Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/49)
  • Publication number: 20080299041
    Abstract: The invention is directed to heterocyclic indene derivatives useful for ?-amyloid plaque imaging, their radiolabeled compounds and their preparation methods. The compounds of the invention are easily labeled with radioisotopes and have high affinities to ?-amyloid depositions, thus they facilitate diagnosis of Alzheimer's disease by imaging the distribution of ?-amyloid depositions.
    Type: Application
    Filed: May 28, 2008
    Publication date: December 4, 2008
    Applicant: SEOUL NATIONAL UNIVERSITY INDUSTRY FOUNDATION
    Inventors: Jae Min JEONG, Dong Soo LEE, June-Key CHUNG, Myung Chul LEE
  • Patent number: 7449483
    Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
    Type: Grant
    Filed: December 6, 2006
    Date of Patent: November 11, 2008
    Assignee: Hoffman-La Roche Inc.
    Inventors: Johannes Aebi, Jean Ackermann, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
  • Publication number: 20080242875
    Abstract: A method for the degradation of polycyclic aromatic compounds is disclosed that involves dissolving ozone in a bipolar solvent comprising a non-polar solvent in which is of sufficiently non-polar character to solubilized the polycyclic aromatic compounds, and a polar-water-compatible solvent which is fully miscible with the non-polar solvent to form a single phase with the non-polar solvent. The bipolar solvent with dissolved ozone is contacted with the polycyclic aromatic compounds to solubilize the polycyclic aromatic compounds and react the dissolved polycyclic aromatic compounds with the ozone to degrade the dissolved polycyclic aromatic compounds to oxygenated intermediates. The bipolar solvent is then mixed with sufficient water to form separate non-polar and polar phases, the non-polar phase comprising the non-polar solvent and the polar phase comprising the non-polar solvent and the oxygenated intermediates.
    Type: Application
    Filed: March 24, 2008
    Publication date: October 2, 2008
    Inventors: P.K. Andy Hong, David A. Wavrek, Jiun-Chi Chao, Yu Zeng
  • Publication number: 20080194608
    Abstract: Compounds of the formula (I): in which R1, R2, R3, R?3 and R4 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, the pharmaceutical compositions comprising them, and the processes for the preparation of these compounds.
    Type: Application
    Filed: December 22, 2005
    Publication date: August 14, 2008
    Inventors: Michel Brunet, Herve Dumas, Catherine Vidal, Nathalie Adje, Benoit Van Hille, Francis Contard
  • Publication number: 20080161281
    Abstract: Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.
    Type: Application
    Filed: March 12, 2008
    Publication date: July 3, 2008
    Applicant: Abbott Laboratories
    Inventors: Michael R. Schrimpf, Kevin B. Sippy, Jianguo Ji, Tao Li, Jennifer M. Frost, Clark A. Briggs, William H. Bunnelle
  • Patent number: 7393865
    Abstract: Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L1, L2 and n are as defined herein. Such compounds generally function as H1 receptor ligands, and thus have utility as sleep inducing agents. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
    Type: Grant
    Filed: June 17, 2005
    Date of Patent: July 1, 2008
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Graham Beaton, Wilna (Willy) J Moree, Florence Jovic, Timothy Coon, Jinghua Yu
  • Publication number: 20080124571
    Abstract: Provided are a pyrene derivative of a specified structure and an organic electroluminescence device including an organic thin film layer formed of one or multiple layers including at least a light emitting layer, the organic thin film layer being interposed between a cathode and an anode, in which at least one layer of the organic thin film layer contains the pyrene derivative alone or as a component of mixture. Thus, there are provided an organic electroluminescence device capable of obtaining long-life blue light emission with high luminous efficiency and a novel pyrene derivative for realization thereof.
    Type: Application
    Filed: October 29, 2007
    Publication date: May 29, 2008
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Mitsunori Ito, Mineyuki Kubota
  • Publication number: 20080105865
    Abstract: An object is to provide a pyrene based compound that is good in both properties of light emission and mobility when the compound is used as a light emitting transistor element; and a light emitting transistor element wherein this specific pyrene based compound is used. A pyrene based compound represented by the following chemical formula (1) is used as a main component of a light emitting layer in a light emitting transistor element: (wherein R1 represents a group selected from a heteroaryl group which may have a substituent, an aryl group which may have a substituent except a phenyl group which does not have any substituent, an alkyl group which may have a substituent and has a main chain having 1 to 20 carbon atoms, an alkenyl group which may have a substituent, an alkynyl group which may have a substituent, a silyl group which may have a substituent, and a halogen atom.
    Type: Application
    Filed: November 25, 2005
    Publication date: May 8, 2008
    Inventors: Takahito Oyamada, Hiroyuki Uchiuzou, Chihaya Adachi, Seiji Akiyama, Takayoshi Takahashi
  • Publication number: 20080100207
    Abstract: Provided are a cyclopentaphenanthrene-based compound and an organoelectroluminescent device employing the same. The cyclopentaphenanthrene-based compound is easy to prepare and excellent in solubility, color purity, color stability, and thermal stability. The cyclopentaphenanthrene-based compound is useful as a material for forming an organic layer, in particular, an emitting layer, in an organoelectroluminescent device, and as an organic dye or an electronic material such as a nonlinear optical material.
    Type: Application
    Filed: July 18, 2007
    Publication date: May 1, 2008
    Inventors: Sang-Hoon Park, Yu-Jin Kim, Jhun-Mo Son
  • Publication number: 20080079356
    Abstract: A cyclopentaphenanthrene-based compound is easy to prepare and excellent in solubility, color purity, and color stability. The cyclopentaphenanthrene-based compound is useful as a material for forming an organic layer, in particular, an emitting layer, in an organoelectroluminescent device, and as an organic dye or an electronic material such as a nonlinear optical material.
    Type: Application
    Filed: July 18, 2007
    Publication date: April 3, 2008
    Inventors: Sang-Hoon Park, Yu-Jin Kim, Jhun-Mo Son, Byoung-Ki Choi, O-Hyun Kwon, Myeong-Suk Kim
  • Patent number: 7329764
    Abstract: Disclosed are compounds of the formula I shown below, wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: February 12, 2008
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Zhidong Chen, John David Ginn, Eugene Richard Hickey, Weimin Liu, Can Mao, Tina Marie Morwick, Peter Allen Nemoto, Denice Spero, Sanxing Sun
  • Patent number: 7300952
    Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.
    Type: Grant
    Filed: May 29, 2003
    Date of Patent: November 27, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: James F. Callahan, Zehong Wan
  • Publication number: 20070270595
    Abstract: Provided are an organic light-emitting compound represented by Formula 1 and an organic electroluminescent (EL) device using the same: The organic light-emitting compound has thermostability and photochemical stability in addition to superior electrical features. The organic EL device using the organic light-emitting compound has low driving voltage, high efficiency, and superior color purity.
    Type: Application
    Filed: May 22, 2007
    Publication date: November 22, 2007
    Inventors: Myeong-Suk Kim, Dong-Woo Shin, Woon-Jung Paek, Byoung-Ki Choi, O-Hyun Kwon, Eun-Sil Han
  • Publication number: 20070240756
    Abstract: The present embodiments relate to a dye for a dye-sensitized solar cell and a dye-sensitized solar cell prepared from the same. The dye includes a fluorenyl-containing compound. The dye according to the present embodiments is applied to a light absorption layer to improve photovoltaic efficiency and increase an open-circuit voltage.
    Type: Application
    Filed: April 16, 2007
    Publication date: October 18, 2007
    Inventors: Jae-Kwan Lee, Ji-Won Lee, Jae-Jung Ko, Sang-Hoon Kim, Soo-Jin Moon, Moon-Sung Kang, Moon-Seok Kwon
  • Patent number: 7276518
    Abstract: Substituted cyclohexane-1,4-diamine compounds, methods for production thereof, pharmaceutical compositions comprising these compounds and methods of treatment using these compounds.
    Type: Grant
    Filed: November 10, 2003
    Date of Patent: October 2, 2007
    Assignee: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Hagen-Heinrich Hennies, Werner Englberger, Babette-Yvonne Koegel
  • Patent number: 7256219
    Abstract: The present invention is directed to multifluoro-substituted Chalcones and analogs thereof, represented by the general Formula I: wherein Ar and R6-R10 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: March 14, 2002
    Date of Patent: August 14, 2007
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, P. Sanjeeva Reddy, John A. Drewe, Bao Ngoc Nguyen, Shailaja Kasibhatla
  • Patent number: 7253165
    Abstract: The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
    Type: Grant
    Filed: May 12, 2004
    Date of Patent: August 7, 2007
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, James A. Hendrix, John G. Jurcak, Brian S. Freed, Nicholas J. Hrib, John D. Tomer, IV, Reda G. Hanna
  • Patent number: 7202369
    Abstract: The present invention relates to a process for preparing 3,4-dialkoxythiophenes or 3,4-alkylenedioxythiophenes in high yield via the rapid decarboxylation of 3,4-dialkoxythiophenedicarboxylic acid or 3,4-aklylenedioxythiophenedicarboxylic acid in a water-miscible polar solvent in the presence of copper catalyst under an oxygen atmosphere.
    Type: Grant
    Filed: November 19, 2003
    Date of Patent: April 10, 2007
    Inventors: Woon-Phil Baik, Young-Sam Kim, Hee-Jung Hong, Sang-Gook Jung
  • Patent number: 7196081
    Abstract: The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): in which R1 represents a hydrogen atom, etc., R2 represents a C1–C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.
    Type: Grant
    Filed: October 29, 2002
    Date of Patent: March 27, 2007
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: JaeChon Jo, HeeAn Kwon, HyunSuk Lim, JaeYoung Choi, Kazumi Morikawa, Yoshitake Kanbe, Masahiro Nishimoto, MyungHwa Kim, Yoshikazu Nishimura
  • Patent number: 7173043
    Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
    Type: Grant
    Filed: July 8, 2005
    Date of Patent: February 6, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Jean Ackermann, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
  • Patent number: 7084136
    Abstract: A compound of the formula (I): wherein A is alkylene optionally having an unsaturated bond; R is —C(?O)—R1; R1 is hydroxy or the like; m is 0 or 1; p is 0 or 1; X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl or the like; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, having a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor is found.
    Type: Grant
    Filed: May 28, 2001
    Date of Patent: August 1, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Norihiko Tanimoto, Akinori Arimura
  • Patent number: 7008958
    Abstract: Compounds having the formula (I), are effective as inhibitors of IMPDH enzyme, wherein R3 is alkyl, substituted alkyl, alkoxy, haloalkoxy, or halogen, preferably methoxy, ethoxy, or trifluoromethoxy; and R1, R2, R4, and R5 are as defined in the specification.
    Type: Grant
    Filed: May 20, 2003
    Date of Patent: March 7, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott H. Watterson, T. G. Murali Dhar, Edwin J. Iwan wicz
  • Patent number: 6946462
    Abstract: New compounds represented by the formula or pharmaceutically acceptable salts or prodrugs thereof, wherein X1 and X2 are each independently selected from a CH group or a nitrogen atom; and R is an optionally substituted five or six membered nonaromatic carbocyclic ring or a nonaromatic or aromatic heterocyclic ring, whereby the ring is optionally condensed with a 6-membered, optionally substituted carbocyclic aromatic ring.
    Type: Grant
    Filed: April 13, 2004
    Date of Patent: September 20, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rainer Haag, Ulrike Leser-Reiff, Anja Limberg, Michael Weidner, Gerd Zimmermann
  • Patent number: 6930190
    Abstract: A process for preparing heterocyclic pentalene derivative having formula (I): wherein w is a sulfur atom (S), an oxygen atom (O) or a NR or PR group, wherein R is an hydrocarbon group; R1, R2, R3, and R4, equal to or different from each other, are hydrogen atoms or hydrocarbon groups; said process comprising the following steps: a) contacting a compound of formula (II) T is a OR, NR2, CCI3, CF3, Cl, Br, I, imidazolil or pirazolyl radical; with at least one molar equivalent of a vinyl compound of formula (III): wherein M is MgHal, Li, K, ZnHal, wherein Hal is chlorine, bromine or iodine; (II), (III) b) treating the compound of formula obtained in step a) with a Bronsted acid; c) treating the compound obtained in step b) with a reducing agent; and d) dehydrating the alcohol obtained in step c) in order to obtain the compound of formula (I).
    Type: Grant
    Filed: July 10, 2002
    Date of Patent: August 16, 2005
    Assignee: Basell Polyolefine GmbH
    Inventors: Ilya E Nifant'ev, Vladimir V. Bagrov
  • Patent number: 6900196
    Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.
    Type: Grant
    Filed: July 6, 2004
    Date of Patent: May 31, 2005
    Assignee: Eli Lilly and Company
    Inventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
  • Patent number: 6884896
    Abstract: The present invention is 3,4-disubstituted-benzo[b]thiophene derivatives represented by general formula (I) and processes for preparing compounds represented by general formula (V) from compounds represented by general formula (IV), preparing a mixture of compounds represented by the following formula (II) and the following formula (III) and preparing the benzo[b]thiophene derivatives represented by the above formula (I): wherein, R1 and R2 represent each a halogen atom, a trihalomethyl group, a C1-4 alkyl group or a C1-4 alkoxy group; X represents a hydroxy group or a halogen atom; R3 and R4 represent each a hydrogen or a halogen atom, a trihalomethyl group, a C1-4 alkyl group or a C1-4 alkoxy group; and R5 represents a C1-3 alkyl group or a trifluoromethyl group.
    Type: Grant
    Filed: February 22, 2002
    Date of Patent: April 26, 2005
    Assignee: Teijin Limited
    Inventors: Hiroshi Saitoh, Naoki Tsuchiya, Tsuyoshi Mizuno, Tomohide Ida, Yoshiyuki Sawai
  • Patent number: 6869953
    Abstract: New compounds represented by the formula or pharmaceutically acceptable salts or prodrugs thereof, wherein X1 and X2 are each independently selected from a CH group or a nitrogen atom; and R is an optionally substituted five or six membered nonaromatic carbocyclic ring or a nonaromatic or aromatic heterocyclic ring, whereby the ring is optionally condensed with a 6-membered, optionally substituted carbocyclic aromatic ring.
    Type: Grant
    Filed: August 6, 2002
    Date of Patent: March 22, 2005
    Assignee: Hoffman-La Roche Inc.
    Inventors: Rainer Haag, Ulrike Leser-Reiff, Anja Limberg, Michael Weidner, Gerd Zimmermann
  • Patent number: 6869974
    Abstract: Compounds or their salts having general formulas (I) and (II): wherein s is an integer equal to 1 or 2, A is the radical of a drug that satisfies certain pharmacological tests, C and C1 are bivalent radicals, and precursors of the radicals B and B1 satisfy certain pharmacological tests.
    Type: Grant
    Filed: April 11, 2000
    Date of Patent: March 22, 2005
    Assignee: Nicox S.A.
    Inventor: Piero Del Soldato
  • Patent number: 6849658
    Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R1 is CH3, —CH2—O—R6, —OR6 or —COR7; R2 is —OR8, —SR8 or a polyether radical if in the latter case R4 is C1-C20alkyl and is in ortho or meta position relative to X—Ar; R3 is alkyl or R2 and R3 together form a cycle optionally interrupted by O or S; R4 is aryl radical; R5 is H, halogen, C1-C20 alkyl or —OR8; R6 is H, alkyl or —COR9; R7 is H, alkyl, —N(r?)(r?) or —OR10; R8 is H, alkyl or —COR9; R9 is alkyl; R10 is H, C1-C20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aralkyl or a sugar residue, r? and r? are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R11 is H or —OR6; R12 is H or alkyl; or R11 and R12 form an oxo radical, and the salts, optical and geometrical isomers of the compounds of formula (I).
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: February 1, 2005
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Simon Trouille
  • Patent number: 6831075
    Abstract: The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.
    Type: Grant
    Filed: August 22, 2002
    Date of Patent: December 14, 2004
    Assignee: Cephalon, Inc.
    Inventors: Jasbir Singh, Rabindranath Tripathy
  • Publication number: 20040242897
    Abstract: Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
    Type: Application
    Filed: December 10, 2003
    Publication date: December 2, 2004
    Inventors: Andrei P. Guzaev, Muthiah Manoharan
  • Patent number: 6818666
    Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.
    Type: Grant
    Filed: August 9, 2002
    Date of Patent: November 16, 2004
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Philippe Diaz
  • Publication number: 20040209778
    Abstract: The invention provides a lactone derivative of formula (I) which exhibits excellent rooting activity, and a plant growth regulator containing the derivative as an active ingredient.
    Type: Application
    Filed: February 20, 2004
    Publication date: October 21, 2004
    Inventors: Koji Kobayashi, Mineyuki Yokoyama
  • Publication number: 20040192940
    Abstract: In various embodiments, chromophores are described that include novel electron acceptors, novel electron donors, and/or novel conjugated bridges that are useful in nonlinear optical applications. In some embodiments, the present invention provides chromophore architectures wherein a chromophore contains more than one electron acceptor in electronic communication with a single electron donor, and/or more than one electron donor in electronic communication with a single electron acceptor. Also described is processes for providing materials comprising the novel chromophores and polymer matrices containing the novel chromophores. Electro-optic devices described herein contain one or more of the described electron acceptors, electron donors, conjugated bridges, or chromophores.
    Type: Application
    Filed: February 10, 2004
    Publication date: September 30, 2004
    Applicant: Lumera Corporation, a Washington corporation
    Inventors: Diyun Huang, Timothy M. Londergan, Galina K. Todorova, Jingsong Zhu
  • Publication number: 20040192931
    Abstract: A process for preparing heterocyclic pentalene derivative having formula (I): wherein w is a sulfur atom (S), an oxygen atom (O) or a NR or PR group, wherein R is an hydrocarbon group; R1, R2, R3, and R4, equal to or different from each other, are hydrogen atoms or hydrocarbon groups; said process comprising the following steps: a) contacting a compound of formula (II) T is a OR, NR2, CCI3, CF3, Cl, Br, I, imidazolil or pirazolyl radical; with at least one molar equivalent of a vinyl compound of formula (III): wherein M is MgHal, Li, K, ZnHal, wherein Hal is chlorine, bromine or iodine; (II), (III) b) treating the compound of formula obtained in step a) with a Bronsted acid; c) treating the compound obtained in step b) with a reducing agent; and d) dehydrating the alcohol obtained in step c) in order to obtain the compound of formula (I).
    Type: Application
    Filed: January 30, 2004
    Publication date: September 30, 2004
    Inventors: Ilya E Nifant'ev, Vladimir V. Bagrov
  • Publication number: 20040138282
    Abstract: The present invention provides compounds and methods of administering compounds to a subject taht can reduce &bgr;APP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce &bgr;APP production and that is not tocix in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease &bgr;APP production.
    Type: Application
    Filed: February 6, 2004
    Publication date: July 15, 2004
    Inventors: Nigel H. Greig, Karen T. Y. Shaw, Qiang-Sheng Yu, Harold W. Holloway, Timothy T. Sencrant, Tada Utsuki, Donald K. Ingram, Arnold Brossi, Anthony Giordano, Gordon Powers, Diane Davidson, Michael Sturgess
  • Publication number: 20040127543
    Abstract: Compounds of the Formula I: 1
    Type: Application
    Filed: September 10, 2003
    Publication date: July 1, 2004
    Inventors: Deborah Ann Evrard, Uresh Shantilal Shah, Gary Paul Stack
  • Publication number: 20040127723
    Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.
    Type: Application
    Filed: January 22, 2004
    Publication date: July 1, 2004
    Inventors: Michelangelo Scalone, Thomas Albert Zeibig
  • Patent number: 6756342
    Abstract: The invention relates to novel substituted thienocycloalk(en)ylamino-1,3,5-triazines of the general formula (I) in which Z, R1, R2, R3 are as defined in the description, and to processes for their preparation, to there use as herbicides and to the intermediates required for their preparation including their preparation processes in the case of the preferred compounds.
    Type: Grant
    Filed: March 4, 2002
    Date of Patent: June 29, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Kristian Kather, Stefan Lehr, Hans-Jochem Riebel, Katharina Voigt, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
  • Publication number: 20040116353
    Abstract: The invention relates to compounds of formula: 1
    Type: Application
    Filed: September 18, 2003
    Publication date: June 17, 2004
    Inventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
  • Publication number: 20040110951
    Abstract: The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands.
    Type: Application
    Filed: July 11, 2003
    Publication date: June 10, 2004
    Inventor: Yuan-Ching P. Chiang
  • Patent number: 6730705
    Abstract: The invention relates to new alkoximinoacetic acid amides, a process for their preparation and their use as agents for combating pests.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: May 4, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Seitz, Gerd Hänssler, Klaus Stenzel
  • Publication number: 20040077882
    Abstract: Bicyclic cyclopropane derivatives of the general Formula (I) 1
    Type: Application
    Filed: September 9, 2003
    Publication date: April 22, 2004
    Inventors: Norbert Moszner, Armin de Meijere, Frank Zeuner, Urs Karl Fischer
  • Publication number: 20040063968
    Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.
    Type: Application
    Filed: September 16, 2003
    Publication date: April 1, 2004
    Inventors: Pete Delgado, Raymond E. Conrow, William D. Dean, Michael S. Gaines
  • Publication number: 20040063755
    Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds of formula (I): 1
    Type: Application
    Filed: August 18, 2003
    Publication date: April 1, 2004
    Inventors: Edmund J. Moran, John R. Jacobsen, Michael R. Leadbetter, Matthew B. Nodwell, Sean G. Trapp, James Aggen, Timothy J. Church
  • Patent number: 6703416
    Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R1 is CH3, —CH2—O—R6, —OR6 or —COR7; R2 is —OR8, —SR8 or a polyether radical if in the latter case R4 is C1-C20alkyl and is in ortho or meta position relative to X—Ar; R3 is alkyl or R2 and R3 together form a cycle optionally interrupted by O or S; R4 is aryl radical; R5 is H, halogen, C1-C20 alkyl or —OR8; R6 is H, alkyl or —COR9; R7 is H, alkyl, —N(r′)(r″) or —OR10; R8 is H, alkyl or —COR9; R9 is alkyl; R10 is H, C1-C20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aralkyl or a sugar residue, r′ and r″ are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R11 is H or —OR6; R12 is H or alkyl; or R11 and R12 form an oxo radical, and the salts, optical and geometrical isomers of
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: March 9, 2004
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Simon Trouille
  • Publication number: 20040044059
    Abstract: A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.
    Type: Application
    Filed: April 29, 2003
    Publication date: March 4, 2004
    Inventors: Kevin G. Pinney, Vani P. Mocharla, Zhi Chen, Charles M. Garner, Mallinath Hadimani, Raymond Kessler, James M. Dorsey, Klaus Edvardsen, David J. Chaplin, Joseph Prezioso, Anjan Ghatak, Usha Ghatak
  • Patent number: 6696110
    Abstract: Liquid crystal mixtures comprising at least one of the compounds of formula (I) containing a heterocyclic five-membered ring and with a carbon-carbon double bond in the termninal group are new. RJ=CnH2n+1CH=CHCmH2mZ1; n=1-5; m=0-5; and q=0, 1 or 2; A1 and A2=2,5-disubstituted furan, 2,5-disubstituted thiophene, 2,5-disubstituted oxazole, 2,5-disubstituted thiazole, 2,5-disubstituted 1,3,4-oxadiazole, 2,5-disubstituted 1,3,4-thiadiazole, 1,4-disubstituted benzene, 2,5-disubstituted pyrimidine, 2,5-disubstituted pyridine, 2,6-disubstituted naphthalene; laterally substituted 1,4-disubstituted benzene, laterally substituted 2,5-disubstituted pyrimidine, laterally substituted 2,5-disubstituted pyridine or laterally substituted 2,6-disubstituted naphthalene (lateral substituents=F, Cl, Br or CN); A3=any A1 or 1,4-disubstituted bicyclo(2.2.
    Type: Grant
    Filed: November 26, 2001
    Date of Patent: February 24, 2004
    Assignee: Qinetiq Limited
    Inventors: Rachel P Tuffin, Steven M Kelly, Neil L Campbell, Warren L Duffy, Janine H Wild
  • Publication number: 20040024190
    Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: 1
    Type: Application
    Filed: July 18, 2002
    Publication date: February 5, 2004
    Applicant: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-Andre Poupart, Jean Rancourt
  • Patent number: RE39754
    Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.
    Type: Grant
    Filed: August 14, 2003
    Date of Patent: July 31, 2007
    Assignee: Schering AG
    Inventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka