Patents Issued in February 21, 2017
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Patent number: 9573897Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.Type: GrantFiled: September 4, 2015Date of Patent: February 21, 2017Assignee: CHEMOCENTRYX, INC.Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
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Patent number: 9573898Abstract: Compounds of the formula (1) and their use as umami tastants: wherein R1 is chosen from Me, Et, Pr, or iPr, R2 is chosen from H or Me, or R1 and R2 together with the aromatic ring carbon atoms, form a 5 or 6 membered ring.Type: GrantFiled: September 20, 2012Date of Patent: February 21, 2017Assignee: Givaudan S.A.Inventors: Jacob Antonius Elings, Cornelis Winkel, Stefan Michael Furrer
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Patent number: 9573899Abstract: 2-Aminopyridine compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for modulating USP7, and for treating cancer and immune disorders such as inflammation mediated by USP7. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: March 18, 2016Date of Patent: February 21, 2017Assignee: Genentech, Inc.Inventors: Robert Blake, Paola Di Lello, Jason Drummond, Christine Johanna Heideker, Lorna Kategaya, Till Maurer, Jeremy M. Murray, Chudi Ndubaku, Richard Pastor, Lionel Rouge, Vickie Tsui, Ingrid E. Wertz, Kebing Yu
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Patent number: 9573900Abstract: The invention relates to polymorphs of deuterated omega-diphenylurea or salts thereof. In particular, the invention provides polymorphs of 4-(4-{3-[4-chloro-3-(trifluoromethyl)phenyl)-ureido]-phenoxy}-2-(N-1?,1?,1?-trideutero-methyl)picolinamide or its salt, namely, polymorphs of the compound as shown in formula (I) or its salt. The polymorphs are suited for preparing the pharmaceutical composition used for inhibiting phosphokinase (such as raf kinases).Type: GrantFiled: July 16, 2013Date of Patent: February 21, 2017Assignee: Suzhou Zelgen Biopharmaceutical Co., Ltd.Inventor: Weidong Feng
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Patent number: 9573901Abstract: The present invention belongs to the field of pharmaceutical chemistry, and disclosed are two crystal forms of Childamide, that is, Chidamide crystal form A and Chidamide crystal form B, and the method for preparing the new crystal forms of Chidamide. The Chidamide crystal form A and Chidamide crystal form B of the present invention can be used for preparing drugs for treating diseases related to cell differentiation and proliferation.Type: GrantFiled: December 18, 2012Date of Patent: February 21, 2017Assignee: SHENZHEN CHIPSCREEN BIOSCIENCES, LTD.Inventors: Xianping Lu, Zhibin Li
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Patent number: 9573902Abstract: The present invention provides novel intermediates of ivacaftor and process for its preparation. The present invention also provides process for the preparation of ivacaftor and pharmaceutically acceptable salt thereof using novel intermediates.Type: GrantFiled: February 14, 2014Date of Patent: February 21, 2017Assignee: LAURUS LABS PRIVATE LTD.Inventors: Suresh Thatipally, Venkata Lakshmi Narasimha Rao Dammalapati, Seeta Ramanjaneyulu Gorantla, Satyanarayana Chava
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Patent number: 9573903Abstract: The present invention provides a heterocyclic compound having a ROR?t inhibitory action. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification. or a salt thereof.Type: GrantFiled: February 26, 2016Date of Patent: February 21, 2017Assignee: Takeda Pharmaceutical Company LimitedInventors: Satoshi Yamamoto, Junya Shirai, Tsuneo Oda, Mitsunori Kono, Atsuko Ochida, Takashi Imada, Hidekazu Tokuhara, Yoshihide Tomata, Naoki Ishii, Michiko Tawada, Yoshiyuki Fukase, Tomoya Yukawa, Shoji Fukumoto
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Patent number: 9573904Abstract: An aromatic compound represented by formula (1): wherein R1 and R2 each independently represents a halogen atom, a C1-C4 alkyl group, or a C1-C4 haloalkyl group; m and n each independently represents an integer of 0 to 4; R3 and R4 each represents a hydrogen atom; Y represents formula: —OC(?X)ZR5 or —SC(?X)ZR5; R5 represents a C1-C3 alkyl group optionally having one or more halogen atoms; Z represents a sulfur atom, NR8, or a direct bond; R8 represents a C1-C3 alkyl group or a hydrogen atom; Q represents a pyrazolyl group optionally having a substituent; and W and X each independently represents an oxygen atom or a sulfur atom, has excellent control activity against pests.Type: GrantFiled: December 10, 2014Date of Patent: February 21, 2017Assignee: Sumitomo Chemical Company, LimitedInventor: Takayuki Shioda
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Patent number: 9573905Abstract: The biphasic extraction from coffee waste without a prior drying process, to obtain coffee oil, which is transesterified with KOH catalyzed methanol to produce mixtures of glycerol free methylic esters, also known as coffee oil biodiesel, which is subjected to an aminolysis reaction with aminoethylethanolamine (AEEA) by heating to 140-160° C. at atmospheric pressure with a subsequent dehydration reaction at the same temperature but at a reduced pressure of 200 to 300 mmHg, in order to achieve cyclization of the intermediary amides into the corresponding imidazolines. Alternatively process, coffee oil can be submitted to the same aminolysis procedure with aminoethylethanolamine (AEEA) at 140 to 160° C. and atmospheric pressure with a subsequent dehydration reaction at the same temperature but at a reduced pressure of 200 to 300 mmHg, to produce imidazolines that contain the residual glycerol of the original triglycerides.Type: GrantFiled: March 20, 2014Date of Patent: February 21, 2017Assignees: CORROSION Y PROTECCION SE DE CV, UNIVERSIDAD NACIONAL AUTONOMA DE MEXICOInventors: Jose Ignacio Regla Contreras, Maria Patricia Shirley Demare Negrete, Jorge Antonio Ascencio Gutierrez, Lorenzo Martinez Gomez, Lorenzo Martinez Martinez De La Escalera, Jorge Joaquin Canto Ibanez, Irene Carrillo Salgado
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Patent number: 9573906Abstract: The invention provides compounds of formulae (I), (II), (III), and (IV): and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers and Alzheimer's disease.Type: GrantFiled: September 13, 2012Date of Patent: February 21, 2017Assignee: Arizona Board of Regents, A Body Corporate of the State of Arizona Acting for and on behalf of Arizona State UniversityInventors: Carl E. Wagner, Peter W. Jurutka, Pamela A. Marshall
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Patent number: 9573907Abstract: The present invention relates to novel 2,4-pyrimidine derivatives and a use thereof, and more particularly, to pyrimidine derivatives which are effective for systemic lupus erythematosus, a composition for preventing and treating systemic lupus erythematosus comprising the same as an active ingredient and a method for screening the same. The present inventors found novel materials inhibiting surface translocation of gp96 by mimicking a function of AIMP1 which is a molecular anchor for an intracellular residence of gp96, and identified in vitro and in vivo activity of the materials for preventing and treating SLE by alleviating SLE plasma in autoimmune diseases. Therefore, the present invention provides a novel method for screening a therapeutic agent for SLE, and preventing or treating SLE using the mechanism.Type: GrantFiled: November 2, 2010Date of Patent: February 21, 2017Assignees: SNU R&DB FOUNDATION, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Sunghoon Kim, Jung Min Han, Hyeong Rae Kim, Dong Ju Jeon, Jong Hwan Song, Kyung Eun Park
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Patent number: 9573908Abstract: Using a whole-cell high-throughput screen, eleven molecules were identified that activate V. cholerae quorum sensing (QS). Eight molecules are receptor agonists and three molecules are antagonists of LuxO, the central NtrC-type response regulator that controls the global V. cholerae QS cascade. Pro-QS molecules are used for the development of novel anti-infectives.Type: GrantFiled: February 20, 2013Date of Patent: February 21, 2017Assignee: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Bonnie L. Bassler, Wai-Leung Ng, Lark J. Perez, Jianping Cong, Martin F. Semmelhack
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Patent number: 9573909Abstract: Disclosed are triazine derivative compounds exhibiting sufficient herbicidal activity at low application dosage when they are applied to soils and foliage, and an agrochemical composition using the same, in particular herbicides.Type: GrantFiled: January 22, 2015Date of Patent: February 21, 2017Assignee: FMC CorporationInventors: Atsushi Shibayama, Ryu Kajiki, Masami Kobayashi, Takashi Mitsunari, Atsushi Nagamatsu
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Patent number: 9573910Abstract: The invention relates to novel oxazolidinone compound. More particularly, the invention relates to novel [(S)—N-[[3-[4-fluoro-3-morpholino phenyl]-2-oxooxazolidin-5-yl] methyl] acetamide] compound of Formula-I which was disclosed in Indian Patent Application No. 5063/CHE/2013 and corresponding PCT/IN2014/000018. The compound is a broad spectrum antimicrobial agent effective against Multi-Drug Resistant S. Maltophilia pathogen and a large number of gram positive and gram negative pathogens. The compound has shown excellent biological activities against S. Maltophilia which has developed resistance against a large number of antibiotics including some of the known and widely used oxazolidinone derivatives.Type: GrantFiled: July 28, 2014Date of Patent: February 21, 2017Assignee: Lee Pharma LimitedInventors: Raghu Mitra Alla, Ajay Kumar Dubey, Srinivas Reddy Mallepalli, Ramakrishna Reddy Pongilati
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Patent number: 9573911Abstract: The present invention provides compounds of Formulae (I)-(V), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. In one aspect, compounds of the present invention are useful as glycosyltransferase inhibitors, in particular, O-linked N-acetylglucosamine (O-GlcNAc) transferase (OGT) inhibitors. In another aspect, compounds of the present invention are useful as kinase inhibitors, in particular, PLK1 inhibitors, GSK3P inhibitors, or MAPKAPK2 inhibitors. The present invention further provides methods of using the inventive compounds, e.g., as biological probes to study the inhibition of OGT and/or kinase activity and as therapeutics, e.g., for the treatment of OGT-associated and/or kinase-associated conditions.Type: GrantFiled: July 6, 2012Date of Patent: February 21, 2017Assignee: President and Fellows of Harvard CollegeInventors: Suzanne Walker Kahne, Jiaoyang Jiang, Michael Block Lazarus
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Patent number: 9573912Abstract: The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10.Type: GrantFiled: September 22, 2015Date of Patent: February 21, 2017Inventors: Iain W. Duncan, Edward A. Kesicki, Carl G. Osborne, William D. Schwieterman, Irina Jacobson
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Patent number: 9573913Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: October 3, 2014Date of Patent: February 21, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Shawn Stachel, Daniel V. Paone, Jing Li, Anthony Ginnetti, John Lim, Jianmin Fu, Shimin Xu
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Patent number: 9573914Abstract: The invention provides a process for preparing a 2,3,4,5-tetrahydro[1,4]benzothiazepine of formula: by reacting a [2-(acylaminoethyl)thio]arene of formula with an aldehyde or a multimer thereof, and with an acid. The invention also provides for first reacting the [2-(acylaminoethyl)thio]arene with the aldehyde or multimer thereof and a base to form an [N-hydroxymethyl-2-[acylaminoethyl)thio]arene of formula then treating the [N-hydroxymethyl-2-(acylaminoethyl)thio]arene with the acid to form the 2,3,4,5-tetrahydro[1,4]benzothiazepine.Type: GrantFiled: December 23, 2013Date of Patent: February 21, 2017Assignees: LES LABORATOIRES SERVIER, ARMGO Pharma, Inc.Inventors: Shixian Deng, Sandro Belvedere, Jiaming Yan, Donald Landry
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Patent number: 9573915Abstract: There are provided an ionic liquid having ether group(s) in which a copper(I) compound is included, a method for preparing the same, and a method for removing traces amounts of acetylene-based hydrocarbon compounds included in olefin by absorption or extraction using the same. When the disclosed solution is used, oxidation of Cu(I) to Cu(II) is prevented since CuX is stabilized by the ionic liquid. Thus, selective removal efficiency of acetylenic compounds is improved greatly while the removal performance is retained for a long period of time. Further, since the solution according to the present disclosure is applicable as an extractant as well as an absorbent, the associated operation is simple and apparatus cost can be decreased.Type: GrantFiled: June 19, 2014Date of Patent: February 21, 2017Assignee: Kolon Industries, Inc.Inventors: Hyun Joo Lee, Byoung Sung Ahn, Hoon Sik Kim, Jin-Hyung Kim, Gyeong Taek Gong
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Patent number: 9573916Abstract: A method for the production of ethylene oxide wherein the partial pressure of water vapor at the inlet of the reactor is at least about 8 kPa using a high purity carrier comprising alpha-alumina, a promoting amount of at least one Group IA metal, and a promoting amount of rhenium.Type: GrantFiled: March 12, 2014Date of Patent: February 21, 2017Assignee: Dow Technology Investments LLCInventors: Liping Zhang, Mark H. McAdon, Ernest R. Frank
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Patent number: 9573917Abstract: A process for manufacturing epoxy monomers and/or epoxides in high yields and useful quality and chemical stability by dehydrochlorination of the corresponding chlorohydrins with an alkaline agent, producing the corresponding side product dry salt in a high purity, characterized in that the process comprises the following steps: a. Reaction of the chlorohydrins with the alkaline agent to form corresponding epoxides and the corresponding precipitated chloride salt; b. Dehydration, and optionally completing the reaction, of the reaction mixture of step (a), by use of an azeotropic agent, added to step (b) or generated in situ in step (a), resulting in the producing of a dehydrated reaction mixture; c. Separating the resulting chloride salt by filtration from the dehydrated reaction mixture (b) and d. Isolating the epoxide from the filtered liquid fraction.Type: GrantFiled: June 9, 2014Date of Patent: February 21, 2017Assignee: SPOLEK PRO CHEMICKOU A HUTNI VYROBU A.S.Inventors: Pavel Kubicek, Bedrich Nemecek, Petr Sladek
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Patent number: 9573918Abstract: The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.Type: GrantFiled: May 8, 2013Date of Patent: February 21, 2017Assignee: Zafgen, Inc.Inventors: Robert Zahler, James E. Vath
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Patent number: 9573919Abstract: The present invention provides a peroxisome proliferator-activated receptor (PPAR) activator, which is free from the problem of side effects, can be taken over a long term and has no characteristics taste. Nobiletin is employed as a PPAR activator. Nobiletin has an excellent PPAR activity and has an excellent adiponectin secretion-promoting effect, and is contained in a large amount in citrus fruits, in particular, in Shiikuwasha (Citrus depressa HAYATA) indigenous to Okinawa (Japan). Since citrus fruits have been consumed for many years, the safety of nobiletin has been proven and besides, nobiletin has a low calorie content. Therefore, it can be taken over a long term. Moreover, because of being tasteless and odorless, nobiletin would not damage the unique taste of a food when added thereto. Therefore, it can be added to foods and taken.Type: GrantFiled: May 7, 2007Date of Patent: February 21, 2017Assignee: ARKRAY, Inc.Inventor: Takao Sasaki
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Patent number: 9573920Abstract: A compound is represented by Formula (I) or (II) described below. A medicine includes, as an active ingredient, a compound represented by Formula (I), (II), or (III) described below.Type: GrantFiled: March 5, 2014Date of Patent: February 21, 2017Assignees: AMINO UP CHEMICAL CO., LTD, THE RITSUMEIKAN TRUSTInventors: Yukinobu Ikeya, Mikio Nishizawa, Takehito Miura
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Patent number: 9573921Abstract: The present invention relates to compounds of formula (I), and salts thereof and the pharmaceutical composition containing them in treatment of various diseases, as allergic rhinitis where R1 and R2 are, independently, hydrogen, halogen, C1_3 alkyl or C1-3alkoxy; R3 is phenyl optionally substituted by R4 and R5 which are, independently hydrogen, halogen, C1-3 alkyl, C1-3-alkoxy, fluoro-, difluoro- and trifluoromethyl, nitrile group, N,N-diC1-3alkyl-amide, carboC1-3 alkoxy or C1-3alkylsulphone groups; R3 is pyridyl group containing nitrogen at various positions in the benzene ring, n is one of the integers 1 or 2.Type: GrantFiled: September 30, 2013Date of Patent: February 21, 2017Assignee: Polfarmex S.A.Inventors: Piotr Kopczacki, Mieczyslaw Wosko, Jaroslaw Walczak, Krzysztof Walczynski
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Patent number: 9573922Abstract: Disclosed is a method of preparing a urolithin, or an intermediate or analog thereof, having a dibenzo[b,d]pyran-6-one core. The method is especially advantageous for the large-scale preparation of urolithins or intermediates or analogs thereof. The method may optionally include the preparation of a urolithin, or an intermediate or analog thereof, as a pharmaceutically acceptable salt.Type: GrantFiled: July 18, 2016Date of Patent: February 21, 2017Assignee: Amazentis SAInventors: Christopher Rinsch, Roland Mueller, Wolfgang Skranc
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Patent number: 9573923Abstract: The present invention relates to a compound having a 2,6-difluorophenylether structure useful as organic electronic materials, pharmaceuticals and agrochemicals, and in particular, liquid crystal display device materials. Provided are a compound represented by general formula (1): and a liquid crystal composition containing the compound and a liquid crystal display device that uses the liquid crystal composition. Since the compound represented by general formula (1) is used as a component of a liquid crystal composition, a liquid crystal composition that exhibits low viscosity and a liquid crystal phase over a wide temperature range can be obtained. Thus, the compound is particularly useful as a component of a liquid crystal composition for high-response-speed liquid crystal display devices.Type: GrantFiled: August 28, 2014Date of Patent: February 21, 2017Assignee: DIC CORPORATIONInventors: Kenta Tojo, Tetsuo Kusumoto
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Patent number: 9573924Abstract: A process for preparing a cyclic ester or a cyclic amide includes contacting hydroxycarboxylic acid and/or amino-carboxylic acid, an ester thereof, or a salt thereof, with acidic zeolite. The hydroxycarboxylic acid is a 2- or 6-hydroxycarboxylic acid, and the amino carboxylic acid is a 2- or 6-amino-carboxylic acid. The zeolite may include two or three interconnected and non-parallel channel systems, in which a channel system includes 10- or more-membered ring channels, and in which a framework Si/X2 ratio is at least 24 as measured by NMR. X is Al or B. The zeolite may include three interconnected and non-parallel channel systems, in which at least two channel systems include 10- or more-membered ring channels, and in which a framework Si/X2 ratio is at least 6 as measured by NMR. The process may be performed at a pressure between 0.5 and 20 bar.Type: GrantFiled: February 7, 2014Date of Patent: February 21, 2017Assignee: TOTAL RESEARCH & TECHNOLOGY FELUYInventors: Bert Sels, Michiel Dusselier
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Patent number: 9573925Abstract: A process for the recovery and production of meso-lactide from a crude lactide containing stream may include subjecting a starting crude lactide stream to a first distillation step to obtain: a top stream mainly containing meso-lactide; a bottom stream; and a side stream mainly containing L-lactide and meso-lactide. The process may include recovering the side stream and subjecting the side stream to a melt crystallization step to obtain: a first purified stream mainly containing L-lactide; and a drain stream mainly containing meso-lactide and L-lactide. The process may include recovering the top stream and drain stream, and subjecting the top stream and drain stream to a second distillation step to obtain a second purified stream containing L-lactide and meso-lactide.Type: GrantFiled: May 6, 2014Date of Patent: February 21, 2017Assignee: FUTERRO S.A.Inventors: Philippe Coszach, Denis Mignon
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Patent number: 9573926Abstract: The invention provides ester compounds for treating ophthalmic diseases. The esters of the invention are particularly advantageous due to their stability in aqueous solutions.Type: GrantFiled: May 22, 2015Date of Patent: February 21, 2017Assignee: ALLERGAN, INC.Inventors: Robert M. Burk, Yariv Donde, Jeremiah H. Nguyen
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Patent number: 9573927Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of severe pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of chronic pain, generalized pain disorders, leukemia, cancer, chronic pain, chemotherapy induced pain, epilepsy, migraine, neuropathic pain, post herpetic neuralgia, neuralgia, pain, drug addiction, detoxification of drugs, Alzheimer's disease, multiple sclerosis, multiple sclerosis, restless legs syndrome (RLS), cluster headache, depression, fibromyalgia, amyotrophic lateral sclerosis (ALS), convulsions, partial seizures, mood-stabilizing agent and bipolar disorder.Type: GrantFiled: February 4, 2013Date of Patent: February 21, 2017Assignee: CELLIX BIO PRIVATE LIMITEDInventor: Mahesh Kandula
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Patent number: 9573928Abstract: The present invention relates to novel amides and a process for preparing these amides.Type: GrantFiled: September 30, 2014Date of Patent: February 21, 2017Assignee: Novartis AGInventors: Olivier Loiseleur, Daniel Kaufmann, Stephan Abel, Hans Michael Bürger, Mark Meisenbach, Beat Schmitz, Gottfried Sedelmeier
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Patent number: 9573929Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.Type: GrantFiled: November 13, 2015Date of Patent: February 21, 2017Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Giles Albert Brown, Julie Elaine Cansfield, Benjamin Gerald Tehan
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Patent number: 9573930Abstract: 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. 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.Type: GrantFiled: January 5, 2016Date of Patent: February 21, 2017Assignee: Celgene Quanticel Research, Inc.Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
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Patent number: 9573931Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by coupling 3-bromopyridine with commercially available 3-aminopyrazole, purifying the 3-(3-amino-1H-pyrazol-1-yl)pyridine by crystallization, and converting the amino group to a chloro group by a Sandmeyer reaction.Type: GrantFiled: May 3, 2016Date of Patent: February 21, 2017Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Carl DeAmicis, Ann Buysse, Ronald Ross, Jr., Xiaoyong Li
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Patent number: 9573932Abstract: The present disclosure provides a method for preparing a compound of formula XVII, comprising: (1) contacting a compound of formula XIV with a compound of formula 3 to obtain a compound of formula 2; and (2) contacting the compound of formula 2 with a compound of formula 4 to obtain a compound of formula XVII. The method is low toxicity, cheap, easy to get, environmentally and friendly, and is economical and industrially applicable.Type: GrantFiled: March 2, 2015Date of Patent: February 21, 2017Inventor: Yong Xu
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Patent number: 9573933Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, R20, X, Y, Q and Z have defined meanings.Type: GrantFiled: September 18, 2008Date of Patent: February 21, 2017Assignee: Janssen Pharmaceutica NVInventors: Virginie Sophie Poncelet, Sophie Coupa, Pierre-Henri Storck, Bruno Schoentjes
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Patent number: 9573934Abstract: The invention features methods and compositions for the synthesis of multimerizing agents.Type: GrantFiled: January 28, 2015Date of Patent: February 21, 2017Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Feng Li, Yihan Wang
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Patent number: 9573935Abstract: 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: GrantFiled: July 23, 2014Date of Patent: February 21, 2017Assignee: ONO PHARMACEUTICAL CO., LTD.Inventors: Takayuki Inukai, Jun Takeuchi, Tomoko Yasuhiro
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Patent number: 9573936Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.Type: GrantFiled: May 18, 2016Date of Patent: February 21, 2017Assignee: AMGEN INC.Inventors: Ning Chen, Xiaoqi Chen, Yinhong Chen, Alan C. Cheng, Richard V. Connors, Jeffrey Deignan, Paul John Dransfield, Xiaohui Du, Zice Fu, Julie Anne Heath, Daniel B. Horne, Jonathan Houze, Matthew R. Kaller, Aarif Yusuf Khakoo, David John Kopecky, Su-Jen Lai, Zhihua Ma, Lawrence R. McGee, Julio C. Medina, Jeffrey T. Mihalic, Nobuko Nishimura, Steven H. Olson, Vatee Pattaropong, Gayathri Swaminath, Xiaodong Wang, Kevin Yang, Wen-Chen Yeh, Mikkel V. Debenedetto, Robert P. Farrell, Simon J. Hedley, Ted C. Judd, Frank Kayser
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Patent number: 9573937Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.Type: GrantFiled: May 22, 2015Date of Patent: February 21, 2017Assignee: Dart NeuroScience (Cayman) Ltd.Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark Wilson, James Zapf
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Patent number: 9573938Abstract: The invention provides compounds of formula (I): and salts and prodrugs thereof wherein R4, X1 and X2 have any of the meanings defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts and methods for their use in therapy. The compounds have useful antiviral properties.Type: GrantFiled: September 11, 2013Date of Patent: February 21, 2017Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. Lavoie, Joseph David Bauman, Ajit Parhi, Hye Yeon Sagong, Disha Patel, Eddy Arnold, Kalyan Das, Suyambu Kesava Vijayan
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Patent number: 9573939Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: GrantFiled: August 16, 2012Date of Patent: February 21, 2017Assignees: Merck Sharp & Dohme Corp., MSD Italia SRLInventors: Casey C. McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Qun Dang
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Patent number: 9573940Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: GrantFiled: March 26, 2015Date of Patent: February 21, 2017Assignee: JANSSEN PHARMACEUTICA NVInventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
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Patent number: 9573941Abstract: The present invention relates to processes for preparing a dihydropyrimidine derivative having Formula (I) or a tautomer thereof having Formula (Ia), as well as a intermediate thereof. The processes of the invention have simple operation, high optical purity of product, high yield and convenient work-up, which is suitable for industrial production.Type: GrantFiled: November 27, 2014Date of Patent: February 21, 2017Assignee: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Qingyun Ren, Xinchang Liu, Zhifu Zou, Guanghua Yan, Mingchao Bi, Siegfried Goldmann, Yingjun Zhang
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Patent number: 9573942Abstract: This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.Type: GrantFiled: December 10, 2014Date of Patent: February 21, 2017Assignee: Janssen Sciences Ireland UCInventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno François Marie Delest
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Patent number: 9573943Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: January 13, 2014Date of Patent: February 21, 2017Assignee: Genentech, Inc.Inventor: Xiaojing Wang
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Patent number: 9573944Abstract: The present invention is related to heteroaryl compounds as MEK inhibitors. The invention includes heteroaryl compounds of formula I, their tautomers and pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present invention also includes process of preparation of the said compounds and intended use in therapy of them.Type: GrantFiled: March 11, 2013Date of Patent: February 21, 2017Assignee: Lupin LimitedInventors: Bhavesh Dave, Rakesh Kumar Banerjee, Samiron Phukan, Abhijit Datta Khoje, Rajkumar Hangarge, Jitendra Sambhaji Jadhav, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 9573945Abstract: The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.Type: GrantFiled: November 5, 2014Date of Patent: February 21, 2017Assignee: Bionomics LimitedInventors: Jonathan Bayldon Baell, Brad Sleebs, Bernard Luke Flynn, Ian Phillip Street, Nurul Quazi, Chinh Thien Bui
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Patent number: 9573946Abstract: Provided are compounds, compositions and methods for inhibiting fascin activity or treating a condition or disorder mediated by fascin activity in a subject in need thereof.Type: GrantFiled: February 19, 2015Date of Patent: February 21, 2017Assignees: Novita Pharmaceuticals, Inc., Cornell UniversityInventors: Xin-Yun Huang, Christy Young Shue