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).

  • Publication number: 20030199513
    Abstract: The invention relates to the use of cinnoline derivatives of formula (I) 1
    Type: Application
    Filed: December 5, 2002
    Publication date: October 23, 2003
    Applicant: ZENECA LIMITED
    Inventors: Andrew Peter Thomas, Laurent Francois Andre Hennequin
  • Publication number: 20030191308
    Abstract: 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 f
    Type: Application
    Filed: October 3, 2002
    Publication date: October 9, 2003
    Inventors: Laurent Francois Andre Hennequin, Elaine Sophie Elizabeth Stokes
  • Patent number: 6514971
    Abstract: 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: Grant
    Filed: April 13, 1999
    Date of Patent: February 4, 2003
    Assignees: Zeneca Limited, Zeneca Pharma S.A.
    Inventors: Andrew Peter Thomas, Laurent Francois Andre Hennequin
  • Publication number: 20020173646
    Abstract: 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 co
    Type: Application
    Filed: February 25, 2002
    Publication date: November 21, 2002
    Applicant: ZENECA LIMITED
    Inventors: Andrew Peter Thomas, Craig Johnstone, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
  • Patent number: 6436691
    Abstract: 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: Grant
    Filed: February 13, 1998
    Date of Patent: August 20, 2002
    Assignee: Zeneca Limited
    Inventors: Anthony Michael Slater, David Charles Blakey, David Huw Davies, John Frederick Hennam, Laurent Francois Andre Hennequin, Peter Robert Marsham, Robert Ian Dowell
  • Patent number: 6414148
    Abstract: 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 alky
    Type: Grant
    Filed: March 25, 1999
    Date of Patent: July 2, 2002
    Assignees: 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
  • Patent number: 6362336
    Abstract: 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: Grant
    Filed: June 11, 2001
    Date of Patent: March 26, 2002
    Assignees: Zeneca Limited, Zeneca Pharma S. A.
    Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
  • Publication number: 20020032208
    Abstract: The invention relates to quinazoline derivatives of the formula: 1
    Type: Application
    Filed: June 11, 2001
    Publication date: March 14, 2002
    Applicant: ZENECA LIMITED
    Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
  • Patent number: 6294532
    Abstract: 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: Grant
    Filed: May 3, 2000
    Date of Patent: September 25, 2001
    Assignee: Zeneca Limited
    Inventors: Andrew Peter Thomas, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Patrick Ple
  • Patent number: 6291455
    Abstract: 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 p
    Type: Grant
    Filed: September 8, 1998
    Date of Patent: September 18, 2001
    Assignees: Zeneca Limited, Zeneca Pharma S.A.
    Inventors: Andrew Peter Thomas, Craig Johnstone, Laurent Francois Andre Hennequin
  • Patent number: 6265411
    Abstract: 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 hydr
    Type: Grant
    Filed: November 6, 1998
    Date of Patent: July 24, 2001
    Assignee: Zeneca Limited
    Inventors: Andrew Peter Thomas, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Patrick Ple
  • Patent number: 6258951
    Abstract: 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: Grant
    Filed: February 9, 2000
    Date of Patent: July 10, 2001
    Assignees: Zeneca Limited, Zeneca Pharma S.A.
    Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
  • Patent number: 6184225
    Abstract: 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 al
    Type: Grant
    Filed: August 13, 1998
    Date of Patent: February 6, 2001
    Assignee: Zeneca Limited
    Inventors: Andrew Peter Thomas, Craig Johnstone, Laurent Francois Andre Hennequin
  • Patent number: 6071921
    Abstract: 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: Grant
    Filed: December 2, 1998
    Date of Patent: June 6, 2000
    Assignees: Zeneca Limited, Zeneca Pharma S.A.
    Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
  • Patent number: 5985281
    Abstract: 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: Grant
    Filed: June 23, 1997
    Date of Patent: November 16, 1999
    Assignee: Zeneca Limited
    Inventors: 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
  • Patent number: 5962458
    Abstract: 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: Grant
    Filed: December 17, 1996
    Date of Patent: October 5, 1999
    Assignees: Zeneca Limited, Zeneca Pharma S.A.,
    Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
  • Patent number: 5747499
    Abstract: 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: Grant
    Filed: October 29, 1996
    Date of Patent: May 5, 1998
    Assignee: British Technology Group Limited
    Inventors: Vassilios Bavetsias, Francis Thomas Boyle, Laurent Francois Andre Hennequin, Jonathan Hugh Marriott