Patents by Inventor Laurent François André Hennequin
Laurent François André Hennequin has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Publication number: 20030199513Abstract: The invention relates to the use of cinnoline derivatives of formula (I) 1Type: ApplicationFiled: December 5, 2002Publication date: October 23, 2003Applicant: ZENECA LIMITEDInventors: Andrew Peter Thomas, Laurent Francois Andre Hennequin
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Publication number: 20030191308Abstract: The invention concerns compounds of the formula (I) wherein ring A is phenyl or 5- or 6-membered heterocyclic ring as defined herein; Z is —O—, —NH— or —S—; m is an integer from 0 to 5 inclusive; R1 is hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, (C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, are hydrogen or C1-3alkyl); R2 is hydrogen, hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, trifluoromethyl, amino or nitro; R3 is hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; provided that when ring A is a 5- or 6-memberecl heterocyclic ring, at least one R3 is either hydroxy or halogeno; X1 is —O—, —CH2—, —S—, —SO—, —SO2—, —NR7—, —NR7CO—, —CONR7, —SO2NR7— or —NR7SO2—, (wherein R7 is hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); and R4 is selected fType: ApplicationFiled: October 3, 2002Publication date: October 9, 2003Inventors: Laurent Francois Andre Hennequin, Elaine Sophie Elizabeth Stokes
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Patent number: 6514971Abstract: The invention relates to the use of cinnoline derivatives of formula (I) wherein Z represents —O—, —NH—, —S— or —CH2—; m is a n integer from 1 to 5; R1 represents hydrogen, hydroxy, halogeno, nitro, cyano, trifluoromethyl, Cp1-3alkyl, C1-3alkoxy, C1-3alkylthio or NR6R7 (wherein R6 and R7, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, auoro, chioro, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; R4 represents hydrogen, hydroxy, halogeno, cyano, nitro, amino, trifluoromethyl, C1-3alkyl or a group R5—X1 (wherein X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR8CO—, —CONR9—, —SO2NR10—, —NR11SO2— or NR12— (wherein R8, R9, R10, R11 and R12 each independently represents hydrogen, C1-Type: GrantFiled: April 13, 1999Date of Patent: February 4, 2003Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Andrew Peter Thomas, Laurent Francois Andre Hennequin
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Publication number: 20020173646Abstract: The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-13 alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—-, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3 alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may coType: ApplicationFiled: February 25, 2002Publication date: November 21, 2002Applicant: ZENECA LIMITEDInventors: Andrew Peter Thomas, Craig Johnstone, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Patent number: 6436691Abstract: Antibody Directed Enzyme Prodrug Therapy (ADEPT) systems for use in cancer based on mutated carboxypeptidase B (CPB) enzymes. Enzyme conjugates for ADEPT are substantially non-immunogenic in humans comprising a targeting moiety (for example an antibody) capable of binding with a tumor associated antigen, the targeting moiety being linked to a mutated form of a CPB enzyme capable of converting a prodrug into an antineoplastic drug wherein the prodrug is not significantly convertible into antineoplastic drug in humans by natural unmutated enzyme. A preferred enzyme mutant is human pancreatic CPB comprising a Lys or Arg residue at position 253. Suitable mustard prodrugs are disclosed in the specification.Type: GrantFiled: February 13, 1998Date of Patent: August 20, 2002Assignee: Zeneca LimitedInventors: Anthony Michael Slater, David Charles Blakey, David Huw Davies, John Frederick Hennam, Laurent Francois Andre Hennequin, Peter Robert Marsham, Robert Ian Dowell
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Patent number: 6414148Abstract: The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyType: GrantFiled: March 25, 1999Date of Patent: July 2, 2002Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Andrew Peter Thomas, Craig Johnstone, Edward Clayton, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Patent number: 6362336Abstract: The invention relates to quinazoline derivatives of the formula: [wherein: Y1 represents —O—, —S—, —CH2—, —SO—, —SO2—, —NR5CO—, —CONR6—, —SO2NR7—, —NR8SO2— or —NR9— (wherein R5, R6, R8 and R9 each independently represents hydrogen, alkyl or alkoxyalkyl); R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino.Type: GrantFiled: June 11, 2001Date of Patent: March 26, 2002Assignees: Zeneca Limited, Zeneca Pharma S. A.Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
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Publication number: 20020032208Abstract: The invention relates to quinazoline derivatives of the formula: 1Type: ApplicationFiled: June 11, 2001Publication date: March 14, 2002Applicant: ZENECA LIMITEDInventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
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Patent number: 6294532Abstract: The invention relates to compounds of formula (I) and salts thereof as further defined herein, wherein ring Z is a 6-membered heterocyclic ring containing 1 to 3 nitrogen atoms, and the use of such compounds and salts to inhibit the effects of VEGF and FGF, and in the treatment of a number of disease states including cancer and rheumatoid arthritis.Type: GrantFiled: May 3, 2000Date of Patent: September 25, 2001Assignee: Zeneca LimitedInventors: Andrew Peter Thomas, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Patrick Ple
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Patent number: 6291455Abstract: The invention relates to quinazoline derivatives of formula (I) (wherein: R1 represents hydrogen or methoxy; R2 represents methoxy, ethoxy, 2-methoxyethoxy, 3-methoxypropoxy, 2-ethoxyethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, 2-hydroxyethoxy, 3-hydroxypropoxy, 2-(N,N-dimethylamino)ethoxy, 3-(N,N-dimethylamino)propoxy, 2-morpholinoethoxy, 3-morpholinopropoxy, 4-morpholinobutoxy, 2-piperidinoethoxy, 3-piperidinopropoxy, 4-piperidinobutoxy, 2-(piperazin-1-yl)ethoxy, 3-(piperazin-1-yl)propoxy, 4-(piperazin-1-yl)butoxy, 2-(4-methylpiperazin-1-yl)ethoxy, 3-(4methylpiperazin-1-yl)propoxy or 4-(4-methylpiperazin-1-yl)butoxy; the phenyl group bearing (R3)2 is selected from: 2-fluoro-5-hydroxyphenyl, 4-bromo-2-fluorophenyl, 2,4-difluorophenyl, 4-chloro-2-fluorophenyl, 2-fluoro-4-methylphenyl, 2-fluoro-4-methoxyphenyl, 4-bromo-3-hydroxyphenyl, 4-fluoro-3-hydroxyphenyl, 4-chloro-3-hydroxyphenyl, 3-hydroxy-4-methylphenyl, 3-hydroxy-4-methoxyphenyl and 4-cyano-2-fluorophenyl); and salts thereof, processes for their pType: GrantFiled: September 8, 1998Date of Patent: September 18, 2001Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Andrew Peter Thomas, Craig Johnstone, Laurent Francois Andre Hennequin
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Patent number: 6265411Abstract: The invention relates to compounds of formula (I), wherein: R2 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino, nitro, C2-4alkanoyl, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylthio, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, {overscore (N)}—C1-4alkylcarbamoyl, {overscore (N)},{overscore (N)}-di(C1-4alkyl)carbamoyl, aminosulphonyl, {overscore (N)}—C1-4alkylaminosulphonyl, {overscore (N)},{overscore (N)}-di(C1-4alkyl)aminosulphonyl, C1-4alkylsulphonylamino, or a group R4X1 wherein X1 represents a direct bond, C2-4alkanoyl, —CONR5R6—, —SO2NR7R8— or —SO2R9— (wherein R5 and R7, each independently represents hydrogen or C1-2alkyl and R6, R8 and R9 each independently represents C1-4alkyl and wherein R4 is linked to R6, R8 or R9) and R4 represents an optionally substituted group selected from phenyl and a 5 or 6-membered heterocyclic group; n is an integer from 0 to 4, R1 represents hydrType: GrantFiled: November 6, 1998Date of Patent: July 24, 2001Assignee: Zeneca LimitedInventors: Andrew Peter Thomas, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Patrick Ple
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Patent number: 6258951Abstract: The invention relates to quinazoline derivatives of the formula: and salts thereof; processes for their preparation and pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.Type: GrantFiled: February 9, 2000Date of Patent: July 10, 2001Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
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Patent number: 6184225Abstract: The invention relates to quinazoline derivatives of formula (I) wherein: Z represents —O—, —NH— or —S—; m is an integer from 1 to 5; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluorometlyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio or NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino, or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, SO2—, —NR6—, NR8CO—, —CONR9—SO2NR10— or —NR11SO2—, (wherein R7, R8, R9, R10 and R11 each represents C1-3alkyl, C1-3alkoxyC2-3alkyl); R4 represents a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alType: GrantFiled: August 13, 1998Date of Patent: February 6, 2001Assignee: Zeneca LimitedInventors: Andrew Peter Thomas, Craig Johnstone, Laurent Francois Andre Hennequin
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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: 5985281Abstract: A two component system for therapeutic treatment of a host, having a first component comprising a targeting moiety capable of binding with a tumour associated antigen, linked to a mutated enzyme capable of converting a prodrug into an antineoplastic drug, and a second component comprising a prodrug convertible under the influence of the mutated enzyme to the antineoplastic drug. The mutated enzyme is a mutated form of a natural host enzyme which recognizes its natural substrate by an ion pair interaction with the substrate, wherein the mutated enzyme and prodrug have structures such that the polarity of the mutated enzyme/prodrug ion pair interaction is reversed relative to the natural host enzyme/natural substrate ion pair interaction. The first component is substantially non-immunogenic in the host and the prodrug second component is not significantly convertible into antineoplastic drug in the host by natural unmutated host enzyme.Type: GrantFiled: June 23, 1997Date of Patent: November 16, 1999Assignee: Zeneca LimitedInventors: Christopher John Taylorson, Hendrikus Johannes Eggelte, Antonio Tarragona-Fiol, Brian Robert Rabin, Francis Thomas Boyle, John Frederick Hennam, David Charles Blakey, Peter Robert Marsham, David William Heaton, David Huw Davies, Anthony Michael Slater, Laurent Francois Andre Hennequin
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Patent number: 5962458Abstract: 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, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, cyano, amino or nitro;R.sup.Type: GrantFiled: December 17, 1996Date of Patent: October 5, 1999Assignees: Zeneca Limited, Zeneca Pharma S.A.,Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
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Patent number: 5747499Abstract: Cyclopentaquinazoline of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, amino, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 hydroxyalkyl or C.sub.1-4 fluoroalkyl;wherein R.sup.2 is hydrogen, C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-4 alkynyl, C.sub.2-4 hydroxyalkyl, C.sub.2-4 halogenoalkyl or C.sub.1-4 cyanoalkyl;Ar.sup.1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; andwherein R.sup.3 is a group of the formula:--A.sup.1 --Ar.sup.2 --A.sup.2 --Y.sup.1in which A.sup.1, A.sub.2, Y.sup.1 and Ar.sub.2 are defined in claim 1;or a pharmaceutically acceptable salt or ester there of are of therapeutic value particularly in the treatment of cancer.Type: GrantFiled: October 29, 1996Date of Patent: May 5, 1998Assignee: British Technology Group LimitedInventors: Vassilios Bavetsias, Francis Thomas Boyle, Laurent Francois Andre Hennequin, Jonathan Hugh Marriott