The Other Ring Nitrogen Is Unsubstituted Or Alkyl Substituted Only, Or Salt Thereof Patents (Class 544/395)
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Patent number: 8008302Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: July 25, 2005Date of Patent: August 30, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Patent number: 7998963Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein Ar is indolyl, indazolyl or dihydroindolyl, and R1, R2, R3 and R4 are as defined herein. Also provided are pharmaceutical compositions, methods of using the compounds in the treatment of depressive, anxiolytic and other disorders associated with inhibition of the reuptake of norepinephrine, serotonin, and dopamine, and methods of preparing the compounds.Type: GrantFiled: February 12, 2009Date of Patent: August 16, 2011Assignee: Roche Palo Alto LLCInventors: David Scott Carter, Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
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Publication number: 20110172246Abstract: The invention relates to compounds of formula I: where a, and R1 through R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: January 10, 2011Publication date: July 14, 2011Inventors: Eric L. Stangeland, Lori Jean Patterson
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Patent number: 7968538Abstract: 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: GrantFiled: January 25, 2006Date of Patent: June 28, 2011Assignee: Galenea Corp.Inventors: Oren Becker, Rosa Melendez, Yael Marantz, Anurag Sharadendu, Merav Fichman, Mercedes Lobera, Hanoch Senderowitz, Srinivasa Rao Cheruku, Silvia Noiman, Xiang Y. Yu, Sharon Shacham, Laurence Wu, Ashis Saha, Pini Orbach, Dale S. Dhanoa
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Publication number: 20110144120Abstract: 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: ApplicationFiled: December 16, 2010Publication date: June 16, 2011Applicant: SANOFI-AVENTISInventors: Marco BARONI, Olaf RITZELER, Marco ZANCHET
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Publication number: 20110118464Abstract: The halogenated xanthine derivatives and the precursors thereof for anti-cancer and anti-metastasis activity and the preparation method thereof are provided. The halogenated xanthine derivatives can further be radio-labeled with the radioactive halide group. The growth of human prostate carcinoma, tongue squamous cell carcinoma, colon adenocarcinoma and lung carcinoma can be inhibited and arrested in G0/G1 phase by KMUP-2Cl (7-[2-[4-(chlorophenyl)-piperazinyl]ethyl]-1,3-dimethyl-8-chloroxanthine). In addition, the growth of human prostate carcinoma LNCaP can be inhibited by KMUP-1 (7-[2-[4-(2-chlorobenzene)-piperazinyl]-ethyl]-1,3-dimethyl-xanthine), and the LNCaP prostate cancer xenograft growth in nude mice is effectively inhibited by the intraperitoneal injection and per oral administration of KMUP-1.Type: ApplicationFiled: November 18, 2009Publication date: May 19, 2011Inventor: Ing-Jun Chen
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Patent number: 7910734Abstract: Salts and crystals of 1-cyclopropylmethyl-4-[2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine have excellent cell adhesion inhibitory action and cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis.Type: GrantFiled: December 16, 2005Date of Patent: March 22, 2011Assignee: Eisai R&D Management Co., Ltd.Inventors: Makoto Kotake, Naoki Yoneda, Katsunobu Osada
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Publication number: 20110065689Abstract: 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: ApplicationFiled: September 1, 2010Publication date: March 17, 2011Inventors: Terence P. Keenan, Alan P. Kaplan
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Patent number: 7897764Abstract: Thiourea compounds of the following formula: wherein n, R1, R2, R3, A1, A2, X, Y, and Z are defined herein. Also disclosed is a method of treating hepatitis C virus infection with these compounds.Type: GrantFiled: May 5, 2008Date of Patent: March 1, 2011Assignee: National Health Research InstitutesInventors: Jyh-Haur Chern, Tsu-An Hsu, Iou-Jiun Kang, Li-Wen Wang, Chung-Chi Lee, Yen-Chun Lee, Yu-Sheng Chao
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Publication number: 20110046376Abstract: A method for synthesizing a heterocyclic compound includes: reacting 1-methylpiperazine with 5-chloro-2-nitroaniline at an internal temperature sufficient to provide a compound of Formula VIH The 1-methylpiperazine and the 5-chloro-2-nitroaniline are reacted in a solvent that comprises water in an amount greater than 50 percent by volume based on the amount of the solvent and/or are reacted in a solvent that comprises an organic solvent component that has a boiling point of greater than 100° C. at atmospheric pressure.Type: ApplicationFiled: May 17, 2006Publication date: February 24, 2011Applicant: NOVARTIS AGInventors: Gabriel Galvin, Eric Harwood, David Ryckman, Shuguang Zhu
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Patent number: 7893261Abstract: A serotonin reuptake inhibitor which can be used in the treatment of depression and which has a decreased occurrence of unwanted side effects. The serotonin reuptake inhibitors are bi-functional organic molecules which combine serotonin transporter reuptake inhibition with serotonin (5-HT, such as 5-HT2A) receptor antagonism in one molecular entity. The serotonin-selective reuptake inhibitor (SSRI) homologue portion of the molecule shows an affinity to the serotonin reuptake transporter (SERT) and has antidepressant properties. The piperazine or piperidine portion of the molecule demonstrates an affinity to 5-HT receptors and restores the undesired side effects of SSRIs.Type: GrantFiled: March 28, 2005Date of Patent: February 22, 2011Assignee: Baylor UniversityInventors: Kevin G. Pinney, Maria Graciela Miranda, James Michael Dorsey
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Publication number: 20110014186Abstract: 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: March 23, 2009Publication date: January 20, 2011Inventors: Claus Ehrhardt, Leslie Wighton McQuire, Pascal Rigollier, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi
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Publication number: 20110009626Abstract: The present invention relates to an adenosine A3 receptor ligand of the general formula (VI?), (VII?) and (VIII?) and their preparation.Type: ApplicationFiled: August 11, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventors: Peter ARANYI, Sandor BATORI, Geza TIMARI, Kinga BOER, Zoltan KAPUI, Endre MIKUS, Katalin URBAN-SZABO, Katalin GERBER, Judit VARGANE SZEREDI, Michel FINET
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Publication number: 20100297240Abstract: 1-[2-(2,4-dimethylphenylsulphanyl)phenyl]piperazine exhibits potent activity on SERT, 5-HT3 and 5-HT1A and may as such be useful for the treatment of cognitive impairment, especially in depressed patients.Type: ApplicationFiled: June 15, 2007Publication date: November 25, 2010Applicant: H. Lundbeck A/SInventors: Benny Bang-Andersen, Andre Faldt, Arne Mork, Heidi Lopez De Diego, Rene Holm, Tine Bryan Stensbol, Lone Munch Ringgaard, Michael J. Mealy, Michael Harold Rock, Jorgen Brodersen, Morten Jorgensen, Nicholas Moore
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Publication number: 20100292221Abstract: 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 n is 1 or 2; R1 is hydrogen or methyl and is positioned vicinal to the radical R1; R2 is hydrogen or methyl; R3 is C1-C3 alkyl; R4 is hydrogen, C1-C4 alkyl, cyclopropyl, C3-C4 cycloalkylmethyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, chlorine, C1-C4 alkyl, fluorinated C1-C4 alkyl, C1-C4 alkoxy or fluorinated C1-C4 alkoxy; and R6 is hydrogen, fluorine or chlorine.Type: ApplicationFiled: April 29, 2010Publication date: November 18, 2010Applicants: 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
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Patent number: 7829713Abstract: 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: February 27, 2007Date of Patent: November 9, 2010Assignee: Helicon Therapeutics, Inc.Inventors: Terrence P. Keenan, Alan P. Kaplan
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Publication number: 20100256163Abstract: The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho,meta-disubstituted phenyl)-1-alkypiperidines and piperazines. wherein R1, R2, R3 and X are as defined.Type: ApplicationFiled: June 14, 2010Publication date: October 7, 2010Inventors: Clas Sonesson, Lars Swanson, Nicholas Ross Waters
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Patent number: 7790727Abstract: 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: GrantFiled: October 31, 2008Date of Patent: September 7, 2010Assignee: 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: 20100216808Abstract: Pyrazolo-quinazoline derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: December 17, 2007Publication date: August 26, 2010Applicant: Nerviano Medical Sciences S.r.lInventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Ronald Ferguson, Helena Posteri, Barbara Valsasina
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Publication number: 20100127210Abstract: A liquid crystal compound of Formula (I) is provided. In Formula (I), Y1, Y2 and Y3 are, independently, hydrogen, halogen, cyano or thiocyano, and R is C1-12 alkyl or C1-12 alkoxy, preferably C3-6 alkyl. The liquid crystal compound is colorless. The invention also provides a liquid crystal composition including the liquid crystal compound.Type: ApplicationFiled: March 9, 2009Publication date: May 27, 2010Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTEInventors: Peu-Jane Huang, An-Cheng Chen, Kung-Lung Cheng, Shih-Hsien Liu
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Patent number: 7642262Abstract: A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.Type: GrantFiled: December 3, 2004Date of Patent: January 5, 2010Assignee: Asubio Pharma Co., Ltd.Inventors: Hirokazu Annoura, Kyoko Nakanishi, Shigeki Tamura
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Publication number: 20090318389Abstract: The invention provides compounds formulae I-III, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.Type: ApplicationFiled: August 2, 2007Publication date: December 24, 2009Applicant: PRAECIS PHARMACEUTICALS INCORPORATEDInventors: Ghotas Evindar, Hongfeng Deng
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Publication number: 20090318696Abstract: A method of synthesizing a crystalline molecular sieve having an MSE framework type comprises crystallizing a reaction mixture comprising a source of water, a source of an oxide of a tetravalent element, Y, selected from at least one of silicon, tin, titanium, vanadium and germanium, a source of an alkali or alkaline earth metal, M, and a source of organic cations, Q, having the following general structure: in which R1 is hydrogen or an alkyl group, and R2 and R3 are alkyl groups.Type: ApplicationFiled: June 20, 2008Publication date: December 24, 2009Inventors: Karl G. Strohmaier, Simon C. Weston, James C. Vartuli, J. Thomas Ippoliti
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Patent number: 7622056Abstract: The invention relates to a high dielectric anisotropy liquid crystal compound which is a pyridyl derivative with substituents of electrons push-pull effect. Furthermore, the high dielectric anisotropy liquid crystal compounds are colorless and have high thermal and photo stability as well as high compatibility in a liquid crystal host. A liquid crystal composition containing the high dielectric anisotropy liquid crystal compound can reduce threshold voltage of cholesteric reflective displays, thus saving power and extending lifetime of driver ICs.Type: GrantFiled: December 3, 2007Date of Patent: November 24, 2009Assignees: Industrial Technology Research Institute, Daily Polymer CorporationInventors: Kung-Lung Cheng, Shih-Hsien Liu, Ann-Cheng Chen, Peu-Jane Haung, Chih-Lung Chin
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Patent number: 7612122Abstract: Compounds of formula (I): [where: the substituents R1 are individually selected from C1-C10 alkyl groups and optionally substituted benzyl groups; the substituents R2 are individually selected from alkyl groups or, together with the nitrogen atom to which they are attached, represent a nitrogen-containing heterocyclic group; Z is selected from C6-C10 arylene groups and groups of formula —(CHR3)n—, where R3 is hydrogen, hydroxy or a C1-C4 alkyl group, and n is 0 to 6; Y is carbonyl or —CH2—; Q is a residue of a mono- or poly-hydroxy compound; and x is 1 to 6; and esters thereof] are useful as multi-functional photoinitiators for use in coating compositions to be cured by radiant energy.Type: GrantFiled: November 9, 2005Date of Patent: November 3, 2009Assignee: Sun Chemical CorporationInventors: Shaun Lawrence Herlihy, Brian Rowatt, Robert Stephen Davidson
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Publication number: 20090203910Abstract: Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.Type: ApplicationFiled: December 11, 2008Publication date: August 13, 2009Inventors: Jason Chi-Chung Choy, Saul Jaime-Figueroa, Joseph M. Muchowski, Paul J. Wagner
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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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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: 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: 7452921Abstract: Compounds of formula (I) where: {R1 is methyl, ethyl, cycloalkyl or optionally substituted aryl; Z is arylene or a group of formula —(CHR4)n-, where R4 is hydrogen, hydroxy or alkyl, and n is a number from 0 to 6; Y is carbonyl or a —CH2— group; Q is a residue of a mono- or poly-hydroxyl compound having from I to 6 hydroxy groups; and x is a number from I to 6; and esters thereof} are useful as sensitizers for use in radiationcurable compositions.Type: GrantFiled: July 2, 2004Date of Patent: November 18, 2008Assignee: Sun Chemical CorporationInventors: Shaun Lawrence Herlihy, Brian Rowett, Robert Stephen Davidson
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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
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Patent number: 7417043Abstract: A 3-substituted 4-(phenyl-N-alkyl)-piperazine compound of the following formula: wherein R1 is selected from the group consisting of OSO2CF3, OSO2CH3, SO2R3, COCF3, COCH3 and COCH2CH3, wherein R3 is as defined hereafter; R2 is selected from the group consisting of C1-C4 alkyls, allyl, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl and 4,4,4-trifluorobutyl; R3 is selected from the group consisting of C1-C3 alkyls, CF3, and N(CH3)2; with the proviso that when R1 is SO2R3 and R3 is a C1-C3 alkyl, then R2 is not CH2CH2OCH3; or a pharmaceutically acceptable salt thereof are provided. Also, pharmaceutical compositions comprising the above compound and methods wherein the above compound is used for the treatment of various disorders are provided.Type: GrantFiled: December 21, 2004Date of Patent: August 26, 2008Assignee: NeuroSearch Sweden ABInventors: Clas Sonesson, Ingela Marianne Svan, legal representative, Anders Kristoffer Lilja, legal representative, Liselott Lilja Rönnqvist, legal representative, Jenny Maria Carlberg, legal representative, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
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Patent number: 7410971Abstract: 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 or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.Type: GrantFiled: December 24, 2004Date of Patent: August 12, 2008Assignee: Eisai R&D Management Co., Ltd.Inventors: Tetsuya Kawahara, Makoto Kotake, Naoki Yoneda, Shinsuke Hirota, Masayoshi Ohkuro
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Patent number: 7381728Abstract: The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Ra, Rb, Rc, Rd, Re, Rf and Y are as defined in the specification. The compounds are partial or full agonists at the growth hormone secretagogue (GHS) receptors. Pharmaceutical compositions comprising the compounds methods of preparing the compounds, uses of the compounds and methods involving the compounds are also provided.Type: GrantFiled: July 26, 2005Date of Patent: June 3, 2008Assignee: Glaxo Group LimitedInventors: David Kenneth Dean, Alessandra Gaiba, Nigel Paul King, Andrew Kenneth Takle, Jason Witherington
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Patent number: 7262188Abstract: This invention relates to novel phenyl sulfone compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.Type: GrantFiled: March 9, 2004Date of Patent: August 28, 2007Assignee: Glaxo Group LimitedInventors: Gregor James MacDonald, Mervyn Thompson
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Patent number: 7226925Abstract: The invention relates to compounds of the general Formula (I): The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of Formula (I).Type: GrantFiled: June 18, 2003Date of Patent: June 5, 2007Assignee: Biovitrum ABInventors: Björn M. Nilsson, Erik Ringberg, Birger Sjöberg, Mattias Jönsson
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Patent number: 7173035Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), 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: May 10, 2002Date of Patent: February 6, 2007Assignee: Biovitrum ABInventors: Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Lori Sutin, Andrew Mott, Jan Tejbrant
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Patent number: 7148238Abstract: 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: GrantFiled: December 6, 2005Date of Patent: December 12, 2006Assignee: H. Lundbeck A/SInventors: Thomas Ruhland, Benny Bang-Andersen, Ask Puschl
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Patent number: 7144884Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application.Type: GrantFiled: October 2, 2002Date of Patent: December 5, 2006Assignee: H. Lundbeck A/SInventors: Thomas Ruhland, Garrick Paul Smith, Benny Bang-Andersen, Ask Puschl, Ejner Knud Moltzen, Kim Andersen
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Patent number: 7138407Abstract: 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: GrantFiled: December 6, 2005Date of Patent: November 21, 2006Assignee: H. Lundbeck A/SInventors: Thomas Ruhland, Garrick Paul Smith, Benny Bang-Andersen, Ask Puschl, Ejner Knud Moltzen, Kim Andersen
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Patent number: 7037914Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.Type: GrantFiled: September 23, 2002Date of Patent: May 2, 2006Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
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Patent number: 6903120Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4,-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.Type: GrantFiled: December 22, 2000Date of Patent: June 7, 2005Assignee: A. Carlsson Research ABInventors: Clas Sonesson, Ingela Marianne Svan, Anders Kristoffer Lilja, Liselott Lilja Rönnqvist, Jenny Maria Carlberg, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
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Patent number: 6825202Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula (I): wherein Ar, R1, R2, R3 or R4 are as defined in the specification, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: August 9, 2002Date of Patent: November 30, 2004Assignee: Syntex (U.S.A.) LLCInventors: Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao
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Patent number: 6762300Abstract: Process for the preparation of 5-(1-piperazinyl)benzofuran-2-carboxamide in which, as intermediate step, 5-bromosalicylaldehyde or one of its derivatives is reacted in a transition metal-catalysed amination with R2-piperazine, in which R2 is as defined in claim 1.Type: GrantFiled: October 10, 2002Date of Patent: July 13, 2004Assignee: Merck Patent GmbHInventors: Andreas Bathe, Steffen Emmert, Bernd Helfert, Henning Boettcher
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Patent number: 6753429Abstract: Compounds of formula I: wherein A, B, D, and R are as defined herein and their agriculturally acceptable salts are disclosed as effective insecticides. In addition, compositions comprising an insecticidally effective amount of a compound of Formula I in admixture with at least one agriculturally acceptable extender or adjuvant and methods of controlling insects comprising applying said compositions to locus on crops where control is desired are disclosed. It is emphasized that this abstract is provided to comply with the rules requiring an abstract that will allow a searcher or other reader to quickly ascertain the subject matter of the technical disclosure. It is submitted with the understanding that it will not be used to interpret or limit the scope or meaning of the claims (see 37 C.F.R. 1.72(b)).Type: GrantFiled: August 29, 2001Date of Patent: June 22, 2004Assignee: FMC CorporationInventors: George Theodoridis, Edward Barron, Daniel H. Cohen, Ellen M. Crawford, Thomas G. Cullen, Hongyan Qi, Elizabeth Rowley, Syed F. Ali, Walter H. Yeager, Christina B. Duggan
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Patent number: 6727257Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: wherein A is which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: December 5, 2000Date of Patent: April 27, 2004Assignee: Synaptic Pharmaceutical CorporationInventors: Dhanapalan Nagarathnam, George Chiu, T. G. Murali Dhar, Wai C. Wong, Mohammad R. Marzabadi, Charles Gluchowski, Bharat Lagu, Shou Wu Miao
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Patent number: 6673799Abstract: This application relates to a piperazino-substituted novel cyanophenyl derivative in which a substituted carbamoyl or substituted sulfamoyl group having an aryl, heterocyclic or the like group that may have a substituent group is bonded to one nitrogen atom on the piperazine ring. The compound of this application has an anti-androgen action and is useful in preventing or treating prostatic cancer, benign prostatic hyperplasia and the like diseases.Type: GrantFiled: March 21, 2001Date of Patent: January 6, 2004Assignee: Yamanouchi Pharmaceutical Co. Ltd.Inventors: Nobuaki Taniguchi, Isao Kinoyama, Takashi Kamikubo, Akira Toyoshima, Kiyohiro Samizu, Eiji Kawaminami, Masakazu Imamura, Hiroyuki Moritomo, Akira Matsuhisa, Masaaki Hirano, Yoji Miyazaki, Eisuke Nozawa, Minoru Okada, Hiroshi Koutoku, Mitsuaki Ohta
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Patent number: 6608195Abstract: The present invention relates to a novel process for the preparation of a compound of formula I: wherein R1 is defined herein and compounds of formula II: wherein R1 and R2 are defined herein. Said compound of formula I is useful in the treatment of various central nervous system disorders including depression.Type: GrantFiled: August 29, 2002Date of Patent: August 19, 2003Assignee: Pfizer Inc.Inventors: Joseph P. Rainville, Terry G. Sinay, Stanley W. Walinsky
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Patent number: 6579870Abstract: The present invention provides pharmaceutically active compounds useful for the treatment of diseases or disorders of the central nervous system.Type: GrantFiled: June 8, 2001Date of Patent: June 17, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Eric Jon Jacobsen, Stephen J. King
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Patent number: 6525099Abstract: The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: January 23, 2001Date of Patent: February 25, 2003Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman