Abstract: The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula, the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5,6 and 13,14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, R1 and R2 independently represent hydrogen atom or a straight or branched C1-10 alkyl- or aralkyl-group, optionally substituted with —ONO2 group, or an aralkyl- or aryl-group, which contains heteroatom, R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl-group, or an optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl-group, Y represents (CH2)n group or O atom or S atom, and where n=0-3.
Type:
Grant
Filed:
December 10, 2015
Date of Patent:
February 21, 2017
Assignee:
CHINOIN ZRT
Inventors:
Gábor Havasi, Tibor Kiss, Irén Hortobágyi, Zsuzsanna Kardos, István Lászlófi, Zoltán Bischof, Ádám Bódis
Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases. (I), (II).
Type:
Grant
Filed:
June 4, 2015
Date of Patent:
February 14, 2017
Assignee:
INCURON, LLC
Inventors:
John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
Abstract: The invention relates to indole carboxamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
Type:
Grant
Filed:
December 17, 2013
Date of Patent:
January 31, 2017
Assignee:
ACTELION PHARMACEUTICALS LTD.
Inventors:
Kurt Hilpert, Francis Hubler, Dorte Renneberg, Simon Stamm
Abstract: Disclosed are compounds of formula (1) and (2) and/or E/E-, E/Z- or Z/Z geometrical isomer forms thereof; wherein R1-R5, R1-R11 and A are defined as in description. The compounds are used as UV absorbers for protecting household products from photolytic and oxidative degradation, as plastic additives, preferably for food and pharmaceutical packaging applications, for preventing photo-degradation of food by incorporation of the compounds of formula (1?) and/or (2?) into transparent food containers, for protection of UV-A sensitive drugs from photo-degradation by incorporation of UV absorber in transparent blister foils or transparent pharmacy containers, as additives for photographic and printing applications, as additives for electronic applications and protecting the ingredients in agriculture applications.
Type:
Grant
Filed:
July 19, 2012
Date of Patent:
January 24, 2017
Assignee:
BASF SE
Inventors:
Barbara Winkler, Dietmar Hueglin, Kai Eichin, Larissa Ehrsam, Xavier Marat, Hervé Richard, ILona Marion Kienzle, Ute Schroeder
Abstract: Heterocycle amino alkyloxy substituted quinazoline derivatives as represented by the structural Formula (I) and pharmaceutically acceptable salts thereof, capable of inhibiting the activity of receptor tyrosine kinase EGFR, and being used to treat cancers related to the expression of the receptor tyrosine kinase of the ErbB family are provided.
Abstract: The present invention discloses a preparation method of 2,3-dimethyl phenyl-1-trityl-imidazole-4-ketone. In accordance with this method, imidazole-4-ethyl formate is used as a raw material; ethyl formate is used for amino protection, 1-trityl-1H-imidazole-4-formic acid is obtained after basic hydrolysis; 1-trityl-1H-imidazole-4-formic acid and N,O-dimethylhydroxylamine hydrochloride are subjected to condensation so as to obtain N-methoxyl-N-methyl-1-trityl-1H-imidazole-4-formamide; and N-methoxyl-N-methyl-1-trityl-1H-imidazole-4-formamide and a Grignard reagent prepared by the reaction of 2,3-dimethylbromobenzene with magnesium are subjected to a Grignard reaction, and then the target product 2,3-dimethyl phenyl-1-trityl-1H-imidazole-4-ketone is obtained. Compared with the reported preparation methods, the preparation method is more convenient to operate and is beneficial for industrial production.
Abstract: An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
Type:
Grant
Filed:
August 8, 2012
Date of Patent:
January 10, 2017
Assignee:
Immunomet Therapeutics, Inc.
Inventors:
Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
Abstract: The present invention is concerned with a novel process for the preparation of a compound of formula I and its hydrates The compounds of formula I and the corresponding hydrates are pharmaceutically active substances.
Type:
Grant
Filed:
October 24, 2014
Date of Patent:
December 27, 2016
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean-Michel Adam, Charles Alois Dvorak, Daniel Fishlock, Eric R. Humphreys, Hans Iding, Christophe Pfleger, Pankaj D. Rege, Xianqing Shi, Justin Vitale, Shaoning Wang, Marian Zajac
Abstract: The present invention relates to novel strigolactam derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.
Type:
Grant
Filed:
November 3, 2015
Date of Patent:
December 20, 2016
Assignee:
Syngenta Participations AG
Inventors:
Mathilde Denise Lachia, Alain De Mesmaeker, Emmanuelle Villedieu-Percheron, Hanno Christian Wolf, Pierre Joseph Marcel Jung, Franciscus Cornelis Lanfermeijer, Paul Willem Jan Van Den Wijngaard, Claudio Screpanti
Abstract: The disclosure describes the use of one or more compounds that fall within the scope of one or more of structural formulae I, II, III, IV, V, or VI for treating triple negative breast Compounds useful for treating breast cancer include those compounds of formulae I, II, III, IV, V, or VI that inhibit proliferation of breast cancer cells and/or lead to the death of breast cancer cells, especially triple negative breast cancer.
Type:
Grant
Filed:
July 27, 2012
Date of Patent:
December 13, 2016
Assignees:
MEDIVATION PROSTATE THERAPEUTICS, INC., THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE
Inventors:
Andrew A. Protter, Jennifer Richer, Dawn Cochrane
Abstract: Derivatives of 1,3-dithianes and 1,3-dithiolanes of the general formula 1a or salts thereof of the general formula 1b where P=polymeric support, m=1 or 2, Z is an organic linker or X=inorganic or organic anion, processes for preparation thereof and use thereof.
Type:
Grant
Filed:
September 23, 2014
Date of Patent:
December 13, 2016
Assignee:
KARLSRUHER INSTITUT FUER TECHNOLOGIE
Inventors:
Nicole Jung, Simone Graessle, Stefan Braese
Abstract: The compounds provided herein are phenyl analine amides and are useful for inhibiting histone deacteylase (“HDAC”) enzymes, such as HDAC1, HDAC2, and HDAC3.
Type:
Grant
Filed:
January 16, 2015
Date of Patent:
December 6, 2016
Assignee:
BIOMARIN PHARMACEUTICAL INC.
Inventors:
Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
Abstract: The invention relates to besylate and tosylate salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-4-yl}acetic acid and solvates thereof, to the use thereof in a method of treating and/or preventing virus infections, and to the use thereof to produce drugs for use in treating and/or preventing diseases, in particular use as antiviral agents, in particular against cytomegaloviruses.
Type:
Grant
Filed:
February 28, 2013
Date of Patent:
December 6, 2016
Assignee:
AICURIS GMBH & CO. KG
Inventors:
Welljanne Maertens, Christian Schickaneder
Abstract: The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.
Type:
Grant
Filed:
December 21, 2012
Date of Patent:
December 6, 2016
Assignee:
Knopp Biosciences, LLP
Inventors:
Weirong Chen, Michael Humora, Daw-long Albert Kwok, William F. Kiesman, Erwin Ayandra Irdam
Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.
Type:
Grant
Filed:
July 1, 2014
Date of Patent:
November 29, 2016
Assignee:
Dana-Farber Cancer Institute, Inc.
Inventors:
Hwan Geun Choi, Taebo Sim, Nathanael Gray, Wenjun Zhou, Jae Won Chang, Jianming Zhang, Ellen Weisberg
Abstract: In a thermoelectric conversion element comprising a thermoelectric conversion layer formed by using a thermoelectric conversion material, the thermoelectric conversion material includes a polythiophene polymer, which includes a main chain made of a repeating unit represented by the following formula (1), and has a side chain R in a regiorandom array with respect to the main chain, a carbon nanotube, and a non-conjugated macromolecule. In Formula (1), R represents an alkyl group having 1 to 20 carbon atoms.
Abstract: An organic light-emitting device having a light-emitting layer containing a compound represented by the general formula below has a high light emission efficiency. In the general formula, at least one of R1 to R5 represents a cyano group, at least one of R1 to R5 represents a 9-carbazolyl group, a 1,2,3,4-tetrahydro-9-carbazolyl group, a 1-indolyl group or a diarylamino group, and the balance of R1 to R5 represents a hydrogen atom or a substituent.
Abstract: There is provided novel fluoro-substituted compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.