Patents Assigned to Zeneca Limited
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Patent number: 6084103Abstract: The present invention provides an improved process for preparing (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VII) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.Type: GrantFiled: May 13, 1998Date of Patent: July 4, 2000Assignee: Zeneca LimitedInventor: Rajnikant Patel
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Patent number: 6083951Abstract: Pyrimidine sulphonamide compounds of the following formula, ##STR1## wherein Q is a naphthyl or biphenyl group either unsubstituted or substituted with A.sup.1, and where A.sup.1, R.sup.1 and R.sup.2 are a variety of alkyl, aryl and cyclic moieties, as described in the specification hereof, which compounds are useful for the treatment of diseases or medical conditions such as hypertension, pulmonary hypertension, cardiac or cerebral circulatory disease and renal disease.Type: GrantFiled: December 14, 1998Date of Patent: July 4, 2000Assignee: Zeneca LimitedInventor: Robert Hugh Bradbury
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Patent number: 6077522Abstract: Microcapsules containing a biologically active material which is sensitive to ultraviolet light are prepared which contain an ultraviolet light protectant selected from titanium dioxide, zinc oxide and mixtures thereof, suspended and thoroughly dispersed in a liquid.Type: GrantFiled: July 23, 1998Date of Patent: June 20, 2000Assignee: Zeneca LimitedInventors: Herbert B. Scher, Jin Ling Chen
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Patent number: 6075131Abstract: Compounds of Formula (1) have utility as dyes for ink-jet printing where Formula (1) comprises:T.sub.q --W Formula (1)which includes all acceptable forms of such compounds selected from one or more of the following (including mixtures thereof and combinations thereof in the same species): stereoisomers, zwitterions, polymorphs, solvates, isotopic forms; and all suitable salts thereof; in which:q represents from 1 to 4 inclusive;W comprises an optionally substituted hydrocarbyl group (preferably an optionally substituted aromatic group, or an optionally substituted aliphatic group); andeach T independently comprises a group of the Formula (2):B--N.dbd.N--J--Y-- Formula (2)in which:B comprises an optionally substituted indanyl group;Y comprises a carbonyl group or a sulphonyl group; andJ comprises a group of Formula (3): ##STR1## in which: R.sup.Type: GrantFiled: October 13, 1999Date of Patent: June 13, 2000Assignee: Zeneca LimitedInventors: Neil Anthony Tallant, Paul Wight, Peter Gregory
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Patent number: 6075172Abstract: The present invention provides the novel chlorofluorohydrocarbon 1,1-difluoro-1,4-dichlorobutane, and a process for its preparation comprising reacting 1,1,1,4-tetrachlorobutane or 1,1,4-trichlorobut-1-ene with hydrogen fluoride in the liquid or vapor phase. The product has useful solvent properties and is also useful in synthetic chemistry for the introduction of fluorocarbon functionality.Type: GrantFiled: January 9, 1998Date of Patent: June 13, 2000Assignee: Zeneca LimitedInventors: Alfred Glyn Williams, Martin Charles Bowden, Stephen Martin Brown
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Patent number: 6072080Abstract: A process for the purification of a compound of general formula I: ##STR1## wherein R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, any of which may optionally be substituted with one or more substituents selected from halogen and hydroxy; or COOR.sup.4, COR.sup.6, CONR.sup.4 R.sup.5 or CONHSO.sub.2 R.sup.4 ;R.sup.4 and R.sup.5 independently represent hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted with one or more halogen atoms;R.sup.6 is a halogen atom or a group R.sup.4 ;R.sup.2 is hydrogen or halo; andR.sup.3 is C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.Type: GrantFiled: March 12, 1998Date of Patent: June 6, 2000Assignee: Zeneca LimitedInventors: Louie Akos Nady, Seyed Mehdi Tavana, Thomas Gray, Stephen Martin Brown, Brian David Gott
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Patent number: 6071856Abstract: This invention is directed to an herbicidal composition comprising,a) an herbicidally effective amount of acetochlor; andb) a non-phytotoxic antidotally effective amount of a compound according to formula (I), ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents one or more substituents selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkylamino, halo, halo(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy-(C.sub.1 -C.sub.6)alkyl and nitro;wherein A is selected from ##STR2## wherein each of R.sup.3 and R.sup.4 is independently selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halo(C.sub.1 -C.sub.6)alkyl, cyano(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy-(C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl, (C.sub.2 -C.sub.6)alkynyl, phenyl, nitrophenyl, benzyl, halobenzyl, pyridinyl(C.sub.1 -C.sub.6)alkyl and (C.sub.1 -C.sub.6)alkylammonium; and n is 0 or 1.Type: GrantFiled: March 4, 1997Date of Patent: June 6, 2000Assignee: Zeneca LimitedInventors: Don R. Baker, Richard L. Franz, Khosro Khodayari
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Patent number: 6071921Abstract: The invention relates to quinazoline derivatives of the formula: ##STR1## [wherein: Y.sup.1 represents --O--, --S--, --CH.sub.2 --, --SO--, --SO.sub.2 --, --NR.sup.5 CO--, --CONR.sup.6 --, --SO.sub.2 NR.sup.7 --, --NR.sup.8 SO.sub.2 -- or --NR.sup.9 -- (wherein R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 each independently represents hydrogen, alkyl or alkoxyalkyl);R.sup.1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino.R.sup.2 represents hydrogen, hydroxy, halogeno, alkyl, alkoxy, trifluoromethyl, cyano, amino or nitro;m is an integer from 1 to 5;R.sup.3 represents hydroxy, halogeno, alky, alkoxy, alkanoyloxy, trifluoromethyl, cyano, amino or nitro;R.sup.Type: GrantFiled: December 2, 1998Date of Patent: June 6, 2000Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
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Patent number: 6069210Abstract: A composition comprising a particulate solid and a dispersant which is a phosphate ester of a compound of formula 1: ##STR1## wherein Y is methoxy or H--(EO).sub.q, m and q are each independently from 5 to 50 and n is from 5 to 70. When Y is a methoxy, n is preferably 20 and m is preferably 10. When Y is H--(EO).sub.q, m and q are preferably 13 and n is preferably 30.Type: GrantFiled: November 4, 1998Date of Patent: May 30, 2000Assignee: Zeneca LimitedInventors: David John Cartridge, Dean Thetford
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Patent number: 6069145Abstract: The invention concerns a compound of formula (I) wherein: R.sup.1 is of the formula --NHC(.dbd.O)(1-4C)alkyl, --NHS(O).sub.n (1-4C)alkyl wherein n is 0, 1 or 2 or R.sup.1 is hydroxy; R.sup.2 and R.sup.3 are independently hydrogen or fluoro; R.sup.4 is hydrogen, methyl, ethyl or oxo; R.sup.5 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or of the formula R.sup.6 (CH.sub.2).sub.m -- wherein either m is 1-4 and R.sup.6 is, for example, trifluoromethyl, difluoromethyl, fluoromethyl, (1-4C)alkoxy, (1-4C)alkyl S(O).sub.p -- wherein p is 0, 1 or 2, (1-6C)alkanoyloxy, di-(N-(1-4C)alkyl)amino, N-((1-4C)alkyl)(1-4C)alkanoylamino, cyano, carboxy, (1-4C)alkoxycarbonyl, carbamoyl, di-(N-(1-4C)alkyl)carbamoyl, N-((1-4C)alkyl)(1-4C)alkanesulphonamido, N.sup.1 -((1-4C)alkyl)-di-(N.sup.3 -(1-4C)alkyl)ureido, or of the formula --OC(.dbd.O)NR.sup.7 (R.sup.8) or --N(R.sup.9)SO.sub.2 NR.sup.7 (R.sup.8) wherein R.sup.7 and R.sup.8 are independently hydrogen or (1-4C)alkyl and R.sup.9 is (1-4C)alkyl; or m is 2-4 and R.sup.Type: GrantFiled: July 27, 1998Date of Patent: May 30, 2000Assignee: Zeneca LimitedInventor: Michael John Betts
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Patent number: 6066780Abstract: The synthesis of lignin by plants is controlled by transformation of the plant genome with a recombinant gene construct which contains the gene specifying an enzyme critical to the synthesis of a lignin precursor, which gene may be in antisense orientation so that it is transcribed to mRNA having a sequence complementary to the equivalent mRNA transcribed from the endogenous gene thus leading to suppression of lignin synthesis. If the recombinant gene has the lignin enzyme gene in normal, or "sense" orientation, increased production of the enzyme may occur when the insert is the full length DNA but suppression may occur it only a partial sequence is employed.Type: GrantFiled: May 26, 1995Date of Patent: May 23, 2000Assignee: Zeneca LimitedInventors: Alain Michel Boudet, Dirk Gustaaf Inze, Wolfgang Walter Schuch
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Patent number: 6066456Abstract: The chemically-inducible 27 kD subunit of the enzyme glutathione-S-transferase, isoform II (GST-II-27) and sequences encoding it are provided. In particular, a genomic DNA sequence encoding the gene promoter for the GST-II-27 subunit is provided. Then linked to an exogenous gene and introduced into a plant by transformation, and GST-II-27 promoter provides a means for the external regulation of expression of that exogenous gene. Transformation with DNA encoding glutathione-S-transferase polypeptides produces herbicide resistance transgenic plants.Type: GrantFiled: March 26, 1998Date of Patent: May 23, 2000Assignee: Zeneca LimitedInventors: Ian George Bridges, Simon William Jonathan Bright, Andrew James Greenland, David Charles Holt, Ian Jepson, Wolfgang Walter Schuch
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Patent number: 6066646Abstract: A compound of formula (I):P--R.sup.2 --Q (I)where each of P and Q is, independently, a group of formula (B): ##STR1## wherein J is a bidentate group of formula --CH.sub.2 --X--CH.sub.2 -- (wherein X is methylene, sulfur or oxygen), X'C.dbd.CY or X'WC--CYZ (wherein X', W, Y and Z are independently hydrogen, hydroxy, acyloxy, alkoxy, alkylsilyloxy or halogen); R.sup.1 is an optionally substituted phenyl or 5-or 6-membered heterocyclic ring system containing from 1 to 3 heteroatoms individually selected from nitrogen, oxygen and sulfur atoms, and at least one unsaturation (double bond) between adjacent atoms in the ring, said heterocyclic ring being optionally fused to a benzene ring, wherein the substutuents, if present, are selected from halogen atoms, cyano, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkenyl, alkylthio and alkyl amino groups, any of which groups contain up to six carbon atoms; R.sup.Type: GrantFiled: February 12, 1999Date of Patent: May 23, 2000Assignee: Zeneca LimitedInventors: Nigel Douglas Bishop, Christopher John Urch, Terence Lewis, Raymond Leo Sunley, Roger Salmon, Christopher Richard Ayles Godfrey
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Patent number: 6063605Abstract: Novel strains of the insecticidal microorganism Bacillus thurinaiensis are described. These contain novel genes, and in particular a gene coding for a novel insecticidal endotoxin, 81 kilodaltons in length, toxic to both Lepidoptera and Coleoptera. The novel strains and the genes they contain may be used to combat insect attack against plants.Type: GrantFiled: August 5, 1994Date of Patent: May 16, 2000Assignee: Zeneca LimitedInventors: Susan Ely, Ravindra Haribhai Tailor, Janet Mary Tippett, Bruce Marvin Held, Robert Gerard Blenk, deceased
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Patent number: 6059870Abstract: An ink composition comprising a water-soluble reactive dye comprising at least three chromophoric groups linked to a polyamine; and 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).Type: GrantFiled: October 23, 1998Date of Patent: May 9, 2000Assignee: Zeneca LimitedInventors: John Anthony Taylor, Peter Gregory
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Patent number: 6060475Abstract: The invention concerns pharmaceutically useful compounds of the formula I, in which A.sup.1, A.sup.2, A.sup.3, A.sup.4, B.sup.1, m, Ar, W, X, Y, Z and R.sup.1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, 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.Type: GrantFiled: December 14, 1998Date of Patent: May 9, 2000Assignee: Zeneca LimitedInventors: Robert Hugh Bradbury, Roger John Butlin, Roger James
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Patent number: 6057345Abstract: Compounds of the formula, ##STR1## and pharmaceutically-acceptable salts thereof, which are useful as antagonists of the pain-enhancing effects of E-type prostaglandins, processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods for treating pain comprising the administration of such compounds.Type: GrantFiled: October 30, 1998Date of Patent: May 2, 2000Assignee: Zeneca LimitedInventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 6054613Abstract: A process for the preparation of a sulfonamide of formula:RSO.sub.2 NR.sup.1 R.sup.2wherein R represents C.sub.1 -C.sub.10 alkyl; andR.sup.1 and R.sup.2 independently represent hydrogen, C.sub.1 -C.sub.10 alkyl or C.sub.6 -C.sub.10 aryl; which comprises reacting the corresponding alkane- or arenesulfonyl halide of formula:RSO.sub.2 Halwherein Hal represents halogen; with the corresponding compound of formula:NHR.sup.1 R.sup.2in an aqueous solvent and extracting the sulfonamide from the resulting mixture into a polar organic solvent.Type: GrantFiled: May 24, 1999Date of Patent: April 25, 2000Assignee: Zeneca LimitedInventors: Brian David Gott, James Peter Muxworthy, Stephen Martin Brown
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Patent number: 6054593Abstract: The present invention relates to particular forms of a novel 1-substituted-N-[2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxam ide 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 pharmaceutical compositions containing such forms, processes for preparing the forms and intermediates useful in the synthesis of the forms.Type: GrantFiled: June 19, 1998Date of Patent: April 25, 2000Assignee: Zeneca LimitedInventors: Chris Allan Veale, Peter Robert Bernstein, Elwyn Peter Davies
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Patent number: 6054282Abstract: A method for the detection of a compound which modulates binding of a ligand to a biological receptor, which method comprises contacting the ligand, biological receptor and test compound at a locus on a solid phase matrix, the matrix allowing movement of fluids therein by capillary action, under conditions which permit binding of the ligand to the biological receptor and partition of any unbound ligand on the solid phase matrix, and detecting any modulation of binding by the test compound by reference to any such partition.Type: GrantFiled: February 14, 1996Date of Patent: April 25, 2000Assignee: Zeneca LimitedInventor: Andrew John Garman