Abstract: Biphenylylquinuclidine compounds of the formula I: ##STR1## and pharmaceutically-acceptable salts thereof; wherein R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 -CR.sup.2 is a double bond; and one or both ring A and ring B may be optionally unsubstituted or independently substituted by one or more substituents selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkylamino, di-?(1-6C)alkyl!amino, N-?(1-6C)alkyl!carbamoyl, N,N-di-?(1-6C)alkyl!carbamoyl, (1-6C)alkoxycarbonyl, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl and halogeno-(1-6C)alkyl; are inhibitors of squalene synthase and are hence useful in treating diseases or medical conditions such as hypercholesterolemia, atherosclerosis and fungal diseases.
Type:
Grant
Filed:
June 30, 1993
Date of Patent:
August 11, 1998
Assignee:
Zeneca Limited
Inventors:
George Robert Brown, Peter John Harrison, deceased, Keith Blakeney Mallion
Abstract: A process for the monodecarboxylation of a halogenated aromatic dicarboxylic acid or derivative thereof in which the halogenated aromatic dicarboxylic acid or derivative thereof in a liquid medium is heated characterized in that the liquid medium is a polar aprotic liquid medium.
Type:
Grant
Filed:
November 4, 1996
Date of Patent:
August 11, 1998
Assignee:
Zeneca Limited
Inventors:
Stewart Reid Korn, Michael Scott Howarth, Gordon Jamieson
Abstract: Phosgenation of carboxylic acids to the corresponding carboxylic acid chlorides in conducted in the presence of a solvent comprising acetonitrile.
Abstract: The invention relates to tricyclic compounds of formula (I) ##STR1## wherein R.sup.1 is hydrogen, amino, (1-4C)alkyl, (1-4C)alkoxy, hydroxy-(1-4C)alkyl or fluoro-(1-4C)alkyl; R.sup.2 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, hydroxy-(2-4C)alkyl, halogeno-(2-4C)alkyl or cyano-(1-4C)alkyl; Ar is optionally-substituted phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl; and R.sup.3 includes a group of the formula --NHCH(CO.sub.2 H)--A.sup.1 --Y.sup.1 wherein A.sup.1 is (1-6C)alkylene and Y.sup.1 is carboxy, tetrazol-5-yl, N-?(1-4C)alkylsulphonyl!carbamoyl, N(phenylsulphonyl)carbamoyl, tetrazol-5-ylthio, tetrazol-5-ylsulphinyl or tetrazol-5-ylsulphonyl; or pharmaceutically-acceptable salts or esters thereof; to processes for their manufacture; to pharmaceutical compositions containing them; and to their use as anti-cancer agents.
Type:
Grant
Filed:
June 28, 1995
Date of Patent:
August 4, 1998
Assignees:
Zeneca Limited, British Technology Group Ltd.
Inventors:
Francis Thomas Boyle, James William Crook, Zbigniew Stanley Matusiak
Abstract: A dispersant for aqueous mill-bases obtainable by reacting a polyethylene glycol with a molar excess of a hydroxycarboxylic acid containing from 4 to 17 carbon atoms or lactone thereof and/or with a C.sub.3-4 -alkylene oxide to form a polymeric diol and phosphating the diol. The preferred hydroxycarboxylic acid or lactone is .epsilon.-caprolactone.
Abstract: A novel method for monitoring the success or the yield of chemical reactions involving a reactant bound to a solid phase support, or to forecast the success of such reactions, or to quantify the number of deuterium containing groups present in a solid-phase bound sample, using infrared spectroscopy and deuterium-carbon absorbances, along with novel compounds and intermediates useful for carring out the method.
Abstract: This invention relates to substituted N-benzotriazoles of the formula ##STR1## in which: R.sup.1, R.sup.2, R.sup.3,R.sup.4, R.sup.5,R.sup.6, R.sup.7, X are as defined in the specification. The compounds exhibit herbicidal activity.
Abstract: Herbicidal compositions containing substituted pyrazole compounds and derivatives thereof of the formula: ##STR1## wherein Y and O or S is Z is a carbon-carbon single bond, O, S, C.dbd.O or C.dbd.N. Methods of controlling undesirable vegetation using these compounds and derivatives are also disclosed. Herbicidal compounds wherein Z is a carbon-carbon single bond, S, C.dbd.O or C.dbd.N are also described.
Type:
Grant
Filed:
August 4, 1997
Date of Patent:
July 28, 1998
Assignee:
Zeneca Limited
Inventors:
Christopher John Mathews, Don Robert Baker
Abstract: A human gene termed APC is disclosed. Methods and kits are provided for assessing mutations of the APC gene in human tissues and body samples. APC mutations are found in familial adenomatous polyposis patients as well as in sporadic colorectal cancer patients. APC is expressed in most normal tissues. These results suggest that APC is a tumor suppressor.
Type:
Grant
Filed:
May 25, 1995
Date of Patent:
July 21, 1998
Assignees:
The Johns Hopkins University, The University of Utah, Zeneca Pharmaceuticals, The Cancer Institute
Inventors:
Hans Albertsen, Rakesh Anand, Mary Carlson, Joanna Groden, Philip John Hedge, Geoff Joslyn, Kenneth Kinzler, Alexander Fred Markham, Yusuke Nakamura, Andrew Thliveris, Bert Vogelstein, Raymond L. White
Abstract: A thermal transfer sheet comprising a substrate having a coating comprising a dye which carries an ##STR1## wherein R.sup.1 is an optionally substituted branched chain alkyl group; andR.sup.2 is an optionally substituted alkyl group or an optionally substituted aryl group provided that the dye is not a monoazo dye or that the dye is not 3-(2,3-dihydroindol-1-yl)-2-?4-(isopropylpropylamino)-2-methylphenylimino! -3-oxo-N-(2,4,5-trichlorophenyl)propionamide.
Abstract: A process for colouring a synthetic textile material or fiber blend thereof which comprises applying to the synthetic textile material a compound of Formula (1):A--N.dbd.N--D--N.dbd.N--E Formula (1)wherein:A, D and E each independently is an optionally substituted heterocyclic or carbocyclic group and at least one of A, D or E carries directly at least one --SO.sub.2 F group or carries a substituent to which at least one --SO.sub.2 F group is attached.A process for the mass coloration of plastics which comprises incorporating into a plastics material a compound or mixture thereof which is free from water solubilising groups, of Formula (1).
Abstract: A process for preparing a compound of formula (I), ##STR1## where R.sup.1 is optionally substituted alkyl or phenyl, R.sup.2 is COOH, and R.sup.3 and R.sup.4 are independently selected from hydrogen, halo, haloalkyl, nitro, hydroxy, alkoxy, haloalkoxy or alkoxyalkoxy; which process comprises oxidising a compound of formula (II) ##STR2## where R.sup.1, R.sup.3 and R.sup.4 are as defined in relation to formula (I) and R.sup.5 is H, halo or C.sub.1-4 alkyl with sodium hypochlorite or sodium chlorite in the presence of a catalytic amount of a ruthenium or palladium compound and a phase transfer catalyst in an organic solvent at a pH of 7-11.
Type:
Grant
Filed:
November 18, 1996
Date of Patent:
July 21, 1998
Assignee:
Zeneca Limited
Inventors:
Stephen Martin Brown, Martin Charles Bowden, Keith Moorhouse
Abstract: An ink composition comprising:(i) a medium comprising a low melting point solid, an organic solvent, or a mixture of water and one or more water-soluble organic solvent(s); and(ii) from 0.5 to 20% based on the total weight of the ink composition of at least one dye selected from a dye of Formula (1), a dye of Formula (2) and a dye of Formula (3) or a mixture thereof: ##STR1## wherein: R and R.sup.1 each independently represent an alkylene group; andR.sup.2 and R.sup.3 each independently represent an alkyl group.Also claimed is a process for ink jet printing of textiles using the inks, a process for ink jet printing a substrate with the inks and a toner resin composition containing a dye of Formula (1), (2) or (3) or a mixture thereof.
Abstract: An ink composition comprising a medium comprising at least one of a low melting point solid, an organic solvent and a mixture of water and one or more water-soluble organic solvent(s); and a mixture of a first, second, third and fourth dye, each of which is of Formula (1) or a salt thereof: ##STR1## wherein: X is a labile or non labile atom or group;A and B are each independently an optionally substituted phenylene group;one or R.sup.1 and R.sup.2 is H and the other is sulpho;one of R.sup.3 and R.sup.4 is H and the other is sulpho;R.sup.5 and R.sup.6 are each independently C.sub.1-4 -alkyl.Also claimed is an ink jet printing process using the inks, a process for ink jet printing textile materials using the inks and a toner containing a mixture of a first, second, third and fourth dyes of the Formula (1).
Abstract: An ink composition comprising:(i) a medium comprising a low melting point solid, an organic solvent, or a mixture of water and one or more water-soluble organic solvent(s); and(ii) an azothiophene of Formula (1): ##STR1## wherein: R, R.sup.1, R.sup.2 and R.sup.3 each independently is optionally substituted alkyl or alkenyl.Also claimed are inks containing mixtures of the azothiophene of Formula (1) with other azothiophenes and with azo dyes, a process for ink jet printing of textiles using the inks, a process for ink jet printing a substrate with the inks and toner resin composition containing an azothiophene of Formula (1).
Abstract: A process comprising the reaction of an optionally substituted benzene with thiophosgene in the presence of a Friedel Crafts catalyst for the preparation of the equivalent optionally substituted benzophenthione. The benzophenthiones are converted into the equivalent benzophenone derivatives by hydrolysis.
Type:
Grant
Filed:
November 18, 1996
Date of Patent:
July 7, 1998
Assignee:
Zeneca Limited
Inventors:
Michael Charles Henry Standen, Nicholas Charles Evens
Abstract: Described herein are compounds of Formula (XX) and Formula (XXIV), shown below, and processes of making same. ##STR1## wherein p is 0 ##STR2## wherein p is 1, and Y is chlorine or bromine.
Type:
Grant
Filed:
November 12, 1996
Date of Patent:
July 7, 1998
Assignee:
Zeneca Limited
Inventors:
Ian Richard Matthews, Christopher Richard Ayles Godfrey, John Martin Clough
Abstract: The present invention provides novel methods of treating pain comprising administering to a mammal in need of such treatment an effective analgesic amount of a peptide having the amino acid sequence of SEQ ID. NO.:1 or SEQ ID NO: 2. The invention further provides a purified peptide having the amino acid sequence of SEQ ID NO: 1. The peptides of SEQ ID NO.: 1 and SEQ ID NO.: 2 can also be used in methods for identifying compounds having analgesia-inducing activity.
Abstract: A method for identifying compounds which modulate protein/cell membrane association which method comprises contacting a test compound with a cell, having (i) a cell membrane, (ii) a heterologous protein comprising a reporter sequence and a recognition sequence for cell membrane association, (iii) a reporter system which is acted upon by the reporter sequence such that there is a measurable change in cell phenotype upon modulation of protein/cell membrane association by the test compound, and detecting any change in cell phenotype.
Abstract: Antimicrobial proteins capable of isolation from seeds of Allium show a wide range of antifungal activity and some activity against Gram-positive bacteria. DNA encoding the proteins may be isolated and incorporated into vectors. Plants transformed with this DNA may be produced. The proteins find commercial application as antifungal or antibacterial agents; transformed plants will show increased disease resistance.
Type:
Grant
Filed:
January 25, 1996
Date of Patent:
June 30, 1998
Assignee:
Zeneca Limited
Inventors:
Willem Frans Broekaert, Bruno Philippe Angelo Cammue, Sarah Bronwen Rees