Carbocyclic Ring Bonded Directly To The Piperazine Ring Patents (Class 514/255.03)
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Publication number: 20090253710Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3?R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(?O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.Type: ApplicationFiled: June 30, 2008Publication date: October 8, 2009Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Scott Myers, Yesim Altas Tahirovic
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Publication number: 20090247509Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: ApplicationFiled: April 17, 2009Publication date: October 1, 2009Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: James A. Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M. Shutske, Joseph T. Strupczewski, Kenneth J. Bordeau, John G. Jurcak, Thaddeus R. Nieduzak, Sharon A. Jackson, Paul Angell, James P. Carey, George Lee, David Fink, Jean-Francois Sabuco, Yulin Chiang, Nicola Collar
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Publication number: 20090239873Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: ApplicationFiled: December 31, 2008Publication date: September 24, 2009Inventors: Miguel Garcia-Guzman Blanco, Daniele Bergeron, Peter D. J. Grootenhuis, Dennis Hurley, Akiko Nakatani, Lewis R. Makings, Daniel DiSepio, Gabriel Raffai
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Publication number: 20090203696Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).Type: ApplicationFiled: December 15, 2008Publication date: August 13, 2009Applicant: SANOFI-AVENTISInventors: Jozsef Zsolt BOCSKEI, Gary MCCORT, Hans MATTER, Henning STEINHAGEN, Berangere THIERS
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Patent number: 7572787Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.Type: GrantFiled: August 25, 2006Date of Patent: August 11, 2009Assignee: Biovitrum ABInventors: Patrizia Caldirola, Ulf Bremberg, Gary Johansson, Andrew Mott, Annika Jenmalm Jensen, Katarina Beierlien, Markus Thor, Lars Tedenborg
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Patent number: 7563795Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: September 27, 2004Date of Patent: July 21, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Miguel Garcia-Guzman Blanco, Daniele Bergeron, Peter D. J. Grootenhuis, Dennis Hurley, Akiko Nakatani, Lewis R. Makings, Daniel DiSepio, Gabriel Raffai
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Publication number: 20090181943Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.Type: ApplicationFiled: April 9, 2008Publication date: July 16, 2009Applicant: METHYLGENE INC.Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
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Publication number: 20090176785Abstract: Methods of preventing or treating arthritis is disclosed.Type: ApplicationFiled: November 14, 2008Publication date: July 9, 2009Applicant: Abbott LaboratoriesInventors: Philip Bardwell, Tariq Ghayur
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Patent number: 7557109Abstract: A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans and the symptoms associated therewith, inattentiveness, and hyperactivity with impulsivity, using eltoprazine and related compounds is provided.Type: GrantFiled: September 2, 2005Date of Patent: July 7, 2009Assignee: Psychogenics, Inc.Inventors: Daniela Brunner, Daniel W. Goodman
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Publication number: 20090170836Abstract: 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: ApplicationFiled: February 18, 2009Publication date: July 2, 2009Inventors: Patrick Rene Angibaud, Isabelle Noelle 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: 20090156589Abstract: A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action and cell infiltration inhibitory action. wherein R10 represents 5- to 10-membered cycloalkyl etc. optionally substituted with hydroxyl etc., R30, R31 and R32 may be the same or different and each represents hydrogen etc., R40 represents C1-10 alkyl etc. optionally substituted with hydroxyl etc., n represents an integer of 0, 1 or 2, X1 represents CH or nitrogen, and R20, R21, R22 and R23 may be the same or different and each represents hydrogen etc.Type: ApplicationFiled: June 14, 2006Publication date: June 18, 2009Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Tetsuya Kawahara, Makoto Kotake, Naoki Yoneda, Shinsuke Hirota, Masayoshi Ohkuro
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Publication number: 20090156614Abstract: This invention provides new compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, prostate cancer, muscle wasting diseases and/or disorders or a bone-related diseases and/or disorders.Type: ApplicationFiled: July 19, 2007Publication date: June 18, 2009Inventors: James T. Dalton, Duane D. Miller, Igor Rakov, Casey Bohl, Michael L. Mohler
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Patent number: 7544716Abstract: This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.Type: GrantFiled: November 28, 2003Date of Patent: June 9, 2009Assignee: Xention LimitedInventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Publication number: 20090143394Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-? signaling are described.Type: ApplicationFiled: October 10, 2008Publication date: June 4, 2009Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Anton Wyss-Coray, Mary J. Tanga
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Publication number: 20090137606Abstract: The invention encompasses a solid dose pharmaceutical composition comprising a disagreeable-tasting drug and processes for preparation of the pharmaceutical composition. The pharmaceutical composition is designed not to be swallowed immediately.Type: ApplicationFiled: November 6, 2008Publication date: May 28, 2009Inventor: Rakefet Cohen
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Publication number: 20090131419Abstract: Disclosed are sulphones which modulate the action of gamma-secretase. The compounds are useful in the treatment or prevention of Alzheimer's disease.Type: ApplicationFiled: May 6, 2008Publication date: May 21, 2009Inventors: Jose Luis Castro Pineiro, Ian Churcher, Kevin Dinnell, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Paul Joseph Oakley, Andrew Pate Owens, Duncan Edward Shaw, Martin Richard Teall, Susannah William, Brian John Williams
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Publication number: 20090104261Abstract: A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans and the symptoms associated therewith, inattentiveness, and hyperactivity with impulsivity, using eltoprazine and related compounds is provided.Type: ApplicationFiled: December 24, 2008Publication date: April 23, 2009Applicant: Psychogenics, Inc.Inventors: Daniela Brunner, Daniel W. Goodman
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Publication number: 20090105275Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of Het, R0, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.Type: ApplicationFiled: October 15, 2008Publication date: April 23, 2009Inventor: Chih Yung HO
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Publication number: 20090105208Abstract: 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: June 25, 2008Publication date: April 23, 2009Inventors: Eric J. Gilbert, Michael W. Miller, Jack D. Scott, Duane Eugene DeMong, Andrew Stamford, William J. Greenlee, Chander Shekher Celly
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Publication number: 20090105237Abstract: A method of conferring a cooling effect on the skin or mucous membranes by applying thereto at least one compound of the Formula I: (a) wherein B is selected from H, CH3, C2H5, OCH3, OC2H5; and OH; and (b) wherein A is a moiety of the formula —CO-D, wherein D is selected from the following moieties: (i) —NR1R2, wherein R1 and R2 are independently selected from H and C1-C8 straight or branched-chain aliphatic, alkoxyalkyl, hydroxyalkyl, araliphatic and cycloalkyl groups, or R1 and R2 together with the nitrogen atom to which they are attached form part of an optionally-substituted, five- or six-membered heterocyclic ring; (ii) —NHCH2COOCH2CH3, —NHCH2CONH2, —NHCH2CH2OCH3, —NHCH2CH2OH, —NHCH2CH(OH)CH2OH and (iii) a moiety selected from the group consisting of: The compounds are useful for providing cooling effects in a variety of products, such as foodstuffs, confectionery, tobacco products, beverages, cosmetics, dentifrices, medicinal preparations, mouthwashes and toiletries.Type: ApplicationFiled: May 24, 2006Publication date: April 23, 2009Inventors: Karen Ann Bell, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack
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Publication number: 20090099199Abstract: The invention relates to compound of the formula I wherein the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: October 15, 2008Publication date: April 16, 2009Inventors: Joachim Nozulak, David Orain, Simona Cotesta
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Patent number: 7517885Abstract: The present invention relates to substituted [4-(4-phenyl-piperazin-1-yl)-cyclohexyl]-urea compounds of Formula (I) and pharmaceutically acceptable forms thereof, as ?1a/?1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as methods of treatment.Type: GrantFiled: June 14, 2006Date of Patent: April 14, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: George Chiu, Peter J. Connolly, Jessica J. Liu, Steven A. Middleton, Virginia L. Pulito, Shengjian Li
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Patent number: 7517884Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: GrantFiled: May 16, 2006Date of Patent: April 14, 2009Assignee: Kalypsys Inc.Inventors: James W. Malecha, Sergio G. Duron, Andrew K. Lindstrom
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Publication number: 20090088444Abstract: Provided herein are substituted phenanthrene diketo acid compounds. These compounds comprise the diketo acid moiety on one of carbons C1-C4 and C9 in the phenanthrene ring and at least one further substitutent on the other ring carbons. Also provided are methods of inhibiting an activity of a human immunodeficiency virus (HIV) integrase protein and treating an HIV infection in a subject using the substituted phenanthrene diketo acid compounds.Type: ApplicationFiled: October 2, 2008Publication date: April 2, 2009Inventor: John K. Buolamwini
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Publication number: 20090054461Abstract: Use of a 1-(3-chlorophenyl)-3-alkylpiperazine of formula (I), in racemic (R, S) form or in the form of the (S) enantiomer, in which R is a linear or branched alkyl group having from 1 to 3 carbon atoms, or of an addition salt thereof with a pharmaceutically acceptable organic or inorganic acid, for treating apetite disorder A pharmaceutical composition that comprises a therapeutically effective amount of a 1-(3-chlorophenyl)-3-alkylpiperazine of formula (I) as previously defined or of an addition salt thereof with a pharmaceutically acceptable organic or inorganic acid, and at least one pharmaceutically acceptable excipient.Type: ApplicationFiled: June 2, 2006Publication date: February 26, 2009Applicant: AZIENDE CHIM. RIUN. ANG. FRANC. A.C.R.A.F. S.P.A.Inventors: Beatrice Garrone, Maurizio Magnani, Guido Furlotti, Nicola Cazzolla, Angelo Guglielmotti
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Publication number: 20090054453Abstract: The present invention relates to new compounds of formula I, or salts, solvates or solvated salts thereof, wherein Q, R1, R2, R3, R4 and n are defined as in claim 1, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.Type: ApplicationFiled: March 15, 2007Publication date: February 26, 2009Inventors: Lilian Alcaraz, Gunnar Nordvall, Didier Rotticci, Daniel Sohn
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Patent number: 7494999Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: GrantFiled: October 25, 2005Date of Patent: February 24, 2009Assignee: Kalypsys, IncInventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steven P. Govek
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Patent number: 7491727Abstract: The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formula I, and synthesis and uses thereof for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.Type: GrantFiled: September 5, 2006Date of Patent: February 17, 2009Assignee: Epix Delaware, Inc.Inventors: Dale S. Dhanoa, Dongli Chen, Oren Becker, Silvia Noiman, Srinivasa R. Cheruku, Yael Marantz, Anurag Sharadendu, Sharon Shacham, Alexander Heifetz, Pradyumna Mohanty, Boaz Inbal, Merav Fichman, Raphael Nudelman, Shay Bar-Haim
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Publication number: 20090042904Abstract: The present invention relates to substituted phenyl-piperazine compounds of general formula (I), a process for their preparation, medicaments comprising said substituted phenyl-piperazine compounds as well as the use of said substituted phenyl-piperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.Type: ApplicationFiled: December 29, 2005Publication date: February 12, 2009Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: Andrea Aschenbrenner, Juergen Kraus, Stefan Tasler, Andreas Wuzik, Jordi-Ramon Quintana-Ruiz
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Patent number: 7488731Abstract: The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formula I, and synthesis and uses thereof for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.Type: GrantFiled: July 24, 2007Date of Patent: February 10, 2009Assignee: Epix Delaware, Inc.Inventors: Dale S. Dhanoa, Dongli Chen, Oren Becker, Silvia Noiman, Srinivasa R. Cheruku, Yael Marantz, Anurag Sharadendu, Sharon Shacham, Alexander Heifetz, Pradyumna Mohanty, Boaz Inbal, Merav Fichman, Raphael Nudelman, Shay Bar-Haim
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Patent number: 7488730Abstract: A series of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides was prepared and their affinity for serotonin 5-HT7, 5-HT1A, and 5-HT2A receptors was measured using in vitro binding assays. In relation to 5-HT7 receptor affinity, receptor binding studies indicated that: (i) the optimal alkyl chain length was five methylenes; (ii) an unsubstituted 1,2,3,4-tetrahydronaphthalenyl nucleus was selected for further substitutions; and (iii) the substitution pattern of the aryl ring linked to the piperazine ring played a significant role. Several compound with high affinity for 5-HT7 receptors were identified.Type: GrantFiled: November 18, 2005Date of Patent: February 10, 2009Assignee: Universita Degli Studi Di BariInventors: Marcello Leopoldo, Francesco Berardi, Nicola Antonio Colabufo, Marialessandra Contino, Enza Lacivita, Mauro Niso, Roberto Perrone, Vincenzo Tortorella
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Publication number: 20090036468Abstract: The present invention relates to pharmaceutical compositions containing dopamine receptor ligands and selective serotonin reuptake inhibitors and to methods of treating disorders such as schizophrenia, major depressive disorder and bipolar depression using combinations of dopamine receptor ligands and selective serotonin reuptake inhibitors. The present invention also relates to methods of treating depression using dopamine receptor ligands.Type: ApplicationFiled: August 4, 2008Publication date: February 5, 2009Applicant: FOREST LABORATORIES HOLDINGS LIMITEDInventors: Gary SAMORISKI, Nika ADHAM
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Patent number: 7485644Abstract: The invention provides compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein ring B represents a monocyclic aryl ring having six ring atoms or a monocyclic heteroaryl ring having up to six ring atoms and containing one or more ring heteroatoms wherein each said heteroatom is nitrogen; R2 represents a group selected from C1-6 alkyl or aryl, which said group is substituted by one or more fluorine groups; n is 1, 2 or 3; and R1 represents an optionally substituted group selected from C1-6 alkyl, C5-7 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C1-6 alkyl-aryl, C1-6 alkyl-heteroaryl, C1-6 alkyl-cycloalkyl or C1-6 alkyl-heterocycloalkyl. Processes for their preparation; pharmaceutical compositions containing them; and their use in the treatment of a disease condition mediated by one or more metalloproteinase enzymes.Type: GrantFiled: June 23, 2004Date of Patent: February 3, 2009Assignee: AstraZeneca ABInventors: Maurice Raymond Verschoyle Finlay, David Waterson
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Publication number: 20090029971Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: ApplicationFiled: September 4, 2008Publication date: January 29, 2009Applicant: KALYPSYS, INC.Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steve P. Govek
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Patent number: 7482346Abstract: The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.Type: GrantFiled: August 22, 2006Date of Patent: January 27, 2009Assignee: Sanofi-AventisInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Tak Adrien Li
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Publication number: 20090023750Abstract: The present invention relates to novel monohydrochloride, dihydrochloride, monohydrobromide, maleate and methanesulphonate salts of trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and/or their hydrates and/or solvates. Moreover, the invention relates to the process for preparing the salts and their hydrates and/or solvates, to their use in the treatment and/or prevention of conditions which require modulation of dopamine receptor and to pharmaceutical compositions containing them.Type: ApplicationFiled: May 9, 2008Publication date: January 22, 2009Applicant: RICHTER GEDEON NYRT.Inventors: Laszlo Czibula, Ferenc Sebok, Istvan Greiner, Gyorgy Domany
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Publication number: 20090012099Abstract: Disclosed is a method for use of phenyl sulfone compounds of formula (I) in the treatment of Alzheimer's disease and age related cognitive decline.Type: ApplicationFiled: September 11, 2008Publication date: January 8, 2009Inventors: Gregor James MacDonald, Mervyn Thompson
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Publication number: 20090012066Abstract: The present invention provides methods of treating and/or preventing pathologic cardiac hypertrophy and heart failure comprising administering hydroxamate compounds which are deacetylase inhibitors.Type: ApplicationFiled: August 9, 2006Publication date: January 8, 2009Inventors: Seigo Izumo, Suraj Shivappa Shetty
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Patent number: 7473692Abstract: The present invention relates to new D3 dopamine receptor subtype selectice ligands of formula (I) to pharmacological compositions containing the same and to their use in therapy and/or prevention of psychoses (e.g. schizophrenia, schizo-affective disorders, etc), drug (e.g. alcohol, cocaine and nicotine, opioids etc.) abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, amnesia, eating disorders (e.g. bulimia nervosa, etc.), attention deficit disorders, hyperactivity disorders in children, psychotic depression, mania, paranoid and delusional disorders, dyskinetic disorders (e.g. Parkinson's diseases, neuroleptic induced Parkinson's dissases, tardive dyskinesias) anxiety, sexual dysfunction, sleep disorders, emesis, aggression, autism, pain ophthalmological diseases (e.g. glaucoma etc.).Type: GrantFiled: September 25, 2002Date of Patent: January 6, 2009Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: János Galambos, Katalin Nógrádi, Éva Ágainé Csongor, György Miklós Keserü, István Vágó, György Domány, Béla Kiss, István Gyertyán, István Laszlovszky, Judit Laszy
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Patent number: 7465733Abstract: A compound selected from those of formula (I): wherein: R1, R2, R3 and R4, which may be the same or different, each represent an atom or group selected from hydrogen, halogen, alkyl, alkoxy, phenyl and cyano, X represents a bond, an oxygen atom or a group selected from —(CH2)m—, —OCH2— and —NR5—, wherein m represents 1 or 2, and R5 is as defined in the description, Y represents an oxygen atom or a group selected from NR7 and CHR8, wherein R7 and R8 are as defined in the description, Z represents a nitrogen atom or a CH group, n represents 1 or 2, Ak represents an alkylene chain, Ar represents an aryl or heteroaryl group, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medical products containing the same which are useful in the treatment of conditions requiring a serotonin reuptake inhibitor and/or NK1 antagonist.Type: GrantFiled: March 31, 2006Date of Patent: December 16, 2008Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Aimée Dessinges, Bertrand Goument, Mark Millan, Clotilde Mannoury La Cour
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Publication number: 20080300261Abstract: Compounds of formula I are useful in treatment of diseases associated with the deposition of ?-amyloid in the brain.Type: ApplicationFiled: July 19, 2005Publication date: December 4, 2008Inventors: Peter Blurton, Frank Burkamp, Ian Churcher, Timothy Harrison, Joseph Neduvelil
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Publication number: 20080293739Abstract: Disclosed are compounds and compositions that modulate T-cells. Such compounds can be used to treat T-cell mediated disease like T-ALL, rheumatoid arthritis, multiple sclerosis, and graft-vs-host disease (GvHD), to name but a few. The compounds have a general structure as shown in Formula I. Ar1-L-Ar2??I wherein Ar1 and Ar2, are independent of one another, a substituted aryl, unsubstituted aryl, substituted heteroaryl, or unsubstituted heteroaryl; and L is a bond or a linker spanning two, three, four, or five atoms.Type: ApplicationFiled: April 11, 2008Publication date: November 27, 2008Inventor: Nikolaus S. Trede
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Patent number: 7452891Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: January 28, 2005Date of Patent: November 18, 2008Assignee: Schering CorporationInventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
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Publication number: 20080279917Abstract: A method of combating infectious agents, such as Pneumocystis pneumonia, and a method of treating a subject in need of such treatment is disclosed. The method comprises administering to the subject a bis-benzamidoxime of formula (I) wherein the linker is a di-substituted cyclic moiety of any ring size and may contain at least one heteroatom; the aromatic group is 1,2-; 1,3-; or 1,4-disubstituted; R is selected from the group consisting of a hydrogen, a linear or branched alkyl group, containing from 1 to 20 carbon atoms; R? is selected from the group consisting of a hydrogen, a linear or branched alkyl group containing from one to twenty carbon atoms, an aromatic ring, a cycloalkyl group containing three to eight carbon atoms, or a hydroxyl group; alternatively, R and R? may form a cyclic structure that can be fused to another cyclic system; or a pharmaceutically acceptable salt thereof. Pharmaceutical formulations and active compounds useful in the practice of the present invention are also disclosed.Type: ApplicationFiled: November 24, 2004Publication date: November 13, 2008Inventors: Peter D. Walzer, Melanie T. Cushion, Annie Mayence, Tien Liang Huang, Jean Jacques Vanden Eynde
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Patent number: 7449466Abstract: This invention provides cyclicamino-phenyl sulfamate derivatives represented by a formula wherein each of R1 and R2 stands for hydrogen or lower alkyl; each of R3 and R4 stands for hydrogen, halogen, cyano or the like; A stands for nitrogen or CH; B stands for CH2, SO2, CO, optionally substituted phenyl or the like; and R5 stands for alkyl, phenyl, amino or the like, or salts thereof which exhibit excellent steroid sulfatase inhibitory activity and are useful for prevention or treatment of diseases associated with steroids such as estrogen, androgen and the like.Type: GrantFiled: May 7, 2004Date of Patent: November 11, 2008Assignee: Aska Pharmaceutical Co., Ltd.Inventors: Shigehiro Takegawa, Shigeki Iwashita, Makoto Okada, Takayoshi Nakagawa, Naoyuki Koizumi, Tomohito Fujii
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Publication number: 20080269248Abstract: A tartrate and malate salt of trans-1-(6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine, in particular for medical use, pharmaceutical formulations thereof, including for treatment of schizophrenia or other diseases involving psychotic symptoms.Type: ApplicationFiled: February 14, 2006Publication date: October 30, 2008Applicant: H. Lundbeck A/SInventors: Ole Nielsen, Heidi Lopez de Diego, Benny Bang-Andersen
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Publication number: 20080269237Abstract: This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula: The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.Type: ApplicationFiled: July 1, 2008Publication date: October 30, 2008Applicant: TOPOTARGET UK LIMITEDInventors: Clare J. WATKINS, Maria-Rosario Romero-Martin, James Ritchie, Paul W. Finn, Ivars Kalvinsh, Einars Loza, Klara Dikovska, Igor Starchenkov, Daina Lolya, Vija Gailite
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Patent number: 7442692Abstract: A compound selected from those of formula (I): wherein: R3 represents a hydrogen atom, and R1 and R2 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, or R1 represents a hydrogen atom, and R2 and R3 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, n represents 1 or 2, —X— represents a group selected from —(CH2)m—O-Ak-, —(CH2)m—NR4-Ak-, —(CO)—NR4-Ak- and —(CH2)m—NR4-(CO)—, m represents an integer between 1 and 6 inclusive, Ak represents an optionally substituted alkylene chain, and R4 represents a hydrogen atom or an alkyl group, Ar represents an aryl or heteroaryl group, its enantiomers, diasteroisomers, and addition salts thereof with a pharmaceutically acceptable acid.Type: GrantFiled: March 29, 2006Date of Patent: October 28, 2008Assignee: Les Laboratoires ServierInventors: Guillaume De Nanteuil, Bernard Portevin, Philippe Gloanec, Mark Millan, Jean-Claude Ortuno, Clotilde Mannoury La Cour, Alain Gobert
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Publication number: 20080260835Abstract: The present invention provides a pharmaceutical composition of a practically insoluble drug, wherein the composition may be administered with food or without food. The composition may be in the form of a solid dispersion of the practically insoluble drug and a polymer having acidic functional groups, and the composition may in vitro form a suspension.Type: ApplicationFiled: June 15, 2007Publication date: October 23, 2008Applicant: F H FAULDING & CO LIMITEDInventors: David HAYES, Angelo Mario Morella
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Patent number: 7439245Abstract: Disclosed is a method for use of phenyl sulfone compounds of formula (I) in the treatment of anxiety.Type: GrantFiled: May 13, 2008Date of Patent: October 21, 2008Assignee: Glaxo Group LimitedInventors: Gregor James MacDonald, Mervyn Thompson