Carbocyclic Ring Bonded Directly To The Piperazine Ring Patents (Class 514/255.03)
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Publication number: 20130115292Abstract: The present invention relates to an enteric tablet with improved bioavailability, which is rapidly disintegrated after reaching the intestine to allow dissolution of the active ingredient, and which characteristically reduces the amount of talc to be used and is free of an alkali component.Type: ApplicationFiled: April 28, 2011Publication date: May 9, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masafumi Misaki, Yuki Tsushima, Masahiro Niwa
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Patent number: 8435992Abstract: Methods for treating cancer by using compound PM00104, in particular, for treating multiple myeloma are provided.Type: GrantFiled: May 18, 2009Date of Patent: May 7, 2013Assignee: Pharma Mar S.A.Inventors: Enrique Ocio, Atanasio Pandiella, Jesús San Miguel, Pablo Manuel Avilés Marín
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Publication number: 20130109701Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfon-amide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 4, 2011Publication date: May 2, 2013Applicant: Pfizer LimitedInventors: Alan Daniel Brown, David James Rawson, Robert Ian Storer, Nigel Alan Swain
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Patent number: 8431563Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: GrantFiled: August 23, 2011Date of Patent: April 30, 2013Assignee: Amgen Inc.Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, Jr., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
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Patent number: 8426423Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1) wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: GrantFiled: October 31, 2007Date of Patent: April 23, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
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Publication number: 20130096105Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: November 30, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Publication number: 20130072468Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.Type: ApplicationFiled: September 14, 2012Publication date: March 21, 2013Inventors: Eric J. Gilbert, William J. Greenlee, Michael W. Miller, Jack D. Scott, Andrew W. Stamford
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Patent number: 8394805Abstract: Novel compounds of which the following is exemplary:Type: GrantFiled: August 12, 2008Date of Patent: March 12, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Publication number: 20130059852Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).Type: ApplicationFiled: April 8, 2011Publication date: March 7, 2013Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
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Novel 1, 2-Disubstituted Amido-anthraquinone Derivatives, Preparation Method and application thereof
Publication number: 20130059862Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: ApplicationFiled: August 1, 2012Publication date: March 7, 2013Inventor: Hsu-Shan HUANG -
Patent number: 8377936Abstract: Use of nicotine receptor agonists for treating inflammatory diseases, including a variety of pulmonary diseases. Such agonists have fewer side effects than other anti-inflammatory drugs, such as steroids. Moreover, these agonists can be used alone or in combination with other anti-inflammatory drugs to alleviate pulmonary diseases. For example, a method of treating pulmonary inflammation of an inflammatory disease selected from the group of asthma, interstitial pulmonary fibrosis (IPF), sarcoidosis, hypersensitivity pneumonitis (HP), and bronchiolitis obliterans with organizing pneumonitis (BOOP) in an animal in need thereof having said inflammation, including administering orally or by inhalation to said animal a nicotinic receptor agonist.Type: GrantFiled: June 15, 2011Date of Patent: February 19, 2013Assignee: Universite LavalInventors: Yvon Cormier, Evelyne Israel-Assayag, Marie-Renée Blanchet
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Publication number: 20130040966Abstract: The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described.Type: ApplicationFiled: October 17, 2012Publication date: February 14, 2013Applicant: Forest Laboratories Holdings Ltd.Inventors: Ranajoy SARKAR, Mahendra G. DEDHIYA, Anil CHHETTRY
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Publication number: 20130035312Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: ApplicationFiled: October 11, 2012Publication date: February 7, 2013Applicants: Axys Pharmaceuticals, Inc., Merck, Sharp & Dohme, Corp.Inventors: Merck, Sharp & Dohme, Corp., Axys Pharmaceuticals, Inc.
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Publication number: 20130018047Abstract: The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Andreas Haupt, Frauke Pohlki, Karla Drescher, Karsten Wicke, Liliane Unger, Ana-Lucia Relo, Anton Bespalov, Barbara Vogg, Gisela Backfisch, Juergen Delzer, Min Zhang, Yanbin Lao
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Publication number: 20130012485Abstract: Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R3, R4, R5, R6, R7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.Type: ApplicationFiled: December 20, 2007Publication date: January 10, 2013Inventors: Daniel Kaspar Bäschlin, Richard Sedrani, Stefanie Flohr, Kenji Namoto, Nils Ostermann, Finton Sirockin, François Gessier, Garry Fenton, Mandy Christine Beswick, David Edward Clark, Bohdan Waszkowycz
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Patent number: 8343959Abstract: The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.Type: GrantFiled: October 28, 2011Date of Patent: January 1, 2013Assignees: Abbott GmbH & Co. KG, Abbott LaboratoriesInventors: Andreas Haupt, Frauke Pohlki, Karla Drescher, Karsten Wicke, Liliane Unger, Ana-Lucia Relo, Anton Bespalov, Barbara Vogg, Gisela Backfisch, Juergen Delzer, Min Zhang, Yanbin Lao
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Patent number: 8338405Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function in animals.Type: GrantFiled: August 23, 2010Date of Patent: December 25, 2012Assignee: Dart Neuroscience LLCInventors: Terence P. Keenan, Alan P. Kaplan
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Publication number: 20120322719Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.Type: ApplicationFiled: June 14, 2012Publication date: December 20, 2012Applicant: The Feinstein Institute For Medical ResearchInventors: Valentin A. Pavlov, Kevin J. Tracey
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Publication number: 20120322811Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.Type: ApplicationFiled: June 19, 2012Publication date: December 20, 2012Inventors: Morten JORGENSEN, Peter Hongaard ANDERSEN, Klaus Gjervig JENSEN, Mette Graulund HVENEGAARD, Lassina BADOLO, Mikkel Fog JACOBSEN
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Patent number: 8324190Abstract: Methods of treating cancer using compounds according to Formula (I) are disclosed herein, wherein X, X1, X2, Ra, R1, R2, R3, R4, R5, R6, R7, g, M, y, a, b, d, e, V, W, Z and Q are as defined herein.Type: GrantFiled: July 14, 2009Date of Patent: December 4, 2012Assignees: Temple University—Of The Commonwealth System of Higher Education, Onconova Therapeutics, Inc.Inventors: E. Premkumar Reddy, M. V. Ramana Reddy, Stanley C. Bell
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Publication number: 20120302553Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.Type: ApplicationFiled: February 6, 2012Publication date: November 29, 2012Applicant: H. LUNDBECK A/SInventors: Thomas Ruhland, Garrick P. Smith, Benny Bang-Anderson, Ask Puschl, Ejner Knud Moltzen, Kim Andersen
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Publication number: 20120302541Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.Type: ApplicationFiled: October 28, 2010Publication date: November 29, 2012Inventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
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Patent number: 8318748Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: May 25, 2011Date of Patent: November 27, 2012Assignees: Merck, Sharp & Dohme Corp., Axys Pharmaceuticals, Inc.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra Baskaran
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Publication number: 20120295919Abstract: Provided are opioid receptor antagonists represented by the formula (I) where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.Type: ApplicationFiled: October 12, 2010Publication date: November 22, 2012Applicant: RESEARCH TRIANGLE INSTITUTEInventors: Frank I. Carroll, Juan P. Cueva, James B. Thomas, S. Wayne Mascarella, Scott P. Runyon
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Patent number: 8309587Abstract: The present invention relates to piperidine and piperazine phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.Type: GrantFiled: March 14, 2012Date of Patent: November 13, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Esther Ann Martinborough, Lev Tyler Dewey Fanning, Urvi Jagdishbhai Sheth, Dean Mitchell Wilson, Andreas P. Termin, Timothy Donald Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
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Publication number: 20120270877Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.Type: ApplicationFiled: November 1, 2010Publication date: October 25, 2012Applicant: MannKind CorporationInventors: Qingping Zeng, Warren S. Wade, John Bruce Patterson
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Patent number: 8293749Abstract: Methods of treating or preventing a vertigo, nausea, or vomiting condition comprising injecting a subject with a pharmaceutically acceptable formulation consisting essentially of an effective amount of meclizine or a pharmaceutically acceptable salt thereof, a chemically modified cyclodextrin, and an aqueous carrier medium having a pH between about 2 and about 7 are disclosed. An injectable pharmaceutical formulation for treating or preventing a vertigo, nausea, or vomiting condition consisting essentially of an effective amount of meclizine, a chemically modified cyclodextrin, and an aqueous carrier medium having a pH between about 2 and about 7 is also disclosed.Type: GrantFiled: January 12, 2012Date of Patent: October 23, 2012Assignee: Genebiology, Inc.Inventors: Walker Anderson Long, Edwin Curran Murphy, III
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Publication number: 20120258954Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: May 29, 2012Publication date: October 11, 2012Applicant: NOVARTIS AGInventors: Claus Ehrhardt, Leslie Wighton McQuire, Pascal Rigollier, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi
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Publication number: 20120252819Abstract: The present invention relates to formulations and methods for increasing the bioavailability of 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one, 1-(3,3-diphenylpropanoyl)piperazine, or a salt thereof. In particular, the formulation can include one or more pharmaceutically acceptable matrix polymers to form a solid dispersion, e.g., a spray dried dispersion or a hot melt extrusion.Type: ApplicationFiled: June 12, 2012Publication date: October 4, 2012Inventors: Mahesh V. Padval, Jeff T. Gautschi, Daniel T. Smithey, Marshall D. Crew, Abizer Harianawala
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Publication number: 20120252820Abstract: Methods of identifying compounds that potentiate the activity of antifungal agents, potentiators identified by these methods, and methods of using potentiators to treat fungal infections are disclosed.Type: ApplicationFiled: April 22, 2009Publication date: October 4, 2012Applicant: NORTHEASTERN UNIVERSITYInventors: Kim Lewis, Michael David Lafleur
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Patent number: 8268833Abstract: This invention comprises the novel compounds of formula (I) wherein n, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: February 18, 2009Date of Patent: September 18, 2012Assignee: Janssen Pharmaceutica, N.V.Inventors: Patrick René Angibaud, Isabelle Noëlle Constance Pilatte, Sven Franciscus Anna Van Brandt, Bruno Roux, Peter Ten Holte, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Alexey Borisovich Dyatkin
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Publication number: 20120225854Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 23, 2011Publication date: September 6, 2012Applicant: AMGEN INC.Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, JR., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
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Patent number: 8252796Abstract: The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art.Type: GrantFiled: September 29, 2009Date of Patent: August 28, 2012Assignees: CSPC Zhonggi Pharmaceutical Technology (Shijiazhuang) Co. Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Jianqi Li, Na Lv, Hua Jin, Zhijie Weng, Yongyong Zheng
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Publication number: 20120214796Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: April 27, 2012Publication date: August 23, 2012Inventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
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Patent number: 8242175Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.Type: GrantFiled: December 7, 2010Date of Patent: August 14, 2012Assignee: DAC S.R.L.Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
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Publication number: 20120196874Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.Type: ApplicationFiled: January 27, 2012Publication date: August 2, 2012Inventors: David WATT, Chunming Liu, Vitaliy M. Sviripa, Wen Zhang
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Publication number: 20120189697Abstract: Pharmaceutical compositions of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine and pharmaceutically acceptable acid addition salts thereof adapted so that release does not take place in the stomach is provided.Type: ApplicationFiled: August 23, 2010Publication date: July 26, 2012Applicant: H. LUNDBECK A/SInventors: Astrid-Maria Hojer, Pernille Gundorf Drewes, Jens Kateb
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Patent number: 8207335Abstract: The present invention relates to a method of preparing compounds of general formula I wherein m, n, R1 and R2 are defined as mentioned hereinafter, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases.Type: GrantFiled: February 8, 2010Date of Patent: June 26, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Adil Duran, Markus Frank, Waldemar Pfrengle, Juergen Schnaubelt
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Publication number: 20120149693Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs.Type: ApplicationFiled: May 5, 2010Publication date: June 14, 2012Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventor: Raymond G. Booth
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Patent number: 8198284Abstract: A method for treating a neurodegenerative disorder. The method includes administering to a subject in need thereof an effective amount of one or more thiourea compounds of formula (I) or (II): Each variable in formula (I) or (II) is defined herein. Also disclosed is use of these thiourea compounds to reduce microglia-mediated neuro-inflammation or enhancing microglial phagocytosis of A?.Type: GrantFiled: March 24, 2009Date of Patent: June 12, 2012Assignee: National Health Research InstitutesInventors: Feng-Shiun Shie, Jyh-Haur Chern, Yu-Sheng Chao
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Publication number: 20120142674Abstract: The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.Type: ApplicationFiled: November 1, 2011Publication date: June 7, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Andreas Haupt, Frauke Pohlki, Liliane Unger, Ana Lucia Relo, Karsten Wicke, Min Zhang
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Publication number: 20120129870Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.Type: ApplicationFiled: December 17, 2008Publication date: May 24, 2012Inventors: Wenying Chai, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
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Patent number: 8183239Abstract: The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.Type: GrantFiled: October 27, 2006Date of Patent: May 22, 2012Assignee: Janssen Pharmaceutica NVInventors: Pascal Bonaventure, Nicholas I. Carruthers, Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Mark Seierstad, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
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Publication number: 20120115850Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.Type: ApplicationFiled: May 10, 2011Publication date: May 10, 2012Inventors: Oren Becker, Rosa Melendez, Yael Marantz, Anurag Sharadendu, Merav Fichman, Mercedes Lobera, Hanoch Senderowitz, Srinivasa Rao Cheruku, Sharon Shacham, Laurence Wu, Ashis Saha, Pini Orbach, Dale S. Dhanoa
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Publication number: 20120115778Abstract: Methods for treating eating disorders associated with excessive weight gain, suppressing appetite, reducing body weight, or treating obesity in an animal by administering one or more antagonists of the serotonin Htr1a or Htr2b receptor, or a Tph2 inhibitor are provided, or combinations thereof.Type: ApplicationFiled: July 15, 2010Publication date: May 10, 2012Applicant: The Trustees of Columbia University in the City of New YorkInventors: Gerard Karsenty, Vijay Yadav, Franck Oury
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Publication number: 20120115867Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen or C1-C6 alkyl, R3, R4 are, independently, hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl or C1-C6 haloalkoxy, and R5 and R6 are as further defined in the specification, and pharmaceutical acceptable salts thereof.Type: ApplicationFiled: May 4, 2011Publication date: May 10, 2012Applicant: DAC S.R.L.Inventors: Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Mario Varasi, Ciro Mercurio
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Publication number: 20120108570Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Miodrag Radulovacki, David W. Carley
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Publication number: 20120095000Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-? signaling are described.Type: ApplicationFiled: December 12, 2011Publication date: April 19, 2012Applicants: SRI International, The Board of Trustees of the Leland Stanford Junior UniversityInventors: Anton Wyss-Coray, Mary J. Tanga
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Patent number: 8153637Abstract: The present invention relates to phenyl-alkyl piperazines of formula (I): in which A, R1, R2 and R3 are as defined herein, having TNF-modulating activity. The invention also relates to the preparation thereof, pharmaceutical compositions thereof, and to the therapeutic use thereof.Type: GrantFiled: December 16, 2010Date of Patent: April 10, 2012Assignee: SanofiInventors: Marco Baroni, Olaf Ritzeler, Marco Zanchet
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Publication number: 20120071461Abstract: Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.Type: ApplicationFiled: September 22, 2011Publication date: March 22, 2012Applicant: GRUENENTHAL GmbHInventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Jean De Vry, Christa Kneip, Tieno Germann, Michael Engels