Patents Examined by Timothy R Rozof
  • Crystalline forms and compositions of CFTR modulators
    Patent number: 11155533
    Abstract: Crystalline Forms of Compound I: and pharmaceutically acceptable salts thereof are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.
    Type: Grant
    Filed: March 25, 2020
    Date of Patent: October 26, 2021
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Varsha Dhamankar, Kirk Raymond Dinehart, Eleni Dokou, Lori Ann Ferris, Nishanth Gopinathan, Katie McCarty, Catherine Metzler, Beili Zhang, Samuel Moskowitz, Sarah Robertson, David Waltz, Eric L. Haseltine, Weichao George Chen
  • Method of preparing 5R-[(benzyloxy) amino] piperidine-2S-carboxylic acid or a derivative thereof
    Patent number: 11142499
    Abstract: The present application relates to methods of preparing 5R-[(benzyloxy) amino] piperidine-2S-carboxylic acid or its derivatives in an environment-friendly way. The method uses L-glutamic acid as a starting material, which is first subjected to esterification reaction in the presence of an acidic reagent, and then reacted successively with 2-haloacetate and N-protecting agent, or with N-protecting agent and 2-haloacetate under a basic condition to obtain compound IV; then, the obtained compound IV is subjected to intramolecular condensation into a ring under the action of a strong base to obtain N-protecting group piperidine-5-one-2S-carboxylate (V).
    Type: Grant
    Filed: March 6, 2018
    Date of Patent: October 12, 2021
    Assignee: XINFA PHARMACEUTICAL CO., LTD
    Inventors: Yuxin Qi, Xinfa Li, Xin Xu, Baolin Wang, Hu Qu, Shungen Xie
  • Antidepressant compound and preparation method and application thereof
    Patent number: 11142543
    Abstract: An antidepressant steroid compound and a preparation method and an application thereof; the structure of said compound is shown in formula (I), and the definition of each substituent is as described in the description and claims. Compound of the present invention may be used in the prevention, treatment, therapy or alleviation of a plurality of diseases and conditions such as depression.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: October 12, 2021
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Chenggang Huang, Yang Li, Hualiang Jiang, Yang Xie, Fei Guo, Zhixiong Li, Mingcang Chen, Mingyue Zheng, Zhaolin Sun, Yu Gao, Xiaoting Tian, Pei Hu, Bing Zhang
  • Compounds useful in inhibiting human trefoil factor 3
    Patent number: 11141402
    Abstract: Disclosed herein are compounds of Formula I, wherein A, R1 to R6, and x to z have the meanings given in the description.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: October 12, 2021
    Assignees: National University of Singapore, University of Mysore, Bangalore University
    Inventors: Peter Edward Lobie, Vijay Kumar Pandey, Rangappa Kanchugarakoppal Subbegowda, Basappa, Mohan Chakrabhavi Dhananjaya, Shobith Rangappa
  • Spirocycle compounds and methods of making and using same
    Patent number: 11142526
    Abstract: Provided herein are compounds and compositions useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
    Type: Grant
    Filed: August 28, 2018
    Date of Patent: October 12, 2021
    Assignee: H. LUNDBECK A/S
    Inventors: Cheryl A. Grice, Olivia D. Weber, Daniel J. Buzard, Michael B. Shaghafi, Todd K. Jones
  • Rhodamine dyes and conjugates
    Patent number: 11130865
    Abstract: The present invention relates generally to novel rhodamine dyes which upon conjugation with another molecule form single isomeric conjugation products. These novel rhodamine dyes contain only one single functional group on the rhodomine molecule for conjugation so that their conjugation products are single isomeric conjugation products.
    Type: Grant
    Filed: December 6, 2019
    Date of Patent: September 28, 2021
    Assignee: PHARMACOPHOTONICS, INC.
    Inventors: Ulf J. Bremberg, Erik Ringberg, Wei Berts, Anthony De Belder, James S. Strickland
  • 2,6-dioxaspiro [4,5] decane derivatives and preparation method therefor and pharmaceutical applications thereof
    Patent number: 11124523
    Abstract: The present invention relates to a series of 2,6-dioxaspiro [4,5] decane derivatives and applications thereof in preparation of opiate receptor ? agonist related drugs; and in particular relates to the derivative compounds shown in formula (I), tautomers thereof or pharmaceutically acceptable compositions thereof.
    Type: Grant
    Filed: October 12, 2018
    Date of Patent: September 21, 2021
    Inventors: Yang Zhang, Wentao Wu, Guangwen Yang, Zhixiang Li, Jikui Sun, Jie Li, Jian Li, Shuhui Chen
  • IRAK degraders and uses thereof
    Patent number: 11117889
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: September 18, 2020
    Date of Patent: September 14, 2021
    Assignee: KYMERA THERAPEUTICS, INC.
    Inventors: Nello Mainolfi, Nan Ji, Arthur F. Kluge, Matthew M. Weiss, Yi Zhang, Xiaozhang Zheng
  • ASH1L degraders and methods of treatment therewith
    Patent number: 11110177
    Abstract: Provided herein are small molecules comprising a first domain that binds to ASH1L and a second domain that facilitates ASH1L degradation. In particular, ASH1L-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for the treatment of disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.
    Type: Grant
    Filed: November 9, 2018
    Date of Patent: September 7, 2021
    Assignee: The Regents of the University of Michigan
    Inventors: Jolanta Grembecka, Szymon Klossowski, Jing Deng, Tomasz Cierpicki, Hao Li, Hongzhi Miao, Trupta Purohit, EunGi Kim, Dong Chen
  • Substituted quinazoline sulfonamides as thioredoxin interacting protein (TXNIP) inhibitors
    Patent number: 11103508
    Abstract: In one aspect, compounds and compositions that inhibit TXNIP expression and/or that lower hepatic glucose production and methods of identifying, making, and using same are disclosed. The disclosed compounds and compositions can be useful for disorders associated with elevated TXNIP and/or elevated glucagon levels such as, for example, diabetes and associated disorders. Further provided are methods for treating hyperlipidemia or fatty liver disease, optionally associated with elevated TXNIP and/or elevated glucagon levels.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: August 31, 2021
    Assignees: SOUTHERN RESEARCH INSTITUTE, THE UAB RESEARCH FOUNDATION
    Inventors: Corinne E. Augelli-Szafran, Omar Moukha-Chafiq, Mark J. Suto, Anath Shalev, Lance Thielen, Junqin Chen, Gu Jing
  • Methods of treating pain and/or inflammatory disorders using lapatinib
    Patent number: 11103509
    Abstract: A method of treating pain is disclosed, which involves administering an effective amount of lapatinib or a pharmaceutically-acceptable salt thereof to a subject in need of treatment for pain.
    Type: Grant
    Filed: November 6, 2019
    Date of Patent: August 31, 2021
    Assignee: University of Kentucky Research Foundation
    Inventors: Chang-Guo Zhan, Fang Zheng, Shuo Zhou, Ziyuan Zhou
  • UDP glycosyltransferase inhibitors and methods of use
    Patent number: 11098056
    Abstract: Described herein is a compound of Formula (I), and pharmaceutically acceptable salts thereof. Also described herein are compositions and the use of such compositions in methods of treating a variety of diseases and conditions, in particular Krabbe's Disease (KD) and Metachromatic leukodystrophy (MLD).
    Type: Grant
    Filed: October 1, 2019
    Date of Patent: August 24, 2021
    Assignee: GENZYME CORPORATION
    Inventors: Sungtaek Lim, Robert H. Barker, Jr., Mary A. Cromwell, Elina Makino, Bradford Hirth, John Jiang, Sachin Maniar, Mark Munson, Yong-Mi Choi, Sukanthini Thurairatnam, Kwon Yon Musick, James Pribish, Michael Angelastro
  • Malate salt of N-(4-{[6,7-bis(methyloxy) quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer
    Patent number: 11098015
    Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide.
    Type: Grant
    Filed: February 9, 2021
    Date of Patent: August 24, 2021
    Assignee: Exelixis, Inc.
    Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
  • Process for the synthesis of aromatic dicarboxylic acids
    Patent number: 11091454
    Abstract: A method is provided for synthesizing an aromatic carboxylic acid compound comprising providing an aromatic compound or an aromatic compound with at least one carboxylic group; providing a metal hydroxide and at least one carboxylate to produce a mixture; and adding carbon dioxide to the mixture under pressures from about atmospheric to 1000 psig and sufficient heat for a time sufficient to produce aromatic carboxylic acid compounds. The aromatic carboxylic acid compounds may include terephthalic acid, naphthalic acid, thiophene dicarboxylic acid, pyridine dicarboxylic acid, carbazole dicarboxylic acid, and dibenzothiophene dicarboxylic acid.
    Type: Grant
    Filed: September 28, 2019
    Date of Patent: August 17, 2021
    Assignee: UOP LLC
    Inventors: Erin Marie Broderick, Hayim Abrevaya, Paul T. Barger, Alakananda Bhattacharyya
  • Malate salt of N-(4-{[6,7-bis(methyloxy) quinolin-4-yl]oxy}phenyl)- N?-(4-fluorophenyl)cyclopropane-1,1 -dicarboxamide, and crystalline forms thereof for the treatment of cancer
    Patent number: 11091440
    Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclo-propane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide.
    Type: Grant
    Filed: January 14, 2021
    Date of Patent: August 17, 2021
    Assignee: Exelixis, Inc.
    Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
  • Malate salt of N-(4-{[6,7-bis(methyloxy) quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms therof for the treatment of cancer
    Patent number: 11091439
    Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.
    Type: Grant
    Filed: October 14, 2020
    Date of Patent: August 17, 2021
    Assignee: Exelixis, Inc.
    Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
  • Solid state crystalline forms of a selective potassium channel modulator
    Patent number: 11091441
    Abstract: The present disclosure provides solid state forms of a selective potassium channel modulator and pharmaceutical compositions comprising the solid state crystalline forms and pharmaceutically acceptable excipients, and methods for preparing and using the solid state forms and the pharmaceutical compositions thereof.
    Type: Grant
    Filed: October 13, 2020
    Date of Patent: August 17, 2021
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Paul Robert Bichler, Jean-Jacques Alexandre Cadieux, Matthew David Tandy, Gregory N. Beatch
  • Solid state forms of Lenvatinib Mesylate
    Patent number: 11084791
    Abstract: The present invention provides a crystalline form of Lenvatinib Mesylate, processes for the preparation of crystalline form of lenvatinib Mesylate and pharmaceutical compositions thereof. The crystalline form of lenvatinib Mesylate designated as Form VN1 is characterized by powder X-ray diffraction pattern. The present invention further provides a process for the preparation of amorphous form of lenvatinib Mesylate. The amorphous form is characterized by powder X-ray diffraction pattern.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: August 10, 2021
    Assignee: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Saladi Venkata Narasayya, Vamsi Krishna Mudapaka, Vishweshwar Peddy
  • Process for producing 5-hydroxymethylfurfural in the presence of an inorganic dehydration and a chloride source
    Patent number: 11084797
    Abstract: The invention relates to a process for converting a feedstock comprising at least one sugar into 5-hydroxymethylfurfural, wherein said feed is brought into contact with one or more inorganic dehydration catalysts and one or more chloride sources in the presence of at least one aprotic polar solvent alone or as a mixture, at a temperature of between 30° C. and 200° C., and at a pressure of between 0.1 MPa and 10 MPa.
    Type: Grant
    Filed: September 25, 2018
    Date of Patent: August 10, 2021
    Assignee: IFP Energies nouvelles
    Inventors: Justine Denis, Marc Jacquin, Damien Delcroix
  • Deuterated fezolinetant
    Patent number: 11078203
    Abstract: Deuterated fezolinetant (R)-(4-fluorophenyl)-(8-methyl-3-(3-(methyl-d3)-1,2,4-thiadiazol-5-yl)-5,6-dihydro-[1,2,4]trizolo[4,3-a]pyrazin-7(8H)-yl)methanone: or a pharmaceutically acceptable salt or solvate thereof, as an NK-3 antagonist. Also, methods of modulating NK-3 receptor activity including administering an effective amount of the compound or pharmaceutically acceptable salt or solvate thereof. Additionally, a process for manufacturing the compound or pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: July 12, 2018
    Date of Patent: August 3, 2021
    Assignee: Ogeda SA
    Inventor: Hamid Hoveyda