Patents Issued in September 17, 2019
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Patent number: 10413508Abstract: 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: GrantFiled: February 5, 2016Date of Patent: September 17, 2019Assignee: R. P. Scherer Technologies, LLCInventors: James Michael Foreman, Anayo Michael Ukeje, Ronald W. Swank, Waiken Wong
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Patent number: 10413509Abstract: 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: GrantFiled: May 30, 2014Date of Patent: September 17, 2019Assignee: NANOBIOTIXInventors: Agnés Pottier, Laurent Levy, Marie-Edith Meyre, Audrey Darmon, Matthieu Germain
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Patent number: 10413510Abstract: 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: GrantFiled: November 29, 2016Date of Patent: September 17, 2019Assignee: Ipsen Biopharm Ltd.Inventors: Keelung Hong, Daryl C. Drummond, Dmitri Kirpotin
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Patent number: 10413511Abstract: 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: GrantFiled: May 20, 2011Date of Patent: September 17, 2019Assignee: SynCore Biotechnology Co., Ltd.Inventors: Heinrich Haas, Ursula Fattler
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Patent number: 10413512Abstract: 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: GrantFiled: September 16, 2009Date of Patent: September 17, 2019Assignee: SIEGFRIED LTD.Inventor: Tillmann Roehrich
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Patent number: 10413513Abstract: 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: GrantFiled: January 31, 2018Date of Patent: September 17, 2019Assignee: Mannkind CorporationInventors: Karine Fabio, Joseph J. Guarneri, Kieran Curley, Marshall L. Grant, Andrea Leone-Bay
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Patent number: 10413514Abstract: 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: GrantFiled: April 8, 2015Date of Patent: September 17, 2019Assignee: OVERSEAS PHARMACEUTICALS, LTD.Inventor: Xiaoguang Wen
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Patent number: 10413515Abstract: 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: GrantFiled: December 29, 2015Date of Patent: September 17, 2019Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.Inventors: Amos Nussinovitch, Orit Dagan
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Patent number: 10413516Abstract: 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: GrantFiled: May 9, 2013Date of Patent: September 17, 2019Assignee: CURE Pharmaceutical CorporationInventors: Eric Allen, Robert Steven Davidson, Jose Bernardo
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Patent number: 10413517Abstract: 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: GrantFiled: June 11, 2015Date of Patent: September 17, 2019Assignee: UNIVERSITY OF NOTRE DAME DU LACInventors: Kasturi Haldar, Md. Suhail Alam
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Patent number: 10413518Abstract: 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: GrantFiled: August 23, 2017Date of Patent: September 17, 2019Assignee: Massachusetts Eye and Ear InfirmaryInventors: Kip M. Connor, Ryoji Yanai
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Patent number: 10413519Abstract: 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: GrantFiled: July 19, 2016Date of Patent: September 17, 2019Assignee: ANAVEX LIFE SCIENCES CORP.Inventors: Linda Sharon Daintree, Daniel Mark Ledger, Lucy Anne Leonard, Peter York
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Patent number: 10413520Abstract: 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: GrantFiled: June 22, 2017Date of Patent: September 17, 2019Assignee: CRYSTALGENOMICS, INC.Inventors: Byung-Ha Kim, Sik II Ahn, Jae-Yeon Park, Tae Ryong Kim, Joong Myung Cho, Seonggu Ro
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Patent number: 10413521Abstract: 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: GrantFiled: February 13, 2015Date of Patent: September 17, 2019Assignee: KIND CONSUMER LIMITEDInventors: Alex Hearn, Ritika Gupta, Moira Bowdrey
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Patent number: 10413522Abstract: 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: GrantFiled: March 17, 2017Date of Patent: September 17, 2019Assignee: MEMORIAL SLOAN-KETTERING CANCER CENTERInventors: Joan Massague, Adrienne Boire, Qing Chen
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Patent number: 10413523Abstract: 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: GrantFiled: November 16, 2017Date of Patent: September 17, 2019Assignee: BIOADATP, LLCInventor: Kevin Meehan
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Patent number: 10413524Abstract: 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: GrantFiled: August 22, 2018Date of Patent: September 17, 2019Inventor: John Michael Pezzuto
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Patent number: 10413525Abstract: 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: GrantFiled: November 7, 2017Date of Patent: September 17, 2019Assignee: Sun Pharmaceutical Industries LimitedInventors: Ravindra Agarwal, Tarun Singhal, Ravi Kochhar
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Patent number: 10413526Abstract: 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: GrantFiled: March 25, 2016Date of Patent: September 17, 2019Assignee: Kolinpharma S.p.A.Inventors: Emanuele Lusenti, Ritapaola Petrelli
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Patent number: 10413527Abstract: Substituted phenylpyrrolecarboxamide compounds such as those represented by Formula A can be used in the treatment of HIV infection and related conditions.Type: GrantFiled: November 1, 2018Date of Patent: September 17, 2019Assignees: New York Blood Center, Inc., The United States of America, as Represented by the Secretary, Department of Health and Human ServicesInventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
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Patent number: 10413528Abstract: 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: GrantFiled: October 20, 2014Date of Patent: September 17, 2019Inventor: John H. Plumb
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Patent number: 10413529Abstract: 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: GrantFiled: April 28, 2017Date of Patent: September 17, 2019Assignee: UNIVERSITY OF MASSACHUSETTSInventors: Murugappan Muthukumar, Benjamin Mohr
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Patent number: 10413530Abstract: 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: GrantFiled: January 18, 2018Date of Patent: September 17, 2019Assignee: Alpha-1 Biologics, LLCInventors: Cynthia L. Bristow, Ronald H. Winston
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Patent number: 10413531Abstract: 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: GrantFiled: March 28, 2018Date of Patent: September 17, 2019Assignee: Abraxis BioScience, LLCInventor: Neil P. Desai
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Patent number: 10413532Abstract: 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: GrantFiled: June 20, 2018Date of Patent: September 17, 2019Assignee: RHIZEN PHARMACEUTICALS SAInventors: Swaroop K. Vakkalanka, Srikant Viswanadha
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Patent number: 10413533Abstract: 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: GrantFiled: November 12, 2015Date of Patent: September 17, 2019Assignee: Memorial Sloan Kettering Cancer CenterInventors: Richard Kolesnick, Adriana Haimovitz-Friedman, Evis Sala, Zvi Fuks
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Patent number: 10413534Abstract: 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: GrantFiled: February 13, 2018Date of Patent: September 17, 2019Assignee: NEURALSTEM, INC.Inventor: Karl K. Johe
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Patent number: 10413535Abstract: 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: GrantFiled: July 7, 2016Date of Patent: September 17, 2019Assignee: AXEROVISION, INC.Inventor: Achim H. Krauss
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Patent number: 10413536Abstract: 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: GrantFiled: September 26, 2017Date of Patent: September 17, 2019Assignee: Boehringer Ingelheim International GmbHInventor: Ulrich Reiser
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Patent number: 10413537Abstract: 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: GrantFiled: October 26, 2018Date of Patent: September 17, 2019Assignee: Samumed, LLCInventors: Sunil Kumar KC, Chi Ching Mak, Brian Walter Eastman, Jianguo Cao, Gopi Kumar Mittapalli
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Patent number: 10413538Abstract: 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: GrantFiled: May 1, 2014Date of Patent: September 17, 2019Assignee: BioNumerik Pharmaceuticals, Inc.Inventor: Frederick H Hausheer
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Patent number: 10413539Abstract: 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: GrantFiled: November 22, 2017Date of Patent: September 17, 2019Assignee: Immunomedics, Inc.Inventors: Serengulam V. Govindan, David M. Goldenberg
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Patent number: 10413540Abstract: 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: GrantFiled: March 30, 2018Date of Patent: September 17, 2019Assignee: Corcept Therapeutics, Inc.Inventor: Hazel Hunt
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Patent number: 10413541Abstract: 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: GrantFiled: November 17, 2017Date of Patent: September 17, 2019Assignee: Lixte Biotechnology, Inc.Inventors: John S. Kovach, Salvatore Lecca, Manuel Mameli
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Patent number: 10413542Abstract: 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: GrantFiled: April 11, 2018Date of Patent: September 17, 2019Assignees: Buck Institute for Research on Aging, Unity Biotechnology, Inc., Mayo Foundation for Medical Education and ResearchInventors: 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
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Patent number: 10413543Abstract: 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: GrantFiled: February 12, 2016Date of Patent: September 17, 2019Assignee: SUN PHARMA ADVANCED RESEARCH COMPANY LTD.Inventors: Nitin Bhalachandra Dharmadikari, Yashoraj Zala, Ashwini Gadkari
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Patent number: 10413545Abstract: 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: GrantFiled: June 23, 2017Date of Patent: September 17, 2019Assignee: Janssen Pharmaceutica NVInventors: Peter J Connolly, Tianbao Lu
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Patent number: 10413546Abstract: 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: GrantFiled: February 23, 2016Date of Patent: September 17, 2019Assignees: NATIONAL UNIVERSITY CORPORATION TOTTORI UNIVERSITY, NIPPON MEDICAL SCHOOL FOUNDATION, NIPPON CHEMIPHAR CO., LTD.Inventors: Takeshi Nishino, Shinsuke Kato, Masako Kato, Hidenori Suzuki, Ken Okamoto
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Patent number: 10413547Abstract: 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: GrantFiled: September 26, 2018Date of Patent: September 17, 2019Assignee: G1 Therapeutics, Inc.Inventors: Jay Copeland Strum, John E. Bisi, Patrick Joseph Roberts, Jessica A. Sorrentino
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Patent number: 10413548Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.Type: GrantFiled: July 10, 2017Date of Patent: September 17, 2019Assignees: Beth Israel Deaconess Medical Center, Inc., The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
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Patent number: 10413549Abstract: 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: GrantFiled: October 24, 2017Date of Patent: September 17, 2019Assignee: Eutropics Pharmaceuticals, Inc.Inventors: David Richard, Michael H. Cardone
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Patent number: 10413550Abstract: 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: GrantFiled: June 23, 2017Date of Patent: September 17, 2019Assignees: The Institute of Cancer Research, Cancer Research Technology Limited, Vernalis (R&D) LimitedInventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Patent number: 10413551Abstract: 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: GrantFiled: February 22, 2018Date of Patent: September 17, 2019Assignee: The General Hospital CorporationInventor: David R. Elmaleh
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Patent number: 10413552Abstract: 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: GrantFiled: June 17, 2016Date of Patent: September 17, 2019Assignee: The Hospital for Sick ChildrenInventors: James Rutka, Claudia Faria
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Patent number: 10413553Abstract: 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: GrantFiled: February 1, 2018Date of Patent: September 17, 2019Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Giles Albert Brown, Julie Elaine Cansfield, Benjamin Gerald Tehan
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Patent number: 10413554Abstract: 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: GrantFiled: January 31, 2018Date of Patent: September 17, 2019Inventors: Paul Donnelly, James Hilton, Peter Crouch
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Patent number: 10413555Abstract: 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: GrantFiled: November 24, 2015Date of Patent: September 17, 2019Assignee: TROPHEA DEVELOPMENT ABInventors: Jan Faergemann, Gudmundur Johannsson, Claes Ohlsson, Derek Gregory Batcheller, Jörgen Johnsson, Jan Törnell
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Patent number: 10413556Abstract: 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: GrantFiled: March 21, 2019Date of Patent: September 17, 2019Inventor: Moshe Shifrine
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Patent number: 10413557Abstract: 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: GrantFiled: December 22, 2015Date of Patent: September 17, 2019Assignee: FORENDO PHARMA LTD.Inventors: Leena Hirvelä, Pasi Koskimies, Risto Lammintausta, Marjo Hakola, Maire Eloranta
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Patent number: 10413558Abstract: 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: GrantFiled: October 19, 2015Date of Patent: September 17, 2019Assignee: TARGETED THERAPIES RESEARCH AND CONSULTING CENTER SPRLInventor: Marc Zeicher