Patents Issued in December 4, 2018
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Patent number: 10144692Abstract: This invention discloses a method of making vitamin K1. The mentioned method of making vitamin K1 comprises performing a first one-pot synthesis with base catalyst, performing a first hydrolysis, performing a substitution, and performing a second one-pot synthesis without metal oxidant. The starting material of this invention is stable 2-methyl-1,4-naphthoquinone. Preferably, this invention provides a method of making vitamin K1 efficiently on simplifying the operation and decreasing the side-product. More preferably, without metal residue, the vitamin K1 of this invention is without metal residue and more safety for clinical application.Type: GrantFiled: October 16, 2014Date of Patent: December 4, 2018Assignee: SUNNY PHARMTECH INC.Inventors: Jien-Heh Tien, Chu-Yi Pang, Nai-Hsuan Hsu
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Patent number: 10144693Abstract: Carboxylic acids are prepared by a one-step gas phase process comprising the step of contacting under halogen-free hydroxycarbonylation conditions an alkene, carbon monoxide, water, and a solid sulfide-containing catalyst.Type: GrantFiled: October 6, 2015Date of Patent: December 4, 2018Assignee: Dow Global Technologies LLCInventors: David G. Barton, Gerolamo Budroni, Steven L. F. Corthals
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Patent number: 10144694Abstract: Disclosed are methods for preparing phenolic branched chain fatty acids or alkyl esters thereof, involving subjecting in a pressurized container (a) at least one phenolic compound, (b) unsaturated fatty acids having 6 to 25 carbon atoms, alkyl esters thereof, or mixtures thereof, and (c) H-ferrierite zeolite catalyst in the presence of distilled water or alcohol and a nitrogen atmosphere at a temperature of about 100° C. to about 400° C. and a pressure of about 10 to about 1000 psi, and isolating saturated phenolic branched chain fatty acids or alkyl esters thereof or mixtures thereof. Also disclosed are methods for killing microorganisms on or in an object, involving contacting said object with an effective microorganisms killing amount of a composition comprising phenolic branched chain fatty acids or alkyl esters thereof, and optionally a carrier; the phenolic branched chain fatty acids or alkyl esters thereof may be produced by the methods described herein.Type: GrantFiled: June 7, 2018Date of Patent: December 4, 2018Assignee: The United States of America, as Represented by the Secretary of AgricultureInventors: Helen N. Lew, Karen Wagner, Xuetong Fan, Alberto Nunez, Robert A. Moreau, Michael J. Haas, Zongcheng Yan
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Patent number: 10144695Abstract: A metal soap, including metal soap particles in which a fatty acid has from 6 to 22 carbons, and an inorganic crystal nucleating agent with an average particle size of 0.01 to 20 ?m absorbed internally into the metal soap particles, wherein the cumulative diameter at 50% of the metal soap particles on a volumetric basis is 1.0 to 30.0 ?m, and the internal absorption rate A, represented by formula (1) below, is 30% or greater. Internal absorption rate A=100?(X/X?)=100??Formula (1) X; amount of inorganic crystal nucleating agent contained within metal soap X?; amount of inorganic crystal nucleating agent contained within pulverized metal soap passed through a 325-mesh filter (wherein X and X? are average values obtained by elemental analysis at three locations in an area of 15 ?m square, using a scanning electron microscope/energy dispersive X-ray spectroscopy (SEM/EDX).Type: GrantFiled: February 9, 2016Date of Patent: December 4, 2018Assignee: NOF CORPORATIONInventor: Takeshi Yoshimura
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Patent number: 10144696Abstract: A transesterification catalyst that is heterogeneous and a method for preparing said transesterification catalyst are provided. The catalyst can be used in a variety of transesterification reactor configurations including CSTR (continuous stirred tank reactors), ebullated (or ebullating) beds or any other fluidized bed reactors, and PFR (plug flow, fixed bed reactors). The catalyst can be used for manufacturing commercial grade biodiesel, biolubricants and glycerin.Type: GrantFiled: April 15, 2016Date of Patent: December 4, 2018Assignee: CRYSTAPHASE PRODUCTS, INC.Inventors: Umakant Pravinchandra Joshi, Peter Gregory Ham
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Patent number: 10144697Abstract: An alkane-containing stream is reacted to produce an alkene, which is carbonylated to produce an alkyl alkanoate, e.g., methyl propanoate, by a gas phase process comprising the step of contacting under carbonylation conditions the alkene, e.g., ethylene, carbon monoxide, an alkanol, e.g., methanol, and a solid sulfide-based metal catalyst.Type: GrantFiled: March 22, 2016Date of Patent: December 4, 2018Assignee: Dow Global Technologies LLCInventors: Gerolamo Budroni, Steven L. F. Corthals
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Patent number: 10144698Abstract: A methanol/MMA azeotrope is broken or avoided by a method comprising the steps of (1) raising the pressure within a first vessel, e.g., a distillation column, that contains a methanol/MMA azeotrope, (2) collecting the azeotrope as a liquid, and then in a second, separate vessel, e.g., another distillation column, (3) raising the pressure sufficiently to allow for the breaking of or avoidance of the azeotrope and the recovery of the methanol.Type: GrantFiled: October 2, 2015Date of Patent: December 4, 2018Assignees: Dow Global Technologies LLC, Rohm and Haas CompanyInventors: John G. Pendergast, William G. Worley, Stacy W. Hoy, IV, Jacob M. Crosthwaite
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Patent number: 10144699Abstract: The present invention is able to provide a bifunctional compound represented by formula (1). (In the formula, R1 represents COOCH3, COOC2H5, COOC3H7, COOC4H9 or CHO; and R2 represents H, CH3 or C2H5.Type: GrantFiled: April 5, 2018Date of Patent: December 4, 2018Assignee: MITSUBISHI GAS CHEMICAL COMPANY, INC.Inventors: Takashi Motoi, Mitsuharu Kitamura, Manabu Hirakawa
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Patent number: 10144700Abstract: The invention generally relates to adenylyl cyclase inhibitor compounds and methods for treating neuropathic or inflammatory pain by using those compounds.Type: GrantFiled: March 14, 2018Date of Patent: December 4, 2018Assignee: PURDUE RESEARCH FOUNDATIONInventors: Mingji Dai, Val J. Watts, Zhishi Ye
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Patent number: 10144701Abstract: The present invention relates to a preparation method of 4-isopropylamino-1-butanol, in which using cheap and readily available tetrahydrofuran and acetic acid solution of hydrogen bromide as starting materials to prepare a novel intermediate of 4-isopropylamino-1-acetoxyl butane and further obtain the target product. The present invention has advantages of convenient process operations, mild reaction conditions, economical and environment-friendly benefits, and suitability for industrial production to obtain the product with high purity and high yield.Type: GrantFiled: March 31, 2016Date of Patent: December 4, 2018Assignee: Seasons Biotechnology (Taizhou) Co., Ltd.Inventors: Fanghui Tang, Chi Ma, Qiang Jia
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Patent number: 10144702Abstract: A method for the manufacture of N,N-dialkyllactamide, whereby at least one of the compounds selected from the series made of alkyl lactate, lactide and polylactic acid is mixed with dialkylamine in order to form a reaction mixture, under conditions whereby aminolysis takes place in the reaction mixture. The method is characterized in that the reaction mixture further includes a Lewis acid. As a result of the method, N,N-dialkyllactamides can be manufactured in high yields and with high optical purity.Type: GrantFiled: October 1, 2015Date of Patent: December 4, 2018Assignee: PURAC BIOCHEM B.V.Inventors: Bastiaan Jeroen Victor Verkuijl, Jurgen Cornelis Henricus Maas
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Patent number: 10144703Abstract: A process for the preparation of 5-(3,4-dimethoxyphenylethyl) methyl-amino-2-(3,4-dimethoxyphenyl)-2-isopropyl valeronitrile, which is known as Verapamil is described. A process for improving the purity of verapamil and therefore of its hydrochloride represented as the compound of formula I, by efficient removal of the impurities formed, affording a product of purity greater than 99% is described.Type: GrantFiled: May 10, 2016Date of Patent: December 4, 2018Assignee: PIRAMAL ENTERPRISES LIMITEDInventors: Dhileep Kumar Krishnamurthy, Milind Gharpure, Narender Rao Somisetti, Murali Rajappa, Rajshekar Aareddy, Damodhar Kasireddy
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Patent number: 10144704Abstract: Novel crystal forms of (R)-(+)-verapamil hydrochloride are disclosed.Type: GrantFiled: March 11, 2018Date of Patent: December 4, 2018Assignee: Center Laboratories, Inc.Inventors: Jui-Pao Hsu, Guang-Tzuu Shane, Yu-Yin Yeh, Meng-Ju Lee
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Patent number: 10144705Abstract: The present invention concerns a method for preparing a creatine fatty ester or derivative thereof comprising at least one step consisting in reacting a diprotected creatinine with a molecule bearing at least one alcohol functional group and of formula R?—OH in which R? represents a hydrocarbon radical containing at least 4 carbon atoms. The present invention also concerns particular creatine fatty esters or derivative thereof and medical uses thereof.Type: GrantFiled: July 17, 2013Date of Patent: December 4, 2018Assignee: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVESInventors: Sophie Dezard, Frederic Taran, Alexandra Trotier-Faurion, Aloise Mabondzo
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Patent number: 10144706Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.Type: GrantFiled: August 29, 2017Date of Patent: December 4, 2018Assignee: Bristol-Myers Squibb CompanyInventors: Kap-Sun Yeung, Katharine A. Grant-Young, Juliang Zhu, Mark G. Saulnier, David B. Frennesson, David R. Langley, Piyasena Hewawasam, Tao Wang, Zhongxing Zhang, Zhaoxing Meng, Li-Qiang Sun, Eric Mull, Paul Michael Scola
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Patent number: 10144707Abstract: Long-term and high-density energy sources are described that utilize radioisotope batteries that provide a tritium (3H)-based direct energy conversion system. The beta radiation source is a nitroxide compound with a synthetic yield near 100%. The nitroxide compound can be molded into flexible films to cover multiple structures, and has a specific activity and gravimetric density (wt % 3H) comparable to that of tritiated hydrides. A carrier system based on such tritiated nitroxides can be scaled up without significant beta self-absorption, permitting the energy source to have higher specific volume power densities than current radioisotope batteries. Such a carrier can be applied directly to a semiconductor array (such as an integrated circuit) in order to provide electrical power or, alternatively, be prepared with a phosphor and applied to a photovoltaic cell.Type: GrantFiled: March 5, 2018Date of Patent: December 4, 2018Assignee: ORGANIC ENERGY DEVICES (OED)Inventors: Johnny Russo, Gerald M. Rosen, David I. Bigio
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Patent number: 10144708Abstract: The present invention provides novel crystal forms of arylalkylamine compounds. Specifically, the novel crystal forms of 4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1-yl)phenylacetic acid have excellent stability and therefore are useful as pharmaceutical ingredients. The present invention also provides industrially advantageous processes for producing the arylalkylamine compounds.Type: GrantFiled: March 30, 2017Date of Patent: December 4, 2018Assignee: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Hiroshi Miyazaki, Takao Komasaka, Joji Tsurumoto, Takeshi Uemura, Yuuji Morita
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Patent number: 10144709Abstract: Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal diseases in a mammal are provided.Type: GrantFiled: June 9, 2017Date of Patent: December 4, 2018Assignee: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Coo-Min Chung, Hyung-Jin Jun, Jin-Sung Kim, Hiu-Ho Kim, Hye-Kyung Min, Yong-Gil Kim, Jong-Gil Choi, Hongwook Kim
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Patent number: 10144710Abstract: The present invention relates to a process for the preparation of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluophenoxy]-N-methylpyridine-2-caroxamide compound of formula-I, its amorphous form and its crystalline polymorph-I which is represented by the following structural formula: (I)Type: GrantFiled: September 29, 2015Date of Patent: December 4, 2018Assignee: MSN LABORATORIES PRIVATE LIMITEDInventors: Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Gutta Madhusudhan
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Patent number: 10144711Abstract: The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.Type: GrantFiled: November 7, 2017Date of Patent: December 4, 2018Assignee: PELOTON THERAPEUTICS, INC.Inventors: Darryl David Dixon, Jonas Grina, John A. Josey, James P. Rizzi, Stephen T. Schlachter, Eli M. Wallace, Bin Wang, Paul Wehn, Rui Xu, Hanbiao Yang
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Patent number: 10144712Abstract: The present invention discloses novel N-Heterocyclic compounds of formula A, [Formula A] And a ligand-enabled palladium-catalyzed process for preparation of novel N-Heterocyclic compounds of Formula A via C—H alkynylation of N-heterocycles with alkynyl halides.Type: GrantFiled: January 15, 2016Date of Patent: December 4, 2018Assignee: Council of Scientific and Industrial ResearchInventors: Balaraman Ekambaram, Vinod Gokulkrishna Landge
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Patent number: 10144713Abstract: Provided are novel bis-cyclic guanidine compounds, and the use thereof for treating bacterial infection.Type: GrantFiled: June 21, 2018Date of Patent: December 4, 2018Assignee: UNIVERSITY OF SOUTH FLORIDAInventors: Jianfeng Cai, Peng Teng, Alekhya Nimmagadda
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Patent number: 10144714Abstract: The present invention relates to methods and intermediates useful for the synthesis of protein deacetylase inhibitors.Type: GrantFiled: June 8, 2016Date of Patent: December 4, 2018Assignee: ACETYLON PHARMACEUTICALS, INC.Inventors: Farzaneh Seyedi, John H. van Duzer
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Patent number: 10144715Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are liver X receptor modulators, and which are useful in the treatment of diseases and disorders associated with the liver X receptor. Also provided are the compounds of Formula (I) and pharmaceutical compositions thereof for treating atherosclerosis, cardiovascular disease, Alzheimer's disease, dermatitis, dyslipidemia, cancer and other diseases or disorders.Type: GrantFiled: August 4, 2015Date of Patent: December 4, 2018Assignee: Vitae Pharmaceuticals, Inc.Inventors: David A. Claremon, Chengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang
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Patent number: 10144716Abstract: This invention relates to a polybenzoxazine precursor and a method of preparing the same, and more particularly, to a polybenzoxazine precursor which includes benzoxazine obtained by reacting a phenol novolak resin with an aldehyde compound and allylamine and diaminodiphenylmethane as an amine compound, and to a method of preparing the same. The polybenzoxazine precursor may serve to prepare a hardened material having excellent thermal and electrical characteristics and dimensional stability. Accordingly, the polybenzoxazine precursor may be available for use in a copper clad laminate, a semiconductor encapsulant, a printed circuit board, an adhesive, a paint, and a mold.Type: GrantFiled: December 7, 2015Date of Patent: December 4, 2018Assignee: KOLON INDUSTRIES, INC.Inventors: Hee Jin Cho, Do Kyung Sung, Ki Hyun Park, Sang Hun Park
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Patent number: 10144717Abstract: Cysteine compounds represented by the following formula wherein each symbol is as defined in the specification, and salts thereof, are superior in stability, have less odor, exhibit an eumelanin production suppressive effect, and are useful as cosmetic agents.Type: GrantFiled: November 6, 2015Date of Patent: December 4, 2018Assignee: AJINOMOTO CO., INC.Inventors: Yusuke Amino, Yoshinobu Takino, Shinji Kuroda, Keiji Iwasaki, Megumi Kaneko, Fumie Okura
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Patent number: 10144718Abstract: The invention relates to a continuous or repetitive batch process for the hydrogenation of levulinic acid (LA) or esters thereof to at least gamma valerolactone (GVL) in a reactor comprising a feed stream and an outlet stream, in the presence of a solid Ru catalyst, said process comprising (a) pretreating said solid Ru catalyst with a reductant; and (b) reacting levulinic acid with hydrogen and the pretreated solid Ru catalyst obtained in step (a) at a temperature and residence time suitable to form at least GVL, characterized in that the pretreatment is in the presence of a first solvent which comprises water. This process is stable and little or no Ru will leak form the support.Type: GrantFiled: February 16, 2016Date of Patent: December 4, 2018Assignee: DSM IP ASSETS B.V.Inventors: Barthel Engendahl, Roel Wim Wiertz, Jan Van Der Spoel
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Patent number: 10144719Abstract: Novel antimicrobial compounds against drug targets such as Eskape pathogens, Leishmania donovani, Mycobacterium tuberculosis, Clostridium difficile, Naegleria fowleri, and cancer are presented herein.Type: GrantFiled: August 11, 2017Date of Patent: December 4, 2018Assignee: University of South FloridaInventors: Danielle H. Demers, Bill J. Baker, Ala Azhari, Renee M. Fleeman, Dennis E. Kyle, Lindsey Neil Shaw
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Patent number: 10144720Abstract: A method of forming a macrocyclic musk compound comprising the steps of:— i) cross-metathesizing a first olefin and a second olefin in the presence of a homogeneous transition metal catalyst comprising an alkylidene ligand, to form a statistical mixture of a hetero-dimer intermediate of said first and second terminal olefin, and homo-dimers ii) separating the hetero-dimer from the statistical mixture of hetero- and homo-dimers iii) and cyclizing the hetero-dimer intermediate to form the macrocyclic musk compound.Type: GrantFiled: March 13, 2015Date of Patent: December 4, 2018Assignee: GIVAUDAN S.A.Inventors: Paul Nicholas Davey, Martin Alan Lovchik, Andreas Goeke, Krisztian Lorincz, Florian Toth, Levente Ondi
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Patent number: 10144721Abstract: There is provided inter alia a compound of formula (I): wherein R1, J, Ar, L, X, R3 and R4 are as defined in the specification, for use in the treatment of inflammatory disorders.Type: GrantFiled: January 6, 2016Date of Patent: December 4, 2018Assignee: Respivert Ltd.Inventors: John King-Underwood, Ito Kazuhiro, Peter Strong, William Garth Rapeport, Catherine Elisabeth Charron, Peter John Murray, Jonathan Gareth Williams, Stuart Thomas Onions
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Patent number: 10144722Abstract: The present invention is to provide highly solid state emissive fluorophores of the formula 1 and 2 useful for the solid state lighting. The formula 1 and 2 have good solid state emission in blue and green region respectively. The zinc complexes of formula 1A and 2A have yellow and red emission respectively in solid state. The present invention also provide high solid state emissive assay of formula 1 and 2 to convert UV light into visible light by coating the color tunable materials on the 365-nm emitting solid state LED. The present invention further provides carbazole end-capped bipyridine for screening of metal salts with different counterions in solutions. The discrimination of the various metal salts can be monitored by noting the fluorescence change in solution. The zinc salts with different counterions have different emission color in solution. The present invention also develop a new two photon active fluorescent Zn2+ specific probe for detecting Zn2+ in cellular environments.Type: GrantFiled: October 4, 2016Date of Patent: December 4, 2018Assignee: Council of Scientific & Industrial ResearchInventors: Ajayaghosh Ayyappanpillai, Divya Kizhumuri, Srinivasan Sampath
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Patent number: 10144723Abstract: Methods and compounds are described for treating solid tumors, and in particular, malignant, neoplastic solid tumors such as glioblastoma and medulloblastoma, by inhibiting protein kinase MRK/ZAK activity. Also provided are pharmaceutical composition containing a MRK/ZAK inhibitor compound and a pharmaceutically acceptable carrier and a method of sensitizing tumor cells to radiation therapy comprising administering an effective amount of the MRK/ZAK inhibitor compound.Type: GrantFiled: April 21, 2015Date of Patent: December 4, 2018Assignee: The Feinstein Institute for Medical ResearchInventors: Rosamaria Ruggieri, Yousef Al-Abed, Marc Symons
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Patent number: 10144724Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R, R1, R2a, R2b, R2c, A, B, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.Type: GrantFiled: July 22, 2016Date of Patent: December 4, 2018Assignee: Araxes Pharma LLCInventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
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Patent number: 10144725Abstract: The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such as an amino-amine or an amino-amide moiety. The lipid compounds are useful for in vivo or in vitro delivery of one or more agents (e.g., a polyanionic payload or an antisense payload, such as an RNAi agent).Type: GrantFiled: January 17, 2017Date of Patent: December 4, 2018Assignee: DICERNA PHARMACEUTICALS, INC.Inventor: Bob Dale Brown
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Patent number: 10144726Abstract: The invention provides compounds for use in the treatment of a disease or condition selected from brain disorders and triple-negative breast cancer, the compounds being of the formula (1): or a salt or tautomer thereof; wherein: X1 is N or N+(O?); X2 is N or CH; Q is selected from a C1-3 alkylene group, cyclopropane-1,1-diyl and cyclobutane-1,1-diyl; R1 is selected from hydrogen and C1-4 alkyl; R2, R3 and R4 are the same or different and each is selected from hydrogen and fluorine; Ar1 is a benzene, thiophene, naphthyl or pyridine ring optionally substituted with 1, 2 or 3 substituents selected from fluorine; chlorine; bromine; C1-4 hydrocarbyl; C1-4 hydrocarbyloxy; trifluoromethyl; difluoromethyl; cyano; trifluoromethoxy; difluoromethoxy; Ar2 is a monocyclic 5- or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S and being optionally substituted with 1, 2 or 3 substituents selected from fluorine; C1-4 hydrocarbyl; amino; mono-C1-4 hydrocarbylamino and diType: GrantFiled: February 15, 2016Date of Patent: December 4, 2018Assignee: SENTINEL ONCOLOGY LIMITEDInventors: Robert George Boyle, David Winter Walker
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Patent number: 10144727Abstract: The present application provide novel iminosugars and their use in treatment of viral infections, such as Dengue infection and Influenza A infection. The present inventors discovered certain deoxynojirimycin derivatives may be effective against one or more viruses, which may be, for example, a Dengue virus and/or a virus belonging to the Orthomyxoviridae family, such as an Influenza A virus. In particular, such deoxynojirimycin derivatives may be useful for treating a disease or condition caused by or associated with one or more viruses. In certain embodiments, the deoxynojirimycin derivatives may increase a survival rate or probability for a subject infected with one or more viruses, which may be, for example, a Dengue virus and/or a virus belonging to the Orthomyxoviridae family, such as an Influenza A virus.Type: GrantFiled: September 15, 2014Date of Patent: December 4, 2018Assignee: Emergent Virology LLCInventors: Urban Ramstedt, Raju Penmasta, Hitesh Batra, Tam Nguyen
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Patent number: 10144728Abstract: A process for the alkylation of picolinamides with substituted chloroacylals to produce a structure of Formula (III), wherein the reaction is performed in the presence of a phase-transfer catalyst and an inorganic halide co-catalyst.Type: GrantFiled: October 3, 2016Date of Patent: December 4, 2018Assignee: Dow AgroSciences LLCInventors: Matthew J. Jansma, Timothy J. Adaway, Michael Lee Trippeer
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Patent number: 10144729Abstract: The present invention provides compounds of Formula I: pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated as FXR modulators. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR, and methods for their preparation and use.Type: GrantFiled: May 17, 2017Date of Patent: December 4, 2018Assignee: ENANTA PHARMACEUTICALS, INC.Inventors: Yat Sun Or, Jun Ma, Bin Wang, Yong He, Xuechao Xing, Ruichao Shen, Brett Granger, Jing He, Jiang Long, Guoqiang Wang
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Patent number: 10144730Abstract: The present invention provides novel compounds according to Formula (I): where Ring A, Ring B, X, L1, L2, RA, RC, RD, RE, m, n, and p are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of human diseases associated with kinase activity, for example, proliferative diseases, neurodegenerative diseases, metabolic disorders, inflammatory diseases, and cardiovascular diseases.Type: GrantFiled: June 21, 2016Date of Patent: December 4, 2018Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Tinghu Zhang
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Patent number: 10144731Abstract: The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.Type: GrantFiled: December 17, 2014Date of Patent: December 4, 2018Assignees: GlaxoSmithKline Intellectual Property Development Limited, Astex Therapeutics, LtdInventors: Thomas Glanmor Davies, Alison Jo-anne Woolford, Hendrika Maria Gerarda Willems, David Norton, Thomas Daniel Heightman, Jeffrey K. Kerns
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Patent number: 10144732Abstract: Compounds of formula (I) can modulate the activity of autotaxin (ATX).Type: GrantFiled: June 5, 2015Date of Patent: December 4, 2018Assignee: BIOGEN MA INC.Inventors: Gnanasambandam Kumaravel, Hairuo Peng, Zhili Xin
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Patent number: 10144733Abstract: A compound of formula (I) or a salt thereof: wherein R1 represents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono- or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when R1 represents an N-linked mono- or di-substituted pyrazole, R1 does not represent 3,5-Dimethyl-1H-pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1-yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H-pyrazol-1-yl or 1H-pyrazol-1-yl.Type: GrantFiled: September 22, 2015Date of Patent: December 4, 2018Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Niall Andrew Anderson, Ian Baxter Campbell, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, Seble Lemma, Simon John Fawcett MacDonald, John Martin Pritchard, Panayiotis Alexandrou Procopiou
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Patent number: 10144734Abstract: Provided herein are compounds of the Formula I: or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.Type: GrantFiled: December 29, 2017Date of Patent: December 4, 2018Assignee: Array BioPharma Inc.Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, James Collier, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Ginelle A. Ramann, Tony P. Tang, Li Ren, Shane M. Walls
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Patent number: 10144735Abstract: The present invention provides an immune response modifier (IRM) composition that includes an IRM moiety and a second active moiety covalently linked to the IRM moiety, wherein the covalent link comprises a labile bond directly attached to the IRM moiety.Type: GrantFiled: June 25, 2018Date of Patent: December 4, 2018Assignee: 3M Innovative Properties CompanyInventors: Doris Stoermer, George W. Griesgraber, Tushar A. Kshirsagar
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Patent number: 10144736Abstract: The invention provides 4,6-di- and 2,4,6-tri-substituted pteridine derivatives with a specific substitution pattern which exhibit a significant and selective activity against certain types of viral infections, in particular selectively inhibit replication of Flaviridae such as the hepatitis C virus, and are useful for the prevention and treatment of such viral infections.Type: GrantFiled: July 20, 2007Date of Patent: December 4, 2018Assignee: Gilead Sciences, Inc.Inventors: Piet AndréMaurits Maria Herdewijn, Steven Cesar Alfons De Jonghe, William John Watkins, Lee Shun Chong
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Patent number: 10144737Abstract: The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.Type: GrantFiled: October 20, 2014Date of Patent: December 4, 2018Assignee: JIANGSU HENGRUI MEDICINE CO., LTD.Inventors: Minsheng Zhang, Yinfa Yan
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Patent number: 10144738Abstract: A compound having the structure: or a pharmaceutically acceptable salt thereof, wherein A, A? and A? are independently O, C?O, etc.; R0 and R are independently H, Br, Cl, F, or C1-C6 alkyl; R1 is H, C1-C6 alkyl, or hydroxy(C1-C6 alkyl); R2 is selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, etc.; R6, R7 and R8 are each independently H, C1-C6 alkyl, C1-C4 alkoxy(C1-C6 alkyl), etc.; and, n is 0, 1, 2 or 3. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.Type: GrantFiled: February 21, 2017Date of Patent: December 4, 2018Assignee: Pfizer Inc.Inventors: Matthew Frank Brown, Alpay Dermenci, Andrew Fensome, Brian Stephen Gerstenberger, Matthew Merrill Hayward, Dafydd Rhys Owen, Stephen Wayne Wright, Li Huang Xing, Xiaojing Yang
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Patent number: 10144739Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R4, R7, A, D, E, F, V, W, X, Y, n, r and q are defined in claim 1, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.Type: GrantFiled: October 7, 2016Date of Patent: December 4, 2018Assignee: Boehringer Ingelheim International GmbHInventors: Andreas Gollner, Joachim Broeker, Nina Kerres, Christiane Kofink, Juergen Ramharter, Harald Weinstabl
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Patent number: 10144740Abstract: The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxycodone (4,5-?-epoxy-14-hydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxycodone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxycodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.Type: GrantFiled: November 14, 2017Date of Patent: December 4, 2018Assignee: KemPharm, Inc.Inventors: Travis Mickle, Sven Guenther, Sanjib Bera, Bindu Bera, Jaroslaw Kanski, Andrea Martin
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Patent number: 10144741Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.Type: GrantFiled: March 2, 2018Date of Patent: December 4, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Katherine Young, David B. Olsen, Sheo B. Singh, Jing Su, Robert R. Wilkening, James M. Apgar, Dongfang Meng, Dann Parker, Mihir Mandal, Lihu Yang, Ronald E. Painter, Qun Dang, Takao Suzuki