Chalcogen Or Additional Nitrogen Attached Directly To Ring Carbon Of The Thiadiazole Ring By Nonionic Bonding Patents (Class 548/141)
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Publication number: 20130289057Abstract: 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: ApplicationFiled: January 12, 2012Publication date: October 31, 2013Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZINInventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
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Patent number: 8524894Abstract: 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: GrantFiled: June 4, 2010Date of Patent: September 3, 2013Assignee: Laboratorios Salvat, S.A.Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleo Mas
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Publication number: 20130184258Abstract: 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: ApplicationFiled: October 26, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Patent number: 8455457Abstract: 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: GrantFiled: March 18, 2011Date of Patent: June 4, 2013Assignee: Inotek Pharmaceuticals CorporationInventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley
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Patent number: 8440639Abstract: 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: GrantFiled: March 18, 2011Date of Patent: May 14, 2013Assignee: Inotek Pharmaceuticals CorporationInventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley
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Publication number: 20110130397Abstract: 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: ApplicationFiled: September 21, 2007Publication date: June 2, 2011Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
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Patent number: 7348440Abstract: 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: GrantFiled: June 12, 2003Date of Patent: March 25, 2008Assignee: 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
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Publication number: 20030216258Abstract: Condensed heterocyclic compounds of the general formula: 1Type: ApplicationFiled: April 25, 2003Publication date: November 20, 2003Applicant: Sumitomo Chemical Company, LimitedInventors: Minoru Takano, Shinichi Kawamura, Takashi Komori
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Patent number: 6239152Abstract: 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: GrantFiled: January 22, 1999Date of Patent: May 29, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Zhi-Jie Ni, Eric Gordon
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Patent number: 6197770Abstract: 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: GrantFiled: March 1, 2000Date of Patent: March 6, 2001Assignee: The Procter & Gamble Co.Inventors: Michael George Natchus, Roger Gunnard Bookland, Neil Gregory Almstead, Stanislaw Pikul, Biswanath De, Menyan Cheng
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Patent number: 5972978Abstract: 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: GrantFiled: February 19, 1999Date of Patent: October 26, 1999Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
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Patent number: 5952475Abstract: 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: GrantFiled: June 4, 1998Date of Patent: September 14, 1999Assignee: Bayer AktiengesellschaftInventor: Horst Berneth
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Patent number: 5874382Abstract: 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: GrantFiled: January 23, 1998Date of Patent: February 23, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Balreddy Kamireddy, William Mark Murray
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Patent number: 5846906Abstract: 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: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: 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
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Patent number: 5846907Abstract: 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: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: 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
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Patent number: 5830869Abstract: 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: GrantFiled: June 18, 1997Date of Patent: November 3, 1998Inventors: Mark Allen Mitchell, Heinrich Josef Schostarez, Linda Louise Maggiora, Thomas J. Lindberg
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Patent number: 5767041Abstract: 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: GrantFiled: January 7, 1997Date of Patent: June 16, 1998Assignee: Bayer AktiengesellschaftInventors: Otto Schallner, Andreas Lender, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5703065Abstract: 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: GrantFiled: May 7, 1996Date of Patent: December 30, 1997Assignee: Pfizer Inc.Inventor: Harry R. Howard, Jr.
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Patent number: 5580964Abstract: 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: GrantFiled: March 23, 1995Date of Patent: December 3, 1996Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Uwe Claussen, Werner Hartwich, Peter Wild
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Patent number: 5512190Abstract: 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: GrantFiled: August 22, 1994Date of Patent: April 30, 1996Assignee: Texaco Inc.Inventors: Gregory P. Anderson, Julian H. Dancy, Doris Love, Jayne M. Lucas
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Patent number: 5484763Abstract: 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: GrantFiled: February 10, 1995Date of Patent: January 16, 1996Assignee: American Cyanamid CompanyInventor: Peter J. Wepplo
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Patent number: 5462952Abstract: 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: GrantFiled: September 8, 1993Date of Patent: October 31, 1995Assignee: Warner-Lambert CompanyInventors: Diane H. Boschelli, David T. Connor, Milton L. Hoefle
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Patent number: 5436323Abstract: 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: GrantFiled: July 1, 1993Date of Patent: July 25, 1995Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Werner Hartwich, Karl-Heinrich Lange
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Patent number: 5401743Abstract: 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: GrantFiled: December 13, 1993Date of Patent: March 28, 1995Assignee: BASF AktiengesellschaftInventors: Beatrice Rendenbach-Mueller, Hans-Juergen Teschendorf, Liliane Unger
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Patent number: 5401853Abstract: 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: GrantFiled: July 9, 1993Date of Patent: March 28, 1995Assignee: Laboratorio Farmaceutico C.T. S.r.l.Inventors: Mario Brufani, Antonella Loche, Vincenzo Perlini, Donato Pocar
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Patent number: 5328994Abstract: 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: GrantFiled: February 19, 1993Date of Patent: July 12, 1994Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Karin Hassenruck
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Patent number: 5314891Abstract: 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: GrantFiled: September 10, 1992Date of Patent: May 24, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Philip N. Edwards, Keith Oldham, David Waterson
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Patent number: 5294709Abstract: 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: GrantFiled: January 14, 1993Date of Patent: March 15, 1994Assignee: Fuji Photo Film Co., Ltd.Inventors: Toshinao Ukai, Yoshio Inagaki
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Patent number: 5294596Abstract: 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: GrantFiled: July 21, 1993Date of Patent: March 15, 1994Assignee: Bayer AktiengesellschaftInventors: Wilhelm Haas, Kurt Findeisen, Karl-Heinz Linker, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 5242937Abstract: 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: GrantFiled: March 19, 1990Date of Patent: September 7, 1993Assignee: Research Corporation Technologies, Inc.Inventor: William M. Pierce, Jr.
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Patent number: 5223616Abstract: 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: GrantFiled: November 4, 1991Date of Patent: June 29, 1993Assignee: Sumitomo Chemical Company, Ltd.Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
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Patent number: 5217502Abstract: Quaternary ammonium salt derived thiadiazoles provide multifunctional antioxidant/antiwear characteristics to fuels.Type: GrantFiled: June 23, 1992Date of Patent: June 8, 1993Assignee: Mobil Oil CorporationInventors: Shih-Ying Hsu, Andrew G. Horodysky
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Patent number: 5205945Abstract: 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: GrantFiled: October 18, 1991Date of Patent: April 27, 1993Assignee: Mobil Oil CorporationInventors: Angeline B. Cardis, Arjun K. Goyal, Virginia C. Wiszniewski
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Patent number: 5196434Abstract: 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: GrantFiled: September 26, 1991Date of Patent: March 23, 1993Assignee: Adir et CompagnieInventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
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Patent number: 5190963Abstract: 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: GrantFiled: February 3, 1992Date of Patent: March 2, 1993Assignee: BASF AktiengesellschaftInventors: Christoph Nuebling, Hans Theobald, Uwe Kardorff, Wolfgang Krieg, Christoph Kuenast
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Patent number: 5126397Abstract: Quaternary ammonium salt derived thiadiazoles provide multifunctional antioxidant/antiwear characteristics to lubricants when incorporated therein.Type: GrantFiled: March 13, 1991Date of Patent: June 30, 1992Assignee: Mobil Oil CorporationInventors: Andrew G. Horodysky, Shih-Ying Hsu
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Patent number: 5116853Abstract: 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: GrantFiled: September 27, 1989Date of Patent: May 26, 1992Inventors: Toshiyasu Mase, Kiyoshi Murase, Hiromu Hara, Kenichi Tomioka
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Patent number: 5102897Abstract: 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: GrantFiled: January 24, 1991Date of Patent: April 7, 1992Assignee: Warner-Lambert CompanyInventors: Diane H. Boschelli, David T. Connor, Catherine R. Kostlan, James B. Kramer, Michael D. Mullican, Jagadish C. Sircar
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Patent number: 5103007Abstract: 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: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
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Patent number: 5082938Abstract: 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: GrantFiled: March 1, 1990Date of Patent: January 21, 1992Assignee: Milliken Research CorporationInventors: Edward W. Kluger, David J. Moody
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Patent number: 5081245Abstract: 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: GrantFiled: August 18, 1989Date of Patent: January 14, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
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Patent number: 5062863Abstract: 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: GrantFiled: May 17, 1990Date of Patent: November 5, 1991Assignee: R. T. Vanderbilt Company, Inc.Inventor: Thomas J. Karol
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Patent number: 5055480Abstract: 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: GrantFiled: March 19, 1990Date of Patent: October 8, 1991Assignee: Research Corporation Technologies, Inc.Inventor: William M. Pierce, Jr.
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Patent number: 4994512Abstract: 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: GrantFiled: May 1, 1989Date of Patent: February 19, 1991Assignee: Eastman Kodak CompanyInventors: Max A. Weaver, Clarence A. Coates, Wayne P. Pruett, Samuel D. Hilbert
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Patent number: 4927822Abstract: 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: GrantFiled: August 27, 1986Date of Patent: May 22, 1990Assignee: Fisons plcInventors: Roger C. Brown, John Dixon, David H. Robinson
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Patent number: 4914206Abstract: 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: GrantFiled: December 15, 1988Date of Patent: April 3, 1990Assignee: Takeda Chemical Industries, LTD.Inventors: Isao Minamida, Naoto Hashimoto
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Patent number: 4889553Abstract: 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: GrantFiled: May 15, 1987Date of Patent: December 26, 1989Assignee: Schering AgrochemicalsInventors: Graham P. Rowson, John C. Head, Jurgen Westermann, Martin Kruger, Friedrich Arndt, Richard Rees
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Patent number: 4861882Abstract: 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: GrantFiled: July 14, 1988Date of Patent: August 29, 1989Assignee: The United States of America as represented by the Administrator of the National Aeronautics and Space AdministrationInventors: Paul M. Hergenrother, John W. Connell, R. Gerald Bass
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Patent number: 4855310Abstract: 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: GrantFiled: March 25, 1988Date of Patent: August 8, 1989Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kiyoshi Murase, Toshiyasu Mase, Hiromu Hara, Kenichi Tomioka
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Lubricant additives derived from aminomercaptothiadiazole and lubricant compositions containing same
Patent number: 4846984Abstract: 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: GrantFiled: May 2, 1988Date of Patent: July 11, 1989Assignee: Mobil Oil CorporationInventors: Angeline B. Cardis, Robert H. Davis, Alfred B. Piotrowski