Abstract: The present invention provides novel, stable, processable and pharmaceutically acceptable salt forms of 2R,6R-hydroxynorketamine or 2S,6S-hydroxynorketamine with high aqueous solubility.
Type:
Grant
Filed:
July 31, 2018
Date of Patent:
July 5, 2022
Assignee:
SMALL PHARMA LTD.
Inventors:
David Pearson, Lorraine Sharp, Alan Armstrong, Richard Myerson, Jonathan Hull, Paul Blaney, Peter Rands, Marie Layzell, Zelah Joel
Abstract: The present invention is directed to novel pyrrolidine carboxylic acid derivatives, pharmaceutical compositions, and their use in treating and/or preventing metabolic diseases as agonists of g-protein coupled receptor 43.
Type:
Grant
Filed:
June 18, 2012
Date of Patent:
July 4, 2017
Assignee:
Ogeda SA
Inventors:
Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
Abstract: Process for preparing a halogenated precursor of an alkenone, which comprises reacting a carboxylic acid halide with a vinyl ether in a liquid reaction medium using an equipment having at least one surface in contact with the liquid reaction medium, wherein said surface consists of a material selected from glass, polytetrafluoroethylene and nickel based metal alloy.
Type:
Grant
Filed:
December 21, 2012
Date of Patent:
November 24, 2015
Assignee:
SOLVAY SA
Inventors:
Max Josef Braun, Uta Claassen, Sara Claessens
Abstract: The present invention relates to a process for preparing a ketosulfone derivative and, more particularly, to an improved method for synthesising 1-(6-methylpyridin-3-yl)-2-[(4-methylsulfonyl)-phenyl]ethanone by means of Pd-catalysed alpha arylation process of a heteroaromatic ketone derivative.
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 provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections.
Type:
Application
Filed:
October 31, 2012
Publication date:
February 19, 2015
Applicant:
ASTEX THERAPEUTICS LIMITED
Inventors:
Andrew James Woodhead, Christopher Charles Frederick Hamlett, Gilbert Ebai Besong, Gianni Chessari, Maria Grazia Carr, Alessia Millemaggi, David Norton, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson, Steven Douglas Hiscock
Abstract: The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3: wherein R1 is a substituted or unsubstituted aryl or heterocyclyl group, R2, R3, and R4 are hydrogen atoms, n is 2, X is halogen, R5 and R6 independently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein R5 and R6 are not hydrogen atoms at the same time, or R5 and R6 may be taken together to form a saturated or unsaturated and substituted or unsubstituted heterocyclyl group containing a nitrogen atom (N); an inhibitor of protein crosslinking comprising the compound; and a composition for preventing or treating a protein-crosslinking causative disease, which comprises the compound or the protein crosslinking inhibitor.
Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.
Abstract: The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation.
Type:
Grant
Filed:
March 5, 2013
Date of Patent:
November 18, 2014
Assignee:
Merck Patent GmbH
Inventors:
Andreas Goutopoulos, Henry Yu, Benny C. Askew, Jr., Lesley Liu-Bujalski
Abstract: Compounds of the formula: are disclosed. The compounds act as phosphodiesterase-4 modulators, and useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions. Other embodiments are also disclosed.
Type:
Grant
Filed:
November 20, 2008
Date of Patent:
November 4, 2014
Assignee:
Decode Genetics EHF
Inventors:
Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov
Abstract: The present invention relates to a compound of formula (I): wherein: X is methyl or chlorine; R1 is methyl or chlorine; R2 is hydrogen, methyl, ethyl, n-propyl, cyclopropyl, vinyl, ethynyl, fluorine, chlorine, bromine, methoxy, ethoxy or fluoromethoxy; and G, R3, R4, R5 and R6 are as defined herein; wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof.
Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
Abstract: The present invention describes a process for preparing a cyclooxygenase-2 selective inhibitor. It provides a synthetic procedure for the said substance namely 5-chloro-3-(4-methylsulphonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine of formula (I). The invention also relates to preparation of a new intermediate of formula (IV) and a process to prepare it. Furthermore, the invention describes a process for preparing another key intermediate of formula (II). Compounds of formula (IV) and formula (II) are useful intermediates in synthesis of the said cyclooxygenase-2 inhibitor.
Abstract: The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.
Type:
Application
Filed:
April 22, 2014
Publication date:
August 14, 2014
Applicant:
Catabasis Pharmaceuticals, Inc.
Inventors:
Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu, Amal Ting
Abstract: The present invention relates to an efficient process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib. Water is employed as reaction medium.
Type:
Grant
Filed:
June 21, 2013
Date of Patent:
July 1, 2014
Assignee:
F.I.S.—Fabrica Italiana Sintetici S.p.A.
Abstract: The present invention relates to an inhibitor for tobacco axillary bud growth, the inhibitor comprising one or more cell division inhibitors selected from the group consisting of pyridine-based compounds and benzamide-based compounds. This inhibitor for tobacco axillary bud growth has excellent sustainability of effect at low concentration, does not cause chemical damage and disease, and can ensure an improvement in labor productivity. An aliphatic alcohol having 6 to 20 carbon atoms is furthermore combined with the cell division inhibitors selected from pyridine-based compounds and benzamide-based compounds to thereby synergistically enhance the effect of inhibiting the emergence and growth of tobacco axillary buds.
Abstract: Disclosed is a practical method for efficiently producing an alcohol compound by hydrogenating an aldehyde by using a homogeneous copper catalyst which is an easily-available low-cost metal species. Specifically disclosed is a method for producing an alcohol compound, which is characterized in that a hydrogenation reaction of an aldehyde compound is performed in the presence of a homogeneous copper catalyst, a monophosphine compound and an alcohol selected from the group consisting of primary alcohols, secondary alcohols and mixtures of those.
Abstract: A process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methyl sulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib. The synthesis of the intermediates useful for such preparation is also described.
Type:
Grant
Filed:
January 11, 2012
Date of Patent:
March 4, 2014
Assignee:
F.I.S. Fabbrica Italiana Sintetici S.p.A.
Inventors:
Andrea Castellin, Paolo Stabile, Francesco Fontana, Ottorino De Lucchi, Andrea Caporale, Stefano Tartaggia
Abstract: Use of substituted spirocyclic sulfonamidocarboxylic acids, -carboxylic esters, -carboxamides and -carbonitriles or salts thereof for enhancement of stress tolerance in plants. The invention relates to the use of spirocyclic sulfonamidocarboxylic acids, -carboxylic esters, -carboxamides and -carbonitriles or salts thereof of the formula (I) in which the respective substituents have the meanings given in the description, for increasing stress tolerance in plants with respect to abiotic stress, and also for increasing plant growth and/or for increasing plant yield.
Type:
Application
Filed:
December 27, 2011
Publication date:
February 6, 2014
Applicant:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Jens Frackenpohl, Lothar Willms, Thomas Müller, Stefan Lehr, Pascal Von Koskull-Döring, Ines Heinemann, Christopher Hugh Rosinger, Isolde Häuser-hahn, Martin Jeffrey Hills
Abstract: This invention relates, e.g., to a compound, aplexone, and pharmaceutically acceptable salts and solvates, and functional variants, thereof. Methods of using the compounds and pharmaceutical compositions comprising them, e.g. to inhibit angiogenesis and to reduce cellular cholesterol levels, are also included.
Type:
Application
Filed:
January 17, 2012
Publication date:
October 31, 2013
Applicant:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Abstract: The present invention describes a process for preparing a cyclooxygenase-2 selective inhibitor. It provides a synthetic procedure for the said substance namely 5-chloro-3-(4-methylsulphonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine of formula (I). The invention also relates to preparation of a new intermediate of formula (IV) and a process to prepare it. Furthermore, the invention describes a process for preparing another key intermediate of formula (II). Compounds of formula (IV) and formula (II) are useful intermediates in synthesis of the said cyclooxygenase-2 inhibitor.
Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.
Abstract: The invention provides novel substituted phenylamino isonicotinamide compounds (I), pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein X, R1, R2, R3, R4, R5 and R6 are as defined in the specification. Said compounds are MEK inhibitors useful in the treatment of hyperproliferative diseases related to the hyperactivity of MEK, such as restenosis, as well as diseases modulated by the MEK cascade, such as cancer and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
Type:
Grant
Filed:
July 27, 2009
Date of Patent:
March 26, 2013
Assignee:
Merck Patent GmbH
Inventors:
Andreas Goutopoulos, Henry Yu, Benny C. Askew, Jr., Lesley Liu-Bujalski
Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2? are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2? together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4? are each independently hydrogen or lower alkyl, or R4 and R4? together form a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
Type:
Application
Filed:
April 11, 2012
Publication date:
October 25, 2012
Inventors:
Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
Abstract: The invention encompasses formulations for increased attachment and retention systems of biologically active organic compounds and methods for the preparation and use thereof.
Abstract: The present invention relates to novel compounds (3-aminopropen-1-ones) useful for binding and imaging beta amyloid deposits and their use in detecting or treating Alzheimer's disease and amyloidosis.
Type:
Application
Filed:
March 26, 2012
Publication date:
September 20, 2012
Applicant:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Ulrike Röhn, Hermann Künzer, Tobias Heinrich, Markus Berger, Damian Brockschnieder, Sabine Krause, Thomas Dyrks, Andrea Thiele, Ursula Mönning, Ulf Bömer
Abstract: A process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methyl sulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib. The synthesis of the intermediates useful for such preparation is also described.
Type:
Application
Filed:
January 11, 2012
Publication date:
September 13, 2012
Inventors:
Andrea Castellin, Paolo Stabile, Francesco Fontana, Ottorino De Lucchi, Andrea Caporale, Stefano Tartaggia
Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
Abstract: The present invention is to provide a compound represented by the general formula (1) exhibiting a high insecticidal effect and an insecticide comprising the compound as an active ingredient. The compound represented by the general formula (1) and an insecticide comprising the compound as an active ingredient, wherein, in the formula, A1, A2, A3 and A4 each represent a carbon atom or the like; R1 and R2 each represent a hydrogen atom or the like; G1 and G2 represent an oxygen atom or the like; Xs each represent a hydrogen atom, a halogen atom or the like; n represents an integer of 0 to 4; Q1 represents a substituted phenyl group, a substituted heterocyclic group or the like; Q2 represents a substituted phenyl group, a substituted heterocyclic group or the like.
Abstract: An essentially nonporous honeycomb substrate having greater than 900 cells per square inch and with a catalyst coating having a thickness less than 1 micron. The coated essentially nonporous honeycomb may be used, for example, for gas phase reactions.
Abstract: New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.
Type:
Grant
Filed:
June 1, 2010
Date of Patent:
November 15, 2011
Assignee:
DAC S.R.L.
Inventors:
Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
Abstract: We disclose agents useful in the treatment of diseases or conditions that would benefit from improved muscle function and including pharmaceutical compositions and diagnostic tests for determining the predisposition of a subject, in particular a male subject, to cardiovascular disease.
Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds (I) pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
Abstract: A compound of formula (I) P—W—C(?X)-L-Q??(I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.
Type:
Grant
Filed:
December 18, 2006
Date of Patent:
May 17, 2011
Assignee:
AstraZeneca AB
Inventors:
Justin Fairfield Bower, Peter Wedderburn Kenny, Jeffrey Philip Poyser
Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein each W and Y is independently CH2, O, C(?O), S(?O)n, NR8 or a direct bond; R4 is H, halogen, cyano, hydroxy, C1-C2 alkyl, C1-C2 haloalkyl, C2 alkenyl, C2 haloalkenyl or C2 alkynyl; m is an integer selected from 0, 1, 2, 3, 4 and 5; and R1, R2, R3, R5, R8 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
Abstract: The present invention is directed toward pyridyl derivatives of formula (I) as antagonists of the mGlu5 receptor.
Type:
Grant
Filed:
March 9, 2005
Date of Patent:
March 29, 2011
Assignee:
Eli Lilly and Company
Inventors:
Francisco Javier Agejas-Chicharro, Bruce Anthony Dressman, Jose Antonio Martinez Perez, James Allen Monn, Mohammad Sadegh Zia-Ebrahimi, Sonia Gutierrez Sanfeliciano, Steven Marc Massey, Steven Scott Henry
Abstract: The present invention relates to, inter alia, the use of a compound capable of inhibiting 4-hydroxyphenylpyruvate dioxygenase (HPPD) in an animal in the manufacture of a medicament for use in the treatment and/or prevention of depression. The invention also provides for the use of a compound capable of inhibiting HPPD in an animal in the manufacture of a medicament for use in the treatment of the withdrawal symptoms associated with an addictive drug which causes dopamine dependant associative learning disorders in said animal. In a particular embodiment said HPPD inhibitor is selected from the group consisting of the compound depicted as compound 1; 2; and 3.22.
Abstract: There is provided compounds of formula (I): wherein Y, ring A, D1, D2, D3, L1, Y1, L2, Y2, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
Type:
Application
Filed:
September 3, 2008
Publication date:
November 11, 2010
Inventors:
Benjamin Pelcman, Peter Nilsson, Martins Katkevics
Abstract: The invention provides a substantially pure amorphous lercanidipine hydrochloride having a purity of at least 95% pure, preferably at least about 97% pure, more preferably at least about 99% pure, and still more preferably at least about 99.5% pure. The invention further relates to methods of preparing substantially pure amorphous lercanidipine, as well as methods of providing rapid relief from hypertension by administering the substantially pure amorphous lercanidipine hydrochloride of the present invention to a patient in need of such treatment.
Abstract: The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in the description.
Type:
Grant
Filed:
February 6, 2009
Date of Patent:
October 12, 2010
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Mirjana Andjelkovic, Agnes Benardeau, Evelyne Chaput, Paul Hebeisen, Matthias Nettekoven, Ulrike Obst Sander, Constantinos G. Panousis, Stephan Roever
Abstract: Provided are dendritic nano-antioxidant compounds according to Formula I, which may further comprise active agents covalently or non-covalently attached. Further provided are compositions comprising the disclosed compounds. Also disclosed are cosmetic compositions and dietary supplements comprising the compounds according to Formula I. The invention additionally provides methods of reducing free radicals or oxidative stress in a cell, a method of treating a subject, and a method of treating a condition comprising administering the compounds according to Formula I.