Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides.
Type:
Application
Filed:
April 17, 2017
Publication date:
August 3, 2017
Applicant:
Dow AgroSciences LLC
Inventors:
Paul R. LePlae, JR., James E. Hunter, Gerald B. Watson, William C. Lo, John Herbert
Abstract: A method for producing a compound of formula (I) or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer, such as compound 1 and compound 2 is disclosed. The method proceeds through an O-allylated tyrosine-based compound, such as compound 3 and preferably comprises [3,3] sigmatropic Claisen rearrangement and olefin cross metathesis reactions. In addition, a pharmaceutical composition comprising a compound of formula (I) a tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL) and a pharmaceutically acceptable carrier or excipient is disclosed.
Type:
Application
Filed:
April 13, 2017
Publication date:
August 3, 2017
Applicant:
King Fahd University of Petroleum and Minerals
Inventors:
Muhammad MANSHA, Yasir ABBAS, Nisar ULLAH
Abstract: The invention provides an antibacterial compound of formula (I) or a salt thereof, as well as an antibacterial compound of formula (II) or a salt thereof, wherein R1, R2, X, Y and n have any of the values defined in the specification.
Type:
Application
Filed:
June 15, 2015
Publication date:
August 3, 2017
Applicant:
Rutgers, the State University of New Jersey
Abstract: Phenylhydrazine/anhydride adducts and anaerobic curable compositions using these adducts are provided. The compositions are particularly useful as adhesives and sealants.
Abstract: Ligand functionalized substrates, methods of making ligand functionalized substrates, and methods of using functionalized substrates are disclosed.
Type:
Application
Filed:
April 12, 2017
Publication date:
August 3, 2017
Inventors:
Catherine A. Bothof, Yi He, Jerald K. Rasmussen, Kannan Seshadri, Clinton P. Waller, JR., Douglas E. Weiss
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:
Application
Filed:
April 11, 2017
Publication date:
August 3, 2017
Inventors:
Lisa Patel, Stephen Allan Smith, Iain Robert Greig, Samuel Cameron Williams
Abstract: This invention provides compounds of formulas (I)-(XIV) as defined in the specification, and pharmaceutical compositions comprising the same, and methods of inhibiting, treating, or abrogating a molluscum contagiosum virus infection in a subject using compounds or compositions of the invention:
Type:
Application
Filed:
September 28, 2015
Publication date:
August 3, 2017
Inventors:
Robert P. RICCIARDI, Allen B. REITZ, Michael H. PARKER, Simon David Peter BAUGH
Abstract: The invention relates to a method for preparing a cyclic ?-ketoalcohol, particularly a 6-hydroxycyclohexenone from a cyclic ?-ketoenol, particularly a 6-hydroxycyclohexadienone, using a reducing agent. This reducing agent is selected from hydrogen gas; a secondary alcohol, formic acid and the salts of formic acid or a mixture of at least two representatives of these compound classes. The invention further comprises the use of an ?-ketoenol, in particular a 6-hydroxycyclohexadienone, as intermediate for preparing astaxanthin.
Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
Type:
Application
Filed:
November 9, 2016
Publication date:
August 3, 2017
Inventors:
Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V. Moody, Xiuwen Zhu, Scott Stirn
Abstract: The present invention relates to a process for preparation of dexmethylphenidate hydrochloride from racemic methylphenidate. The process involves the treatment of racemic mixture of dl-throe-methylphenidate base in the presence of di-pivaloyl-D-tartaric acid (D-DPTA) in a solvent to isolate dipivaloyl tartrate salt of d-threo-methylphenidate. The dipivaloyl tartrate salt of d-threo-methylphenidate is treated with a base to obtain a d-threo-methylphenidate base, which is extracted using a suitable solvent. The d-threo-methylphenidate base is treated with hydrochloric acid-isopropyl alcohol solution to obtain slurry of d-threo-methylphenidate hydrochloride also known as dexmethylphenidate hydrochloride. The dexmethylphenidate hydrochloride slurry is filtered and washed with acetone. The invention also discloses a process for recovery of D-DPTA from the salt mother liquor and from the spent aqueous layer.
Type:
Application
Filed:
November 3, 2014
Publication date:
August 3, 2017
Inventors:
Ashutosh Digambar GUPTE, Sunil Vaman JOSHI, Amit Hari PAKHURDE
Abstract: The present invention belongs to the field of antibacterial agents, more specifically to antibacterials for treating Acinetobacter baumannii infections. The invention provides arylhydrazides containing a 2-pyridone moiety, according to formula (I), which show selective antibacterial activity against A. baumannii. The invention also relates to their use as medicaments and specifically as antibacterials for the treatment of A. baumannii infections, as well as to a process for their preparation and to pharmaceutical compositions containing them.
Type:
Application
Filed:
July 29, 2015
Publication date:
August 3, 2017
Applicant:
ABAC THERAPEUTICS, S.L.
Inventors:
Domingo GARGALLO VIOLA, Albert PALOMER BENET
Abstract: The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 channel-related diseases.
Abstract: The present invention relates to novel 4-substituted pyridine-2,6-dicarboxylic acid derivatives, compounds of formula I, wherein R1 and R2 are defined herein. The compounds of formula I are useful for making pharmaceutical compositions to treat proliferative diseases. The present invention also relates to concise methods for preparing compounds of formula I that may be performed under mild reaction conditions.
Type:
Application
Filed:
September 9, 2015
Publication date:
August 3, 2017
Applicant:
Okinawa Institute of Science and Technology School Corporation
Abstract: 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:
Application
Filed:
February 22, 2017
Publication date:
August 3, 2017
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
Abstract: 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:
Application
Filed:
February 22, 2017
Publication date:
August 3, 2017
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
Abstract: The present invention relates to sulfonamide derivatives of formula (I) where the substituents R1-R6 and R8, L, A and n are as defined in the application, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants, improving plant tolerance to abiotic stress (including environmental and chemical stresses), inhibiting seed germination and/or safening a plant against phytotoxic effects of chemicals.
Type:
Application
Filed:
August 7, 2015
Publication date:
August 3, 2017
Inventors:
Olivier LOISELEUR, Sebastian Volker WENDEBORN, Sean R. CUTLER
Abstract: The present invention relates to a method of preparing Cabozantinib (Cyclopropane-1,1-dicarboxylic acid [4-(6,7-dimethoxy-quinolin-4-yloxy)-phenylo]amide(4-fluoro-phenyl)amide) and 18F labeled Cabozantinib.
Type:
Application
Filed:
July 31, 2015
Publication date:
August 3, 2017
Inventors:
Wei XU, David J. Donnelly, Patrick L. Chow, Benjamin J. Henley
Abstract: This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof, that inhibit bacterial gyrase. The compounds are useful as inhibitors of bacterial gyrase activity and bacterial infections, and have the structure of Formula (I) as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.
Type:
Application
Filed:
August 3, 2015
Publication date:
August 3, 2017
Inventors:
Javier de Vicente FIDALGO, Haiying HE, Cheng HU, Zhigan JIANG, Xiaolin LI, Peichao LU, Wosenu MERGO, Daniel MUTNICK, Folkert RECK, Alexey RIVKIN, Colin Keith SKEPPER, Xiaojing Michael WANG, Jianhua XIA, Yongjin XU
Abstract: The invention relates inter alia to halogen-substituted compounds of the general formula (I) in which the substituents A1, R1-R3 and Z1-Z3 have the meanings given in the description. Also described are processes for preparing the compounds of the formula (I) and possible intermediates for the preparation of these compounds. The compounds according to the invention are particularly suitable for controlling insects, arachnids and nematodes in agriculture and ectoparasites in veterinary medicine.
Type:
Application
Filed:
August 5, 2015
Publication date:
August 3, 2017
Inventors:
MICHAEL MAUE, TOBIAS HARSCHNECK, REINER FISCHER, THOMAS BRETSCHNEIDER, JULIA JOHANNA HAHN, ANNE DECOR, WERNER HALLENBACH, HANS-GEORG SCHWARZ, JOHANNES KOEBBERLING, WALTER HUEBSCH
Abstract: Provided is a method of preparing 3-fluoroalkyl-1-substituted pyrazol-4-carboxylic acid by air oxidation. The methoduses 3-fluoroalkyl-1-substituted pyrazol-4-formaldehyde as raw material for reaction in a neutral or alkaline condition under the action of a catalyst and with air as an oxidizing agent, to obtain 3-fluoroalkyl-1-substituted pyrazol-4-carboxylic acid. The method employs a mild, safe and clean reaction, and is suitable for industrial mass production.
Abstract: The invention concerns a process for the manufacture of pyrazole-4-carboxamides, in particular, of 3-difluoromethyl-1-methyl-H-pyrazole-4-carboxamides which are useful as pharmaceuticals and agrochemicals. The carboxamides are prepared from the corresponding pyzole-4-carboxylic acid esters and appropriate amine in the presence of a Lewis acid comprising at least one halogen ligand. Alternatively, the reaction is performed in the presence of a Lewis acid comprising at least one halogen ligand and a base.
Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2 , R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.
Abstract: A novel class of drugs for treating androgen receptor (AR) positive cancer including prostate cancer and breast cancer are described. The drugs include the chemical scaffolds of a high affinity androgen receptor ligand and a histone deacetylase inhibitor. Also described are compositions including the novel drugs and methods of treating AR positive cancer using the compositions.
Abstract: The present invention provides a salt form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibits desirable characteristics for the same.
Type:
Application
Filed:
January 9, 2017
Publication date:
August 3, 2017
Inventors:
Mei Lai, Steven Richard Witowski, Richland Wayne Tester, Kwangho Lee
Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Type:
Application
Filed:
April 18, 2017
Publication date:
August 3, 2017
Inventors:
Ruoxi LAN, Bayard R. HUCK, Xiaoling CHEN, Lizbeth C. DESELM, Hui QIU, Yufang XIAO, Constantin NEAGU, Igor MOCHALKIN, Theresa L. JOHNSON
Abstract: Provided are 5-(trifluoromethyl)pyrimidine derivatives useful as intermediates for pharmaceuticals and agrochemicals and as intermediates for electronic materials and methods for producing the same. 2,4-dichloro-5-(trifluoromethyl)pyrimidine is reacted with 2,2,2-trifluoroethanol, benzyl alcohol, or benzenethiol to obtain the intended 2-(2,2,2-trifluoroethoxy)-4-chloro-5-(trifluoromethyl)pyrimidine, 2-benzyloxy-4-chloro-5-(trifluoromethyl)pyrimidine, 2,4-bis(2,2,2-trifluoroethoxy)-5-(trifluoromethyl)pyrimidine, or 2-chloro-4-phenylthio-5-(trifluoromethyl)pyrimidine.
Abstract: The present invention relates to novel heterocyclic compounds based on a quinazoline scaffold, which bind effectively to the mitochondrial translocator protein (TSPO), and counteract cell death processes. These compounds can also stimulate neuronal differentiation. The present invention further relates to pharmaceutical compositions including such compounds, and methods of using these compounds for the prevention and treatment of brain damage resulting from brain injury, especially secondary brain damage due to traumatic brain injury (TBI). The compounds of the invention are also useful in preventing, treating, and curing brain damage due to neurodegenerative diseases, including underlying and associated pathological and mental disorders. The compounds can also be used to prevent and treat brain damage due to infection, toxic challenges, and excessive drug use, e.g., recreational, over the counter, or prescription drugs.
Type:
Application
Filed:
April 22, 2015
Publication date:
August 3, 2017
Inventors:
Moshe GAVISH, Jehuda (leo) Arieh VEENMAN, Alex SHTERENBERG, Ilan MAREK, Alex VAINSHTEIN, Avraham AVITAL
Abstract: Bicyclic arylcarboxamides of the general formula (I) are described as herbicides. In this formula (I), Z1, Z2, Z3, Z4 and Z5 are a bond, O, S(O)n or a substituted carbon atom. X is a radical such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a substituted heterocycle.
Type:
Application
Filed:
July 24, 2015
Publication date:
August 3, 2017
Inventors:
Ralf BRAUN, Christian WALDRAFF, Hansjörg DIETRICH, Dirk SCHMUTZLER, Elmar GATZWEILER, Christopher Hugh ROSINGER
Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
Type:
Application
Filed:
April 14, 2017
Publication date:
August 3, 2017
Applicant:
LEO LABORATORIES LIMITED
Inventors:
Gunnar GRUE-SØRENSEN, Xifu LIANG, Thomas HÖGBERG, Kristoffer MÅNSSON, Per VEDSØ, Thomas VIFIAN
Abstract: The present invention relates to an improved process for the preparation of Linezolid of Formula-I comprising reacting compound of Formula-II with compound of Formula-III in presence of metal base wherein, said metal base is prepared in situ in a single lot. The invention also relates to an isolated acetamide impurity of Formula-IV produced in the process for preparation of Linezolid, its purification and its use as a reference marker.
Type:
Application
Filed:
December 15, 2016
Publication date:
August 3, 2017
Inventors:
Sonu Kumar, Bhuwan Bhashkar, Anil Kumar
Abstract: Compounds represented by structural formulas described herein, such as Structural Formula (I): or a pharmaceutically acceptable salt thereof are useful in treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.
Type:
Application
Filed:
February 9, 2017
Publication date:
August 3, 2017
Applicant:
University of Florida Research Foundation, Inc.
Abstract: The present invention includes compounds useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention.
Type:
Application
Filed:
July 28, 2015
Publication date:
August 3, 2017
Inventors:
Arun K. Sharma, Manoj Pandey, Shantu Amin, Mohinder P. Mahajan, Gurleen Kaur
Abstract: Methods of preparing a second high-efficiency, rhenium-promoted silver catalyst for producing alkylene oxide from an alkylene based on a first catalyst are disclosed and described. In accordance with the disclosed methods, the first and second catalysts include at least one promoter that includes a rhenium promoter. The target catalyst concentrations of one or more promoters of the at least one promoter on the second catalyst are determined based on the values of a catalyst reference property for the two catalysts and the concentration of the one or more promoters of the at least one promoter on the first catalyst. Suitable catalyst reference properties include carrier specific surface area and silver specific surface area. Reaction systems utilizing the first and second catalysts are also described.
Type:
Application
Filed:
April 11, 2017
Publication date:
August 3, 2017
Inventors:
Hirokazu Shibata, Arun Basrur, Srikant Gopal, Mark McAdon, Albert Cheng-Yu Liu, Liping Zhang, Ernest R. Frank
Abstract: A process for the production of aromatic primary amines, by reacting an aromatic dialdehyde with hydrogen and ammonia or an ammonia-liberating compound, in the presence of a hydrogenation catalyst and an amine, wherein the molar ratio of the amine to the aromatic dialdehyde is no less than 1:4 at the start of the reaction.
Abstract: A process is described for converting hydroxymethylfurfural to furanic products inclusive of 2,5-furandicarboxylic acid, comprising combining a quantity of hydroxymethylfurfural with water to provide an aqueous solution containing at least about five percent by weight of hydroxymethylfurfural, and combining the aqueous solution with an oxygen source in the presence of a heterogeneous ruthenium-based catalyst and under conditions which are effective for oxidizing hydroxymethylfurfural to furanic oxidation products inclusive of 2,5-furandicarboxylic acid, but in the substantial absence of any solvent for either hydroxymethylfurfural or 2,5-furandicarboxylic acid other than water.
Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
Type:
Application
Filed:
August 6, 2015
Publication date:
August 3, 2017
Inventors:
Helen Chen, Steven L. Colletti, Duane DeMong, Yan Guo, Michael Miller, Anilkumar Nair, Christopher W. Plummer, Dong Xiao, De-Yi Yang
Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
Type:
Application
Filed:
August 3, 2015
Publication date:
August 3, 2017
Inventors:
Harry Chobanian, Duane DeMong, Yan Guo, Barbara Pio, Christopher W. Plummer
Abstract: Described herein are coformer salts of (2S,3S)-methyl 7-fluoro-2-(4-fluorophenyl)-3-(1-methyl-1H-1,2,4-triazol-5-yl)-4-oxo-1,2,3,4-tetrahydroquinoline-5-carboxylate optionally as a solvate and additionally optionally as a hydrate, including crystalline forms, and methods of preparing the (2S,3S)-methyl 7-fluoro-2-(4-fluorophenyl)-3-(1-methyl-1H-1, 2,4-triazol-5-yl)-4-oxo-1,2,3,4-tetrahydroquinoline-5-carboxylate optionally as a coformer salts.
Type:
Application
Filed:
July 30, 2015
Publication date:
August 3, 2017
Inventors:
Mark HENDERSON, Colm CAMPBELL, Carsten JAGUSCH, Christian Klaus HERZ, Nico BAUER, Thierry BONNAUD, Olivier LAMBERT
Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Abstract: Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP) are described herein. Exemplary disorders include schizophrenia and cognitive deficit.
Type:
Application
Filed:
March 13, 2017
Publication date:
August 3, 2017
Inventors:
Masaki Suzuki, Kazumi Kondo, Muneaki Kurimura, Krishna Reddy Valluru, Akira Takahashi, Takeshi Kuroda, Haruka Takahashi, Tae Fukushima, Shin Miyamura, Indranath Ghosh, Abhishek Dogra, Geraldine Harriman, Amy Elder, Satoshi Shimizu, Kevin J. Hodgetts, Jason S. Newcom
Abstract: This disclosure relates to the field of preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine and intermediates therefrom. These intermediates are useful in the preparation of certain pesticides.
Abstract: A process for preparing 3-[(S)-7-bromo-2-(2-oxo-propylamino)-5-pyridin-2-yl-3H-1,4,-benzodiazepin-3-yl]propionic acid methyl ester at a high conversion rate with good reproducibility by oxidizing 3-[(S)-7-bromo-2-(2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]propionic acid methyl ester in the presence of an oxidation catalyst is provided by defining the ammonium ion content of 3-[(S)-7-bromo-2-(2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]propionic acid methyl ester.