Abstract: Provided are a pyridine derivative represented by the formula (1): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently represent a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.1-4 haloalkyl group, a C.sub.1-4 alkoxy group, a cyano group, a nitro group or a halogen atom,Qa represents a phenyl, pyrazolyl or pyridyl which may be substituted, Qb represents an azole, and X represents oxygen, sulfur or N-R.sup.4,R.sup.4 represents hydrogen or an alkyl group, and an agricultural chemical containing the same, particularly a herbicide.
Abstract: In accordance with the present invention, there are provided combinational therapeutic methods for the in vivo inactivation or inhibition of formation (either directly or indirectly) of species which induce the expression of nitric oxide synthase, as well as reducing nitric oxide levels produced as a result of .NO synthase expression. In contrast to the inhibitory approach described in the prior art (i.e., wherein the function of the enzymes responsible for nitric oxide production is inhibited), the present invention employs a combination of inactivation (or inhibition) and scavenging approach whereby the stimulus of nitric oxide synthase expression is inactivated, or the production thereof is inhibited, and overproduced nitric oxide is bound in vivo to a suitable nitric oxide scavenger. The resulting complexes render the stimulus of nitric oxide synthase expression inactive (or inhibit the production thereof), and nitric oxide harmless.
Abstract: N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R"' and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion. They are manufactured by cleaving off protecting groups in corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.
Type:
Grant
Filed:
May 25, 1995
Date of Patent:
May 5, 1998
Assignee:
Hoffman-La Roche Inc.
Inventors:
Leo Alig, Paul Hadvary, Marianne Hurzeler, Marcel Muller, Beat Steiner, Thomas Weller
Abstract: A process for preparing a composition suitable for topical application to human skin is disclosed. The process comprises mixing particles of metallic oxide dispersed in oil and having a primary particle size less than 0.2 micrometer with one or more emulsifiers, an aqueous phase and a hydrophilic organic sunscreen so as to prepare an emulsion. The composition contains up to 10 percent by weight metallic oxide and up to 7 percent by weight hydrophilic organic sunscreen. The emulsions are useful as sunscreen compositions, skin protectants, moisturisers, and after-sun lotions. The measured Sun Protection Factor for a composition of the invention is considerably higher than would be expected from a knowledge of the individual UV absorbing characteristics of the metallic oxide and the hydrophilic organic sunscreen.
Abstract: The use of sulfuric monoesters of the formulae (I) and (II)R.sup.1 --O--(CH.sub.2 O).sub.n --SO.sub.3 .sup.- M.sup.+ (I)R.sup.1 --CO--NR.sup.2 --(CH.sub.2 O)(.sub.n+1)--SO.sub.3 .sup.- M.sup.+ (II)in whichR.sup.1 is a straight-chain or branched alkyl group of 10 to 24 carbon atoms,R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.6 -alkyl group,M.sup.+ is a hydrogen ion, an alkali metal ion, 1/2 an alkaline earth metal ion, or an ammonium ion of the formula N.sup.+ R.sup.3 R.sup.4 R.sup.5 R.sup.6, where the substituents R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently of one another are each hydrogen atoms or C.sub.1 -C.sub.6 -alkyl groups, which alkyl groups can be substituted by 1 to 3 hydroxyl groups, andn is a number from 0 to 4; or of a mixture of at least two sulfuric monoesters of the formulae (I) and/or (II),for preparing surface-treated pigments from the classes of the quinacridones and dioxazines.
Abstract: A method for treating a depressive disorder which comprises administering to a patient in need thereof a therapeutically effective amount of a combination of(i) hydroxyzine, an individual optical isomer thereof, or a pharmaceutically acceptable salt thereof, and(ii) at least one therapeutic substance which is a serotonin uptake inhibitor, an individual optical isomer thereof or a pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to compositions and methods for treating equines, such as horses, afflicted with equine protozoal myeloencephalitis or EPM. The therapeutic compositions comprise a combination of pyrimethamine and a sulfonamide, preferably, sulfadiazine, in the absence of known therapeutic amounts of trimethoprim.
Type:
Grant
Filed:
July 17, 1996
Date of Patent:
May 5, 1998
Assignee:
Mortar & Pestle Veterinary Pharmacy, Inc.
Abstract: Novel pharmaceutically/cosmetically-active dibenzofuran compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (II) to (VI): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
Type:
Grant
Filed:
October 30, 1995
Date of Patent:
May 5, 1998
Assignee:
Centre International de Recherches Dermatologiques Galderma
Abstract: Titanovanadosilicalites have been found to be very selective, active catalysts in the epoxidation of olefins by peroxides. Dilute hydrogen peroxide suffices to afford high yields of the epoxide. Vanadium incorporation at levels of Si:V in the range 100-2500 effectively changes the characteristics of the titanosilicalite into which it is incorporated to give near quantitative conversion of propylene at selectivities greater than 90%.
Type:
Grant
Filed:
March 17, 1997
Date of Patent:
April 28, 1998
Assignee:
UOP LLC
Inventors:
Laszlo T. Nemeth, Gregory J. Lewis, Richard R. Rosin
Abstract: The present invention relates to methods of preventing or treating an infection or disease caused by an infectious agent. The present invention also relates to the augmentation of the efficacy of existing anti-infective agents by the co-administration of the compounds described herein.
Type:
Grant
Filed:
January 5, 1996
Date of Patent:
April 28, 1998
Inventors:
Clifford S. Mintz, Natan A. Kogan, Ramesh Kakarla, Helena R. Axelrod, Michael J. Sofia
Abstract: Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.
Type:
Grant
Filed:
January 8, 1997
Date of Patent:
April 28, 1998
Assignee:
Schering Corporation
Inventors:
Brian A. McKittrick, Sundeep Dugar, Duane A. Burnett
Abstract: The present invention is directed to methods for manufacturing 3-(aminomethyl)-6-chloropyridines represented by a general formula ?II!; ##STR1## wherein R.sup.2 represents hydrogen or a lower alkyl and R.sup.3 represents hydrogen, a lower alkyl or an halogen atom, characterized in that the compound represented by the general formula ?II! is manufactured by allowing 3-(substituted-aminomethyl)pyridine 1-oxide represented by a general formula ?I!; ##STR2## wherein R.sup.1 represents alkyl, aryl, aralkyl or alkoxy, R.sup.2 and R.sup.3 are as described above, to react with a base represented by a general formula ?a!;R'R"R'"N ?a!wherein R', R" and R'" may be the same or different one another and represent each independently a lower alkyl or an aromatic group, or R', R" , R'" and N may form together an optionally-substituted pyridine ring, in the presence of an electrophilic reagent having at least one chlorine atom, and subsequently treating the reaction product with hydrogen chloride and water.
Abstract: Dibenzyl ether can be readily cleaved to form primarily benzaldehyde and toluene as products, along with minor amounts of bibenzyl and benzyl benzoate, in the presence of a catalyst system comprising a Group 6 metal, preferably molybdenum, a salt, and an organic halide. Although useful synthetically for the cleavage of benzyl ethers, this cleavage also represents a key model reaction for the liquefaction of coal; thus this catalyst system and process should be useful in coal liquefaction with the advantage of operating at significantly lower temperatures and pressures.
Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and have the following structure: ##STR1## for example: ##STR2##
Type:
Grant
Filed:
March 31, 1997
Date of Patent:
April 28, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Philip E. Sanderson, Adel M. Naylor-Olsen, Dona L. Dyer, Joseph P. Vacca, Richard C. A. Isaacs, Bruce D. Dorsey, Mark E. Fraley
Abstract: 3R*4S*3-?4-(4-fluorophenyl)-4-hydroxy-piperidin-1-yl!-chroman-4,7-diol, its enantiomers and pharmaceutically acceptable salts are effective oral agents for treating diseases and conditions susceptible to treatment by NMDA blocking drugs.
Abstract: A process for separating and recovering para-ethylphenol from methyl-ethylphenol and other alkyl phenols is described using an X zeolite adsorbent having ion exchangeable sites exchanged with barium ions, potassium ions or a mixture of barium and potassium ions. Selective adsorption of para-ethylphenol occurs possibly for recovery of the para-ethylphenol.
Abstract: Cyclic ethers are polymerized or copolymerized in homogeneous liquid phase using very low concentrations of heteropolyacid catalyst to produce essentially linear polyoxyalkylene polymers. The product of the polymerization contains less than 2 weight percent cyclic oligomer by-product and has a molecular weight distribution (M.sub.w /M.sub.n) between 1 and 2. Alcohols, acyl-containing compounds and alkalies can be used as end-caping groups to terminate polymerization or modify the properties of the polymer produced. The process produces novel polyoxyalkylene copolymers and block copolymers that are useful as lubricants. The copolymers have a high viscosity index and are compatible with mineral oil and synthetic hydrocarbon lubricants. Preferred comonomers are tetrahydrofuran, C.sub.2 -C.sub.20 monoepoxides and oxetan.
Abstract: A process for the preparation of organic pentafluorosulphur compounds which comprises reacting an organic disulphide in a substantially inert solvent with elemental fluorine.
Type:
Grant
Filed:
March 28, 1997
Date of Patent:
April 21, 1998
Assignee:
British Nuclear Fuels plc
Inventors:
Roy D. Bowden, Martin P. Greenhall, John S. Moilliet, Julie Thomson
Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
Type:
Grant
Filed:
June 21, 1996
Date of Patent:
April 21, 1998
Assignee:
ALLERGAN
Inventors:
Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6 ', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.
Type:
Grant
Filed:
November 8, 1995
Date of Patent:
April 21, 1998
Assignee:
Bristol-Myers Squibb Company
Inventors:
Spencer D. Kimball, Jagabandhu Das, Wan Fang Lau, Steven E. Hall, Wen-Ching Han