Abstract: There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C1-C6 alcohol and an aprotic polar solvent in the presence of a base and water.
Abstract: The invention relates to compounds of formula (I) where A1, A2, A3, A4, G, R1, R2, R3 and R4 are as defined in claim 1; or a salt or JV-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
Abstract: The present invention is directed to benzazole compounds that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.
Type:
Grant
Filed:
October 28, 2013
Date of Patent:
February 3, 2015
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Adnan M. M. Mjalli, David Robert Jones, Devi Reddy Gohimukkula, Guoxiang Huang, Jeff Jiqun Zhu, Mohan Rao, Robert Carl Andrews, Tan Ren
Abstract: The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.
Type:
Grant
Filed:
October 17, 2011
Date of Patent:
January 27, 2015
Assignees:
Korea Research Institute of Bioscience and Biotechnology, Dongguk University Industry-Academic Cooperation Foundation
Inventors:
Kyeong Lee, Mi Sun Won, Hwan Mook Kim, Song Kyu Park, Kiho Lee, Ki Hoon Lee, Chang Woo Lee, Jung Joon Lee, Kyung Sook Chung, Bo Kyung Kim, Yinglan Jin, Seung-hee Lee
Abstract: The invention relates to compounds of formula (I): The invention likewise relates to a cosmetic method for depigmenting, lightening and/or whitening keratin materials, more particularly the skin, that utilizes these compounds.
Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.
Type:
Grant
Filed:
October 4, 2013
Date of Patent:
January 13, 2015
Assignee:
Amura Limited
Inventors:
Martin Quibell, John Paul Watts, Nicholas Sean Flinn
Abstract: The present invention relates to a process for the activation of double metal cyanide (DMC) catalysts for the preparation of polyether carbonate polyols by catalytic copolymerisation of carbon dioxide (CO2) with alkylene oxides in the presence of one or more H-functional starter substances.
Type:
Grant
Filed:
January 18, 2011
Date of Patent:
January 13, 2015
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Christoph Gürtler, Stefan Grasser, Jörg Hofmann, Aurel Wolf
Abstract: The invention relates to the use of diazonium salts for the formation of thick layers on at least one surface of a substrate. The diazonium salts used in the invention have the following formula (I): wherein R is a group that can be electrochemically reduced in a reversible manner to a cathodic potential between 0 and ?1.5 V, E is a spacer chain consisting of at least one aromatic cyclic group having between 5 and 6 links, optionally containing at least one heteroatom preferably selected from N, S, O or P and optionally substituted by at least one group selected from the C1-C5 alkyls and the halogens, r is 1 or 2, m is a whole number between 1 and 5 inclusive, p is a whole number between 1 and 5, and B is a counter-ion. The invention can be especially applied to the field of gas sensors.
Type:
Grant
Filed:
August 31, 2011
Date of Patent:
January 6, 2015
Assignee:
Commissariat a l'Energie Atomique et aux Energies Alternatives
Abstract: The present invention relates to novel 5-hydroxy-5-aryl-pyrrol-2-ones, their preparation and their use as non-peptide CCK ligands, particularly in pharmaceutical formulations thereof.
Type:
Grant
Filed:
July 2, 2012
Date of Patent:
December 30, 2014
Assignee:
PNB Vesper Life Sciences Pvt. Ltd.
Inventors:
Padijarethakkal N Balaram, Pornthip Lattmann
Abstract: New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.
Type:
Grant
Filed:
April 9, 2012
Date of Patent:
December 9, 2014
Assignee:
Bial-Portela & Ca, S.A.
Inventors:
David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto Dos Santos Ferreira, Patricio Manuel Vieira Araújo Soares da Silva
Abstract: Crosslinked polymers, methods for their preparation and use, are described in which the crosslinked polymers are formed from at least two polymer precursors, one of which is designed, upon degradation of the crosslinked polymer, to release the second polymer precursor in its original, unmodified chemical form.
Type:
Grant
Filed:
April 15, 2013
Date of Patent:
November 18, 2014
Assignee:
Confluent Surgical, Inc.
Inventors:
Rachit Ohri, Phillip Blaskovich, Joshua Kennedy, Steven L. Bennett, Arthur Driscoll
Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.
Type:
Grant
Filed:
September 23, 2013
Date of Patent:
November 18, 2014
Assignee:
LG Life Sciences Ltd.
Inventors:
Soon Ha Kim, Hyoung Jin Kim, Sun Young Koo, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Seung Yup Paek, Hyo Shin Kwak, Dong Ook Seo, Eok Park
Abstract: The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a salt thereof, where R1-3 are as defined in the specification.
Abstract: The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof; to a composition comprising a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluent; and also to use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, or preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, or preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
Type:
Grant
Filed:
May 16, 2011
Date of Patent:
November 11, 2014
Assignee:
Institute of Pharmacology and Toxicology Medical Sciences P.L.A. China
Inventors:
Song Li, Wu Zhong, Juan Liu, Lili Wang, Kunlun He, Long Long, Junhai Xiao, Zhibing Zheng, Wei Li, Xin Li, Guoliang Hu
Abstract: This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration.
Type:
Grant
Filed:
July 1, 2010
Date of Patent:
November 11, 2014
Assignee:
Dermira (Canada), Inc.
Inventors:
Timothy Scott Daynard, Geoffrey C. Winters, David W. C. Hunt
Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.
Type:
Grant
Filed:
February 19, 2013
Date of Patent:
November 4, 2014
Assignee:
Board of Regents of The University of Texas System
Inventors:
Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
Abstract: Disclosed are furo[3,2-g]chromene derivatives represented by formula (I), stereoisomers, pharmaceutically acceptable salts, and pharmaceutical compositions thereof, as well as uses thereof as estrogen receptor modulators.
Type:
Grant
Filed:
April 13, 2011
Date of Patent:
November 4, 2014
Assignee:
Shenyang Pharmaceutical University
Inventors:
Chun Hu, Shihui Wang, Yan Wang, Erfang Huang, Xiaoping Liu, Dawei Li
Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.
Type:
Grant
Filed:
September 14, 2012
Date of Patent:
October 28, 2014
Assignee:
Arena Pharmaceuticals, Inc.
Inventors:
Bradley Teegarden, Honnappa Jayakumar, Hongmei Li, Sonja Strah-Pleynet, Peter I. Dosa
Abstract: Novel agents exhibiting anti-biofilm formation activity while being non-cytotoxic are provided, as well as methods of using the same, either per se or conjugated to a polymer, for preventing and/or reducing the formation of microbial biofilms and/or for disrupting microbial biofilms. The novel agents described herein include thiazolidine-2,4-diones (TZDs), pyrrolidine-2,5-diones (PYDs), imidazolidine-2,4-diones or oxazolidine-2,4-diones, substituted by an alkyl having 7-20 carbon atoms in its backbone chain.
Type:
Grant
Filed:
November 19, 2009
Date of Patent:
October 21, 2014
Assignees:
Yissum Research Development Company of the Hebrew University of Jerusalem Ltd., Hadasit Medical Research Services and Development Ltd.