Benzene Ring Bonded Directly To The Diazole Ring By Nonionic Bonding Patents (Class 514/391)
  • Patent number: 6380200
    Abstract: 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: Grant
    Filed: December 1, 2000
    Date of Patent: April 30, 2002
    Assignee: Pfizer, Inc.
    Inventor: Banavara L. Mylari
  • Patent number: 6365608
    Abstract: 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 1
    Type: Grant
    Filed: June 19, 2000
    Date of Patent: April 2, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
  • Patent number: 6355623
    Abstract: 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: Grant
    Filed: April 8, 1999
    Date of Patent: March 12, 2002
    Assignee: Hopital-Sainte-Justine
    Inventors: Ernest G. Seidman, Yves Théorêt
  • Publication number: 20010047020
    Abstract: Benzimidazole derivatives of the formula (I): 1
    Type: Application
    Filed: March 27, 2001
    Publication date: November 29, 2001
    Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
  • Patent number: 6319949
    Abstract: 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: Grant
    Filed: November 4, 1996
    Date of Patent: November 20, 2001
    Assignee: Syngenta Limited
    Inventors: Jeffrey R. Schussler, Robert E. Moser, Kevin E. Crosby, John R. Washington
  • Publication number: 20010039276
    Abstract: 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: Application
    Filed: December 20, 2000
    Publication date: November 8, 2001
    Applicant: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Taracad K. Ventatachalam
  • Patent number: 6313102
    Abstract: 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: Grant
    Filed: September 3, 1999
    Date of Patent: November 6, 2001
    Assignee: Quardrant Holdings Cambridge, Ltd.
    Inventors: Camilo Colaco, Bruce J. Roser, Shevanti Sen
  • Patent number: 6294562
    Abstract: 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: Grant
    Filed: April 29, 1999
    Date of Patent: September 25, 2001
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans Ulrich Stilz, Gerhard Beck, Manfred Radau
  • Patent number: 6284784
    Abstract: 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: Grant
    Filed: June 23, 1999
    Date of Patent: September 4, 2001
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Shaomeng Wang, Lixin Qiao
  • Publication number: 20010006970
    Abstract: 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: Application
    Filed: April 8, 1999
    Publication date: July 5, 2001
    Applicant: HOPITAL SAINTE-JUSTINE
    Inventors: ERNEST G. SEIDMAN, YVES THEORET
  • Patent number: 6255331
    Abstract: 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: Grant
    Filed: August 16, 2000
    Date of Patent: July 3, 2001
    Assignee: Rohm and Haas Company
    Inventors: Beverly Jean El A'mma, Susan Lynn Nagahashi
  • Patent number: 6232301
    Abstract: 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: Grant
    Filed: August 27, 1998
    Date of Patent: May 15, 2001
    Assignee: Seikagaku Corporation
    Inventors: Katsuya Takahashi, Satoshi Miyauchi
  • Patent number: 6191282
    Abstract: 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: Grant
    Filed: July 28, 1999
    Date of Patent: February 20, 2001
    Assignee: Hoechst Marion Roussel
    Inventors: Gerhard Zoller, Otmar Klingler, Bernd Jablonka, Melitta Just, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig, Hans-Ulrich Stilz
  • Patent number: 6136816
    Abstract: 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: Grant
    Filed: October 9, 1998
    Date of Patent: October 24, 2000
    Assignee: Novartis Crop Protection, Inc.
    Inventors: Gertrude Knauf-Beiter, Hans Steiner
  • Patent number: 6121303
    Abstract: 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: Grant
    Filed: February 23, 1999
    Date of Patent: September 19, 2000
    Assignee: Orion-yhtyma Oy
    Inventors: Reijo Backstrom, Erkki Honkanen, Inge-Britt Linden, Erkki Nissinen, Aino Pippuri, Pentti Pohto, Tapio Korkolainen
  • Patent number: 6114366
    Abstract: 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: Grant
    Filed: July 2, 1999
    Date of Patent: September 5, 2000
    Assignee: Lonza Inc.
    Inventors: Patrick J. Lutz, John Gerald Maroski
  • Patent number: 6103768
    Abstract: 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: Grant
    Filed: September 8, 1997
    Date of Patent: August 15, 2000
    Assignee: Mycogen Corporation
    Inventors: Steven D. Savage, Steven L. Evans, Robert A. Haygood, Paul S. Zorner, Keith Jones
  • Patent number: 6100252
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: August 8, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takehiko Naka, Yoshiyuki Inada
  • Patent number: 6090835
    Abstract: 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: Grant
    Filed: September 14, 1998
    Date of Patent: July 18, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Schelberger, Maria Scherer, Hubert Sauter, Manfred Hampel, Joachim Leyendecker, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Peter Irwin, Randall Evan Gold
  • Patent number: 6057331
    Abstract: 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: Grant
    Filed: July 2, 1998
    Date of Patent: May 2, 2000
    Assignee: Rhone-Poulenc Agrochimie
    Inventor: Patrice Duvert
  • Patent number: 5998437
    Abstract: 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: Grant
    Filed: March 6, 1997
    Date of Patent: December 7, 1999
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Takao Nishi, Seiji Sato, Takeshi Nagatani, Hirotaka Yukawa, Nobuyuki Koga, Masahiro Saito, Shinji Yoshinaga
  • Patent number: 5981492
    Abstract: 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: Grant
    Filed: July 19, 1996
    Date of Patent: November 9, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Zoller, Otmar Klingler, Bernd Jablonka, Melitta Just, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig, Hans-Ulrich Stilz
  • Patent number: 5955448
    Abstract: 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: Grant
    Filed: August 19, 1994
    Date of Patent: September 21, 1999
    Assignee: Quadrant Holdings Cambridge Limited
    Inventors: Camilo Colaco, Bruce J. Roser, Shevanti Sen
  • Patent number: 5948414
    Abstract: 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: Grant
    Filed: March 24, 1998
    Date of Patent: September 7, 1999
    Assignee: Nouveau Technologies, Inc.
    Inventor: Jack G. Wiersma
  • Patent number: 5866582
    Abstract: 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: Grant
    Filed: February 19, 1997
    Date of Patent: February 2, 1999
    Assignee: Rhone-Poulenc Agrochimie
    Inventor: Patrice Duvert
  • Patent number: 5817685
    Abstract: 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: Grant
    Filed: August 21, 1996
    Date of Patent: October 6, 1998
    Assignee: Arzneimittelwerk Dresden GmbH
    Inventors: Hans-Joachim Lankau, Manfred Menzer, Angelika Rostock, Klaus Unverferth
  • Patent number: 5733915
    Abstract: 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: Grant
    Filed: March 30, 1995
    Date of Patent: March 31, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventor: William J. Sandborn
  • Patent number: 5668163
    Abstract: 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: Grant
    Filed: September 3, 1996
    Date of Patent: September 16, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz-Wilhelm Dehne, Winfried Lunkenheimer
  • Patent number: 5656651
    Abstract: 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: Grant
    Filed: June 16, 1995
    Date of Patent: August 12, 1997
    Assignee: Biophysica Inc.
    Inventors: Milos Sovak, Jerome C. Bressi, James Gordon Douglass, III, Brian Campion, Wolfgang Wrasidlo
  • Patent number: 5650424
    Abstract: 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: Grant
    Filed: August 29, 1995
    Date of Patent: July 22, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Wolfgang Eisert
  • Patent number: 5646172
    Abstract: 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: Grant
    Filed: September 7, 1995
    Date of Patent: July 8, 1997
    Assignee: Roussel Uclaf
    Inventors: Andre Claussner, Francois Goubet, Jean-Georges Teutsch
  • Patent number: 5629330
    Abstract: 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: Grant
    Filed: December 3, 1993
    Date of Patent: May 13, 1997
    Assignee: Rhone Poulenc Secteur Agrochimie
    Inventors: Alfred Greiner, Jean Hutt, Jacques Mugnier, Regis Pepin
  • Patent number: 5627201
    Abstract: 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: Grant
    Filed: January 13, 1995
    Date of Patent: May 6, 1997
    Assignee: Roussel Uclaf
    Inventors: Martine Gaillard-Kelly, Francois Goubet, Daniel Philibert, Jean-Georges Teutsch
  • Patent number: 5599829
    Abstract: 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: Grant
    Filed: November 28, 1995
    Date of Patent: February 4, 1997
    Assignee: American Home Products Corporation
    Inventors: Hassan M. Elokdah, Theodore S. Sulkowski, Donald P. Strike
  • Patent number: 5589497
    Abstract: 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: Grant
    Filed: April 8, 1994
    Date of Patent: December 31, 1996
    Assignee: Roussel Uclaf
    Inventors: Andr e Claussner, Fran.cedilla.ois Goubet, Jean-Georges Teutsch
  • Patent number: 5565481
    Abstract: (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: Grant
    Filed: January 13, 1995
    Date of Patent: October 15, 1996
    Assignee: Rhone-Poulenc Agrochimie
    Inventor: Patrice Duvert
  • Patent number: 5455261
    Abstract: 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: Grant
    Filed: July 7, 1994
    Date of Patent: October 3, 1995
    Assignee: Rhone-Poulenc Secteur Agrochimie
    Inventors: Alfred Greiner, Jean Hutt, Jacques Mugnier, Regis Pepin
  • Patent number: 5436260
    Abstract: 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: Grant
    Filed: January 4, 1994
    Date of Patent: July 25, 1995
    Assignee: Warner-Lambert Company
    Inventors: John C. Hodges, Sylvester Klutchko
  • Patent number: 5434176
    Abstract: 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: Grant
    Filed: May 28, 1993
    Date of Patent: July 18, 1995
    Assignee: Roussel Uclaf
    Inventors: Andre Claussner, Francois Goubet, Jean-Georges Teutsch
  • Patent number: 5422360
    Abstract: 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: Grant
    Filed: July 23, 1993
    Date of Patent: June 6, 1995
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Keisuke Miyajima, Bonpei Yasui, Masaaki Motoyama, Shintaro Ishikawa, Koichi Yasumura
  • Patent number: 5411981
    Abstract: 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: Grant
    Filed: May 18, 1993
    Date of Patent: May 2, 1995
    Assignee: Roussel Uclaf
    Inventors: Martine Gaillard-Kelly, Francois Goubet, Daniel Philibert, Jean-Georges Teutsch
  • Patent number: 5397796
    Abstract: 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: Grant
    Filed: April 12, 1993
    Date of Patent: March 14, 1995
    Assignee: Cassella AG
    Inventors: Gerhard Zoller, Wolfgang Konig, Jochen Knolle, Melitta Just, Bernd Jablonka
  • Patent number: 5294616
    Abstract: 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: Grant
    Filed: March 25, 1992
    Date of Patent: March 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
  • Patent number: 5240952
    Abstract: 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: Grant
    Filed: May 19, 1992
    Date of Patent: August 31, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wilhelm Brandes, Gerd Hanssler, Paul Reinecke, Hans Scheinpflug, Graham Holmwood
  • Patent number: 5234929
    Abstract: 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: Grant
    Filed: July 20, 1992
    Date of Patent: August 10, 1993
    Inventor: William Chelen
  • Patent number: 5225431
    Abstract: 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: Grant
    Filed: February 26, 1991
    Date of Patent: July 6, 1993
    Assignee: Burroughs Wellcome Co.
    Inventors: Alan D. Robertson, Graeme R. Martin, Janet S. Buckingham
  • Patent number: 5137905
    Abstract: 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: Grant
    Filed: April 5, 1991
    Date of Patent: August 11, 1992
    Assignee: The Upjohn Company
    Inventors: Malcolm W. Moon, Richard F. Heier
  • Patent number: 5137904
    Abstract: 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: Grant
    Filed: May 30, 1989
    Date of Patent: August 11, 1992
    Assignee: G. D. Searle & Co.
    Inventors: John S. Baran, Tom Lindberg, Robert H. Mazur, Alan E. Moorman, Doug Steinman
  • Patent number: 5116858
    Abstract: 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: Grant
    Filed: April 26, 1990
    Date of Patent: May 26, 1992
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Yoshio Hayashi, Yasuhiro Morinaka, Masaki Shinoda, Hiroyoshi Nishi, Kazutoshi Watanabe, Nobuko Fukushima
  • Patent number: RE35956
    Abstract: 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: Grant
    Filed: February 27, 1997
    Date of Patent: November 10, 1998
    Assignee: Roussel Uclaf
    Inventors: Martine Gaillard-Kelly, Francois Goubet, Daniel Phiibert, Jean-Georges Teutsch