Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
Type:
Application
Filed:
November 17, 2009
Publication date:
April 1, 2010
Inventors:
Jeffrey Michael Axten, Robert A. Daines, David Thomas Davies, Timothy Francis Gallagher, Graham Elgin Jones, William Henry Miller, Neil David Pearson, Israil Pendrak
Abstract: Physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
Type:
Application
Filed:
July 21, 2009
Publication date:
February 18, 2010
Applicant:
PROBIODRUG AG
Inventors:
Torsten Hoffmann, Stephan Schilling, Andre J. Niestroj, Hans-Ulrich Demuth, Ulrich Heiser, Mirko Buchholz
Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
Type:
Application
Filed:
April 2, 2008
Publication date:
February 11, 2010
Applicant:
Anadys Pharmaceuticals, Inc.
Inventors:
Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich, Yuefen Zhou, Lijian Chen, David Kucera, Fritz Blatter, Martin Viertelhaus
Abstract: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.
Abstract: The invention relates to compounds of formula (I) wherein R0 represents H or OH; R1 represents alkoxy; U and W represent N, V represents CH and R2 represents H or F, or U and V represent CH, W represents N and R2 represents H or F, or U and V represent N, W represents CH and R2 represents H, or U represents N. V represents CH, W represents CRa and R2 represents H; Ra represents CH2OH or alkoxycarbonyl; A represents the group CH?CH—B or a binuclear heterocyclic system D, B representing a mono- or di-substituted phenyl group wherein the substituents are halogen atoms and D representing one of the following groups wherein Z represents CH or N, and Q represents O or S; and to salts of such compounds. These compounds are useful as antibacterial agents.
Type:
Application
Filed:
December 21, 2007
Publication date:
February 4, 2010
Applicant:
Actelion Pharmaceuticals Ltd.
Inventors:
Christian Hubschwerlen, Georg Rueedi, Jean-Phillippe Surivet, Cornelia Zumbrunn
Abstract: The present invention relates to extended benzamide derivatives of the general formula I, to processes for preparation thereof and to use thereof for production of pharmaceutical compositions for treatment of disorders and indications associated with the EP2 receptor.
Type:
Application
Filed:
July 24, 2009
Publication date:
February 4, 2010
Applicant:
Bayer Schering Pharma AG
Inventors:
Marcus Kopitz, Bernhard Lindenthal, Antonius Ter Laak, Tim Wintermantel, Olaf Peters, Gernot Langer, Nico Braeuer, Bernd Buchmann
Abstract: Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
Type:
Grant
Filed:
August 2, 2005
Date of Patent:
February 2, 2010
Assignee:
Glaxo Group Limited
Inventors:
William Henry Miller, Mark Andrew Seefeld
Abstract: Compounds characterized by thiolactone or thiomorpholino cores display useful antibiotic and radioprotective properties. The latter properties are believed to arise from an ability of the compounds to inhibit proteins involved in apoptosis.
Abstract: A medicine which contains as an active ingredient a benzothiazin-3-one-compound represented by the formula (1): (wherein n is 3 or 4; R represents ethyl or hydrogen; and R1 represents hologeno, alkoxy, haloalkyl, or haloalkoxy) or a pharmaceutically acceptable salt thereof. It is useful as a therapeutic or preventive agent for arthrosis deformans, chondrodegenerative discases such as chronic articular rheumatism, cancers, gingivitis, etc. Also provided are an intermediate for the compound and a process for producing the compound.
Abstract: The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.
Type:
Application
Filed:
July 6, 2009
Publication date:
January 14, 2010
Inventors:
Jailall Ramnauth, Subhash C. Annedi, Sarah Silverman, Peter Dove, Shawn Maddaford, Suman Rakhit
Abstract: The present invention relates to pyridin-3-yl pyridin-3-amine compounds and derivatives thereof having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Application
Filed:
January 29, 2007
Publication date:
January 7, 2010
Inventors:
Mark T. Bilodeau, Jacob M. Hoffman, M. Brad Nolt
Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
Type:
Grant
Filed:
June 23, 2008
Date of Patent:
December 29, 2009
Assignee:
Wyeth
Inventors:
An Thien Vu, Paige Erin Mahaney, Stephen Todd Cohn
Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
Type:
Application
Filed:
September 4, 2007
Publication date:
December 24, 2009
Inventors:
Konrad Honold, Wolfgang Schaefer, Stefan Scheiblich
Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed.
Type:
Application
Filed:
December 28, 2005
Publication date:
December 17, 2009
Inventors:
Werner Breitenstein, Takeru Ehara, Claus Ehrhardt, Philipp Grosche, Yuko Hitomi, Yuki Iwaki, Takanori Kanazawa, Kazuhide Konishi, Juergen K. Maibaum, Keiichi Masuya, Atsuko Nihonyanagi, Nils Ostermann, Masaki Suzuki, Atsushi Toyao, Fumiaki Yokokawa
Abstract: A pharmaceutical composition comprising losartan and pharmaceutically acceptable salts thereof and a process of forming the same. The pharmaceutical composition of losartan comprises an active agent comprising an effective amount of losartan or its pharmaceutical salt thereof, and pharmaceutically acceptable additives, wherein d(0.9) of losartan is less than 50? and/or specific surface area is more than 0.6 m2/gm. The process of preparation of pharmaceutical composition of losartan, comprises the steps of blending the losartan having d(0.9) less than 50? and/or specific surface area more than 0.6 m2/gm, with the other intragranular excipients, dry compression, milling and screening to obtain granules, said granules being subsequently blended with extragranular excipients and compressed to tablets which is further coated.
Abstract: The present invention relates to novel substituted aralkyl derivatives of the general formula (I) and (IIIa), their derivatives, their analogs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, pharmaceutical compositions containing them, use of these compounds in medicine and the intermediates involved in their preparation.
Type:
Application
Filed:
July 8, 2009
Publication date:
November 5, 2009
Applicant:
CADILA HEALTHCARE LIMITED
Inventors:
Braj B. Lohray, Vidya B. Lohray, Mukul R. Jain, Sujay Basu, Harikishore Pingali, Saurin K. Raval, Preoti S. Raval
Abstract: The invention relates to compounds of formula (I) wherein R1 represents H, alkyl, alkoxy, cyano or halogen; one of U and X represents CH or N and the other represents CH, or, in the case of U, may also represent CRa and, in the case of X, may also represent CRb; Ra represents halogen; Rb represents halogen or alkoxy; B represents N, D represents CH2 and A represents CH(OH)CH2 or CH2CH2, or B represents CH, D represents CH2 or O and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH?CH, CH2CH2 Or NHCO, or also B represents C(OH), D represents CH2 and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH?CH, CH2CH2 Or NHCO; R2 represents H, alkyl, alkenyl, hydroxyalkyl or alkoxycarbonylalkyl; and E represents naphthyl or a binuclear heterocyclic group; and to salts of such compounds. These compounds are useful as antimicrobial agents.
Type:
Application
Filed:
August 29, 2007
Publication date:
October 29, 2009
Applicant:
Actelion Pharmaceuticals Ltd.
Inventors:
Christian Hubschwerlen, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
Abstract: Bicyclic nitrogen containing compounds and their use as antibacterials.
Type:
Application
Filed:
July 18, 2007
Publication date:
October 29, 2009
Inventors:
Llius Ballell, David Barros, Gerald Brooks, Julia Castro Pichel, Steven Dabbs, Robert A. Daines, David Thomas Davies, Jose Maria Fiandor Roman, Israil Pendrak, Modesto J. Remuinan Blanco, Jason Anthony Rossi, Ilaria Giordano, Alan Joseph Hennessy, James B. Hoffman, Graham Elgin Jones, Timothy James Miles, Neil David Pearson, Lihua(lily) Zhang
Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
Type:
Application
Filed:
June 23, 2009
Publication date:
October 15, 2009
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Matthias ECKHARDT, Norbert HAUEL, Elke LANGKOPF, Frank HIMMELSBACH, Iris KAUFFMANN-HEFNER, Mohammad TADAYYON, Michael MARK
Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.
Type:
Application
Filed:
December 27, 2006
Publication date:
October 8, 2009
Inventors:
Shoji Fukumoto, Nobuyuki Matsunaga, Taiichi Ohra, Norio Ohyabu, Tomoaki Hasui, Takashi Motoyaji, Christopher Stephen Siedem, Tony Pisal Tang, Lisa A. Demeese, Cassandra Gauthier
Abstract: A medicine which contains as an active ingredient a benzothiazin-3-one-compound represented by the formula (1): (wherein n is 3 or 4; R represents ethyl or hydrogen; and R1 represents hologeno, alkoxy, haloalkyl, or haloalkoxy) or a pharmaceutically acceptable salt thereof. It is useful as a therapeutic or preventive agent for arthrosis deformans, chondrodegenerative discases such as chronic articular rheumatism, cancers, gingivitis, etc. Also provided are an intermediate for the compound and a process for producing the compound.
Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Type:
Grant
Filed:
September 12, 2002
Date of Patent:
September 29, 2009
Assignee:
MethylGene, Inc.
Inventors:
Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
Abstract: The present invention provides a salt form, and compositions thereof, useful as a modulator of one or more GPCRs and which exhibits desirable characteristics for the same. The present invention also provides methods for preparing said salt form.
Type:
Grant
Filed:
September 12, 2006
Date of Patent:
September 29, 2009
Assignee:
Solvay Pharmaceuticals, B.V.
Inventors:
Subodh S. Deshmukh, Kadum Ali, Christopher R. Diorio, Eric C. Ehrnsperger, Mahdi B. Fawzi, Syed Muzafar Shah, Mahmoud Mirmehrabi
Abstract: The present invention relates to novel benzothiazin derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria. The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance.
Type:
Application
Filed:
May 24, 2006
Publication date:
September 24, 2009
Inventors:
A. Vadim Makarov, Stewart T. Cole, Ute Möllmann
Abstract: The invention relates, in general, to new formulations and dosage units containing losartan and/or its salts (e.g., losartan potassium) that are useful for the therapeutic treatment (including prophylactic treatment) of mammals, including humans, and a process for making the same. The process generally includes (i) mixing and blending losartan potassium and a first portion of at least one of pre-gelatinized starch, microcrystalline cellulose and magnesium stearate to the mixture of step (i); (ii) compacting the mixture obtained in step (i) to form an agglomerate; (iii) breaking apart the agglomerate in order to obtain a granulate; (iv) adding lactose monohydrate and a second portion of at least one of pre-gelatinized starch, microcrystalline cellulose and magnesium stearate to the granulate and blending; and (v) tableting the granulate mixture into tablets. The process can further include coating the prepared tablets with a suitable coating material.
Abstract: The invention provides pteridine compounds of formula (I), processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. Formula (I) in which A is a group of formula (a) or (b).
Type:
Grant
Filed:
July 15, 2004
Date of Patent:
August 25, 2009
Assignee:
AstraZeneca
Inventors:
Roger Bonnert, Stewart Gardiner, Fraser Hunt, Iain Walters
Abstract: An antimicrobial additive composition is provided which economically and efficiently imparts antimicrobial characteristics to acrylic polymers, and particularly thermoformable acrylic sheets made from such polymers. The antimicrobial composition comprises an alkyl dimethyl ammonium saccharinate, an oxathiazine, an azole, an isothiazoline, a chlorothalonil, and/or mixtures thereof, among others.
Abstract: 1H-Pyrrolo-1,4-thiazines and a process for the preparation thereof are described. These compounds are useful as enzyme inhibitors in cells, particularly for medical uses.
Type:
Grant
Filed:
September 6, 2006
Date of Patent:
August 25, 2009
Assignee:
Board of Trustees of Michigan State University
Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
Type:
Grant
Filed:
May 3, 2006
Date of Patent:
August 18, 2009
Assignee:
Acadia Pharmaceuticals, Inc.
Inventors:
Niels Skjaerbaek, Kristian Norup Koch, Bo Lennart Mikael Friberg, Bo-Ragnar Tolf
Abstract: Novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R1, R1?, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
Type:
Application
Filed:
April 12, 2007
Publication date:
July 30, 2009
Applicant:
SPEEDEL EXPERIMENTA AG
Inventors:
Peter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Christiane Marti, Stjepan Jelakovic, Bibia Bennacer, Stefan Stutz
Abstract: The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof in which R, R1, R2, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
Type:
Application
Filed:
April 12, 2007
Publication date:
July 30, 2009
Applicant:
SPEEDEL EXPERIMENTA AG
Inventors:
Peter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Stjepan Jelakovic, Stefan Stutz
Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
Type:
Application
Filed:
January 21, 2009
Publication date:
July 23, 2009
Inventors:
Corey Don Anderson, Andreas P. Termin, Pramod Joshi, Sara S. Hadida Ruah, Daniele Bergeron, Sanghee Yoo
Abstract: Naphthyridine and quinoline derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
Type:
Application
Filed:
March 26, 2009
Publication date:
July 16, 2009
Inventors:
William Henry Miller, Meagan B. Rouse, Mark Andrew Seefeld
Abstract: The invention relates to 3-pyridylcarboxamide derivatives of formula (I): wherein the various symbols are as defined in the description, compositions thereof, methods for controlling pests by applying same, and processes for their preparation.
Type:
Grant
Filed:
May 6, 2003
Date of Patent:
July 14, 2009
Assignee:
Merial Limited
Inventors:
Koichi Araki, Tetsuya Murata, Koshi Gunjima, Norihiko Nakakura, Eiichi Shimojo, Dale Robert Mitchell, Henricus Maria Martinus Bastiaans, David Stephen Carver, Daniel Allen, Christian Arnold, Waltraud Hempel, Olga Malsam, Jutta Maria Waibel
Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
Abstract: The present invention relates to method of reversing left ventricle remodeling by combined administration of therapeutically effective amounts ranolazine and at least one co-remodeling agent, which may be an ACE inhibitor, an ARB, or a beta-blocker. The method finds utility in the treatment of heart failure. This invention also relates to pharmaceutical formulations that are suitable for such combined administration.
Abstract: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.
Abstract: The invention relates to substituted 3,4- or higher substituted piperididine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds preferably have the formula I, wherein the moieties R1, R2, R11 and W are as defined in the specification.
Abstract: The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
Abstract: Compounds having the formula Ia or Ib wherein R1, R2, R3 and R4 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
Type:
Grant
Filed:
February 15, 2007
Date of Patent:
May 12, 2009
Assignee:
Roche Palo Alto LLC
Inventors:
Jay Bradford Fell, Peter Mohr, Peter J. Stengel
Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
Type:
Application
Filed:
December 10, 2008
Publication date:
April 9, 2009
Applicant:
BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
Inventors:
Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ