Abstract: Antagonists at the NMDA receptor complex which are benz[b]azepines having a hydroxy, alkoxy or amino substituent at the 3-position and a 4-position alkenyl, alkynyl, aryl or heteroaryl substituent for treatment of stroke and/or other neurodegenerative disorders.
Type:
Grant
Filed:
October 19, 1995
Date of Patent:
August 12, 1997
Assignee:
Zeneca Limited
Inventors:
Marc Jerome Chapdelaine, Timothy W. Davenport, Laura E. Garcia-Davenport, Paul Francis Jackson, Jeffrey A. McKinney, Charles D. McLaren
Abstract: Benz[b]azepine compounds, pharmaceutical compositions containing them and methods for the treatment of neurological disorders utilizing them.
Type:
Grant
Filed:
September 7, 1995
Date of Patent:
August 5, 1997
Assignee:
Zeneca Limited
Inventors:
Gregory David Harris, Marc Jerome Chapdelaine, Paul Francis Jackson
Abstract: The present invention concerns the novel use of aryl substituted heterocycles of formula I, set out below, which antagonize the pharmacological actions of one of ent endogenous neuropeptide tachykinins an the neurokinin 2 (NK2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the aryl substituted heterocycles for use in such treatment. Certain novel aryl substituted heterocycles of formula I and novel intermediates for their manufacture are also provided.
Type:
Grant
Filed:
April 18, 1994
Date of Patent:
August 5, 1997
Assignee:
Zeneca Limited
Inventors:
Ashokkumar Bhikkappa Shenvi, Robert Toms Jacobs
Abstract: Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Novel intermediates are also disclosed.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
July 29, 1997
Assignee:
Zeneca Limited
Inventors:
Michael Garth Wayne, Michael James Smithers, John Wall Rayner, Alan Wellington Faull, Robert James Pearce, Andrew George Brewster, Richard Eden Shute, Stuart Dennett Mills, Peter William Rodney Caulkett
Abstract: The present invention relates to carbapenems and provides a compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein:R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl;R.sup.4 and R.sup.5 are the same or different and are selected from hydrogen, halo, cyano, C.sub.1-4 alkyl, nitro, hydroxy, carboxy, C.sub.1-4 alkoxy, C.sub.1-4 alkoxycarbonyl, aminosulphonyl, C.sub.1-4 alkylaminosulphonyl, di-C.sub.1-4 -alkylaminosulphonyl, carbamoyl, C.sub.1-4 alkylcarbamoyl, di-C.sub.1-4 alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.1-4 alkanoylamino, C.sub.1-4 alkanoyl(N-C.sub.1-4 alkyl)amino, C.sub.1-4 alkanesulphonamido and C.sub.1-4 alkylS(O)n- wherein n is zero, one or two:with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the link to --NR.sup.3 --.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
July 29, 1997
Assignee:
Zeneca Limited
Inventors:
Michael John Betts, Gareth Morse Davies, Michael Lingard Swain
Abstract: A method for the preparation of 2-(substituted)-4-methylsulfonylbenzoic acid by reacting a 2-(substituted)-4-nitrobenzoic acid with sodium methyl sulfinate.
Abstract: Methods 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. APC is a tumor suppressor.
Type:
Grant
Filed:
August 12, 1994
Date of Patent:
July 15, 1997
Assignees:
The John Hopkins University, University of Utah, Japanese Foundation for Cancer Research Cancer Institute, Zeneca Limited
Inventors:
Hans Albertsen, Rakesh Anand, Mary Carlson, Joanna Groden, Philip John Hedge, Geoff Joslyn, Kenneth Kinzler, Alexander Markham, Yusuke Nakamura, Andrew Thliveris, Bert Vogelstein, Raymond L. White
Abstract: Polymer compositions are provided which comprise a first polyhydroxyalkanoate component and optionally a second polymer component, the composition have enhanced properties by using an inorganic oxygen containing compound in the composition. The inorganic oxygen containing compound may be acting as a transesterification catalyst.
Abstract: The invention concerns pharmaceuticaly useful compounds of the formula I, in which Q, A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutically compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
Abstract: Microspheres containing an agriculturally active material are produced by mixing a liquid phase containing the agriculturally active material and optionally an emulsifying agent and an aqueous phase containing polyvinyl alcohol and adding a material selected from clays, silicas, starch, and starch derivatives, followed by spray drying.
Abstract: This invention comprises a granular pesticidal composition having improved attrition resistance comprising from about 10 to about 20% by weight of a pesticide, a glycol or polyvinyl alcohol, the remainder comprising montmorillonite or kaolin clay granules.
Abstract: Described herein is a process for the preparation of (1S,2R)-1,2-epoxy-1,2,3,4-tetrahydronaphthalene having the Formula (I): ##STR1## which comprises the steps of (a) hydrogenating the compound of Formula (II) to form cis-(1R, 2S)-1,2-dihydroxy-1,2,3,4-tetrahydronaphthalene having the Formula (V): ##STR2## (b) reacting the dihydroxy compound of Formula (V) with a sulphonyl halide of formula R.sup.1 SO.sub.2 Z wherein R.sup.1 is methyl, ethyl, trifluoromethyl, phenyl or p-tolyl, and Z is fluorine, chlorine, bromine or iodine to give a bis-sulphonyl ester of formula (X): ##STR3## and (c) treating the bis-sulphonyl ester (X) with an alkali metal carbonate or alkali metal hydroxide to give the compound of Formula (I).
Type:
Grant
Filed:
August 25, 1995
Date of Patent:
June 10, 1997
Assignee:
Zeneca Limited
Inventors:
Andrew J. Blacker, Stephen M. Brown, Derek R. Boyd, Gary N. Sheldrake
Abstract: A process for transforming a carbonyl compound into its corresponding epoxide, which comprises contacting the carbonyl compound with either trimethylsulphonium hydrogen sulphate and/or bis(trimethylsulphonium) sulphate or trimethylsulphoxonium hydrogen sulphate and/or bis(trimethylsulphoxonium) sulphate, in the presence of a base.
Type:
Grant
Filed:
August 10, 1993
Date of Patent:
June 10, 1997
Assignee:
Zeneca Limited
Inventors:
Raymond V. H. Jones, Elizabeth S. C. Simpson
Abstract: A method for the preparation of a 2-hydroxybenzonitrile which comprises reacting hydroxylamine with a 2-hydroxyarylaldehyde which is at least partially in the form of a salt and/or complex of a metal of Group II, Group III, Group IVA or Group VIA of the Periodic Table and dehydrating the 2-hydroxyarylaldoxime so formed.
Abstract: Aqueous coating composition for a plastics, especially a polypropylene, substrate comprising a stable aqueous dispersion derived from dispersing into water with the aid of a surfactant(s) an organic solvent solution of a composition comprising a chlorinated polyolefine(s), at least one olefinically unsaturated monomer which is polymerisable to a polymer during and/or after coating formation and a filmogenic polymer(s).
Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
Type:
Grant
Filed:
May 1, 1995
Date of Patent:
June 3, 1997
Assignee:
Zeneca Limited
Inventors:
Robert T. Jacobs, Scott C. Miller, Ashokkumar B. Shenvi, Cyrus J. Ohnmacht, Jr., Chris A. Veale
Abstract: This invention relates to derivatives of acrylic acid useful in agriculture (especially as fungicides but also as plant growth regulators, insecticides and nematocides), to processes for preparing them, to agricultural (especially fungicidal) compositions containing them, and to methods of using them to combat fungi, especially fungal infections in plants, to regulate plant growth and to kill or control insect or nematode pests. The invention provides a compound having the formula (I): ##STR1## and stereoisomers thereof, wherein W is a substituted pyridinyl or substituted pyrimidinyl group linked to A by any of its ring carbon atoms; A is either an oxygen atom or S(O).sub.
Type:
Grant
Filed:
March 29, 1995
Date of Patent:
May 27, 1997
Assignee:
Zeneca Limited
Inventors:
Vivienne M. Anthony, John M. Clough, Paul DeFraine, Christopher R. A. Godfrey
Abstract: A treatment for tumors to which antibody A5B7 binds is disclosed. A5B7 is a monoclonal antibody which binds to carcinoembryonic antigen. The treatment comprises administering to a host in need of such treatment an effective amount of a system which comprises: a conjugate comprising antibody A5B7 or a humanized version of A5B7 linked to an enzyme selected from the group consisting of carboxypeptidase G2 (CPG2), nitroreductase, a human enzyme, a non-human enzyme rendered non-immunogenic in man and a humanized catalytic antibody; and a prodrug convertible under the influence of the conjugate into a cytotoxic drug.
Type:
Grant
Filed:
September 28, 1994
Date of Patent:
May 27, 1997
Assignees:
Cancer Research Campaign Tech. Ltd., Zeneca Ltd.
Inventors:
Kenneth D. Bagshawe, Gordon T. Rogers, Surinder K. Sharma
Abstract: A gene promoter sequence has been isolated and characterised from the plant gene encoding the enzyme cinnamyl alcohol dehydrogenase (CAD), an enzyme which participates in the biosynthesis of lignins. The promoter may be used to control expression of exogenous genes placed under its control. Genes controlled by the CAD promoter is inducible by wounding.
Abstract: The use of oligomeric imidazolium, pyrazolium and triazolium salts as swimming pool sanitizers having improved compatibility with chlorine. Bisimidazolium salts are preformed.
Type:
Grant
Filed:
April 11, 1995
Date of Patent:
May 20, 1997
Assignee:
Zeneca Limited
Inventors:
Peter W. Austin, Clive H. Barlow, Brian D. Bothwell, Andrew N. Collins, Mark R. James