Chalcogen Or Additional Nitrogen Attached Directly To Ring Carbon Of The Thiadiazole Ring By Nonionic Bonding Patents (Class 548/141)
  • Publication number: 20130289057
    Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.
    Type: Application
    Filed: January 12, 2012
    Publication date: October 31, 2013
    Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN
    Inventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
  • Patent number: 8524894
    Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: September 3, 2013
    Assignee: Laboratorios Salvat, S.A.
    Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleo Mas
  • Publication number: 20130184258
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: October 26, 2012
    Publication date: July 18, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: Vertex Pharmaceuticals Incorporated
  • Patent number: 8455457
    Abstract: Provided herein is a pharmaceutical composition or a kit comprising a combination of a non-selective beta-adrenergic receptor blocker and an adenosine A1 receptor agonist. Also provided herein is a method of reducing intraocular pressure (IOP) in a subject using such a combination or kit. In a particular embodiment, provided herein is a combination of timolol marketed under the brand Timopticâ„¢ and Compound A.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: June 4, 2013
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley
  • Patent number: 8440639
    Abstract: Provided herein is a pharmaceutical composition or a kit comprising a combination of a carbonic anhydrase inhibitor analog and an adenosine A1 receptor agonist. Also provided herein is a method of reducing intraocular pressure (IOP) in a subject using such a combination or kit. In a particular embodiment, provided herein is a combination of dorzolamide marketed under the brand Trusoptâ„¢ and Compound A.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: May 14, 2013
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley
  • Publication number: 20110130397
    Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.
    Type: Application
    Filed: September 21, 2007
    Publication date: June 2, 2011
    Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
  • Patent number: 7348440
    Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: June 12, 2003
    Date of Patent: March 25, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Arrington, Paul J. Coleman, Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, William F. Hoffman, Edward S. Tasber
  • Publication number: 20030216258
    Abstract: Condensed heterocyclic compounds of the general formula: 1
    Type: Application
    Filed: April 25, 2003
    Publication date: November 20, 2003
    Applicant: Sumitomo Chemical Company, Limited
    Inventors: Minoru Takano, Shinichi Kawamura, Takashi Komori
  • Patent number: 6239152
    Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
    Type: Grant
    Filed: January 22, 1999
    Date of Patent: May 29, 2001
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Zhi-Jie Ni, Eric Gordon
  • Patent number: 6197770
    Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where X, W, Z, A, G, R1, R2, R3, R4, R5, R5′ and k have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof Also described are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: March 6, 2001
    Assignee: The Procter & Gamble Co.
    Inventors: Michael George Natchus, Roger Gunnard Bookland, Neil Gregory Almstead, Stanislaw Pikul, Biswanath De, Menyan Cheng
  • Patent number: 5972978
    Abstract: The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: October 26, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
  • Patent number: 5952475
    Abstract: The novel cationic thiadiazolediphenylamine dyes of the formula (I) ##STR1## in which the substituents R.sup.1 to R.sup.9 have the meaning indicated in the description, and their anhydro bases, are suitable for use for inkjet printing and in light-writable data storage media and in dye transfer films.
    Type: Grant
    Filed: June 4, 1998
    Date of Patent: September 14, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventor: Horst Berneth
  • Patent number: 5874382
    Abstract: Compounds of Formula I and II, and their agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein X is a direct bond; O; S; NH; N(C.sub.1 -C.sub.3 alkyl); N(C.sub.1 -C.sub.3 haloalkyl); or N(allyl);R.sup.1 is H; F; Cl; or Br;R.sup.2 is H; F; Cl; Br; CF.sub.3 ; nitro; or cyano;R.sup.4 is H; C.sub.1 -C.sub.3 alkyl; or halogen;R.sup.5 is H; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl; halogen; S(O).sub.2 (C.sub.1 -C.sub.6 alkyl); or C(.dbd.O)R.sup.8 ; orR.sup.4 and R.sup.5 are taken together along with the carbon to which they are attached to form a spiro-cyclopropane ring;and R.sup.3, R.sup.8, and J are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formulae I and II and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I or II.
    Type: Grant
    Filed: January 23, 1998
    Date of Patent: February 23, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Balreddy Kamireddy, William Mark Murray
  • Patent number: 5846906
    Abstract: Herbicidally active phenyldiketone compounds of the formula I ##STR1## in which the substituents have the following meanings: L and M are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.1 -C.sub.4 -alkoxy, it being possible for these groups to be unsubstituted or substituted by one to five halogen atoms or C.sub.1 -C.sub.4 -alkoxy, or halogen, cyano, nitro, a group --(Y).sub.n --S(O).sub.m R.sup.7 or a group --(Y).sub.n --CO--R.sup.8,Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical which has one to three hetero atoms selected from the group consisting of oxygen, sulfur or nitrogen and which is unsubstituted or substituted by halogen, cyano, nitro, a group --CO--R.sup.8, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, di-C.sub.1 -C.sub.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
  • Patent number: 5846907
    Abstract: Pyrazol-4-ylbenzoyl compounds of the formula I ##STR1## where Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical, Q is a pyrazole ring and L and M are as defined in the specification, their use as herbicidal compounds and to processes for preparing the compounds.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslizt
  • Patent number: 5830869
    Abstract: The present invention provides novel thiadiazole amide derivatives represented by formula I ##STR1## The compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, predominantly stromelysins, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthritis, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis, periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, inflammation and other diseases related to connective tissue degradation.
    Type: Grant
    Filed: June 18, 1997
    Date of Patent: November 3, 1998
    Inventors: Mark Allen Mitchell, Heinrich Josef Schostarez, Linda Louise Maggiora, Thomas J. Lindberg
  • Patent number: 5767041
    Abstract: The invention relates to new substituted aryliminoheterocycles of the general formula (I) ##STR1## in which A represents oxygen, sulphur or the group N--R.sup.1 whereR.sup.1 represents hydrogen or in each case optionally substituted alkyl, alkenyl or akinyl,E represents one of the following groups ##STR2## where Q represents oxygen, sulphur or the group N--R.sup.1 (where R.sup.1 has the abovementioned meaning) andR.sup.2 represents hydrogen, cyano or in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl or cycloalkenyl,R represents hydrogen or in each case optionally substituted alkyl, alkenyl or alkinyl, andAr represents in each case optionally substituted monocyclic or bicyclic aryl or heteroaryl,to processes for their preparation and to their use as herbicides.
    Type: Grant
    Filed: January 7, 1997
    Date of Patent: June 16, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Otto Schallner, Andreas Lender, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 5703065
    Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein A, W, P, R.sup.3, Q and R.sup.1 are as defined herein. The compounds of formula I, and pharmaceutically acceptable salts thereof, are substance P antagonists and as such are useful in the treament of various inflammatory and central nervous system disorders.
    Type: Grant
    Filed: May 7, 1996
    Date of Patent: December 30, 1997
    Assignee: Pfizer Inc.
    Inventor: Harry R. Howard, Jr.
  • Patent number: 5580964
    Abstract: Cationic 1,3,4-thiadiazole dyestuffs of the formula ##STR1## in which the symbols used have the meaning given in the description, corresponding anhydrobases, processes for the preparation of the cationic 1,3,4-thiadiazole dyestuffs, their use for dyeing and printing various materials and as dichroic dyestuffs in polarizing films, and various materials which comprise such dyestuffs.
    Type: Grant
    Filed: March 23, 1995
    Date of Patent: December 3, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Berneth, Uwe Claussen, Werner Hartwich, Peter Wild
  • Patent number: 5512190
    Abstract: The present invention provides a lubricating oil additive which provides anti-wear properties to a lubricating oil. The additive is the reaction product of 2,5-dimercapto-1,3,4-thiadiazole and a mixture of unsaturated mono-, di-, and tri-glycerides. The present invention also provides a lubricating oil additive with anti-wear properties produced by reacting a mixture of unsaturated mono-, di-, and tri-glycerides with diethanolamine to provide an intermediate reaction product and reacting the intermediate reaction product with 2,5-dimercapto-1,3,4-thiadiazole.
    Type: Grant
    Filed: August 22, 1994
    Date of Patent: April 30, 1996
    Assignee: Texaco Inc.
    Inventors: Gregory P. Anderson, Julian H. Dancy, Doris Love, Jayne M. Lucas
  • Patent number: 5484763
    Abstract: There are provided substituted benzisoxazole and benzisothiazole compounds having the structural formula I ##STR1## Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.
    Type: Grant
    Filed: February 10, 1995
    Date of Patent: January 16, 1996
    Assignee: American Cyanamid Company
    Inventor: Peter J. Wepplo
  • Patent number: 5462952
    Abstract: The present invention is novel compounds which are 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, and pharamaceutically acceptable acid addition or base salts thereof having activity as inhibitors of singly or together 5-lipoxygenase and cyclooxygenase, and pharmaceutical compositions or methods of use therefor.
    Type: Grant
    Filed: September 8, 1993
    Date of Patent: October 31, 1995
    Assignee: Warner-Lambert Company
    Inventors: Diane H. Boschelli, David T. Connor, Milton L. Hoefle
  • Patent number: 5436323
    Abstract: Cationic 1,3,4-thiadiazolyldiphenylamine dyestuffs and corresponding anhydro bases, the dyestuffs having the formula (I) ##STR1## their preparation and their use, and materials dyed with such dyestuffs.
    Type: Grant
    Filed: July 1, 1993
    Date of Patent: July 25, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Berneth, Werner Hartwich, Karl-Heinrich Lange
  • Patent number: 5401743
    Abstract: Aminoalkyl-substituted 2-amino-5-mercapto-1,3,4-thiadiazole derivatives of the formula ##STR1## where A and n have the meanings stated in the description, and the preparation thereof are described. The compounds are suitable for controlling diseases.
    Type: Grant
    Filed: December 13, 1993
    Date of Patent: March 28, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Beatrice Rendenbach-Mueller, Hans-Juergen Teschendorf, Liliane Unger
  • Patent number: 5401853
    Abstract: Thiadiazole derivatives of general formula (I) ##STR1## wherein R.sub.1 is selected from the class consisting of: C.sub.1 -C.sub.10 linear or branched alkyl, benzyl, optionally substituted at the aromatic ring with one or more groups selected on their turn from the class consisting of : C.sub.1 -C.sub.20 linear or branched alkyl residues , nitro groups, halogen atoms, C.sub.1 -C.sub.20 linear or branched alkoxy, hydroxy and C.sub.2 -C.sub.20 linear or branched acyloxy groups, R.sub.2 is selected from H, C.sub.2 -C.sub.10 alkanoyl, cycloalkanoyl wherein this ring has from 3 to 10 carbon atoms, aroyl, and R.sub.3 is selected from H and C.sub.1 -C.sub.10 alkyl, for the treatment of depressive states and anxiety, a process for their preparation and relative pharmaceutical compositions containing them as the active ingredient.
    Type: Grant
    Filed: July 9, 1993
    Date of Patent: March 28, 1995
    Assignee: Laboratorio Farmaceutico C.T. S.r.l.
    Inventors: Mario Brufani, Antonella Loche, Vincenzo Perlini, Donato Pocar
  • Patent number: 5328994
    Abstract: New azinoneutromethines of the formula ##STR1## in which the symbols used have the meaning given in the description, a process for their preparation and their use in thermal and photochromic recording materials, as nonlinear optical materials, as photoconductors in electrophotography and for dyeing fibres and woven fabrics of polyester and plastics.
    Type: Grant
    Filed: February 19, 1993
    Date of Patent: July 12, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Berneth, Karin Hassenruck
  • Patent number: 5314891
    Abstract: The invention concerns benzenesulphonamide derivatives of the formula I ##STR1## wherein R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl;R.sup.2 and R.sup.3 together form --A.sup.2 --X.sup.2 --A.sup.3 -- which defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio or imino;Ar is optionally substituted phenylene;R.sup.4 is (1-4C)alkyl, fluoro-(2-4C)alkyl or optionally substituted phenyl or a heterocyclic moiety;R.sup.5 is hydrogen or (1-4C)alkyl; andR.sup.6 is hydrogen, halogeno, trifluoromethyl, (1-4C)alkyl or (1-4C)alkoxy;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: May 24, 1994
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Philip N. Edwards, Keith Oldham, David Waterson
  • Patent number: 5294709
    Abstract: Methine compounds represented by the following general formula (Ia) or (Ib); ##STR1## wherein CYA represents atoms having a cyanine chromogen structure, MER represents atoms having a merocyanine chromogen structure, L represents a divalent linkage group composed of an atom or atoms containing at least one of a carbon atom, a nitrogen atom, a sulfur atom and an oxygen atom, Het represents a group containing a 5- to 7-membered hetero ring containing at least one nitrogen atom, l.sub.1 represents 1 or 2, l.sub.2 represents 0 or 1, and l.sub.3 represents 1, 2 or 3. Methine dyes using same are also disclosed.
    Type: Grant
    Filed: January 14, 1993
    Date of Patent: March 15, 1994
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Toshinao Ukai, Yoshio Inagaki
  • Patent number: 5294596
    Abstract: The invention relates to novel heterocyclyltriazolinones of the general formula (I) ##STR1## in which R.sup.1 represents hydrogen or represents alkyl or cycloalkyl, each of which is optionally substituted,R.sup.2 represents hydrogen, hydroxyl, mercapto or halogen or represents alkyl, alkenyl, alkinyl, cycloalkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, arylalkyl, amino or heterocyclyl, each of which is optionally substituted, andHet represents an optionally substituted heterocycle of the formula ##STR2## in which X in each case represents oxygen, sulphur, an NH group or an N-alkyl group,a process for their preparation and their use as herbicides.
    Type: Grant
    Filed: July 21, 1993
    Date of Patent: March 15, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wilhelm Haas, Kurt Findeisen, Karl-Heinz Linker, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
  • Patent number: 5242937
    Abstract: The present invention is directed to a compound of the formula: ##STR1## or pharmaceutically acceptable salts thereof which are useful in the treatment of glaucoma and in the assessment of corneal function.
    Type: Grant
    Filed: March 19, 1990
    Date of Patent: September 7, 1993
    Assignee: Research Corporation Technologies, Inc.
    Inventor: William M. Pierce, Jr.
  • Patent number: 5223616
    Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: June 29, 1993
    Assignee: Sumitomo Chemical Company, Ltd.
    Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
  • Patent number: 5217502
    Abstract: Quaternary ammonium salt derived thiadiazoles provide multifunctional antioxidant/antiwear characteristics to fuels.
    Type: Grant
    Filed: June 23, 1992
    Date of Patent: June 8, 1993
    Assignee: Mobil Oil Corporation
    Inventors: Shih-Ying Hsu, Andrew G. Horodysky
  • Patent number: 5205945
    Abstract: A multifunctional antioxidant, antiwear and dispersancy additive for fuels and lubricants is a reaction product of a thiol-substituted diazole, such as aminomercaptothiadiazole (AMTD) or dimercaptothiadiazole (DMTD), an aldehyde and a hydrocarbon-substituted succinimide dimer. The succinimide dimer is derived from polyisobutenyl succinimide and tetraethylenepentamine which are reacted in a mole ratio of 2:1.
    Type: Grant
    Filed: October 18, 1991
    Date of Patent: April 27, 1993
    Assignee: Mobil Oil Corporation
    Inventors: Angeline B. Cardis, Arjun K. Goyal, Virginia C. Wiszniewski
  • Patent number: 5196434
    Abstract: Compound of general formula (I): ##STR1## where R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description.Medicinal products.
    Type: Grant
    Filed: September 26, 1991
    Date of Patent: March 23, 1993
    Assignee: Adir et Compagnie
    Inventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
  • Patent number: 5190963
    Abstract: Cyclopropane(thio)carboxamides of the general formula I ##STR1## where the index and the substituents have the following meanings: n is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different when n is 2;A.sup.1 and A.sup.2 are substituted or unsubstituted alkylene;R.sup.1 is hydrogen, halogen or alkyl;R.sup.2 is halogen or alkyl;X is substituted or unsubstituted 5-membered heteroaryl, substituted or unsubstituted pyrazolyl-1-oxy or triazolyl-1-oxy; andY is oxygen or sulfur,processes for their manufacture, intermediates therefor, and the use of compounds I.
    Type: Grant
    Filed: February 3, 1992
    Date of Patent: March 2, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Christoph Nuebling, Hans Theobald, Uwe Kardorff, Wolfgang Krieg, Christoph Kuenast
  • Patent number: 5126397
    Abstract: Quaternary ammonium salt derived thiadiazoles provide multifunctional antioxidant/antiwear characteristics to lubricants when incorporated therein.
    Type: Grant
    Filed: March 13, 1991
    Date of Patent: June 30, 1992
    Assignee: Mobil Oil Corporation
    Inventors: Andrew G. Horodysky, Shih-Ying Hsu
  • Patent number: 5116853
    Abstract: Novel phenylene derivatives shown by the general formula ##STR1## wherein A represents a hydrogen atom, a phenyl group or a phenoxy group, n represents an integer of 3 to 10, R.sub.1 represents a hydrogen atom or a lower alkoxy group, X.sub.1 represents --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CONH--, B represents ##STR2## (wherein R.sub.2 represents a hydrogen atom, a halogen, atom, a nitro group, etc.), ##STR3## (wherein R.sub.3 represents a hydrogen atom, a hydroxyl group or a lower alkoxy group), X.sub.2 represents --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, etc. and D represents a carboxy group, a lower alkoxycarbonyl group or ##STR4## which are useful as drugs, particularly SRS-A (slow reacting substance of anaphylaxis) antagonist, i.e. they are useful as prophylaxis and treatment for various allergic diseases (e.g. bronchial asthma, allergic rhinitis, urticaria) or, ischemic heart diseases, inflammation, etc. induced by SRS-A.
    Type: Grant
    Filed: September 27, 1989
    Date of Patent: May 26, 1992
    Inventors: Toshiyasu Mase, Kiyoshi Murase, Hiromu Hara, Kenichi Tomioka
  • Patent number: 5102897
    Abstract: The novel 3,5-ditertiarybutyl-4-hydroxyphenylthio-1,3,4-thiadiazoles and oxadiazoles and 3,5-ditertiarybutyl-4-hydroxyphenylmethanone-1,3,4-thiadiazoles and oxadiazoles and related compounds of the present invention are antiinflammatory agents having activity as inhibitors of 5-lipoxygenase, cyclooxygenase or both.
    Type: Grant
    Filed: January 24, 1991
    Date of Patent: April 7, 1992
    Assignee: Warner-Lambert Company
    Inventors: Diane H. Boschelli, David T. Connor, Catherine R. Kostlan, James B. Kramer, Michael D. Mullican, Jagadish C. Sircar
  • Patent number: 5103007
    Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.
    Type: Grant
    Filed: October 27, 1989
    Date of Patent: April 7, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
  • Patent number: 5082938
    Abstract: Enhanced branched chain hydroxyl compounds are provided of formulaY--(Z).sub.1-6wherein Y is the residue of a nucleophile devoid of conjugated divalent linking moieties, and each Z is a poly(oxyalkylene) moiety having a molecular weight of from about 200-10,000 and containing at least one glycidol residue, wherein at least one of the primary oxy sites of said glycidol residue is linked preferably directly to a first epoxide residue of three or more carbons, and wherein said first epoxide residue is linked through a secondary oxy site preferably directly to a second epoxide reside having a primary terminal hydroxyl.
    Type: Grant
    Filed: March 1, 1990
    Date of Patent: January 21, 1992
    Assignee: Milliken Research Corporation
    Inventors: Edward W. Kluger, David J. Moody
  • Patent number: 5081245
    Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.
    Type: Grant
    Filed: August 18, 1989
    Date of Patent: January 14, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
  • Patent number: 5062863
    Abstract: A diesel fuel composition comprising a major portion of middle distillates and a minor wear improving amount of a 1,3,4-thiadiazole derived from 2,5-dimercapto-1,3,4-thiadiazole and one or two moles of polyolefin having 50 to 400 carbon atoms. Furthermore, the 5-position of the 2-mercapto-1,3,4-thiadiazole may be substituted by alkylthio, 2-hydroxyalkylthio, amino or hydroxy group. The 1,3,4-thiadiazole compounds are also effective dispersants when incorporated into fuel compositions.
    Type: Grant
    Filed: May 17, 1990
    Date of Patent: November 5, 1991
    Assignee: R. T. Vanderbilt Company, Inc.
    Inventor: Thomas J. Karol
  • Patent number: 5055480
    Abstract: This invention relates to compounds of the following formula useful as a carbonic anhydrase inhibitor:A compound of the formula: ##STR1## and pharmaceutically acceptable salts thereof wherein X is NR.sub.12 ;R.sub.1 is ##STR2## R.sub.2 is ##STR3## R.sub.3 is hydrogen or lower alkyl; R is hydrogen or lower alkyl;each R.sub.4 and R.sub.5 are independently hydrogen or lower alkyl;each R.sub.7 and R.sub.8 are independently hydrogen or lower alkyl;R.sub.6 is OR.sub.10 or NR.sub.10 R.sub.11 ;R.sub.9 is OR.sub.13 OR NR.sub.11 R.sub.13 ;R.sub.10, R.sub.11 R.sub.12, and R.sub.13 are independently hydrogen or lower alkyl; andn and m are independently 0-6.
    Type: Grant
    Filed: March 19, 1990
    Date of Patent: October 8, 1991
    Assignee: Research Corporation Technologies, Inc.
    Inventor: William M. Pierce, Jr.
  • Patent number: 4994512
    Abstract: Disclosed are poly-methine compounds having the formula: ##STR1## wherein R.sup.1 is an unsubstituted or substituted alkoxycarbonyl, cycloalkoxycarbonyl or aryloxycarbonyl radical; an unsubstituted or substituted carbamoyl radical; or an unsubstituted or substituted alkylsulfonyl, cycloalkylsulfonyl or arylsulfonyl radical, or an unsubstituted or substituted aryl radical;R.sup.2 is an unsubstituted or substituted alkyl, cycloalkyl or aryl radical;R.sup.3 is hydrogen, alkyl, --OR.sup.2 or halogen; andL is an organic linking group bonded by non-oxo carbon atoms to the oxygen atoms adjacent to L. Also disclosed are admixtures of about 100 to 10,000 ppm of at least one of the poly-methine compounds and certain condensation polymers. The resulting polymer compositions are useful to protect substrates or materials susceptible to degradation by ultraviolet light.
    Type: Grant
    Filed: May 1, 1989
    Date of Patent: February 19, 1991
    Assignee: Eastman Kodak Company
    Inventors: Max A. Weaver, Clarence A. Coates, Wayne P. Pruett, Samuel D. Hilbert
  • Patent number: 4927822
    Abstract: There are described compounds of formula I, ##STR1## in which Y is S, O or NR.sub.9,n is 0 or 1,R.sub.9 is hydrogen or alkyl C 1 to 10,R.sub.3 is hydrogen, alkyl C 1 to 10, cycloalkyl C3 to 10, CF.sub.3, SR.sub.10, a 5 or 6 membered heterocyclic group containing one or more S, O or N atoms, NR.sub.4 R.sub.5, phenyl or phenylalkyl C7 to 12, the phenyl, phenylalkyl and heterocyclic groups optionally being fused to a further phenyl group, the heterocyclic group and any phenyl group optionally being substituted by alkyl C 1 to 6, halogen, alkoxy C 1 to 6, nitro, nitrile, CF.sub.3, SR.sub.6, NR.sub.7 R.sub.11 or hydroxy,R.sub.6, R.sub.7 and R.sub.11, which may be the same or different, are each hydrogen or alkyl C 1 to 10,R.sub.4 and R.sub.5, which may be the same or different, are each hydrogen, alkyl C 1 to 10 or phenyl,R.sub.10 is alkyl C 1 to 10,X.sub.1 is S or O, andA is a chain comprising from 2-16 atoms, which chain carries an O or S containing substitutent at a position 2-6 atoms away from the group C=X.
    Type: Grant
    Filed: August 27, 1986
    Date of Patent: May 22, 1990
    Assignee: Fisons plc
    Inventors: Roger C. Brown, John Dixon, David H. Robinson
  • Patent number: 4914206
    Abstract: The present invention provides lankacidin derivatives of the formula ##STR1## and procedures for the production thereof. The lankacidin derivatives [1] show excellent antimicrobial activities and thus can be used for prophylaxis and treatment of infectious disease in animals.
    Type: Grant
    Filed: December 15, 1988
    Date of Patent: April 3, 1990
    Assignee: Takeda Chemical Industries, LTD.
    Inventors: Isao Minamida, Naoto Hashimoto
  • Patent number: 4889553
    Abstract: Herbicidal triazole sulphonamides of the formula: ##STR1## and salts thereof, where: R.sup.1 represents hydrogen or a substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, acyl, alkoxycarbonyl, aminocarbonyl, sulphonyl or heterocyclic group;R.sup.2 represents hydrogen, halo, cyano, hydroxy, mercapto, a substituted or unsubstituted alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, acyl, alkoxycarbonyl, aminocarbonyl, aryl or amino group, or a heterocyclic group;R.sup.3 represents a substituted or unsubstituted heterocyclic, benzheterocyclic, aryl or aralkyl group; andR.sup.4 represents hydrogen, a substituted or unsubstituted alkyl, alkenyl, alkynyl, acyl, aroyl, alkylsulphonyl, alkoxycarbonyl, aminocarbonyl, aralkyl, or a group of the formula: ##STR2## where R.sup.1 and R.sup.2 are as defined hereinbefore, processes for their preparation and compositions containing them.
    Type: Grant
    Filed: May 15, 1987
    Date of Patent: December 26, 1989
    Assignee: Schering Agrochemicals
    Inventors: Graham P. Rowson, John C. Head, Jurgen Westermann, Martin Kruger, Friedrich Arndt, Richard Rees
  • Patent number: 4861882
    Abstract: Ethynyl terminated imidothioethers (ETIs) are prepared by the reaction of a dimercaptan, such as 4,4'-dimercaptodiphenyl ether, and an ethynyl containing maleimide, such as N-(3-ethynylphenyl)maleimide. Blends of thse ETIs and ethynyl terminated polymeric materials, such as ethynyl terminated sulfones and ethynyl terminated arylene ethers, are also prepared. These resin blends exhibit excellent processability, and the cured blends show excellent fracture toughness and solvent resistance, as well as excellent adhesive and composite properties.
    Type: Grant
    Filed: July 14, 1988
    Date of Patent: August 29, 1989
    Assignee: The United States of America as represented by the Administrator of the National Aeronautics and Space Administration
    Inventors: Paul M. Hergenrother, John W. Connell, R. Gerald Bass
  • Patent number: 4855310
    Abstract: Novel heterocyclic compounds shown by the general formula ##STR1## or the pharmaceutically acceptable salts thereof useful as medicament in particular as antagonist of slow reacting substance of anaphylaxis (SRS-A).
    Type: Grant
    Filed: March 25, 1988
    Date of Patent: August 8, 1989
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Murase, Toshiyasu Mase, Hiromu Hara, Kenichi Tomioka
  • Patent number: 4846984
    Abstract: Disclosed herein is the reaction product of 5-amino-2-mercapto-1,3,4-thiadiazole with hydrocarbyl epoxides. The resulting reaction product finds use as an additive in lubricating oil compositions.
    Type: Grant
    Filed: May 2, 1988
    Date of Patent: July 11, 1989
    Assignee: Mobil Oil Corporation
    Inventors: Angeline B. Cardis, Robert H. Davis, Alfred B. Piotrowski