers dissolved and/or dispersed in an aqueous medium.
    Type: Grant
    Filed: December 1, 2023
    Date of Patent: December 31, 2024
    Assignee: Covestro (Netherlands) B.V.
    Inventors: Gerardus Cornelis Overbeek, Patrick Johannes Maria Stals, Daan Van Der Zwaag, Alfred Jean Paul Bückmann