Patents Issued in April 18, 2017
  • Patent number: 9624152
    Abstract: The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.
    Type: Grant
    Filed: March 31, 2015
    Date of Patent: April 18, 2017
    Assignee: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis H. Dasseux, Carmen D. Oniciu
  • Patent number: 9624153
    Abstract: The invention relates to processes for preparing aldehydes by hydroformylation of alkenes, in which an alkene-containing feed mixture is subjected to a primary hydroformylation with synthesis gas in the presence of a homogeneous catalyst system, the primary hydroformylation being effected in a primary reaction zone from which a cycle gas containing at least some of the products and unconverted reactants of the primary hydroformylation are drawn off continuously and partly condensed, with recycling of uncondensed components of the cycle gas into the primary reaction zone, and with distillative separation of condensed components of the cycle gas in an aldehyde removal stage to give an aldehyde-rich mixture and a low-aldehyde mixture. The problem that it addresses is that of developing the process such that it achieves high conversions and affords aldehyde in good product quality even in the case of a deteriorating raw material position.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: April 18, 2017
    Assignee: Evonik Degussa GmbH
    Inventors: Marc Becker, Katrin Marie Dyballa, Robert Franke, Dirk Fridag, Hanna Hahn, Marina Lazar, Markus Priske, Guido Stochniol
  • Patent number: 9624154
    Abstract: The presently disclosed and/or claimed inventive concept(s) relates generally to the reduction of carbon dioxide by heterogeneous catalysis. More particularly, but not by way of limitation, the presently disclosed and/or claimed inventive concept(s) relates to the reduction of carbon dioxide by heterogeneous catalysis with a heterogeneous hydrogenation catalyst comprising structurally frustrated Lewis pairs, wherein, for example but not by way of limitation, formic acid is produced and hydrocarbons are indirectly produced. In one non-limiting embodiment, the heterogeneous catalyst comprises hexagonal boron nitride (h-BN) having structurally frustrated Lewis pairs therein.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: April 18, 2017
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventor: Richard G. Blair
  • Patent number: 9624155
    Abstract: This invention provides a method for producing high-purity iron(III) citrate substantially free of beta-iron hydroxide oxide, high-purity iron(III) citrate substantially free of beta-iron hydroxide oxide, and medical uses thereof.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: April 18, 2017
    Assignee: Japan Tobacco Inc.
    Inventors: Koji Ando, Naoki Manta
  • Patent number: 9624156
    Abstract: This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis.
    Type: Grant
    Filed: October 28, 2015
    Date of Patent: April 18, 2017
    Assignee: United Therapeutics Corporation
    Inventors: Ken Phares, David Mottola, Roger Jeffs
  • Patent number: 9624157
    Abstract: The present invention provides a method for preparing ingenol-3-angelate.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: April 18, 2017
    Assignee: LEO Laboratories Limited
    Inventor: Xifu Liang
  • Patent number: 9624158
    Abstract: New hydroxy aliphatic substituted phenyl aminoalkyi ether compounds of formula (I), compositions thereof and their use as a medicament in the treatment of nervous system diseases and/or the treatment of developmental, behavioral and/or mental disorders associated with cognitive deficits.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: April 18, 2017
    Assignee: Prous Institute for Biomedical Research, S.A.
    Inventors: Josep R. Prous, Neus Serradell, Ramon Flores, Noemi Garcia-Delgado, Marcel-li Carbo Banus
  • Patent number: 9624159
    Abstract: The present invention relates to therapeutic applications of aniline derivatives of formula (I), for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C1-C6)alkyl or a CN; R1b represents H, an halogen or a (C1-C6)alkyl; R1c represents H or a (C1-C6)alkyl; R2 represents H, an halogen, an OH, an O—(C1-C6)alkyl or (C1-C6)alkyl; R3 represents H, an halogen, a (C1-C6)alkyl, an OH, an O—(C1-C6)alkyl, a CONH2 or CN; R4 represents H, an halogen or a (C1-C6)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C1-C6)alkyl, or one of its enantiomers.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: April 18, 2017
    Assignee: SANOFI
    Inventors: John Feutrill, Caroline Leriche, David Middlemiss
  • Patent number: 9624160
    Abstract: The invention relates to reactive ionic liquids containing organic cations with groups or substituents which are susceptible to electrochemical reduction and anions obtained from fluoroalkyl phosphates, fluoroalkyl phosphinates, fluoroalkyl phosphonates, acetates, triflates, imides, methides, borates, phosphates and/or aluminates, for use in electrochemical cells, such as lithium ion batteries and double-layer capacitors.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: April 18, 2017
    Assignee: BASF SE
    Inventors: Michael Schmidt, Nikolai (Mykola) Ignatyev, William-Robert Pitner
  • Patent number: 9624161
    Abstract: The present invention relates to methods for reducing testosterone levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC), metastatic castration resistant prostate cancer (mCRPC), and methods of reducing high or increasing PSA levels and/or increasing SHBG levels in a subject suffering from prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC) and metastatic castration resistant prostate cancer (mCRPC). The compounds of this invention suppress free or total testosterone levels despite castrate levels secondary to ADT and reduce high or increasing PSA levels. This reduction in testosterone levels may be used to treat prostate cancer, advanced prostate cancer, CRPC and mCRPC without causing bone loss, decreased bone mineral density, increased risk of bone fractures, increased body fat, hot flashes and/or gynecomastia.
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: April 18, 2017
    Assignee: GTX, INC.
    Inventors: James T. Dalton, Mitchell S. Steiner, Christopher C. Coss, Robert H. Getzenberg
  • Patent number: 9624162
    Abstract: The present invention provides a method for preparing 3-aminomethyl-3,5,5-trimethyl cyclohexylamine. The method comprises: a) reacting 3-cyano-3,5,5-trimethyl cyclohexanone with excess primary amine as well as removing the water generated from the reaction, so that IPN is substantially converted into imine compounds; b) in the presence of an ammonolysis catalyst, mixing the product of step a) with liquid ammonia, making the imine compound perform ammonolysis reaction to generate 3-cyano-3,5,5-trimethyl cyclohexylimine and the primary amine; and c) in the presence of hydrogen and a hydrogenation catalyst, hydrogenating 3-cyano-3,5,5-trimethyl cyclohexylimine obtained in step b) to obtain 3-aminomethyl-3,5,5-trimethyl cyclohexylamine. The method of the present invention avoids the generation of 3,5,5-trimethyl cyclohexanol and 3-aminomethyl-3,5,5-trimethyl cyclohexanol as the major by-products in the prior art, thereby improving the yield of 3-aminomethyl-3,5,5-trimethyl cyclohexylamine.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: April 18, 2017
    Assignee: Wanhua Chemical Group Co., Ltd.
    Inventors: Changsheng Chen, Jinke Jiang, Zhongying Chen, Jiaoying Cui, Jing Wang, Fuguo Li, Chengge Lv, Wenjuan Zhao, Yuan Li, Weiqi Hua
  • Patent number: 9624163
    Abstract: The invention relates to a new enantioselective process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a ?-amino-?-biphenyl-?-methylalkanoic acid, or acid ester, backbone.
    Type: Grant
    Filed: September 2, 2013
    Date of Patent: April 18, 2017
    Assignees: NOVARTIS AG, ZHEJIANG JIUZHOU PHARMACEUTICAL CO., LTD.
    Inventors: Guoliang Zhu, Wenfa Ye, Hui Zheng, Lingfeng Qian, Junhui Wei, Lijun Yang, Yunguang Li, Lijun Luo
  • Patent number: 9624164
    Abstract: A method for treatment or prevention epilepsy comprising administering a phenyl carbamate compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of epilepsy is provided.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: April 18, 2017
    Assignee: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Patent number: 9624165
    Abstract: Xylylene dicarbamate contains impurities represented by formulas (1) to (4) below at a ratio of less than 100 ppm as a total amount thereof on a mass basis. (In the above-described formulas (1) to (4), R represents a monovalent hydrocarbon group.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: April 18, 2017
    Assignee: MITSUI CHEMICALS, INC.
    Inventors: Koji Takamatsu, Hideki Sone, Masaaki Sasaki
  • Patent number: 9624166
    Abstract: The present invention is directed to a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.
    Type: Grant
    Filed: August 27, 2010
    Date of Patent: April 18, 2017
    Assignee: Tetraphase Pharmaceuticals, Inc.
    Inventors: Yonghong Deng, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Jingye Zhou, Joyce A. Sutcliffe, Magnus P. Ronn
  • Patent number: 9624167
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain substituted N-(4-hydroxy-4-methyl-cyclohexyl)-4-phenyl-benzenesulfonamide and N-(4-hydroxy-4-methyl -cyclohexyl)-4-(2-pyridyl)benzenesulfonamide compounds (collectively referred to herein as HMC compounds) that are useful, for example, in the treatment of disorders (e.g.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: April 18, 2017
    Assignee: PIMCO 2664 Limited
    Inventors: Lisa Patel, Stephen Allan Smith, Iain Robert Greig, Samuel Cameron Williams
  • Patent number: 9624168
    Abstract: The invention relates to the compounds of formula I and formula II 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 or formula II; and methods for treating or preventing inflammation and lipid disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of hypertriglyceridemia, steatohepatitis, cystinosis and inflammatory diseases.
    Type: Grant
    Filed: August 17, 2013
    Date of Patent: April 18, 2017
    Assignee: CELLIX BIO PRIVATE LIMITED
    Inventor: Mahesh Kandula
  • Patent number: 9624169
    Abstract: The application relates to novel compounds and their use in treating and preventing diseases and conditions mediated by modulation of voltage-gated sodium channels. Novel aryl- and heteroaryl-pyrrolidine-2-carboxamide compounds and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Grant
    Filed: March 25, 2016
    Date of Patent: April 18, 2017
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Ben C. Askew, Takeru Furuya
  • Patent number: 9624170
    Abstract: The present invention aims to provide a compound having an MAGL inhibitory action, and useful as a prophylactic or therapeutic agent for neurodegenerative diseases (e.g., Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury, glaucoma, multiple sclerosis and the like), anxiety disorder, pain (e.g., inflammatory pain, carcinomatous pain, nervous pain and the like), epilepsy and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
    Type: Grant
    Filed: December 25, 2014
    Date of Patent: April 18, 2017
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tatsuki Koike, Makoto Fushimi, Jumpei Aida, Shuhei Ikeda, Tomokazu Kusumoto, Hideyuki Sugiyama, Hidekazu Tokuhara
  • Patent number: 9624171
    Abstract: Photoinitiator mixture comprising at least one alpha-amino ketone compound; and at least one compound of the Formula (I) or (I?) wherein R1 and R?1 for example are hydrogen, C3-C8cycloalkyl or C1-C12alkyl R2 and R2? for example are hydrogen; unsubstituted C1-C20alkyl or substituted C1-C20alkyl; and R8 and R9 for example are hydrogen, C1-C12alkyl which optionally is substituted, or phenyl which optionally is substituted; exhibit an unexpectedly good performance in photopolymerization reactions.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: April 18, 2017
    Assignee: BASF SE
    Inventors: Akira Matsumoto, Hisatoshi Kura, Katia Studer, Sébastien Villeneuve
  • Patent number: 9624172
    Abstract: The present invention provides novel polymorphs of Lomitapide, process for their preparation and pharmaceutical compositions comprising them. The present invention also provides a novel polymorph of Lomitapide mesylate, process for its preparation and pharmaceutical compositions comprising it.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: April 18, 2017
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Jambula Mukunda Reddy, Bandi Vamsi Krishna
  • Patent number: 9624173
    Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: April 18, 2017
    Assignee: 3-V Biosciences, Inc.
    Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
  • Patent number: 9624174
    Abstract: Compounds of Formula (I) are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), useful in the treatment of obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as mycocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.
    Type: Grant
    Filed: November 17, 2015
    Date of Patent: April 18, 2017
    Assignee: GlaxoSmithKline LLC
    Inventors: Mui Cheung, Raghuram S. Tangirala
  • Patent number: 9624175
    Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, B, U, V, Z, W1, W2, W3, and R1-R6 are described herein.
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: April 18, 2017
    Assignee: FORMA THERAPEUTICS, INC.
    Inventors: Jian Lin, Anna Ericsson, Ann-Marie Campbell, Gary Gustafson, Zhongguo Wang, R. Bruce Diebold, Susan Ashwell, David R. Lancia, Jr., Justin Andrew Caravella, Wei Lu
  • Patent number: 9624176
    Abstract: A method for preparing caprolactam by using a microreactor under Lewis acid catalysis, wherein a hydroxyl group in a cyclohexanone oxime is activated to obtain a cyclohexanone oxime sulfonates intermediate, then rearranged under Lewis acid catalysis to prepare the caprolactam. The method of this invention has a simple process and a high operation safety and selectivity, the reaction condition is mild, an efficient reaction can take place even at room temperature, the reaction time is short, the conversion of the cyclohexanone oxime can reach 100% within a short time, the selectivity of the caprolactam can reach 99%, the energy consumption is greatly reduced in the premise of maintaining a high yield, and the production cost is reduced, being an efficient and green and environmentally friendly method of for synthesizing the caprolactam.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: April 18, 2017
    Assignee: NANJING TECH UNIVERSITY
    Inventors: Kai Guo, Xin Li, Zheng Fang, Kai Zhang, Qi Yu, Pingkai Ouyang
  • Patent number: 9624177
    Abstract: A method for producing a pyrazole compound represented by formula (1): (wherein R1 represents an optionally substituted C1-12 alkyl group, an optionally substituted C3-12 cycloalkyl group, an optionally substituted C6-16 aryl group, or an optionally substituted pyridyl group, R2 and R3 each independently represent a hydrogen atom, a halogen atom, a C1-3 alkyl group, or a C1-3 haloalkyl group), said method including a step in which a pyrazolidine compound represented by formula (2): (wherein R1, R2, and R3 are as defined above) is reacted with a nitrite in the presence of an acid, allows a pyrazole compound to be produced industrially.
    Type: Grant
    Filed: February 16, 2015
    Date of Patent: April 18, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yasuyuki Nakae, Takashi Miyamoto
  • Patent number: 9624178
    Abstract: The present invention provides substituted cyclopenta and cyclopentyl pyrimidine bicyclic compounds of Formula III, and 5,6-saturated and unsaturated and pharmaceutically acceptable salts, prodrugs, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: April 18, 2017
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 9624179
    Abstract: The invention discloses a novel quinazoline derivative LU1501 and a preparing method thereof, wherein the quinazoline derivative has a chemical name of N-[(4-fluorophenyl)methyl]-4-N-{7-methoxy-6-[(2-pyrrolidin-1-yl)hydroxyethyl]quinazoline-4-yl}phen-1,4-diamine. The quinazoline derivative and a pharmaceutically acceptable salt, a solvate and a hydrate thereof have excellent anti-tumor activity in vitro and in vivo to MCF-7, SK-BR-3, A549, HCT 116, U-118 MG; U-87 MG and MDA-MB-468, and have preferable application prospects on preparing anti-tumor drugs.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: April 18, 2017
    Assignee: NANJING GENERAL HOSPITAL OF NANJING MILITARY REGION OF PLA
    Inventors: Guangming Lu, Zhuoli Zhang, Jing Pan
  • Patent number: 9624180
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: April 18, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhongxing Zhang, Paul Michael Scola
  • Patent number: 9624181
    Abstract: The invention provides a production method of a biaryl compound of the formula [3] or a salt thereof, including reacting a 2-phenylazole derivative of the formula [1] or a salt thereof, with a benzene derivative of the formula [2] or a salt thereof in the presence of a metal catalyst, a base, and one or more of (a) a monocarboxylic acid metal salt, (b) a dicarboxylic acid metal salt, (c) a sulfonic acid metal salt, and (d) a phosphate or phosphoric amide metal salt represented by RAxP(O)(OM)y wherein each symbol is as defined herein.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: April 18, 2017
    Assignee: API Corporation
    Inventor: Masahiko Seki
  • Patent number: 9624182
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: April 18, 2017
    Assignee: AMIRA PHARMACEUTICALS, INC.
    Inventors: Thomas J. Seiders, Lucy Zhao, Jeannie Arruda, Bowei Wang, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Ryan Clark, Heather Renee Coate, Nicholas Simon Stock, Deborah Volkots
  • Patent number: 9624183
    Abstract: A novel process for the preparation of a fluorolactone derivative of the formula and of its acylated derivative of formula wherein R1 stands for a hydroxy protecting group is described. The acylated fluorolactones of formula V, particularly the benzoyl derivative with R1=benzyl are important precursors for the synthesis of prodrug compounds which have the potential to be potent inhibitors of the Hepatitis C Virus (HCV) NS5B polymerase.
    Type: Grant
    Filed: July 14, 2015
    Date of Patent: April 18, 2017
    Assignee: Gilead Pharmasset LLC
    Inventors: Rongmin Chen, Yuanqiang Li, Jianqiang Zhao, Jianbing Zheng, Guoliang Zhu
  • Patent number: 9624184
    Abstract: The present invention relates to a compound represented by the formula (I), which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. In the formula (I), each symbol is as defined in the specification.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: April 18, 2017
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tatsuki Koike, Masato Yoshikawa, Izumi Nomura, Yoshiteru Ito, Eiji Kimura, Haruhi Ando, Tomoaki Hasui, Toshiya Nishi
  • Patent number: 9624185
    Abstract: The present disclosure provides a new method for preparing IDO inhibitor epacadostat. The whole reaction route is simple, easy to control and has high yield.
    Type: Grant
    Filed: January 20, 2016
    Date of Patent: April 18, 2017
    Inventor: Yong Xu
  • Patent number: 9624187
    Abstract: New oxathiazin-like compounds and their derivatives are useful as antineoplastic and antimicrobial agents. Compositions and methods of using oxathiazin-like compounds and their derivatives are disclosed.
    Type: Grant
    Filed: December 3, 2015
    Date of Patent: April 18, 2017
    Assignee: Geistlich Pharma AG
    Inventor: Rolf W. Pfirrmann
  • Patent number: 9624188
    Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compounds of the invention. Formula (I).
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: April 18, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: James Aaron Balog, Audris Huang, Bin Chen, Libing Chen, Weifang Shan
  • Patent number: 9624189
    Abstract: The invention relates to fluorinated compounds and their use in the field of pathological syndromes of the cardiovascular system. Novel fluorinated benzofuran derivatives of amiodarone and pharmaceutically acceptable salts or solvates thereof and their use for the treatment of arrhythmias are described.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: April 18, 2017
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards
  • Patent number: 9624190
    Abstract: Methods to access 2-aryl chromene compounds via an asymmetric catalytic process.
    Type: Grant
    Filed: April 11, 2016
    Date of Patent: April 18, 2017
    Assignee: Northwestern University
    Inventors: Karl A. Scheidt, Bi-Shun Zeng
  • Patent number: 9624191
    Abstract: Eight-membered ring cyclic carbonates having an oxygen or an acylated nitrogen at position 6 were prepared by reaction of precursor diols with ethyl chloroformate. The cyclic carbonates undergo organocatalyzed ring opening polymerization. In one instance, the initial polymer formed comprises a carbonate repeat unit having a Boc-protected nitrogen in the polymer backbone. Deprotecting the nitrogen with acid forms a cationic carbonate repeat unit having a positive charged secondary ammonium nitrogen in the polymer backbone.
    Type: Grant
    Filed: September 23, 2015
    Date of Patent: April 18, 2017
    Assignees: International Business Machines Corporation, Agency For Science, Technology And Research
    Inventors: Mareva B. Fevre, James L. Hedrick, Victor W. L. Ng, Robert J. Ono, Shrinivas Venkataraman, Zhi Xiang Voo, Yi Yan Yang
  • Patent number: 9624192
    Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Grant
    Filed: February 22, 2016
    Date of Patent: April 18, 2017
    Assignee: Novartis AG
    Inventors: Yves Auberson, Mark Gary Bock, Dario Braga, Marco Curzi, Stephanie Kay Dodd, Stefano Luca Giaffreda, Haiyang Jiang, Piotr Karpinski, Thomas J. Troxler, Tie-Lin Wang, Xiaoyang Wang, Xuechun Zhang
  • Patent number: 9624193
    Abstract: A cyclic azine compound represented by general formula (1): wherein each Ar1 represents an aromatic group, which is unsubstituted or substituted by a C1-4 alkyl group, a phenyl group or a pyridyl group; and A represents a group selected from those which are represented by general formulae (2) to (5), described in the description. The cyclic azine compound is useful for an organic compound layer of fluorescent or phosphorescent EL device.
    Type: Grant
    Filed: July 27, 2015
    Date of Patent: April 18, 2017
    Assignees: TOSOH CORPORATION, SAGAMI CHEMICAL RESEARCH INSTITUTE
    Inventors: Hidenori Aihara, Akitoshi Ogata, Yousuke Hisamatsu, Tsuyoshi Tanaka, Nobumichi Arai, Mayumi Abe, Yuichi Miyashita, Takashi Iida, Naoki Uchida
  • Patent number: 9624194
    Abstract: The invention relates to aryl substituted compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein Het, G, A, R, and n are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: April 18, 2017
    Assignee: Purdue Pharma L.P.
    Inventor: Jiangchao Yao
  • Patent number: 9624195
    Abstract: Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.
    Type: Grant
    Filed: December 23, 2015
    Date of Patent: April 18, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Yunfeng Eric Hu, Petr Jansa, Eric Lansdon, Richard L. Mackman
  • Patent number: 9624196
    Abstract: A compound of formula (XV): wherein R1 represents an amino group, a protected amino group or nitro group; or a salt thereof. The compound is a p38 MAP kinase inhibitor. The compound and its pharmaceutically acceptable salts can be used for treatment of conditions, such as inflammatory diseases.
    Type: Grant
    Filed: August 31, 2016
    Date of Patent: April 18, 2017
    Assignees: RESPIVERT LTD., TOPIVERT PHARMA LTD.
    Inventors: Alistair Ian Longshaw, Euan Alexander Fraser Fordyce, Stuart Thomas Onions, John King-Underwood, Jennifer Venable
  • Patent number: 9624197
    Abstract: The present invention is directed to 2-pyridylamino-4-nitrile-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridylamino-4-nitrile-piperidinyl compounds described herein in the 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 pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: April 18, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 9624198
    Abstract: The present application relates to novel substituted piperidinyltetrahydroquinolines, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardial vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: April 18, 2017
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Eva Maria Becker-Pelster, Philipp Buchgraber, Anja Buchmüller, Karen Engel, Volker Geiss, Andreas Göller, Herbert Himmel, Raimund Kast, Andreas Knorr, Dieter Lang, Gorden Redlich, Carsten Schmeck, Hanna Tinel, Frank Wunder
  • Patent number: 9624199
    Abstract: The invention relates to novel substituted bipiperidinyl derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardial vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: April 18, 2017
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Eva Maria Becker-Pelster, Philipp Buchgraber, Anja Buchmüller, Karen Engel, Andreas Göller, Herbert Himmel, Raimund Kast, Joerg Keldenich, Carsten Schmeck, Hanna Tinel, Frank Wunder
  • Patent number: 9624200
    Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.
    Type: Grant
    Filed: October 7, 2014
    Date of Patent: April 18, 2017
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
  • Patent number: 9624201
    Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: April 18, 2017
    Assignees: HOFFMANN-LA ROCHE INC., CHUGAI PHARMACEUTICAL CO.
    Inventors: Francisco Javier Lopez-Tapia, Sung-Sau So, Qi Qiao, Romyr Dominique
  • Patent number: 9624202
    Abstract: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
    Type: Grant
    Filed: September 21, 2016
    Date of Patent: April 18, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventor: Jae U. Jeong