Patents Issued in July 6, 2021
  • Compositions and methods for treating and preventing neurodegenerative disorders
    Patent number: 11053192
    Abstract: Compounds, pharmaceutical compositions, methods and kits are described for treating or preventing neurodegenerative diseases such as Alzheimer's disease.
    Type: Grant
    Filed: March 3, 2020
    Date of Patent: July 6, 2021
    Assignee: Alzheon, Inc.
    Inventors: Petr Kocis, Martin Tolar, John Hey
  • Mixed salts of hydroxyalkane sulfinic acid
    Patent number: 11053193
    Abstract: The preparation and use of mixed salts of hydroxyalkane sulfinic acids and optionally hydroxyalkane sulfonic acids as a reducing agent are disclosed. The reducing power of the salts is significantly higher than the reducing power of the corresponding zinc salt. The storage stability of the salts as solids and as aqueous solution is significantly higher than one of the corresponding sodium salts.
    Type: Grant
    Filed: December 12, 2017
    Date of Patent: July 6, 2021
    Assignee: L. BRÜGGEMANN GMBH & CO. KG
    Inventors: Josef Berghofer, Stefan Mark, Tamara Bittlingmayer, Jessica Schreiweis
  • Production process for magnesium N-acetyl taurinate
    Patent number: 11053194
    Abstract: The present invention concerns a process for the production of magnesium N-acetyl taurinate, in particular a process for the production of magnesium N-acetyltaurinate dihydrate.
    Type: Grant
    Filed: June 9, 2020
    Date of Patent: July 6, 2021
    Assignee: SYNAPHARM INDUSTRIAL SYNTHESIS
    Inventors: Philippe Danhier, Pascale Azzam
  • Compounds and uses thereof for the modulation of hemoglobin
    Patent number: 11053195
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Grant
    Filed: November 9, 2018
    Date of Patent: July 6, 2021
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Qing Xu, Zhe Li, Stephen L. Gwaltney, II
  • Substituted indoline derivatives as dengue viral replication inhibitors
    Patent number: 11053196
    Abstract: The present invention concerns substituted indoline derivatives, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.
    Type: Grant
    Filed: May 18, 2018
    Date of Patent: July 6, 2021
    Assignees: Janssen Pharmaceuticals, Inc., Kathalieke Universiteif Leuven
    Inventors: Jean-François Bonfanti, Bart Rudolf Romanie Kesteleyn, Dorothée Alice Marie-Eve Bardiot, Arnaud Didier M Marchand, Erwin Coesemans, Benoît Christian Albert Ghislain De Boeck, Pierre Jean-Marie Bernard Raboisson
  • Carbazole derivatives
    Patent number: 11053197
    Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein Q, R1a, R1b, R2a, R2b, R3, R4, R5a, R5b, R6a, R6c, R7a, R7b, R7c, and R7d are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Grant
    Filed: April 27, 2020
    Date of Patent: July 6, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Douglas G. Batt, Qingjie Liu, John E. Macor, Joseph A. Tino, Scott Hunter, Satheesh Kesavan Nair, Tarun Kumar Maishal
  • 1-cyano-pyrrolidine compounds as USP30 inhibitors
    Patent number: 11053198
    Abstract: The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (II) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, R10, R12, Z, Y and m are as defined herein.
    Type: Grant
    Filed: March 11, 2019
    Date of Patent: July 6, 2021
    Assignee: MISSION THERAPEUTICS LIMITED
    Inventors: Alison Jones, Mark Kemp, Martin Stockley, Karl Gibson, Gavin Whitlock
  • Crystalline (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, compositions and methods of use thereof
    Patent number: 11053199
    Abstract: Provided herein are crystalline forms of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate. Pharmaceutical compositions comprising crystalline forms of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate are also disclosed.
    Type: Grant
    Filed: September 12, 2019
    Date of Patent: July 6, 2021
    Assignees: Celgene Corporation, Abide Therapeutics, Inc.
    Inventors: Lianfeng Huang, Nancy Tsou, Nicole Suzanne White, Jun Xu, Qun Zhang
  • Precursors for radiofluorination
    Patent number: 11053200
    Abstract: A method for producing a radiofluorinated compound having an aromatic or heteroaromatic ring carrying [18F] fluorine as first substituent, a bonding unit, which can bind to a peptide or peptide mimetic, and a spacer group connected via bond A1 to the bonding unit and via bond A2 to the ring, wherein the bonding unit has second substituent(s) —OH, —CONH, and/or —COOH. The steps include (a) providing a precursor having the ring carrying a substituent Y, bonding unit with the second substituent(s), and spacer group, wherein substituent Y is —N+(R1R2R3), —NO2, —Cl, —Br, —F, or —I, and R1, R2, and R3 are independently C1-C6 alkyl; and (b) reacting the precursor with a [18F] fluoride anion in the presence of an activation salt to the radiofluorinated compound, which has a cation N+(R4R5R6R7) with R4, R5, R6, and R7 being independently C1-C6 alkyl, wherein the substituent Y is replaced by [18F] fluoride.
    Type: Grant
    Filed: January 31, 2020
    Date of Patent: July 6, 2021
    Assignee: ABX advanced biochemical compounds GmbH
    Inventors: René Martin, René Smits, Ronny Hesse, Alexander Hoepping, Marco Müller, Sandra Hübner
  • Crystalline forms
    Patent number: 11053201
    Abstract: The invention relates to crystalline forms of N-[2-(2,4-dichlorophenyl)cyclobutyl]-2-(trifluoromethyl)pyridine-3-carboxamide of formula (I), compositions comprising said crystalline forms and methods of their use as nematicides or fungicides.
    Type: Grant
    Filed: February 11, 2019
    Date of Patent: July 6, 2021
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: John Hone, Ian Kevin Jones
  • Compositions for the treatment of hypertension and/or fibrosis
    Patent number: 11053202
    Abstract: The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of hypertension and/or fibrosis.
    Type: Grant
    Filed: September 21, 2017
    Date of Patent: July 6, 2021
    Assignee: Vectus Biosystems Limited
    Inventor: Karen Annette Duggan
  • One-pot homogeneous process for the large scale manufacture of 2-substituted benzimidazoles
    Patent number: 11053203
    Abstract: 2-substituted benzimidazoles and methods of preparing the same are disclosed. The compositions may include a compound or salt thereof, an acid, and a polar aprotic solvent. The compositions may be used to inhibit corrosion of a metal surface in contact with an aqueous system, and provide enhanced protection against corrosion of metals in the aqueous system.
    Type: Grant
    Filed: November 9, 2018
    Date of Patent: July 6, 2021
    Assignee: ECOLAB USA INC.
    Inventors: Pradeep Cheruku, Suresh R. Sriram, James Joseph Michels
  • Pyrimidinyloxy benzene derivatives as herbicides
    Patent number: 11053204
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, Z, R1 R2, R3 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: June 1, 2016
    Date of Patent: July 6, 2021
    Assignee: FMC Corporation
    Inventors: Nicholas Ryan Deprez, John Robbins Debergh
  • Phenazine derivatives as antimicrobial agents
    Patent number: 11053205
    Abstract: The present invention provides novel phenazine derivatives, such as compounds of Formula (I) (e.g., Formulae (II)-(XIX)), and pharmaceutically acceptable salts thereof. The compounds of the invention are expected to be antimicrobial agents and may act by a microbial warfare strategy (e.g., a reactive oxygen species (ROS)-based competition strategy). The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the compounds of the invention and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection or mycobacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium or mycobacterium), killing a microorganism (e.g., a bacterium or mycobacterium), inhibiting the formation and/or growth of a biofilm, reducing or clearing a biofilm, and/or disinfecting a surface.
    Type: Grant
    Filed: February 17, 2018
    Date of Patent: July 6, 2021
    Assignee: University of Florida Research Foundation, Incorporated
    Inventors: Robert William Huigens, III, Aaron Garrison, Yasmeen Abouelhassan, Hongfen Yang, Gena Burch
  • Hydrofluorocarboximidate and methods of making and using the same
    Patent number: 11053206
    Abstract: Described herein is an hydrofluorocarboximidate of formula (I) where: RH is a linear or branched alkyl group comprising 1 or 2 carbon atoms and (a) Rf1 and Rf2 are independent-selected from a linear or branched perfluorinated alkyl group comprising 1-8 carbon atoms and optionally comprising at least one catenated atom selected from oxygen, nitrogen, or combinations thereof; or (b) Rf1 and Rf2 are connected to form a ring structure comprising a total of 4-8 carbon atoms and in addition to the nitrogen atom from the carboximidate the ring structure may optionally comprises at least one catenated atom selected from oxygen, nitrogen, or combinations thereof. A method of making the hydrofluorocarboximidate with improved yield is described as well as various uses for the hydrofluorocarboximidate of Formula (I).
    Type: Grant
    Filed: August 23, 2018
    Date of Patent: July 6, 2021
    Assignee: 3M Innovative Properties Company
    Inventor: Sean M. Smith
  • Indoleamine-2,3-dioxygenase inhibitor and preparation method therefor
    Patent number: 11053207
    Abstract: Disclosed are a compound represented by general formula I and a preparation method therefor. The compound can be used as indoleamine-2,3-dioxygenase inhibitor to prepare medicines for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.
    Type: Grant
    Filed: September 15, 2015
    Date of Patent: July 6, 2021
    Assignee: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
    Inventors: Zhaoyin Wang, Wei Guo, Jidong Zhu
  • Compound having oxadiazole and pharmaceutical composition containing the same
    Patent number: 11053208
    Abstract: Disclosed are oxadiazole compounds and pharmaceutically acceptable salts thereof. The compounds and pharmaceutically acceptable salts thereof are specifically suitable for the treatment of neurological diseases such as epilepsy.
    Type: Grant
    Filed: September 20, 2019
    Date of Patent: July 6, 2021
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Choon Ho Ryu, Min Soo Han, Yeo Jin Yoon, Yu Jin Kim, Ka Eun Lee, Ju Young Lee, Myung Jin Jung, Eun Hee Baek, Yu Jin Shin, Eun Ju Choi, Young Soon Kang, Yong Soo Kim, Yea Mi Song, Jin Sung Kim, Hee Jeong Lim
  • Highly efficient synthesis of z-macrocycles using stereoretentive, ruthenium-based metathesis catalysts
    Patent number: 11053209
    Abstract: A highly efficient, Z-selective ring-closing metathesis system for the formation of macrocycles using a stereoretentive, ruthenium-based catalyst supported by a dithiolate ligand is reported. This catalyst is demonstrated to be remarkably active as observed in initiation experiments showing complete catalyst initiation at ?20° C. within 10 min. Using easily accessible diene starting materials bearing a Z-olefin moiety, macrocyclization reactions generated products with significantly higher Z-selectivity in appreciably shorter reaction times, in higher yield, and with much lower catalyst loadings than in previously reported systems. Macrocyclic lactones ranging in size from twelve-membered to seventeen-membered rings are synthesized in moderate to high yields (68-79% yield) with excellent Z-selectivity (95%-99% Z).
    Type: Grant
    Filed: April 24, 2018
    Date of Patent: July 6, 2021
    Assignee: CALIFORNIA INSTITUTE OF TECHNOLOGY
    Inventors: Tonia S. Ahmed, Robert H. Grubbs
  • Process to continuously prepare a cyclic carbonate
    Patent number: 11053210
    Abstract: Process to continuously prepare a cyclic carbonate product by reacting an epoxide compound with carbon dioxide in the presence of a supported dimeric aluminium salen complex which complex is activated by a halide compound comprising the following steps, (a) contacting carbon dioxide with the epoxide compound in a suspension of liquid cyclic carbonate and the supported dimeric aluminium salen complex which complex is activated by a halide compound, (b) separating part of the cyclic carbonate product from the supported dimeric aluminium salen complex, (c) separating the halide compound from the cyclic carbonate product to obtain purified cyclic carbonate product, (d) use all or part of the halide compound as obtained in step (c) to activate deactivated supported dimeric salen complex.
    Type: Grant
    Filed: December 18, 2018
    Date of Patent: July 6, 2021
    Assignee: NEW GREEN WORLD B.V.
    Inventors: Frank Vergunst, Sander Laurentius
  • Process for pomalidomide
    Patent number: 11053211
    Abstract: The present invention provides a novel process for the preparation of pomalidomide crystalline Form I. The present invention also provides a process for the purification of pomalidomide.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: July 6, 2021
    Assignee: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Matta Ramakrishna Krishna Reddy, Bandi Vamsi Krishna
  • Benzimidazole derivatives as bromodomain inhibitors
    Patent number: 11053212
    Abstract: Compounds of formula (I) and salts thereof: wherein R1, R2, R3, R4 are defined herein. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET family of bromodomain proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as rheumatoid arthritis; and cancers.
    Type: Grant
    Filed: August 22, 2019
    Date of Patent: July 6, 2021
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Rino Antonio Bit, John Alexander Brown, Philip G. Humphreys, Katherine Louise Jones
  • Pharmaceutical compounds
    Patent number: 11053213
    Abstract: The present invention relates to compounds of Formula (I) that are useful as inhibitors of the activity of the ubiquitin specific protease USP19. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in therapy.
    Type: Grant
    Filed: July 26, 2017
    Date of Patent: July 6, 2021
    Assignee: ALMAC DISCOVERY LIMITED
    Inventors: Peter Hewitt, Mary Melissa McFarland, James Samuel Shane Rountree, Frank Burkamp, Christina Bell, Lauren Proctor, Matthew Duncan Helm, Colin O'Dowd, Timothy Harrison
  • Compositions and methods related to pyridinoylpiperidine 5-HTagonists
    Patent number: 11053214
    Abstract: The present invention provides new pseudo-polymorphs of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide which are useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine headache.
    Type: Grant
    Filed: December 5, 2017
    Date of Patent: July 6, 2021
    Assignee: CoLucid Pharmaceuticals, Inc.
    Inventors: Brigida Allieri, Paul Fagan, Emma Sharp, Raymond D. Skwierczynski
  • Heterocyclic compounds useful as Pim kinase inhibitors
    Patent number: 11053215
    Abstract: The present application is concerned with heterocyclic compounds that inhibit the activity of Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancers and other diseases.
    Type: Grant
    Filed: September 9, 2019
    Date of Patent: July 6, 2021
    Assignee: Incyte Corporation
    Inventors: Oleg Vechorkin, Yun-Long Li, Alexander Sokolsky, Anlai Wang, Wenyu Zhu, Jincong Zhuo
  • Compounds and methods of use
    Patent number: 11053216
    Abstract: This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGF?) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.
    Type: Grant
    Filed: October 22, 2019
    Date of Patent: July 6, 2021
    Assignee: Medivation Technologies LLC
    Inventors: Roopa Rai, Sarvajit Chakravarty, Brahmam Pujala, Bharat Uttam Shinde, Anjan Kumar Nayak, Anil Kumar Agarwal, Sreekanth A. Ramachandran, Son Minh Pham
  • Optically active pyrrolidine compound and method for producing same
    Patent number: 11053217
    Abstract: The present invention provides: a methyl 1-{2-[(3S,4R)-1-[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidine-3-carbonyl]-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylate 1/2 ethane-1,2-disulfonic acid which is represented by formula (1) and is excellent in crystallinity; and a method for producing the same; and a production intermediate thereof; and a production method using this compound.
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: July 6, 2021
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Joji Tsurumoto, Kenji Morokuma
  • 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
    Patent number: 11053218
    Abstract: The present disclosure provides a compound of Formula (I?): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein R1, R2, Rx, X1, n, n1, and q are as defined herein, and methods of making and using same.
    Type: Grant
    Filed: March 31, 2020
    Date of Patent: July 6, 2021
    Inventors: Rohan Eric John Beckwith, Simone Bonazzi, Artiom Cernijenko, Aleem Fazal, Ritesh Bhanudasji Tichkule, Michael Scott Visser
  • Substituted pyridines as TYK2 inhibitors
    Patent number: 11053219
    Abstract: Described herein are pyridine compounds of Formula (XIII) that are useful in treating a TYK2-mediated disorder.
    Type: Grant
    Filed: July 24, 2020
    Date of Patent: July 6, 2021
    Assignee: Esker Therapeutics, Inc.
    Inventors: Bohan Jin, Qing Dong, Gene Hung, Stephen W. Kaldor
  • Process for 3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl) aniline
    Patent number: 11053220
    Abstract: The present invention relates to an improved process for the preparation of 3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl) aniline of Formula (I).
    Type: Grant
    Filed: December 28, 2018
    Date of Patent: July 6, 2021
    Assignee: LAURUS LABS LTD
    Inventors: Ravindra Babu Bollu, Veera Narayana Bandlamudi, Vivek Kumar Kudirilla, Rambabu Vemula, Uma Maheswer Rao Vasireddi
  • Substituted pyrimidines for inhibiting embryonic leucine zipper kinase activity
    Patent number: 11053221
    Abstract: Compounds having activity as chemotherapeutic agents are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1a, R1b, R1c, R1d, L, and are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods for treating cancer (e.g., hematological cancers) are also provided.
    Type: Grant
    Filed: October 25, 2019
    Date of Patent: July 6, 2021
    Assignee: ARRIEN PHARMACEUTICALS LLC
    Inventor: Hariprasad Vankayalapati
  • Fluorescent compounds
    Patent number: 11053222
    Abstract: Compounds used as labels with properties comparable to known fluorescent compounds. The compounds can be conjugated to proteins and nucleic acids for biological imaging and analysis. Synthesis of the compounds, formation and use of the conjugated compounds, and specific non-limiting examples of each are provided.
    Type: Grant
    Filed: June 10, 2019
    Date of Patent: July 6, 2021
    Assignees: Pierce Biotechnology, Inc., Dyomics GmbH
    Inventors: Greg Hermanson, Peter T. Czerney, Surbhi Desai, Matthias S. Wenzel, Boguslawa Dworecki, Frank G. Lehmann
  • Phenoxyquinazoline compounds and their use in treating cancer
    Patent number: 11053223
    Abstract: The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 have any of the meanings hereinbefore defined in the description; process for their preparation, pharmaceutical compositions containing them and their use in treating KIT mediated diseases.
    Type: Grant
    Filed: April 26, 2018
    Date of Patent: July 6, 2021
    Assignee: AstraZeneca AB
    Inventors: Tudor Grecu, Jason Grant Kettle, Martin John Packer, Stuart Eric Pearson, James Michael Smith
  • Polymorphic forms of kinase inhibitor compound, pharmaceutical composition containing same, preparation method therefor and use thereof
    Patent number: 11053224
    Abstract: The invention discloses polymorphic forms of a compound of formula I, pharmaceutical compositions containing same, preparation method therefor and use thereof. The compound of formula I of the present invention is as shown in formula I, of which the crystalline form can be crystalline form 1, crystalline form 2, crystalline form 3, crystalline form 5, crystalline form 6 or crystalline form 7. All the crystalline forms of the compound of formula I in the present invention have good crystalline stability and chemical stability and a decrease in purity of their main ingredient less than 2%. The preparation method of the present invention may be used to produce the various crystalline forms of the compound of formula I with high purity, and suitable for large scale production.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: July 6, 2021
    Assignee: EQUINOX SCIENCES, LLC
    Inventors: Congxin Liang, Lihua Xie
  • Pyrimidine derivative compound, optical isomer thereof, or pharmaceutically acceptable salt thereof, and composition for preventing or treating Tyro 3 related disease comprising same as active ingredient
    Patent number: 11053225
    Abstract: A pyrimidine derivative compound of Chemical Formula 1, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, and a composition for preventing or treating cancer comprising the same as an active ingredient. The pyrimidine derivative compound of Chemical Formula 1, the optical isomer thereof, or the pharmaceutically acceptable salt thereof has an excellent selective inhibitory effect especially against TYRO 3 among TAM receptor inhibitory effects, and thus can be used as an excellent composition of preventing or treating cancer without adverse effects resulting from the inhibition of Axl and Mer.
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: July 6, 2021
    Assignee: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Sung Yun Cho, Chang Hoon Lee, Yong Ki Min, Jong Yeon Hwang
  • KRAS G12C inhibitors and methods of using the same
    Patent number: 11053226
    Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
    Type: Grant
    Filed: November 18, 2019
    Date of Patent: July 6, 2021
    Assignee: AMGEN INC.
    Inventors: Youngsook Shin, Victor J. Cee, Christopher M. Tegley, Brian Alan Lanman, Ryan Paul Wurz, Kevin C. Yang, Vu Van Ma, Daniel Erlanson, Joon Won Jeong, Raymond V. Fucini, Jeffrey Iwig
  • Process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction and novel synthesis intermediates
    Patent number: 11053227
    Abstract: Subject-matter of the present invention is a process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction of the corresponding beta-amino ketones. Subject-matter of the invention are also said novel synthesis intermediates and the use thereof in the preparation of active pharmaceutical ingredients, among which vilanterol and the salts thereof.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: July 6, 2021
    Assignee: OLON S.P.A.
    Inventors: Corrado Colli, Giorgio Bertolini, Mara Sada, Faris Garis, Filippo Nisic, Aldo Bianchi, Cinzia Biaggi, Romano Di Fabio, Silvano Ronzoni, Stefania Bertuolo, Adolfo Prandi, Stefano Maiorana
  • Condensed cyclic compound, composition including the condensed cyclic compound, and organic light-emitting device including the condensed cyclic compound
    Patent number: 11053228
    Abstract: A condensed cyclic compound represented by Formula 1: Ar1-L1-Ar2??Formula 1 wherein, in Formula 1, Ar1, Ar2, and L are the same as described in the specification.
    Type: Grant
    Filed: July 12, 2019
    Date of Patent: July 6, 2021
    Assignees: SAMSUNG ELECTRONICS CO., LTD., SAMSUNG SDI CO., LTD.
    Inventors: Yongsik Jung, Soonok Jeon, Eunsuk Kwon, Sangmo Kim, Juhyun Kim, Jhunmo Son, Yeonsook Chung, Joonghyuk Kim
  • Compound, material for organic electroluminescent element, organic electroluminescent element, and electronic device
    Patent number: 11053229
    Abstract: A compound represented by formula (1): wherein R1 to R7, R11 to R18, L1 to L3, a to c, n, and Ar are as defined in the description, provides an organic electroluminescence device having an emission efficiency and a device lifetime further improved.
    Type: Grant
    Filed: March 7, 2018
    Date of Patent: July 6, 2021
    Assignee: IDEMITSU KOSAN CO., LTD.
    Inventors: Hirokatsu Ito, Tasuku Haketa, Yu Kudo, Yumiko Mizuki
  • 3-hydroxy-imidazolidin-4-one compounds as inhibitors of indoleamine 2,3-dioxygenase
    Patent number: 11053230
    Abstract: The invention relates to a compound of Formula (I): Formula (I), or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenase. The invention also relates to the use of the compounds of Formula (I) for the treatment or prevention of diseases cancer, infections, central nervous system disease or disorder, and immune-related disorders, either as a single agent or in combination with other therapies.
    Type: Grant
    Filed: August 30, 2018
    Date of Patent: July 6, 2021
    Inventors: Adrianus Petrus Antonius De Man, Joost Cornelis Marinus Uitdehaag, Jan Gerard Sterrenburg, Joeri Johannes Petrus De Wit, Freek Van Cauter, Nicole Wilhelmina Cornelia Seegers, Antonius Maria Van Doornmalen, Rogier Christian Buijsman, Guido Jenny Rudolf Zaman
  • Compounds for the treatment of glycogen storage disorders
    Patent number: 11053231
    Abstract: Compounds represented by general Formulae I to IV as described herein are disclosed. Further disclosed are composition utilizing the herein disclosed compounds and using the same for the treatment of glycogen storage disorders.
    Type: Grant
    Filed: February 22, 2018
    Date of Patent: July 6, 2021
    Assignees: Hadasit Medical Research Services and Development Ltd., Ramot at Tel-Aviv University Ltd.
    Inventors: Or Kakhlon, Miguel Enrique Weil, Leonardo Javier Solmesky
  • 1,3,5-dioxazine derivatives, method of preparation and application thereof as sulfide scavenger
    Patent number: 11053232
    Abstract: The present disclosure relates to 1,3,5-dioxazine derivatives of formula (I) capable of reducing or eliminating hydrogen sulfide and other objectionable sulfides from oil field produced hydrocarbon fluids such as petroleum, fuel oil, gasoline, diesel, liquid propane, liquid butane, an aquaculture and production/processing of syngas/natural gas. The present disclosure further provides a method for preparing 1,3,5-dioxazine derivatives of formula I, and a method for scavenging sulfur-based species including, but not limited to hydrogen sulfide or alkyl/aryl mercaptans from a medium.
    Type: Grant
    Filed: July 5, 2017
    Date of Patent: July 6, 2021
    Inventor: Kishor Prabhakar Kumbhar
  • Solid form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)-methanol
    Patent number: 11053233
    Abstract: An anhydrous disordered crystalline (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be used in pharmaceutical compositions.
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: July 6, 2021
    Assignee: Merck Patent GmbH
    Inventors: Michael Lange, Clemens Kuehn, Thomas Fuchss, David Maillard, Marcel Breuníng, Marco Poma, Edoardo Burini
  • 1,3 di-substituted cyclobutane or azetidine derivatives as hematopoietic prostaglandin D synthase inhibitors
    Patent number: 11053234
    Abstract: A compound of formula (I) wherein R, R1, R2, R3, Y, Y1, a, X, and Z are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne Muscular Dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: July 6, 2021
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: David Norman Deaton, Yu Guo, Ashley Paul Hancock, Christie Schulte, Barry George Shearer, Emilie Despagnet Smith, Eugene L. Stewart, Stephen Andrew Thomson
  • Substituted 1,4-dihydropyrimidines for the treatment of HBV infection or HBV-induced diseases
    Patent number: 11053235
    Abstract: The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.
    Type: Grant
    Filed: August 9, 2019
    Date of Patent: July 6, 2021
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: Gang Deng, Yimin Jiang, Qian Liu, Chao Liang, Zhao-Kui Wan, Wing Shun Cheung, Zhanling Cheng, Yanping Xu
  • Substituted isoselenazolone anti-infective, anti-inflammatory, anti-cancer, cytoprotective, neuroprotective, and anti-oxidant agents
    Patent number: 11053236
    Abstract: Compounds, compositions, and methods for the treatment of infections, inflammation, cancers, tinnitus, Meniere's disease, hearing loss, or bipolar disorder, or for providing cytoprotection against Clostridium difficile toxins, are disclosed.
    Type: Grant
    Filed: June 21, 2017
    Date of Patent: July 6, 2021
    Assignee: The University of Toledo
    Inventors: Steven Sucheck, Sandeep Thanna, Donald Ronning, Alexander Landgraf
  • Process for the manufacture of 6-alkynyl-pyridine derivatives
    Patent number: 11053237
    Abstract: The application includes a description of novel intermediates, of new manufacturing steps resulting in a novel and improved process for producing the intermediates and the final compounds, i.e., 6-alkynyl-pyridine derivatives. The intermediates of the invention are useful to produce 6-alkynyl-pyridine derivatives, which compounds are useful for the treatment of cancer.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: July 6, 2021
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Guanghua Lu, Guenther Huchler, Thomas Krueger, Michael Pangerl, Marco Santagostino, Jean-Nicolas Desrosiers
  • Benzimidazole derivatives, preparation methods and uses thereof
    Patent number: 11053238
    Abstract: The present invention relates to benzimidazole compounds useful in treating for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention of one or more symptoms of cancer, transplant rejections. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK4 and/or CDK6, using the compounds provided herein.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: July 6, 2021
    Assignee: BETTA PHARMACEUTICALS CO., LTD.
    Inventors: Yiqian Wang, Jiabing Wang, Lieming Ding
  • Compounds as BLC-2-selective apoptosis-inducing agents
    Patent number: 11053239
    Abstract: Bcl-2 inhibitors, pharmaceutical compositions thereof, and methods of use thereof are provided. In particular, Bcl-2 inhibitors of formula (I) are provided, wherein the variable groups are as defined in the specification. The Bcl-2 inhibitors can be used to treat cell proliferative disorders.
    Type: Grant
    Filed: January 5, 2018
    Date of Patent: July 6, 2021
    Assignee: Fochon Pharmaceuticals, Ltd.
    Inventors: Xingdong Zhao, Zuwen Zhou, Chengxi He, Zhifu Li, Yue Rong, Rui Tan, Huajie Zhang, Hongbin Liu, Weipeng Zhang, Haohan Tan, Zhifang Chen, Lihua Jiang, Yanxin Liu, Min Lin, Jing Sun, Weibo Wang
  • 2-amino-quinoline derivatives
    Patent number: 11053240
    Abstract: Described herein are 2-amino-quinoline derivatives that are agonists of toll-like receptors 7 and 8 (TLR7/8), pharmaceutical compositions, and methods of use of the compounds and compositions to treat various diseases, such as viral, cancer, and allergic diseases, in need thereof by administering a therapeutically effective amount of a 2-amino-quinoline derivative.
    Type: Grant
    Filed: April 26, 2018
    Date of Patent: July 6, 2021
    Assignee: Birdie Biopharmaceuticals, Inc.
    Inventors: Lixin Li, Huiping Guan
  • TYK2 inhibitors and uses thereof
    Patent number: 11053241
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: November 27, 2019
    Date of Patent: July 6, 2021
    Assignee: Nimbus Lakshmi, Inc.
    Inventors: Jeremy Robert Greenwood, Craig E. Masse