The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/267)
  • Publication number: 20150057280
    Abstract: The invention relates to pyridylidene compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted pyridylidene compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted pyridylidene compounds. The N-substituted pyridylidene compounds of the present invention are defined by the following formula I: wherein X, Het, R1, R2, R3, R4 and R6 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Applicant: BASF SE
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Korber
  • Publication number: 20140343284
    Abstract: A compound of Formula 2 is disclosed wherein R1, MA and MB are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 1 wherein RI and X are as defined in the disclosure comprising contacting a compound of Formula 2 with a halogenating agent. Also disclosed is a method for preparing a compound of Formula 4 wherein R1, R3 and R4 are as defined in the disclosure, comprising reacting a compound of Formula 5 wherein R3 and R4 are as defined in the disclosure with a compound of Formula 1, with a compound of Formula 1, the process of preparing the compound of Formula 4 includes the step of preparing the compound of Formula 1 from the compound of Formula 2 by the method disclosed above. Also disclosed is compound that is methyl 3,5-dichlorobenzeneethanimidate methyl 3,5-dichlorobenzeneethanimidate or ethyl 3,5-dichlorobenzeneethanimidate or salts thereof.
    Type: Application
    Filed: December 13, 2012
    Publication date: November 20, 2014
    Inventor: Wenming Zhang
  • Publication number: 20140193518
    Abstract: The invention relates to kinase inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating disorders, especially cancer.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 10, 2014
    Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
    Inventor: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
  • Patent number: 8569345
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: October 29, 2013
    Inventors: Valentina Molteni, Xiaolin Li, Juliet Nabakka, David Archer Ellis, Beth Anaclerio, Enrique Saez, John Wityak
  • Patent number: 8470854
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Grant
    Filed: April 12, 2012
    Date of Patent: June 25, 2013
    Assignee: Bristol-Meyers Squibb Company
    Inventor: Donald J. P. Pinto
  • Patent number: 8455654
    Abstract: A nanoscale pigment particle composition includes an organic benzimidazolone pigment, and a sterically bulky stabilizer compound, wherein the benzimidazolone pigment associates non-covalently with the sterically bulky stabilizer compound that is a substituted pyridine derivative; and the presence of the associated stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: June 4, 2013
    Assignees: Xerox Corporation, National Research Council of Canada
    Inventors: Rina Carlini, Darren Andrew Makeiff
  • Publication number: 20120214996
    Abstract: Dibenzylidene and heterobenzylideneacetone derivatives, related 4-piperidones, related 4-thiopyranones and the corresponding sulfinyl- and sulfonyl-analogues for their use for prophylaxis or treatment of trypanosomiasis and leishmaniasis.
    Type: Application
    Filed: September 20, 2010
    Publication date: August 23, 2012
    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Elisabeth Davioud-Charvet, Ingrid Nicole Wenzel, Thomas J.J. Muller, Gilles Hanquet, Don Antoine Lanfranchi, Frederic Leroux, Thibault Gendron
  • Patent number: 8188120
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: May 29, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventor: Donald J. P. Pinto
  • Publication number: 20120095051
    Abstract: This invention provides a compound having the structure wherein ?, ?, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.
    Type: Application
    Filed: May 14, 2010
    Publication date: April 19, 2012
    Inventors: Francis Johnson, Lorne Golub
  • Patent number: 8093385
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: January 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Romyr Dominique, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri
  • Publication number: 20110235150
    Abstract: Disclosed is an electrochromic material including a compound represented by Chemical Formula 1 and an electrochromic device including the electrochromic material. In Chemical Formula 1, R1, R2, L1, and L2 are as defined in the detailed description.
    Type: Application
    Filed: March 3, 2011
    Publication date: September 29, 2011
    Applicant: SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Rupasree Ragini DAS, Ji-Min LEE, Chang-Ho NOH, Seog-Jin JEON
  • Publication number: 20110105432
    Abstract: The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.
    Type: Application
    Filed: January 7, 2011
    Publication date: May 5, 2011
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromu HABASHITA, Haruto Kurata, Shinji Nakade
  • Patent number: 7901559
    Abstract: It is intended to provide a method for easily detecting a phosphorylated peptide (protein) in a test sample by using SDS-polyacrylamide gel electrophoresis (SDS-PAGE) which has been conventionally employed in analyzing a protein; a polyacrylamide gel for electrophoresis to be used in the method; a method of producing the gel; and a synthesizing intermediate in producing the gel. The polyacrylamide gel for electrophoresis to be used in the method of the invention is characterized in that at least a part of the structure thereof has a structure represented by the following formula (I); wherein M2+represents a transition metal ion; and X represents a linker group.
    Type: Grant
    Filed: August 1, 2005
    Date of Patent: March 8, 2011
    Assignee: Nard Institute, Ltd.
    Inventors: Tohru Koike, Akihiko Kawasaki, Tatsuhiro Kobashi
  • Publication number: 20110039841
    Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.
    Type: Application
    Filed: May 3, 2005
    Publication date: February 17, 2011
    Applicants: Novo Nordisk A/S
    Inventors: Zdenék Polivka, Karel Sindelar, Per Sauerberg, Ingrid Pettersson
  • Publication number: 20100261758
    Abstract: Compounds of Formula (I) wherein R1 is aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R2 is defined heterocyclyl, R3 is alkyl, aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R4 is H or alkyl, or R3 and R4 together with the carbon atom to which they are attached are cycloalkyl fused with aryl, and their use as pharmaceuticals.
    Type: Application
    Filed: March 28, 2007
    Publication date: October 14, 2010
    Applicant: NOVARTIS AG
    Inventors: Luca Arista, Klemens Hogenauer, Niko Schmiedeberg, Gudrun Werner, Herbert Jaksche
  • Publication number: 20100249139
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: March 19, 2010
    Publication date: September 30, 2010
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Publication number: 20090209588
    Abstract: Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hyper-triglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.
    Type: Application
    Filed: May 3, 2005
    Publication date: August 20, 2009
    Applicant: Novo Nordisk A/S
    Inventors: Miroslav Havranek, Per Sauerberg, Ingrid Pettersson, Pavel Pihera, Søren Ebdrup
  • Publication number: 20090054466
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification.
    Type: Application
    Filed: July 28, 2008
    Publication date: February 26, 2009
    Inventors: Romyr Dominique, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri
  • Patent number: 7459415
    Abstract: Embodiments relate to lubricants disposed over magnetic storage media, such as rotatable thin film magnetic discs. One embodiment comprises a lubricant compound of a fluoropolyether chain having one or more carbonyl-imide pairs. For example, the carbonyl-imide pair may be located at one end, both ends, and/or in the middle of the fluoropolyether chain.
    Type: Grant
    Filed: October 13, 2004
    Date of Patent: December 2, 2008
    Assignee: Seagate Technology LLC
    Inventors: Jianwei Liu, Michael Joseph Stirniman, Jing Gui
  • Patent number: 7273878
    Abstract: A difluoroalkene derivative which is sufficiently effective in controlling various pests even when used in a small dose and is highly safe for crops, natural enemies to the pests, and animals; and an intermediate for the derivative.
    Type: Grant
    Filed: September 30, 2002
    Date of Patent: September 25, 2007
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Tetsuya Abe, Ryuji Tamai, Minoru Ito, Masatoshi Tamaru, Hiroyuki Yano, Satoru Takahashi, Norimichi Muramatsu
  • Patent number: 6953798
    Abstract: Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra?)R??(1) Ar1 is an optionally substituted aromatic or heteroarotic group; L1 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of ?4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: October 11, 2005
    Assignee: Celltech R&D Limited
    Inventors: John Robert Porter, John Clifford Head, Graham John Warrellow, Sarah Catherine Archibald
  • Patent number: 6833378
    Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.
    Type: Grant
    Filed: January 17, 2001
    Date of Patent: December 21, 2004
    Assignee: Pfizer Inc
    Inventor: Yuhpyng L. Chen
  • Patent number: 6794380
    Abstract: The invention concerns amide derivatives of the Formula I wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Grant
    Filed: January 29, 2003
    Date of Patent: September 21, 2004
    Assignee: AstraZeneca AB
    Inventor: Dearg S Brown
  • Publication number: 20040147559
    Abstract: There are disclosed compounds of the formula 1
    Type: Application
    Filed: July 30, 2003
    Publication date: July 29, 2004
    Applicant: Schering Corporation and Pharmacopeia, Inc.
    Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, Laura L. Rokosz, James P. Jakway, Gaifa Lai, Minglang Wu, Evan A. Hecker, Daniel Lundell, Jay S. Fine
  • Publication number: 20030225099
    Abstract: Ortho, meta-substituted bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.
    Type: Application
    Filed: June 4, 2003
    Publication date: December 4, 2003
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
  • Publication number: 20030203933
    Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.
    Type: Application
    Filed: April 17, 2002
    Publication date: October 30, 2003
    Inventors: Kuo-Hsiung Lee, Junko Ishida, Hironori Ohtsu, Hui-Kang Wang, Hideji Itokawa, Chawnshang Chang, Charles C-Y. Shih
  • Publication number: 20030114701
    Abstract: In a process for producing a polynitrile compound comprising introducing a polysubstituted organic compound (POC) which is a carbon ring or heterocyclic compounds having a plurality of organic substituents into a reactor with ammonia and a gas containing oxygen and ammoxidizing POC in the presence of a catalyst, at least a portion of the unreacted POC and a mononitrile compound of an intermediate product in the reaction gas discharged from the reactor is separated, recovered and recycled to the reactor so that the flow rate of the mononitrile compound at the outlet of the reactor is 2 to 16% by mole of the total flow rate of POC and the mononitrile compound supplied to the reactor.
    Type: Application
    Filed: December 6, 2002
    Publication date: June 19, 2003
    Inventors: Kenichi Nakamura, Shuji Ebata, Fumio Tanaka, Takuji Shitara
  • Patent number: 6548514
    Abstract: The invention concerns amide derivatives of the Formula I wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: April 15, 2003
    Assignee: Astrazeneca AB
    Inventor: Dearg S. Brown
  • Patent number: 6531495
    Abstract: Compounds of the formula I, in which R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(8), R(30) and R(31) have the meanings indicated in the claims, are very particularly suitable as novel and antiarrythmic active compounds, in particular for the treatment and prophylaxis of atrial arrythmias, e.g. atrial fibrillation (AF), or atrial flutter.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: March 11, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Joachim Brendel, Wolfgang Schmidt, Peter Below
  • Patent number: 6458957
    Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.
    Type: Grant
    Filed: July 12, 2000
    Date of Patent: October 1, 2002
    Assignee: Geneva Pharmaceuticals, Inc.
    Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
  • Patent number: 6436963
    Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with (derivatised) hydroxyalkyl substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: August 20, 2002
    Assignee: Dow AgroSciences LLC
    Inventors: Emily J. Canada, Robert P. Gajewski, Christopher S. Galka, Neil V. Kirby, Irene M. Morrison, Jeannie R. Phillips, Mary E. Pieczko, Brent J. Rieder, Chrislyn M. Carson, Zhengyu Huang
  • Patent number: 6355810
    Abstract: Disclosed are multibinding compounds which inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-COA reductase), the rate limiting enzyme in cholesterol biosynthesis. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to HMG-CoA reductase and the distance between ligands is at least 10 Å. The multibinding compounds of this invention are useful in the treatment and prevention of hypercholesterolemia, hyperlipidemia, atherosclerosis and the like.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: March 12, 2002
    Assignee: Advanced Medicine, Inc.
    Inventors: John H. Griffin, Michael R. Leadbetter, Donald E. Schmidt, Jr.
  • Publication number: 20010039353
    Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided.
    Type: Application
    Filed: February 21, 2001
    Publication date: November 8, 2001
    Inventors: Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
  • Patent number: 6127529
    Abstract: Bifuncitonal chelating pyridine compound and its use for conferring chelating properties on organic compounds. The pyridine compound has the structure ##STR1## where (i) n is an integer 1 or 2,(ii) R.sub.1, R.sub.2 and R.sub.3 represent groups that have no electrons capable of significantly delocalizing or resonating with the pyridine ring, such as hydrogen, alkyl or aralkyl having an aliphatic carbon atom next to the pyridine ring; at least two of R.sub.1, R.sub.2 and R.sub.
    Type: Grant
    Filed: September 13, 1991
    Date of Patent: October 3, 2000
    Assignee: Wallac Oy
    Inventors: Marek Kwiatkowski, Christian Sund, Jyrki Ylikoski, Veli-Matti Mukkala, Ilkka Hemmila
  • Patent number: 5962479
    Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: October 5, 1999
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng Liang Chen
  • Patent number: 5912388
    Abstract: A process for preparing an aldehyde or ketone comprising reacting a primary or secondary alcohol with oxygen in the presence of a base, a catalytic amount of a copper salt and a suitable lignad under anhydrous conditions.
    Type: Grant
    Filed: November 12, 1997
    Date of Patent: June 15, 1999
    Assignee: Zeneca Limited
    Inventors: Christopher John Urch, Istvan Ettienne Marko, Masao Tuskazaki, Paul Richard Giles, Stephen Martin Brown
  • Patent number: 5908931
    Abstract: The present invention relates particularly to novel preorganized hexadentate ligands that are suitable for completing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.
    Type: Grant
    Filed: December 14, 1990
    Date of Patent: June 1, 1999
    Assignee: Mallinckrodt Inc.
    Inventors: Raghavan Rajagopalan, William L. Neumann, Dennis L. Nosco
  • Patent number: 5719182
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: February 17, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
  • Patent number: 5618826
    Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification; and acid addition and quaternary ammonium salts of formula (I) compounds are described. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: April 8, 1997
    Assignee: University of Florida
    Inventors: Richard H. Hammer, Nicholas S. Bodor
  • Patent number: 5614634
    Abstract: Leukotriene-B.sub.4 analogs of formula I ##STR1## in which R.sup.1 means radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group or R.sup.1 means radical CH.sub.2 OH,B means an alkylene group with 1-3 C atoms in the chain, a radical ##STR2## or a radical ##STR3## with R.sup.3 meaning a hydrogen atom, a carboxy or methoxycarbonyl group, A means groups ##STR4## --NH--CO--, --CO--NH--, --OCH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --COCH.sub.2 -- or --CHOH--CH.sub.2 --,X means N or CH,D means groups or ##STR5## and . . . . . means a single or double bond, as well as optionally their salts with physiologically harmless bases, process for their production and their pharmaceutical use.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: March 25, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5594001
    Abstract: Compounds of Formula (I) have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man where subnormal levels of this neurochemical are found, such as in Alzheimer's disease, and other conditions involving learning and cognition.
    Type: Grant
    Filed: March 28, 1994
    Date of Patent: January 14, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Christopher A. Teleha, Wendell W. Wilkerson, Richard A. Earl
  • Patent number: 5585327
    Abstract: 4-substituted pyridyl-3-carbinols of the formula ##STR1## wherein R is hydrogen, or an acyl, alkyl or carbamyl group exhibit desirable preemergent and postemergent herbicidal activity. Also disclosed are herbicidal compositions comprising such compounds and methods of controlling undesirable vegetation employing such compounds. The compounds wherein AR is hydroxyl serve as useful intermediates for the production of the alpha-benzyl substituted compounds as well as exhibiting herbicidal activity.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: December 17, 1996
    Assignee: Zeneca Limited
    Inventors: Hsiao-Ling Chin, Yi-Qiu Wei, Nhan H. Nguyen, Michael P. Ensminger, Linda Willitts, Derek P. Dagarin
  • Patent number: 5567716
    Abstract: Traumatic acid salts, wherein B is a cation selected from:a) a quaternary ammonium,b) a cation of a linear or branched C.sub.1 -C.sub.20 mono-, di- or trialkanolamine,c) a cation of a biologically active primary, secondary or tertiary amine,d) silver or zinc cation,and relative pharmaceutical compositions administrable by topical or parenteral route For the therapeutic treatment of cutaneous pathologies in which it is important to associate an a bacteriostatic, antibiotic, antifungal or an antiviral activity, to the cicatrizant effect, typical of traumatic acid.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: October 22, 1996
    Assignee: Lifegroup S.p.A.
    Inventors: Francesco Della Valle, Silvana Lorenzi, Gabriele Marcolongo
  • Patent number: 5543423
    Abstract: The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: August 6, 1996
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Robert E. Zelle, Matthew W. Harding
  • Patent number: 5374724
    Abstract: A process for the preparation of a substituted acetic acid of the Formula (2): ##STR1## wherein --X--Z is an optionally substituted aromatic or heteroaromatic optionally substituted amino radical; by reacting a compound of the Formula (7):Z--Y--H Formula 7with glyoxylic acid. The compounds of Formula (2) are useful as intermediates in the preparation of polycyclic dyes.
    Type: Grant
    Filed: November 2, 1992
    Date of Patent: December 20, 1994
    Assignee: Zeneca, Limited
    Inventors: Nigel Hall, Nigel Hughes, Prakash Patel
  • Patent number: 5274184
    Abstract: The present invention relates to compounds of the general formula I ##STR1## wherein A.sup..sym. and B.sup..sym. independently of one another denote a proton, with the limitation that they do not both simultaneously denote protons, the equivalent part of the barium ion, an ion of the general formula II ##STR2## or an ion of the general formula III ##STR3## and wherein R.sup.1 to R.sup.8, R.sup.11 to R.sup.16, X and m and n are as defined in the description, processes for their preparation and their use as charge control agents in toners and developers and as charge improving agents in powders and varnishes.
    Type: Grant
    Filed: October 2, 1991
    Date of Patent: December 28, 1993
    Assignee: Cassella Aktiengesellschaft
    Inventors: Gert Nagl, Hans-Tobias Macholdt
  • Patent number: 5240942
    Abstract: The invention relates to compounds of formula I: ##STR1## in which R.sub.1 represents a naphthyl radical, a dihydronaphthyl radical, a tetrahydronaphthyl radical, a quinolyl radical or a 1,4-benzodioxanyl radical, A represents a single bond, a double bond, a methylene radical, a radical of formula z.sub.1 :--CH.dbd. (z.sub.1)or a radical of formula z.sub.2 :.dbd.CH-- (z.sub.2)the ring B represents a piperidyl radical, a pyrrolidinyl radical, or a 1,2,3,6-tetrahydropyridyl radical, and R.sub.2 represents: a hydrogen atom, a benzyl radical, or an alkyl radical having 1 to 6 carbon atoms, on condition that in one of these cases R.sub.1 is other than a naphthyl (y.sub.1), dihydronaphthyl (y.sub.2) or tetrahydronaphthyl (y.sub.3) radical and B is other than a piperidinyl radical, or an aminoalkyl radical having 1 to 6 carbon atoms, a cyanoalkyl radical having 1 to 6 carbon atoms,or a radical of formula w.sub.1 : ##STR2## in which n is 1-6 and R.sub.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: August 31, 1993
    Assignee: Adir et Compagnie
    Inventors: Gilbert Lavielle, Michel Laubie, Francis Colpaert
  • Patent number: 5185375
    Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl group, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl or two R.sup.1 substituents on the same nitrogen atom may together form optionally substituted alkylene, and salts thereof, processes for their preparation and compositions containing them are described.
    Type: Grant
    Filed: March 30, 1990
    Date of Patent: February 9, 1993
    Assignee: May & Baker Limited
    Inventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. A. Walsh
  • Patent number: 5175167
    Abstract: Hetarylalkenes of the general formula I ##STR1## where Ar is hetaryl,A is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.3 -alkyl or unsubstituted or monosubstituted, disubstituted or trisubstituted aryl or aralkyl, ##STR2## Z is whereR is hydrogen, C.sub.2 -C.sub.4 -acyl, unsubstituted or substituted benzoyl, C.sub.1 -C.sub.4 -alkylsulfonyl, unsubstituted or C.sub.1 -C.sub.4 -alkyl-substituted phenylsulfonyl or a radical R.sup.1,R.sup.1 is C.sub.1 -C.sub.4 -alkyl or unsubstituted or substituted phenyl or benzyland Hal is fluorine, chlorine, bromine or iodine,and B is unsubstituted or substituted mononuclear or dinuclear aryl, aralkyl or hetaryl,and their N-oxides and addition salts, the preparation of these substances, intermediates for this purpose and the preparation thereof, fungicides containing hetarylalkenes and a corresponding method for controlling harmful fungi.
    Type: Grant
    Filed: February 8, 1991
    Date of Patent: December 29, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernhard Zipperer, Manfred Lauer, Norbert Goetz, Thomas Zierke, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5151436
    Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Het represents pyrid-3-yl, isoquinolin-4-yl, tetrahydroquinolin-3-yl, quinolin-3-yl, pyridazin-4-yl, pyrimid-5-yl, thiazol-5-yl, thieno[2,3-b]-pyridin-5-yl, pyrazin-2-yl, indol-3-yl and thieno[3,2-b]-pyridin-6-yl, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl, or two R.sup.1 substituents on the same nitrogen atom may together form an optionally substituted alkylene radical chain and salts thereof, processes for their preparation and compositions containing them are described.
    Type: Grant
    Filed: August 23, 1990
    Date of Patent: September 29, 1992
    Assignee: Rhone-Poulenc Sante
    Inventors: David C. Cook, Terance W. Hart, Iain M. Mc Lay, Malcolm N. Palfreyman, Brian W. Sharp, Roger J. A. Walsh