Patents Issued in July 3, 2018
  • Method for producing dry etching gas
    Patent number: 10011553
    Abstract: Provided is a method for producing fluoromethane and 3,3,3-trifluoro-2-(trifluoromethyl)propanoyl fluoride ((CF3)2CHCOF), which are useful as dry etching gases etc., safely and inexpensively with high purity. According to the method in which 1,1,3,3,3-pentafluoro-2-trifluoromethylpropyl methyl ether is pyrolyzed in a gas phase in the presence of a catalyst, the desired fluoromethane and 3,3,3-trifluoro-2-(trifluoromethyl)propanoyl fluoride can be obtained with high selectivity and high conversion of the starting material by a simple process in which a pyrolysis reaction is performed in a gas phase using the inexpensive starting material.
    Type: Grant
    Filed: November 12, 2013
    Date of Patent: July 3, 2018
    Assignee: DAIKIN INDUSTRIES, LTD.
    Inventors: Shingo Nakamura, Yuusuke Etou, Tatsuya Ohtsuka, Kanako Fukumoto, Masato Naitou
  • Alpha-branched alkenoic acids and the use of alpha-branched alkanoic and alkenoic acids as a fragrance
    Patent number: 10011554
    Abstract: The present invention refers to alpha branched alkanoic and alkenoic acids of formula (I) wherein X and R have the same meaning as given in the description. The invention further refers to perfume compositions and fragrance applications comprising them.
    Type: Grant
    Filed: July 31, 2017
    Date of Patent: July 3, 2018
    Assignee: Givaudan, S.A.
    Inventor: Jean-Pierre Bachmann
  • Methods of treating Parkinson's disease
    Patent number: 10011555
    Abstract: This invention is directed to novel compounds isolated or derived from Alpiniae oxyphyllae fructus, chemically synthesized novel compounds, methods of preparing the novel compounds and uses thereof as neuroprotectants or drugs for treating neurodegenerative diseases such as Parkinson's disease.
    Type: Grant
    Filed: October 9, 2017
    Date of Patent: July 3, 2018
    Assignee: University of Macau
    Inventors: Ming Yuen Lee, Zaijun Zhang, Guohui Li
  • Processes for preparing estolide base oils and oligomeric compounds that include cross metathesis
    Patent number: 10011556
    Abstract: Provided herein are estolide base oils and oligomeric compounds prepared from processes that include cross metathesis.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: July 3, 2018
    Assignee: Biosynthetic Technologies, LLC
    Inventors: Kelly Forest, Jeremy Forest, Jakob Bredsguard, Travis Thompson
  • Method for producing biphenylamines from azobenzenes by ruthenium catalysis
    Patent number: 10011557
    Abstract: The present invention relates to a novel method for preparing substituted biphenylamines.
    Type: Grant
    Filed: November 2, 2015
    Date of Patent: July 3, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Thomas Himmler, Lars Rodefeld, Jonathan Hubrich, Lutz Ackermann
  • Preparation of chiral amides and amines
    Patent number: 10011559
    Abstract: This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine substructure.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: July 3, 2018
    Assignee: SUNOVION PHARMACEUTICALS INC.
    Inventors: Hang Zhao, Stefan G. Koenig, Charles P. Vandenbossche, Surendra Singh, Harold Scott Wilkinson, Roger P. Bakale
  • Alternative process for the purification of an intermediate in the synthesis of non-ionic X-ray contrast agents
    Patent number: 10011560
    Abstract: Alternative continuous downstream processes for the production of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”) are described. Compound A is a key intermediate in the production of iodixanol and iohexol, which are two of the biggest commercially available non-ionic x-ray contrast media agents.
    Type: Grant
    Filed: May 24, 2017
    Date of Patent: July 3, 2018
    Assignee: GE HEALTHCARE AS
    Inventors: Torfinn Haaland, Arne Askildsen, Rita Heskestad Kalleberg, Sumihar Silalahi, Alf Martin Farbrot, Inger Dagny Saanum
  • Thickening/stabilizing agent and thickened/stabilized composition using the same
    Patent number: 10011561
    Abstract: A compound that thickens and/or gelatinizes a fluid organic substance to a desired viscosity, or uniformly stabilizes a composition containing the fluid organic substance. Also, a thickening/stabilizing agent including the compound, a thickened/stabilized composition including the thickening/stabilizing agent and a fluid organic substance, and a method for producing the composition. The compound according to the present invention is represented by Formula (1): (R2—HNOC)4-n—R1—(CONH—R3)n??(1) where R1 is a group resulting from removing four hydrogen atoms from the structural formula of an aromatic hydrocarbon or cyclohexane, R2 is, independently in each occurrence, an aliphatic hydrocarbon group containing 1 to 4 carbon atoms, R3 is, independently in each occurrence, an aliphatic hydrocarbon group containing 6 or more carbon atoms, and n is an integer of 1 to 3.
    Type: Grant
    Filed: July 7, 2015
    Date of Patent: July 3, 2018
    Assignees: DAICEL CORPORATION, YAMAGUCHI UNIVERSITY
    Inventors: Yuichi Sakanishi, Takashi Saeki, Mami Itoh
  • Long-chain dimethylaniline derivative compounds, their preparation methods, self-assembled textures, and uses thereof
    Patent number: 10011562
    Abstract: The present invention relates to long-chain dimethylaniline derivative compounds, their preparation methods, self-assembled texture, and uses thereof. Said compounds show ultralong acting anaesthetic effect, and belong to N-diethylaminoacetyl-2,6-dimethylaniline compounds, having a structure according to formula (I). Said compounds may self-assemble into micelle or gel in an aqueous solvent, and exert an in vivo elongated local anesthetic actions. Local anesthesia and/or analgesic activity can last more than 72 hours. The biomaterials can self-assemble into micelles or gels in water and have local anesthetic effect, as well as can further be used as the coating of medicinal bioactive molecules for treatment of pain, itching and the like and/or the drug carriers, together with as pharmaceutical adjuvants for delivery system. Thus, said materials have a favorable perspective.
    Type: Grant
    Filed: July 22, 2015
    Date of Patent: July 3, 2018
    Assignee: WEST CHINA HOSPITAL, SICHUAN UNIVERSITY
    Inventors: Lei Tang, Jin Liu, Wensheng Zhang, Jun Yang, Bowen Ke, Qinqin Yin
  • Lithium styrene sulfonate
    Patent number: 10011563
    Abstract: To provide a novel lithium styrene sulfonate which is capable of solving a problem of an increase of the production cost due to drying under atmospheric pressure or reduced pressure at a temperature of at least 40° C. and a problem of polymerization of lithium styrene sulfonate. The lithium styrene sulfonate is characterized in that when measured by using a Thermogravimetric-Differential Thermal Analyzer under measuring condition of heating at a temperature raising rate of 2° C./min in a nitrogen stream, the temperature at the top of the main endothermic peak in a range of from 80 to 170° C., is at least 120° C.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: July 3, 2018
    Assignee: TOSOH CORPORATION
    Inventors: Chikara Shiraishi, Senshi Kasahara
  • Mixed decyl mercaptans compositions and methods of making same
    Patent number: 10011564
    Abstract: Compositions comprising branched C10 mercaptans selected from the group consisting of 5-methyl-1-mercapto-nonane, 3-propyl-1-mercapto-heptane, 4-ethyl-1-mercapto-octane, 2-butyl-1-mercapto-hexane, 5-methyl-2-mercapto-nonane, 3-propyl-2-mercapto-heptane, 4-ethyl-2-mercapto-octane, 5-methyl-5-mercapto-nonane, and combinations thereof. Compositions comprising C11+ mercaptans, wherein the C11+ mercaptans are characterized by structure R6—SH, wherein R6 is an alkyl group derived from one or more C11+ monoolefins, and wherein the one or more C11+ monoolefins comprise C11 internal monoolefins, C12 internal monoolefins, C13 internal monoolefins, C14 internal monoolefins, 1-tetradecene, 1-hexadecene, or combinations thereof.
    Type: Grant
    Filed: August 4, 2017
    Date of Patent: July 3, 2018
    Assignee: Chevron Phillips Chemical Company LP
    Inventors: Michael S. Matson, Jim D. Byers, Jason L. Kreider
  • Compounds
    Patent number: 10011566
    Abstract: The present specification provides a compound of formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an ROR? and/or ROR?t mediated disease state.
    Type: Grant
    Filed: December 14, 2016
    Date of Patent: July 3, 2018
    Assignee: AstraZeneca AB
    Inventors: Frank Narjes, Roine Ingemar Olsson, Stefan Von Berg, Sarah Lever
  • Method for the synthesis of acrylate derivatives
    Patent number: 10011567
    Abstract: The present invention provides an improved synthesis of a salt of acrylate derivatives. The synthesis generally includes the preparation of an ester or an amide containing a leaving group followed by the formation of a salt.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: July 3, 2018
    Assignee: INNOSCI LLC
    Inventors: Mingwen Wang, Yue Zhang
  • Cyclohexyl pyridine derivative
    Patent number: 10011568
    Abstract: A problem of the present invention is to provide a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to cyclohexyl pyridine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof, wherein, ring A is 4-fluoro-2-methylphenyl or the like; X is a hydrogen atom or the like; R1 is carboxymethyl or the like; R2 is alkyl or the like; Y is 0-2 or the like; U is —N(CH3)COC(CH3)2-3,5-bistrifluoromethylphenyl or the like.
    Type: Grant
    Filed: June 22, 2017
    Date of Patent: July 3, 2018
    Assignee: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Kazuo Shimizu, Kohsuke Ohno, Takashi Miyagi, Yasunori Ueno, Hikaru Suzuki
  • Process for synthesizing oxidized lactam compounds
    Patent number: 10011569
    Abstract: The invention provides a method for the synthesis of dehydrogenated lactam drugs of Formula I:
    Type: Grant
    Filed: April 10, 2017
    Date of Patent: July 3, 2018
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Nucleic acid binding dyes with improved safety
    Patent number: 10011570
    Abstract: The invention provides compounds, including fluorescent nucleic acid dyes, and methods for use including nucleic acid detection. Further provided are kits, instruments and systems comprising compounds of the invention or adapted for use with compounds of the invention or other nucleic acid dyes.
    Type: Grant
    Filed: October 3, 2014
    Date of Patent: July 3, 2018
    Assignee: Biotium, Inc.
    Inventors: Fei Mao, Wai-Yee Leung, Lori M. Roberts, Patrick Gordon McGarraugh
  • Preparation method for aromatic heterocyclic compound used as selective JAK3 and/or JAK1 kinase inhibitor and application of aromatic heterocyclic compound
    Patent number: 10011571
    Abstract: An application of a compound having general formula (I) as JAK3 and/or JAK1 kinase and a preparation method for the compound.
    Type: Grant
    Filed: September 14, 2015
    Date of Patent: July 3, 2018
    Assignee: SHENZHEN CHIPSCREEN BIOSCIENCES, LTD.
    Inventors: Xianping Lu, Jindi Yu, Qianjiao Yang, Zhibin Li, Desi Pan, Song Shan, Jiangfei Zhu, Xianghui Wang, Xiangheng Liu, Zhiqiang Ning
  • Monocyclic isoxazolines as inhibitors of cholesterol ester transfer protein
    Patent number: 10011572
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein D1, D2 and D3 are each N, CH, or substituted CH, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: July 3, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pengcheng Patrick Shao, Feng Ye, Petr Vachal, Jayanth Thiruvellore Thatal
  • Human androgen receptor DNA-binding domain (DBD) compounds as therapeutics and methods for their use
    Patent number: 10011573
    Abstract: A compound having the structure of Formula I, wherein A is a substituted or unsubstituted aryl or heteroaryl group, D is a substituted or unsubstituted 5- or 6-membered heteroaryl or heterocyclyl group and E is a substituted or unsubstituted aryl, heteroaryl, cycloalkyl or heterocyclyl group. The compounds are used for the treatment of androgen modulated indications including cancer (prostate, breast, ovarian, endometrial or bladder cancer), hair loss, acne, hirsutism, ovarian cysts, polycystic ovary disease, precocious puberty and age related macular degeneration. The use of the compounds for the manufacture of a medicament for modulating AR activity, a method of treatment using such compounds and a pharmaceutical composition and a commercial package comprising said compounds are also described.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: July 3, 2018
    Assignee: The University of British Columbia
    Inventors: Artem Tcherkassov, Paul Rennie, Fuqiang Ban, Huifang Li, Eric Joseph Jean LeBlanc, Kush Dalal, Anton V. Tverdokhlebov, Sergiy Babiy, Evgeniia Bogomol, Kateryna Dunayenko
  • Glutaminase inhibitors and method of use
    Patent number: 10011574
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: July 3, 2018
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Shunqi Yan
  • Method for fabricating titanium-containing silicon oxide material and application of the same
    Patent number: 10011575
    Abstract: A method for fabricating a titanium-containing silicon oxide material and an application of the same are disclosed. The method needn't use a template but directly use an amorphous silicon dioxide and a titanium source as the reactants. The reactants are mixed with a solvent and react in the solvent. The suspension generated by the reaction is processed by solid-liquid separation, flushing and drying to obtain a titanium-containing silicon oxide material. The method features a simplified fabrication process and a low fabrication cost. The titanium-containing silicon oxide material fabricated by the method has a superior catalytic activity, able to catalyze an epoxidation reaction of an olefin-group compound to generate an epoxide.
    Type: Grant
    Filed: July 25, 2016
    Date of Patent: July 3, 2018
    Assignee: Oriental Union Chemical Corp.
    Inventors: Yu-Chuan Hsu, Chia-Yao Tseng, Po-Sung Wu, Hsi-Chin Tsai
  • Actinic ray-sensitive or radiation-sensitive resin composition, actinic ray-sensitive or radiation-sensitive film, mask blank provided with actinic ray-sensitive or radiation-sensitive film, pattern forming method, method for manufacturing electronic device, electronic device, and compound
    Patent number: 10011576
    Abstract: The actinic ray-sensitive or radiation-sensitive resin composition includes a crosslinking agent having a polarity converting group and an alkali-soluble resin, in which the polarity converting group is a group capable of decomposing by the action of an alkaline aqueous solution to generate a carboxylic acid or sulfonic acid on the side having a crosslinking group.
    Type: Grant
    Filed: June 8, 2016
    Date of Patent: July 3, 2018
    Assignee: FUJIFILM Corporation
    Inventors: Shuhei Yamaguchi, Koutarou Takahashi, Tomotaka Tsuchimura, Natsumi Yokokawa, Hidehiro Mochizuki
  • Methods for producing 5-(halomethyl)furfural
    Patent number: 10011577
    Abstract: The present disclosure provides methods to produce 5-(halomethyl)furfural, including 5-(chloromethyl)furfural, by acid-catalyzed conversion of C6 saccharides, including isomers thereof, polymers thereof, and certain derivatives thereof. The methods make use of acids with lower concentrations, and allows for conversion of sugars into 5-(halomethyl)furfural at higher temperatures and faster reaction or residence times.
    Type: Grant
    Filed: September 19, 2014
    Date of Patent: July 3, 2018
    Assignee: MICROMIDAS, INC.
    Inventors: Alex B. Wood, Makoto N. Masuno, Ryan L. Smith, John Bissell, Dimitri A. Hirsch-Weil, Robert Joseph Araiza, Daniel R. Henton, James H. Plonka
  • Compounds for stabilizing ryanodine receptors from aberrant levels of calcium release
    Patent number: 10011578
    Abstract: Disclosed herein are methods and compositions comprising compounds capable of normalizing neuronal calcium dyshomeostasis. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, Pick's disease, chronic traumatic encepholopathy, traumatic brain injury, stroke, cerebellar ataxia, multiple sclerosis, Down syndrome, and aging-related CNS disorders.
    Type: Grant
    Filed: August 8, 2017
    Date of Patent: July 3, 2018
    Assignee: Rosalind Franklin University of Medicine and Science
    Inventors: Grace E. Stutzmann, Russell Dahl, Christopher H. Kaiho
  • Oxidation process to produce a purified carboxylic acid product via solvent displacement and post oxidation
    Patent number: 10011579
    Abstract: Disclosed is a process to produce a dry purified carboxylic acid product comprising furan-2,5-dicarboxylic acid (FDCA). The process comprises oxidizing at least one oxidizable compound selected from the following group: 5-(hydroxymethyl)furfural (5-HMF), 5-HMF esters (5-R(CO)OCH2-furfural where R is alkyl, cycloalkyl, or aryl), 5-HMF ethers (5-R?OCH2-furfural where R? is alkyl, cycloalkyl, or aryl), 5-alkyl furfurals (5-R?-furfural where R? is alkyl, cycloalkyl, or aryl), mixed feedstocks of 5-HMF and 5-HMF esters, mixed feedstocks of 5-HMF and 5-HMF ethers, and mixed feedstocks of 5-HMF and 5-alkyl furfurals to generate a crude carboxylic acid slurry comprising FDCA.
    Type: Grant
    Filed: May 22, 2017
    Date of Patent: July 3, 2018
    Assignee: Eastman Chemical Company
    Inventors: Mesfin Ejerssa Janka, Kenny Randolph Parker, Paula Moody, Ashfaq Shahanawaz Shaikh, Lee Reynolds Partin, Bradford Russell Bowers, Michael Charles Morrow
  • Diastereoselective synthesis of (±)-epianastrephin, (±)-anastrephin and analogs thereof
    Patent number: 10011580
    Abstract: A process for the synthesis of trans-fused ?-lactones having Formula (IV) from substituted cyclic ketones having Formula (I).
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: July 3, 2018
    Assignee: The United States of America, as Represented by the Secretary of Agriculture
    Inventors: Spencer S. Walse, Daniel Kuzmich
  • Process for preparing 4-amino-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-pentanoic acid compound
    Patent number: 10011581
    Abstract: The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a tautomer or salt thereof, where R1-R5, a, b, X and P2, are as defined in the specification.
    Type: Grant
    Filed: May 12, 2017
    Date of Patent: July 3, 2018
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventor: Miroslav Rapta
  • Substituted delta-lactones and methods of preparing same
    Patent number: 10011582
    Abstract: The invention relates to substituted delta-lactones as well as to processes for synthesizing them, e.g., using fatty acids as starting material.
    Type: Grant
    Filed: February 18, 2015
    Date of Patent: July 3, 2018
    Assignee: P2 SCIENCE, INC.
    Inventors: Patrick Foley, Yonghua Yang
  • Inhibitors of lysine specific demethylase-1
    Patent number: 10011583
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds as exemplified as follows, The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: July 3, 2018
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal
  • Polymorphic form of [5-fluoro-3-({2-[(4-fluorobenzene) sulfonyl]pyridin-3-yl}methyl)-2-methylindol-1-yl]-acetic acid
    Patent number: 10011584
    Abstract: The invention relates to a polymorphic form of [5-fluoro-3-({2-[(4-fluorobenzene)sulfonyl]pyridin-3-yl}methyl)-2-methylindol-1-yl]-acetic acid which is stable at room temperature and is therefore useful for preparing stable pharmaceutical formulations.
    Type: Grant
    Filed: May 1, 2015
    Date of Patent: July 3, 2018
    Assignee: ATOPIX THERAPEUTICS LIMITED
    Inventors: Katja Grosse-Sender, Rolf Hilfiker
  • Factor XIa inhibitors
    Patent number: 10011585
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Grant
    Filed: July 23, 2015
    Date of Patent: July 3, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Weiguo Liu, Scott D Edmondson, Zhuyan Guo, Alan Hruza, Sung-Sau So, Wanying Sun, Amjad Ali, Rongze Kuang, Ying-Duo Gao, Anthony K Ogawa
  • Heterocyclic compound, method for preparing the same, and pharmaceutical composition comprising the same
    Patent number: 10011586
    Abstract: The present invention relates to a heterocyclic compound having a novel structure that can be used in the prevention or treatment of diseases caused by abnormality in a PRS (prolyl-tRNA synthetase) activity, a method for preparing the same, and a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: July 3, 2018
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Joon Seok Park, Youn Jung Yoon, Min Jae Cho, Ho Bin Lee, Ja Kyung Yoo, Bong Yong Lee
  • Multivalent ligands targeting VEGFR
    Patent number: 10011587
    Abstract: Compounds that target vascular endothelial growth factor receptors for therapy and imaging are disclosed. Methods for making the compounds and detecting or imaging cells expressing VEGFR using the compounds are also provided. In accordance with the purposes of the disclosed subject matter, as embodied and broadly described herein, disclosed are compounds, and methods of making and using the compounds. The disclosed compounds, in one aspect, are quinazoline compounds.
    Type: Grant
    Filed: May 14, 2015
    Date of Patent: July 3, 2018
    Assignee: The Methodist Hospital System
    Inventors: Zheng Li, Feng Li
  • 1,2-substituted cyclopentanes as orexin receptor antagonists
    Patent number: 10011588
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, (I) wherein L, X, Ra, Rb, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: February 19, 2015
    Date of Patent: July 3, 2018
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Charlotte Fieldhouse, Angela Glen, Stephanie Maine, Tatsuhiko Fujimoto, John Stephen Robinson
  • Treatments for gastrointestinal conditions
    Patent number: 10011589
    Abstract: Compounds for the treatment of bacterial and parasitic infections which are hybrid compounds of compounds having antibacterial or antiparasitic activity and compounds that decrease the absorption of the hybrid compound from the gastrointestinal tract. The compounds are preferably for use against C. difficile infections and comprise a hybrid molecule of an anti-C. difficile compound such as a nitroimidazole and a tetramic acid derivative.
    Type: Grant
    Filed: March 12, 2015
    Date of Patent: July 3, 2018
    Assignees: Board of Regents, The University of Texas System, St. Jude Children's Research Hospital, Inc.
    Inventors: Richard E. Lee, Philip T. Cherian, Julian G. Hurdle, Xiaoqian Wu
  • Crystalline forms of vilazodone hydrochloride and vilazodone free base
    Patent number: 10011590
    Abstract: The present application relates to crystalline and amorphous Vilazodone hydrochloride. The present application further relates to amorphous solid dispersions of vilazodone hydrochloride with pharmaceutically acceptable carriers. The present application also relates to a process for the preparation of form I of vilazodone free base.
    Type: Grant
    Filed: April 13, 2017
    Date of Patent: July 3, 2018
    Assignee: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Javed Iqbal, Srinivas Oruganti, Rajesh Kumar Rapolu, Vishweshwar Peddy, Rajesham Boge, Deepika Pathivada, Dharma Jagannadha Rao Velaga, Sesha Reddy Yarraguntla, Sudhakar Reddy Baddam, Anitha Naredla, Kiran Kumar Doniparthi, Srividya Ramakrishnan
  • Crystalline form of afatinib dimaleate
    Patent number: 10011591
    Abstract: The present invention provides a crystalline Form I of afatinib dimaleate, its process for preparation and pharmaceutical composition thereof, and its use in the treatment of metastatic non-small cell lung cancer.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: July 3, 2018
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Shravan Kumar Singh, Shyam Sunder Verma, Kaptan Singh, Mohan Prasad
  • Polycyclic inhibitor of anaplastic lymphoma kinase
    Patent number: 10011592
    Abstract: Disclosed is a polycyclic inhibitor of anaplastic lymphoma kinase as represented by Formula (I), or a pharmaceutically acceptable salt or stereoisomer thereof. Also disclosed is a method for preparing the compound, a pharmaceutical preparation and a pharmaceutical composition comprising the compound, and use of the compound, the pharmaceutically acceptable salt or stereoisomer thereof in manufacture of a medicament for the treatment and/or prevention of, for example, an anaplastic lymphoma kinase-mediated cancer or non-cancer related diseases.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: July 3, 2018
    Assignee: XUANZHU PHARMA CO., LTD.
    Inventor: Frank Wu
  • Heterocycle-substituted pyridyl benzothiophenes as kinase inhibitors
    Patent number: 10011593
    Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and X are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: July 3, 2018
    Assignee: ALLERGAN, INC.
    Inventors: Sougato Boral, Thomas C. Malone, Shimiao Wang, Sandhya Rao, Rong Yang
  • 4-hydroxy-3-(heteroaryl)pyridine-2-one APJ agonists
    Patent number: 10011594
    Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
    Type: Grant
    Filed: June 2, 2016
    Date of Patent: July 3, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, Soong-Hoon Kim, R. Michael Lawrence, Michael C. Myers, Hannguang J. Chao, Monique Phillips, Ji Jiang
  • Ethyldiamine orexin receptor antagonists
    Patent number: 10011595
    Abstract: The present invention is directed to ethyldiamne compounds which are antagonists of orexin receptors. Such compounds are of the general structural formula I: The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: July 3, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Scott D. Kuduk, Nigel Liverton, Gang Zhou
  • 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors
    Patent number: 10011596
    Abstract: The present invention provides compounds of Formula I for the treatment of neurodegenerative or cognitive diseases. The method further provides for piperidine-2-one and piperidine-2-thione intermediates to compounds of formula I.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: July 3, 2018
    Assignee: H. Lundbeck A/S
    Inventors: Karsten Juhl, Lena Tagmose, Mauro Marigo
  • Derivatives of 2-(1,2,4-triazol-3-ylsulfanyl)-N-1,3,4-thiadiazol-2-yl acetamide which are useful for the treatment of inter alia diabetes
    Patent number: 10011597
    Abstract: Disclosed are compounds, pharmaceutical compositions and methods for modulating aquaporin 9.
    Type: Grant
    Filed: October 28, 2015
    Date of Patent: July 3, 2018
    Assignee: APOGLYX AB
    Inventors: Michael Rützler, Thomas Brimert, Klaus Dreisch, Johan Evenäs, Joakim Larsson
  • Small molecules targeting repeat r(CGG) sequences
    Patent number: 10011598
    Abstract: The invention provides a series of bioactive small molecules that target expanded r(CGG) repeats, termed r(CGG)exp, that causes Fragile X-associated Tremor Ataxia Syndrome (FXTAS). The compound was identified by using information on the chemotypes and RNA motifs that interact. Specifically, 9-hydroxy-5,11-dimethyl-2-(2-(piperidin-1-yl)ethyl)-6H-pyrido[4,3-b]carbazol-2-ium, binds the 5?CGG/3?GGC motifs in r(CGG)exp and disrupts a toxic r(CGG)exp-protein complex. Specifically, dimeric compounds incorporating two 9-hydroxyellipticine analog structures can even more potently bind the 5?CGG/3?GGC motifs in r(CGG)exp and disrupts a toxic r(CGG)exp-protein complex. Structure-activity relationships (SAR) studies determined that the alkylated pyridyl and phenolic side chains are important chemotypes that drive molecular recognition of r(CGG) repeats, such as r(CGG)exp.
    Type: Grant
    Filed: January 23, 2017
    Date of Patent: July 3, 2018
    Assignee: The Scripps Research Institute
    Inventors: Matthew D. Disney, Biao Liu, Jessica L. Childs-Disney, Wang-Yong Yang
  • Compounds and compositions as inhibitors of MEK
    Patent number: 10011599
    Abstract: The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
    Type: Grant
    Filed: March 16, 2017
    Date of Patent: July 3, 2018
    Assignee: Novartis AG
    Inventors: Mark Gary Bock, Henrik Moebitz, Sunil Kumar Panigrahi, Ramulu Poddutoori, Susanta Samajdar
  • Methods and compositions for inhibition of Ras
    Patent number: 10011600
    Abstract: Inhibitors of Ras protein, methods to modulate the activity of Ras protein, and methods of treatment of disorders mediated by Ras protein are provided. A method for regulating activity of a K-Ras, H-Ras or N-Ras mutant protein with a compound is described. Disorders that can be treated include cancer, such as hematological cancer, pancreatic cancer, MYH associated polyposis, colorectal cancer, or lung cancer.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: July 3, 2018
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Pingda Ren, Yi Liu
  • Substituted spirocyclic inhibitors of autotaxin
    Patent number: 10011601
    Abstract: The present invention relates to compounds according to Formula 1 and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.
    Type: Grant
    Filed: April 3, 2015
    Date of Patent: July 3, 2018
    Assignee: X-Rx, Inc.
    Inventors: Lee Babiss, Matthew Clark, Anthony D. Keefe, Mark J. Mulvihill, Haihong Ni, Louis Renzetti, Frank Ruebsam, Ce Wang, Zhifeng Xie, Ying Zhang
  • Immunological reagents and uses therefor
    Patent number: 10011602
    Abstract: The present invention provides a ligand which binds to MR1 wherein said binding results in binding of the MR1 to MAIT cells.
    Type: Grant
    Filed: July 5, 2013
    Date of Patent: July 3, 2018
    Assignee: THE UNIVERSITY OF MELBOURNE
    Inventors: Lars Kjer-Nielsen, James McCluskey, Alexandra Corbett, Jamie Rossjohn, Patel Onisha, David Paul Fairlie, Ligong Liu
  • Process for preparing a carbapenem antibiotic
    Patent number: 10011603
    Abstract: A process for the preparation of a carbapenem, includes the step of treating a solution of a protected carbapenem with hydrogen gas in the presence of a heterogeneous catalyst to form the carbapenem, wherein the heterogeneous catalyst includes at least two platinum group metals.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: July 3, 2018
    Assignee: Johnson Matthey Public Limited Company
    Inventors: James Cookson, Robert John McNair, Deepak Vasant Satoskar
  • Method of treatment using substituted imidazo[1,2b]pyridazine compounds
    Patent number: 10011604
    Abstract: Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.
    Type: Grant
    Filed: December 30, 2015
    Date of Patent: July 3, 2018
    Assignee: Array BioPharma, Inc.
    Inventors: Steven W. Andrews, Julia Haas, Yutong Jiang, Gan Zhang