Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperazine Ring Patents (Class 514/255.01)
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Publication number: 20090176803Abstract: The present invention relates to compounds of general formula (I): wherein: R1 represents: halogen, CN or NO2; R2 represents: hydrogen or halogen; n represents: 1 or 2; R3 represents: phenyl substituted by one or more halogens or C1-C6 alkyls; or a cyclohexyl; as well as the therapeutically-acceptable salts or solvates thereof. These compounds are useful as protease-activated receptor-1 (PAR-1) antagonists, particularly in the treatment of thrombosis.Type: ApplicationFiled: June 19, 2007Publication date: July 9, 2009Inventors: Michel Perez, Marie Lamothe, Bruno Le Grand, Robert Letienne
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Publication number: 20090170870Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: December 12, 2008Publication date: July 2, 2009Inventors: YuHua Ji, Craig Husfeld, Rick Lee, YongQi Mu, Cameron Smith
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Publication number: 20090163508Abstract: An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. The present invention relates to a compound represented by formula (I): wherein symbols are as defined in the specification, or salt thereof.Type: ApplicationFiled: October 9, 2008Publication date: June 25, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni KORI, Mitsunori Kouno
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Publication number: 20090163480Abstract: The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.Type: ApplicationFiled: December 17, 2008Publication date: June 25, 2009Applicant: Dr. Karl Thomae GmbHInventors: Klaus RUDOLF, Wolfgang EBERLEIN, Wolfhard ENGEL, Helmut PIEPER, Henri DOODS, Gerhard HALLERMAYER, Michael ENTZEROTH, Wolfgang WIENEN
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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: 20090156611Abstract: The disclosure relates to compositions for and methods of inhibiting the mammalian Hedgehog signaling pathway.Type: ApplicationFiled: November 10, 2006Publication date: June 18, 2009Applicant: Licentia Ltd.Inventors: Antti Oinas, Jussi Taipale, Juhani Lahdenperä
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Publication number: 20090149448Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: November 22, 2005Publication date: June 11, 2009Applicant: ASTRAZENECA ABInventors: Lilian Alcaraz, Roger Victor Bonnert, Anthony Ronald Cook, Timothy Jon Luker, Rukhsana Tasneem Mohammed, Stephen Thom
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Patent number: 7544683Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: June 10, 2008Date of Patent: June 9, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Delphine Gaufreteau, Matthias Nettekoven, Jean-Marc Plancher, Olivier Roche, Sebastien Schmitt, Tadakatsu Takahashi
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Publication number: 20090143374Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, use in the reduction of A? peptide in vivo, use in modulating APP processing, and use in modulating the activity of APP secretase.Type: ApplicationFiled: December 8, 2008Publication date: June 4, 2009Inventors: Alan D. Snow, Qubai Hu, Judy A. Cam
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Publication number: 20090143365Abstract: 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: ApplicationFiled: December 15, 2008Publication date: June 4, 2009Applicant: SANOFI-AVENTISInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Tak Adrien Li
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Publication number: 20090137570Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: ApplicationFiled: January 28, 2009Publication date: May 28, 2009Applicant: IRM LLCInventors: Hong LIU, Arnab K. CHATTERJEE, David C. TULLY, Phillip B. ALPER, Badry BURSULAYA, Jianhua GUO, David H. WOODMANSEE, Daniel MUTNICK, Donald S. KARANEWSKY, Yun HE
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Publication number: 20090137562Abstract: Certain substituted benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.Type: ApplicationFiled: December 9, 2008Publication date: May 28, 2009Inventors: Brett Allison, Michael P. Curtis, Cheryl A. Grice, John M. Keith, Michael A. Letavic, Jennifer M.B. Miller, Emily M. Stocking
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Publication number: 20090131441Abstract: Metabolites of 2-(R)-4-isobutylarylpropionamides and pharmaceutical compositions containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: January 24, 2006Publication date: May 21, 2009Applicant: DOMPE phar.r.ma S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Marco Mosca, Marcello Allegretti, Francesco Colotta
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Publication number: 20090131452Abstract: The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I? and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl fluorinated C1-C2 alkyl C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine or chlorine.Type: ApplicationFiled: October 31, 2008Publication date: May 21, 2009Applicant: Abbott GmbH & Co. KGInventors: Wilfried Martin Braje, Sean Colm Turner, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Wolfgang Wernet, Matthias Mayrer, Ana Jongen-Relo, Anton Bespalov, Min Zhang
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Publication number: 20090131453Abstract: The invention relates to compounds of formula (I): processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.Type: ApplicationFiled: June 14, 2007Publication date: May 21, 2009Inventors: Jonathan Thomas Seal, Geoffrey Stemp, Mervyn Thompson, Susan Marie Westaway
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Patent number: 7534790Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.Type: GrantFiled: November 21, 2007Date of Patent: May 19, 2009Assignee: Cardiome Pharma Corp.Inventors: Allen I. Bain, Gregory N. Beatch, Cindy J. Longley, Bertrand M. C. Plouvier, Tao Sheng, Michael J. A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zolotoy
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Publication number: 20090118268Abstract: This invention relates to the use of a group of aryl ureas in treating p38 mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: October 10, 2008Publication date: May 7, 2009Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
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Publication number: 20090118303Abstract: A serotonin 5-HT3 receptor agonist containing a compound represented by the general formula (1) [R1, R3 and R5 represent hydrogen atom, a lower alkyl group, a lower alkenyl group, a halogen atom, hydroxyl group, amino group, a lower alkoxy group, carboxyl group, carbamoyl group, or nitro group, R2 and R4 represent a halogen atom, hydroxyl group, or amino group, R6 represents hydrogen atom, a lower alkyl group, or a lower alkenyl group, R7 represents hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aralkyl group, and m and n are integers of 1 to 3] or a physiologically acceptable salt thereof as an active ingredient and having both a serotonin 5-HT3 receptor antagonistic action and a serotonin 5-HT3 receptor activating action.Type: ApplicationFiled: December 29, 2008Publication date: May 7, 2009Applicant: Research Foundation Itsuu LaboratoryInventors: Tamaki JIKYO, Koichi SHUDO
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Publication number: 20090118169Abstract: A compound comprising the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: wherein N1 represents an atom to which a donative hydrogen atom in a hydrogen-bond donating group is bonded or a hydrogen-bond accepting atom in a hydrogen-bond accepting group; N3 represents a hydrogen-bond accepting atom in a hydrogen-bond accepting group; and N2, N4 and N5 independently represents an arbitrary carbon atom constituting a hydrophobic group and defined by the interatomic distances between N1, N2, N3, N4 and N5; and, in the optimized three-dimensional structure thereof, the distances between the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, in the optimized steric structure thereof, are the interatomic distances in a pharmacophore; or a salt thereof; inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases iType: ApplicationFiled: November 16, 2007Publication date: May 7, 2009Applicant: TOYAMA CHEMICAL CO., LTD.Inventors: Hisaaki Chaki, Tadakazu Takakura, Keiichi Tsuchida, Hironori Kotsubo, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
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Publication number: 20090118298Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.Type: ApplicationFiled: September 25, 2008Publication date: May 7, 2009Inventors: Dawn M. George, Lu Wang, Biqin Li, Anna M. Ericsson, Graham K. Ansell
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Publication number: 20090118269Abstract: Methods for using tetracycline compounds for the treatment of spinal muscular atrophy are described.Type: ApplicationFiled: April 14, 2008Publication date: May 7, 2009Inventors: Joel Berniac, Todd Bowser, Michael Draper, Stuart B. Levy, Mark L. Nelson
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Patent number: 7524848Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.Type: GrantFiled: March 22, 2007Date of Patent: April 28, 2009Assignee: Amgen Inc.Inventors: Jay P. Powers, Daqing Sun, Xuelei Yan
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Publication number: 20090105251Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: December 10, 2007Publication date: April 23, 2009Inventors: Benjamin Jones, Andrey A. Kiryanov, Stephen W. Kaldor
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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: 20090076020Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.Type: ApplicationFiled: August 21, 2008Publication date: March 19, 2009Applicant: ASTRAZENECA ABInventors: James Arnold, Todd Andrew Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
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Publication number: 20090075974Abstract: Disclosed is a pharmaceutical composition for prophylaxis and treatment of pancreatitis comprising a 5-HT2A receptor antagonist as an effective component, wherein the binding activity (pKi) of the 5-HT2A receptor antagonist to a 5-HT2A receptor is higher at least by 1.0 than the binding activities to a 5-HT2B receptor and a 5-HT2C receptor. Preferably the binding activity (pKi) of the 5-HT2A receptor antagonist to the 5-HT2A receptor is at least 7.0, and more preferably at least 8.0. The present invention also provides a method of identifying a candidate substance for prophylactic and therapeutic agent for pancreatitis, comprising determining whether a test substance has a 5-HT2A receptor antagonistic activity.Type: ApplicationFiled: April 27, 2006Publication date: March 19, 2009Applicant: UMN Pharma Inc.Inventors: Isamu Yamaguchi, Kentaro Hamada, Yasunari Kashihara
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Publication number: 20090069335Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: September 5, 2008Publication date: March 12, 2009Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20090062261Abstract: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: February 21, 2007Publication date: March 5, 2009Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Makoto Adachi, Hidenori Mikamiyama, Akira Matsumura, Naoki Tsuno
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Patent number: 7498436Abstract: This present invention relates to prodrug compounds of the formula (Y) and pharmaceutical salts thereof: where RN, R1, R2, R3R4 and RC are defined herein, which are useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: February 27, 2003Date of Patent: March 3, 2009Assignees: Pharmacia & Upjohn Company LLC, Elan Pharmaceuticals, Inc.Inventors: Varghese John, Barbara Jagodzinska, Michel Maillard, James P. Beck, Ruth E. TenBrink, Daniel Getman
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Publication number: 20090054438Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.Type: ApplicationFiled: August 15, 2008Publication date: February 26, 2009Applicant: Burnham Institute for Medical ResearchInventors: Ze'ev A. Ronai, Anindita Bhoumik, Nicholas D.P. Cosford, Russell Dahl
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Publication number: 20090048226Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1? converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), or interferon-?-(“IFN-?”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-? production and methods for treating interleukin-1, apoptosis-, and interferon-?-mediated diseases using the compounds and compositions of this invention.Type: ApplicationFiled: January 22, 2008Publication date: February 19, 2009Inventors: Marion W. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
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Patent number: 7491724Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.Type: GrantFiled: October 15, 2004Date of Patent: February 17, 2009Assignee: Incyte CorporationInventors: Yun-Long Li, Jincong Zhuo, David Burns, Wenqing Yao, Ravi Kumar Jalluri
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Publication number: 20090042907Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.Type: ApplicationFiled: June 20, 2008Publication date: February 12, 2009Applicants: Cephalon, Inc., Cephalon FranceInventors: Edward R. Bacon, Sankar Chatterjee, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet
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Publication number: 20090042855Abstract: In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, 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: June 3, 2008Publication date: February 12, 2009Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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Publication number: 20090042883Abstract: The present invention provides a therapeutic agent for a tumor selected from a hematopoietic tumor and a solid tumor which comprises, as an active ingredient, a benzoyl compound represented by General Formula (I): (wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONR7R8 or the like; R2 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R3 and R5 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl or the like; R4 represents a hydrogen atom, hydroxy or halogen; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl or the like), a prodrug thereof or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 21, 2006Publication date: February 12, 2009Applicant: KYOWA HAKKOKOGYO CO.Inventors: Yutaka Kanda, Shiro Soga, Takayuki Nakashima, Shinji Nara, Hiroshi Nakagawa, Yukimasa Shiotsu
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Publication number: 20090035292Abstract: Disclosed herein are methods of treating neuroblastomas and medulloblastomas in a subject comprising administering to the subject a phosphatase ligand in an amount effective to treat the subject. Also disclosed herein are method of treating neuroblastomas and medulloblastomas in a subject comprising administering to the subject a histone deacteylase ligand in an amount effective to treat the subject.Type: ApplicationFiled: August 1, 2008Publication date: February 5, 2009Inventors: John S. Kovach, Zhengping Zhuang
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Patent number: 7485646Abstract: A serotonin 5-HT3 receptor agonist containing a compound represented by the general formula (1) [R1, R3 and R5 represent hydrogen atom, a lower alkyl group, a lower alkenyl group, a halogen atom, hydroxyl group, amino group, a lower alkoxy group, carboxyl group, carbamoyl group, or nitro group, R2 and R4 represent a halogen atom, hydroxyl group, or amino group, R6 represents hydrogen atom, a lower alkyl group, or a lower alkenyl group, R7 represents hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aralkyl group, and m and n are integers of 1 to 3] or a physiologically acceptable salt thereof as an active ingredient and having both a serotonin 5-HT3 receptor antagonistic action and a serotonin 5-HT3 receptor activating action.Type: GrantFiled: September 8, 2005Date of Patent: February 3, 2009Assignee: Research Foundation Itsuu LaboratoryInventors: Tamaki Jikyo, Koichi Shudo
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Publication number: 20090030015Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) or (IIa) or (IIb) and a pharmaceutically acceptable carrier wherein the symbols and substituents have the following meaning —X— is e.g. and Y being e.g. or the pharmaceutically acceptable salts can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.Type: ApplicationFiled: September 20, 2006Publication date: January 29, 2009Applicant: REVOTAR BIOPHARMACEUTICALS AGInventors: Remo Kranich, Ewald M. Aydt, Anke S. Busemann
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Publication number: 20090023718Abstract: The present invention relates to a novel class of hydroxamic acid derivatives having a diamine or iminodiacetic acid backbone. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively including terminal differentiation, arresting cell growth and/or apoptosis of neo-plastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compound of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: November 23, 2004Publication date: January 22, 2009Applicant: Aton Pharma, Inc.Inventors: Thomas A. Miller, David J. Witter, Sandro Belvedere
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Publication number: 20090023711Abstract: Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: wherein Ar1, Ar2, A, X, Y, m, n and R1, R2, R3, R4 and R5 are as described in the specification, processes for their preparation, pharmaceutical formulations comprising them and their use in therapy, particularly in the therapy of neurological and psychiatric disorders associated with glutamate dysfunction.Type: ApplicationFiled: January 5, 2007Publication date: January 22, 2009Applicant: AstraZeneca ABInventors: Abdelmalik Slassi, Methvin Isaac, Jalaj Arora, Dean Brown
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Patent number: 7479493Abstract: Certain substituted benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.Type: GrantFiled: June 21, 2007Date of Patent: January 20, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Brett Allison, Michael P. Curtis, Cheryl A. Grice, John M. Keith, Michael A. Letavic, Jennifer M. B. Miller, Emily M. Stocking
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Publication number: 20090018143Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.Type: ApplicationFiled: November 8, 2007Publication date: January 15, 2009Applicants: Cephalon, Inc., Cephalon FranceInventors: Brigitte Lesur, Philippe Louvet, Rabindranath Tripathy
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Publication number: 20090018141Abstract: Provided herein are Compounds having the following structure: wherein A, L, X and ring B are as defined herein, compositions comprising an effective amount of a Compound and methods for treating or preventing cancer, hypoxia, diabetes, stroke, autoimmune disease or a condition treatable or preventable by inhibition of Chk2, the ATM-Chk2 pathway or RSK2 comprising administering an effective amount of a Compound to a patient in need thereof.Type: ApplicationFiled: June 9, 2008Publication date: January 15, 2009Inventors: Robert Shoemaker, John Cardellina, Michael Currens, Sudhir Kondapaka, Yves Pommier, Andy Jobson, Dominic Scudiero, David Waugh, George Lountos, Charles M. Cook, Guangtao Zhang, Andrew Colasanti, Christopher R. Self, Janet Cicariello Cook
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Publication number: 20090018142Abstract: This invention provides a method of treating a patient suffering from a tumor overexpressing N—CoR comprising administering to the patient a phosphatase ligand, alone or in combination with a retinoid receptor ligand, a histone deacetylase ligand, or both, in amounts effective to treat the patient. This invention also provides a method of inhibiting tumor growth in a patient suffering from a tumor overexpressing N—CoR. This invention further provides a method of identifying a compound or a mixture of compounds capable of inducing differentiation of cells of a tumor overexpressing N—CoR. This invention still further provides a method of determining the likelihood of successfully treating a subject suffering from a tumor overexpressing N—CoR. This invention also provides a method of assessing the likelihood that a patient is suffering from a tumor overexpressing N—CoR.Type: ApplicationFiled: February 6, 2007Publication date: January 15, 2009Inventors: Zhengping Zhuang, Edward H. Oldfield, Deric M. Park, Irina Lubensky, Jie Li, John S. Kovach
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Publication number: 20090012086Abstract: The invention relates to the use of substance P antagonists and, in particular, the use of non-peptidic NK1 receptor antagonists for the treatment of cancer and, more specifically, human melanoma, neuroblastoma, glioma, human Hodgkin's lymphoma KM-H2, lymphoblastic leukaemia, human rhabdomyosarcoma, human breast carcinoma, human Burkitt's lymphoma, human lung carcinoma, human Ewing's sarcoma, human glioma and human osteosarcoma.Type: ApplicationFiled: February 10, 2005Publication date: January 8, 2009Inventor: Miguel Munoz Saez
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Publication number: 20090005380Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: June 10, 2008Publication date: January 1, 2009Inventors: Delphine Gaufreteau, Matthias Nettekoven, Jean-Marc Plancher, Olivier Roche, Sebastien Schmitt, Tadakatsu Takahashi
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Publication number: 20080318958Abstract: Pharmaceutical compositions for enhancing the expression of apoAI are provided, which are used as medicaments for treatment of cardiovascular diseases on the basis of improving the functions of HDL. Pharmaceutical compositions for enhancing the expression of apoAI which comprises a compound of formula (I): in which X1 and X1 are independently an aryl or heteroaryl that may be optionally substituted, a hydrogen, a halogen, or the like; ring A is a benzene ring or 6-membered aromatic heterocyclic ring containing 1 to 3 N atoms that may be optionally condensed with another aromatic ring; R1 to R4 are independently a hydrogen, a halogen, a lower alkyl, a lower alkoxy or the like; a prodrug thereof, a pharmaceutically acceptable salt or solvate of them are disclosed.Type: ApplicationFiled: August 15, 2008Publication date: December 25, 2008Inventors: Natsuki Ishizuka, Katsunori Sakai, Kunio Hayashi
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Publication number: 20080318945Abstract: This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted piperazines, according to Formula I A compound of formula I wherein Z is bond or NH; R1 is aryl or optionally substituted heteroaryl; R2 is H, optionally substituted C1-6alkyl, or optionally substituted C2-6alkenyl; R3 and R7 are independently H, optionally substituted C1-6alkyl, or aryl; R4 is H or optionally substituted C1-6alkyl; R5 is H or C1-6alkyl; R6 is H or C1-6alkyl; and X and X? are independently O or H2; or wherein R3 and R4 together form a part of morpholinyl, piperadinyl, or aziridinyl ring; and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: December 15, 2006Publication date: December 25, 2008Inventors: Linda N. Casillas, Robert W. Marquis, JR.
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Publication number: 20080317806Abstract: A compound of Formula (A), wherein R1 is C1-C5 alkyl, C3-C6 branched alkyl, C4-C7 cycloalkyl, C8-C12 fused or bridged polycycloalkyl, or heterocyclic ring, where any of the preceding alkyl, cycloalkyl or heterocyclic ring groups may be singly or multiply substituted with X; R2 is H or R1; and X is halo, carbonyl carboxylic acid, carboxylic ester, carboxamide, substituted carboxamide, hydroxy, alkoxy, thioalkyl, sulphoxide, sulphone, sulphonamide, substituted sulphonamide, phenoxy, substituted phenoxy, phenyl, substituted phenyl, amino, substituted amino (including quaternary ammonium salts), N-oxide, imino, 5-7 membered heterocycle, or substituted heterocycle.Type: ApplicationFiled: April 11, 2006Publication date: December 25, 2008Applicant: Murdoch UniversityInventors: Wayne Morris Best, Colette Gloria Sims, Richard Christopher Andrew Thompson, Simon Andrew Reid, Anthony Armson, James Alexander Reynoldson
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Publication number: 20080312231Abstract: Substituted sulfonamide compounds corresponding to formula I pharmaceutical compositions comprising them, a process for preparing them, and the use of such compounds to treat or inhibit pain and other disorders or disease states.Type: ApplicationFiled: April 30, 2008Publication date: December 18, 2008Applicant: Gruenenthal GmbHInventors: Beatrix MERLA, Stefan Oberboersch, Melanie Reich, Bernd Sundermann, Werner Englberger, Timo Struenker, Ruth Jostock, Sabine Hees, Edward Bijsterveld, Fritz Theil, Heinz Graubaum