Abstract: Novel ligand compounds having the structural formula (I): in which: Ar is a radical selected from among the radical of formulae (a) to (c) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, or, alternatively, into cosmetic compositions.
Abstract: A PEPCK inhibitor can include identifying a molecule that has a size capable of fitting into and interacting with the PEPCK binding site and at least one of the following: (a) a first terminal substituent having co-planar atoms acting as metal ligands to the active site metal ion PEPCK; (b) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent includes a neutral carbon center or include an oxygen, sulfur, selenium, or other atom with similar physiochemical properties; (c) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent is devoid of an electropositive atom or substituents; or (d) a second terminal substituent opposite of the first terminal substituent, said second terminal substituent having an atom that is a hydrogen boding acceptor and/or is negatively charged.
Type:
Application
Filed:
July 12, 2010
Publication date:
January 13, 2011
Inventors:
Gerald Carlson, Todd Holyoak, Sarah Sullivan, Rose Mary Stiffin
Abstract: A method for producing a compound represented by the formula (I) the method comprising reacting in the presence of a condensation agent a compound represented by the formula (II) or a salt thereof with a compound represented by the formula (III) wherein R1 represents a 4-(4-methylpiperadin-1-yl) group or 3-hydroxyazetidin-1-yl group, R2, R3, R4 and R5 may be the same or different and each represents a hydrogen atom or a fluorine atom and R6 represents a hydrogen atom or a fluorine atom.
Abstract: The present invention relates to the use of aminoazoline and urea derivatives for com-bating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds and to specific azoline and urea derivatives.
Type:
Application
Filed:
May 23, 2008
Publication date:
November 25, 2010
Applicant:
BASF SE
Inventors:
Christopher Koradin, Markus Kordes, Ernst Baumann, Ronan Le Vezouet, Deborah L. Culbertson
Abstract: The present invention relates to novel 2-phenoxy-6-phenyl- and 2-phenoxy-6-pyridylnicotinic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis and heart failure.
Abstract: This invention relates to protein kinase inhibitors useful for treating cancers. The present protein kinase inhibitors are those having the structures of the following formula or pharmaceutically acceptable salts thereof. The present compounds can be used to treat protein kinase related diseases such as cancers.
Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
Type:
Application
Filed:
April 27, 2010
Publication date:
November 11, 2010
Applicant:
Abbott GmbH & Co. KG
Inventors:
Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger
Abstract: The present invention relates to dihydropyridine mineralocorticoid receptor modulating compounds having the structure: and their use in treating cardiovascular events.
Type:
Application
Filed:
December 10, 2008
Publication date:
October 14, 2010
Inventors:
Philip E. Brandish, Mark E. Fraley, James C. Hershey, Justin T. Steen
Abstract: The present invention provides a black pigment consisting of an oxonol compound having a mean particle diameter ranging from 0.01 to 10.0 micrometers, and a black pigment dispersion and a black resin composition comprising the black pigment.
Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
Type:
Grant
Filed:
June 26, 2007
Date of Patent:
October 12, 2010
Assignee:
Warner Chilcott Company, LLC
Inventors:
Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Type:
Application
Filed:
January 7, 2010
Publication date:
September 30, 2010
Applicant:
SANOFI-AVENTIS
Inventors:
Henning STEINHAGEN, Hauke SZILLAT, Markus FOLLMANN, Reinhard KIRSCH, Volkmar WEHNER, Hans MATTER, Martin LORENZ, Kent W. Neuenschwander, Anthony C. SCOTESE
Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
Type:
Application
Filed:
May 28, 2010
Publication date:
September 23, 2010
Inventors:
Lawrence M. Blatt, Scott D. Seiwert, Leonid Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
Abstract: The present invention relates to a method for identifying a compound capable of modulating an anxiety or depression disorder comprising the steps of: (a) contacting a composition comprising a B-Raf protein or a B-Raf gene in expressible form or a transcript thereof with a compound under conditions that allow for an interaction of the B-Raf protein or the B-Raf gene or a transcript thereof and the compound; and (b) measuring whether said interaction, if any, results in (i) a change of B-Raf kinase activity compared to B-Raf kinase activity in the absence of said compound; (ii) a modulation of the expression of the B-Raf gene compared to B-Raf gene expression in the absence of said compound; or (iii) the formation of a complex between the compound and the B-Raf protein, wherein such a change in activity, modulation of expression or the formation of a complex is indicative of the compound being a modulator of an anxiety or depression disorder.
Abstract: The invention relates to substituted nicotinamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.
Type:
Application
Filed:
March 10, 2010
Publication date:
September 16, 2010
Applicant:
GRÜNENTHAL GMBH
Inventors:
Sven Kühnert, Beatrix Merla, Gregor Bahrenberg, Wolfgang Schröder
Abstract: The present application relates to novel substituted 6-phenylnicotinic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders, in particular dyslipidaemias, arteriosclerosis and heart failure.
Type:
Application
Filed:
August 26, 2008
Publication date:
September 16, 2010
Applicant:
BAYER ANIMAL HEALTH GMBH
Inventors:
Lars Baerfacker, Barbara Albrecht-Kuepper, Peter Kolkhof, Yolanda Cancho Grande, Adam Nitsche, Heinrich Meier, Carsten Schmeck, Jens Schamberger, Klemens Lustig
Abstract: A pyridone derivative represented by Formula [1] or an agriculturally acceptable salt thereof: wherein R1 is a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or the like; R2 and R3 are each independently a hydrogen atom, a nitro group, a cyano group, or the like; and A is a group represented by Formula A-1, Formula A-2, Formula A-3, Formula A-4, or Formula A-5: The compounds represented by general formula [1] control various weeds growing in upland fields, orchards, paddy fields, and non-crop lands while showing high safety to useful plants and crops.
Type:
Application
Filed:
January 31, 2007
Publication date:
September 2, 2010
Applicants:
Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
Abstract: The present invention relates to compositions comprising 1,2-dihydropiridin-2-one compounds and an immunoregulatory or anti-inflammatory agent. The compositions are useful for the prevention or the treatment of neurodegenerative diseases, for example demyelinating disorders.
Abstract: The present invention relates to 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide monohydrate, to processes for its preparation, to pharmaceutical compositions comprising it and to its use in the control of disorders.
Abstract: The invention discloses an improved process for producing an intermediate to produce large quantity of 2-(Phenyl methyl thio)-3-pyridine carboxylic acid. The process comprises reacting 2-chloro-3-cyanopyridine with benzyl mercaptan in presence of a base and an aprotic solvent. The resulting intermediate 2-(phenyl methyl thio)-3-cyanopyridine is hydrolyzed in presence of a base in an autoclave and isolated under acidic condition to get the desired product.
Abstract: The present invention relates to novel 4-phenoxy-6-phenyl- and 4-phenoxy-6-pyridylnicotinic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis and heart failure.
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
Type:
Application
Filed:
December 15, 2009
Publication date:
June 24, 2010
Inventors:
Jacob Berger, Joan Marie Caroon, Francisco Javier Lopez-Tapia, Dov Nitzan, Keith Adrian Murray Walker, Shu-Hai Zhao
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
Type:
Application
Filed:
December 15, 2009
Publication date:
June 24, 2010
Inventors:
Jacob Berger, Joan Marie Caroon, Nancy Elisabeth Krauss, Keith Adrian Murray Walker, Shu-Hai Zhao, Francisco Javier Lopez-Tapia
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
Type:
Application
Filed:
December 15, 2009
Publication date:
June 24, 2010
Inventors:
Christine E. Brotherton-Pleiss, Joan Marie Caroon, Francisco Javier Lopez-Tapia
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
Type:
Application
Filed:
December 14, 2009
Publication date:
June 24, 2010
Inventors:
Francisco Javier Lopez-Tapia, Keith Adrian Murray Walker, Shu-Hai Zhao
Abstract: Disclosed is a plant disease control agent containing an amide compound represented by formula (1) below which has an excellent plant disease controlling effect as an active ingredient. (In the formula, X1, X2, Z1 and E1 are as defined in the description.
Abstract: The present invention relates to pharmaceutical compositions for treating virus infections and/or diseases caused thereby comprising 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide optionally combined with at least one additional therapeutic agent.
Abstract: The present invention relates to the polymorph II of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, to processes for its preparation, to pharmaceutical compositions comprising it and to its use in the control of disorders.
Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
March 9, 2008
Publication date:
April 29, 2010
Inventors:
Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
Abstract: A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HTV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other anti-HIV integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described. Compounds of the present application include those of formula I and include tautomers, regioisomers, geometric isomers, and pharmaceutically acceptable salts thereof, wherein the pyridinone scaffold and R groups are as otherwise defined in the specification.
Type:
Application
Filed:
July 13, 2007
Publication date:
April 15, 2010
Applicant:
THE UNIVERSITY OF GEORGIA RESEARCH FOUNDATION
Inventors:
Vasu Nair, Byung I. Seo, Vinod R. Uchil, Guochen Chi
Abstract: Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with pyridinic compounds to produce functionalized pyridinic compounds.
Type:
Application
Filed:
December 18, 2009
Publication date:
April 15, 2010
Inventors:
Christopher J. Woltermann, Douglas E. Sutton
Abstract: The invention relates to a process for the preparation of pyridylcarboxylic amides and esters I, Formula (I) wherein Hal, X and R1 have the meanings given in claim 1, which comprises the following steps: (a) heating a mixture consisting essentially of trichloromethylpyridine II, Formula (II), wherein Hal has the meaning given, and 1.0 to 1.5 equivalents of concentrated sulfuric acid, characterized in that the trichloromethylpyridine II in a liquid form is added to the concentrated sulfuric acid at a temperature from 110° C. to 160° C.; and (b) reacting the intermediate product obtained in step (a) with an amine or alcohol III, HXR1, wherein X and R1 have the meaning given, optionally in the presence of a solvent and/or a base.
Type:
Grant
Filed:
October 26, 2006
Date of Patent:
April 6, 2010
Assignee:
BASF SE
Inventors:
Monika Brink, Marcus Knell, Jan Hendrik Wevers
Abstract: A compound of general formula (I): A process for preparing this compound. An intermediate of general formula (II) for the preparation of a compound of general formula (I). A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
Type:
Grant
Filed:
April 25, 2005
Date of Patent:
March 30, 2010
Assignee:
Bayer Cropscience S.A.
Inventors:
Pierre-Yves Coqueron, Darren James Mansfield, Philippe Desbordes, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Pierre Genix, Alain Villier
Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.
Type:
Application
Filed:
December 1, 2009
Publication date:
March 25, 2010
Inventors:
Jacques DUMAS, Wendy Lee, Yuanwei Chen, Lila Adnane, William J. Scott, Sharad Verma, Jianqing Chen, Zhi Chen, Lin Yi
Abstract: The present invention relates to the polymorph III of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, to processes for its preparation, to pharmaceutical compositions comprising it and to its use in the control of disorders.
Abstract: A compound represented by the formula (I): wherein R1 is lower alkyl, cycloalkyl or aromatic hydrocarbon ring, each of which is optionally substituted with one or more substituents; R2 is hydrogen atom, halogen atom, lower alkyl, halo(lower)alkyl or lower alkoxy; and R3 is (1) a group represented by the formula: wherein R4 is lower alkyl, etc.; (2) a group represented by the formula: wherein R5 is lower alkyl, etc.; (3) a group represented by the formula: wherein R6 is lower alkyl, etc.; or (4) a group selected from halogen atom, carboxy, hydroxy and lower alkoxy, or a salt thereof.
Abstract: The present disclosure provides compounds having the general structure A or pharmaceutically acceptable salts thereof: R—X??(A) wherein R is an alkyl or aryl moiety comprising heterocyclic structures; and X is a metal-chelatin group selected from: This disclosure further provides a focused library of compounds for use in the discovery and design of metallo-enzyme inhibitors. This fragment-based approach provides an assembly of a library of low molecular weight compounds (MW<300 Da) containing a variety of potential metal-chelating groups. The identification of the inhibitory scaffolds among these compounds provides the initial hit fragments that may be optimized for affinity against a particular target using common medicinal chemistry, structure-based or NMR-based approaches.
Type:
Application
Filed:
August 14, 2009
Publication date:
February 18, 2010
Applicants:
BURNHAM INSTITUTE FOR MEDICAL RESEARCH, THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Abstract: Compounds of formula (I): wherein variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are described.
Type:
Application
Filed:
July 26, 2007
Publication date:
January 28, 2010
Inventors:
William McCoull, Martin Packer, James Stewart Scott, Paul Robert Owen Whittamore
Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
Type:
Application
Filed:
June 10, 2009
Publication date:
December 31, 2009
Applicant:
Emisphere Technologies, Inc.
Inventors:
Donald J. Sarubbi, Eugene N. Barantsevitch
Abstract: Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with pyridinic compounds to produce functionalized pyridinic compounds.
Type:
Grant
Filed:
October 10, 2006
Date of Patent:
December 29, 2009
Assignee:
FMC Corporation Lithium Division
Inventors:
Christopher J. Woltermann, Douglas E. Sutton
Abstract: The present invention relates to methylene urea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
Type:
Application
Filed:
June 19, 2009
Publication date:
December 3, 2009
Applicant:
Merck Patent GmbH
Inventors:
Hans-Peter Buchstaller, Matthias Wiesner, Oliver Schadt, Christiane Amendt, Frank Zenke, Christian Sirrenberg, Matthias Grell, Dirk Finsinger
Abstract: This invention pertains to the discovery of a novel family of thiolesters and uses thereof. Also provided for are viricidal compounds and pharmaceutical formulations comprising these novel thiolesters. The invention also provides thiolester-inactivated viruses and thiolester-complexed viral proteins.
Type:
Grant
Filed:
December 16, 2003
Date of Patent:
December 1, 2009
Inventors:
James A. Turpin, Yongsheng Song, Ettore Appella, John K. Inman, David G. Covell, William G. Rice, Anders Wallqvist, Andrew Maynard, Mingjun Huang
Abstract: Methods for the synthesis of the N-carbamoyl imidazole (I) and its 1:1 adduct with imidazole are provided. Methods for the preparation of these crystalline intermediates in a high state of purity are also provided. These intermediates react cleanly under mild conditions to produce sorafenib in high yield and purity, without generating difficult-to-remove impurities.
Type:
Application
Filed:
March 5, 2009
Publication date:
October 8, 2009
Inventors:
Pierluigi Rossetto, Peter Lindsay MacDonald, Augusto Canavesi
Abstract: The invention relates to medicine, in particular to mono- and divalent salts of N-(5-hydroxynicotinoil)-L-glutaminic acid exhibiting psychotropic antidepressant, anxiolytic, heroprotective, neuroprotective, antihypoxia cerebroprotective and nootropic action. The novel compounds differ from the known preparations, including the closest prior art in the form of a N-(5-hydroxynicotinoil)-L-glutaminic acid base (nooglucotyl), in that they produce psychotropic effects, namely antidepressant, anxiolytic, neuroprotective and heroprotective actions, in such a way that lesion focuses caused by apoplectic attacks are reduced and age-specific neurological deficiencies and intellectual and physical work capacities are improved.
Type:
Application
Filed:
June 6, 2007
Publication date:
September 24, 2009
Applicant:
OBSCHESTVO S OGRANICHENNOY OTVESTVENNOSTYU " NATSIONALNAYA ISSLEDOVATELSKAYA KOMPANIYA"
Inventors:
Pavel Vasilyevich Yakimuk, Sergey Vitalyevich Stovbun, Alexandr Anatolyevich Litvin
Abstract: The present invention relates to methylene urea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
Type:
Grant
Filed:
October 8, 2003
Date of Patent:
September 15, 2009
Assignee:
Merck Patent GmbH
Inventors:
Hans-Peter Buchstaller, Matthias Wiesner, Oliver Schadt, Christiane Amendt, Frank Zenke, Christian Sirrenberg, Matthias Grell, Dirk Finsinger
Abstract: The present invention is directed to substituted pyridines, methods for their preparation and methods for their use in the treatment and/or prevention of mast cell related conditions.
Type:
Grant
Filed:
October 31, 2005
Date of Patent:
September 8, 2009
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Ankush Argade, David Carroll, Alexander B. Rossi
Abstract: The invention concerns a method for preparing compounds of general formula (I) wherein: n, Q1, Q2, X1, X2, Y and Z are as defined in the description.
Type:
Grant
Filed:
January 8, 2001
Date of Patent:
July 14, 2009
Assignees:
Bayer Cropscience SA, Aventis Pharma SA
Inventors:
Eric Bacque, Jean-Pierre Vors, Francisco Nieto-Roman, Alain Villier, William Henri Barriere, legal representative, Nathalie Hélène Barriere, legal representative, Jean-Claude Barriere