Patents Issued in June 12, 2018
  • Patent number: 9994510
    Abstract: The present invention relates to anaerobic curable compositions, such as adhesives and sealants, containing blocked acrylic acid compounds. The blocked acrylic acid compounds are labile (meth)acrylic acid compounds having an acetal linkage, which cleaves to release (meth)acrylic acid during anaerobic cure. In this way, the block acrylic acid compounds acts as an adhesion promoter thereby promoting adhesion to various substrates.
    Type: Grant
    Filed: November 1, 2016
    Date of Patent: June 12, 2018
    Assignee: Henkel IP & Holding GmbH
    Inventors: Andrew D. Messana, Sean M. Burdzy, Joel D. Schall, Anthony F. Jacobine
  • Patent number: 9994511
    Abstract: The present invention is directed to pharmaceutical compositions comprising compounds found in Harderian gland secretions, a method of treating dry eye in a human comprising ophthalmically administering an effective amount of a compound, e.g. a lipid compound, found in Harderian gland secretions, pharmaceutical compositions comprising said lipid compounds, as identified by characteristic chemical data and mass spectra of said lipid compounds, said lipid compound in essentially pure form, and an ophthalmic vehicle comprising a therapeutic agent and a compound present in the secretions of the Harderian gland, e.g. a lipid compound, found in the secretions of the Harderian gland, e.g. a rabbit Harderian gland.
    Type: Grant
    Filed: February 23, 2016
    Date of Patent: June 12, 2018
    Assignee: RestorTears, LLC
    Inventors: Daniel M. Albert, Arthur S. Polans
  • Patent number: 9994512
    Abstract: A processes is for purifying an amine compound from a feed solvent which includes an amine salt of the amine compound. The process includes heating the feed solvent in a single stage evaporator of a reclaimer at a reduced operating pressure by feeding the evaporator with a constant amount of thermal energy; and evaporating the amine compound to purity the amine compound from the feed solvent.
    Type: Grant
    Filed: March 28, 2013
    Date of Patent: June 12, 2018
    Assignee: HTC Purenergy Inc.
    Inventors: Ahmed A. Aboudheir, Walid H. Elmoudir
  • Patent number: 9994513
    Abstract: Provided are a resist and a compound for the resist improving the sensitivity, the resolution and the line edge roughness (LER) in a good balance without spoiling basic properties of a chemical amplification resist such as pattern shape, dry etching resistance, heat resistance and the like. Provided are a method for producing an alicyclic ester compound expressed by general formula (1), an alicyclic ester compound expressed by general formula (1), a (meth)acrylic copolymer obtained by polymerization of the alicyclic ester compound, and a photosensitive resin composition containing the (meth)acrylic copolymer. A method for producing an alicyclic ester compound expressed by general formula (1) includes reacting an adamantane compound expressed by general formula (2) with hydroxyalkylamine expressed by general formula (3) to produce an adamantaneamide compound expressed by general formula (4), and then reacting the adamantaneamide compound expressed by general formula (4) with (meth)acrylic acid.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: June 12, 2018
    Assignee: Mitsubishi Gas Chemical, Inc.
    Inventors: Shoichi Hayakawa, Hiroshi Horikoshi, Kikuo Furukawa, Hiroyasu Tanaka, Hiroyuki Tanagi
  • Patent number: 9994514
    Abstract: The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g.
    Type: Grant
    Filed: May 8, 2013
    Date of Patent: June 12, 2018
    Assignee: AEROMICS, INC.
    Inventors: Marc F. Pelletier, George William Farr, Paul Robert McGuirk, Christopher H. Hall, Walter F. Boron
  • Patent number: 9994515
    Abstract: The present invention relates to substituted aryl naphthyl methanone oximes of general formula (I), their process for preparation and their derivatives, salts, pharmaceutical composition thereof and their use in treatment of chronic myelogenous leukemia, acute myelogenous leukemia, lymphoma, multiple myeloma, solid tumor forming cell-lines including such as breast cancer, endometrial cancer colon cancer, prostate cancer and killing of drug resistant cancer stem cells, as subject in need thereof.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: June 12, 2018
    Assignee: Council of Scientific & Industrial Research
    Inventors: Sabyasachi Sanyal, Atul Kumar, Naibedya Chattopadhyay, Jawahar Lal, Arun Kumar Trivedi, Dipak Datta, Srikanta Kumar Rath, Tahseen Akhtar, Shailendra Kumar Dhar Dwivedi, Manisha Yadav, Bandana Chakravarti, Abhishek Kumar Singh, Jay Sharan Mishra, Nidhi Singh, Anil Kumar Tripathi
  • Patent number: 9994516
    Abstract: Novel urethane-acrylate (UAC) Star monomers and polyurethane-acrylate (PUAC) aerogel polymers derived therefrom are described herein, along with other novel, related monomers and polymers. Also described herein are processes for preparing the UAC Star monomers, the PUAC aerogel polymers, and the other related monomers and polymers. The PUAC and related polymers herein are useful in various applications including in structural and thermal insulation.
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: June 12, 2018
    Assignee: The Curators of The University of Missouri
    Inventors: Nicholas Leventis, Chariklia Sotiriou-Leventis, Abhishek Bang
  • Patent number: 9994517
    Abstract: There is disclosed a process for preparing taurine from alkali taurinate or a mixture of alkali taurinate, alkali ditaurinate and alkali tritaurinate by reacting alkali taurinate with an ammonium salt to yield ammonium taurinate, which is decomposed by heating and removing ammonia to afford taurine. Suitable ammonium salt is selected from the group of ammonium sulfate, ammonium bisulfate, ammonium chloride, ammonium bromide, ammonium carbonate, ammonium bicarbonate, ammonium phosphate, ammonium hydrogen phosphate, ammonium dihydrogen phosphate, ammonium nitrate, ammonium carboxylate, ammonium alkyl sulfonate, ammonium aryl sulfonate, and a mixture of two or more thereof.
    Type: Grant
    Filed: November 17, 2017
    Date of Patent: June 12, 2018
    Assignee: VITAWORKS IP, LLC
    Inventor: Songzhou Hu
  • Patent number: 9994518
    Abstract: Disclosed are compounds of Formula (IVA), or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof: Formula (IVA), wherein “RIa”, “RIb”, “RIc”, “RId”, “RIe”, are defined herein above, which compounds are believed suitable for use in positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7 nAChR) receptors, for example, those found in the cerebral cortex and the hippocampus. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Alzheimer's disease (AD), schizophrenia, and Parkinson's disease (PD), or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
    Type: Grant
    Filed: June 11, 2015
    Date of Patent: June 12, 2018
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Kenneth Leavitt, Brendan Crowley, Ian M. Bell, Andrew Harvey, Thomas Avery, Dharam Paul, Justin Ripper, Belinda Huff, Rajinder Singh, Laurent Schaeffer, Christophe Joseph, Christophe Morice, Bruno Giethlen, Patrick Bazzini, Aurelie Fromeyer
  • Patent number: 9994519
    Abstract: The present invention relates to synthetic organic antioxidants of small molecules. The novel dithiol-containing compounds in this invention possess strongest possible capability as both scavenger for free radicals and antioxidant. This invention is directed to novel molecules as prodrugs of the novel dithiol-containing compounds, their rational design, their feasible preparation route by means of synthetic organic chemistry, and their potential uses in application to treatment and/or prevention of major diseases associated with oxidative stress, such as Alzheimer's disease, Parkinson's disease, cancer, diabetes, HIV, acne, cardiovascular disease, renal disease, hypertension, hypercholesterolemia, hyperlipidemia, rheumatoid arthritis, inflammation, pain, aging, stroke, cataract, glaucoma, age-related macular degeneration, etc.
    Type: Grant
    Filed: April 18, 2013
    Date of Patent: June 12, 2018
    Inventor: Yansong Lu
  • Patent number: 9994520
    Abstract: The present invention provides an enzymatic process for the preparation of (S)-5-(4-Fluoro-phenyl)-5-hydroxy-Imorpholin-4-yl-pentan-1-one by the reduction of 1-(4-Fluoro-phenyl)-5-morpholin-4-yl-pentane-1,5-dione by using a suitable enzyme or by the resolution of (R, S)-5-(4-Fluoro-phenyl)-5-hydroxy-1 morpholin-4-yl-pentan-1-one by using an enzyme. The present invention also provides process for the preparation of Ezetimibe comprising the steps of a) protecting the compound (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1 morpholin-4-yl-pentan-1-one with hydroxy protecting group b) hydrolyzing the obtained compound c) condensing with a chiral auxiliary d) reacting with an protected imine compound e) converting to alkyl ester f) cyclizing and g) deprotecting to obtain Ezetimibe.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: June 12, 2018
    Assignee: Mylan Laboratories Limited
    Inventors: Mofazzal Husain, Srikanth G. S. C., Swapna Thorpunuri, Debashish Datta
  • Patent number: 9994521
    Abstract: The present invention provides compounds and compositions that inhibit Factor XIa or kallikrein and methods of using these compounds and composition.
    Type: Grant
    Filed: October 11, 2016
    Date of Patent: June 12, 2018
    Assignee: eXIthera Pharmaceuticals, Inc.
    Inventors: Robert A. Chrusciel, Robert C. Gadwood, Neil J. Hayward, Michael J. Melnick, Manuel A. Navia, Toni J. Poel, Frans L. Stassen, Catherine A. Stewart
  • Patent number: 9994522
    Abstract: The present invention provides a new amorphous form of apremilast, pharmaceutical compositions comprising same, methods for preparation and use thereof in treating conditions mediated by inhibition of TNF-? production or inhibition of phosphodiesterase 4 (PDE4), e.g., psoriatic arthritis and other chronic inflammatory diseases.
    Type: Grant
    Filed: July 20, 2014
    Date of Patent: June 12, 2018
    Assignee: MAPI PHARMA LTD.
    Inventors: Shai Rubnov, Ehud Marom
  • Patent number: 9994523
    Abstract: The invention relates to organic salts of Saxagliptin and processes for their preparation.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: June 12, 2018
    Assignee: Apotex Inc.
    Inventors: Padiyath Mohammed Akbarali, Venkata Ramana Kintali, Shreenivasa Murthy H N, Prakash Bhaskar Shetty, Narendra Manjeshwar Mallya, Venkataramana Lachhi Reddy
  • Patent number: 9994524
    Abstract: The T cells specific to human collagen type II, one of the possible autoantigens, have a crucial role in the development of rheumatoid arthritis in the context of HLA-DR4. The protein-protein interactions between the T cell receptor (TCR) and the type II collagen linked to the allele MHC of class II HLA-DR4 may thus represent the target for the development of new drugs against rheumatoid arthritis. Using computational virtual screening techniques, families of pharmacologically active molecules have been identified that interfere with the TCR/collagen II-MHCII interaction. The compounds identified here open up new possibilities in the treatment of rheumatoid arthritis.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: June 12, 2018
    Assignees: CONSIGLIO NAZIONALE DELLE RICERCHE, UNIVERSITÀ CATTOLICA DEL SACRO CUORE
    Inventors: Maria Cristina De Rosa, Francesco Ria, Bruno Giardina, Gianfranco Ferraccioli, Davide Pirolli, Chiara Nicolo′
  • Patent number: 9994525
    Abstract: The present invention relates to new histamine H3 (H3) receptor subtype selective ligands of the general formula (I) and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and the use of these compounds as medicaments for treatment and/or prevention of conditions which require modulation of H3 receptors. The invention also cover the combinations of a compound of the general formula (I) and an acetylcholinesterase inhibitor.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: June 12, 2018
    Assignee: Richter Gedeon Nyrt.
    Inventors: Gizella Bartáné Szalai, Gäbor András Wágner, Béla Kiss, Éva Schmidt, Ottília Balázs, Noémi Nagy
  • Patent number: 9994526
    Abstract: Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.
    Type: Grant
    Filed: August 12, 2016
    Date of Patent: June 12, 2018
    Assignee: LUNDBECK PHARMACEUTICALS ITALY S.p.A.
    Inventors: Mariano Stivanello, Florian Anton Martin Huber, Antonio Ricci
  • Patent number: 9994527
    Abstract: Provided herein are modified amino acids comprising an azido group, polypeptides, antibodies and conjugates comprising the modified amino acids, and methods of producing the polypeptides, antibodies and conjugates comprising the modified amino acids. The polypeptides, antibodies and conjugates are useful in methods of treatment and prevention, methods of detection and methods of diagnosis.
    Type: Grant
    Filed: May 24, 2017
    Date of Patent: June 12, 2018
    Assignee: SUTRO BIOPHARMA, INC.
    Inventors: Ryan Stafford, Christopher D. Thanos, Wenjin Yang
  • Patent number: 9994528
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R2, R4, R5, R6, R7, R8, R9, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 11, 2015
    Date of Patent: June 12, 2018
    Assignee: Cytokinetics, Inc.
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Scott Collibee, Chihyuan Chuang, Jeff Gardina, Bradley P. Morgan, Alex R Muci, Xiangping Qian, Antonio Romero, Jeffrey Warrington, Zhe Yang
  • Patent number: 9994529
    Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, and Z are as defined herein, and methods of making and using the same.
    Type: Grant
    Filed: February 14, 2017
    Date of Patent: June 12, 2018
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Michael Jonathan Bury, Linda N. Casillas, Adam K. Charnley, Michael P. Demartino, Xiaoyang Dong, Patrick M. Eidam, Pamela A. Haile, Robert W. Marquis, Jr., Joshi M. Ramanjulu, Joseph J. Romano, Ami Lakdawala Shah, Robert R. Singhaus, Jr., Gren Wang
  • Patent number: 9994530
    Abstract: A method of producing an optically active 2-methylpiperazine includes: adding a solvent to a solution of the optically active 2-methylpiperazine to carry out solvent replacement, and then being crystallized to obtain crystals of the optically active 2-methylpiperazine. The method allows the optically active 2-methylpiperazine to be purified during the crystallization process, and thus it is possible to obtain an optically active 2-methylpiperazine having a high quality.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: June 12, 2018
    Assignee: Toray Fine Chemicals Co., Ltd.
    Inventors: Seiji Morii, Takeshi Nishikawa
  • Patent number: 9994531
    Abstract: An antioxidant composition which comprises: (a) methylenebis(di-n-butyldithiocarbamate); and (b) an alkylated diphenylamine derivative of triazole wherein the alkyl group on at least one of the phenyl groups is C8 or higher. Lubricating compositions containing the antioxidant composition are also contemplated.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: June 12, 2018
    Assignee: VANDERBILT CHEMICALS, LLC
    Inventor: Vincent J. Gatto
  • Patent number: 9994532
    Abstract: A method and compound includes mixing a salt compound to 2-butyne-1,4-diol in an alcohol to create a mixture; adding a solution of dichloroglyoxime in an alcohol to the mixture to create 3,3?-bis-isoxazole-4,4?,5,5?-tetryltetramethanol; and nitrating the 3,3?-bis-isoxazole-4,4?,5,5?-tetryltetramethanol to create 3,3?-bis-isoxazole-4,4?,5,5?-tetrylbis(methylene) tetranitrate, which has the structural formula: The alcohol may include ethanol, wherein the adding may occur at 60° C., or alternatively the adding may occur at 80° C. The alcohol may include n-butanol, wherein the adding may occur at 100° C., or alternatively the adding may occur at 120° C. The mixing may occur at 120° C. The method may further include cooling the nitrated 3,3?-bis-isoxazole-4,4?,5,5?-tetryltetramethanol to 0° C.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: June 12, 2018
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Jesse J. Sabatini, Gregory W Drake, Leah A. Wingard
  • Patent number: 9994533
    Abstract: The present invention provides the use of ATG in the preparation of a reagent for adjusting the activity of PP2A; and the use of ATG in increasing the activity of PP2A in 293T cells. The present invention also provides the use of the arctigenin in the preparation of the medicine for reducing the proteinuria of the diabetic mice. The present invention also provides the use of the arctigenin in the preparation of the reagent for inhibiting the expression of the NOX4 gene. The present invention also provides analogs of arctigenin and application thereof. The present invention provides a novel use of ATG for modulating PP2A activity, and ATG can also significantly reduce proteinuria in diabetic mice. At the same time, arctigenin could significantly inhibit the expression of NOX4 in STZ-eNOS?/? mice glomeruli. The ATG analogs of the present invention are more effective than the native ATG.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: June 12, 2018
    Assignee: Longhua Hospital Shanghai University of Traditional Chinese Medicine
    Inventors: Yifei Zhong, Honggang Gu
  • Patent number: 9994534
    Abstract: Compositions and methods are for inducing, promoting or otherwise facilitating pain relief. More particularly, sub-normovasodilatory doses of nitric oxide donors are used in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, especially neuropathic pain. In some applications of the method, nitric oxide donors can be administered by any suitable route so as to provide concentrations of NO that are about ½ to 10?15 times those known to induce vasodilation in normal circulations.
    Type: Grant
    Filed: August 4, 2017
    Date of Patent: June 12, 2018
    Assignee: THE UNIVERSITY OF QUEENSLAND
    Inventor: Maree Therese Smith
  • Patent number: 9994535
    Abstract: Compounds represented by structural formulas described herein, such as Structural Formula (I): or a pharmaceutically acceptable salt thereof are useful in treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.
    Type: Grant
    Filed: February 9, 2017
    Date of Patent: June 12, 2018
    Assignee: University of Florida Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 9994536
    Abstract: Embodiments of the present disclosure provide for compositions including a compound, pharmaceutical compositions including the compound, methods of treatment of a disease or related condition (e.g., neurological disease on condition), methods of treatment using compositions or pharmaceutical compositions, and the like.
    Type: Grant
    Filed: May 1, 2015
    Date of Patent: June 12, 2018
    Assignee: Torrey Pines Institute for Molecular Studies
    Inventors: Madepalli K. Lakshmana, Adel Nefzi, Richard Houghten, Dmitriy Minond
  • Patent number: 9994537
    Abstract: Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
    Type: Grant
    Filed: August 8, 2017
    Date of Patent: June 12, 2018
    Assignee: ABIDE THERAPEUTICS, INC.
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Olivia D. Weber, Dong-Hui Wang
  • Patent number: 9994538
    Abstract: Compounds of the formula (I) and (IA) wherein X is —O(CO)—; R1 is C1-C12haloalkyl or C6-C10haloaryl; R2 is located in position 7 of the coumarinyl ring and is OR8; R2a, R2b and R2C independently of each other are hydrogen; R3 is C1-C8haloalkyl or C1-C8haloalkyl; R4 is hydrogen; and R8 is C1-C6alkyI; are suitable as photosensitive acid donors in the preparation of photoresist compositions such as used for example in the preparation of spacers, insulating layers, interlayer dielectric films, insulation layers, planarization layers, protecting layers, overcoat layers, banks for electroluminescence displays and liquid crystal displays (LCD).
    Type: Grant
    Filed: January 29, 2016
    Date of Patent: June 12, 2018
    Assignee: BASF SE
    Inventors: Keita Tanaka, Yuki Matsuoka, Kazuhiko Kunimoto, Toshikage Asakura, Hisatoshi Kura
  • Patent number: 9994539
    Abstract: The disclosure relates to a method for forming 2,5-furan dicarboxylic acid (FDCA) from aldaric acids. The aldaric acids are dehydrating and cyclizing via acid catalysis to form the FDCA product. Aldaric acids such as galactaric acid, gularic acid, mannaric acid, and glucaric acid can be used in the disclosed method, and the aldaric acids can be obtained from form renewable biomass sources which contain pectin, alginate, and/or other biomass carbohydrates. The FDCA can be used as a renewable feedstock for consumer product polymeric materials such as polyalkylene furoate polymers.
    Type: Grant
    Filed: July 11, 2017
    Date of Patent: June 12, 2018
    Assignee: BOARD OF TRUSTEES OF MICHIGAN STATE UNIVERSITY
    Inventors: Dennis J. Miller, Lars Peereboom, Evan Wegener, Matthew Gattinger
  • Patent number: 9994540
    Abstract: The invention relates to a method for producing 2-substituted 4-methyl-tetrahydropyrans of general formula (I) from starting materials containing at least one 2-substituted 4,4-dimethyl-1,3-dioxane of general formula (II).
    Type: Grant
    Filed: April 8, 2015
    Date of Patent: June 12, 2018
    Assignee: BASF SE
    Inventors: Stefan Rüdenauer, Timon Stork
  • Patent number: 9994541
    Abstract: The present invention is directed to a class of anti-inflammatory, antioxidant nitroalkene compounds used in biological or biochemical applications to reduce oxidative stress or damage. The nitroalkene compounds described herein further avoid disadvantageous metabolism currently present in this field.
    Type: Grant
    Filed: August 23, 2016
    Date of Patent: June 12, 2018
    Inventors: Carlos Batthyány, Gloria Virginia López, Rosina Dapueto, Carlos Escande, Jorge Rodriguez Duarte
  • Patent number: 9994542
    Abstract: The invention provides compounds of formula (I) or salts thereof: wherein: A, B, C, D, W, X, Y and Z are as defined in the specification, and at least one of A, B, C, D, W, X, Y and Z is OR1; each R1 being independently H or C(?O)R2, and at least one R1 group being C(?O)R2; where each R2 is selected from: CHR3NHR4, where R4 is H and R3 is a group selected from CH3, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-3-(1H-indole), CH2CH2SCH3, CH2OH, CHOHCH3, CH2SH, CH2SeH and CH2PhpOH, wherein said R3 group can optionally be substituted by one or more groups selected from halogen, cyano, nitro, ORA or C1-C4 alkyl; or R3 and R4 together with the C and N atoms to which they are attached form a 5-membered heteroalkyl ring, wherein said heteroalkyl ring can optionally be substituted by one or more groups selected from halogen, cyano, nitro, ORA or C1-C3 alkyl, wherein RA is C1-C4 alkyl optionally substituted with one or more halogen, cyano or nitro groups.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: June 12, 2018
    Assignee: Amazentis SA
    Inventors: Christopher Lawrence Rinsch, Rune Andreas Ringom
  • Patent number: 9994543
    Abstract: Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: wherein R2, R3 and R4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.
    Type: Grant
    Filed: July 17, 2015
    Date of Patent: June 12, 2018
    Assignee: CHIROGATE INTERNATIONAL INC.
    Inventors: Shih-Yi Wei, Yu-Chih Yeh, Min-Kuan Hsu, Li-Ta Kao
  • Patent number: 9994544
    Abstract: The present invention concerns a method for preparing 1,3,5-trioxane by trimerization of formaldehyde in the presence of methanesulfonic acid. The invention also concerns the use of at least one catalyst comprising methanesulfonic acid for the trimerization of formaldehyde into 1,3,5-trioxane.
    Type: Grant
    Filed: July 17, 2015
    Date of Patent: June 12, 2018
    Assignee: Arkema France
    Inventors: Bernard Monguillon, Jean-Alex Laffitte
  • Patent number: 9994545
    Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: June 12, 2018
    Assignees: Aragon Pharmaceuticals, Inc., Sloan-Kettering Institute For Cancer Research
    Inventors: Anna Dilhas, Mark R. Herbert, Ouathek Ouerfelli, Nicholas D. Smith
  • Patent number: 9994546
    Abstract: The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: June 12, 2018
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Wenqing Yao
  • Patent number: 9994547
    Abstract: Disclosed are compounds of formula 1: which are useful as inhibitors of TBK1. Also disclosed are pharmaceutical compositions which contain the compounds, methods for treatment of conditions associated with TBK1, and processes for making the compounds and intermediates thereof.
    Type: Grant
    Filed: October 2, 2015
    Date of Patent: June 12, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Simone Bigi, Walter Keung, Steve Swann, Phong H. Vu, Steven John Woodhead, Anthony R. Gangloff
  • Patent number: 9994548
    Abstract: Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: June 12, 2018
    Assignees: Georgetown University, Duke University
    Inventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar, Venkata M. Yenugonda, Edward D. Levin, Amir H. Rezvani
  • Patent number: 9994549
    Abstract: A compound represented by general formula (I) has a strong Axl inhibitory activity by introducing a distinctive bicyclic structure in which a saturated carbon ring is fused to a pyridone ring, and can be a therapeutic agent for Axl-related diseases, for example, cancer such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases
    Type: Grant
    Filed: December 8, 2016
    Date of Patent: June 12, 2018
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Takayuki Inukai, Jun Takeuchi, Tomoko Yasuhiro
  • Patent number: 9994550
    Abstract: Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds.
    Type: Grant
    Filed: January 7, 2015
    Date of Patent: June 12, 2018
    Assignee: 3-V Biosciences, Inc.
    Inventors: Allan S. Wagman, Russell J. Johnson, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu, Greg Duke, Yamini Ohol-Gupta, Timothy Heuer, Marie O'Farrell
  • Patent number: 9994551
    Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: June 12, 2018
    Assignee: Genentech, Inc.
    Inventors: Benjamin Fauber, Monique Bodil van Niel, Andrew Cridland, Christopher Hurley, Jonathan Killen, Stuart Ward, Paul Winship
  • Patent number: 9994552
    Abstract: Compounds and compositions useful for treating disorders related to Kit are described herein.
    Type: Grant
    Filed: October 17, 2016
    Date of Patent: June 12, 2018
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Lucian V. DiPietro, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Steven Mark Wenglowsky, Douglas Wilson, Yulian Zhang
  • Patent number: 9994553
    Abstract: A process for purifying 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazine-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulene-2-yl)-1H-1,2,4-triazole-3,5-diamine free base is described, the process comprising a) dissolving a quantity of crude 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazine-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulene-2-yl)-1H-1,2,4-triazole-3,5-diamine in a mixed solvent of C1-5 alcohol and water, together with an acid, and b) increasing the pH of the solution resulting from (a) until 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazine-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulene-2-yl)-1H-1,2,4-triazole-3,5-diamine free base is precipitated from the alcohol-water mixed solvent.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: June 12, 2018
    Assignee: BerGenBio AS
    Inventor: Lene Raunkjaer Petersen
  • Patent number: 9994554
    Abstract: Provided are methods and compositions for use in therapy, and in particular for treating cancer, preferably drug-resistant cancer, and/or radiation resistant cancer. The compounds may be used for reducing tumor size in a mammalian subject and for inducing apoptosis in a tumor cell. The methods are effective on tumor cells that are resistant to drugs such as temozolomide, doxorubicin, and geldanamycin, as well as non-resistant tumor cells. Further provided are barbiturate and thiobarbiturates diene compounds for use in treating cancer, and uses, methods and compositions relating to these compounds.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: June 12, 2018
    Assignee: NUHOPE LLC
    Inventors: James R. Connor, Sang Yong Lee, Thomas James Brown, Phillip Martin Cowley
  • Patent number: 9994555
    Abstract: The invention provides compounds effective as inhibitors of monocarboxylate transporters such as MCT1 and MCT4, which can be used for treatment of medical conditions wherein treatment of the condition with a compound having an inhibitor effect on MCT1, MCT4, or both is medically indicated. Compounds of the invention can have antitumor, antidiabetes, anti-inflammatory, or immunosuppressive pharmacological effects, and can be effective for treatment of cancer and of type II diabetes.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: June 12, 2018
    Assignee: The Scripps Research Institute
    Inventors: Thomas D. Bannister, Hui Wang, Chao Wang, John L. Cleveland
  • Patent number: 9994556
    Abstract: Provided herein are compounds of the formulas: which are 90-kDa heat shock protein inhibitors. Pharmaceutical compositions of the compounds are also provided. In some aspects, these compounds may be used for the treatment of diseases, including cancer, e.g., cancers of the breast, the prostate, and the head & neck.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: June 12, 2018
    Assignee: UNIVERSITY OF KANSAS
    Inventors: Jinbo Zhao, Huiping Zhao, Brian S. J. Blagg
  • Patent number: 9994557
    Abstract: Disclosed herein plant propagation materials, methods of manufacturing, formulations and uses thereof. The plant propagation materials disclosed herein may comprise a strigolactone obtained by a biosynthetic process. The plant propagation material may comprise a chemical mimic of a strigolactone. The strigolactone may be 5-deoxystrigol. Methods of manufacturing the plant propagation materials may comprise a chemical process. Alternatively, methods of manufacturing the plant propagation material may comprise a biosynthetic process. The methods may comprise use of one or more polynucleotides. The polynucleotides may encode a metabolite. The polynucleotides may comprise one or more genes encoding one or more components of a strigolactone pathway.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: June 12, 2018
    Assignee: Asilomar Bio, Inc.
    Inventors: Eric A. Davidson, Travis S. Bayer, Oliver Windram, Yonek Hleba
  • Patent number: 9994558
    Abstract: The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).
    Type: Grant
    Filed: September 19, 2014
    Date of Patent: June 12, 2018
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Erkan Baloglu, Sharon Shacham, William Senapedis, Dilara McCauley, Yosef Landesman, Gali Golan, Ori Kalid, Sharon Shechter
  • Patent number: 9994559
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicycloheteroaryl-heteroaryl-benzoic acid compounds of the following formula (for convenience, collectively referred to herein as “BHBA compounds”), which, inter alia, are (selective) retinoic acid receptor beta (RAR?) (e.g., RAR?2) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR? (e.g., RAR?2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RAR? (e.g., RAR?2), that are ameliorated by the activation of RAR? (e.g., RAR?2), etc., including, e.g., neurological injuries such as spinal cord injuries.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: June 12, 2018
    Assignee: KING'S COLLEGE LONDON
    Inventors: Alan David Borthwick, Mark Trevor Mills, Jane Theresa Brown, Jonathan Patrick Thomas Corcoran, Maria Beatriz De Castro Vasconcelos Goncalves, Sarkis Barret Kalindjian