Chalcogen Attached Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 544/398)
  • Publication number: 20110021538
    Abstract: The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.
    Type: Application
    Filed: April 1, 2009
    Publication date: January 27, 2011
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Ashwin M. Krishnan, Tawfik Gharbaoui
  • Publication number: 20110009423
    Abstract: 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: Application
    Filed: February 4, 2010
    Publication date: January 13, 2011
    Applicant: H. Lundbeck A/S
    Inventors: Thomas Ruhland, Garrick P. Smith, Benny Bang-Andersen, Ask Puschl, Ejner K. Moltzen, Kim Andersen
  • Publication number: 20100326277
    Abstract: The present invention provides a novel piperazinium trifluoroacetate compound prepared by reacting piperazine with trifluoroacetic acid and a carbon dioxide absorbent prepared by dissolving the compound in an ionic liquid or organic solvent. According to the present invention, the carbon dioxide absorbent has excellent carbon dioxide absorption capacity and low solvent loss, and the energy consumption required for the carbon dioxide absorption and desorption is significantly reduced.
    Type: Application
    Filed: November 4, 2009
    Publication date: December 30, 2010
    Applicants: HYUNDAI MOTOR COMPANY
    Inventors: Sung Yeup Chung, Ki Chun Lee, Seok Jin Choi, Hoon Sik Kim, Jelliarko Palgunadi, Je Eun Kang
  • Publication number: 20100305116
    Abstract: The present invention relates to compounds comprising a cyclobutoxy group, processes for preparing them, phar-maceutical compositions comprising said compounds and their use as pharmaceuticals.
    Type: Application
    Filed: April 14, 2008
    Publication date: December 2, 2010
    Applicant: UCB PHARMA, S.A.
    Inventors: Sylvain Celanire, Frederic Denonne, Anne Valade
  • Patent number: 7834008
    Abstract: The present invention relates to cyclopropyl derivatives of formula (I) and salt thereof. These compounds are NK3 receptor antagonists and may therefore be useful for treatment of diseases where the NK3 receptor is implicated, e.g. psychotic disorders.
    Type: Grant
    Filed: August 13, 2004
    Date of Patent: November 16, 2010
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Tore Hansen, Anders Poulsen, Berith Bjørnholm, Thomas Ruhland, Morten Bang Nørgaard, Søren Møller Nielsen
  • Publication number: 20100286123
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: April 27, 2010
    Publication date: November 11, 2010
    Inventors: Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Nardos H. Teumelsan, Lihu Yang, Yuping Zhu, Shawn P. Walsh
  • Publication number: 20100286073
    Abstract: The present invention relates to compounds, as well as to compositions, methods and kits comprising such compounds, for use in the treatment or prophylaxis of fibromyalgia, chronic fatigue syndrome, myofascial pain syndrome, Gulf War syndrome and related conditions, wherein the compound is a fatty acid oxidation inhibitor and/or a carbohydrate oxidation activator.
    Type: Application
    Filed: October 3, 2008
    Publication date: November 11, 2010
    Inventor: Paul JENKINS
  • Publication number: 20100280014
    Abstract: The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein X is a bond or a group N—R4; R1 is hydrogen or methyl; R2 is hydrogen or methyl; R3 is hydrogen, C1-C3 alkyl, fluorine, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl, C3-C4 cycloalkyl, or C3-C4 cycloalkyl-CH2—; R5 is hydrogen, fluorine, chlorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R6 is hydrogen, fluorine or chlorine; and n is 1 or 2.
    Type: Application
    Filed: April 30, 2010
    Publication date: November 4, 2010
    Applicants: Abbott GmbH & Co. KG, Abbott Laboratories
    Inventors: Andreas Haupt, Frauke Pohlki, Karla Drescher, Karsten Wicke, Liliane Unger, Ana-Lucia Relo, Anton Bespalov, Barbara Vogg, Gisela Backfisch, Juergen Delzer, Min Zhang, Yanbin Lao
  • Publication number: 20100280188
    Abstract: The present invention relates to a compound represented by the following general formula (I): wherein R1 and R2 independently represent a monovalent hydrocarbon group; R3 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; X represents a divalent hydrocarbon group; and R4, R5 and R6 independently represent a monovalent organic group or a group represented by the following general formula (II): in which R7 and R8 independently represent a monovalent hydrocarbon group; and R9 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, with the proviso that R5 and R6 may combine together to form a divalent hydrocarbon group. The aforementioned compounds are useful as a polymerization inhibitor and the like.
    Type: Application
    Filed: December 16, 2008
    Publication date: November 4, 2010
    Inventors: Takeaki Saiki, Keiji Wakita, Yasushi Sugiura, Yoshinori Taniguchi
  • Publication number: 20100256162
    Abstract: Compounds of general formula (I) in which R1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Application
    Filed: October 10, 2006
    Publication date: October 7, 2010
    Applicant: AGY THERAPEUTICS, INC.
    Inventor: Connie L Sun
  • Publication number: 20100249411
    Abstract: In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process:
    Type: Application
    Filed: March 29, 2010
    Publication date: September 30, 2010
    Inventors: Wenxue Wu, Hongbiao Liao, David J.S. Tsai, David R. Andrews, Dinesh Gala, Gary M. Lee, Martin Lawrence Schwartz, Timothy L. McAllister, Xiaoyong Fu, Donal Maloney, Tiruvettipuram K. Thiruvengadam, Chou-Hang Tann
  • Patent number: 7781613
    Abstract: Disclosed are compounds of the general formula (I), with the definitions of the substituents R1 to R5, A and X being detailed in the text, and to their physiologically tolerated salts, to processes for preparing these compounds and to the use thereof as inhibitors of hormone-sensitive lipase (HSL).
    Type: Grant
    Filed: June 25, 2007
    Date of Patent: August 24, 2010
    Assignee: Sanofi-Aventis
    Inventors: Karl Schoenafinger, Stefan Petry, Guenter Mueller, Karl-Heinz Baringhaus
  • Patent number: 7767666
    Abstract: Certain substituted butyl and butynyl 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: Grant
    Filed: June 21, 2007
    Date of Patent: August 3, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: John M. Keith, Michael A. Letavic, Emily M. Stocking
  • Publication number: 20100137334
    Abstract: Compounds of general formula (Ia): in which R1, A1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Application
    Filed: January 22, 2007
    Publication date: June 3, 2010
    Inventors: Connie L. Sun, Xiaoyuan Li
  • Patent number: 7708907
    Abstract: 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: Grant
    Filed: March 9, 2009
    Date of Patent: May 4, 2010
    Assignee: Industrial Technology Research Institute
    Inventors: Peu-Jane Huang, An-Cheng Chen, Kung-Lung Cheng, Shih-Hsien Liu
  • Publication number: 20100105680
    Abstract: The present invention relates to substituted dimethylcyclobutyl compounds of general formula I, a process for their preparation, medicaments comprising said substituted dimethylcyclobutyl compounds as well as the use of said substituted dimethylcyclobutyl 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 sigma receptors.
    Type: Application
    Filed: August 3, 2007
    Publication date: April 29, 2010
    Inventors: Maria Rosa Cuberes Altisent, Jordi Corbera Arjona, Jorg Holenz, Rosa Maria Ortuno Mingarro, Sandra Izquierdo Salado
  • Publication number: 20100105908
    Abstract: The present invention describes a novel process for the preparation of levocetirizine and pharmaceutically acceptable acid addition salts thereof using diglycolic acid or derivatives thereof and new intermediates used in that process.
    Type: Application
    Filed: March 12, 2008
    Publication date: April 29, 2010
    Applicant: KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO
    Inventors: Jaroslav Tihi, Rok Zupet, Anica Pecavar, Ivanka Kolenc, Darja Pavlin
  • Publication number: 20100069378
    Abstract: The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.
    Type: Application
    Filed: July 25, 2007
    Publication date: March 18, 2010
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria de las Ermitas Alcalde-Pais, Maria de les Neus Mesquida-Estevez, Sara Lopez-Perez
  • Publication number: 20100035879
    Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Application
    Filed: May 29, 2009
    Publication date: February 11, 2010
    Inventors: Steven W. Elmore, Milan Bruncko, Cheol-Min Park
  • Patent number: 7645754
    Abstract: The subject invention provides compounds having the structure: wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(?O)NRaRb, —NRaRb, —NRaC(?O)NRaRb, —NRaC(?O)ORa, —OC(?O)NRaRb, or —NHC(?O) Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(?O)NRaRb, —NRaRb, —NRaC(?O)NRaRb, —NRaC(?O)ORa, —OC(?O)NRaRb, or —NHC(?O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH2)2OH or —CH2C(?O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxy, or —NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is —(CH2)mOR6, —CHNOR7, —C(?O)NR8R9, —(CH2)mC(?O)OR10, —(CH2)kC(?O)NR11R12; wherein R6 is a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl
    Type: Grant
    Filed: June 19, 2007
    Date of Patent: January 12, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig
  • Patent number: 7595399
    Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.
    Type: Grant
    Filed: February 4, 2004
    Date of Patent: September 29, 2009
    Assignee: Genentech, Inc.
    Inventors: David Y. Jackson, Frederick C. Sailes, Daniel P. Sutherlin
  • Patent number: 7589094
    Abstract: Disclosed are compounds of the formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
    Type: Grant
    Filed: December 7, 2005
    Date of Patent: September 15, 2009
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Andrea Gailunas, John A. Tucker, Ruth TenBrink, John Mickelson
  • Patent number: 7585858
    Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: May 26, 2005
    Date of Patent: September 8, 2009
    Assignee: Abbott Laboratories
    Inventors: Steven W. Elmore, Milan Bruncko, Cheol-Min Park
  • Publication number: 20090221607
    Abstract: Compounds of general formula (I) in which R1, A1, A2 and R2 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Application
    Filed: January 23, 2007
    Publication date: September 3, 2009
    Applicant: M's Science Corporation
    Inventors: Connie L. Sun, Xiaoyuan Li
  • Patent number: 7569691
    Abstract: A novel organoxysilane compound bearing a protected piperazino group is provided. It can impart rigidity, high mechanical strength, and transparency in the UV region when used in paints, adhesives and the like.
    Type: Grant
    Filed: April 19, 2006
    Date of Patent: August 4, 2009
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Yoichi Tonomura, Tohru Kubota
  • Patent number: 7553831
    Abstract: The present invention is disubstituted amines of formula (I) and disubstituted amines of formula (II) useful in treating Alzheimer's disease and other similar diseases.
    Type: Grant
    Filed: January 25, 2005
    Date of Patent: June 30, 2009
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: James Beck, Andrea Gailunas, Roy Hom, Barbara Jagodinska, Varghese John, Michael Maillaird
  • Publication number: 20090163462
    Abstract: The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
    Type: Application
    Filed: June 11, 2008
    Publication date: June 25, 2009
    Applicant: deCODE genetics, ehf
    Inventors: Vincent SANDANAYAKA, Jasbir Singh, Mark Gurney, Bjorn Mamat, Peng Yu, Louis Bedell, Lei Zhao, Rama K. Mishra
  • Publication number: 20090163496
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Application
    Filed: October 30, 2007
    Publication date: June 25, 2009
    Applicant: UNIVERSITY OF WASHINGTON
    Inventors: Niels H. ANDERSEN, Jason BOWMAN
  • Publication number: 20090149465
    Abstract: The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: December 10, 2008
    Publication date: June 11, 2009
    Inventors: Michael R. Leadbetter, Sean G. Trapp, Daniel D. Long, John R. Jacobsen, Sabine Axt
  • Publication number: 20090149464
    Abstract: Use of 1,4-bis(3-aminoalkyl)piperazine derivatives as defined in formula I or II for the manufacture of a pharmaceutical composition intended for the treatment of neurodegenerative diseases, related neurodegenerative diseases, developmental diseases or cancer. The instant invention is also directed to some specific 1,4-bis(3-aminoalkyl)piperazine derivatives and pharmaceutical composition including them.
    Type: Application
    Filed: November 8, 2005
    Publication date: June 11, 2009
    Applicants: UNIVERSITE DU DROIT ET DE LA SANTE- LILLE II, Institut National De La Sante Et De La Recherche Medicale (Inserm)
    Inventors: Nicolas Sergeant, Andre Delacourte, Patricia Melnyk, Luc Buee
  • Publication number: 20090143395
    Abstract: Compounds of general formula (I) in which R1 and R0 have any of the meanings given in the specification have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Application
    Filed: August 2, 2006
    Publication date: June 4, 2009
    Inventor: Connie L. Sun
  • Publication number: 20090137585
    Abstract: N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
    Type: Application
    Filed: February 3, 2009
    Publication date: May 28, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: David J. Augeri, Steven A. Baumeister, Milan Bruncko, Daniel A. Dickman, Hong Ding, Jurgen Dinges, Stephen W. Fesik, Philip J. Hajduk, Aaron R. Kunzer, William Mcclellan, David G. Nettesheim, Thorsten Oost, Andrew M. Petros, Saul H. Rosenberg, Wang Shen, Sheela A. Thomas, Xilu Wang, Michael D. Wendt
  • Publication number: 20090131419
    Abstract: Disclosed are sulphones which modulate the action of gamma-secretase. The compounds are useful in the treatment or prevention of Alzheimer's disease.
    Type: Application
    Filed: May 6, 2008
    Publication date: May 21, 2009
    Inventors: 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
  • Publication number: 20090082328
    Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 9, 2008
    Publication date: March 26, 2009
    Inventors: Yingfu Li, Joachim Rudolph, Jacques P. Dumas, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther
  • Publication number: 20090030007
    Abstract: The present invention relates to novel solvate and crystalline forms of carbamoyl-cyclohexane derivatives and, more particularly, to novel solvate and crystalline forms of trans-1{4-[2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-3,3-dimethyl-urea hydrochloride. Processes for the preparation of these forms, compositions containing these forms, and methods of use thereof are also described.
    Type: Application
    Filed: May 9, 2008
    Publication date: January 29, 2009
    Applicant: FOREST LABORATORIES HOLDINGS LIMITED
    Inventors: Xiangmin Liao, Haijian Zhu, Andreas Grill
  • Patent number: 7465733
    Abstract: 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: Grant
    Filed: March 31, 2006
    Date of Patent: December 16, 2008
    Assignee: Les Laboratoires Servier
    Inventors: Jean-Louis Peglion, Aimée Dessinges, Bertrand Goument, Mark Millan, Clotilde Mannoury La Cour
  • Patent number: 7442692
    Abstract: 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: Grant
    Filed: March 29, 2006
    Date of Patent: October 28, 2008
    Assignee: Les Laboratoires Servier
    Inventors: Guillaume De Nanteuil, Bernard Portevin, Philippe Gloanec, Mark Millan, Jean-Claude Ortuno, Clotilde Mannoury La Cour, Alain Gobert
  • Publication number: 20080261978
    Abstract: The invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula (I).
    Type: Application
    Filed: March 7, 2008
    Publication date: October 23, 2008
    Inventors: Michael P. Clark, Mark A. Lockwood, Florence F. Wagner, Michael G. Natchus
  • Publication number: 20080234282
    Abstract: Compounds of the following formula (I) wherein R1R2, n, Ar1 and A2 are as defined in the specification, in vivo-hydrolysable precursors thereof, pharmaceutically acceptable salts thereof, the use in therapy and pharmaceutical compositions and methods of treatment using the same. The example compounds are 1-(2-(naphthylmethoxy)-1-phenylethyl)piperazine derivatives. The compounds are neurokinin 1 (NK1) receptor antagonist and/or serotonin reuptake inhibitors, with medical indications for depression and other disorders.
    Type: Application
    Filed: March 21, 2008
    Publication date: September 25, 2008
    Applicant: ASTRAZENECA AB
    Inventor: Cathy Dantzman
  • Publication number: 20080176854
    Abstract: The present invention relates to nitro-substituted phenyl-piperazine compounds of general formula I, a process for their preparation, medicaments comprising said nitro-substituted phenyl-piperazine compounds as well as the use of said nitro-substituted phenylpiperazine 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: Application
    Filed: December 29, 2005
    Publication date: July 24, 2008
    Applicant: Laboratorios Del Dr. Esteve S.A
    Inventors: Andrea Aschenbrenner, Juergen Kraus, Stefan Tasler, Andreas Wuzik, Jordi-Ramon Quintana-Ruiz
  • Publication number: 20080176856
    Abstract: This invention relates to novel alkyl substituted piperazine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: June 14, 2005
    Publication date: July 24, 2008
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Jorgen Scheel-Kruger
  • Publication number: 20080171870
    Abstract: The present invention is directed to a novel process for the preparation of piperazinyl and diazepanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
    Type: Application
    Filed: December 10, 2007
    Publication date: July 17, 2008
    Inventors: Anusuya Choudhury, Jeffrey S. Grimm, Kirk L. Sorgi, David Palmer, Jing Liu
  • Publication number: 20080153826
    Abstract: The present invention is directed to substituted aryl cycloalkanoyl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
    Type: Application
    Filed: February 14, 2008
    Publication date: June 26, 2008
    Applicant: Wyeth
    Inventors: Eugene John Trybulski, Joseph Peter Sabatucci, An Thien Vu, Stephen Todd Cohn, Arthur Attilio Santilli, Lori Krim Gavrin, Fei Ye, Paige Erin Mahaney
  • Patent number: 7378446
    Abstract: The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its having a high degree of replication inhibitory activity against HCV, its production method, an intermediate compound useful for its production and a pharmaceutical composition containing these compounds, and the present invention relates to a compound represented by the formula (I): (wherein A represents —(CH2)n—, etc.; B represents —(C?O)—, etc.; D represents —(CH2)m—R?, etc.; E represents a hydrogen atom, etc.; G represents —(CH2)p-J, etc.; bond Q represents a single bond or double bond; and R1, R2 and R3 may be the same or different and each represent a hydrogen atom, etc.), a prodrug thereof or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 9, 2004
    Date of Patent: May 27, 2008
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Masayuki Sudoh, Takuo Tsukuda, Miyako Masubuchi, Kenichi Kawasaki, Takeshi Murata, Fumio Watanabe, Hiroshi Fukuda, Susumu Komiyama, Tadakatsu Hayase
  • Publication number: 20080113976
    Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
    Type: Application
    Filed: November 28, 2007
    Publication date: May 15, 2008
    Inventor: Percy H. Carter
  • Patent number: 7368448
    Abstract: Compounds of the following formula (I) wherein R1 R2, n, Ar1 and A2 are as defined in the specification, in vivo-hydrolysable precursors thereof, pharmaceutically acceptable salts thereof, the use in therapy and pharmaceutical compositions and methods of treatment using the same. The example compounds are 1-(2-(naphthylmethoxy)-1-phenylethyl)piperazine derivatives.
    Type: Grant
    Filed: April 6, 2005
    Date of Patent: May 6, 2008
    Assignee: AstraZeneca AB
    Inventor: Cathy Dantzman
  • Publication number: 20080004258
    Abstract: Certain substituted butyl and butynyl 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: Application
    Filed: June 21, 2007
    Publication date: January 3, 2008
    Inventors: John M. Keith, Michael A. Letavic, Emily M. Stocking
  • Patent number: 7307169
    Abstract: In some embodiments, this invention pertains to isotopically enriched N-substituted piperazines. In some embodiments, this invention pertains to methods for the preparation of isotopically enriched N-substituted piperazines.
    Type: Grant
    Filed: January 5, 2004
    Date of Patent: December 11, 2007
    Assignee: Applera Corporation
    Inventors: Darryl J. C. Pappin, Sasi Pillai, James M. Coull
  • Patent number: 7297697
    Abstract: A compound of formula I wherein X, Y, X? & Y? are selected from hydrogen, halogen, substituted or unsubstituted alkyl (linear, branched or cyclo), aryl, alkyloxy and haloalkyl group; R1, R2, R3 & R4 are selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: November 20, 2007
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Ajay Sohanlal Midha, Hemant Ashvinbhai Chokshi, Trinadha Rao Chitturi, Rajamannar Thennati
  • Patent number: 7285553
    Abstract: Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for treating sleep disorders, depression, and other psychiatric disorders, such as, schizophrenia, anxiety, obsessive compulsive disorder, circadian rhythm disorders, and centrally and peripherally mediated hypertension. Compositions and methods for their use are also disclosed.
    Type: Grant
    Filed: November 2, 2005
    Date of Patent: October 23, 2007
    Assignee: Alcon Manufacturing, Ltd.
    Inventors: Jesse A. May, Thomas R. Dean, Najam A. Sharif, Hwang-Hsing Chen