Abstract: The present invention concerns the novel alkyl substituted heterocycles of formula I, set out below, wherein Q, Q.sup.1, Q.sup.2 and R have the values defined herein, which antagonize the pharmacological actions of one of the endogenous neuropeptide tachykinins at the neurokinin 2 (NK.sup.2) 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 alkyl substituted heterocycles for use in such treatment, methods for their use, and processes and novel intermediates for their manufacture.
Abstract: Haloalkanoic acid impurities are decomposed in the presence of certain surfactants carboxymethyl cellulose or thioglycollic acids salts which may contain them as unconverted reactants by contacting them with dehalogenase enzyme.
Abstract: 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 thienyl ring is optionally further substitued by one or two substituents selected from halo, cyano, C.sub.1-4 alkyl, nitro, hydroxy, carboxy, C.sub.1-4 alkoxy, trifluoromethyl, C.sub.1-4 alkoxycarbonyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, sulfonic acid, C.sub.1-4 alkylS(O).sub.n -- (wherein n is 0-2), C.sub.1-4 alkanoylamino, C.sub.1-4 alkanoyl(N-C.sub.1-4 alkyl)amino, carbamoyl, C.sub.1-4 alkylcarbamoyl, di-C.sub.1-4 alkylcarbamoyl and N-C.sub.1-4 alkanesulfonamido; or by a tetramethylene group attached to adjacent carbon atoms on the thienyl ring; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.
Abstract: A high strength aqueous solution comprising a first and second dye each of which, in the free acid form, is of Formula (1): ##STR1## wherein: R.sup.1 is NH.sub.2 or alkyl;W is H, alkyl or alkoxy;X is a labile atom or group;A is ##STR2## Y is H or alkyl; Z is an optionally substituted phenyl group; andn has a value of 1 to 3;provided that(i) the groups defined by A in the first and second dye are different to one another; and(ii) the solution contains less than 5% by weight of inorganic compounds.Also claimed are compositions and dyes of Formula (1).
Type:
Grant
Filed:
March 7, 1995
Date of Patent:
May 14, 1996
Assignee:
Zeneca Limited
Inventors:
Brian Lamble, Aiden Lavery, John A. Taylor
Abstract: A phthalocyanine of Formula (1): ##STR1## wherein: M.sub.k PC iS a phthalocyanine nucleus of Formula (2): ##STR2## M is a metal atom, a chloro-metal group, and oxy-metal group or hydrogen; k is inverse of 1/2 valency of M;R and R.sup.1 each independently is an organic radical;R.sup.2 is H or optionally substituted alkyl;a is an average value from 15 to 8;b is an average value from 1 to 8; anda+b is from 15 to 16; and sulphonated derivatives thereof and process for their preparation.The phthalocyanines of the present invention are useful for absorbing electro-magnetic radiation from for example a laser source and may be used in a coating for optical data storage disks, or in security applications such as printing banknotes or checks, or in the preparation of lithographic printing plates or in washing powders to assist in bleaching.
Type:
Grant
Filed:
July 20, 1994
Date of Patent:
May 14, 1996
Assignee:
Zeneca Limited
Inventors:
James S. Campbell, Peter Gregory, Dean Thetford
Abstract: Biodegradable polyesters derived from hydroxy alkenoic acids may be plasticised with an esterified hydroxycarboxylic acid which has at least three ester groups, at least some of the hydroxy groups being esterified with a carboxylic acid and at least some of the carboxy groups being esterified with an alcohol and/or phenol.
Abstract: Biocidal proteins capable of isolation from seeds have been characterized. The proteins have an amino acid sequence containing the common cysteine/glycine domain of Chitin-binding Plant Proteins but show substantially better activity against pathogenic fungi, a higher ratio of basic amino acids to acidic amino acids, and/or antifungal activity which results in increased hyphal branching. Antimicrobial proteins isolated from Amaranthus, Capsicum, Briza and related species are provided. The proteins show a wide range of antifungal activity and are active against Gram-positive bacteria. DNA encoding the proteins may be isolated and incorporated into vectors. Plants may be transformed with this DNA. The proteins find agricultural or pharmaceutical application as antifungal or antibacterial agents. Transgenic plants expressing the protein will show increased disease resistance.
Type:
Grant
Filed:
November 10, 1993
Date of Patent:
May 7, 1996
Assignee:
Zeneca Limited
Inventors:
Willem F. Broekaert, Bruno P. A. Cammue, Sarah B. Rees, Jozef Vanderleyden
Abstract: Solid herbicidal compositions contain N-phosphonomethylglycine and an alkyl phenol polyoxyethylene surfactant containing from about 50 to about 90 weight percent of an alkyl phenol polyoxyethylene carboxylic acid.
Abstract: The invention concerns ether derivatives of the formula IQ.sup.1 -X-Ar-Q.sup.2 Iwherein Q.sup.1 is an optionally substituted 9-, 10- or 11-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur; X is oxy, thio, sulphinyl or sulphonyl; Ar is optionally substituted phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazolediyl, thiadiazolediyl or oxadiazolediyl; and Q.sup.2 is selected from the groups of the formulae II and III: ##STR1## wherein R.sup.1 is hydrogen, (2-5C)alkanoyl or optionally substituted benzoyl; R.sup.2 is (1-4C)alkyl; and R.sup.3 is hydrogen or (1-4C)alkyl; or R.sup.2 and R.sup.3 are linked to form a methylene, vinylene, ethylene or trimethylene group; or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
Type:
Grant
Filed:
May 12, 1995
Date of Patent:
April 30, 1996
Assignees:
Zeneca Limited, Zeneca Pharma S.A.
Inventors:
Thomas G. C. Bird, Graham C. Crawley, Michael S. Large, Patrick Ple
Abstract: Compounds of formula I or I', ##STR1## wherein X and Y are independently selected from hydrogen, halo, and (1-6C)alkoxy;R.sup.1 is selected from(A) (1-6C)alkyl;(B) phenyl and naphthyl or substituted versions thereof;(C) phenyl (1-3C)alkyl and naphthyl (1-3C) alkyl;(D) five- and six-membered heteroaryl rings;(E) heteroaryl (1-3C)alkyl and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I or I' and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropsychiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I or I', or a pharmaceutically acceptable salt thereof are claimed. The invention also relates to novel processes for producing enantiomeric methanoanthracenyl sulfoxides.
Type:
Grant
Filed:
October 19, 1993
Date of Patent:
April 30, 1996
Assignee:
Zeneca Limited
Inventors:
Robert T. Jacobs, Michael T. Klimas, Cyrus J. Ohnmacht, Marc O. Terpko
Abstract: Herbicidal compounds have the formula ##STR1## in which R.sub.1 is hydrogen, methyl, ethyl, phenyl, 2-methylphenyl, 3-trifluoromethylphenyl, benzyl, 2-methylbenzyl or vinyl;R.sub.2 is hydrogen, methyl, ethyl or chloro;R.sub.3 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, nitro, p-tolyloxy or p-chlorophenoxy;R.sub.4 is hydrogen or a methyl, methoxy, trifluoromethoxy or halo group at the 2, 4- or 5-position;m is --CH or N; andX is O or NOR.sub.5 in which R.sub.5 is methyl or ethyl; provided that:(a) when R.sub.1 is methyl, and(i) R.sub.3 is methyl, then R.sub.4 is 4-methyl, 4-methoxy or chloro;(ii) R.sub.3 is nitro, then R.sub.4 is methoxy;(b) when R.sub.1 is ethyl, R.sub.3 is methyl or methoxy;(c) when R.sub.2 is chloro, R.sub.3 and R.sub.4 are independently C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy or C.sub.1 -C.sub.4 alkoxy;(d) when R.sub.2 is methyl or ethyl, R.sub.1 is hydrogen;(e) when R.sub.3 is hydrogen, R.sub.
Abstract: A process for the solid phase synthesis of peptides containing an aza-amino acid, for example the decapeptide goserelin, which comprises:(i) assembling all the amino acids of the peptide except the C-terminal aza-amino acid by conventional solid phase synthesis;(ii) cleaving the peptide from the support with hydrazine or a substituted hydrazine; and(iii) reacting the hydrazide thus released with a cyanate ion.
Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A-B have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
Type:
Grant
Filed:
March 11, 1994
Date of Patent:
April 23, 1996
Assignee:
Zeneca Limited
Inventors:
James R. Empfield, Daniel R. Mayhugh, Keith Russell
Abstract: Novel substituted cis-1,2-dihydroxy-cyclohexadiene compounds, useful as intermediates in the production of compounds for use as intermediates in the production of agrochemicals and pharmaceuticals, and a microbial process for the preparation thereof.
Type:
Grant
Filed:
November 17, 1994
Date of Patent:
April 16, 1996
Assignee:
Zeneca Limited
Inventors:
Andrew J. Blacker, Martin Brown, Martin C. Bowden
Abstract: A method of selectively controlling undesirable vegetation in corn by applying an herbicidally effective amount of 2-(2'-nitro-4'-methylsulfonylbenzoyl)-1,3-cyclohexanedione to the locus of such vegetation.
Abstract: A compound of the general formula ##STR1## or a salt or complex thereof, in which X, Y and Z are all optionally substituted carbon atoms and R is hydrogen, optionally substituted hydrocarbyl or acyl or --COOR.sup.7 and R.sup.7 is hydrocarbyl has anti-microbial properties. Particular examples are compounds in which X is --CH.sub.2 -- or --C(CH.sub.3).sub.2 -- and Y and Z are both --CH.sub.2 -- or X is is --CH.sub.2 -- and Y and Z are carbon atoms of a benzene ring. The zinc complexes have useful properties.
Abstract: The invention provides a pharmaceutical composition comprising a particular physical form of N- 4- 5-(cyclopentyloxy-carbonyl)amino-1-methylindol-3-yl-methyl!-3-methox ybenzoyl!-2-methylbenzenesulphonamide and polyvinylpyrrolidone. It also provides methods for preparing this physical form, and another physical form of N- 4- 5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-methyl!-3-methoxy benzoyl!-2-methylbenzenesulphonamide useful in the preparation of the first mentioned physical form. The compositions are useful in the treatment of diseases in which leukotrienes are implicated, for example asthma.
Abstract: Process for preparing the (E)-isomer of a compound (II) by contacting the (E) or (Z) isomer of the 2-methylphenyl precursor, or a mixture of both, with bromine in an organic solvent, in the presence of a polymeric base and light.
Abstract: Compounds of formula I ##STR1## wherein R.sup.1 -R.sup.4, X, Y, and Z have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful as potassium channel openers for the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
Abstract: A plant which produces polyhydroxyalkanoate polymer has a recombinant genome which contains one or more than one of the genes specifying enzymes critical to the polyhydroxyalkanoate biosynthetic pathway which occurs in certain micro-organisms such as Alcaligenes eutrophus which naturally produce same. The plant species is preferably an oil-producing plant.
Type:
Grant
Filed:
September 28, 1994
Date of Patent:
March 26, 1996
Assignee:
Zeneca Limited
Inventors:
Simon W. J. Bright, David Byrom, Philip A. Fentem