Benzene Ring Bonded Directly To The Diazole Ring By Nonionic Bonding Patents (Class 514/391)
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Patent number: 6380200Abstract: This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug and selective serotonin reuptake inhibitor (SSRI), a prodrug thereof or a pharmaceutically acceptable salt of said SSRI or said prodrug. This invention further relates to methods of using those pharmaceutical compositions for the treatment of diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, myocardial infarction, cataracts and diabetic cardiomyopathy.Type: GrantFiled: December 1, 2000Date of Patent: April 30, 2002Assignee: Pfizer, Inc.Inventor: Banavara L. Mylari
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Patent number: 6365608Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2 I in which A is an aryl group or an aromatic or non-aromatic, 5- or 6-membered heterocycle which has from 1 to 3 hetero atoms selected from O, N and S; where the aryl group or the heterocycle may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, halogen, CHF2, CF3, alkoxy, haloalkoxy, alkylthio, alkylsulfynyl and alkylsulfonyl; R1 is a hydrogen atom; R2 is a phenyl or cycloalkyl group which may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxy, phenyl and halogen, where the aliphatic and cycloaliphatic radicals may be partially or fully halogenated and/or the cycloaliphatic radicals may be substituted by from 1 to 3 alkyl groups and where the phenyl group may have from 1Type: GrantFiled: June 19, 2000Date of Patent: April 2, 2002Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6355623Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.Type: GrantFiled: April 8, 1999Date of Patent: March 12, 2002Assignee: Hopital-Sainte-JustineInventors: Ernest G. Seidman, Yves Théorêt
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Publication number: 20010047020Abstract: Benzimidazole derivatives of the formula (I): 1Type: ApplicationFiled: March 27, 2001Publication date: November 29, 2001Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Patent number: 6319949Abstract: A method for preventing fungal diseases in crops which comprises the steps of: (a) applying to a crop an aqueous or a non-aqueous spray composition which includes a pesticide and a spray adjuvant including a solvent and an emulsifier, wherein the solvent is a mixture of aliphatic hydrocarbons having a distillation range of about 520 to 600° F. and an aromatic content of about 1% or less, or the solvent is a single or combination of C6-C18 fatty alcohol(s); and (b) applying chlorothalonil to the crop previously to, simultaneously with, or subsequently to the application of the aqueous spray composition, wherein phytotoxicity associated with the application of chlorothalonil is reduced or eliminated.Type: GrantFiled: November 4, 1996Date of Patent: November 20, 2001Assignee: Syngenta LimitedInventors: Jeffrey R. Schussler, Robert E. Moser, Kevin E. Crosby, John R. Washington
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Publication number: 20010039276Abstract: Novel phenylethyl-thiourea (PHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.Type: ApplicationFiled: December 20, 2000Publication date: November 8, 2001Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Taracad K. Ventatachalam
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Patent number: 6313102Abstract: The present invention encompasses methods of increasing stability of biological substances during drying and the dried compositions derived therefrom. The compositions have improved storage stability.Type: GrantFiled: September 3, 1999Date of Patent: November 6, 2001Assignee: Quardrant Holdings Cambridge, Ltd.Inventors: Camilo Colaco, Bruce J. Roser, Shevanti Sen
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Patent number: 6294562Abstract: The present invention relates to ethyl 3-(2-(4-(4-(amino-imino-methyl)-phenyl)-4-methyl-2,5-dioxoimidazolidin-1-yl)acetylamino)-3-phenylpropionate salts of the formula I, in which HM is maleic acid, and to their physiologically tolerated salts, thereof, to processes for their preparation and to their use in pharmaceuticals.Type: GrantFiled: April 29, 1999Date of Patent: September 25, 2001Assignee: Hoechst AktiengesellschaftInventors: Hans Ulrich Stilz, Gerhard Beck, Manfred Radau
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Patent number: 6284784Abstract: Compounds of formula I: wherein R1 and R2 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are PKC activators and are useful for treating diseases, such as, for example, cancer. Also disclosed are pharmaceutical compositions comprising compounds of formula I, processes for preparing compounds of formula I, and intermediates useful for preparing compounds of formula I.Type: GrantFiled: June 23, 1999Date of Patent: September 4, 2001Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Shaomeng Wang, Lixin Qiao
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Publication number: 20010006970Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.Type: ApplicationFiled: April 8, 1999Publication date: July 5, 2001Applicant: HOPITAL SAINTE-JUSTINEInventors: ERNEST G. SEIDMAN, YVES THEORET
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Patent number: 6255331Abstract: Disclosed are biocidal compositions comprising mixtures of formaldehyde-releasing imidazolidines, such as 1,3-dimethylol-5,3-dimethylhydantoin, and 3-isothiazolones stabilized with low levels of copper salts.Type: GrantFiled: August 16, 2000Date of Patent: July 3, 2001Assignee: Rohm and Haas CompanyInventors: Beverly Jean El A'mma, Susan Lynn Nagahashi
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Patent number: 6232301Abstract: In order to provide an agent for treatment of bladder troubles that has vesical mucosa epithelium dilatation promoting action and/or vesical mucosa healing action, and exhibits excellent curative effect for bladder troubles, in particular, non-bacterial intractable bladder troubles, the agent for treatment of bladder troubles is formulated with hyaluronic acid and/or a pharmaceutically acceptable salt thereof, preferably hyaluronic acid and/or a pharmaceutically acceptable salt thereof having the following physicochemical properties: (A) endotoxin content; 0.03 EU (endotoxin unit)/10 mg or less, (B) sulfur content; 0.01% or less as determined by coulometric titration, (C) iron content; 20 ppm or less, (D) protein content; 0.1% or less, and (E) weight average molecular weight; 500,000 or more, in an amount effective for promoting vesical mucosa epithelium dilatation and/or healing vesical mucosa, preferably in an amount of 0.2-0.6% by weight based on total amount of the agent.Type: GrantFiled: August 27, 1998Date of Patent: May 15, 2001Assignee: Seikagaku CorporationInventors: Katsuya Takahashi, Satoshi Miyauchi
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Patent number: 6191282Abstract: 5-Membered ring heterocycle of the formula I, in which D includes a COOR15, CON(CH3)R15 or CONHR15 radical and R15 includes a 6-24 member bicyclic or tricyclic radical, compositions, preparation and use as inhibitors of thrombocyte aggregation, metastasization of carcinoma cells, binding of osteoclasts to bone surfaces and for the treatment of tromboses.Type: GrantFiled: July 28, 1999Date of Patent: February 20, 2001Assignee: Hoechst Marion RousselInventors: Gerhard Zoller, Otmar Klingler, Bernd Jablonka, Melitta Just, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig, Hans-Ulrich Stilz
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Patent number: 6136816Abstract: This invention relates to fungicidal active ingredient mixtures comprising at least two active ingredient components together with a suitable carrier material, wherein component I is cyprodinil [=2-anilino-4-cyclopropyl-6-methyl-pyrimidine] and wherein component II is A) myclobutanil [=2-p-chlorophenyl-2-(1H-1,2,4-triazol-1-ylmethyl)hexanenitrile]; or B) iprodione [=3-(3,5-dichlorophenyl)-N-isopropyl-2,4-dioxoimidazolidine-1-carboxamide] , and to methods of using such mixtures in crop protection, especially in the control and prevention of disease infestation.Type: GrantFiled: October 9, 1998Date of Patent: October 24, 2000Assignee: Novartis Crop Protection, Inc.Inventors: Gertrude Knauf-Beiter, Hans Steiner
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Patent number: 6121303Abstract: A compound of formula I ##STR1## wherein R.sub.1 is nitro, halogeno or cyano group and R.sub.2 is a group selected from ##STR2## wherein Y and Z are independently oxygen, sulfur or NR, wherein R is hydrogen, straight or branched C.sub.1-8 alkyl, C.sub.5-7 cycloalkyl, phenylC.sub.1-8 alkyl or phenyl group and X.sub.1 and X.sub.2 are NR, where R is hydrogen, straight or branched C.sub.1-8 alkyl, C.sub.5-7 cycloalkyl, phenylC.sub.1-8 alkyl or phenyl group, or a pharmaceutically acceptable salt or ester thereof. Pharmaceutical compositions are also disclosed.Type: GrantFiled: February 23, 1999Date of Patent: September 19, 2000Assignee: Orion-yhtyma OyInventors: Reijo Backstrom, Erkki Honkanen, Inge-Britt Linden, Erkki Nissinen, Aino Pippuri, Pentti Pohto, Tapio Korkolainen
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Patent number: 6114366Abstract: The present invention relates to compositions containing a preservative system containing a two biocidal components, a first component comprising a formaldehyde donor compound, and the second component comprising one or more isothiazolone compounds, where the weight ratio of the first component to the second component ranges from about 1:1 to about 10,000:1.Type: GrantFiled: July 2, 1999Date of Patent: September 5, 2000Assignee: Lonza Inc.Inventors: Patrick J. Lutz, John Gerald Maroski
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Patent number: 6103768Abstract: The invention described here concerns the unique utility of fatty acids and their derivatives to eradicate existing fungal and bacterial infections in plants. Also, described herein are combination treatments whereby fatty acids are used to enhance or augment the activity of fungicides, bactericides, and biological control agents.Type: GrantFiled: September 8, 1997Date of Patent: August 15, 2000Assignee: Mycogen CorporationInventors: Steven D. Savage, Steven L. Evans, Robert A. Haygood, Paul S. Zorner, Keith Jones
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Patent number: 6100252Type: GrantFiled: December 8, 1998Date of Patent: August 8, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Yoshiyuki Inada
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Patent number: 6090835Abstract: Fungicidal mixtures, comprisinga.1) a phenyl-benzylether of the formula I.a, I.b or I.c, ##STR1## or a.1) a carbamate of the formula I.d, ##STR2## where X is CH and N, n is 0, 1 or 2 and R is halogen, C.sub.1 -C.sub.4 -alkyl and C.sub.1 -C.sub.4 -haloalkyl, it being possible for the radicals R to be different when n is 2, andb) a dicarboximide-type fungicide (II)in a synergistically active amount.Type: GrantFiled: September 14, 1998Date of Patent: July 18, 2000Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Hubert Sauter, Manfred Hampel, Joachim Leyendecker, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Peter Irwin, Randall Evan Gold
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Patent number: 6057331Abstract: A synergistic fungicidal composition comprising a compound A having the formula ##STR1## and a compound B which is a dicarboximide derivative such as iprodione, procymidone or vinchlozolin, and a method for controlling or preventing the development of phytopathogenic fungi employing said composition.Type: GrantFiled: July 2, 1998Date of Patent: May 2, 2000Assignee: Rhone-Poulenc AgrochimieInventor: Patrice Duvert
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Patent number: 5998437Abstract: The present invention provides novel benzimidazole derivatives or salts thereof represented by the general formula, ##STR1## wherein R.sup.1 is a hydrogen atom or a halogen atom; R.sup.2 is a phenyl-lower alkyl group; R.sup.3 is a heterocyclic group selected from the group consisting of an indolyl group, indolinyl group, 1H-indazolyl group, 2(1H)-quinolinonyl group, 3,4-dihydro-2(1H)-quinolinonyl group and 1,4-benzoxazinyl group; A is a lower alkylene group; n is 0 or 1.The benzimidazole derivatives or salts of the present invention are effective agents for treating various arteriosclerotic diseases.Type: GrantFiled: March 6, 1997Date of Patent: December 7, 1999Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Takao Nishi, Seiji Sato, Takeshi Nagatani, Hirotaka Yukawa, Nobuyuki Koga, Masahiro Saito, Shinji Yoshinaga
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Patent number: 5981492Abstract: The present invention pertains to 5-ring heterocycles of general formula (I), wherein W, Y, Z, B, D, E and R as well as b, c, d, e, f, g, and h are as indicated in the description; to methods for preparing them, and to their use as inhibitors of platelet aggregation, metastasizing of carcinomatous cells and the attachment of osteoclasts to the bone surface.Type: GrantFiled: July 19, 1996Date of Patent: November 9, 1999Assignee: Hoechst AktiengesellschaftInventors: Gerhard Zoller, Otmar Klingler, Bernd Jablonka, Melitta Just, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig, Hans-Ulrich Stilz
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Patent number: 5955448Abstract: The present invention encompasses methods of increasing stability of biological substances during drying and the dried compositions derived therefrom. The compositions have improved storage stability.Type: GrantFiled: August 19, 1994Date of Patent: September 21, 1999Assignee: Quadrant Holdings Cambridge LimitedInventors: Camilo Colaco, Bruce J. Roser, Shevanti Sen
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Patent number: 5948414Abstract: This invention relates to an improved herbal-based decongestant and antihistamine nasal spray which includes known constituents in specific ratios and further includes a saponin. The invention further relates to a method for treating nasal congestion which results in enhanced decongestant action and surprising curative effects.Type: GrantFiled: March 24, 1998Date of Patent: September 7, 1999Assignee: Nouveau Technologies, Inc.Inventor: Jack G. Wiersma
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Patent number: 5866582Abstract: Fungicidal combination comprising a compound A which is iprodione, vinclozoline or procymidone, and a compound B which is cyprodinil, also known as 2-phenylamino-4-cyclopropyl-6-methylpyrimidine, fungicidal compositions comprising same, and method of preventing fungal attacks on crops.Type: GrantFiled: February 19, 1997Date of Patent: February 2, 1999Assignee: Rhone-Poulenc AgrochimieInventor: Patrice Duvert
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Patent number: 5817685Abstract: Anticonvulsive compounds and compositions, of the formula ##STR1## in which X is a C.sub.1-4 -alkyl, trifluoromethyl, or halogen residue, Y is hydrogen or halogen, n is 0 or 1, and m is 0 or a cardinal number from 1 to 4, and its pharmacologically acceptable acid addition salts.Type: GrantFiled: August 21, 1996Date of Patent: October 6, 1998Assignee: Arzneimittelwerk Dresden GmbHInventors: Hans-Joachim Lankau, Manfred Menzer, Angelika Rostock, Klaus Unverferth
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Patent number: 5733915Abstract: A therapeutic method for the treatment of Crohn's disease is provided, comprising administering to a patient in need of said treatment an intravenous dose of azathioprine or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: March 30, 1995Date of Patent: March 31, 1998Assignee: Glaxo Wellcome Inc.Inventor: William J. Sandborn
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Patent number: 5668163Abstract: A novel fungicidal composition comprising a fungicidally effective amount of a combination consisting of the known 2-cyanobenzimidazole of the formula ##STR1## in which A has the meanings given in the description and at least one other known fungicidally active compound selected from the group mentioned in the specification.The novel compositions show a synergistic activity.Type: GrantFiled: September 3, 1996Date of Patent: September 16, 1997Assignee: Bayer AktiengesellschaftInventors: Heinz-Wilhelm Dehne, Winfried Lunkenheimer
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Patent number: 5656651Abstract: Substituted phenylthiohydantoins are provided for use in detecting the presence of tumor cells having androgenic receptors and providing for cytostatic and cytotoxic activity toward such cells. The subject compounds provide for vehicles for specific targeting to the androgenic receptor containing cells of cytostatic and/or cytotoxic agents, heavy or light radioactive or radioopaque atoms, and the like for detection and treatment of cancer cells involving androgenic receptors or blocking androgenic receptors.Type: GrantFiled: June 16, 1995Date of Patent: August 12, 1997Assignee: Biophysica Inc.Inventors: Milos Sovak, Jerome C. Bressi, James Gordon Douglass, III, Brian Campion, Wolfgang Wrasidlo
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Patent number: 5650424Abstract: The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.Type: GrantFiled: August 29, 1995Date of Patent: July 22, 1997Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Wolfgang Eisert
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Patent number: 5646172Abstract: Novel imidazoles of the formula ##STR1## wherein the substituents are as defined in the disclosure and their non-toxic, pharmaceutically acceptable addition salts with acids and bases having antiandrogenic activity.Type: GrantFiled: September 7, 1995Date of Patent: July 8, 1997Assignee: Roussel UclafInventors: Andre Claussner, Francois Goubet, Jean-Georges Teutsch
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Patent number: 5629330Abstract: The present invention relates to a fungicidal composition intended for the protection of the multiplication products of cultivated plants, containing:(a) 2-(4-chlorobenzylidene)-5,5-dimethyl-1-(1H-1,2,4-triazol-1-ylmethyl)-1-cyc lopentanol;(b) one or more fungicides suitable for the protection of the said multiplication products, optionally one or more insecticides,(c), an agriculturally acceptable inert vehicle and an agriculturally acceptable surfactant.The invention also relates to a method for protecting the multiplication products of plants against fungal diseases using these compositions.Type: GrantFiled: December 3, 1993Date of Patent: May 13, 1997Assignee: Rhone Poulenc Secteur AgrochimieInventors: Alfred Greiner, Jean Hutt, Jacques Mugnier, Regis Pepin
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Patent number: 5627201Abstract: A compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of --CN, --NO.sub.2 and halogen, R.sub.2 is --CF.sub.3 or halogen, --A--B-- is selected from the group consisting of ##STR2## X is --O-- or --S--, R.sub.3 is selected from the group consisting of hydrogen, alkyl, alkenyl and alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted with at least one member of the group consisting of --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted with a member of the group consisting of halogen, --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl and alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH.sub.Type: GrantFiled: January 13, 1995Date of Patent: May 6, 1997Assignee: Roussel UclafInventors: Martine Gaillard-Kelly, Francois Goubet, Daniel Philibert, Jean-Georges Teutsch
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Patent number: 5599829Abstract: A method for increasing blood serum HDL cholesterol levels in a mammal in need of increased HDL cholesterol blood serum levels, which comprises administering to said mammal, an effective amount of a compound of formula I: ##STR1## wherein R is phenyl or phenyl optionally substituted with one or more groups selected from halogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, hydroxy, alkanoyloxy, aroyloxy or arylalkanoyloxy; R.sup.3 is alkyl, aryl or arylalkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 28, 1995Date of Patent: February 4, 1997Assignee: American Home Products CorporationInventors: Hassan M. Elokdah, Theodore S. Sulkowski, Donald P. Strike
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Patent number: 5589497Abstract: A compound selected from the group consisting of compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of --CN, --NO.sub.2, halogen, --CF.sub.3, free carboxy, salified carboxy, and carboxy esterified with lower alkyl; -A-B- is selected from the group consisting of ##STR2## wherein X is --O-- or --S--, R.sub.3 is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, aryl, and aralkyl each of up to 12 carbon atoms, all optionally substituted with at least one member of the group consisting of --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --S-aryl of up to 12 carbon atoms optionally substituted with a member of the group consisting of --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl and alkynyloxy, with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, .dbd.NH.sub.Type: GrantFiled: April 8, 1994Date of Patent: December 31, 1996Assignee: Roussel UclafInventors: Andr e Claussner, Fran.cedilla.ois Goubet, Jean-Georges Teutsch
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Patent number: 5565481Abstract: (1) Fungicidal combinations and compositions, comprising a compound A of the formula: ##STR1## wherein the symbol ##STR2## represents ##STR3## and a compound B chosen from bromuconazole, tebuconazole, epoxiconazole, cyproconazole, flusilazole, metconazole, hexaconazole and difenoconazole.(2) Process for treating crops using these combinations/compositions.Type: GrantFiled: January 13, 1995Date of Patent: October 15, 1996Assignee: Rhone-Poulenc AgrochimieInventor: Patrice Duvert
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Patent number: 5455261Abstract: The present invention relates to a process for the control of fungal disease of plants by applying to the leaves of the plants:a) 2-(4-chlorobenzylidene)-5,5-diemthyl-1-(1H-1, 2,4-triazol-1-ylmethyl)-1-cyclopentanol;b) one or more fungicides suitable for protecting against the said fungal diseases and to compositions which may be used in the process.Type: GrantFiled: July 7, 1994Date of Patent: October 3, 1995Assignee: Rhone-Poulenc Secteur AgrochimieInventors: Alfred Greiner, Jean Hutt, Jacques Mugnier, Regis Pepin
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Patent number: 5436260Abstract: Substituted 1-benzylimidazole-5-methylidene hydantoins are disclosed as well as methods of preparing them, pharmaceutical compositions containing them, and methods of using them. Intermediates useful in the preparation of the compounds of the invention are also disclosed and synthetic methods for preparing the novel intermediates. The compounds are useful as antagonists of angiotensin II and thus are useful in the control of hypertension, hyperaldosteronism, congestive heart failure, surgically induced vascular smooth muscle proliferation, and glaucoma.Type: GrantFiled: January 4, 1994Date of Patent: July 25, 1995Assignee: Warner-Lambert CompanyInventors: John C. Hodges, Sylvester Klutchko
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Patent number: 5434176Abstract: A compound selected from the group consisting of compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of --CN, --NO.sub.2, halogen, --CF.sub.3, free carboxy, salified carboxy, and carboxy esterified with lower alkyl; -A-B- is selected from the group consisting of ##STR2## and X, R.sub.3, R.sub.4 and R.sub.5 are defined as in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-androgenic activity.Type: GrantFiled: May 28, 1993Date of Patent: July 18, 1995Assignee: Roussel UclafInventors: Andre Claussner, Francois Goubet, Jean-Georges Teutsch
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Patent number: 5422360Abstract: A novel Maillard reaction inhibitor containing at least one compound represented by formula (1) and the salts thereof; methods for producing the compounds of formula (1) and the salts thereof; a composition for inhibiting the Maillard reaction in living body comprising at least one compound of formula (1) and the salts thereof; and a method for inhibiting the Maillard reaction in living body by administration of a compound of formula (1') or a salt thereof are disclosed.Type: GrantFiled: July 23, 1993Date of Patent: June 6, 1995Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Keisuke Miyajima, Bonpei Yasui, Masaaki Motoyama, Shintaro Ishikawa, Koichi Yasumura
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Patent number: 5411981Abstract: A compound of the formula ##STR1## wherein R.sub.1 is --CN, --NO.sub.2 or halogen, R.sub.2 is --CF.sub.3 or halogen, --A-B-- is of ##STR2## X is --O-- or --S--, R.sub.3 is hydrogen, alkyl, alkenyl or alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted by --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted by halogen, --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl or alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH.sub.Type: GrantFiled: May 18, 1993Date of Patent: May 2, 1995Assignee: Roussel UclafInventors: Martine Gaillard-Kelly, Francois Goubet, Daniel Philibert, Jean-Georges Teutsch
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Patent number: 5397796Abstract: The present invention relates to 2,4-dioxoimidazolidine compounds of the formula I ##STR1## a process for their preparation and their use as inhibitors of platelet aggregation, metastasis of carcinoma cells and osteoclast binding to the bone surfaces.Type: GrantFiled: April 12, 1993Date of Patent: March 14, 1995Assignee: Cassella AGInventors: Gerhard Zoller, Wolfgang Konig, Jochen Knolle, Melitta Just, Bernd Jablonka
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Patent number: 5294616Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 15, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
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Patent number: 5240952Abstract: A fungicidal composition comprising a fungicidally effective amount of (i) a substituted 1-hydroxyethyl-triazole of the formula ##STR1## in which A is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--,or an addition product thereof with an acid or metal salt, and (ii) at least one member selected from the group consisting ofA) wettable sulphur,B) a polyhalogenoalkylthio derivative,C) a guanidine derivative,D) an aromatic carboxylic acid derivative,E) a dithocarbamate,F) a benzimidazole derivative,G) an imidazole or triazole derivative,H) a phosphoric acid ester,I) a tetrahydroquinoline derivative,J) an S,N-heterocyclene compound,K) a urea derivative,L) a sulphonamide derivative,M) a polyhydroxy ether derivative,N) a triazine derivative,O) a copper complex salt,P) an N-formyl derivative,Q) a morpholine derivative,R) a quinoxaline derivative, andS) a dicarboximide derivative.Type: GrantFiled: May 19, 1992Date of Patent: August 31, 1993Assignee: Bayer AktiengesellschaftInventors: Wilhelm Brandes, Gerd Hanssler, Paul Reinecke, Hans Scheinpflug, Graham Holmwood
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Patent number: 5234929Abstract: A method of treating or preventing motion sickness is disclosed which comprises administering an anti-motion sickness effective amount of an anticonvulsant compound such as phenytoin, ethotoin, primidone, ethosuximide or carbamazepine, in combination with a potentiating amount of an antitussive or cough suppressant agent such as dextromethorphan, levopropoxyphene, muscaphene, pholocodeine, or carbetapentene. The antitussive compounds of the present invention act as potentiating agents so as to enable effective treatment or prevention of motion sickness using a reduced amount of the anticonvulsant compound normally used in such treatment. The method of the present invention reduces the potential for various side effects and thus provides a safer and more effective method of treatment for motion sickness than prior art methods.Type: GrantFiled: July 20, 1992Date of Patent: August 10, 1993Inventor: William Chelen
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Patent number: 5225431Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein R, R.sup.1 and R.sup.2 are independently selected from hydrogen and C.sub.1-4 alkyl;R.sup.3 and R.sup.4 are independently selected from hydrogen, C.sub.1-6 alkyl (including cycloalkyl) and aryl (wherein the alkyl or aryl group, which latter includes benzyl, is optionally substituted by one or more atoms or groups independently selected from halogen, C.sub.1-4 alkyl and aryl), provided R.sup.3 benzyl or substituted benzyl when R.sup.4 =H;m is an integer of from 0 to 2;n is an integer of from 0 to 3;(W) is a group of formula (i), (ii), (iii), or (iv) ##STR2## wherein Y is selected from oxygen, methylene and >N--R.sup.5, where R.sup.5 is hydrogen, C.sub.1-4 alkyl, or benzyl, Z and Z' are independently selected from >C.dbd.O, >C.dbd.Type: GrantFiled: February 26, 1991Date of Patent: July 6, 1993Assignee: Burroughs Wellcome Co.Inventors: Alan D. Robertson, Graeme R. Martin, Janet S. Buckingham
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Patent number: 5137905Abstract: Heterocyclic acetylenic amine compounds having the following structural formula ##STR1## having cholinergic agonist or antagonist activity useful in the treatment of mental disorders, extrapyramidal motor disorders, disorders of the parasympathetic nervous system and glaucoma or as analgesics for the treatment of pain. Typical central nervous system disorders for which the subject compounds can be used include cognitive disorders of all ages, including senile dementia, Alzheimer's disease and other related disorders. The compounds are particularly developed to improve mental performance when a mental deficiency is diagnosed.Type: GrantFiled: April 5, 1991Date of Patent: August 11, 1992Assignee: The Upjohn CompanyInventors: Malcolm W. Moon, Richard F. Heier
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Patent number: 5137904Abstract: A series of ethers and thioethers of 5-methanol thiohydantoins, unsubstituted at the number one position heterocyclic nitrogen atom of the thiohydantoin ring, useful in reversing the effects of collagen and ADP-induced platelet aggregation.Type: GrantFiled: May 30, 1989Date of Patent: August 11, 1992Assignee: G. D. Searle & Co.Inventors: John S. Baran, Tom Lindberg, Robert H. Mazur, Alan E. Moorman, Doug Steinman
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Patent number: 5116858Abstract: 4-Imidazoline derivatives represented by the formula (I) and/or formula (II): ##STR1## wherein R.sup.1 represents C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, or optionally substituted aralkyl; R.sup.2 and R.sup.3 independently represent hydrogen, C.sub.3 -C.sub.20 alkyl, C.sub.3 -C.sub.20 alkenyl, C.sub.3 -C.sub.20 alkynyl, C.sub.3 -C.sub.20 alkoxy, C.sub.3 -C.sub.20 alkenyloxy, C.sub.3 -C.sub.20 alkynyloxy, C.sub.3 -C.sub.8 cyloalkyl, C.sub.1 -C.sub.10 alkylthio, or optionally substituted aralkyl or aralkyloxy; R.sup.4 represents C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or optionally substituted aralkyl; provided that R.sup.2 and R.sup.3 cannot be hydrogen at the same time, and pharmaceutically acceptable salts thereof. A pharmaceutical formulation containing the compound is also provided.Type: GrantFiled: April 26, 1990Date of Patent: May 26, 1992Assignee: Mitsubishi Kasei CorporationInventors: Yoshio Hayashi, Yasuhiro Morinaka, Masaki Shinoda, Hiroyoshi Nishi, Kazutoshi Watanabe, Nobuko Fukushima
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Patent number: RE35956Abstract: A compound of the formula ##STR1## wherein R.sub.1 is --CN, --NO.sub.2 or halogen, R.sub.2 is --CF.sub.3 or halogen, --A--B-- is of ##STR2## X is --O-- or --S--, R.sub.3 is hydrogen, alkyl, alkenyl or alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted by --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted by halogen, --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl or alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH.sub.Type: GrantFiled: February 27, 1997Date of Patent: November 10, 1998Assignee: Roussel UclafInventors: Martine Gaillard-Kelly, Francois Goubet, Daniel Phiibert, Jean-Georges Teutsch