Patents Assigned to Zeneca
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Patent number: 5443971Abstract: A process for the separation of at least one isomer from a mixture of isomers of a tetrahydropyran-2-one, having at least two chiral centers which comprises selective reaction of at least one isomer with a reagent catalyzed by a hydrolase enzyme whereby at least one isomer is preferentially converted into a distinct chemical species from the other isomers so that it is susceptible of separation by an appropriate chemical or physical separation process in which the tetrahydropyran-2-one is of Formula (1): ##STR1## wherein: Z is --H or a protecting group susceptible of reaction with the reagent under the influence of the enzyme; andY is formyl or protected formyl.Type: GrantFiled: September 17, 1992Date of Patent: August 22, 1995Assignee: Zeneca LimitedInventors: Andrew J. Blacker, John Crosby, John A. L. Herbert
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Patent number: 5444038Abstract: This invention relates to substituted aryl indazoles, a process for producing them and their use as herbicides. In particular this invention relates to substituted aryl indazoles of the formula ##STR1## wherein all variables are as defined in the specification.Type: GrantFiled: March 2, 1993Date of Patent: August 22, 1995Assignee: Zeneca LimitedInventors: Donald R. James, Don R. Baker, Steven D. Mielich, William J. Michaely, Steven Fitzjohn, Christopher G. Knudsen, Christopher Mathews, John M. Gerdes
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Patent number: 5443970Abstract: A process for the separation of at least one isomer from a mixture of isomers of a tetrahydropyran-2-one, having at least two chiral centres, which comprises selective reaction of at least one isomer with a reagent catalysed by a hydrolase enzyme whereby at least one isomer is preferentially converted into a distinct chemical species from the other isomers so that it is susceptible of separation by an appropriate chemical or physical separation process in which the tetrahydropyranone is of Formula (1): ##STR1## wherein: Z is --H or a protecting group susceptible of reaction with the reagent under the influence of the enzyme; andY is optionally substituted hydrocarbyl.Type: GrantFiled: September 17, 1992Date of Patent: August 22, 1995Assignee: Zeneca LimitedInventors: Andrew J. Blacker, John Crosby, John A. L. Herbert
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Patent number: 5444057Abstract: The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## 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;and the pyridyl group is bonded to the nitrogen of the linking carbamoyl group by a carbon atom, is substituted with the carboxy group on a carbon atom and is optionally substituted on one or two pyridyl ring carbon atoms; or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.Type: GrantFiled: September 15, 1994Date of Patent: August 22, 1995Assignee: Zeneca LimitedInventor: Frederic H. Jung
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Patent number: 5441867Abstract: Pre-activated stable protein reagents are provided. The reagents can be made by reaction of the protein and a heterobifunctional linker and have extended stability especially after lyophilisation. The reagents can be used in assay kits to form conjugates with proteins e.g. antibodies or polynucleotides e.g. oligonucleotides probes.Type: GrantFiled: January 7, 1992Date of Patent: August 15, 1995Assignee: Zeneca LimitedInventors: Andrew J. Garman, John R. Parker
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Patent number: 5441960Abstract: The present invention relates to certain novel substituted ketones which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates ##STR2## useful in the synthesis of these substituted ketones processes for preparing the substituted ketones pharmaceutical compositions containing such substituted ketones and methods for their use.Type: GrantFiled: April 8, 1993Date of Patent: August 15, 1995Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Philip D. Edwards, Andrew Shaw, Royston M. Thomas, Chris A. Veale, Peter Warner, Donald J. Wolanin
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Patent number: 5441949Abstract: The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## 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;P.sup.1 is of the formula: ##STR2## and one or two of A,B,C,D,E,F,G and H, are nitrogen and the remainder are CH; and P is bonded to the nitrogen of the linking carbamoyl group by a carbon atom, in either ring, is substituted by the carboxy group on a carbon atom, in either ring, and is optionally further substituted, by up to three substitutents, on a carbon atom, in either ring; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them are also described.Type: GrantFiled: September 16, 1994Date of Patent: August 15, 1995Assignee: Zeneca LimitedInventors: Frederic H. Jung, Jean-Claude Arnould
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Patent number: 5442052Abstract: DNA construct for use in transforming plant cells comprises and exogenous gene with upstream promoter and downstream terminator sequences, the promoter being a DNA sequence of not less than about 5 kilobases homologous to the DNA control sequence found upstream of the tomato PG gene. Preferably the terminator is homologous to the DNA control sequence of about 1.6 kilobases found downstream of the tomato polygalacturonase gene. Enhanced expression of the exogenous gene is obtained. The invention also included plant cells containing such constructs and plants derived therefrom.Type: GrantFiled: July 8, 1993Date of Patent: August 15, 1995Assignee: Zeneca LimitedInventors: Colin R. Bird, Donald Grierson, Wolfgang W. Schuch
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Patent number: 5440035Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: October 25, 1994Date of Patent: August 8, 1995Assignee: Zeneca Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 5439910Abstract: Compounds having formula (I) ##STR1## wherein R.sup.1, R.sup.2 and A are defined as in the specification. The compounds are useful as fungicides.Type: GrantFiled: October 12, 1993Date of Patent: August 8, 1995Assignee: Zeneca LimitedInventors: Paul J. de Fraine, John M. Clough, Paul A. Worthington, Brian L. Pilkington, Ian R. Matthews
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Patent number: 5438066Abstract: Fungicidal and insecticidal compounds having the general formula (I): ##STR1## or a stereoisomer thereof, wherein A is CH or N; B is OCH.sub.3 or NHCH.sub.3 ; one of L and M is N and the other is S or O; X is an optionally substituted carbocyclic or heterocyclic group; and n is 0 or 1.Type: GrantFiled: October 27, 1993Date of Patent: August 1, 1995Assignee: Zeneca LimitedInventor: Ian R. Matthews
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Patent number: 5438059Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is optionally substituted aryl or optionally substituted heteroaryl; Y is oxygen, sulphur or NR.sup.4 ; R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, are hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl; X is halogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkoxy, nitro or cyano; and n is 0 or an integer of 1 to 4; provided that when Y is oxygen, n is 0 and R.sup.1 is unsubstituted phenyl at least one of R.sup.2 and R.sup.3 is other than hydrogen or methyl.Type: GrantFiled: July 6, 1993Date of Patent: August 1, 1995Assignee: Zeneca LimitedInventors: John M. Clough, Christopher R. A. Godfrey, Paul J. de Fraine, Michael G. Hutchings, Vivienne M. Anthony
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Patent number: 5433855Abstract: A process for extracting metal values especially zinc values from aqueous solutions of metal salts which comprises contacting the aqueous solution with an organic phase comprising a compound of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4, independently, represents an optionally substituted hydrocarbyl or hydrocarbyloxy group or R.sup.1 and R.sup.2 together with the attached phosphorus atom and/or R.sup.3 and R.sup.4 together with the attached phosphorus atom form a 5- to 8-membered heterocyclic ring.Type: GrantFiled: December 3, 1993Date of Patent: July 18, 1995Assignee: Zeneca LimitedInventors: John Campbell, Raymond F. Dalton, Peter M. Quan
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Patent number: 5434184Abstract: Compounds of the formula (I): ##STR1## and bioprecursors and pharmaceutically acceptable salts thereof are described as .beta..sub.3 -adrenoceptor agonsists having anti-obesity, hypoglycaemic and related therapeutic utilities. Processes for their preparation are described as are compositions containing them.Type: GrantFiled: November 18, 1994Date of Patent: July 18, 1995Assignee: Zeneca LimitedInventors: Brian R. Holloway, Ralph Howe, Balbir S. Rao
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Patent number: 5432197Abstract: Compounds having the formula (I) : ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.Type: GrantFiled: August 25, 1994Date of Patent: July 11, 1995Assignee: Zeneca LimitedInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5430007Abstract: Novel substituted pyrazolo-rings fused to nitrogen containing heterocyclic rings having the following formula ##STR1## in which at least one of Y, Z or W is N or N-O and the remainder of Y, Z or W is C-R wherein the remainder of the variables are as defined in the specification and agriculturally effective salts thereof are herbicides.Type: GrantFiled: January 3, 1994Date of Patent: July 4, 1995Assignee: Zeneca LimitedInventors: William J. Michaely, Jeff K. Curtis, Christopher G. Knudsen
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Patent number: 5430060Abstract: The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.Type: GrantFiled: September 15, 1993Date of Patent: July 4, 1995Assignee: Zeneca LimitedInventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Slater
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Patent number: 5426091Abstract: A compound of formula (I): ##STR1## or a salt, enamine or the like, acylate, sulphonate, carbamate or ether derivative thereof; wherein X, X.sup.1 and X.sup.2 are independently oxygen or sulphur, R.sup.1 is an optionally substituted heterocyclic or cycloalkyl group, and Y is an optionally substituted C.sub.2 -C.sub.4 alkylene group which is optionally interposed by an oxygen atom, a group ##STR2## or an optionally mono-substituted nitrogen atom, wherein p is 0, 1 or 2, s is 0 or 1 and R.sup.b is alkyl or alkoxy; provided that when X, X.sup.1 and X.sup.2 are oxygen, R.sup.1 is not pyridyl or pyrimidinyl. Processes for the preparation of these compounds and herbicidal compositions containing them are also described and claimed.Type: GrantFiled: August 4, 1993Date of Patent: June 20, 1995Assignee: Zeneca LimitedInventors: John E. D. Barton, David Cartwright, John M. Cox, Glynn Mitchell, Charles G. Carter, David L. Lee, Francis H. Walker, Frank X. Woolard
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Patent number: 5423906Abstract: A compound of Formula (1) or salt thereof: ##STR1## wherein: R.sup.1 is H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, CO.sub.2 H, SO.sub.3 H or --NR.sup.3 R.sup.4 ;R.sup.2 is H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, CO.sub.2 H or SO.sub.3 H;R.sup.3 and R.sup.4 are each independently H, C.sub.1-18 -alkyl or R.sup.3 and R.sup.4, together with the nitrogen atom to which they are attached, form an optionally substituted 5- or 6-membered ring;W is --OH and X is --NH.sub.2, or W is --NH.sub.2 and X is --OH; andY and Z are each independently --OH or --NR.sup.3 R.sup.4.The compound is suitable for use as a black component of ink jet printing inks.Type: GrantFiled: August 19, 1993Date of Patent: June 13, 1995Assignee: Zeneca LimitedInventors: Peter Gregory, Prahalad M. Mistry
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Patent number: 5420298Abstract: The invention concerns pyrrolidine derivatives of the formula ##STR1## wherein Ar.sup.1 is optionally-substituted phenyl, naphthyl or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A is a direct link to the group X or A is (1-4C)alkylene;X is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophendiyl, furandiyl or thiazolediyl;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl;R.sup.2 is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, halogeno-(1-4C)alkyl, halogeno-(2-4C)alkenyl, halogeno-(2-4C)alkynyl, (1-4C)alkoxy-(2-4C)alkyl, hydroxy-(2-4C)alkyl, cyano-(1-4C)alkyl, carboxy-(1-4C)alkyl, carbamoyl-(1-4C)alkyl, (1-4C)alkoxycarbonyl-(1-4C)alkyl, N-(1-4C)alkylcarbamoyl-(1-4C)alkyl or N,N-di-(1-4C)alkylcarbamoyl-(1-4C)alkyl; andn is 1 or 2 and each R.sup.Type: GrantFiled: September 1, 1993Date of Patent: May 30, 1995Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Philip N. Edwards, Michael S. Large