Hetero Ring Is Six-membered And Includes Only One Ring Nitrogen Patents (Class 514/89)
  • Patent number: 11814405
    Abstract: The present invention relates to the technical field of biomedicine, particularly to a pyridine sulfonamide phosphate compound, a preparation method therefor, and a use thereof. The invention provides the following technical benefits: the pyridine sulfonamide phosphate compound has characteristics of high solubility, high stability, ease of being made into preparations, etc., which is easy to be industrially scaled up for medical use.
    Type: Grant
    Filed: February 18, 2022
    Date of Patent: November 14, 2023
    Assignee: Shanghai Xunhe Pharmaceutical Technology Co. Ltd.
    Inventors: Nongnong Wei, Hua Jin, Yongyong Zheng, Feng Zhou, Meihua Huang
  • Patent number: 11452702
    Abstract: Composition for promoting mitochondrial biogenesis and improving mitochondrial function in a subject, the composition comprising an active agent, said active agent containing the amino acids leucine, isoleucine, valine, threonine, lysine and citric acid, succinic acid, malic acid.
    Type: Grant
    Filed: July 20, 2018
    Date of Patent: September 27, 2022
    Assignee: Professional Dietetics International S.R.L.
    Inventor: Paolo Luca Maria Giorgetti
  • Patent number: 11382971
    Abstract: Disclosed are inhibitors of mevalonate pathway as an efficient vaccine adjuvant and use thereof. In particular, the inhibitor is an acetoacetyl-CoA transferase inhibitor, a HMG-CoA synthase inhibitor, a HMG-CoA reductase inhibitor, a mevalonate kinase inhibitor, a phosphomevalonate kinase inhibitor, a mevalonate-5-pyrophosphate decarboxylase inhibitor, an isopentenyl pyrophosphate isomerase inhibitor, a farnesyl pyrophosphate synthase inhibitor, a geranylgeranyl pyrophosphate synthase inhibitor or a geranylgeranyl transferase (I, II) inhibitor. Also disclosed is an immunogenic composition comprising inhibitors of mevalonate pathway as an adjuvant.
    Type: Grant
    Filed: September 8, 2016
    Date of Patent: July 12, 2022
    Assignee: Tsinghua University
    Inventors: Yonghui Zhang, Yun Xia, Yonghua Xie, Zhengsen Yu, Xiaoying Zhou, Xin Li, Liping Li, Yunyun Yang, Kanzhao Gao, Ke Wang, Wanli Liu, Meng Zhao
  • Patent number: 11260060
    Abstract: Methods, formulations and kits for treating and/or protecting against acute liver failure and other hepatotoxicities in an individual employ a combination of a first active agent which replenishes, or decreases a loss of, functional glutathione in the individual, and a second active agent comprising a manganese complex selected from the group consisting of (i) a calcium manganese mixed metal complex of N,N?-bis-(pyridoxal-5-phosphate)-ethylenediamine-N,N?-diacetic acid (DPDP) having a molar ratio of calcium to manganese in a range of from 1 to 10, or a pharmaceutically acceptable salt thereof, (ii) a mixture of manganese DPDP (MnDPDP), or a pharmaceutically acceptable salt thereof, and a non-manganese-containing DPDP compound, or (iii) a mixture of manganese pyridoxyl ethylenediamine (MnPLED), or a pharmaceutically acceptable salt thereof, and a non-manganese-containing pyridoxyl ethylenediamine (PLED) compound.
    Type: Grant
    Filed: January 10, 2017
    Date of Patent: March 1, 2022
    Assignee: EGETIS THERAPEUTICS AB
    Inventors: Jacques Näsström, Sven Jacobsson, Dennis Henriksen, James Van Alstine
  • Patent number: 11254659
    Abstract: The invention provides capsaicinoid prodrug compounds (e.g., prodrugs of resiniferatoxin, tinyatoxin, iodoresiniferatoxin, and related compounds), pharmaceutical compositions, and their use in the treatment of medical conditions, such as pain, and in agonizing TRPV1 activity.
    Type: Grant
    Filed: January 17, 2020
    Date of Patent: February 22, 2022
    Assignee: Centrexion Therapeutics Corporation
    Inventors: James N. Campbell, Scott M. Duncan
  • Patent number: 11192907
    Abstract: The present invention relates to a novel compound, to a composition comprising the same, to methods for preparing the compound, and the use of this compound in therapy. In particular, the present invention relates to a compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.
    Type: Grant
    Filed: October 25, 2019
    Date of Patent: December 7, 2021
    Assignees: QUANTUM GENOMICS, INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, COLLEGE DE FRANCE
    Inventors: Fabrice Balavoine, Delphine Compere, Catherine Llorens-Cortes, Yannick Marc
  • Patent number: 11161887
    Abstract: Described herein is the use of a uromodulin polypeptide in prevention or therapy of vascular calcification or a disease caused by, or related to, vascular calcification, particularly vascular calcification in chronic kidney disease, in diabetes, in aging and in atherosclerosis.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: November 2, 2021
    Assignee: CHARITÉ UNIVERSITÄTSMEDIZIN BERLIN
    Inventors: Jakob Völkl, Ioana Alesutan, Jürgen Scherberich
  • Patent number: 11021459
    Abstract: The present technology is directed to d-threo-methylphenidate conjugates and a composition comprising d-threomethylphenidate conjugated to nicotinoyl-L-serine, or salt thereof. The present technology also relates to a composition comprising at least one conjugate of d-methylphenidate having at least two or more chiral centers. The composition is optically active. The present technology additionally relates to oral formulations and pharmaceutical kits comprising at least one d-threo-methylphenidate conjugate. The pharmaceutical kit may comprise a specified amount of individual doses in a package. Each individual dose in the package may contain a pharmaceutically effective amount of a conjugate of d-threo methylphenidate.
    Type: Grant
    Filed: September 20, 2019
    Date of Patent: June 1, 2021
    Assignee: KemPharm, Inc.
    Inventors: Travis Mickle, Sven Guenther, Guochen Chi
  • Patent number: 11021460
    Abstract: The present technology is directed to d-threo-methylphenidate conjugates and a composition comprising d-threomethylphenidate conjugated to nicotinoyl-L-serine, or salt thereof. The present technology also relates to a composition comprising at least one conjugate of d-methylphenidate having at least two or more chiral centers. The composition is optically active. The present technology additionally relates to oral formulations and pharmaceutical kits comprising at least one d-threo-methylphenidate conjugate. The pharmaceutical kit may comprise a specified amount of individual doses in a package. Each individual dose in the package may contain a pharmaceutically effective amount of a conjugate of d-threo methylphenidate.
    Type: Grant
    Filed: September 20, 2019
    Date of Patent: June 1, 2021
    Assignee: KemPharm, Inc.
    Inventors: Travis Mickle, Sven Guenther, Guochen Chi
  • Patent number: 11014908
    Abstract: The invention relates to pyrazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to HbS modulators of formula (I) or tautomers thereof, or pharmaceutically acceptable salts of said modulators or tautomers thereof, wherein X, Y, R2 and R3 are as defined in the description. HbS modulators are potentially useful in the treatment of a wide range of disorders, including sickle cell disease (SCD).
    Type: Grant
    Filed: November 26, 2019
    Date of Patent: May 25, 2021
    Assignee: Pfizer Inc.
    Inventors: Ariamala Gopalsamy, Arjun Venkat Narayanan, Agustin Casimiro-Garcia, Chulho Choi, David Hepworth, David Walter Piotrowski, Hatice Gizem Yayla, Jayasankar Jasti, Lee Richard Roberts, Lyn Howard Jones, Mihir Dineshkumar Parikh, Ming Zhu Chen, Olugbeminiyi Omezia Fadeyi, Ralph Pelton Robinson, Jr., Robert Lee Dow, Shawn Cabral
  • Patent number: 10995085
    Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Grant
    Filed: March 16, 2020
    Date of Patent: May 4, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yongxin Han, Abdelghani Achab, Yongqi Deng, Xavier Fradera, Craig Gibeau, Brett A. Hopkins, Derun Li, Kun Liu, Meredeth A. McGowan, Nunzio Sciammetta, David Sloman, Catherine White, Hongjun Zhang, Hua Zhou
  • Patent number: 10954213
    Abstract: The present technology is directed to compositions comprising d-threo-methylphenidate conjugates and unconjugated methylphenidate. The present technology also relates to compositions and oral formulations comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to a pharmaceutical kit containing the composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 18, 2020
    Date of Patent: March 23, 2021
    Assignee: KemPharm, Inc.
    Inventors: Travis Mickle, Sven Guenther, Guochen Chi
  • Patent number: 10919874
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders, or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: July 31, 2019
    Date of Patent: February 16, 2021
    Assignee: NQP 1598, LTD.
    Inventors: William J. Hoekstra, Christopher M. Yates
  • Patent number: 10858341
    Abstract: The present technology is directed to compositions comprising d-threo-methylphenidate conjugates and unconjugated methylphenidate. The present technology also relates to compositions and oral formulations comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to a pharmaceutical kit containing the composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 18, 2020
    Date of Patent: December 8, 2020
    Assignee: KemPharm, Inc.
    Inventors: Travis Mickle, Sven Guenther, Guochen Chi
  • Patent number: 10772889
    Abstract: A liquid nutritional composition including 5-methyltetrahydrofolic acid (5-MTHF) is provided. The liquid nutritional composition also includes ascorbic acid and a protein system containing methionine to inhibit or reduce oxidation of the 5-MTHF and provide an active folate level of the liquid nutritional composition that remains stable over the shelf life of the liquid nutritional composition.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: September 15, 2020
    Assignee: ABBOTT LABORATORIES
    Inventors: Paul Johns, Jeffrey Baxter, Megan Terp, Normanella Dewille, Youngsuk Heo
  • Patent number: 10759778
    Abstract: The present technology is directed to compositions comprising d-threo-methylphenidate conjugates and unconjugated methylphenidate. The present technology also relates to compositions and oral formulations comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to a pharmaceutical kit containing the composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 4, 2019
    Date of Patent: September 1, 2020
    Assignee: KemPharm, Inc.
    Inventors: Travis Mickle, Sven Guenther, Guochen Chi
  • Patent number: 10695360
    Abstract: The present disclosure provides for the administration of ?-NMN, which increases the secretion of adiponectin. The present disclosure also provides an adiponectin secretion enhancer comprising ?-nicotinamide mononucleotide, a pharmaceutically acceptable salt thereof or a solvate thereof, and a dietary supplement containing the aforementioned secretion enhancer, which can be ingested in order to increase the secretion of adiponectin. Also disclosed are methods of treating insulin resistance-related diseases such as of metabolic syndrome, diabetes, hyperlipidemia, fatty liver disease, hypertension, obesity, and arteriosclerosis.
    Type: Grant
    Filed: February 15, 2018
    Date of Patent: June 30, 2020
    Assignee: Washington University
    Inventors: Jun Yoshino, Hisataka Yasuda, Hideo Arai, Tetsuro Enomoto
  • Patent number: 10662477
    Abstract: Disclosed herein are markers associated with sensitivity to treatment with therapeutic agents. Methods to identify markers for predicting outcome to treatment with a therapeutic agent are disclosed as well as methods to predict outcome of treatment using markers. Compositions and methods are provided to predict response to NAE inhibition or EGFR inhibition treatment.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: May 26, 2020
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Stephen J. Blakemore, Bin Li, Hyunjin Shin, William L. Trepicchio
  • Patent number: 10660851
    Abstract: A polyfunctional radical scavenger hydrogel formulation providing extended protection of the extracellular space within a wound site. The polyfunctional radical scavenger hydrogel formulation is generally formed from a hydrogel, a sterically hindered nitrone and a sterically hindered amine differing from nitrone with respect to at least one property. A portion of the nitrone included with the formulation and/or amine included within the formulation may be dissolved, suspended and/or bonded to a polymer of the hydrogel.
    Type: Grant
    Filed: January 2, 2015
    Date of Patent: May 26, 2020
    Assignee: RXOS MEDICAL
    Inventors: Richard Millis, Jeffrey Niezgoda, Rajagopalan Sridhar
  • Patent number: 10588884
    Abstract: The present disclosure provides, in part, modulators of prostate-specific G-protein receptor (OR51E2/PSGR) and methods of treating, preventing, and diagnosing prostate cancer using the same.
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: March 17, 2020
    Assignee: Duke University
    Inventors: Tatjana Abaffy, Hiro Matsunami
  • Patent number: 10442767
    Abstract: The present disclosure provides novel compounds, including compounds that bind to potassium channels, methods for their manufacture, and methods for their use, including their use to diagnose and/or assess traumatic brain injury and use to treat demyelinating diseases, and/or in vivo imaging of the central nervous system, and to diagnose and/or assess the progression of MS or other diseases.
    Type: Grant
    Filed: March 7, 2017
    Date of Patent: October 15, 2019
    Assignee: The University of Chicago
    Inventors: Pedro Brugarolas, Brian Popko, Daniel Appelbaum, Chin-Tu Chen
  • Patent number: 10370354
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: April 9, 2018
    Date of Patent: August 6, 2019
    Assignee: NQP 1598, LTD.
    Inventors: William J. Hoekstra, Christopher M. Yates
  • Patent number: 10350224
    Abstract: A stabilized formulation for controlled release of a vitamin D compound is disclosed. The formulation comprises one or both of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3 and a cellulosic compound. The stabilized formulations exhibit a stable dissolution profile following exposure to storage conditions and demonstrate improved pharmacokinetic parameters compared to unstabilized formulations.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: July 16, 2019
    Assignee: OPKO IRELAND GLOBAL HOLDINGS, LTD.
    Inventors: Jay A. White, Samir P. Tabash, Sammy A. Agudoawu, Joel Z. Melnick
  • Patent number: 10154971
    Abstract: Methods of nighttime administration of amantadine to reduce sleep disturbances in patient undergoing treatment with amantadine are described, as well as compositions of extended release amantadine that are suitable for nighttime administration.
    Type: Grant
    Filed: June 17, 2014
    Date of Patent: December 18, 2018
    Assignee: Adamas Pharma, LLC
    Inventors: Gregory T. Went, Timothy J. Fultz, Natalie McClure
  • Patent number: 10112963
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: October 30, 2018
    Assignee: Novartis AG
    Inventors: David Weninger Barnes, Scott Louis Cohen, Dean Franklin Rigel
  • Patent number: 10106565
    Abstract: Dendrimers with monophosphonic or bisphosphonic terminations for the treatment of inflammatory diseases.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: October 23, 2018
    Assignees: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), UNIVERSITE PAUL SABATIER (TOULOUSE III)
    Inventors: Mary Poupot, Remy Poupot, Jean-Jacques Fournie, Damien Portevin, Severine Fruchon, Jean-Luc Davignon, Cedric-Olivier Turrin, Anne-Marie Caminade, Jean-Pierre Majoral, Olivier Rolland
  • Patent number: 10098353
    Abstract: The present disclosure provides compositions comprising Root-Knot Nematode (RKN)-active Methylobacterium sp., methods for controlling RKN infections of plants, and methods of making the compositions.
    Type: Grant
    Filed: November 15, 2016
    Date of Patent: October 16, 2018
    Assignee: NEWLEAF SYMBIOTICS, INC.
    Inventors: Natalie Breakfield, Gregg Bogosian
  • Patent number: 10046082
    Abstract: Provided are a collagen sponge containing a drug for promoting fracture healing and a method for preparing the same, the method comprises the steps of: 1) adding bisphosphonate containing phosphonate radical in an equivalent dosage of 70 to 140 mg and/or strontium salt in a dosage of 100 to 800 mg into 1 kg of the enzymolysis solution of collagen; 2) adding a crosslinking agent into the solution, the crosslinking agent being added in a proportion where 40 to 60 U of crosslinking agent is added per gram of enzymolysis solution; 3) stirring the mixed solution in step 2) uniformly, then putting it into a stainless steel tray, and placing the tray in a vacuum lyophilizer for lyophilizing for 10 to 16 hours so that it is lyophilized into a sponge-like shape; and 4) allowing the collagen sponge in step 3) to be cut, packaged and sealed, and sterilized by irradiation with cobalt 60.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: August 14, 2018
    Assignee: WUHAN VSD MEDICAL SCIENCE & TECHNOLOGY CO., LTD.
    Inventors: Yansong Liu, Yingze Zhang, Zhidao Xia, Hongxia Guan
  • Patent number: 10010559
    Abstract: Use of a derivative containing C—O—P bonds in a controlled release form to treat patients with kidney failure. Moreover, it comprises the use of said derivatives together with other active substances, which particularly may be selected from a list comprising a calcimimetic, vitamin, phosphate binder, thiosulfate, bisphosphonate, pyrophosphate, citrate, diuretic, antihypertensive and anticholesteraemic agent.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: July 3, 2018
    Assignee: LABORATORIOS SANIFIT, S.L.
    Inventors: Joan Perello Bestard, Carolina Salcedo Roca, Miguel David Ferrer Reynes, Bernat Isern Amengual, Pieter H. Joubert
  • Patent number: 9896431
    Abstract: The present invention provides compounds of Formula (I): a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, a solvate 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 23, 2017
    Date of Patent: February 20, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventor: Saleem Ahmad
  • Patent number: 9707198
    Abstract: Composition for use in the treatment of stroke, particularly in patients with dysphagia, the composition comprising an active agent, said active agent comprising the amino acids leucine, isoleucine, valine, lysine, threonine and at least one of histidine, phenylalanine, methionine, tryptophan, tyrosine, cystine. The composition further comprises one or more thickener agents in an amount between 10% and 50% by weight, more preferably between 20% and 30% by weight, with respect to the active agent weight.
    Type: Grant
    Filed: October 8, 2015
    Date of Patent: July 18, 2017
    Assignee: Professional Deitetics S.p.A.
    Inventor: Paolo Luca Maria Giorgetti
  • Patent number: 9688656
    Abstract: The present invention provides compounds of Formula (I): a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, a solvate 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: March 5, 2015
    Date of Patent: June 27, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventor: Saleem Ahmad
  • Patent number: 9649321
    Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
    Type: Grant
    Filed: November 16, 2015
    Date of Patent: May 16, 2017
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle
  • Patent number: 9617215
    Abstract: The present disclosure provides novel compounds, including compounds that bind to potassium channels, methods for their manufacture, and methods for their use, including their use to diagnose and/or assess traumatic brain injury and use to treat dymeylinating diseases, and/or in vivo imaging of the central nervous system, and to diagnose and/or assess the progression of MS or other diseases.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: April 11, 2017
    Assignee: THE UNIVERSITY OF CHICAGO
    Inventors: Pedro Brugarolas, Brian Popko, Daniel Appelbaum, Chin-Tu Chen
  • Patent number: 9579335
    Abstract: The invention described herein pertains to the treatment of cystic diseases. More particularly, the invention described herein relates to methods for treating cystic disease using one or more lysophosphatidic acid antagonists, TMEM16a inhibitors, and/or peroxisome proliferator-activated receptor modulators.
    Type: Grant
    Filed: September 14, 2015
    Date of Patent: February 28, 2017
    Assignee: Indiana University Research and Technology Corporation
    Inventor: Bonnie Blazer-Yost
  • Patent number: 9480693
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Grant
    Filed: September 10, 2015
    Date of Patent: November 1, 2016
    Assignee: NOVARTIS AG
    Inventors: David Weninger Barnes, Scott Louis Cohen, Dean Franklin Rigel
  • Patent number: 9346836
    Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula I: (I) wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyper-proliferative disorders, also are disclosed.
    Type: Grant
    Filed: July 10, 2014
    Date of Patent: May 24, 2016
    Assignee: ZIOPHARM Oncology, Inc.
    Inventor: Lee R. Morgan
  • Patent number: 9340565
    Abstract: Preparation and characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.
    Type: Grant
    Filed: November 23, 2011
    Date of Patent: May 17, 2016
    Assignee: THAR PHARMACEUTICALS, INC.
    Inventors: Mazen Hanna, Ning Shan, Miranda L. Cheney, David R. Weyna, Paul K. Isbester, Xufeng Sun
  • Patent number: 9320270
    Abstract: Microencapsulated formulations of macrolide lactones (abamectin, milbemectin, milbemycins emamectin, avermectins, ivermectins) wherein the active ingredient is protected from UV-degradation, with exceptional release characteristics resembling those of an emulsion concentrate or, if desired, of long-lasting effect; further with appropriate rheological properties, and with reduced toxicity. The invention provides a unique microencapsulation process for the chemical stability and biological activity of mectins, e.g. abamectin, and provides microcapsules of mectins to be used in formulations CS, WG/CS, ZC, EC/CS and any formulation type containing microcapsules and combination with other biologically active ingredients.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: April 26, 2016
    Inventors: Victor Casana Giner, Miguel Gimeno Sierra, Barbara Gimeno Sierra
  • Patent number: 9243014
    Abstract: A prodrug can have a structure of Formula 10 or derivative thereof or stereoisomer thereof or pharmaceutically acceptable salt thereof. The prodrug can be included in a pharmaceutical composition for use in treatment of fungus, cancer, dermatitis, superficial mycoses; inflammation, tinea pedis, tinea cruris, and tinea corporis, Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis, candidiasis (moniliasis), Candida albicans, tinea (pityriasis) vesicolor, Malassezia furfur, acute myeloid leukemia, acute lymphoid leukemia, chronic myelogenous leukemia, lymphoma or multiple myeloma.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: January 26, 2016
    Assignee: The University of Kansas
    Inventors: Mehmet Tanol, Scott J. Weir
  • Patent number: 9216204
    Abstract: The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.
    Type: Grant
    Filed: October 25, 2013
    Date of Patent: December 22, 2015
    Assignee: MBC PHARMA, INC.
    Inventors: Alexander Karpeisky, Shawn Patrick Zinnen
  • Patent number: 9200021
    Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) catalyst compositions comprising phosphacycle ligands; and (c) methods of using such phosphacycle ligands and catalyst compositions in bond forming reactions.
    Type: Grant
    Filed: February 2, 2015
    Date of Patent: December 1, 2015
    Assignee: AbbVie Inc.
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Patent number: 9187424
    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: June 16, 2014
    Date of Patent: November 17, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Dong Cheng, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
  • Patent number: 9181186
    Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
    Type: Grant
    Filed: February 12, 2013
    Date of Patent: November 10, 2015
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata
  • Patent number: 9163040
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: October 20, 2015
    Assignee: NOVARTIS AG
    Inventors: David Weninger Barnes, Scott Louis Cohen, Dean Franklin Rigel
  • Patent number: 9155750
    Abstract: This invention relates to a composition that comprises inositol phosphates and/or bisphosphonates, and to the use thereof to prevent the loss of substances of biological interest in the body of patients subjected to dialysis and to maintain sufficient physiological levels of said substances to regulate physiological and/or pathological processes, these substances being inhibitors of pathological crystallization.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: October 13, 2015
    Assignee: Universitat de les Illes Balears
    Inventors: Félix Grases Freixedas, Joan Perello Bestard, Fernando Tur Espinosa, Antonia Costa Bauza, Rafael M. Prieto Almirall, Isabel Gomila Muñiz
  • Patent number: 9125412
    Abstract: Insect controlling compositions including an N-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximine compound exhibiting increased stability, along with methods for preparing same, are disclosed.
    Type: Grant
    Filed: July 1, 2014
    Date of Patent: September 8, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Kuide Qin, Raymond E. Boucher, Jr.
  • Patent number: 9089484
    Abstract: The present invention provides pharmaceutical compositions for oral administration comprising a therapeutically effective amount of a selective factor Xa inhibitor or a pharmaceutically acceptable salt thereof and an enhancer, wherein the enhancer is a medium chain fatty acid or a salt, ester, ether, or derivative of a medium chain fatty acid and has a carbon chain length of from about 4 to about 20 carbon atoms. The present invention also provides a method for obtaining a reproducible bioavailability of selective factor Xa inhibitor in an object after oral administration comprising orally administering a pharmaceutical composition as described above.
    Type: Grant
    Filed: March 28, 2011
    Date of Patent: July 28, 2015
    Assignee: Merrion Research III Limited
    Inventors: Thomas W. Leonard, David C. Coughlan, Alan Cullen
  • Patent number: 9073894
    Abstract: The present invention provides novel phenicol derivatives of formula I their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: July 7, 2015
    Assignee: Zoetis Services LLC
    Inventors: Richard A. Ewin, Timothy Allan Johnson, Susan M. K. Sheehan
  • Publication number: 20150148312
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 28, 2015
    Inventors: Herriot Tabuteau, Graeme Jones