Abstract: The formation of undesirable sludge in the course of spraying a solution or dispersion of a water-soluble or water-dispersible solid or a structured gel formulation is reduced by the incorporation in the formulation of a low-density solid particulate material having a density of less than one and a diameter of less than the spray nozzle filter through which it will pass. The low-density solid particulate material is preferably a hollow glass or plastic particle having a density of less than 0.8 g/cm3. The invention is particularly applicable to agrochemical formulations.
Abstract: The present invention relates to drug-ligand conjugates wherein the drug is linked to the ligand through a protein peptide linker and a connector, a process for the preparation of the conjugates, method of controlling the growth of undesirable cells, pharmaceutical compositions, and intermediates thereof.
Type:
Grant
Filed:
May 14, 1993
Date of Patent:
April 10, 2001
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Raymond Armand Firestone, Gene Michael Dubowchik
Abstract: 3-Isochromanone is prepared by contacting an o-xylene-&agr;,&agr;′-dihalide with carbon monoxide in a two-phase liquid medium, in which one phase is aqueous and the other phase is water-immiscible, in the presence of a catalyst and a hindered amine base.
Type:
Grant
Filed:
January 24, 2000
Date of Patent:
March 27, 2001
Assignee:
ZENECA Limited
Inventors:
David John Ritchie, Hannah Sallie Robertson McCann, Jennifer Ann White, Kirstin MacCormick, Raymond Vincent Heavon Jones, Robin Fieldhouse
Abstract: An agrochemical composition packaged in a water soluble or water dispersible sachet is taught. The agrochemical composition is comprised of water-soluble, agrochemically active agent, water and an agent to minimize water loss through the walls of the sachet, wherein the is an ester of an alkyl, alkenyl, aryl, or arylalkyl acid; an ester or a naturally occurring oil; or a mineral or a synthetic oil; provided that the agent is not dibutylphtalate.
Type:
Grant
Filed:
June 19, 1998
Date of Patent:
March 20, 2001
Assignee:
Zeneca Limited
Inventors:
Peter Holmes, Richa Shaunak, Rowena Roshanthi Landham, Rupert Heinrich Sohm
Abstract: 3-Isochromanome is prepared by reacting an o-xylene-&agr;,&agr;′-dihalide with carbon monoxide and water in the presence of a metal catalyst such that the pH of the reaction is maintained between about 7 and 11.
Type:
Grant
Filed:
December 8, 1999
Date of Patent:
February 6, 2001
Assignee:
Zeneca Limited
Inventors:
Hannah Sallie Robertson McCann, Raymond Vincent Heavon Jones
Abstract: A fungicidal compound having general formula (I)
or a stereoisomer thereof, wherein A is CH or N, B is OCH3 or NHCH3, R1 is H, chloro or methyl and R2 is H, fluoro, chloro or methyl.
Abstract: A process for preparing agrochemical intermediates of formula (I), wherein W is (CH.sub.3 O).sub.2 CH.CHCO.sub.2 CH.sub.3 or CH.sub.3 O.CH.dbd.CCO.sub.2 CH.sub.3 ; Z.sup.1 is a halogen atom; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen, halogen, C.sub.1-4 alky, C alkoxy, acetoxy or acyl; the process comprising the steps of: (a) reacting a compound of formula (II), wherein X, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, with a compound of formula ROCH.sub.3, wherein R is a metal; and, (b) reacting the product of (a) with a compound of formula (III), wherein Z.sup.1 and Z.sup.2 are halogen atoms. A process for the preparation of compounds of formula (II) and compounds of formula (II) themselves. A process for obtaining, in substantially pure form, a compound of formula (11) and compounds of formula (II) themselves. A process for obtaining, in substantially pure form, a compound of formula (11) wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are all hydrogen.
Type:
Grant
Filed:
February 16, 1999
Date of Patent:
December 19, 2000
Assignee:
Zeneca Limited
Inventors:
Alan John Whitton, Brian Geoffrey Cox, Gareth Andrew De Boos, Ian Gordon Berry, Ian George Fleming, Raymond Vincent Heavon Jones
Abstract: 4,6-Dichloropyrimidine is prepared by treating 4,6-dihydroxypyrimidine with a chlorinating agent of the formula R.sup.1 R.sup.2 R.sup.3 PCl.sub.2 wherein R.sup.1, R.sup.2 and R.sup.3 are independently alkyl or aryl, or one or more of the groups R.sup.1, R.sup.2 and R.sup.3 is linked to a polymer support. Conveniently, the chlorinating agent may be prepared in situ by reacting the corresponding phosphine oxide with phosgene. Thus, in a preferred process, 4,6-dichloropyrimidine is prepared by treating 4,6-dihydroxypyrimidine with phosgene in the presence of a phosphine oxide.
Type:
Grant
Filed:
November 5, 1998
Date of Patent:
December 12, 2000
Assignee:
Zeneca Limited
Inventors:
Alan John Whitton, Ewan Campbell Boyd, Michael Charles Henry Standen, Peter Karl Wehrenberg, Raymond Vincent Heavon Jones, Timothy John Doyle, David Alan Glanville
Abstract: A process for preparing (E)-methyl 2-[2-(6-(-cyanophenoxy)pyrimidin-4-yloxy)phenyl]-3-methoxypropenoate comprising contacting (E)-methyl 2-[2-(6-chloropyrimidin-4-yloxy)phenyl]-3-methoxypropenoate or methyl 2-[2-(6-chloropyrimidin-4-yloxy)phenyl]-3,3-dimethoxypropanoate with 2-cyanophenate anions, the process being conducted in the absence of copper or a copper salt and in the absence of N,N-dimethylformamide. The 2-cyanophenate anions are generated in situ by reacting 2-cyanophenol with an alkali metal carbonate.
Type:
Grant
Filed:
June 10, 1999
Date of Patent:
November 28, 2000
Assignee:
ZENECA Limited
Inventors:
Alan John Whitton, Ian George Fleming, Robert Comgall Ewins, Raymond Vincent Heavon Jones, Samuel McNeish
Abstract: A process for the preparation of 2-hydroxy-6-trifluoromethylpyridine which comprises reacting 2-fluoro-6-trifluomethylpyridine or a mixture of 2-fluoro-6-trifluoromethylpyridine and 2-chloro-6-trifluoromethylpyridine with an alkali metal hydroxide at a temperature of from 50.degree. C. to 160.degree. C. and acidifying the product so formed.
Type:
Grant
Filed:
September 3, 1999
Date of Patent:
November 7, 2000
Assignee:
Zeneca Limited
Inventors:
Alexander Pai-Yung Fung, David Dale Friese, Erwin Michael Seidel, Alan John Whitton, Alastair lain Currie Stewart, Jennifer Ann White, Raymond Vincent Heavon Jones, John Desmond Hunt
Abstract: Processes for stereoselective enzymatic conversion of certain keto carboxylic acid derivatives to form the corresponding alkylamino acid compounds are described. The invention also concerns an engineered yeast host cell containing recombinant nucleic acid capable of expressing a phenylalanine dehydrogenase, as well as an engineered host cell containing recombinant nucleic acid capable of expressing a phenylalanine dehydrogenase enzyme and nucleic acid capable of expressing a formate dehydrogenase enzyme.
Type:
Grant
Filed:
July 8, 1999
Date of Patent:
October 31, 2000
Assignee:
Bristol-Myers Squibb Company
Inventors:
Ronald Hanson, Mary Jo Donovan, Steven Goldberg, Paul A. Jass, Wen-Sen Li, Ramesh Patel, Keith Ramig, Laszlo J. Szarka, John J. Venit
Abstract: A fungicidal compound of formula (I): or a stereoisomer thereof, wherein A is CH or N, B is OCH.sub.3 or NHCH.sub.3, E is --NR.sup.1 --C(CH.sub.3).dbd.N-- or --N.dbd.C(CH.sub.3)--NR.sup.1 --, R.sup.1 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or optionally substitute benzyl, R.sup.2 is H, C.sub.1-4 alkyl, halo(C.sub.1-4)alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl, and R.sup.3 is optionally substituted aryl or optionally substituted heterocyclyl.
Type:
Grant
Filed:
January 6, 1999
Date of Patent:
September 26, 2000
Assignee:
Zeneca Limited
Inventors:
George Tseriotis, Ian Henry Aspinall, Paul Anthony Worthington
Abstract: High expression vectors for expression of heterologous genes in Escherichia coli. The expression vectors contain, the tac promoter, an intergenic region, a restriction site, and, optionally, groES DNA.
Abstract: A D-amino acid oxidase promoter isolated from T. variabilis has been incorporated into S. cerevisiae expression vectors to increase the expression of heterologous genes. The heterologous promoter has been placed upstream of selective markers, auxotrophic nutritional and/or dominant selectable markers. Because the promoter is from another yeast specie, it is weakly recognized by and S. cerevisiae. To compensate for the weak transcripts of selectable marker genes transcribed from the weak heterologous promoter, the plasmid containing the gene of the interest is amplified leading to a higher expression of protein of interest.
Abstract: The invention provides compositions for providing body, fullness and texture to otherwise fine or very fine keratinous fibers, particularly human hair. The compositions of the present invention have a high pH, e.g., about 8 to about 10 when the compositions contain cationic polymer, and a pH of about 8 to about 14, preferably about 8.5 to about 13, and more preferably, about 8.5 to about 10 when the compositions contain no cationic polymer. The compositions include one or more nonionic and/or cationic polymers, which, in combination with the high pH of the composition, lift the hair cuticle and allow the deposition of polymer, thus resulting in increased fullness and texture to the hair. The compositions of the present invention may be in the form of known hair care products such as, for example, shampoos, rinses and conditioners. In addition, the compositions can be formulated, for example, as lotions or creams, and the like, for consumer use.
Abstract: A hair treatment composition comprising a mixture of polyvinylpyrrolidone and a member selected from the group consisting of an ethoxylated triglyceride, a quaternary ammonium chloride, phenyl trimethicone, an acrylate containing polymer and dimethicone copolyol ester and mixtures thereof, provided that the weight ratio of the polyvinylpyrrolidone to the ethoxylated triglyceride is greater than about 7:1 and the weight ratio of the polyvinylpyrrolidone to the acrylate containing polymer is greater than about 7:1 is described herein.
Abstract: The novel primary intermediate, 1-(5-amino-2-hydroxyphenyl)ethane-1,2-diol and a method for producing same, are disclosed. The novel intermediate can be employed as a replacement for p-aminophenol in oxidation dye formulations.
Type:
Grant
Filed:
November 3, 1998
Date of Patent:
November 9, 1999
Assignee:
Bristol-Myers Squibb Company
Inventors:
Mu-III Lim, Linas R. Stasaitis, Yuh-Guo Pan, Michael Y. M. Wong
Abstract: The invention provides a safe and economical nonprescription combination of acetaminophen, aspirin and caffeine (APAP/ASA/CAF) for use in treating migraine pain and the cluster of symptoms characteristic of migraine attack, such as nausea, photophobia, phonophobia and functional disabilities. The use of the APAP/ASA/CAF combination is also effective in aborting the prodrome phase of a migraine attack.
Abstract: Yeast cell having the ability to express the kinase domain of N-Pak. The expressed kinase domain restores the mating function of a ste20 mutant and such cells are therefore useful in an assay to screen for inhibitors of N-Pak. Such inhibitors may be useful in treatment and/or prevention of Alzheimer's Disease.
Abstract: A method of coloring keratinous fibers with, and coloring compositions comprising, a sulfo-containing, water-dispersible polymer having carbonyloxy linking groups, and a colorant reacted into or onto the polymer backbone.
Type:
Grant
Filed:
January 8, 1998
Date of Patent:
September 14, 1999
Assignee:
Bristol-Myers Squibb Company
Inventors:
James J. Krutak, Dante J. Rutstrom, Keith C. Brown, Mario L. Garcia