Phenyl Or Naphthyl Bonded Directly To Ring Nitrogen Of The Piperazine Ring Patents (Class 544/392)
  • Patent number: 9533967
    Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: January 3, 2017
    Assignee: VERSEON CORPORATION
    Inventors: Kevin Michael Short, Son Minh Pham, David Charles Williams, Somalee Datta
  • Patent number: 9273027
    Abstract: Provided are opioid receptor antagonists represented by the formula (I) where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: March 1, 2016
    Assignee: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. Carroll, Juan P. Cueva, James B. Thomas, S. Wayne Mascarella, Scott P. Runyon
  • Publication number: 20150105399
    Abstract: Disclosed in the present invention is a 3-cyanoanilinoalkylarylpiperazine derivatives and use thereof in preparing drugs; the 3-cyanoanilinoalkylarylpiperazine derivatives disclosed by the present invention has very useful pharmaceutical properties and good tolerance, especially the use as novel analgesic drugs, novel antidepressants, and novel analgesic and antidepressive drugs. This class of compounds are central analgesics regulating 5-hydroxytrptamine, and also are novel antidepressants regulating 5-hydroxytrptamine. This class of compounds also has less toxic and side effects and a higher safety range.
    Type: Application
    Filed: April 9, 2013
    Publication date: April 16, 2015
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Yali Li, Xiangqing Xu, Xiaowen Chen, Shicheng Liu, Song Zhao, Minquan Yu
  • Patent number: 8946228
    Abstract: The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof, and methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: February 3, 2015
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Pierre André Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J. M. De Waepenaert, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
  • Patent number: 8927546
    Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z 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 and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.
    Type: Grant
    Filed: September 22, 2010
    Date of Patent: January 6, 2015
    Assignee: Dart Neuroscience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
  • Publication number: 20140378473
    Abstract: This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: COGNITION THERAPEUTICS, INC.
    Inventors: Susan M. Catalano, Gilbert Rishton, Nicholas J. Izzo
  • Patent number: 8883796
    Abstract: Provided are biphenyl derivatives exhibiting activity towards central nervous system diseases by acting on the 5-HT7 receptor, pharmaceutically acceptable salts thereof, a method for preparing the compounds and pharmaceutical compositions including the compounds as an active ingredient.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: November 11, 2014
    Assignee: Korea Institute of Science and Technology
    Inventors: Hyunah Choo, Young-Jae Kim, Jeeyeon Kim, Mi Young Yeom
  • Patent number: 8809381
    Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: August 19, 2014
    Assignees: The University of Mississippi, L'Universite Catholique de Louvain
    Inventors: Christopher R. McCurdy, Christophe Mesangeau, Sanju Narayanan, Rae Reiko Matsumoto, Jacques Henri Poupaert
  • Publication number: 20140228568
    Abstract: Provided are biphenyl derivatives exhibiting activity towards central nervous system diseases by acting on the 5-HT7 receptor, pharmaceutically acceptable salts thereof, a method for preparing the compounds and pharmaceutical compositions including the compounds as an active ingredient.
    Type: Application
    Filed: February 8, 2013
    Publication date: August 14, 2014
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Hyunah CHOO, Young-Jae KIm, Jeeyeon KIM, Mi Young YEOM
  • Patent number: 8778949
    Abstract: 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: Grant
    Filed: January 10, 2011
    Date of Patent: July 15, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric L. Stangeland, Lori Jean Patterson
  • Publication number: 20140163228
    Abstract: The present invention relates to molecular sieves having the structure of ITQ-32 is synthesized from a reaction mixture substantially free of fluoride ions and comprising 4,4-dimethyl, 1-cyclohexyl-piperazinium cations in its pore structure, as well as methods of making such molecular sieves and methods of using them.
    Type: Application
    Filed: November 12, 2013
    Publication date: June 12, 2014
    Applicant: EXXONMOBIL RESEARCH AND ENGINEERING COMPANY
    Inventors: Allen W. Burton, Simon C. Weston, Karl G. Strohmaier, Hilda B. Vroman
  • Patent number: 8710059
    Abstract: The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: April 29, 2014
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Andreas Haupt, Frauke Pohlki, Liliane Unger, Ana Lucia Relo, Karsten Wicke, Min Zhang
  • Patent number: 8686136
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: April 1, 2014
    Assignee: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Xiaohong Song, Xilu Wang, Michael Wendt
  • Publication number: 20140057889
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • Publication number: 20140057890
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • Publication number: 20140030189
    Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.
    Type: Application
    Filed: June 12, 2013
    Publication date: January 30, 2014
    Inventors: Ajay Purohit, Thomas D. Harris, Heike S. Radeke, Simon P. Robinson, Ming Yu, David S. Casebier, Michael T. Azure
  • Patent number: 8633197
    Abstract: The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof, and methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
    Type: Grant
    Filed: June 5, 2008
    Date of Patent: January 21, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Pierre André Marc Bongartz, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Christophe Francis Robert Nestor Buyck
  • Patent number: 8624027
    Abstract: The present disclosure relates to a combination of therapeutic agents for use in treating a patient a subject suffering from cancer. In addition, the present disclosure also relates to diagnostic assays useful in classification of patients for treatment with one or more therapeutic agents.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: January 7, 2014
    Assignee: AbbVie Inc.
    Inventors: Omar Jameel Shah, Yu Shen, Xiaoyu Lin, Mark Anderson, Xiaoli Huang, Junling Li, Leiming Li
  • Patent number: 8569071
    Abstract: The present teachings provide methods for analyzing one or more amine-containing compounds in one or more samples using isobaric labels and parent-daughter ion transition monitoring (PDITM). In various embodiments, the methods comprise the steps of: (a) labeling one or more amine-containing compounds with different isobaric tags from a set of isobaric tags, each isobaric tag comprising a reporter ion portion; (b) combining at least a portion of each of the isobarically labeled amine-containing compounds to produce a combined sample; (c) subjecting at least a portion of the combined sample to PDITM; (d) measuring the ion signal of one or more of the transmitted reporter ions; and (e) determining the concentration of one or more of the isobarically labeled amine-containing compounds based at least on a comparison of the measured ion signal of the corresponding reporter ion to one or more measured ion signals of a standard compound.
    Type: Grant
    Filed: September 8, 2009
    Date of Patent: October 29, 2013
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subodh B. Nimkar, Subhasish Purkayastha, Darryl Pappin, Scott Daniels
  • Patent number: 8569496
    Abstract: The invention relates to novel trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate and a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the steps a) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)amino]-cyclohexyl}-acetic acid ester with sodium borohydride and aluminum trichloride to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethanol; b) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-ethanol obtained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate; c) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate obtained with 2,3-dichlorophenyl-piperazine in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carb
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: October 29, 2013
    Assignee: Richter Gedeon Nyrt.
    Inventors: Laszlo Czibula, Eva Againe Csongor, Katalin Nogradi, Balint Juhasz, Ferenc Sebok, Janos Galambos, Istvan Vago
  • Patent number: 8569495
    Abstract: This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments.
    Type: Grant
    Filed: December 16, 2008
    Date of Patent: October 29, 2013
    Assignee: Intervet International B.V.
    Inventors: Christophe Pierre Alain Chassaing, Jörg Schröder, Thomas Simon Ilg, Manfred Uphoff, Thorsten Meyer
  • Publication number: 20130281462
    Abstract: Disclosed herein are compounds (for example, diamidine derivatives and prodrugs) and methods of use thereof, for example in treating muscular dystrophy (DM) or disease caused by a toxic RNA in a subject. In some embodiments, the methods include administering an effective amount of one of more of the disclosed compounds to a subject to treat or inhibit DM or a disease caused by or associated with toxic RNA, such as DM1, DM2, spinocerebellar ataxia type 8 (SCA8), fragile X tremor ataxia syndrome (FXTAS), or Huntington disease-like 2 (HLD2). In some examples, the methods include selecting a subject for treatment, for example selecting a subject with DM1, DM2, SCA8, FXTAS, or HLD2.
    Type: Application
    Filed: April 19, 2013
    Publication date: October 24, 2013
    Applicants: University of Oregon
    Inventor: State of Oregon, acting by and through the State Board of Higher Education, on behalf of the University of Oregon
  • Publication number: 20130274270
    Abstract: Polymorphs of 3-chloro-4[(2R)-2-(4-chlorophenyl)-4-[(1R)-1-(4-cyanophenyl)ethyl]-1-piperazinyl]-benzonitrile are disclosed, as well as pharmaceutical compositions comprising said polymorphs, methods of using the polymorphs, and a process for preparing them.
    Type: Application
    Filed: December 21, 2011
    Publication date: October 17, 2013
    Inventors: Monika Brink, Hans-Peter Niedermann, Marcus Knell, Tao Feng, Scott T. Trzaska, Arthur J. Cooper, Shaileshkumar Ramanial Desai, Vinayak Keshav Gore
  • Publication number: 20130225561
    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: October 21, 2011
    Publication date: August 29, 2013
    Inventors: Haifeng Tang, Alexander Pasternak, Lihu Yang, Shawn P. Walsh, Barbara Pio, Aurash Shahripour, Nardos Teumelsan
  • Patent number: 8513253
    Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: August 20, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
  • Publication number: 20130209483
    Abstract: The disclosure relates to cannabinoid derivative compounds, pharmaceutical compositions made thereof, and methods for treating various diseases and disorders including cancer.
    Type: Application
    Filed: November 30, 2012
    Publication date: August 15, 2013
    Applicant: SUTTER WEST BAY HOSPITALS
    Inventor: SUTTER WEST BAY HOSPITALS
  • Patent number: 8501763
    Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
    Type: Grant
    Filed: March 10, 2008
    Date of Patent: August 6, 2013
    Assignee: The Scripps Research Institute
    Inventors: Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
  • Patent number: 8492163
    Abstract: This invention pertains to methods, mixtures, kits and compositions pertaining to analyte determination by mass spectrometry using labeling reagents that comprise a nucleophilic reactive group that reacts with a functional group of an analyte to produce a labeled analyte. The labeling reagents can be used as isobaric sets, mass differential labeling sets or in a combination of isobaric and mass differential labeling sets.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: July 23, 2013
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subhasish Purkayastha, Subhakar Dey, Scott B. Daniels
  • Publication number: 20130115168
    Abstract: One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to arylammonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the ammonium compound is a tetraaryl ammonium salt. Another aspect of the invention relates to arylsulfonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the sulfonium compound is a triaryl sulfonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.
    Type: Application
    Filed: September 4, 2012
    Publication date: May 9, 2013
    Applicant: The General Hospital Corporation
    Inventors: David R. Elmaleh, Alan J. Fischman, Timothy M. Shoup
  • Patent number: 8431699
    Abstract: There is provided a method for manufacture of 2-oxoimidazolidines of Formula I comprising one or more of the steps of converting an amine to an acylation agent, condensation of the acylation agent with a bi-functional compound of structure L-C(R4)(R5)—C(R2)(R3)—NHR1, wherein L is a leaving group, and ring closure of the resulting urea. In this manner, certain 2-oxoimidazolidines may be manufactured that are useful intermediates for the production of Pramiconazole and structurally related compounds.
    Type: Grant
    Filed: March 1, 2010
    Date of Patent: April 30, 2013
    Assignee: Vertichem Corporation
    Inventors: John R. Peterson, Christopher M. Yost
  • Patent number: 8354404
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Grant
    Filed: April 25, 2011
    Date of Patent: January 15, 2013
    Assignee: Abbott Laboratories
    Inventors: Milan Bruncko, Hong Ding, Steven Elmore, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Andrew Petros, Xiaohong Song, Xilu Wang, Noah Tu, Michael Wendt, Alexander Shoemaker, Michael Mitten
  • Patent number: 8343967
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: January 1, 2013
    Assignee: Abbott Laboratories
    Inventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
  • Publication number: 20120295919
    Abstract: Provided are opioid receptor antagonists represented by the formula (I) where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.
    Type: Application
    Filed: October 12, 2010
    Publication date: November 22, 2012
    Applicant: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. Carroll, Juan P. Cueva, James B. Thomas, S. Wayne Mascarella, Scott P. Runyon
  • Patent number: 8309587
    Abstract: The present invention relates to piperidine and piperazine phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: November 13, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Esther Ann Martinborough, Lev Tyler Dewey Fanning, Urvi Jagdishbhai Sheth, Dean Mitchell Wilson, Andreas P. Termin, Timothy Donald Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
  • Patent number: 8287969
    Abstract: An isosorbide derivative of Formula (I) is provided. In Formula (I), Z is —CH2—CH2—, —CH?CH—, —C?C—, —CH2—O—, —CH2—S—, —CH?N—O—, —CO—O—, —CO—S—, single bond, -ph-, —CO—O-ph- or —CO—O-ph-CO—O—, and ph represents benzene, R1 and R2 are, independently, C1-25 alkyl, —CN, —NCS, —CX3 or —OCX3, and X represents halogen, and m and n are, independently, 0, 1 or 2. The invention also provides a liquid crystal display including the isosorbide derivative.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: October 16, 2012
    Assignee: Industrial Technology Research Institute
    Inventors: Chun-Ming Wu, Kevin Lin, Shih-Hsien Liu, Chih-Lung Chin, An-Cheng Chen, Kung-Lung Cheng, Chien-Hsien Cheng
  • Patent number: 8227604
    Abstract: Hybrid compounds containing an aminotetralin moiety or a heterocyclic and/or open chain analog thereof linked through an alkylene group to an aryl ring system-substituted piperidiene moiety exhibit high levels of CNS activity, in some cases exhibiting especially high relative binding efficiencies between D3 and D2 dopaminergic receptor subtypes.
    Type: Grant
    Filed: April 29, 2010
    Date of Patent: July 24, 2012
    Assignee: Wayne State University
    Inventor: Aloke K. Dutta
  • Patent number: 8188077
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: March 16, 2011
    Date of Patent: May 29, 2012
    Assignee: Abbott Laboratories
    Inventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
  • Patent number: 8158790
    Abstract: The present invention provides an excellent antihypertensive medicament. The medicament of the present invention comprises a compound having the general formula (I) and the like: [wherein R1: H, substitutable alkyl, substitutable alkenyl, substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; R2: H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R3, R4; H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R5, R6: H, substitutable alkyl, substitutable cycloalkyl, substitutable alkoxy or the like; R7, R8: H, substitutable alkyl, substitutable cycloalkyl or the like; X: the formula (II) or the like; A: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; Y: a single bond, substitutable alkylene, substitutable alkenylene, —(CH2)a—X1—(CH2)b—(X1: the formula —NH—, —O— or the like; a, b: 0-5) or the like; B: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like].
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: April 17, 2012
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shojiro Miyazaki, Yuji Nakamura, Takahiro Nagayama, Taro Tokui, Yasuyuki Ogawa
  • Patent number: 8153637
    Abstract: 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: Grant
    Filed: December 16, 2010
    Date of Patent: April 10, 2012
    Assignee: Sanofi
    Inventors: Marco Baroni, Olaf Ritzeler, Marco Zanchet
  • Publication number: 20120016124
    Abstract: 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: Application
    Filed: February 21, 2011
    Publication date: January 19, 2012
    Applicant: Baylor University
    Inventors: Kevin G. Pinney, Mada Graciata Miranda, James Michael Dorsey
  • Patent number: 8084607
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Grant
    Filed: February 23, 2009
    Date of Patent: December 27, 2011
    Assignee: Abbott Laboratories
    Inventors: Milan Bruncko, Hong Ding, Steven Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol-min Park, Andrew M. Petros, Xiaohong Song, Noah P. Tu, Xilu Wang, Michael D. Wendt
  • Publication number: 20110275816
    Abstract: The invention relates to novel trans N-{4-{2-[4-(2, 3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate and a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the steps a) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl) amino]-cyclohexyl}-acetic acid ester with sodium borohydride and aluminium trichloride to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethanol; b) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-ethanol obtained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate; c) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate obtained with 2,3-dichlorophenyl-piperazine in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl
    Type: Application
    Filed: December 17, 2009
    Publication date: November 10, 2011
    Inventors: Laszlo Czibula, Eva Againe Csongor, Katalin Nogradi, Balint Juhasz, Ferenc Sebok, Janos Galambos, Istvan Vago
  • Patent number: 7985752
    Abstract: The present invention relates to novel piperazine derivatives or pharmaceutically acceptable salts thereof, a process for preparing the same, and in particular, a high binding for Serotonin 1A(5-hydroxytryptamine; 5-HT1A) receptor, a pharmaceutical composition for treatment and/or prevention of depression and anxiety including an effective amount of the piperazine compound, and a method of treating depression, anxiety and other conditions related to 5-HT1A receptor in a mammal.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: July 26, 2011
    Assignee: SK Holdings Co., Ltd.
    Inventors: Yonggil Kim, Nahmryune Cho, Yunhee Kim, Joon Heo, Seonmin Dong, Mi Kyung Ji, Man-Young Cha, Kiho Lee
  • Patent number: 7947839
    Abstract: Bis 1,8 naphthalimide compounds including antibody drug conjugate (ADC) are described. Pharmaceutical compositions comprising an effective amount of a 1,8 bis-naphthalimide compound for treatment of hyperproliferative disorders and other disorders are described. Methods are described for killing or inhibiting the proliferation of tumor cells or cancer cells including administering to a patient an effective amount of a 1,8 bis-naphthalimide compound.
    Type: Grant
    Filed: January 30, 2006
    Date of Patent: May 24, 2011
    Assignee: Genentech, Inc.
    Inventors: Lewis J. Gazzard, Edward HyungSuk Ha, David Y. Jackson, Joann M. Um
  • Publication number: 20110112073
    Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.
    Type: Application
    Filed: November 12, 2010
    Publication date: May 12, 2011
    Applicant: DUKE UNIVERSITY
    Inventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
  • Patent number: 7932388
    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: December 11, 2007
    Date of Patent: April 26, 2011
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Darryl J. C. Pappin, Sasi Pillai, James M. Coull
  • Publication number: 20110092703
    Abstract: A P2X4 receptor antagonist is a compound represented by the formula (I) or a pharmacologically acceptable salt thereof, which is used as a preventive or therapeutic agent for neuropathic pains: Wherein B is aryl or the like that can have a substituent; Y is C1-5 alkylene that can have a double bond; Z is O, S or the like; each of R1, R2 and R3 independently is hydrogen, C1-8 alkyl or the like; R4 is hydrogen, C1-8 alkyl or the like; each of P and Q independently is hydrogen, halogen, C1-8 alkyl or the like; W is C1-8 alkyl or the like; and each of n and m independently is 1 or 2.
    Type: Application
    Filed: August 8, 2008
    Publication date: April 21, 2011
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Shogo Sakuma, Tsuyoshi Endo, Noriko Kanakubo, Masahiko Arai, Toshihiro Takahashi, Toshiyasu Imai, Kumiko Taguchi, Eriko Nakata, Nobutaka Mochiduki, Masatoshi Ushioda, Makoto Tsuda, Kazuhide Inoue
  • Publication number: 20110086863
    Abstract: 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 and chlorine.
    Type: Application
    Filed: August 5, 2010
    Publication date: April 14, 2011
    Applicants: Abbott GmbH & Co. KG, Abbott Laboratories
    Inventors: 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
  • Patent number: 7910734
    Abstract: 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: Grant
    Filed: December 16, 2005
    Date of Patent: March 22, 2011
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Makoto Kotake, Naoki Yoneda, Katsunobu Osada
  • Publication number: 20110065691
    Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z 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 and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.
    Type: Application
    Filed: September 22, 2010
    Publication date: March 17, 2011
    Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen