Patents Examined by Taylor V. Oh
  • Patent number: 11071734
    Abstract: A tableted pharmaceutical composition contains nalfurafine or a pharmaceutically acceptable acid addition salt thereof and is excellent in formability and quality control of related substances. The tableted pharmaceutical composition includes nalfurafine or a pharmaceutically acceptable acid addition salt thereof, a binder component, and a carrier, wherein the above mentioned nalfurafine or a pharmaceutically acceptable acid addition salt thereof is contained in an amount of 0.1 to 10 ?g, and the weight of the above mentioned binder component is 100,000 to 2,000,000 weight % based on the weight of the above mentioned nalfurafine or a pharmaceutically acceptable acid addition salt thereof and 5 to 20 weight % based on the total weight of the resulting pharmaceutical composition, or 20,000 to 500,000 weight % and 1 to 5 weight % based on the total weight of the resulting pharmaceutical composition.
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: July 27, 2021
    Assignee: Toray Industries, Inc.
    Inventors: Satoshi Minakami, Suguru Takaki, Kotoe Ohta, Yasuhide Horiuchi
  • Patent number: 11065258
    Abstract: The present invention relates generally to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathy, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to methods for the use of calmodulin inhibitors and calcium channel blockers for treatment of ribosomal disorders and ribosomopathy, e.g. Diamond Blackfan anemia (DBA).
    Type: Grant
    Filed: August 12, 2019
    Date of Patent: July 20, 2021
    Inventors: Leonard I. Zon, Alison M. Taylor
  • Patent number: 11053189
    Abstract: A method for producing a homocyclic or heterocyclic compound includes reacting a compound of formula (I) with a compound of formula (II) in presence of a base: In formula (I), B is an unsaturated moiety selected from substituted or unsubstituted vinylene, ethynylene, aryleneethynylene, substituted or unsubstituted arylenevinylene, and a combination thereof, the vinylene or arylenevinylene has n (=0, 1 or 2) substituent(s) R2, G is an electron-withdrawing group, R1 is hydrogen or a substituent, and two of R1, R2 and G may joint together to form a ring. In formula (II), R3 and R4 are independently hydrogen or a substituent, R5 is an electron-withdrawing group, and two of R3, R4 and R5 may joint together to form a ring. The conjugate acid of the base has a pKa in the range of 1 to 15.
    Type: Grant
    Filed: March 25, 2019
    Date of Patent: July 6, 2021
    Assignee: National Tsing Hua University
    Inventors: Chien-Chung Han, Suman Alishetty
  • 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
    Inventors: Tonia S. Ahmed, Robert H. Grubbs
  • Patent number: 11046684
    Abstract: Provided are a compound of formula (I), a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof, use thereof as a selective inhibitor for FGFR4 kinase and use thereof in manufacturing a medicament or pharmaceutical composition for treating diseases due to FGFR4 or FGF19. The compound disclosed by the invention has selective and significant inhibitory activities against FGFR4, and has wide application prospect in the field of tumor treatment.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: June 29, 2021
    Inventors: Jianyu Liu, Haidong Zhang
  • Patent number: 11046676
    Abstract: The present invention relates to process for the preparation of Empagliflozin or its co-crystals, solvates and/or polymorphs thereof. The present invention also relates to novel intermediates used therein, and process for the preparation thereof. The present invention further relates to process for preparation of amorphous and crystalline form of Empagliflozin.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: June 29, 2021
    Assignee: Laurus Labs Limited
    Inventors: Uma Maheswar Rao Vasireddi, Sanjay Kumar Dehury, Nagaraju Mekala, Jahangeer Baba Shaik, Srinivas Lagadapati
  • Patent number: 11040019
    Abstract: Methods are disclosed for treating and/or preventing retinal degeneration is a subject. In some embodiments, the method includes administering to the subject a therapeutically effective amount of a selective estrogen receptor modulator (SERM) to treat the retinal degeneration in the subject. In other embodiments, the SERM is administered orally. In some examples, the SERM is tamoxifen, afimoxifene, raloxifene, bazedoxifene, arzoxifene, desmethylarzoxifene, or a salt or derivative thereof, or combinations thereof.
    Type: Grant
    Filed: August 10, 2017
    Date of Patent: June 22, 2021
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Wenxin Ma, Lian Zhao, Xu Wang, Wai T. Wong
  • Patent number: 11034664
    Abstract: Techniques regarding the synthesis of cyclic carbonate monomers are provided. For example, one or more embodiments described herein can comprise a method, which can include cyclizing a functionalized diol monomer with N,N?-carbonyldiimidazole, wherein the cyclizing produces a cyclic carbonate monomer and an imidazole carbamate. The method can also include activating the imidazole carbamate with an acid, wherein the activating promotes cyclization of the imidazole carbamate into the cyclic carbonate monomer.
    Type: Grant
    Filed: May 11, 2020
    Date of Patent: June 15, 2021
    Inventors: Nathaniel H. Park, James L. Hedrick, Victoria A Piunova, Pedro Arrechea, Tim Erdmann
  • Patent number: 11028063
    Abstract: An integrated process is useful for producing 2,5-furandicarboxylic acid (FDCA) and/or a derivative thereof from a six-carbon sugar-containing feed. The process includes a) dehydrating a feed containing a six-carbon sugar unit, in the presence of a bromine source and of a solvent, to generate an oxidation feed that contains at least one of 5-hydroxymethylfurfural (HMF) and/or a derivative or derivatives of HMF in the solvent, together with at least one bromine containing species; b) contacting the oxidation feed from step (a) with a metal catalyst and with an oxygen source under oxidation conditions to produce an oxidation product mixture of at least FDCA and/or a derivative thereof, the solvent, and a residual catalyst; c) purifying and separating the mixture obtained in step (b) to obtain FDCA and/or a derivative thereof and the solvent; and d) recycling at least a portion of the solvent obtained in step (c) to step (a).
    Type: Grant
    Filed: July 9, 2020
    Date of Patent: June 8, 2021
    Inventors: Stephen J. Howard, Kristina A. Kreutzer, Bhuma Rajagopalan, Eric R. Sacia, Alexandra Sanborn, Brennan Smith
  • Patent number: 11028065
    Abstract: In one embodiment, a continuous process for preparing organic carbonate solvent of Formula (I) as described herein comprises contacting a first reactant (an alcohol) with a reactive carbonyl source (carbonyldiimidazole (CDI) or an alkylchloroformate) in the presence of a catalyst in reaction stream flowing through a continuous flow reactor at temperature 20° C. to about 160° C. and at a flow rate providing a residence time in the range of about 0.1 minute to about 24 hours; collecting a reactor effluent exiting from the continuous flow reactor; recovering a crude product from the reactor effluent; and distilling the crude product to obtain the organic carbonate compound of Formula (I). In another embodiment, the first reactant is an epoxide and the carbonyl source is carbon dioxide.
    Type: Grant
    Filed: March 9, 2020
    Date of Patent: June 8, 2021
    Inventors: Trevor L. Dzwiniel, Krzysztof Pupek
  • Patent number: 11014927
    Abstract: The disclosure relates to modulating pyruvate kinase and provides novel chemical compounds of formula (I) useful as activators of PKR, as well as various uses of these compounds. PKR activating compounds are useful in the treatment of diseases and disorders associated with PKR and/or PKM2, such as pyruvate kinase deficiency (PKD), sickle cell disease (SCD), and thalassemia.
    Type: Grant
    Filed: March 20, 2018
    Date of Patent: May 25, 2021
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Anna Ericsson, Neal Green, Gary Gustafson, Bingsong Han, David R. Lancia, Jr., Lorna Mitchell, David Richard, Tatiana Shelekhin, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
  • Patent number: 11014886
    Abstract: Disclosed is a method for preparing 2,2?-dipyridine and derivatives thereof. The method includes: using pyridine represented by formula I or a derivative thereof as a raw material to generate 2,2?-dipyridine represented by formula II by performing dehydrogenative coupling under the action of a supported catalyst in the presence of additives, where R is H, C1-C2 alkyl, Cl, or Br. The method of the present invention features wide adaptability to raw materials, high atomic utilization rate, high catalyst activity, long service life, and fewer by-products.
    Type: Grant
    Filed: April 4, 2018
    Date of Patent: May 25, 2021
    Inventors: Chaoran Luo, Wenkui Wang, Yi Xue, Xinchun Chen, Dianhai Zhou, Jianhua Jiang, Fujun Wang
  • Patent number: 11015151
    Abstract: The present invention relates to novel sulfoperoxycarboxylic acid compounds, and methods for making and using them. The sulfoperoxycarboxylic compounds of the invention are storage stable, water soluble and have low to no odor. Further, the compounds of the present invention can be formed from non-petroleum based renewable materials. The compounds of the present invention can be used as antimicrobials, and bleaching agents. The compounds of the present invention are also suitable for use as coupling agents.
    Type: Grant
    Filed: April 27, 2020
    Date of Patent: May 25, 2021
    Assignee: Ecolab USA Inc.
    Inventors: Junzhong Li, Richard K. Staub, David D. McSherry, Keith G. LaScotte, Steven J. Lange, Frank Everts
  • Patent number: 11008296
    Abstract: The present invention relates to novel intermediates of Eribulin and process for the preparation of the same. The process of the present invention is commercially viable and can be easily adopted for plant scale operations. The present invention relates to tetrahydrofuran compounds of formula I, X, XI, D and B.
    Type: Grant
    Filed: November 20, 2018
    Date of Patent: May 18, 2021
    Assignee: Natco Pharma Limited
    Inventors: Bulli Babi Vipparla, Sreenivas Nagapuri, Sathaiah Kandula, Janaki Rama Rao Ravi, Durga Prasad Konakanchi, Pulla Reddy Muddasani, Venkaiah Chowdary Nannapaneni
  • Patent number: 11008312
    Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein m, n, p, q A, B, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Grant
    Filed: April 30, 2019
    Date of Patent: May 18, 2021
    Assignee: Genentech, Inc.
    Inventors: Sarah M. Bronner, James J. Crawford, Andrew Cridland, Patrick Cyr, Benjamin Fauber, Emanuela Gancia, Alberto Gobbi, Christopher Hurley, Jonathan Killen, Wendy Lee, Olivier Rene, Monique Bodil Van Niel, Stuart Ward, Paul Winship, Jason Zbieg
  • Patent number: 11007157
    Abstract: The present invention provides for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE.
    Type: Grant
    Filed: January 27, 2020
    Date of Patent: May 18, 2021
    Assignee: Aldeyra Therapeutics, Inc.
    Inventors: Todd Brady, Scott Young, William A. Kinney, Kenneth J. Mandell
  • Patent number: 11008310
    Abstract: The present invention provides compounds that modulate the interaction of TCR with Nck, compositions thereof, and methods of treatment using the same.
    Type: Grant
    Filed: May 20, 2020
    Date of Patent: May 18, 2021
    Assignee: Artax Biopharma Inc.
    Inventors: Julio Castro, Andrés Gagete Mateos, Peter J. Machin, Christopher Loren Vandeusen
  • Patent number: 11001565
    Abstract: The object of the present invention is to provide a glycolide production method capable of further increasing the production rate of glycolide. The glycolide production method according to the present invention includes adding metal iron to an aqueous glycolic acid solution, subjecting glycolic acid contained in the aqueous glycolic acid solution to which the metal iron is added, to dehydrating polycondensation to obtain a glycolic acid oligomer, and heating and depolymerizing the glycolic acid oligomer to obtain glycolide.
    Type: Grant
    Filed: February 20, 2019
    Date of Patent: May 11, 2021
    Inventors: Yuta Yamadoi, Yoshinori Suzuki, Takenori Tose, Haruyasu Yamaji, Toshihiko Ono
  • Patent number: 10995083
    Abstract: The present invention relates to a cocrystal of 2-(6-methyl-pyridine-2-yl)-3-yl-[6-amide-quinoline-4-yl]-5,6-dihydro-4H-pyrrole[1,2-b]pyrazole (Galunisertib or LY2157299) represented by formula (I) and a cocrystal former. Compared with the known solid form of Galunisertib, the cocrystal of the present invention has advantages in terms of stability, solubility, etc. The present invention also relates to a crystal form of the cocrystal, a preparation method therefor, a pharmaceutical composition thereof, and an application thereof in preparation of drugs for preventing and/or treating diseases relevant to TGF-?.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: May 4, 2021
    Assignee: Hangzhou Solipharma Co., Ltd.
    Inventors: Xiaohong Sheng, Xiaoxia Sheng, Jing Wang
  • Patent number: 10980812
    Abstract: Provided herein are methods of using compounds and compositions for treating, managing, and/or preventing systemic lupus erythematosus (SLE). Pharmaceutical compositions and dosing regimens for use in the methods are also provided herein.
    Type: Grant
    Filed: February 25, 2020
    Date of Patent: April 20, 2021
    Inventors: Peter H. Schafer, Lei Wu, Ying Ye