Patents Examined by Zinna Northington Davis
  • Apoptosis signal-regulating kinase inhibitors and uses thereof
    Patent number: 11034671
    Abstract: Described herein are ASK1 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of blood disease, autoimmune disorders, pulmonary disorders, hypertension, inflammatory diseases, fibrotic diseases, diabetes, diabetic nephropathy, renal diseases, respiratory diseases, cardiovascular diseases, acute lung injuries, acute or chronic liver diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: September 7, 2018
    Date of Patent: June 15, 2021
    Assignee: SICHUAN HAISCO PHARMACEUTICAL CO., LTD.
    Inventors: Bohan Jin, Qing Dong, Gene Hung
  • Indazole derivatives as alpha v integrin antagonists
    Patent number: 11028071
    Abstract: The present invention provides compounds of Formula (Ia) or (Ib): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to ?V-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of ?V-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
    Type: Grant
    Filed: July 9, 2020
    Date of Patent: June 8, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Xiang-Yang Ye, Christian L. Morales, Mendi A. Higgins, Eric Mull
  • Tricyclic heterocyclic derivatives and uses thereof
    Patent number: 11028064
    Abstract: Disclosed are tricyclic heterocyclic compounds having kinase inhibitory activity, pharmaceutical compositions and kits comprising the compounds, and use of the compounds in the treatment of or in medicaments for the treatment of various diseases and conditions. In particular, disclosed are tricyclic heterocyclic compounds of the formula (I) having CSF-1R (c-FMS kinase) inhibitory activity and their use in the treatment of various diseases and conditions, such as those mediated by CSF-1R, including proliferative or neoplastic diseases and conditions, including cancers, and bone, inflammatory, and autoimmune diseases and conditions.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: June 8, 2021
    Assignee: AUCKLAND UNISERVICES LIMITED
    Inventors: Swarnalatha Akuratiya Gamage, Peter Robin Shepherd, Jack Urquhart Flanagan, Gordon William Rewcastle, Andrew James Marshall, Christina Maree Buchanan, Guo-Liang Lu, Muriel Bonnet, Stephen Michael Frazer Jamieson, William Alexander Denny
  • Substituted 6-membered aryl or heteroaryl allosteric modulators of nicotinic acetylcholine receptors
    Patent number: 11026958
    Abstract: The present disclosure relates to compounds of formula (I) that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
    Type: Grant
    Filed: October 30, 2017
    Date of Patent: June 8, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Brendan M. Crowley, Ian M. Bell, Andrew John Harvey, Brian T. Campbell, Thomas J. Greshock, Vanessa L. Rada
  • Biaryloxy derivatives as TTX-S blockers
    Patent number: 11020381
    Abstract: The present invention relates to biaryloxy derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channel is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: June 1, 2021
    Assignees: RaQualia Pharma Inc., XuanZhu Pharma Co., Ltd.
    Inventors: Kiyoshi Kawamura, Tatsuya Yamagishi, Yuji Shishido, Mikio Morita, Ryuichi Yamaguchi, Masashi Ohmi
  • Substituted pyridinone-containing trycyclic compounds, and methods using same
    Patent number: 11013726
    Abstract: The present invention includes substituted pyridinone-containing tricyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infection in a patient. In certain embodiments, the compounds and compositions of the invention inhibit and/or reduce HBsAg secretion.
    Type: Grant
    Filed: March 30, 2020
    Date of Patent: May 25, 2021
    Assignee: Arbutus Biopharma Corporation
    Inventors: Laurèn Danielle Bailey, Yingzhi Bi, Shuai Chen, Bruce D. Dorsey, Dimitar B. Gotchev, Richard James Holland, Ramesh Kakarla, Duyan Nguyen, Mark Christopher Wood
  • Octendidine based compounds
    Patent number: 11014907
    Abstract: The present invention discloses Octenidine based compounds of formula (A) or formula (B) and formula (C) where in, n=1, 2, 3, 4 and R?=un-substituted or substituted aryl or alkyl group; R is hydroxy or hydrogen, X is chlorine, bromine and iodine. The present invention also relates to a process for the preparation thereof.
    Type: Grant
    Filed: August 21, 2018
    Date of Patent: May 25, 2021
    Assignee: Dishman Carbogen Amcis Ltd.
    Inventors: Janmejay Rajnikant Vyas, Nilesh D. Patel
  • Compounds and pharmaceutical compositions containing at least one of the compounds
    Patent number: 11014918
    Abstract: The present disclosure is generally directed to the manufacture and use of compounds described herein for preventing, inhibiting or treating cancer, AIDS and/or premature aging, or the manufacture and use of a pharmaceutical composition comprising at least one of the compounds, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier for preventing, inhibiting or treating cancer, AIDS and/or premature aging.
    Type: Grant
    Filed: February 11, 2020
    Date of Patent: May 25, 2021
    Assignees: ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE DE MONTPELLIER
    Inventors: Jamal Tazi, Florence Mahuteau, Romain Najman, Didier Scherrer, Julien Santo
  • Process for the production of tetraaminobiphenol macrocyclic ligands; and novel tetraaminobiphenol macrocyclic ligands
    Patent number: 11014894
    Abstract: A process for preparing a tetra-substituted aminobiphenol macrocyclic ligand having the structure (I), comprising the step of treating a precursor compound having the structure (II) with a compound having the structure R6-L where L represents a leaving group (hereinafter compound (III)) in the presence of a base.
    Type: Grant
    Filed: March 2, 2018
    Date of Patent: May 25, 2021
    Assignee: ECONIC TECHNOLOGIES LIMITED
    Inventors: Michael Kember, Anthony Chartoire, Anthea Blackburn, Samuel Drane
  • Method of synthesizing (1S,12bS) lactam ester compound
    Patent number: 11008322
    Abstract: Disclosed herein is a method of synthesizing a (1S,12bS) lactam ester compound, including: subjecting a dihydrocarboline diester compound of formula (II) to asymmetric hydrogenation and lactamization in an organic solvent in the presence of an iridium catalyst precursor, a chiral diphosphine ligand and a halogen-containing reagent under hydrogen atmosphere to produce the (1S,12bS) lactam ester compound of formula (I), as shown in the following reaction scheme, where R1, R2 and R3 are defined in the same manner with the specification.
    Type: Grant
    Filed: April 7, 2020
    Date of Patent: May 18, 2021
    Assignee: Sichuan University
    Inventors: Fener Chen, Pei Tang, Wen Zhang, Lin Dong, Youcai Xiao
  • Synthesis of 5-hydroxymethylfurfural
    Patent number: 11008298
    Abstract: The present disclosure relates to a novel and improved synthesis of 5-hydroxymethylfurfural (HMF) from a glucose source. The synthesis of 5-hydroxymethylfurfural (HMF) is carried out by reacting a mixture comprising a Brønsted acid, a Lewis acid, water, dimethyl sulfoxide (DMSO), acetonitrile, and a glucose source.
    Type: Grant
    Filed: May 5, 2020
    Date of Patent: May 18, 2021
    Assignee: Purdue Research Foundation
    Inventors: Nathan Scott Mosier, Jonathan Christopher Overton
  • Compositions and methods for the treatment of chronic pain
    Patent number: 11000487
    Abstract: The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX, formula X, formula XI, formula XII, formula XIII, formula XIV and formula XV and the methods for the treatment of chronic pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of chronic pain.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: May 11, 2021
    Assignee: Cellix Bio Private Limited
    Inventor: Mahesh Kandula
  • Phenylpiperazine proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators and their use
    Patent number: 10980801
    Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.
    Type: Grant
    Filed: January 10, 2020
    Date of Patent: April 20, 2021
    Assignee: SRX Cardio, LLC
    Inventors: Thomas E. Barta, Jonathan William Bourne, Kyle D. Monroe, Michael M. Muehlemann, Anjali Pandey, Simeon Bowers
  • Inhibitors of interleukin-1 receptor-associated kinases and uses thereof
    Patent number: 10975055
    Abstract: The present invention provides novel compounds of Formula (I?), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma)), inflammatory diseases, autoinflammatory diseases, and autoimmune diseases in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as an interleukin-1 receptor-associated kinase (IRAK) (e.g., IRAKI and/or IRAK4) in the subject.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: April 13, 2021
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Tinghu Zhang, John Hatcher, Sara Jean Buhrlage
  • Blood-brain barrier-penetrant dopamine-?-hydroxylase inhibitors
    Patent number: 10975083
    Abstract: This invention relates to: (a) compounds of formula (I) (with R1 to R5, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-?-hydroxylase inhibitors; (b) pharmaceutical compositions comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: April 13, 2021
    Assignee: BIAL—PORTELA & CA, S.A.
    Inventors: Patrício Soares Da Silva, Tino Rossi, Laszlo Erno Kiss, Alexander Beliaev, Pedro Nuno Leal Palma
  • Perfluoropyridine derived aromatic monomers and processes of making and using same
    Patent number: 10975032
    Abstract: The present invention relates to perfluoropyridine derived aromatic monomers and processes of making and using same. Such monomers can be easily and selectively functionalized and yet still synthesized by an efficient and environmentally friendly pathway. In addition, such monomers can be used to produce polymers with highly satisfactory char yields.
    Type: Grant
    Filed: July 28, 2020
    Date of Patent: April 13, 2021
    Assignee: United States of America as represented by the Secretary of the Air Force
    Inventors: Scott T. Iacono, Matthew B Houck
  • Heterocyclic compound
    Patent number: 10975043
    Abstract: Provided is a heterocyclic compound having a superior RBP4-lowering action and useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4. A compound represented by the formula (I): wherein each symbol is as defined in the Description, or a salt thereof has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4.
    Type: Grant
    Filed: January 27, 2020
    Date of Patent: April 13, 2021
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Yoshihiro Banno, Masahiro Kamaura, Kazuaki Takami, Koichiro Fukuda, Shigekazu Sasaki
  • Compound, and production method thereof, and methods of treatment using the compound
    Patent number: 10975063
    Abstract: The manufacture of 8-chloro-N-[4-(trifluoromethoxy)phenyl]quinolin-2-amine, or a pharmaceutically acceptable salt thereof, and use of 8-chloro-N-[4-(trifluoromethoxy)phenyl]quinolin-2-amine, or a pharmaceutically acceptable salt thereof, for treating various conditions, and/or inhibiting replication of HIV-1 in a patient infected with HIV-1, by administering to a patient in need thereof an effective quantity of 8-chloro-N-[4-(trifluoromethoxy)phenyl]quinolin-2-amine, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 3, 2019
    Date of Patent: April 13, 2021
    Assignees: ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE DE MONTPELLIER
    Inventors: Florence Mahuteau, Romain Najman, Jamal Tazi
  • Aryl dihydropyridinones and piperidinone MGAT2 inhibitors
    Patent number: 10966967
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Grant
    Filed: May 21, 2020
    Date of Patent: April 6, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
  • Catalytic system for scalable preparation of indoxacarb
    Patent number: 10961206
    Abstract: It is an object of the present invention to provide a novel and advantageous process for commercially preparing of indoxacarb which is racemic or enantiomerically enriched at chiral center from its amide precursor using a new catalytic system. More particularly, it relates to an efficient method of preparation of indoxacarb which is racemic or enantiomerically enriched at chiral center from methyl-7-chloro-2,5-dihydro-2-[[[(4-tritluoromethoxy)phenyl]amino]carbonyl]-indeno[1,2-e][1,3,4]oxadiazine-4a(3H) carboxylate represented as formula (I) using methoxycarbonylation agent and metal salt of methylsulfinylmethylide in hydrocarbon solvent in the presence of organic base and phase transfer catalyst.
    Type: Grant
    Filed: March 27, 2018
    Date of Patent: March 30, 2021
    Assignee: Adama Makhteshim Ltd.
    Inventors: Rajuri Venkataramana, Jayapal Reddy Bicidi, Bijukumar Gopinathan Pillai, Sreedevi Mannam