At Imidazole Ring Carbon Patents (Class 514/400)
  • Patent number: 10550089
    Abstract: The present application relates to certain substituted imidazole and triazole compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating pain, musculoskeletal inflammation, neuroinflammatory disorders, airway inflammation, itch, dermatitis, colitis and related conditions. The compounds are of Formula (I) where X is N or CH, Z and Y are N or C (but both not N) and R1-R3 are as defined herein.
    Type: Grant
    Filed: May 11, 2017
    Date of Patent: February 4, 2020
    Assignee: Heptares Therapeutics Limited
    Inventors: John Graham Cumming, Frank Xinhe Wu, Karl Henrik Edman, Hongming Chen, Dean Gordon Brown, Roland Werner Burli, Shawn Donald Johnstone, Giles Albert Brown, Benjamin Gerald Tehan, Barry John Teobald, Miles Stuart Congreve
  • Patent number: 10435376
    Abstract: Disclosed are derivatives of 1H-imidazole-4,5-dicarboxamide and use thereof in preparation of anticoccidial drugs. The derivatives have structural formulae as shown in formulae (I) to (VI). The derivatives of 1H-imidazole-4,5-dicarboxamide as disclosed in the present invention have significant anticoccidial effect, especially against coccidia that show a resistance to other anticoccidial drugs, and thus they can be used in preparation of anticoccidial drug.
    Type: Grant
    Filed: November 26, 2015
    Date of Patent: October 8, 2019
    Assignee: GUANGZHOU INSIGHTER BIOTECHNOLOGY CO., LTD.
    Inventors: Xianfeng Peng, Zonghua Qin
  • Patent number: 10390553
    Abstract: Ingesting a food etc. which is in a unit package form per meal and contains, in the unit, not less than 0.3 g of histidine as an ingestion amount per meal is effective for improving mental energy and biorhythm.
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: August 27, 2019
    Assignee: AJINOMOTO CO., INC.
    Inventors: Tetsuro Shibakusa, Mayu Sugita, Ikuko Sasahara, Naoto Koyama, Shinobu Seki
  • Patent number: 10342826
    Abstract: The present invention concerns the use of a combination consisting of D-aspartic and L-aspartic acids or L-aspartic acid used alone to stimulate the procreative activity in the man by increment of spermatozoon number and motility.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: July 9, 2019
    Assignee: MERCK SERONO S.P.A.
    Inventors: Salvatore D'Aniello, Enrico D'Aniello
  • Patent number: 10028935
    Abstract: Disclosed are novel stable compounds having anti-oxidant properties and methods of using the compounds for the treatment of diseases or injuries associated with oxidative stress.
    Type: Grant
    Filed: January 31, 2017
    Date of Patent: July 24, 2018
    Assignee: XPD Holdings, LLC
    Inventors: Marc Bailie, Steven K. Duddy, Jim Herman
  • Patent number: 9931371
    Abstract: A method and a pharmaceutical composition for increasing wound healing in an individual in need thereof, the method comprising administering an angiopoietin like 4 (ANGPTL4) polypeptide or a therapeutically active fragment thereof.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: April 3, 2018
    Assignee: Nanyang Technologies University
    Inventors: Nguan Soon Tan, Han Chung Kelvin Chong
  • Patent number: 9907770
    Abstract: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: March 6, 2018
    Assignee: Natural Alternatives International, Inc.
    Inventors: Roger Harris, Mark Dunnett
  • Patent number: 9895344
    Abstract: Novel compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of 7,8-dihydroxyflavone or derivative thereof. Specifically, methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of 7,8-dihydroxyflavone or a derivative thereof. A further method of promoting neuroprotection in a subject also is provided, which includes selecting a subject in need of neuroprotection, and administering to the subject a therapeutically effective amount of 7,8-dihydroxyflavone or a derivative thereof.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: February 20, 2018
    Assignee: EMORY UNIVERSITY
    Inventor: Keqiang Ye
  • Patent number: 9808444
    Abstract: Several embodiments provided herein relate to histamine dosing regimens are and uses of such regimens in the restoration of histamine balance in subjects suffering from, for example, histapenia and/or histadelia. Several embodiments also relate to the use of histamine dosing regimens for the treatment and/or prevention of migraine headaches.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: November 7, 2017
    Assignee: BioHealthonomics Inc.
    Inventor: Cristian Arnou
  • Patent number: 9789125
    Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.
    Type: Grant
    Filed: June 2, 2016
    Date of Patent: October 17, 2017
    Assignee: Allergan Holdings Unlimited Company
    Inventors: Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
  • Patent number: 9700548
    Abstract: The present invention provides combinations comprising a sedating antihistamine and selected indole-based natural products such as L-tryptophan, 5-hydroxytryptophan and melatonin, along with pharmaceutically acceptable calcium and magnesium salts and selected B vitamins. These combinations are useful in providing a medicament for improving sleep in mammals, especially humans.
    Type: Grant
    Filed: June 8, 2012
    Date of Patent: July 11, 2017
    Assignee: REQUIS PHARMACEUTICALS INC.
    Inventors: Lars Jacob Stray Knutsen, Judi Lois Knutsen
  • Patent number: 9668994
    Abstract: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.
    Type: Grant
    Filed: March 30, 2015
    Date of Patent: June 6, 2017
    Assignee: Natural Alternatives International, Inc.
    Inventors: Roger Harris, Mark Dunnett
  • Patent number: 9669010
    Abstract: A method of treating chronic kidney disease by administering to a subject a composition that includes L-arginine, glycine, L-glutamine, L-histidine, L-aspartic acid L-glutamic acid, and L-carnosine.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: June 6, 2017
    Assignee: Bio Health Solutions, LLC
    Inventor: James Archer
  • Patent number: 9629800
    Abstract: The present invention concerns gastroretentive formulation comprising an active substance granulated with a mixture of a weak gelling agent, a strong gelling agent, and a gas generating agent and process for manufacturing said formulation.
    Type: Grant
    Filed: July 19, 2006
    Date of Patent: April 25, 2017
    Assignee: ETHYPHARM
    Inventors: Mahendra Chaudhari, Omprakash D. Chandwani, Rajashree S. Yelegaonkar
  • Patent number: 9539278
    Abstract: It has been found that high amounts of aspartate equivalents in combination with vitamin B12 and/or biotin, especially in relative absence of glutamate equivalents, improve the metabolism of ketobodies and/or lactate in a mammal's body, especially in diseased or traumatic conditions. As a result, levels of ketobodies and lactate can be decreased and unphysicologically high acidity normalised. Thus, it is an object of the invention to provide an enteral nutritional or a pharmaceutical composition for the treatment and/or prevention of disturbed ketone and lactate metabolism, i.e. elevated concentrations of ketone bodies, lactate and/or other organic acids and/or insufficient pH homeostasis, especially elevated concentrations of ketone bodies and/or lactate, in a mammal's blood, wherein the composition comprises high amounts of aspartate equivalents in combination with vitamin B12 and/or biotin, preferably in relative absence of glutamate equivalents.
    Type: Grant
    Filed: October 16, 2014
    Date of Patent: January 10, 2017
    Assignee: N.V. Nutricia
    Inventor: Robert Johan Joseph Hageman
  • Patent number: 9511054
    Abstract: Several embodiments provided herein relate to histamine dosing regimens are and uses of such regimens in the restoration of histamine balance in subjects suffering from, for example, histapenia and/or histadelia. Several embodiments also relate to the use of histamine dosing regimens for the treatment and/or prevention of migraine headaches.
    Type: Grant
    Filed: April 10, 2015
    Date of Patent: December 6, 2016
    Assignee: BioHealthonomics Inc.
    Inventor: Cristian Arnou
  • Patent number: 9504673
    Abstract: The invention relates to an agent for the treatment and/or prophylaxis of highly pathogenic infectious diseases, such as highly pathogenic influenza A (in particular, subtypes H5 and H7) and severe acute respirator syndrome caused by the genotype IV coronavirus. The agent is in the form of glutaryl histamine or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition based on glutaryl histamine or a pharmaceutically acceptable salt thereof and to a method for the treatment and/or prophylaxis of highly pathogenic infectious diseases.
    Type: Grant
    Filed: May 10, 2010
    Date of Patent: November 29, 2016
    Assignee: LTD “Valenta-Intellekt”
    Inventors: Vladimir Evgenievich Nebolsin, Galina Alexandrovna Zheltukhina, Sergey Vladimirovich Borisevich, Svetlana Yakovlevna Loginova, Alexander Grigorievich Chuchalin
  • Patent number: 9500660
    Abstract: The present invention relates generally to the field of nutrition and health. In particular, the present invention relates to a new biomarker, its use and a method that allows it to diagnose the likelihood to resist diet induced weight gain, and/or to be susceptible to a diet induced weight gain. For example, the biomarker may be isovalerylglycine.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: November 22, 2016
    Assignee: Nestec S.A.
    Inventors: Francois-Pierre Martin, Claire L. Boulange, Ivan Montoliu Rora, Sebastiano Collino, Marc-Emmanuel Dumas, Elaine Holmes, Serge Andre Dominique Rezzi, Jeremy Nicholson, Sunil Kochhar
  • Patent number: 9480669
    Abstract: Disclosed is a method comprising the administration of a 3% amino acid and 3% glycerin solution for the use of prevention and disruption of bacterial biofilms. Also disclosed is method comprising the administration of L-cysteine 0.4 g per 100 ml for the prevention and destruction of fungal biofilms.
    Type: Grant
    Filed: January 6, 2015
    Date of Patent: November 1, 2016
    Assignee: The Regents of The University of California
    Inventors: Thomas Benedict Bryan, Clarissa J. Nobile
  • Patent number: 9447112
    Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 me
    Type: Grant
    Filed: June 1, 2015
    Date of Patent: September 20, 2016
    Assignee: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Patent number: 9421267
    Abstract: Provided herein, in part, is a method of treating a neurological or movement disorder in a patient in need thereof, comprising subcutaneously administering to said patient a pharmaceutically acceptable composition comprising levodopa and optionally carbidopa and optionally entacapone or tolcapone, or pharmaceutically acceptable salts thereof, wherein said composition is administered substantially continuously, and compositions that can be used in the disclosed methods.
    Type: Grant
    Filed: November 15, 2011
    Date of Patent: August 23, 2016
    Assignee: NeuroDerm, Ltd.
    Inventors: Oron Yacoby-Zeevi, Mara Nemas
  • Patent number: 9364489
    Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.
    Type: Grant
    Filed: July 22, 2015
    Date of Patent: June 14, 2016
    Assignee: Forest Tosara Limited
    Inventors: Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
  • Patent number: 9351960
    Abstract: The invention relates to medicine and comprises an agent for the treatment of a viral hepatitis C, which is glutaryl histamine or a pharmaceutically acceptable salt thereof. This agent can also be administered in combination with a pegylated interferon and ribavirin. The invention further relates to a pharmaceutical composition for the treatment of a viral hepatitis C. This invention solves the problem of providing a novel agent, which is effective in the treatment of a viral hepatitis C and makes it possible to produce a sustained virologic response.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: May 31, 2016
    Assignee: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”
    Inventors: Vladimir Evgenievich Nebolsin, Dmitry Yurievich Konstantinov, Larisa Leonidovna Popova, Elena Alekseevna Strebkova, Petr Grigorievich Deryabin
  • Patent number: 9295649
    Abstract: The present disclosure relates in part to pharmaceutical compositions comprising polymeric nanoparticles having certain glass transition temperatures. Other aspects of the invention include methods of making such nanoparticles.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: March 29, 2016
    Assignee: BIND Therapeutics, Inc.
    Inventors: Mir Mukkaram Ali, Abhimanyu Sabnis, David Dewitt, Greg Troiano, James Wright, Maria Figueiredo, Michael Figa, Christina Van Geen Hoven, Young-Ho Song, Jason Auer, Tarikh Christopher Campbell
  • Patent number: 9193690
    Abstract: Disclosed herein is a pharmaceutical composition comprising (3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl)methanol and methods of using the composition to treat chronic pain.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: November 24, 2015
    Assignee: Allergan, Inc.
    Inventor: Daniel W. Gil
  • Patent number: 9150514
    Abstract: The invention is directed to methods for treating hypertension or heart failure using compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. In particular embodiments, the invention uses compounds having formula IIIa, IVa, Va: These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity.
    Type: Grant
    Filed: October 23, 2014
    Date of Patent: October 6, 2015
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Patent number: 9115091
    Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.
    Type: Grant
    Filed: August 14, 2014
    Date of Patent: August 25, 2015
    Assignee: FURIEX PHARMACEUTICALS, INC.
    Inventors: Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
  • Patent number: 9045434
    Abstract: A compound and method for treating myocilin glaucoma using a selective Grp94 inhibitor is presented. Clearance of mutant myocilin can be promoted by selectively targeting the endoplasmic reticulum (ER) chaperone Grp94 using siRNA knockdown or small molecule inhibitors. Grp94 contributes to the intracellular accumulation of mutant myocilin. Tailored treatments aimed at disrupting the Grp94/mutant myocilin interaction can be used as a new therapeutic strategy for myocilin glaucoma. The inventors developed a compound having a general backbone structure of geldanamycin (GDA) and radicicol (RDC) in which a more hydrophobic surrogate of the quinone in GDA is linked to the resorcinol in RDC through a cis-amide bioisostere.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: June 2, 2015
    Assignees: University of South Florida, The University of Kansas
    Inventors: Chad Anthony Dickey, Amirthaa Suntharalingam, Brian S. J. Blagg
  • Publication number: 20150148395
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Applicant: ALLERGAN, INC.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20150147309
    Abstract: The present invention relates to an allosteric non-inhibitory chaperone of the lysosomal acid alpha-glucosidase (GAA) for use in the treatment of a pathological condition characterized by a deficiency of the lysosomal acid alpha-glucosidase (GAA), to pharmaceutical composition thereof, to a method for increasing the activity of GAA in a subject and to a method for identifying an allosteric non-inhibitory chaperone for GAA.
    Type: Application
    Filed: June 6, 2013
    Publication date: May 28, 2015
    Inventors: Giancarlo Parenti, Caterina Porto, Marco Moracci, Maria Carmina Ferrara, Beatrice Cobucci-Ponzano, Generoso Andria
  • Publication number: 20150148394
    Abstract: The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Inventors: Mohammed I. Dibas, Daniel W. Gil, John E. Donnello, Ken Chow, Liming Wang, Michael E. Garst
  • Patent number: 9040563
    Abstract: Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I).
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: May 26, 2015
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Yale University
    Inventors: Said M. Sebti, Andrew Hamilton
  • Publication number: 20150133370
    Abstract: The present invention relates to dietary compositions comprising reduced level of methionine, tryptophan, all amino acids, or protein, dietary compositions comprising glycerol as a substitute for monosaccharides, disaccharides, and polysaccharides, and hypocaloric or calorie free diets with reduced level of energy, carbohydrates, or protein. Also disclosed are methods of using these compositions and diets, as well as fasting, to protect subjects against chemotherapy, radiotherapy, oxidative stress, or aging.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 14, 2015
    Inventor: Valter Longo
  • Publication number: 20150126571
    Abstract: Disclosed is a method comprising the administration of a 3% amino acid and 3% glycerin solution for the use of prevention and disruption of bacterial biofilms. Also disclosed is method comprising the administration of L-cysteine 0.4 g per 100 ml for the prevention and destruction of fungal biofilms.
    Type: Application
    Filed: January 6, 2015
    Publication date: May 7, 2015
    Inventor: THOMAS BENEDICT BRYAN
  • Publication number: 20150126437
    Abstract: The disclosure provides compounds useful as insect repellents, compositions comprising such repellents, and methods of repelling an arthropod using such compounds and compositions. The disclosure further provides insect traps and method for identifying ligands and cognates for biological molecules.
    Type: Application
    Filed: October 17, 2012
    Publication date: May 7, 2015
    Applicant: The Regents of the University of California
    Inventors: Anandasankar Ray, Sean Michael Boyle
  • Patent number: 9023881
    Abstract: Several embodiments provided herein relate to histamine dosing regimens are and uses of such regimens in the restoration of histamine balance in subjects suffering from, for example, histapenia and/or histadelia. Several embodiments also relate to the use of histamine dosing regimens for the treatment and/or prevention of migraine headaches.
    Type: Grant
    Filed: June 25, 2014
    Date of Patent: May 5, 2015
    Assignee: BioHealthonomics Inc.
    Inventor: Cristian Arnou
  • Patent number: 9018241
    Abstract: Hetero-substituted acetanilide derivatives are disclosed as analgesic agents. The compounds of the invention are useful in methods for treating a disease or condition in a mammal characterized by pain and/or fever.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: April 28, 2015
    Assignee: Janssen Pharmaceutica, NV
    Inventors: John R. Carson, James J. McNally
  • Patent number: 9006249
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n 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 a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: April 14, 2015
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Publication number: 20150094317
    Abstract: The invention provides improved methods for coadministration of colchicine with drugs metabolized by CYP3A4 (anciently referred to as cytochrome P450 isozyme 3A4) or the P-glycoprotein transporter, but not both. The method enables non-toxic coadministration of colchicine and the second drug at their ordinary levels safely and effectively without reducing the dose or frequency for either drug.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 2, 2015
    Applicant: Hikma Pharmaceuticals LLC
    Inventor: Murray DUCHARME
  • Publication number: 20150094318
    Abstract: The invention provides improved methods for coadministration of colchicine with drugs metabolized by CYP3A4 (anciently referred to as cytochrome P450 isozyme 3A4) or the P-glycoprotein transporter, but not both. The method enables non-toxic coadministration of colchicine and the second drug at their ordinary levels safely and effectively without reducing the dose or frequency for either drug.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 2, 2015
    Applicant: HIKMA PHARMACEUTICALS LLC
    Inventor: Murray Ducharme
  • Publication number: 20150094343
    Abstract: The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as inhibitors of Jak2/STAT3 pathways and downstream targets and inhibit the growth and survival of cancerous cell lines.
    Type: Application
    Filed: June 4, 2014
    Publication date: April 2, 2015
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Waldemar PRIEBE, Izabela FOKT, Slawomir SZYMANSKI, Timothy MADDEN, Jeffrey MYERS, Charles CONRAD
  • Patent number: 8993611
    Abstract: The invention relates to a family of stable polyamine arylethylamide compounds, and to the use of these compounds as agents inhibiting DNA damages induced by by-products of the non-enzymatic glycosylation of skin tissues. The invention also relates to cosmetic or dermocosmetic compositions intended to fight skin disorders associated with said glycosylation by-products.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: March 31, 2015
    Assignee: Exsymol
    Inventor: Marie-Christine Seguin
  • Patent number: 8993610
    Abstract: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: March 31, 2015
    Assignee: Natural Alternatives International, Inc.
    Inventors: Roger Harris, Mark Dunnett
  • Publication number: 20150087677
    Abstract: The present invention relates to a method for treating platinum drugs induced vestibulotoxicity, comprising administering a compound that impairs or prevents accumulation of platinum drugs within vestibular hair cells and/or vestibular primary neurons.
    Type: Application
    Filed: November 28, 2014
    Publication date: March 26, 2015
    Inventor: Sophie Gaboyard-Niay
  • Patent number: 8987316
    Abstract: The present invention relates to novel isocyanate and isothiocyanate compounds, to pharmaceutical compositions comprising them, and to the use thereof in the treatment of cancer diseases in humans and animals. The novel isocyanate and isothiocyanate compounds are distinguished, as compared with the known isocyanate and isothiocyanate compounds, by improved therapeutical breadth, i.e. fewer side effects while having high anti-tumor activity.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: March 24, 2015
    Assignee: DoubleHill GmbH
    Inventor: Jochen Kalbe
  • Publication number: 20150080445
    Abstract: Disclosed herein is a pharmaceutical composition comprising (3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl)methanol and methods of using the composition to treat chronic pain.
    Type: Application
    Filed: November 21, 2014
    Publication date: March 19, 2015
    Inventor: Daniel W. Gil
  • Patent number: 8980933
    Abstract: The present invention relates to specific analogs of combretastatin, in particular the compounds of formula (I) as described and defined herein, and pharmaceutical compositions comprising the compounds, as well as their medical use, in particular in the treatment or prevention of cancer, including multidrug-resistant cancer.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: March 17, 2015
    Assignees: Universitat Bayreuth, Martin-Luther-Universitat Halle-Wittenberg
    Inventors: Rainer Schobert, Bernhard Biersack, Thomas Müller
  • Patent number: 8980868
    Abstract: Novel solution complexes of zoledronic acid are described which give rise to improved properties of zoledronic acid. The invention includes aqueous solution and molecular complexes of zoledronic acid with and optical isomers of asparagine, histidine, arginine and proline as well as pharmaceutical complexes containing them and methods of treatment using them.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: March 17, 2015
    Assignee: Thar Pharmaceuticals, Inc.
    Inventors: Mazen Hanna, Ning Shan, Miranda Cheney, David Weyna
  • Publication number: 20150065543
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: October 23, 2014
    Publication date: March 5, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Publication number: 20150064135
    Abstract: The invention relates to medicine and comprises an agent for the treatment of a viral hepatitis C, which is glutaryl histamine or a pharmaceutically acceptable salt thereof. This agent can also be administered in combination with a pegylated interferon and ribavirin. The invention further relates to a pharmaceutical composition for the treatment of a viral hepatitis C. This invention solves the problem of providing a novel agent, which is effective in the treatment of a viral hepatitis C and makes it possible to produce a sustained virologic response.
    Type: Application
    Filed: March 13, 2013
    Publication date: March 5, 2015
    Inventors: Vladimir Evgenievich Nebolsin, Dmitry Yurievich Konstantinov, Larisa Leonidovna Popova, Elena Alekseevna Strebkova, Petr Grigorievich Deryabin