Bicyclo Ring System Patents (Class 564/460)
  • Patent number: 8946482
    Abstract: The present invention relates to salts of rasagiline and pharmaceutical preparations thereof. The invention further provides a method of preparing the salts of rasagiline.
    Type: Grant
    Filed: July 7, 2010
    Date of Patent: February 3, 2015
    Assignee: Ratiopharm GmbH
    Inventors: Thomas Thyrann, Christian Janssen, Ramesh Matioram Gidwani
  • Publication number: 20140378360
    Abstract: The present application relates to perfume raw materials, perfume delivery systems and consumer products comprising such perfume raw materials and/or such perfume delivery systems, as well as processes for making and using such perfume raw materials, perfume delivery systems and consumer products. Such perfume raw materials and compositions, including the delivery systems, disclosed herein expand the perfume communities' options as such perfume raw materials can provide variations on character and such compositions can provide desired odor profiles.
    Type: Application
    Filed: September 12, 2014
    Publication date: December 25, 2014
    Inventors: Hugo Robert Germain DENUTTE, Johan SMETS, An PINTENS, Koen VAN AKEN, Freek Annie Camiel VRIELYNCK
  • Publication number: 20140343113
    Abstract: The present invention relates to fungicidal N-bicycloalkyl and N-tricycloalkyl pyrazole-4-(thio)carboxamide derivatives of formula (I), wherein T represents 0 or S; n represents 0 or 1; and B represents where the bond marked by * is attached to the (CZ2Z3)n-N amide moiety, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 20, 2014
    Inventors: Jürgen Benting, Stéphane Brunet, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stéphanie Gary, Jörg Greul, Hélène Lachaise, Jan-Peter Schmidt, Philippe Rinolfi, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
  • Patent number: 8884059
    Abstract: The present invention is directed towards an electrocoating composition comprising a cyclic guanidine.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: November 11, 2014
    Assignee: PPG Industries Ohio, Inc.
    Inventors: Steven R. Zawacky, Thomas C. Moriarity, Donald W. Boyd, Geoffrey R. Webster, Joseph Lucas, Alan J. Kaylo, Chester J. Szymanski, Venkatachalam Eswarakrishnan
  • Patent number: 8846765
    Abstract: A pharmaceutical combination comprising as components (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and (b) at least one NMDA-antagonist, a pharmaceutical formulation and a dosage form comprising such a combination, and a method of treating pain, e.g. inflammatory pain or neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, with component (a) being administered either before or after component (b), and with components (a) or (b) being administered to the mammal either via the same pathway of administration or via different pathways of administration.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: September 30, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Klaus Schiene, Petra Bloms-Funke
  • Publication number: 20140288169
    Abstract: The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for their use, and their pharmaceutical compositions.
    Type: Application
    Filed: January 5, 2012
    Publication date: September 25, 2014
    Applicant: TARGACEPT, INC.
    Inventors: Srinivasa Rao Akireddy, Scott R. Breining, Matt S. Melvin, Srinivasa V. Murthy, Anatoly A. Mazurov, Balwinder Singh Bhatti, Jon-Paul Strachan, Ronald Joseph Heemstra, Todd Showalter, Yunde Xiao, Philip S. Hammond, Lan Miao, David Kombo, Daniel Yohannes, Jason Speake
  • Publication number: 20140275245
    Abstract: Analgesic compounds for treatment of pain or fever, comprising a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering the compounds.
    Type: Application
    Filed: March 6, 2014
    Publication date: September 18, 2014
    Applicant: KALYRA PHARMACEUTICALS, INC.
    Inventor: Kevin Duane Bunker
  • Patent number: 8809397
    Abstract: The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: August 19, 2014
    Assignee: Targacept, Inc.
    Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Matt S. Melvin, Jason D. Speake, Yunde Xiao, Daniel Yohannes
  • Publication number: 20140135529
    Abstract: Compositions and methods for administering memantine to a subject are provided. In particular, a solid pharmaceutical composition in a unit dosage form for once daily oral administration is provided. The compositions comprises an extended release formulation of 22.5 mg to 33.75 mg memantine, or a pharmaceutically acceptable salt thereof, wherein administration of a dose of the composition to a human subject provides a mean plasma memantine concentration profile characterized by a change in memantine xconcentration as a function of time (dC/dT) that is less than 50% of the dC/dT provided by the same quantity of an immediate release form of memantine, determined in a time period between 0 hours to 6 hours after administration of memantine, and wherein dC/dT is measured in a single-dose human PK study. Methods of treating dementia, in particular Alzheimer's diseases, using the compositions are provided.
    Type: Application
    Filed: November 15, 2013
    Publication date: May 15, 2014
    Applicant: ADAMAS PHARMACEUTICALS, INC.
    Inventors: Gregory T. Went, Timothy J. Fultz, Laurence R. Meyerson
  • Patent number: 8673975
    Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: March 18, 2014
    Assignee: Aquinox Pharmaceuticals Inc.
    Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
  • Patent number: 8669367
    Abstract: To provide a method whereby a 2-azaadamantane can easily be obtained in good yield. A method for producing a 2-azaadamantane represented by the formula (1), which comprises cyclizing a compound represented by the following formula (2) in the presence of an acid.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: March 11, 2014
    Assignees: Nissan Chemical Industries, Ltd., Tohoku Techno Arch Co., Ltd.
    Inventors: Toshimasa Hamada, Noriaki Nagahama, Masami Kozawa, Yoshiharu Iwabuchi, Masatoshi Shibuya, Masaki Tomizawa, Yusuke Sasano
  • Publication number: 20140057877
    Abstract: This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists/partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicity of neurotoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan.
    Type: Application
    Filed: October 18, 2011
    Publication date: February 27, 2014
    Inventors: Michael A. Murphy, Mitchell R. Malachowski
  • Publication number: 20130210904
    Abstract: Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds.
    Type: Application
    Filed: August 15, 2012
    Publication date: August 15, 2013
    Inventors: Jeremy E. Wulff, Michael G. Brant, Jeremy W. Mason, Caleb M. Bromba, Martin J. Boulanger
  • Publication number: 20130203860
    Abstract: The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.
    Type: Application
    Filed: May 24, 2011
    Publication date: August 8, 2013
    Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Matt S. Melvin, Jason D. Speake, Yunde Xiao, Daniel Yohannes
  • Publication number: 20130102794
    Abstract: The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R1, R2 and R3 are as defined for compound of formula (I).
    Type: Application
    Filed: June 24, 2011
    Publication date: April 25, 2013
    Applicant: UCB PHARMA GMBH
    Inventors: Celal Ates, Arnaud Schule, Magali Palacio, Paul Deutsch, David Vasselin, Nicolas Carly, Ganesh Phadtare, Swapnil Yerande, Jean-Pierre Delatinne, Maria Luisa Escudero Hernandez, Veronique Pinilla
  • Patent number: 8273889
    Abstract: The invention provides a method for producing 2-azaadamantanes represented by formula (1) in good yields. The method includes cyclizing a compound represented by formula (2) in the presence of an acid.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: September 25, 2012
    Assignees: Nissan Chemical Industries, Ltd., Tohoku Techno Arch Co., Ltd.
    Inventors: Toshimasa Hamada, Noriaki Nagahama, Masami Kozawa, Yoshiharu Iwabuchi, Masatoshi Shibuya, Masaki Tomizawa, Yusuke Sasano
  • Patent number: 8138377
    Abstract: The invention provides novel arylbicyclo[3.1.0]hexylamines, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety.
    Type: Grant
    Filed: November 6, 2007
    Date of Patent: March 20, 2012
    Assignee: DOV Pharmaceutical, Inc.
    Inventors: Phil Skolnick, Zhengming Chen, Ji Yang
  • Patent number: 8138375
    Abstract: The invention relates to a method for producing 1-formamido-3,5-dimethyladamantane in only two reaction steps by direct formamide formation of 1,3-dimethyladamantane, the 1,3-dimethyladamantane being reacted with formamide in concentrated acids.
    Type: Grant
    Filed: February 20, 2007
    Date of Patent: March 20, 2012
    Assignee: MERZ PHARMA GmbH & Co. KGaA
    Inventors: Peter R. Schreiner, Andrey A. Fokin, Lukas Wanka, Derek M. Wolfe
  • Publication number: 20120028957
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: August 1, 2010
    Publication date: February 2, 2012
    Inventors: William F. DeGrado, Jun Wang
  • Publication number: 20110294785
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: August 21, 2009
    Publication date: December 1, 2011
    Applicant: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Jun Wang
  • Publication number: 20110009439
    Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Application
    Filed: February 23, 2010
    Publication date: January 13, 2011
    Applicant: AQUINOX PHARMACEUTICALS INC.
    Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
  • Publication number: 20100311977
    Abstract: To provide a method whereby a 2-azaadamantane can easily be obtained in good yield. A method for producing a 2-azaadamantane represented by the formula (1), which comprises cyclizing a compound represented by the following formula (2) in the presence of an acid.
    Type: Application
    Filed: November 20, 2008
    Publication date: December 9, 2010
    Applicants: Nissan Chemical Industries, Ltd., Tohoku Techno Arch Co., Ltd.
    Inventors: Toshimasa Hamada, Noriaki Nagahama, Masami Kozawa, Yoshiharu Iwabuchi, Masatoshi Shibuya, Masaki Tomizawa, Yusuke Sasano
  • Publication number: 20090299097
    Abstract: The invention relates to a method for producing 1-formamido-3,5-dimethyladamantane in only two reaction steps by direct formamide formation of 1,3-dimethyladamantane, the 1,3-dimethyladamantane being reacted with formamide in concentrated acids.
    Type: Application
    Filed: February 20, 2007
    Publication date: December 3, 2009
    Applicant: MERZ PHARMA GMBH & CO. KGAA
    Inventors: Peter R. Schreiner, Andrey A. Fokin, Lukas Wanka, Derek M. Wolfe
  • Patent number: 7601874
    Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Grant
    Filed: April 15, 2004
    Date of Patent: October 13, 2009
    Assignee: Aquinox Pharmaceuticals Inc.
    Inventors: Jeffery R Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
  • Publication number: 20090082596
    Abstract: The invention relates to a process for preparing certain adamantanamines, of formula wherein R, R? are each methyl and X is halogen, to intermediates used in the process, and to processes for preparing such intermediates.
    Type: Application
    Filed: February 20, 2007
    Publication date: March 26, 2009
    Inventor: Christian Pahick Schickaneder
  • Publication number: 20090076165
    Abstract: The present application describes deuterium-enriched memantine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 22, 2008
    Publication date: March 19, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 6649658
    Abstract: A description is given here of novel solid and stable derivatives of (−)-verbenone having formula (I) wherein, when X=O Z=H, ═CHAr, ═C(OH)COOEt, ═NOR; Y=H, NH2, NH3+X1−, NHCOAr, NHCOR, NHCONHR, NHCONHAr, X1-=pharmaceutically acceptable anion; Ar-aryl or heteroaryl, preferably phenyl, 4-chlorophenyl, 2-furyl, 2-thienyl, 2-hydroxyphenyl, 2-acetoxyphenyl; R=H, C1-C4 alkyl, C4-C6 cycloalkyl, CH2COOH, CH2COOEt, CH2COCH3, CH2CN, CH2COCH2COOEt, CH2C6H5; and, when X=dimethylamino, diethylamino, pyrrolidino, piperidino or morpholino: Y=H; Z=H, CONHAr, COHNR; Ar=aryl, preferably phenyl; R=H, C1-C4 alkyl, C4-C6 cycloakyl. A description is also given of the processes for the preparation of these derivatives and of the novel intermediates used in those processes. The novel derivatives are characterized by their solubility in water; some of them also have a high anti-inflammatory activity.
    Type: Grant
    Filed: October 15, 2001
    Date of Patent: November 18, 2003
    Assignee: Euphar Group SRL
    Inventors: Paolo Corvi Mora, Angelo Ranise
  • Patent number: 6635783
    Abstract: Bicyclic amino alcohols, whose amino group and hydroxy group are bonded in positions 1,3 adjacent to the bridge, for example are valuable ligands for metal complexes of the d-8 metals of the periodic table of elements. The metal complexes in question are catalysts or catalyst precursors for the asymmetric hydrogenation or asymmetric transfer hydrogenation with hydrogen donors of prochiral organic compounds with carbon double bonds or carbon/hetero atom double bonds, for example ketones and imines.
    Type: Grant
    Filed: March 6, 2001
    Date of Patent: October 21, 2003
    Assignee: Solvias AG
    Inventor: Peter Herold
  • Publication number: 20020016371
    Abstract: A pharmaceutical composition includes a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of exo-R-mecamylamine in combination with a pharmaceutically acceptable carrier. Preferably the amount is about 0.5 mg to about 20 mg. Medical conditions are treated by administering a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of its exo-R-mecamylamine, said amount being sufficient to ameliorate the medical condition.
    Type: Application
    Filed: June 15, 2001
    Publication date: February 7, 2002
    Inventors: Douglas Shytle, Paul Sanberg, Mary Newman, Archie A. Silver
  • Publication number: 20020016370
    Abstract: A pharmaceutical composition includes a therapeutically effective amount of exo-R-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of exo-S-mecamylamine in combination with a pharmaceutically acceptable carrier. Preferably the amount is about 0.5 mg to about 20 mg. Medical conditions are treated by administering a therapeutically effective amount of exo-R-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of its exo-S-mecamylamine, said amount being sufficient to ameliorate the medical condition.
    Type: Application
    Filed: June 15, 2001
    Publication date: February 7, 2002
    Inventors: Douglas Shytle, Paul Sanberg, Mary Newman, Archie A. Silver
  • Patent number: 6166234
    Abstract: Novel tripodal cyclopentadiene derivatives have the formula (I) ##STR1## where E are identical or different and are --N(R)(R), --P(R)(R), --As(R)(R), --Sb(R)(R), --OR, --SR, --SeR, --TeR, where R are identical or different and are each hydrogen, a C.sub.1 -C.sub.20 -carboorganic radical or a C.sub.1 -C.sub.30 -organosilicon radical, or E is a leaving group X andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 are identical or different and are each hydrogen, a C.sub.1 -C.sub.20 -carboorganic radical or a C.sub.1 -C.sub.30 -organosilicon radical,Z is a cyclopentadienyl radical or a substituted cyclopentadienyl structural unit andT is hydrogen, a C.sub.1 -C.sub.20 -carboorganic radical or a C.sub.1 -C.sub.30 -organosilicon radical or a group E--Y--, where E is --N(R)(R), --P(R)(R), --As(R)(R), --Sb(R)(R), --OR, --SR, --SeR, --TeR or a leaving group X, where R are identical or different and are each hydrogen, a C.sub.1 -C.sub.20 -carboorganic radical or a C.sub.1 -C.sub.
    Type: Grant
    Filed: January 13, 1998
    Date of Patent: December 26, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Gottfried Huttner, Joachim Vogelgesang, Ute Winterhalter, Bjorn Antelmann
  • Patent number: 6137019
    Abstract: Process for converting a geminally substituted cyclopentadiene containing 2-6 substituents into a non-geminally substituted cyclopentadiene by reacting the geminally substituted cyclopentadiene with a base, sodium or potassium at a temperature of 0-200.degree. C. The invention also relates to mixtures of non-geminally substituted cyclopentadienes obtained by means of this process.
    Type: Grant
    Filed: March 3, 1999
    Date of Patent: October 24, 2000
    Assignee: DSM N.V.
    Inventors: Gerardus J. M. Gruter, Johannes A. M. van Beek
  • Patent number: 6114392
    Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.
    Type: Grant
    Filed: April 16, 1996
    Date of Patent: September 5, 2000
    Inventors: Gad M. Gilad, Varda H. Gilad
  • Patent number: 6025328
    Abstract: The present invention provides illudin analogs of the general formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.
    Type: Grant
    Filed: February 20, 1998
    Date of Patent: February 15, 2000
    Assignee: The Regents of the University of California
    Inventors: Trevor C. McMorris, Michael J. Kelner
  • Patent number: 5986142
    Abstract: The present invention provides a process for preparing compounds of Formula I: ##STR1## wherein R.sub.1 is methyl by reduction of a camphene intermediate with a reducing agent.
    Type: Grant
    Filed: September 23, 1997
    Date of Patent: November 16, 1999
    Assignee: Poli Industria Chimica SpA
    Inventors: Ambrogio Magni, Giovanni Signorelli
  • Patent number: 5763647
    Abstract: A process for preparing an optically active 1,4-bridged-cyclohexane carboxylic acid derivatives which are clinically important thromboxane A.sub.2 thromboxane of formula (IV): ##STR1## wherein, R is phenyl or phenyl substituted with hydroxy, lower alkoxy, halogen, or lower alkyl; Y is oxygen, methylene, substituted methylene; m is 0 or 1; n is 0, 1 or 2; q is 3 or 4 with the proviso that when m is 1, n is 0 or 1 from an optically active norbornyl amine derivative.
    Type: Grant
    Filed: July 11, 1997
    Date of Patent: June 9, 1998
    Assignee: Shionogi & Co., LTD.
    Inventors: Mitsuaki Ohtani, Hisanori Takahashi, Fumihiko Watanabe, Masami Takayama
  • Patent number: 5719280
    Abstract: The present invention relates to novel benzocycloalkylazolethione compounds which are dopamine .beta.-hydroxylase inhibitors in which the benzocycloalkyl portion of the compound is selected from indanyl, 1,2,3,4-tetrahydronaphthalenyl and 6,7,8,9-tetrahydro-5H-benzocycloheptenyl (in which the benzo is optionally substituted with one to three substituents) and the azolethione portion of the compound is selected from 2-thioxo-2,3-dihydro-1H-imidazol-3-yl, 5-thioxo-4,5-dihydro-1H-?1,2,4!triazol-4-yl and 5-thioxo-4,5-dihydro-1H-?1,2,4!triazol-1-yl (each optionally substituted with one to three substituents); and the prodrugs, pharmaceutically acceptable salts, individual isomers and mixtures of isomers and the methods of using and preparing such benzocycloalkylazolethione compounds.
    Type: Grant
    Filed: April 7, 1997
    Date of Patent: February 17, 1998
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gregory Ricardo Martinez, Owen Will Gooding, David Bruce Repke, Philip Jay Teitelbaum, Keith Adrian Murray Walker, Roger Lewis Whiting
  • Patent number: 5610300
    Abstract: Compounds of the formulae I and Ia and their racemates ##STR1## in which A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, R.sub.1 is hydrogen or a protective group, R.sub.2 is hydrogen or a protective group or a radical forming a phosphorus-containing nucleotide bridge group and B is a purine or pyrimidine radical or an analogue thereof, can be used as antiviral active ingredients or for the preparation of biologically active oligonucleotides.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 11, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Karl-Heinz Altmann, Ren e Imwinkelried, Albert Eschenmoser
  • Patent number: 5461152
    Abstract: Compounds of the formulae I and Ia and their racemates ##STR1## in which A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, R.sub.1 is hydrogen or a protective group, R.sub.2 is hydrogen or a protective group or a radical forming a phosphorus-containing nucleotide bridge group and B is a purine or pyrimidine radical or an analogue thereof, can be used as antiviral active ingredients or for the preparation of biologically active oligonucleotides.
    Type: Grant
    Filed: June 28, 1993
    Date of Patent: October 24, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Karl-Heinz Altmann, Rene Imwinkelried, Albert Eschenmoser
  • Patent number: 5454720
    Abstract: A method for providing detection of timing anomalies and eliminating falsely detected positions in a hyperbolic positioning system for a simulated battlefield system. The method selects a large number of transmitters for calculation of position of an object or person on the battle field. In addition, transmitters are selected which have a high dilution of precision factor.
    Type: Grant
    Filed: May 31, 1994
    Date of Patent: October 3, 1995
    Assignee: Motorola, Inc.
    Inventors: Mark R. FitzGerald, Craig T. Griffin, Glen E. Sater
  • Patent number: 5399673
    Abstract: Compounds containing at least one alkenyl group, at least one maleimide group and at least one rodlike mesogenic moiety are prepared by reacting one or more aminophenols containing one or more rodlike mesogenic moieties with a stoichiometric quantity of a maleic anhydride per amine group of said aminophenol and then alkenylating the resulting phenolic functional maleimide.
    Type: Grant
    Filed: February 9, 1993
    Date of Patent: March 21, 1995
    Assignee: The Dow Chemical Company
    Inventor: Robert E. Hefner, Jr.
  • Patent number: 5284976
    Abstract: A novel process for producing hindered and unhindered primary amines represented by the formula RNH.sub.2 and R*NH.sub.2 in high yields from novel intermediates RBMe.sub.2 or R*BMe.sub.2 wherein R is an organo group, R* is a chiral organo group. attached to boron, B is boron and Me is methyl.
    Type: Grant
    Filed: July 19, 1993
    Date of Patent: February 8, 1994
    Assignee: Aldrich Chemical Company, Inc.
    Inventor: Herbert C. Brown
  • Patent number: 5276195
    Abstract: A process for preparing a dimethylorganoborane represented by the formula R*BMe.sub.2 wherein R* is a chiral organyl group attached to the boron, B is boron and Me is methyl comprising treating a chiral boronic ester R*B(OR').sub.2 with a methyl magnesium salt or trimethylaluminum wherein R* is the same chiral organyl group and R' is alkyl.
    Type: Grant
    Filed: July 14, 1993
    Date of Patent: January 4, 1994
    Assignee: Aldrich Chemical Company, Inc.
    Inventor: Herbert C. Brown
  • Patent number: 5254707
    Abstract: The process for preparing a compound of the formula:Cp'YNHRwherein: Cp' is a cyclopentadienyl or a substituted cyclopentadienyl group, Y is a covalent bridging group which contains one or more group 14 elements, and R is a C.sub.1 to C.sub.20 hydrocarbyl or substituted hydrocarbyl group, the process comprising reacting a ligand of the formula Cp'YX, wherein Cp' and Y are as defined above and X is halogen, with a substantially equimolar amount of a primary amine of the formula NH.sub.2 R, wherein R is as defined above, in an inert solvent in the presence of a HX scavenger at an elevated temperature of at least about 35.degree. C., so as to form said compound.
    Type: Grant
    Filed: December 7, 1992
    Date of Patent: October 19, 1993
    Assignee: Ethyl Corporation
    Inventors: Jamie R. Strickler, John M. Power, Meng-Sheng Ao
  • Patent number: 5243080
    Abstract: The present invention provides a novel compound represented as ##STR1## The present novel compound is prepared by reacting fluorine with pyridine-boron trifluoride and is useful as a fluorinating agent in the fluorination of organic compounds.
    Type: Grant
    Filed: July 8, 1992
    Date of Patent: September 7, 1993
    Assignee: AlliedSignal Inc.
    Inventors: Michael Van Der Puy, David Nalewajek, George A. Shia, William J. Wagner
  • Patent number: 5214209
    Abstract: A novel process for producing hindered and unhindered primary amines represented by the formula RNH.sub.2 and R*NH.sub.2 in high yields from novel intermediates RBMe.sub.2 or R*BMe.sub.2 wherein R is an organo group, R* is a chiral organo group,attached to boron, B is boron and Me is methyl.
    Type: Grant
    Filed: March 26, 1990
    Date of Patent: May 25, 1993
    Assignee: Aldrich Chemical Company, Inc.
    Inventor: Herbert C. Brown
  • Patent number: 5210310
    Abstract: A novel process for producing hindered and unhindered primary amines represented by the formula RNH.sub.2 and R*NH.sub.2 in high yields from novel intermediates RBMe.sub.2 or R*BMe.sub.2 wherein R is an organo group, R* is a chiral organo group, attached to boron, B is boron and Me is methyl.
    Type: Grant
    Filed: March 26, 1990
    Date of Patent: May 11, 1993
    Assignee: Aldrich Chemical Co., Inc.
    Inventor: Herbert C. Brown
  • Patent number: 5196542
    Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
    Type: Grant
    Filed: February 20, 1991
    Date of Patent: March 23, 1993
    Assignee: The Upjohn Company
    Inventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased
  • Patent number: 5084592
    Abstract: Azulenesquaric acid dyes of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each have specified meanings are prepared from azulene derivatives of the formula ##STR2## where R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each have specified meanings as intermediates, and used in an optical recording medium.
    Type: Grant
    Filed: September 30, 1988
    Date of Patent: January 28, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang Schrott, Peter Neumann, Sibylle Brosius, Helmut Barzynski, Klaus D. Schomann, Harald Kuppelmaier
  • Patent number: 5051409
    Abstract: 2-Aminodecalin derivatives of the formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are H or methyl,A is H, OH, O-alkylcarbonyl, O-benzoyl or O-CH.sub.3,R.sup.4 is H, cyclopropyl, alkyl, alkenyl, or alkynyl,R.sup.5 is alkyl, alkenyl or alkynyl which is substituted or unsubstituted,cycloalkyl or cycloalkenyl whic is substituted or unsubstituted, substituted phenylalkyl, substituted cycloalkyl-alkyl, substituted 5-membered heterocyclic ring, bicycloalkyl-alkyl orR.sup.4 and R.sup.5, together with the nitrogen atom, are a substituted or unsubstituted, saturated or unsaturated piperidine radical,their plant-tolerated salts and N-oxides, and fungicides containing these compounds.
    Type: Grant
    Filed: November 1, 1989
    Date of Patent: September 24, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Zipplies, Bernhard Zipperer, Hubert Sauter, Norbert Goetz, Franz Roehl, Eberhard Ammermann, Gisela Lorenz