Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/298)
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Publication number: 20120157476Abstract: The present invention relates to compounds of the formula wherein A1 to A3 and R1 to R9 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: December 8, 2011Publication date: June 21, 2012Inventors: Paul Hebeisen, Stephan Roever
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Publication number: 20120149735Abstract: The present invention relates to 1,4-dihydropyridine derivatives of the formula (I) and their uses in the treatment and/or prevention of diseases and disorders directly or indirectly associated with the modification (increase or decrease) of the activity of the cannabinoid receptor 2 (CB2).Type: ApplicationFiled: May 19, 2010Publication date: June 14, 2012Applicants: CENTRE HOSPITALIER REGIONAL UNIVERSITAIRE DE LILLE, UNIVERSITE LILLE 2 DROIT ET SANTEInventors: Regis Millet, Jamal El Bakali, Philippe Chavatte, Nicolas Renault, Didier Lambert, Giulo Muccioli, Mathilde Body-Malapel, Pierre Desreumaux
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Publication number: 20120122784Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.Type: ApplicationFiled: May 26, 2010Publication date: May 17, 2012Applicant: LEO PHARMA A/SInventors: Bjarne Nørremark, Lars Kristian Albert Blæhr, Anne Eeg Knapp, Kristoffer Månsson
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Patent number: 8173684Abstract: 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.Type: GrantFiled: May 2, 2008Date of Patent: May 8, 2012Assignees: Astellas Pharma Inc., Wakunaga Pharmaceutical Co., Ltd.Inventors: Chiyoshi Kasahara, Hitoshi Yamazaki
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Publication number: 20120101261Abstract: A multi-kinase inhibitor, in particular Sorafenib, is used for the preparation of a pharmaceutical composition in the treatment of a variety of pathological conditions involving vascular hyperpermeability in order to reduce vascular hyperpermeability.Type: ApplicationFiled: April 15, 2009Publication date: April 26, 2012Applicant: Fondazione IRCCS Istituto Nazionale Dei TumoriInventors: Alessandro Massimo Gianni, Carmelo Carlo-Stella
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Publication number: 20120101282Abstract: The present invention relates to a process for the preparation of nicotinamide derivatives of formula I, wherein R1 to R7 are as defined above and to pharmaceutically acceptable salts thereof. The compounds of formula I are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of cannabinoid 1 receptors (CB1 receptors) as described in the PCT Publ. WO 2006/106054.Type: ApplicationFiled: October 12, 2011Publication date: April 26, 2012Inventors: Pascal Dott, Pius Waldmeier
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Patent number: 8163929Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, R1, R2, R3, R4, R5 and R6 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: GrantFiled: December 15, 2009Date of Patent: April 24, 2012Assignee: Roche Palo Alto LLCInventors: Jacob Berger, Christine E. Brotherton-Pleiss, Francisco Javier Lopez-Tapia, Keith Adrian Murray Walker, Shu-Hai Zhao
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Publication number: 20120094998Abstract: The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer.Type: ApplicationFiled: April 19, 2010Publication date: April 19, 2012Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Wen Zhang
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Patent number: 8153809Abstract: 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: GrantFiled: December 15, 2009Date of Patent: April 10, 2012Assignee: Roche Palo Alto LLCInventors: Christine E. Brotherton-Pleiss, Joan Marie Caroon, Francisco Javier Lopez-Tapia, Dov Nitzan, Keith Adrian Murray Walker
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Patent number: 8143242Abstract: 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: GrantFiled: January 7, 2010Date of Patent: March 27, 2012Assignee: Sanofi-AventisInventors: Henning Steinhagen, Hauke Szillat, Markus Follmann, Reinhard Kirsch, Volkmar Wehner, Hans Matter, Martin Lorenz, Kent W. Neuenschwander, Anthony C. Scotese
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Publication number: 20120059004Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.Type: ApplicationFiled: February 16, 2011Publication date: March 8, 2012Applicant: CANTHERA THERAPEUTICS, INC.Inventors: PETER ELLIOTT, ANNA MANDINOVA, MICHAEL ANDREW FOLEY, ROBERT GOULD, SAM LEE
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Patent number: 8124630Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: GrantFiled: November 27, 2001Date of Patent: February 28, 2012Assignee: Bayer Healthcare LLCInventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Reina Natero
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Patent number: 8124782Abstract: The present invention relates to a process for preparing 4-{4-[({[4-chloro-3-(trifluoro-methyl)phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine-2-carboxamide and its tosylate salt.Type: GrantFiled: September 20, 2005Date of Patent: February 28, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Michael Lögers, Reinhold Gehring, Oliver Kuhn, Mike Matthäus, Klaus Mohrs, Matthias Müller-Gliemann, Jürgen Stiehl, Mathias Berwe, Jana Lenz, Werner Heilmann
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Patent number: 8101638Abstract: A compound of the formula (I) or a pharmaceutically acceptable salt, enantiomer, racemate, diasteromers or mixtures thereof, or a solvate thereof, formulations and methods of use thereof, as opioid receptor antagonists are disclosed wherein the variables are as described herein.Type: GrantFiled: July 8, 2008Date of Patent: January 24, 2012Assignee: Eli Lilly and CompanyInventors: Miles Goodman Siegel, Russell Dean Stucky, Kumiko Takeuchi
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Patent number: 8097624Abstract: The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2R5N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups.Type: GrantFiled: May 9, 2008Date of Patent: January 17, 2012Assignee: Apotex Inc.Inventors: Tim Fat Tam, Michael Spino, Wanren Li, Yingsheng Wang, Yanqing Zhao, Birenkumar Hasmukhbhai Shah
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Publication number: 20120004244Abstract: There is provided compounds of formula I, wherein E1, E2a, E2b, E2c, E4, D1, D2, D3, L1, Y1, L2 and Y2 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: ApplicationFiled: March 12, 2010Publication date: January 5, 2012Applicant: BIOLIPOX ABInventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics
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Publication number: 20120004349Abstract: The present invention provides a liquid curable epoxy resin composition that has excellent storage stability and curing properties and provides a cured product having excellent properties, particularly, excellent organic solvent resistance. For that purpose, a clathrate containing a carboxylic acid compound and at least one selected from the group consisting of an imidazole compound represented by formula (I), wherein R1 to R4 each represent a hydrogen atom or the like, and 1,8-diazabicyclo[5.4.0]undecene-7 (DBU) is mixed in an epoxy resin. The liquid curable epoxy resin composition uses a liquid epoxy resin or an organic solvent.Type: ApplicationFiled: March 9, 2010Publication date: January 5, 2012Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya
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Patent number: 8076487Abstract: 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: GrantFiled: January 31, 2007Date of Patent: December 13, 2011Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Fumiaki Takabe, Shunichirou Fukumoto, Ryu Kajiki, Sohei Asakura, Ryohei Ueno, Masami Kobayashi, Satoru Takahashi, Norihisa Yonekura, Ryo Hanai, Takashi Mitsunari
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Patent number: 8076488Abstract: 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: GrantFiled: March 1, 2004Date of Patent: December 13, 2011Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, Stephen Boyer, Sharad Verma, Lila Adnane, Yuanwei Chen, Wendy Lee, Barton Phillips, Roger A. Smith, William J. Scott, Jennifer Burke, Jianqing Chen, Zhi Chen, Jianmei Fan, Karl Miranda, Brian Raudenbush, Aniko Redman, Jianxing Shao, Ning Su, Gan Wang, Lin Yi, Qingming Zhu
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Publication number: 20110294837Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-6, L1, R1, R4-6 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds and methods of treating disease states related to the activity of Aurora kinase.Type: ApplicationFiled: August 7, 2009Publication date: December 1, 2011Inventors: Holly L. Deak, Brian L. Hodous, Jason B. Human, Hanh Nho Nguyen, Karina Romero
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Patent number: 8067595Abstract: In order to efficiently supply CPT, which is a starting compound of irinotecan hydrochloride and a variety of camptothecin derivatives, by a practical total synthesis, the invention provides a means of efficiently preparing a tricyclic ketone that corresponds to a CDE ring moiety of a camptothecin (CPT) skeleton.Type: GrantFiled: June 8, 2006Date of Patent: November 29, 2011Assignee: Kabushiki Kaisha Yakult HonshaInventors: Hiroyuki Nishiyama, Seigo Sawada
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Publication number: 20110288076Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particularly, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.Type: ApplicationFiled: October 16, 2009Publication date: November 24, 2011Applicant: EXELIXIS, INC.Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
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Patent number: 8058447Abstract: The present application relates to novel 4-chromenonyl-1,4-dihydropyridinecarbonitriles, processes for their preparation, pharmaceutical compositions containing them, and their use for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.Type: GrantFiled: July 14, 2006Date of Patent: November 15, 2011Assignee: Bayer Pharma AktiengesellschaftInventors: Alexander Kuhl, Peter Kolkhof, Heike Heckroth, Karl-Heinz Schlemmer, Ingo Flamme, Santiago Figueroa Perez, Heike Gielen-Haertwig, Rolf Grosser, Jens-Kerim Ergüden, Dieter Lang
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Publication number: 20110263626Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: August 28, 2008Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-metz, Rainer Walter
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Patent number: 8030493Abstract: 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: GrantFiled: June 6, 2007Date of Patent: October 4, 2011Assignee: Obschestvo S Ogranichennoy Otvetstvennostyu “Natsionalnaya Isseldovatelskaya Kompaniya”Inventors: Pavel Vasilyevich Yakimuk, Sergey Vitalyevich Stovbun, Alexandr Anatolyevich Litvin
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Publication number: 20110218199Abstract: Compounds of formula I are disclosed. These compounds are useful in the control or prevention of cancer.Type: ApplicationFiled: August 20, 2008Publication date: September 8, 2011Inventors: Guy Georges, Klaus Kaluza, Matthias Koerner, Ulrike Reiff, Stefan Scheiblich, Wolfgang Von Der Saal, Stefan Weigand
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Publication number: 20110207935Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused ring derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), X1 and X2 represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.Type: ApplicationFiled: October 14, 2009Publication date: August 25, 2011Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuo Shimizu, Masato Iizuka, Hideki Fujikura, Yasushi Takigawa, Masahiro Hiratochi
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Publication number: 20110201817Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.Type: ApplicationFiled: April 27, 2011Publication date: August 18, 2011Applicant: XenoPort, Inc.Inventors: Jia-Ning XIANG, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
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Patent number: 7994142Abstract: The invention relates to agents that contain folic acid, vitamin B6 and vitamin B12, and to the use thereof in hyperhomocysteinemia for controlling homocysteine levels. The agents are mainly suitable for the preventive and acute treatment of vascular diseases, of pregnant women and neurodegenerative diseases and are particularly advantageous in cases where the homocysteine levels to be controlled are found in an individual suffering from renal failure or being treated with immune suppressors. The invention particularly relates to pharmaceutical agents and food supplements comprising a corresponding active ingredient combination and to agents in the form of commercial packages containing corresponding combination preparations or monopreparations for the combined use.Type: GrantFiled: January 11, 2006Date of Patent: August 9, 2011Assignee: Phrontier S.A.R.L.Inventor: Martin Goerne
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Patent number: 7989633Abstract: The present application relates to novel 4-chromenonyl-1,4-dihydropyridines, process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.Type: GrantFiled: July 12, 2006Date of Patent: August 2, 2011Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Alexander Kuhl, Peter Kolkhof, Heike Heckroth, Karl-Heinz Schlemmer, Ingo Flamme, Santiago Figueroa Perez, Heike Gielen-Haertwig, Rolf Grosser, Jens-Kerim Ergüden, Dieter Lang
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Publication number: 20110184029Abstract: The present invention relates to 2-pyridone derivatives of Formula I or IV as herein described, compositions containing such compounds, synthetic processes for making such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 13, 2009Publication date: July 28, 2011Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Choung U. Kim, Michael L. Mitchell, Jong Chan Son
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Publication number: 20110183980Abstract: In one aspect, the invention relates to O-benzyl nicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: September 21, 2010Publication date: July 28, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Shaun Stauffer, Richard Williams, Gregor MacDonald, Ya Zhou, José Manuel Bartolomé-Nebreda
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Publication number: 20110178137Abstract: The present invention relates to pharmaceutical compositions and combinations for treating, preventing or managing heart failure and/or connected diseases therewith 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.Type: ApplicationFiled: June 16, 2009Publication date: July 21, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Barbara Albrecht-Küpper, Stefan Schäfer, Elodie Kienlen
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Publication number: 20110178089Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: January 13, 2011Publication date: July 21, 2011Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ulmer
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Publication number: 20110178120Abstract: The present invention relates to pyridoxine (vitamin B6) derived compounds of formula (I), pharmaceutically acceptable salts, or solvates thereof, wherein R1, R2, R4, A, L B1 and B2 are as defined in the specification, and pharmaceutical compositions comprising the compounds. Compounds of formula (I) inhibit Human Immunodeficiency Virus (HIV)-integrase enzyme and are useful for preventing and treating HIV infection and AIDS.Type: ApplicationFiled: June 4, 2009Publication date: July 21, 2011Applicant: AMBRILIA BIOPHARMA, INC.Inventors: Brent Stranix, Francis Beaulieu, Jean-Emmanuel Bouchard, Guy Milot, Wang Zhigang, Réjean Ruel
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Publication number: 20110178138Abstract: The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of protein prenyltransferases including GGTase I and/or RabGGTase. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.Type: ApplicationFiled: July 28, 2008Publication date: July 21, 2011Applicant: The Regents of the University of CaliforniaInventors: Ohyun Kwon, Fuyuhiko Tamanoi, Hanna Fiji, Masaru Watanabe
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Patent number: 7981901Abstract: Methods and compositions for targeting cerebral circulation and treatment of headache include formulations comprising a pharmacologically active substance in a transdermal formulation, which is topically applied to an area of skin superficial to a carotid artery, a temporal artery, a vertebral artery, or to a tender spot associated with a headache. Particularly preferred formulations include a xanthine derivative (e.g., theophylline, caffeine, aminophylline), and may further comprise ketoprofen. Contemplated methods further include methods of advertising use of contemplated compositions.Type: GrantFiled: August 20, 2002Date of Patent: July 19, 2011Inventor: Bruce Frome
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Publication number: 20110160207Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: March 2, 2011Publication date: June 30, 2011Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
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Publication number: 20110144164Abstract: The present invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.Type: ApplicationFiled: December 14, 2010Publication date: June 16, 2011Applicant: H. LUNDBECK A/SInventors: Nikolay Khanzhin, Søren Møller Nielsen, Karsten Juhl, Lars Kyhn Rasmussen
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Publication number: 20110117073Abstract: The invention relates to protein conjugates that contain a protein kinase containg a cysteine residue in the ATP binding site and an inhibitor that is covalently and irreversibly bonded to said cysteine residue, such that the activity of the protein kinase is irreversibly inhibited. The invention also relates to compounds that irreversibly inhibit protein kinases.Type: ApplicationFiled: September 15, 2010Publication date: May 19, 2011Applicant: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Russell Colyn Petter, Deqiang Niu, Lixin Qiao, Arthur Kluge, Roy Lobb, Shomir Ghosh, Zhendong Zhu
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Publication number: 20110112114Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.Type: ApplicationFiled: June 9, 2010Publication date: May 12, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Roger D. Tung, Govinda Rao Bhisetti, Luc J. Farmer
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Publication number: 20110065759Abstract: The present invention relates to a compound of formula I, in all its isomeric forms and pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 3, 2010Publication date: March 17, 2011Inventors: Stephan Roever, Matthew Wright
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Patent number: 7902372Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.Type: GrantFiled: April 2, 2008Date of Patent: March 8, 2011Assignee: Eli Lilly and CompanyInventors: Mark Donald Chappell, Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
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Publication number: 20110053938Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.Type: ApplicationFiled: September 2, 2010Publication date: March 3, 2011Applicant: CANTHERA THERAPEUTICS, INC.Inventors: Michael Andrew Foley, Robert Gould, Peter Elliott, Anna Mandinova, Sam Lee
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Patent number: 7897621Abstract: The present invention relates to compounds formula I: and pharmaceutically acceptable salts thereof, wherein R1 to R8 are as defined in the description and claims for use as HDL-cholesterol raising agents in the treatment and/or prophylaxis of diseases or disorders that can be treated with such agents such as dyslipidemia.Type: GrantFiled: March 16, 2009Date of Patent: March 1, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Paul Hebeisen, Constantinos G. Panousis, Stephan Roever, Pius Waldmeier, Matthew Wright
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Patent number: 7893269Abstract: The present invention relates to a novel process for the preparation of 1-alkyl or 1-cycloalkyl derivatives of 3-hydroxy-4-oxo-1,4-dihydropyridine-2-carboxamide of formula (I). The process includes reacting an amine R2NH2 with a compound of formula (II) in a solution of metal hydroxide in water to give a compound of formula (III). Subsequent reaction of the compound of formula (III) with an acid chloride formation reagent in an inert solvent gives compounds of formula (I). The acid chloride formation reagent is selected from oxalyl chloride and dimethylformamide, dimethylchloromethylene-ammonium chloride and thionyl chloride and dimethylformamide. If desired, a compound of formula (I) where R5 is hydrogen may be formed when an intermediate substituent is used wherein R5 is an alcohol protective group removable by catalytic hydrogenation.Type: GrantFiled: November 17, 2005Date of Patent: February 22, 2011Assignee: Apotex IncInventors: Tim Fat Tam, Regis Leung-Toung, Yanqing Zhao, Wanren Li, Yingsheng Wang, Sandra Vittoria Agostino, Birenkumar Hasmukhbhai Shah
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Publication number: 20110039851Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.Type: ApplicationFiled: October 14, 2008Publication date: February 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
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Patent number: 7888375Abstract: A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HIV 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 integrase-based anti-HIV agents). Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.Type: GrantFiled: July 13, 2007Date of Patent: February 15, 2011Assignee: The University of Georgia Research Foundation, IncInventors: Vasu Nair, Byung I. Seo, Vinod R. Uchil
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Publication number: 20110034463Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.Type: ApplicationFiled: April 1, 2009Publication date: February 10, 2011Inventors: Jon Goguen, Ning Pan, Kyungae Lee
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Publication number: 20110028463Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.Type: ApplicationFiled: July 2, 2008Publication date: February 3, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo