Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/453)
  • Patent number: 10322097
    Abstract: A quinonemethide triterpenoid is administered to subjects with multidrug-resistant cancer, in particular a cancer with enhanced expression and/or functional activity of ABC transporter proteins such as P-glycoprotein and/or an apoptosis-deficient, in particular p53-, Bax- or Bak-deficient, cancer, i.e. specific subgroups of subjects with cancer. The quinonemethide triterpenoid is suitable to treat cancer allowing for an accumulation of cytotoxic or therapeutic compounds in the cells while having exceptionally increased cytotoxic activity towards the multidrug-resistant cancer cells and while allowing for an increased activity of chemotherapeutic compounds. Methods for specifically targeting cancer cells with multidrug-resistance and methods for potentiating the activity of a chemotherapeutic compound in those cancer cells are also disclosed. A kit including a quinonemethide triterpenoid and a chemotherapeutic compound is also provided.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: June 18, 2019
    Inventors: Kam Wai Wong, Yuen Kwan Law, Thomas Efferth, Su-Wei Xu, Sami Hamdoun, Liang Liu
  • Patent number: 10266545
    Abstract: The present invention discloses the novel coumarin derivative of formula (1): its synthesis, pharmaceutical composition, preparation and use thereof. The pharmaceutical composition including: (1) the novel coumarin derivative of formula (1) as active pharmaceutical ingredient; and (2) one or more pharmaceutical excipients, required to yield final dosage forms suitable for therapeutic administration. The composition is safe and efficient therapeutic agent for viral diseases including the acquired immunodeficiency syndrome (AIDS).
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: April 23, 2019
    Inventors: Mladen Trkovnik, Milan Cacic, Jonuz Rizvani
  • Patent number: 10159681
    Abstract: The invention relates to a method for on-demand contraception, which method comprises administering a progestogen agent or progesterone receptor modulator, such as 17a-acetoxy-11b-[4-N,N-dimethylamino-phenyl)-19-norpregna-4,9-diene-3,20-dione (ulipristal acetate) in a woman, within 72 hours before an intercourse or within 120 hours after the intercourse.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: December 25, 2018
    Assignees: Laboratoire HRA-Pharma, The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Andre Ulmann, Erin Gainer, Henri Camille Mathe, Diana Blithe, Lynnette Nieman
  • Patent number: 10059684
    Abstract: ?9-THC acid is extracted from cannabis flowers using a first organic solvent, then separated using a second aqueous solvent. ?9-THC acid is converted to ?9-THC carboxylic salt before being extracted by a third organic solvent and converted back to ?9-THC carboxylic acid. Using a solvent swap, ?9-THC carboxylic acid is decarboxylated and extracted again with an organic solvent prior to purification to give ?9-THC.
    Type: Grant
    Filed: May 4, 2016
    Date of Patent: August 28, 2018
    Assignee: Axim Biotechnologies, Inc.
    Inventors: Lekhram Changoer, Cornelis Herman Michel Van Der Loo, Erik Keller
  • Patent number: 10058564
    Abstract: A method of treating acne in a human in need thereof comprising administering systemically to said human a tetracycline compound in an amount that is effective to treat acne but has substantially no antibiotic activity, without administering a bisphosphonate compound.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: August 28, 2018
    Assignee: Galderma Laboratories Inc.
    Inventor: Robert A. Ashley
  • Patent number: 9980937
    Abstract: The present invention aims to provide a pharmaceutical agent for the prophylaxis and/or treatment of Alzheimer's disease, which has a novel action mechanism and shows less side effects. A polyphenol derivative having liposolubility enhanced by the introduction of at least one kind of a liposoluble group selected from the group consisting of a chain saturated hydrocarbon group, a chain unsaturated hydrocarbon group, a cyclic saturated hydrocarbon group, a cyclic unsaturated hydrocarbon group, an aromatic hydrocarbon group, a liposoluble vitamin residue and a sterol residue has an action to potentiate neprilysin activity, and is useful as a pharmaceutical agent for the prophylaxis and/or treatment of Alzheimer's disease.
    Type: Grant
    Filed: March 16, 2017
    Date of Patent: May 29, 2018
    Inventors: Nobuhisa Iwata, Keiro Shirotani, Masashi Asai, Takashi Tanaka
  • Patent number: 9868745
    Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: November 13, 2014
    Date of Patent: January 16, 2018
    Assignee: Gilead Pharmasset LLC
    Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James G. Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
  • Patent number: 9725460
    Abstract: Certain embodiments are directed to oridonin analogs or derivatives. In certain aspects, the derivatives are used as anticancer or anti-inflammatory agents.
    Type: Grant
    Filed: October 5, 2015
    Date of Patent: August 8, 2017
    Inventors: Jia Zhou, Chunyong Ding, Qiang Shen
  • Patent number: 9675630
    Abstract: The invention relates to compositions, such as pharmaceuticals, foods, food additives, or dietary supplements, containing A-type procyanidins, and methods of use thereof, for prophylactic or therapeutic treatment of a human or a veterinary animal to treat or prevent NO-responsive health conditions, treat hypertension, cardiovascular disease, coronary artery disease and/or vascular circulation disorders, prevent or reduce the risk of heart attack, stroke, congestive heart failure and/or kidney failure, or to improve blood flow, for example renal blood flow. The composition may optionally contain an additional NO modulating agent and/or a cardiovascular-protective or therapeutic agent, or may be administered in combination with such an agent.
    Type: Grant
    Filed: January 28, 2005
    Date of Patent: June 13, 2017
    Inventors: Harold H. Schmitz, Catherine L. Kwik-Uribe, Mark A. Kelm, John F. Hammerstone, Jr.
  • Patent number: 9630972
    Abstract: Crystalline solid forms of methyl {(2S)-1-[(2S,5S)-2-(9-{2-[(2S,4S)-1-{(2R)-2-[(methoxycarbonyl)amino]-2-phenylacetyl}-4-(methoxymethyl)pyrrolidin-2-yl]-1H-imidazol-5-yl}-1,11-dihydroisochromeno[4?,3?:6,7]naphtho[1,2-d]imidazol-2-yl)-5-methylpyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl}carbamate (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using these crystalline forms.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: April 25, 2017
    Assignee: Gilead Pharmasset LLC
    Inventors: Olga Viktorovna Lapina, Bing Shi, Fang Wang, Scott Alan Wolckenhauer
  • Patent number: 9572809
    Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: February 21, 2017
    Assignee: SPERO TRINEM, INC.
    Inventors: Christopher Phillip Locher, Youssef Laafiret Bennani, Anne-Laure Grillot, Hardwin O'Dowd, Emanuele Perola, Arnaud Le Tiran, Paul S. Charifson
  • Patent number: 9493515
    Abstract: The invention relates to agents and to pharmaceutical compositions for reducing the formation of amyloid and/or for promoting the disaggregation of amyloid proteins. The compositions may also be used to detect amyloid.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: November 15, 2016
    Inventors: Rajaraman Krishnan, Richard Fisher
  • Patent number: 9453016
    Abstract: The invention relates to compositions and methods (with regard to animals and humans) for utilizing an extract and/or one or more natural spiro triterpenoids and derivatives thereof alone or as a supplement. Certain materials utilized are from the blazeispirol family, obtainable from Agaricus species. Treatments include the prophylactic and/or therapeutic treatment of a disease, disorder or condition that responds to the modulation of Liver X receptor, as well as corresponding methods of treatment, the manufacture of a pharmaceutical and nutraceutical formulation for said treatment. The invention also relates to the use of the extract and compound(s) in the treatment or in the preparation of a medicament (e.g. a nutraceutical) for the prophylactic and/or therapeutic treatments, as well as their preparation. It also relates to pharmaceutical or nutraceutical formulations described herein which are useful in prophylactic and therapeutic treatments. They can also be used for non-therapeutic, e.g.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: September 27, 2016
    Inventors: Torsten Grothe, Marc Stadler, Bärbel Köpcke, Ernst Roemer, Jens Bitzer, Philipp Wabnitz, Thomas Küper
  • Patent number: 9445979
    Abstract: The present invention relates to a cosmetic composition comprising compounds or salts of formula (I) or formula (II), wherein R1 and R2 are both independently hydrogen (H), or a saturated, straight or branched C1-C8 alkyl group. More particularly, the present invention also relates to the use of said cosmetic composition for the prevention of the graying of hair and/or for restoration and/or maintenance of the natural hair color.
    Type: Grant
    Filed: April 12, 2011
    Date of Patent: September 20, 2016
    Assignee: DSM IP ASSETS B.V.
    Inventor: Eva Peters
  • Patent number: 9408882
    Abstract: Methods and compositions are provided for alleviating and/or preventing one or more side effects associated with exposure to radiation in a subject exposed to radiation or at risk for exposure to radiation comprising oral administration to the subject of an amount of an edible source of melanin effective to alleviate a side effect associated with radiation.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: August 9, 2016
    Assignee: Albert Einstein College of Medicine, Inc.
    Inventors: Ekaterina Dadachova, Arturo Casadevall
  • Patent number: 9283206
    Abstract: The invention relates to the use of 4,6,4?-trimethylangelicin (TMA) and structural analogs thereof to prepare a medicament for the treatment of cystic fibrosis with the primary objective of correcting the defective CFTR in a sub-group of cystic fibrosis patients consisting of patients carrying the F508del-CFTR mutation.
    Type: Grant
    Filed: June 13, 2012
    Date of Patent: March 15, 2016
    Assignees: Azienda Ospedaliera Universitaria Integrata di Verona, Universita' degli Studi di Ferrara, Universita' degli Studi di Bari, Rare Partners S.r.l.
    Inventors: Giulio Cabrini, Valeria Casavola, Roberto Gambari
  • Patent number: 9283233
    Abstract: The invention relates to a method for on-demand contraception, which method comprises administering a progestogen agent or progesterone receptor modulator, such as 17a-acetoxy-11b-(4-N,N-dimethylamino-phenyl)-19-norpregna-4,9-diene-3,20-dione (ulipristal acetate) in a woman, within 72 hours before an intercourse or within 120 hours after the intercourse.
    Type: Grant
    Filed: March 2, 2015
    Date of Patent: March 15, 2016
    Assignees: LABORATOIRE HRA-PHARMA, The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Andre Ulmann, Erin Gainer, Henri Camille Mathe, Diana Blithe, Lynnette Nieman
  • Patent number: 9248313
    Abstract: A therapy system includes a diagnostic image scanner (12) that acquires a diagnostic image of a target region to be treated. A planning processor (70) is configured to generate a patient specific adaptive radiation therapy plan based on patient specific biomarkers before and during therapy. A first set of patient specific biomarkers is determined then used for the determination of a first normal tissue complication probability (NTCP) model and a first tumor control probability (TCP) model. A radiation therapy device (40) administers a first dose of radiation to the target region with a protocol based on the first NTCP model and the first TCP model. A second set of patient specific biomarkers is determined. A relationship between the first set and second set of patient specific biomarkers is used to determine a second NTCP model and a second TCP model.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: February 2, 2016
    Inventors: Martin Weibrecht, Jens Christoph Georgi, Carolina M. Ribbing
  • Patent number: 9085549
    Abstract: Compounds and their pharmaceutically acceptable salts for treatment of synucleinopathies, such as Parkinson's disease and tauopathies.
    Type: Grant
    Filed: September 15, 2014
    Date of Patent: July 21, 2015
    Assignee: PROTEOTECH INC
    Inventors: Esposito A Luke, Marisa C Yadon, Joel Cummings, F Michael Hudson, Thomas Lake, Qubai Hu, Judy Cam, Alan D. Snow
  • Patent number: 9018222
    Abstract: The present invention refers to the use of sodium channel blockers such as tetrodotoxin or saxitoxin, its analogues/derivatives as well as their acceptable salts, for the production of a medicament for the treatment of neuropathic pain resulting from chemotherapy.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: April 28, 2015
    Assignee: Wex Medical Limited
    Inventors: Helmut Heinrich Buschmann, Jose Miguel Vela Hernandez, Jose Manuel Baeyens
  • Publication number: 20150111842
    Abstract: Provided are an attractant for bone marrow stem cells containing at least one of cinnamtannin B1 and pentagalloylglucose, and a method for attracting bone marrow stem cells in which bone marrow stem cells are attracted by the attractant.
    Type: Application
    Filed: May 31, 2013
    Publication date: April 23, 2015
    Inventors: Tadashi Furumoto, Koichi Nakaoji, Kazuhiko Hamada, Noriyasu Ozawa, Yuta Inami, Misaki Toyoshima, Kosuke Fujita, Akito Maeda, Yasufumi Kaneda, Katsuto Tamai
  • Publication number: 20150105454
    Abstract: Use of sparstolonin B in inhibition of growth and/or viability of human neuroblastoma cells is described. The sparstolonin B can be naturally derived from the Chinese herb Sparganium stoloniferum or can be synthetic. The sparstolonin B is shown to be effective both in vitro and in vivo in inhibition of growth and/or viability of neuroblastoma cells of multiple different genetic backgrounds including N-myc amplified with wild p53 neuroblastoma cells, N-myc amplified with mutated p53 neuroblastoma cells, and N-myc nonamplified neuroblastoma cells.
    Type: Application
    Filed: September 11, 2014
    Publication date: April 16, 2015
    Inventors: Ambrish Kumar, Ugra Sen Singh, Daping Fan, Donald J. Dipette
  • Patent number: 8993618
    Abstract: New pharmaceutical compositions extracted from Ferula assa-foetida are confirmed to effectively treat influenza A (H1N1) virus. The extraction method of the new pharmaceutical compositions mainly includes steps of: (a) extracting F. assa-foetida with methanol to obtain a crude extract; (b) fractioning the crude extract with n-hexane-methanol to obtain a methanol extract; (c) fractioning the methanol extract with chloroform-water to obtain a chloroform extract; and (d) chromatographing the chloroform extract to obtain the pharmaceutical compositions, which can be further fractioned and chromatographed to obtain various sesquiterpene coumarins.
    Type: Grant
    Filed: July 21, 2014
    Date of Patent: March 31, 2015
    Assignee: Kaohsiung Medical University
    Inventors: Yang-Chang Wu, Fang-Rong Chang, Lien-Chai Chiang
  • Patent number: 8987324
    Abstract: The invention relates to Simalikalactone E (SkE) to be used for preventing and/or treating cancers.
    Type: Grant
    Filed: January 13, 2012
    Date of Patent: March 24, 2015
    Assignee: Institut de Recherche pour le Developpement
    Inventors: Geneviève Bourdy, Patrick Auberger, Valérie Jullian, Guillaume Robert, Eric Deharo
  • Publication number: 20150079189
    Abstract: In one embodiment, the present application discloses synthetic LDL nanoparticles comprising mixtures of components selected from the group consisting of phospholipids, triglycerides, cholesterol ester and free cholesterol; optionally further comprising an agent selected from the group consisting of natural antioxidants, ubiquinol and vitamin E, and methods for preparing the synthetic nanoparticles. The disclosed synthetic LDL nanoparticles are capable of selectively delivering lipophilic drugs and prodrugs to cellular targets expressing LDL receptors after intra venous injection.
    Type: Application
    Filed: September 13, 2014
    Publication date: March 19, 2015
    Applicant: Arbor Therapeutics, LLC
    Inventors: James D. McChesney, Igor Nikoulin, Steve J. Bannister, Douglas L. Rodenburg
  • Patent number: 8980940
    Abstract: A composition comprising a high purity cannabinoid, an acid, and a pharmaceutically-acceptable solvent achieves room temperature stability for over 24 months. The acid improves the stability of the composition and the solvent enhances the solubility of the acid, thereby allowing the acid to have an improved stabilizing effect on the highly pure cannabinoid. Preferably, the solvent is an alcohol and, more preferably, the composition contains an oil. A method for making the composition includes combining the cannabinoid and the solvent and evaporating a portion of the solvent, along with adding an acid to the composition, before, during, or after the evaporating step. A method for making and storing the composition includes storing the composition in a manner adapted to maintain its stability. Pharmaceutical dosage forms include a formulated composition, such as having the oil. A method of treating a subject comprises administering to the subject the dosage form.
    Type: Grant
    Filed: November 22, 2011
    Date of Patent: March 17, 2015
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Ronald Rossi, Lee Jonathan Silverberg, Robert Hogan, Ramesh M. Shah
  • Publication number: 20150072012
    Abstract: A highly bioavailable, water soluble, sustained release nanoformulation comprising a hydrophobic plant derived compound(s) in an emulsifier phase, and aqueous phase. The formulation provides sustained release of the hydrophobic plant derived compound(s) over a 24 hr time period. A process for preparation of the water soluble nanoformulation is described.
    Type: Application
    Filed: November 13, 2014
    Publication date: March 12, 2015
    Inventors: Ravichandran SRIPATHY, Venkata Narasimha Siva Rama Raju MANDAPATI, Gopaal AJAY, Nirvanashetty SOMASHEKARA, Ramchand Nanappan CHANIYILPARAMPU, Rama Raju GOKARAJU, Ganga Raju GOKARAJU, Kiran BHUPATHIRAJU, Dwarakanath ANJANA
  • Patent number: 8975236
    Abstract: There is disclosed a dietary supplement composition of alkaloids and flavonoids extracted from citrus fruits that exhibits lipolytic and thermogenic activity and increases RMR, while at the same time exhibiting no negative side effects such as increase in blood pressure or heart rate. The composition essentially comprises two components: (A) the protoalkaloids synephrine, tyramine, N-methyltyramine, hordenine and octopamine; and (B) at least one of hesperidin, naringin and mixtures thereof.
    Type: Grant
    Filed: June 13, 2011
    Date of Patent: March 10, 2015
    Inventors: Sidney J. Stohs, Howard Miller
  • Patent number: 8974363
    Abstract: New photodynamic, topically-applicable medicaments and certain medical uses of such photodynamic medicaments for treatment of human or animal tissue are described, wherein a primary active component of such medicaments is a halogenated xanthene. The halogenated xanthenes constitute a family of potent photosensitizers that become photoactivated upon illumination of the treatment site with visible wavelengths of light. In preferred embodiments, such medicaments are used for treatment of a variety of conditions affecting the skin and related organs; the mouth and digestive tract and related organs; the urinary and reproductive tracts and related organs; the respiratory tract and related organs; various other internal or external tissue surfaces, such as tissue surfaces exposed during surgery; and for treatment of a variety of conditions related to microbial or parasitic infection.
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: March 10, 2015
    Assignee: Provectus Pharmatech, Inc.
    Inventors: H. Craig Dees, Timothy C. Scott, John Smolik, Eric A. Wachter, Walter G. Fisher
  • Publication number: 20150065431
    Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 5, 2015
    Inventors: Wei Xu, Seok Jong Hong, Robert D. Galiano, Thomas A. Mustoe
  • Publication number: 20150057342
    Abstract: Provided are oral pharmaceutical compositions comprising sustained release or a combination of sustained and immediate release formulation of cannabinoids, a process for their preparation and methods of use thereof.
    Type: Application
    Filed: July 31, 2014
    Publication date: February 26, 2015
    Inventors: Zohar KOREN, Eyal BALLAN, Itamar BOROCHOV, Shay Avraham SARID
  • Publication number: 20150051207
    Abstract: The present invention is directed to unsaturated sphingosine compounds which are useful as therapeutic agents for the treatment of cancer and for the treatment of other diseases including diabetes and infection with intracellular bacteria. The invention is also directed to methods of using the compounds and pharmaceutical compositions comprising the compounds in treating these diseases.
    Type: Application
    Filed: April 24, 2014
    Publication date: February 19, 2015
    Inventors: Julie D. Saba, Henrik Fyrst, Robert Bittman
  • Publication number: 20150045422
    Abstract: Novel methods are presented for treating Influenza by using Targeted Transient Ribosomal Inhibition (TTRI), with TTRI drugs administered by inhalation, to silence expression of every protein underlying the etiology and pathology of the influenza infection, and without adversely effecting normal cells in the lungs. The therapeutic effect is dual Antiviral and Anti-Inflammatory activity which is localized to the lungs. Pulmonary TTRI for influenza silences expression of all 10 influenza viral proteins and de novo synthesis of cytokines and leukotrienes produced in the lungs. By targeting ribosomes, TTRI is insensitive to viral mutations or human alterations to the virus. TTRI provides an off-the-shelf solution for preventing mortality from any strain of influenza.
    Type: Application
    Filed: January 31, 2012
    Publication date: February 12, 2015
    Inventor: Mark John Zamoyski
  • Publication number: 20150045358
    Abstract: A pharmaceutical composition for treating disorders associated with insulin resistance is disclosed, and the composition comprises at least one inhibitor which is an effective agent to suppress endothelin-1-stimulated resistin gene expression through decreasing the endothelin-1-stimulated phosphorylation of proteins downstream of endothelin type A receptor, wherein the downstream signaling molecules comprise ERK1/2, JNKs, AKT, and STAT3 proteins, and wherein the inhibitor is selected from at least one antagonist of the endothelin type A receptor or downstream signaling proteins.
    Type: Application
    Filed: May 21, 2013
    Publication date: February 12, 2015
    Inventors: Yung-hsi KAO, Ya-chu Tang, Hsin-huei Chang, Hui-chen Ku
  • Patent number: 8952054
    Abstract: The invention provides methods for the identification of small molecules that inhibit MUC1 oligomerization, and the functions flowing therefrom. In addition, small molecules that prevent MUC1 oligomerization are disclosed. Identified molecules will find use in treating a variety of MUC1-related inflammatory conditions, including MUC1-related cancers.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: February 10, 2015
    Assignees: Dana-Farber Cancer Institute, Inc., Genus Oncology, LLC
    Inventors: Donald W. Kufe, Surender Kharbanda
  • Patent number: 8952003
    Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: February 10, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd
    Inventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
  • Publication number: 20150030587
    Abstract: Methods of treating a head and neck cancer are disclosed.
    Type: Application
    Filed: February 11, 2014
    Publication date: January 29, 2015
    Inventors: Chris Hendrik Boshoff, Timothy Robert Fenton, Matthias Alexander Lechner, Philip James Stephens, Matthew J. Hawryluk, Garrett Michael Frampton, Roman Yelensky
  • Publication number: 20150031656
    Abstract: The present invention relates to a combination therapy for elevating testosterone levels in male mammals in which an antiestrogen or pharmaceutically acceptable salt thereof is co-administered to the mammal with an additional therapeutic agent selected from an androgen and an aromatase inhibitor. The invention is also directed to a combination therapy for treating males with hypogonadism and disorders related thereto, including reduction of muscle mass. limitation of body performance capacity, reduction of bone density, reduction of libido, reduction of potency, reduction of benign prostatic hyperplasia and infertility.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 29, 2015
    Inventors: Joseph S. Podolski, Ronald D. Wiehle
  • Publication number: 20150017216
    Abstract: Biodegradable and nutritionally attractive composition comprising biocidal or antibiotic compounds and/or microbes having bio-adhesion and controlled buoyancy properties are selectively fed to an aquatic organism in open or closed water-bodies, and bioactive components are released upon contact with mucosal tissues such as gill, skin or along the digestive tract of the selected aquatic organism.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 15, 2015
    Inventors: Moti Harel, Brian Carpenter, Pete Schmalz
  • Patent number: 8927598
    Abstract: Oncogenic Ras-driven cancer is treated with agent by interrupting pathway comprising activation of Akt by oncogenic Ras, activated Akt causing phosphorylation of eNOS at S1177 site of eNOS to provide activated eNOS in cancer cells and activated eNOS causing activation of wildtype Ras by nitrosylation thereof at C118 to provide GTP-bound activated wildtype H and N Ras. L-NAME can be orally administered to interrupt this pathway. Wortmannin can be administered intravenously to interrupt this pathway. Novel siRNAs are disclosed useful to interrupt said pathway.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: January 6, 2015
    Assignee: Duke University
    Inventors: Christopher M. Counter, Kian-Huat Lim, Brooke B. Ancrile, David F. Kashatus
  • Publication number: 20150004237
    Abstract: Provided are cellulose esters useful for inhibiting solution crystallization of drugs. Specific polymers include cellulose esters of formula I: wherein n of the ?-carboxyalkanoyl group, is 3, 4, 6, or 8 to provide a ?-carboxyalkanoyl group chosen from succinoyl, glutaroyl, adipoyl, sebacyl, and suberyl groups; and wherein R is chosen from: a hydrogen atom; and an alkanoyl group chosen from acetyl, propionyl, butyryl, valeroyl, hexanoyl, nonanoyl, decanoyl, lauroyl, palmitoyl, and stearoyl groups; wherein there is a total degree of substitution of the alkanoyl group and the ?-carboxyalkanoyl group of at least 2.0; and wherein the polymer comprises m repeating units where n=1 to 1,000,000, or 10 to 100,000, or 100 to 1,000, such as 1 to 6,000. Embodiments further include compositions comprising cellulose esters and poorly water-soluble drugs, which compositions exhibit greater solubility and stability in solution as compared to the drugs alone.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 1, 2015
    Inventors: Kevin J. Edgar, Bin Li, Lynne Taylor, Grace Ilevbare, Stephanie M. Williams, Haoyu Liu
  • Publication number: 20140371303
    Abstract: Compositions and methods for providing anti-diabetic and anti-hyperlipidemia benefits to diabetic subjects currently on medication but not meeting recommended targets for blood glucose, HbA1c, blood pressure and total cholesterol.
    Type: Application
    Filed: June 17, 2013
    Publication date: December 18, 2014
    Inventor: Najla Guthrie
  • Patent number: 8912229
    Abstract: The present application discloses new taxane analogs, intermediates and methods for producing them. The present application is also directed to pharmaceutical formulations comprising abeo-taxanes and methods of treating cancer with the abeo-taxanes.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: December 16, 2014
    Assignee: Arbor Therapeutics, LLC
    Inventors: James D. McChesney, John T. Henry, Sylesh Venkataraman, Mahesh Kumar Gundluru
  • Publication number: 20140364490
    Abstract: The present invention relates to the fields of natural medicine and medicinal chemistry, and more particularly to a 1-oxo/acylated-14-acylated oridonin derivative of a general formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing the compounds, a pharmaceutical composition comprising the compounds, and application thereof in preparation of antitumor drugs.
    Type: Application
    Filed: January 21, 2013
    Publication date: December 11, 2014
    Inventors: Rongzhen Xu, Frank Rong, Fuwen Xie, Hongxi Lai
  • Publication number: 20140364387
    Abstract: Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the GI tract of an individual.
    Type: Application
    Filed: June 30, 2014
    Publication date: December 11, 2014
    Inventors: William A. GODDARD, III, Mark MENNA, Stephan PANDOL, Ravinder ABROL
  • Patent number: 8906956
    Abstract: A composition comprising a tetrahydrocannabinol compound, a solvent and an acid, wherein the tetrahydrocannabinol compound may be ?8 tetrahydrocannabinol, (?)-?9-trans-tetrahydrocannabinol or a side chain alkyl derivative of either compound, the solvent may be an oil or C1-C4 alcohol (e.g. sesame oil or ethanol), and the acid may be an organic acid or a mineral acid.
    Type: Grant
    Filed: June 7, 2013
    Date of Patent: December 9, 2014
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Ronald Rossi, Lee Jonathan Silverberg, Robert Hogan, Ramesh M. Shah
  • Patent number: 8895576
    Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: November 25, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Michael J. Grogan, Karen J. McGovern, Martin R. Tremblay
  • Patent number: 8895605
    Abstract: The present invention relates to a combination for the treatment of cancer wherein the combination exhibits a synergistic effect. The combination comprises radiation and at least one cyclin dependent kinase (CDK) inhibitor selected from the compounds of formula I or a pharmaceutically acceptable salt or a solvate thereof. The present invention also relates to a method for the treatment of cancer, which method comprises administering to a patient in need of such a treatment, a therapeutically effective amount of the combination. The present invention also relates to the use of a CDK inhibitor selected from the compounds of formula I as a radiosensitizer that enhances the efficacy of radiotherapy for the treatment of cancer, particularly head and neck cancer.
    Type: Grant
    Filed: May 3, 2010
    Date of Patent: November 25, 2014
    Assignee: Piramal Enterprises Limited
    Inventors: Maggie Joyce Rathos, Kalpana Sanjay Joshi, Nikhil Krishnamurthy Hebbar, Somesh Sharma
  • Publication number: 20140343135
    Abstract: A biotechnology process that employs membrane technology for obtaining an extract rich in tannins of ellagic acid from blackberries (Rubus spp.) and from other fruits that contain these compounds, as well as to the extract obtained using this method. The method is essentially based on baromembrane technologies that allow mechanical separation and effective fractionation between the polyphenol compounds, by interactions between the physico-chemical properties thereof, the material of the membrane and the molar mass of same, thereby allowing enrichment of a fraction of the natural extract with ellagic acid tannins and modification of the content thereof in terms of anthocyanins and other compounds such as sugars and acids.
    Type: Application
    Filed: May 11, 2012
    Publication date: November 20, 2014
    Inventors: Oscar Gerardo Acosta Montoya, Ana Mercedes Perez Carvajal, Manuel Dornier, Fabrice Vaillant
  • Patent number: 8889176
    Abstract: A composition for the intranasal delivery of fentanyl or a pharmaceutically acceptable salt thereof to an animal includes an aqueous solution of fentanyl or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable additive selected from (i) a pectin and (ii) a poloxamer and chitosan or a salt or derivative thereof; provided that when the composition comprises a pectin it is substantially free of divalent metal ions; and which, in comparison to a simple aqueous solution of fentanyl administered intranasally at the same dose, provides a peak plasma concentration of fentanyl (Cmax) that is from 10 to 80% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose. A method for treating or managing pain by intranasally administering the composition is also disclosed.
    Type: Grant
    Filed: July 3, 2012
    Date of Patent: November 18, 2014
    Assignee: Depomed, Inc.
    Inventors: Peter James Watts, Jonathan David Castile, William Columbus Lafferty, Alan Smith