Patents Examined by Karen Cheng
  • Pyrazolopyrimidine derivatives as BTK inhibitors for the treatment of cancer
    Patent number: 10611766
    Abstract: This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.
    Type: Grant
    Filed: September 16, 2016
    Date of Patent: April 7, 2020
    Assignee: Loxo Oncology Inc.
    Inventor: Nicolas Guisot
  • Organo-1-oxa-4-azonium cyclohexane compounds
    Patent number: 10597373
    Abstract: Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. A substituted hydrocarbon is added to water to form a mixture, and a 1-oxa-4-azacyclohexane derivative is then added. The reaction mixture stirred until a solution containing the 1-oxa-4-azonium cyclohexane salt is obtained.
    Type: Grant
    Filed: May 16, 2018
    Date of Patent: March 24, 2020
    Inventors: Christopher P. Nicholas, Mark A. Miller, Melissa M. Galey, Benjamin D. Yuhas, Sesh Prabhakar
  • Prodrug of 1,1?-(1,6-dioxo-1,6-hexanediyl)bis-D-proline
    Patent number: 10597385
    Abstract: The present invention relates to the compound (2R,2?R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1?-adipoylbis(pyrrolidine-2-carboxylate), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
    Type: Grant
    Filed: December 11, 2017
    Date of Patent: March 24, 2020
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Alexis Denis, Olivier Mirguet, Jérôme Toum
  • Chemical compounds
    Patent number: 10590130
    Abstract: The specification relates to compounds of Formula (I): and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cell proliferative disorders.
    Type: Grant
    Filed: October 9, 2018
    Date of Patent: March 17, 2020
    Assignee: AstraZeneca AB
    Inventors: Bernard Christophe Barlaam, Daniel Hillebrand O'Donovan, Samantha Jayne Hughes, Thomas Andrew Moss, Johannes Wilhelmus Maria Nissink, James Stewart Scott, Bin Yang
  • Cyanopyrrolidine derivatives as inhibitors for DUBs
    Patent number: 10590075
    Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of Cezanne 1 and ubiquitin C-terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of cancer. Compounds of the invention include compounds having the formula (I): pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f and A are as defined herein.
    Type: Grant
    Filed: December 21, 2016
    Date of Patent: March 17, 2020
    Assignee: MISSION THERAPEUTICS LIMITED
    Inventors: Mark Ian Kemp, Michael David Woodrow
  • Process for the preparation of aclidinium bromide
    Patent number: 10590124
    Abstract: A process for preparing (3R)-3-[2-Hydroxy(di-2-thienyl)acetoxy]-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide) comprises reacting 2-hydroxy-2,2-dithien-2-ylacetic acid 1-azabicyclo[2.2.2]oct-3(R) yl methyl ester and 3-phenoxypropyl bromide, wherein the reaction takes place in a solvent or mixture of solvents selected from the group of amides and/or the group of solvents with a sulfoxide group. Also provided is a crystalline aclidinium bromide characterized by a powder XRPD pattern having peaks at 7.7±0.2° 2?, 10.4±0.2° 2?, 13.2±0.2° 2?, 13.8±0.2° 2?, 19.9±0.2° 2?, 20.3±0.2° 2?, 20.8±0.2° 2?, 24.2±0.2° 2?, 25.7±0.2° 2?, 26.1±0.2° 2?, 29.2±0.2° 2?, 30.8±0.2° 2?. A pharmaceutical composition comprises aclidinium bromide according to the invention and a pharmaceutically acceptable excipient.
    Type: Grant
    Filed: August 28, 2018
    Date of Patent: March 17, 2020
    Assignee: Hovione Scienta Limited
    Inventors: Zita Mendes, Constança Cacela, Ana Carina Constantino, Bruno Santos
  • Process for the manufacture of isavuconazole or ravuconazole
    Patent number: 10590092
    Abstract: The invention relates to a process for the manufacture of diastereomerically and enantiomerically enriched triazole compounds isavuconazole and ravuconazole, comprising a Reformatsky reaction between a ketone and a 2-halozincpropionate ester, followed by a resolution step, preferably an enzymatic resolution with an esterase enzyme.
    Type: Grant
    Filed: September 11, 2017
    Date of Patent: March 17, 2020
    Assignee: Basilea Pharmaceutica AG
    Inventors: Ruben Van Summeren, Harrie Vaessen, Daniel Mink, Mario Waser
  • Amine salt of (1R, 3S)-3-(5-cyano-4-phenyl-1,3- thiazol-2-ylcarbamoyl)cyclopentane carboxylic acid
    Patent number: 10583127
    Abstract: The present invention relates to the tromethamine salt of (1R,3S)-3-(5-cyano-4-phenyl-1,3-thiazol-2-ylcarbamoyl)cyclopentane carboxylic acid, a process for obtaining said salt, combination products and pharmaceutical compositions comprising said salts and their medical uses, in particular for the treatment or prevention of diseases known to ameliorate by A1 adenosine receptor antagonism.
    Type: Grant
    Filed: March 6, 2018
    Date of Patent: March 10, 2020
    Assignee: PALOBIOFARMA, S.L.
    Inventors: Julio Castro Palomino Laria, Juan Camacho Gómez
  • Heterocyclic compounds useful in the treatment of disease
    Patent number: 10570103
    Abstract: A method for treating a lysophosphatidic acid-dependent disease or condition in a subject in need thereof is provided. The method includes administering to the subject a therapeutically effective amount of a heterocyclic compound. The heterocyclic compound is a lysophosphatidic acid receptor ligand. Lysophosphatidic acid-dependent diseases and conditions include diseases involving fibrosis, such as fibrosis of the heart, kidney, liver and lung, and scleroderma; inflammatory diseases such as diabetic nephropathy and inflammatory bowel disease; ocular diseases such as diseases involving retinal degeneration; nerve diseases such as pruritus and pain.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: February 25, 2020
    Assignee: EPIGEN BIOSCIENCES, INC.
    Inventors: Graham Beaton, Fabio C. Tucci, Satheesh B. Ravula, Chandravadan R. Shah, Hiep Luu
  • Triazolone compounds and uses thereof
    Patent number: 10568871
    Abstract: The invention disclosed herein is directed to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a therapeutically effective amount of a selective PPAR? antagonist.
    Type: Grant
    Filed: May 9, 2017
    Date of Patent: February 25, 2020
    Assignee: TEMPEST THERAPEUTICS, INC.
    Inventors: Nicholas Simon Stock, Austin Chih-Yu Chen, Yalda Mostofi Bravo, Jason Duarte Jacintho, Jill Melissa Baccei, Brian Andrew Stearns, Ryan Christopher Clark
  • Salts and crystal forms of GABApositive allosteric modulator
    Patent number: 10562930
    Abstract: The invention relates to salts of Compound 1, crystalline forms thereof, methods of their preparation, pharmaceutical compositions thereof and methods of their use.
    Type: Grant
    Filed: July 19, 2019
    Date of Patent: February 18, 2020
    Assignee: PRAXIS PRECISION MEDICINES, INC.
    Inventors: Nelson B. Olivier, Kiran Reddy, Gabriel Martinez Botella, Magnus Ronn, Paul A. Laskar
  • Cytochrome P450 inhibitors and uses thereof
    Patent number: 10556893
    Abstract: The present invention provides compounds having the general structural formula (I) (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
    Type: Grant
    Filed: May 25, 2018
    Date of Patent: February 11, 2020
    Assignee: ANGION BIOMEDICA CORP.
    Inventor: Bijoy Panicker
  • Crystalline form of (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, preparation method therefor and use thereof
    Patent number: 10556863
    Abstract: A crystalline form of (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide is disclosed. The crystalline form has a diffraction peak when a diffraction angle, 2?, is 16.66±0.2°, 17.54±0.20, 21±0.2°, 22.16±0.20, or 30.96±0.20. The crystalline form can be dissolved quickly in water with a solubility greater than or equal to 90 mg/mL, features high bioavailability, has high stability at high temperature, is suitable for preparing multiple pharmaceutical compositions, and can prepare multiple formulations, such as tablets, capsules, dripping pills, sustained-release and controlled-release formulations, and lyophilized powder for injection. The method for preparing the crystalline form is carried out under a mild condition, is easy to operate, introduces a few impurities, and features good reproducibility, an easy-to-control production process and high safety, and is suitable for industrial production.
    Type: Grant
    Filed: July 7, 2017
    Date of Patent: February 11, 2020
    Assignee: CHONGQING RUZER PHARMACEUTICAL COMPANY LIMITED
    Inventor: Lei Ye
  • 3-indol substituted derivatives, pharmaceutical compositions and methods for use
    Patent number: 10544095
    Abstract: A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.
    Type: Grant
    Filed: August 4, 2016
    Date of Patent: January 28, 2020
    Assignees: Pfizer Inc., iTeos Therapeutics
    Inventors: Sacha Ninkovic, Michael Raymond Collins, Stefano Crosignani, Andreas Maderna, Indrawan James McAlpine, Stephanie Anne Scales, Martin Wythes
  • NK-3 receptor selective antagonist compounds, pharmaceutical composition and methods for use in NK-3 receptors mediated disorders
    Patent number: 10544150
    Abstract: The present invention is directed to novel compounds of formula I and their use as therapeutic compounds.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: January 28, 2020
    Assignee: Ogeda SA
    Inventors: Hamid R. Hoveyda, Marie-Odile Roy, Graeme Lovat Fraser, Guillaume Dutheuil
  • Chiral dihydrobenzooxaphosphole ligands and synthesis thereof
    Patent number: 10544177
    Abstract: This invention relates to novel phosphorous ligands useful for organic transformations. Methods of making and using the ligands in organic synthesis are described. The invention also relates to processes for preparing the novel ligands.
    Type: Grant
    Filed: January 10, 2019
    Date of Patent: January 28, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jean-Nicolas Desrosiers, Daniel Robert Fandrick, Nizar Haddad, Guisheng Li, Nitinchandra D. Patel, Bo Qu, Sonia Rodriguez, Chris Hugh Senanayake, Joshua Daniel Sieber, Zhulin Tan, Xiao-Jun Wang, Nathan K. Yee, Li Zhang, Yongda Zhang
  • Substituted pyrazole and pyrrole compounds and methods for using them for inhibition of initiation of translation and treatment of diseases and disorders relating thereto
    Patent number: 10537558
    Abstract: Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure (I) and pharmaceutically acceptable salts and/V-oxides thereof, wherein X1, X2, Z1, Z2, the ring system denoted by “a”, R1, A1A, L1B, A1B, L1A, L2, Q, L3, R3, A4A, L4B, A4B, L4A, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein disrupt the eIF4E/eiF4G interaction, and can be used to treat hyperproliferative disorder, a neurological disease or disorder, or autism.
    Type: Grant
    Filed: June 1, 2016
    Date of Patent: January 21, 2020
    Assignee: Bantam Pharmaceutical, LLC
    Inventors: M. Arshad Siddiqui, Stephane Ciblat, Martin Dery, Lea Constantineau-Forget, Chantal Grand-Maitre, Xiangyu Guo, Sanjay Srivastava, Gerald W. Shipps, Alan B. Cooper, Nicolas Bruneau-Latour, Vu Linh Ly
  • Tricyclic benzoxaborole compounds and uses thereof
    Patent number: 10526352
    Abstract: Compounds of Formula II, wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, or —CH(CH3)2; compositions containing them, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.
    Type: Grant
    Filed: April 16, 2019
    Date of Patent: January 7, 2020
    Assignees: GlaxoSmithKline Intellectual Property (No.2) Limited, Anacor Pharmaceuticals, Inc.
    Inventors: Michael Richard Kevin Alley, Vincent S. Hernandez, Jacob J. Plattner, Xianfeng Li, David Barros-Aguirre, Ilaria Giordano
  • Heterocyclic compounds useful in the treatment of disease
    Patent number: 10526298
    Abstract: Heterocyclic compounds are described that are lysophosphatidic acid receptor ligands that are useful in the treatment of lysophosphatidic acid receptor-dependent diseases and conditions, including but not limited to diseases involving fibrosis, such as fibrosis of the heart, kidney, liver and lung, and scleroderma; inflammatory diseases such as diabetic nephropathy and nonalcoholic steatohepatitis (NASH); ocular diseases such as diseases involving retinal degeneration; nerve diseases such as pruritus and pain.
    Type: Grant
    Filed: June 18, 2018
    Date of Patent: January 7, 2020
    Assignee: EPIGEN BIOSCIENCES, INC.
    Inventors: Graham Beaton, Fabio C. Tucci, Satheesh B. Ravula, Chandravadan R. Shah, Hiep Luu
  • Solid state forms of spiro-oxindole compounds
    Patent number: 10513526
    Abstract: The present invention provides solid state forms of certain spiro-oxindole compounds, such as funapide and the racemic mixture of funapide and its corresponding (R) enantiomer, pharmaceutical compositions comprising the solid state forms and processes for preparing the solid state forms and the pharmaceutical compositions.
    Type: Grant
    Filed: October 10, 2018
    Date of Patent: December 24, 2019
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Ronen Ben-David, Stephen Bierlmaier, Ralph Curtis Haltiwanger, Alexandr Jegorov, Raeann Ruiyun Wu, Mehran Yazdanian