Patents Issued in September 17, 2019
  • Patent number: 10413508
    Abstract: An improved process for producing an oil-in-water emulsion to deliver a substantially water insoluble active pharmaceutical ingredient includes creating a microemulsion containing such ingredient in the oil phase of the emulsion by mixing an aqueous phase including non-ionic surfactant, polyol, and water, wherein the weight ratio of the surfactant to polyol to water is between 10:20:70 and 1:1:1, to generate a mixture, with an oil phase comprising a substantially water insoluble active pharmaceutical ingredient and a long-chain triglyceride; circulating the said mixture through a homogenizer at a temperature from 20° C. to 60° C. to generate a coarse emulsion; passing the coarse emulsion through a microfluidizer at a pressure of from 70 MPa to 150 MPa at least once to produce an oil-in-water microemulsion; and, optionally, filtering the microemulsion through a 0.2 ?m filter and/or mixing the microemulsion with a polymeric stabilizer.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: September 17, 2019
    Assignee: R. P. Scherer Technologies, LLC
    Inventors: James Michael Foreman, Anayo Michael Ukeje, Ronald W. Swank, Waiken Wong
  • Patent number: 10413509
    Abstract: The present invention relates to a pharmaceutical composition comprising the combination of (i) a biocompatible nanoparticle and of (ii) a pharmaceutical compound of interest, to be administered to a subject in need of such a compound of interest, wherein the nanoparticle potentiates the compound of interest efficiency. The longest dimension of the biocompatible nanoparticle is typically between about 4 and about 500 nm, and its absolute surface charge value is of at least 10 mV (|10 mV|). The invention also relates to such a composition for use for administering the compound of interest to a subject in need thereof, wherein the nanoparticle and the compound of interest are to be administered to said subject between more than 5 minutes and about 72 hours from each other.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: September 17, 2019
    Assignee: NANOBIOTIX
    Inventors: Agnés Pottier, Laurent Levy, Marie-Edith Meyre, Audrey Darmon, Matthieu Germain
  • Patent number: 10413510
    Abstract: The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.
    Type: Grant
    Filed: November 29, 2016
    Date of Patent: September 17, 2019
    Assignee: Ipsen Biopharm Ltd.
    Inventors: Keelung Hong, Daryl C. Drummond, Dmitri Kirpotin
  • Patent number: 10413511
    Abstract: The present invention relates to the preparation of liposomes with enhanced loading capacity for pharmaceutically and/or diagnostically active agents and/or cosmetic agents which are substantially solubilized by the liposomal membranes, to liposome dispersions with enhanced stability with respect to release of the active agent and/or cosmetic agent from the liposomes obtainable by the process, and to pharmaceutical or cosmetic compositions comprising said stabilized liposome dispersions. The preparation may involve dehydration and rehydration steps of liposome dispersions which may be carried out by spray drying.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: September 17, 2019
    Assignee: SynCore Biotechnology Co., Ltd.
    Inventors: Heinrich Haas, Ursula Fattler
  • Patent number: 10413512
    Abstract: A dust-reduced nicotine-containing granulate comprising a homogenous mixture of nicotine or a pharmaceutically acceptable nicotine derivative and an excipient, the granulate having a particle size of at least 150 ?m. Method for the preparation of a dust-reduced nicotine-containing granulate, and use of the nicotine-containing granulate for the preparation of pharmaceutical products.
    Type: Grant
    Filed: September 16, 2009
    Date of Patent: September 17, 2019
    Assignee: SIEGFRIED LTD.
    Inventor: Tillmann Roehrich
  • Patent number: 10413513
    Abstract: Disclosed herein are heat-stable dry powders which include peptides or protein such as oxytocin for use as a pharmaceutical composition. The composition is highly stable at increased temperatures and relatively high humid environments, and are intended for storage at room temperature with an improved shelf-life. In particular, the dry powders are intended for inhalation, however, other routes of administration can be used when reconstituted in solution.
    Type: Grant
    Filed: January 31, 2018
    Date of Patent: September 17, 2019
    Assignee: Mannkind Corporation
    Inventors: Karine Fabio, Joseph J. Guarneri, Kieran Curley, Marshall L. Grant, Andrea Leone-Bay
  • Patent number: 10413514
    Abstract: Disclosed is a controlled-release solid preparation, which consists of an internal core and a coating layer, wherein part of the surface of the internal core is not covered with the coating, and is exposed to the surface of the solid preparation. Since the medicament just releases at the exposed part, the aim of controlled release can be achieved by controlling this exposed surface area.
    Type: Grant
    Filed: April 8, 2015
    Date of Patent: September 17, 2019
    Assignee: OVERSEAS PHARMACEUTICALS, LTD.
    Inventor: Xiaoguang Wen
  • Patent number: 10413515
    Abstract: Provided are hydrocolloid core-shell capsules including a liquid core including a non-crosslinked alginate solution and a solid or semi-solid shell including a hydrocolloid other than alginate crosslinked with metal ions, which do not crosslink alginate. Further provided is a method for the preparation of the liquid-core capsules including non-crosslinked alginate. The subject matter further provides the use of the capsules, inter alia, in the water treatment technology.
    Type: Grant
    Filed: December 29, 2015
    Date of Patent: September 17, 2019
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Amos Nussinovitch, Orit Dagan
  • Patent number: 10413516
    Abstract: A method of preparing a thin film, the method comprising: (a) mixing a lipid, emulsifier, and solvent to provide a uniform first mixture; (b) contacting an active ingredient with the uniform first mixture to provide a thickened second mixture; (c) contacting a binder with the thickened second mixture to provide a slurry; and (d) hot extruding, casting, and condensing the slurry to provide the thin film; or cooling, shearing, mixing, casting, and condensing the slurry to provide the thin film.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: September 17, 2019
    Assignee: CURE Pharmaceutical Corporation
    Inventors: Eric Allen, Robert Steven Davidson, Jose Bernardo
  • Patent number: 10413517
    Abstract: Methods and compositions which include or include the administration of a hydrophobic drug, prodrug thereof, salt thereof, isoform thereof, or a combination thereof; cyclodextrin, prodrug thereof, salt thereof, or a combination thereof; polyethylene glycol, propylene glycol, or combination thereof; and optionally, a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 11, 2015
    Date of Patent: September 17, 2019
    Assignee: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Kasturi Haldar, Md. Suhail Alam
  • Patent number: 10413518
    Abstract: Methods for reducing angiogenesis, inflammation, and vascular permeability in a subject by administering an epoxymetabolite of Docosahexaenoic acid (DHA) and Eicosapentaenoic acid (EPA), e.g., as listed in Table A, e.g., one or both of 17,18-epoxyeicosatetraenoic acid (EEQ) and 19,20-epoxydocosapentaenoic acid (EDP), e.g., for the treatment of conditions associated with inflammation or excess angiogenesis or neovascularization, including age-related macular degeneration, cancer, stroke, and arthritis.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: September 17, 2019
    Assignee: Massachusetts Eye and Ear Infirmary
    Inventors: Kip M. Connor, Ryoji Yanai
  • Patent number: 10413519
    Abstract: Polymorphic forms of tetrahydro-N,N-dimethyl-2,2-diphenyl-3 -furanmethanamine hydrochloride (ANAVEX2-73) and a metabolite of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73) are disclosed and characterized. Compositions and method for treatment of Alzheimer's disease that includes the polymorphic forms and metabolite of tetrahydro-N,N-dimethyl-2,2 -diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73).
    Type: Grant
    Filed: July 19, 2016
    Date of Patent: September 17, 2019
    Assignee: ANAVEX LIFE SCIENCES CORP.
    Inventors: Linda Sharon Daintree, Daniel Mark Ledger, Lucy Anne Leonard, Peter York
  • Patent number: 10413520
    Abstract: The present invention relates to a pharmaceutical composition including (i) as a major ingredient, a novel 5-{4-(Aminosulfonyl)phenyl}-2,2-dimethyl-4-(3-fluorophenyl)-3(2H)-furanone compound (Formula 1) or a pharmaceutically acceptable salt thereof, which has a crystalline form A or G, or a mixed form thereof and has a 50% volume particle diameter (d(0.5)) of 3 ?m to 9 ?m and a 90% volume particle diameter (d(0.9)) of 10 ?m to 50 ?m, (ii) a pharmaceutically acceptable diluent, and (iii) a pharmaceutically acceptable lubricant. The pharmaceutical composition of the present invention has the advantages of good stability, high dissolution rate, improved content uniformity, and excellent pharmacokinetic properties. Due to these advantages, as a non-steroidal anti-inflammatory drug, the pharmaceutical composition of the present invention may be effective in treating inflammation or pain.
    Type: Grant
    Filed: June 22, 2017
    Date of Patent: September 17, 2019
    Assignee: CRYSTALGENOMICS, INC.
    Inventors: Byung-Ha Kim, Sik II Ahn, Jae-Yeon Park, Tae Ryong Kim, Joong Myung Cho, Seonggu Ro
  • Patent number: 10413521
    Abstract: An inhalable composition for use as a medicament in the treatment of a subject wherein said composition comprises: one or more cannabinoids or a pharmaceutically acceptable derivative or salt thereof; a propellant; a monohydric or polyhydric alcohol; and a glycol and/or glycol ether, characterized in that the ratio of monohydric or polyhydric alcohol to glycol or glycol ether by weight is from 6:1 to 1:1, wherein the composition is administered in the form of an aerosol having a fine particle fraction of 60% or more.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: September 17, 2019
    Assignee: KIND CONSUMER LIMITED
    Inventors: Alex Hearn, Ritika Gupta, Moira Bowdrey
  • Patent number: 10413522
    Abstract: The present invention relates to methods for treating brain metastasis by inhibiting gap junction functionality. It is based, at least in part, on the discovery that cancer cells expressing Protocadherin 7 and Connexin 43 form gap junctions with astrocytes that promote the growth of brain metastases, and that inhibition of Protocadherin 7 and/or Connexin 43 expression in cancer cells reduce progression of brain metastases. It is further based on the discovery that treatment with gap junction inhibitors tonabersat and meclofenamate inhibited progression of brain metastatic lesions and enhanced the anti-cancer activity of the conventional chemotherapeutic agent, carboplatin.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: September 17, 2019
    Assignee: MEMORIAL SLOAN-KETTERING CANCER CENTER
    Inventors: Joan Massague, Adrienne Boire, Qing Chen
  • Patent number: 10413523
    Abstract: A composition which includes Phenylalanine, Serine, Glutamine and GABA (?-aminobutyric acid). The composition contains the essential amino acids Phenylalanine; Glutamine; the non-essential amino acid Serine; and GABA (?-aminobutyric acid) in concentrations effective to influence or modulate the neurotransmitter pentapeptide enkephalin. The composition may further comprise tetrahydrocannabinol (THC).
    Type: Grant
    Filed: November 16, 2017
    Date of Patent: September 17, 2019
    Assignee: BIOADATP, LLC
    Inventor: Kevin Meehan
  • Patent number: 10413524
    Abstract: Antioxidative stress compositions, methods of using antioxidative stress composition and methods of preparing antioxidative stress composition compositions are described. The antioxidative stress compositions may be chemopreventive and/or immunomodulatory. Resveratrol, genistein, ellagic acid, curcumin and quercetin may be included in the antioxidative stress composition compositions individually or in any combination.
    Type: Grant
    Filed: August 22, 2018
    Date of Patent: September 17, 2019
    Inventor: John Michael Pezzuto
  • Patent number: 10413525
    Abstract: The present invention relates in part a to multiparticulate sprinkle dosage form comprising duloxetine or a pharmaceutically acceptable salt thereof, having higher acid resistance as compared to commercially available delayed release formulations. It further relates to various methods of administering the said multiparticulate sprinkle dosage forms.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: September 17, 2019
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Ravindra Agarwal, Tarun Singhal, Ravi Kochhar
  • Patent number: 10413526
    Abstract: A pharmaceutical composition or dietary supplement effective in the treatment of neuropathies and/or neuropathic pain is described, which comprises, as the active ingredients, the combination of curcumin, N-acetyl-L-carnitine and alpha-lipoic acid, wherein N-acetyl-L-carnitine and alpha-lipoic acid are present in the composition in the form of coated particles.
    Type: Grant
    Filed: March 25, 2016
    Date of Patent: September 17, 2019
    Assignee: Kolinpharma S.p.A.
    Inventors: Emanuele Lusenti, Ritapaola Petrelli
  • Patent number: 10413527
    Abstract: Substituted phenylpyrrolecarboxamide compounds such as those represented by Formula A can be used in the treatment of HIV infection and related conditions.
    Type: Grant
    Filed: November 1, 2018
    Date of Patent: September 17, 2019
    Assignees: New York Blood Center, Inc., The United States of America, as Represented by the Secretary, Department of Health and Human Services
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Patent number: 10413528
    Abstract: A method that inhibits infection during wound healing by topical application of a single composition, which contacts a wound for a period of time to initiate wound healing. The single composition may include a mixture of all or some of the amino acids including: histidine monohydrochloride monohydrate; isoleucine; leucine; lysine acetate; methionine; phenylalanine; threonine; tryptophan; valine; alanine; arginine acetate; aspartic acid; glutamine; glycine; proline; serine; and tyrosine, which may provide aqueous mixtures of a range of osmolarities or a powdered mixture of amino acids. The single composition may also include any of a carbohydrate, a mixture of fatty acids, vitamins, and mineral nutrients, and another mixture of amino acid derivatives and preservatives. The number of moles of the carbohydrate is less than and proportional to a sum of the number of moles of any mixture of amino acids in the single composition.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: September 17, 2019
    Inventor: John H. Plumb
  • Patent number: 10413529
    Abstract: Described herein are methods of inhibiting or reversing the progression of cataract formation or presbyopia in an eye by administering a ?-crystallin charge masking agent. Both presbyopia and cataracts are caused by aggregation of the soluble crystalline lens proteins called the crystallins.
    Type: Grant
    Filed: April 28, 2017
    Date of Patent: September 17, 2019
    Assignee: UNIVERSITY OF MASSACHUSETTS
    Inventors: Murugappan Muthukumar, Benjamin Mohr
  • Patent number: 10413530
    Abstract: A method for increasing the number of CD4+ T-lymphocytes in the serum of a subject in need of such treatment comprising administering to the subject a pharmaceutical composition comprising an amount of an L-isomer of ?-lactam effective to increase the number of CD4+ T-lymphocytes in said patient's serum.
    Type: Grant
    Filed: January 18, 2018
    Date of Patent: September 17, 2019
    Assignee: Alpha-1 Biologics, LLC
    Inventors: Cynthia L. Bristow, Ronald H. Winston
  • Patent number: 10413531
    Abstract: The present invention provides methods and compositions for treating bladder cancer, including metastatic bladder cancer and non-muscle-invasive bladder cancer, by administering a composition comprising nanoparticles that comprise mTOR inhibitor and optionally an albumin.
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: September 17, 2019
    Assignee: Abraxis BioScience, LLC
    Inventor: Neil P. Desai
  • Patent number: 10413532
    Abstract: This present invention relates to a method of treating a autoimmune, respiratory and/or inflammatory disease or condition (e.g., psoriasis, rheumatoid arthritis, asthma, COPD). The method comprises administering a PI3K Delta inhibitor or a dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor. The present invention also relates to pharmaceutical compositions containing a PI3K Delta or dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor.
    Type: Grant
    Filed: June 20, 2018
    Date of Patent: September 17, 2019
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Swaroop K. Vakkalanka, Srikant Viswanadha
  • Patent number: 10413533
    Abstract: Disclosed is a method for enhancing tumor response to chemotherapy, the method comprising administering a short-acting anti-angiogenic agent (AAA) capable of activating ASMase to a subject afflicted with a solid tumor, and thereby creating a time interval of increased susceptibility of said tumor to one or more chemotherapeutic agents, followed by administration of at least one chemotherapeutic agent within the interval. The interval can be defined in terms of a short-duration activation of ASMase signaling by the AAA. Disclosed are also methods for predicting the tumor response in a patient afflicted with a solid tumor to a chemotherapeutic agent, using as an indicator of the response ASMase level or activity (or ceramide level) in the patient following the administration of the chemotherapeutic agent to the patient, or dynamic IVIM based DW-MRI to measure perfusion alterations following administration of the chemotherapeutic agent.
    Type: Grant
    Filed: November 12, 2015
    Date of Patent: September 17, 2019
    Assignee: Memorial Sloan Kettering Cancer Center
    Inventors: Richard Kolesnick, Adriana Haimovitz-Friedman, Evis Sala, Zvi Fuks
  • Patent number: 10413534
    Abstract: Motor skill deficits and cognitive deficits associated with stroke and secondary neuronal cell death are ameliorated by treatment with pharmaceutically acceptable salts of 2-amino substituted nicotinamides.
    Type: Grant
    Filed: February 13, 2018
    Date of Patent: September 17, 2019
    Assignee: NEURALSTEM, INC.
    Inventor: Karl K. Johe
  • Patent number: 10413535
    Abstract: The invention relates to antagonists of integrin ?4 and their use in pharmaceutical compositions, primarily topically administered ophthalmic compositions. The pharmaceutical compositions are useful for treating ocular inflammatory conditions, such as dry eye disease, non-infectious uveitis (e.g., anterior, intermediate, posterior, pan-uveitis), non-infectious conjunctivitis, iritis, or scleritis in animals, and particularly mammals, including humans.
    Type: Grant
    Filed: July 7, 2016
    Date of Patent: September 17, 2019
    Assignee: AXEROVISION, INC.
    Inventor: Achim H. Krauss
  • Patent number: 10413536
    Abstract: 6-Alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer.
    Type: Grant
    Filed: September 26, 2017
    Date of Patent: September 17, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Ulrich Reiser
  • Patent number: 10413537
    Abstract: Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
    Type: Grant
    Filed: October 26, 2018
    Date of Patent: September 17, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, Chi Ching Mak, Brian Walter Eastman, Jianguo Cao, Gopi Kumar Mittapalli
  • Patent number: 10413538
    Abstract: The present invention discloses and claims methods and compositions for the treatment of subjects having advanced ovarian cancer, including platinum and/or taxane chemotherapy resistant or refractory sub-populations, with the administration to the subject having advanced ovarian cancer of the silicon-containing highly lipophilic camptothecin derivative (HLCD), Karenitecin (also known as BNP1350; cositecan; 7-[(2?-trimethylsilyl)ethyl]-20(S) camptothecin) in an amount sufficient to provide a therapeutic benefit. The administration of Karenitecin by intravenous (i.v.) and/or oral methodologies are also disclosed and claimed. Methods for the administration of Karenitecin to increase Progression Free Survival (PFS) are also disclosed and claimed herein.
    Type: Grant
    Filed: May 1, 2014
    Date of Patent: September 17, 2019
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventor: Frederick H Hausheer
  • Patent number: 10413539
    Abstract: The present invention relates to therapeutic ADCs comprising SN-38 attached to an anti-Trop-2 antibody or antigen-binding antibody fragment. The ADC may be administered at a dosage of between 4 mg/kg and 18 mg/kg, preferably 4, 6, 8, 9, 10, 12, 16 or 18 mg/kg, most preferably 8 to 10 mg/kg. When administered at specified dosages and schedules, the ADC can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy. Preferably, the ADC is administered in combination with one or more other therapeutic agents, such as a PARP inhibitor, a microtubule inhibitor, a Bruton kinase inhibitor or a PI3K inhibitor. Most preferably, the ADC is of use for treating a Trop-2 expressing cancer, such as metastatic urothelial cancer.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: September 17, 2019
    Assignee: Immunomedics, Inc.
    Inventors: Serengulam V. Govindan, David M. Goldenberg
  • Patent number: 10413540
    Abstract: Methods for treating a subject having a cancerous tumor are disclosed. The methods comprise administering to the subject an effective amount of a non-steroidal selective glucocorticoid receptor modulator (SGRM) and an effective amount of a chemotherapeutic agent. The tumor may be cervical cancer. The SGRM may be a fused azadecalin. In embodiments, the SGRM may be a heteroaryl ketone fused azadecalin or an octahydro fused azadecalin.
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: September 17, 2019
    Assignee: Corcept Therapeutics, Inc.
    Inventor: Hazel Hunt
  • Patent number: 10413541
    Abstract: A method of treating a depressive or stress disorder in a subject afflicted therewith comprising administering to the subject an effective amount of a compound having the structure:
    Type: Grant
    Filed: November 17, 2017
    Date of Patent: September 17, 2019
    Assignee: Lixte Biotechnology, Inc.
    Inventors: John S. Kovach, Salvatore Lecca, Manuel Mameli
  • Patent number: 10413542
    Abstract: Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders.
    Type: Grant
    Filed: April 11, 2018
    Date of Patent: September 17, 2019
    Assignees: Buck Institute for Research on Aging, Unity Biotechnology, Inc., Mayo Foundation for Medical Education and Research
    Inventors: Remi-Martin Laberge, Nathaniel David, Alain Philippe Vasserot, Darren J. Baker, Bennett G. Childs, James L. Kirkland, Tamar Tchkonia, Jan M. A. van Deursen, Yi Zhu
  • Patent number: 10413543
    Abstract: A stable multi-particulate pharmaceutical composition comprising pellets, the pellets comprising a mixture of rosuvastatin or its pharmaceutically acceptable salts as a sole active ingredient, one or more osmotic release modifiers and one or more stabilizers.
    Type: Grant
    Filed: February 12, 2016
    Date of Patent: September 17, 2019
    Assignee: SUN PHARMA ADVANCED RESEARCH COMPANY LTD.
    Inventors: Nitin Bhalachandra Dharmadikari, Yashoraj Zala, Ashwini Gadkari
  • Patent number: 10413545
    Abstract: The present invention is directed to imidazolin-5-one derivatives, pharmaceutical compositions containing them, and their use as FASN inhibitors, in for example, the treatment of cancer, obesity related disorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein R1, R2, R3, R4, R5, m, n, and are defined herein.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: September 17, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J Connolly, Tianbao Lu
  • Patent number: 10413546
    Abstract: A medicament for prophylactic and/or therapeutic treatment of dementia, which comprises a compound represented by the formula (I) having a xanthine oxidase inhibitory action as an active ingredient.
    Type: Grant
    Filed: February 23, 2016
    Date of Patent: September 17, 2019
    Assignees: NATIONAL UNIVERSITY CORPORATION TOTTORI UNIVERSITY, NIPPON MEDICAL SCHOOL FOUNDATION, NIPPON CHEMIPHAR CO., LTD.
    Inventors: Takeshi Nishino, Shinsuke Kato, Masako Kato, Hidenori Suzuki, Ken Okamoto
  • Patent number: 10413547
    Abstract: This invention is in the area of improved therapeutic combinations for and methods of treating selected retinoblastoma (Rb)-negative cancers and Rb-negative abnormal cellular proliferative disorders using particular topoisomerase inhibitors and specific cyclin-dependent kinase 4/6 (CDK4/6) inhibitors. In one aspect, the improved treatment of select Rb-negative cancers is disclosed using specific compounds disclosed herein in combination with a topoisomerase I inhibitor.
    Type: Grant
    Filed: September 26, 2018
    Date of Patent: September 17, 2019
    Assignee: G1 Therapeutics, Inc.
    Inventors: Jay Copeland Strum, John E. Bisi, Patrick Joseph Roberts, Jessica A. Sorrentino
  • Patent number: 10413548
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: September 17, 2019
    Assignees: Beth Israel Deaconess Medical Center, Inc., The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Patent number: 10413549
    Abstract: The present invention relates to a compositions for and methods for cancer treatment, for example, hematopoietic cancers (e.g. B-cell Lymphoma). In other aspects, the invention provides methods for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more of the disclosed compounds and, for example, 26S proteasome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with the disclosed compounds. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.
    Type: Grant
    Filed: October 24, 2017
    Date of Patent: September 17, 2019
    Assignee: Eutropics Pharmaceuticals, Inc.
    Inventors: David Richard, Michael H. Cardone
  • Patent number: 10413550
    Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO.sub.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: September 17, 2019
    Assignees: The Institute of Cancer Research, Cancer Research Technology Limited, Vernalis (R&D) Limited
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • Patent number: 10413551
    Abstract: The present invention relates to combination therapies for treating Alzheimer's disease or an amyloidosis-associated pathological condition comprising co-administering a therapeutically effective amount of a first compound, and a therapeutically effective amount of a second compound. In certain embodiments, the first compound or the second compound inhibits AB peptide polymerization; is an anti-inflammatory; improves cognitive function, mood, or social behavior; is associated with Tau or alpha-synuclein; or regulates amyloid peptide washout.
    Type: Grant
    Filed: February 22, 2018
    Date of Patent: September 17, 2019
    Assignee: The General Hospital Corporation
    Inventor: David R. Elmaleh
  • Patent number: 10413552
    Abstract: A method of treating a medulloblastoma in a mammal is provided comprising administering to the mammal a compound having the following general formula (1): wherein X is selected from the group consisting of hydrogen, hydroxyl (—OH), halogen, thio (—SH), sulfanyl (—SR), sulfinyl (—SOR), sulfonyl (—SO2R), carboxyl (—COOH), carbonyl (COOR), nitro (—NO2), nitroso (—NOR), amino (NH2), NHR, NRR1, cyano (—CN) and isocyano (—NC), wherein R and R1 are independently C1-C5 branched or unbranched lower alkyl; and Y is a 5- or 6-membered unsaturated ring, optionally substituted, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 17, 2016
    Date of Patent: September 17, 2019
    Assignee: The Hospital for Sick Children
    Inventors: James Rutka, Claudia Faria
  • Patent number: 10413553
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.
    Type: Grant
    Filed: February 1, 2018
    Date of Patent: September 17, 2019
    Assignee: Heptares Therapeutics Limited
    Inventors: Miles Stuart Congreve, Giles Albert Brown, Julie Elaine Cansfield, Benjamin Gerald Tehan
  • Patent number: 10413554
    Abstract: The present invention relates to metal complexes, processes for their preparation and their use as pharmaceutical or veterinary agents, in particular for the treatment of conditions in which metal delivery can prevent, alleviate or ameliorate the condition. There are a number of clinical conditions which are caused by or associated with abnormal levels of metals (typically low metal levels). Conditions in of this type include cancer and conditions characterized by or associated with oxidative damage, more specifically neurodegenerative conditions such as Alzheimer's disease, Parkinson's disease or Huntington's disease. The invention also relates to ligands useful in the preparation of metal complexes of this type.
    Type: Grant
    Filed: January 31, 2018
    Date of Patent: September 17, 2019
    Inventors: Paul Donnelly, James Hilton, Peter Crouch
  • Patent number: 10413555
    Abstract: The aim of the present study was to investigate the effect of a combination of triiodothyroacetic acid (TRIAC) and dehydroepiandrosterone (DHEA) compared with TRIAC, DHEA or placebo alone on corticosteroid induced effect on collagen synthesis in humans. Six healthy male human volunteers aged 40-65 participated. Four areas of abdominal skin were pre-treated for 3 weeks with betamethasone valerate cream. The same areas were then treated with one of the following alternatives in the same cream vehicle: TRIAC, DHEA, TRIAC+DHEA and placebo for 2 weeks. Then suction blisters were raised in each of these areas with a vacuum pump. The blister fluid from each area was collected and frozen until analysis. Analysis of amino terminal propeptide of human type I procollagen (PINP) in suction blister fluid was performed using a commercially available immunoassay (Orion Diagnostics) kit.
    Type: Grant
    Filed: November 24, 2015
    Date of Patent: September 17, 2019
    Assignee: TROPHEA DEVELOPMENT AB
    Inventors: Jan Faergemann, Gudmundur Johannsson, Claes Ohlsson, Derek Gregory Batcheller, Jörgen Johnsson, Jan Törnell
  • Patent number: 10413556
    Abstract: A method of inducing the production of insulin in the body by an individual smelling a composition of a solution including testosterone, and inducing the production of insulin in the body of the individual. A method of treating diabetes type 2 by an individual having diabetes type 2 smelling a composition of a solution including testosterone, inducing the production of insulin in the body of the individual, and treating diabetes type 2 in the individual.
    Type: Grant
    Filed: March 21, 2019
    Date of Patent: September 17, 2019
    Inventor: Moshe Shifrine
  • Patent number: 10413557
    Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17?-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17?-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: September 17, 2019
    Assignee: FORENDO PHARMA LTD.
    Inventors: Leena Hirvelä, Pasi Koskimies, Risto Lammintausta, Marjo Hakola, Maire Eloranta
  • Patent number: 10413558
    Abstract: A pharmaceutical composition or kit of parts comprising at least three ingredients from a HMG-CoA reductase inhibitor, a leukotriene antagonist, a proton pump inhibitor, melatonin or a melatonin receptor agonist, a bioavailable preparation of a curcuminoid, a calciferol derivative, a compound from the group consisting of metformin and phenformin, valproate, minocycline and chloroquine and one or more pharmaceutically acceptable carriers or excipients.
    Type: Grant
    Filed: October 19, 2015
    Date of Patent: September 17, 2019
    Assignee: TARGETED THERAPIES RESEARCH AND CONSULTING CENTER SPRL
    Inventor: Marc Zeicher