Patents by Inventor Francisco Javier Fernández-Gadea

Francisco Javier Fernández-Gadea 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).

  • Patent number: 6511976
    Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.
    Type: Grant
    Filed: April 6, 2000
    Date of Patent: January 28, 2003
    Assignee: Jannsen Pharmaceutica, N.V.
    Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Pilar Gil-Lopetegui, Adolfo Díaz-Martinez
  • Patent number: 6403805
    Abstract: The present invention describes compounds useful for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the formula the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof.
    Type: Grant
    Filed: July 27, 1999
    Date of Patent: June 11, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eddy Jean Edgard Freyne, Gaston Stanislas Marcella Diels, José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea
  • Publication number: 20020068830
    Abstract: The present invention describes the use of compounds for the manufacture of a medicament for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the formula 1
    Type: Application
    Filed: July 27, 1999
    Publication date: June 6, 2002
    Inventors: EDDY JEAN EDGARD FREYNE, GASTON STANISLAS MARCELLA DIELS, JOSE IGNACIO ANDRES-GIL, FRANCISCO JAVIER FERNANDEZ-GADEA
  • Patent number: 6288058
    Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: September 11, 2001
    Assignee: Janssen Pharmceutica N.V.
    Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernández-Gadea, Theo Frans Meert
  • Patent number: 6194405
    Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3
    Type: Grant
    Filed: March 22, 2000
    Date of Patent: February 27, 2001
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernández-Gadea, Theo Frans Meert
  • Patent number: 6156747
    Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero to 6; p is zero to 3; q is zero to 3; r is zero to 3; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl or C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or trihalomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: December 5, 2000
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jose Ignacio Andres-Gil, Pedro Martinez-Jimenez, Francisco Javier Fernandez-Gadea, Victor Karel Sipido
  • Patent number: 6057441
    Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: May 2, 2000
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
  • Patent number: 6051718
    Abstract: The present invention concerns 2-cyanoiminoimidazole derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; 6,7-dihydro-5H-cyclopentapyridinyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-6 alkyloxy; R.sup.4 is hydrogen; halo; C.sub.1-6 alkyl; trifluoromethyl; C.sub.3-6 cycloalkyl; carboxyl; C.sub.1-4 alkyloxycarbonyl; C.sub.3-6 cycloalkylaminocarbonyl; aryl; Het.sup.1 ; or substituted C.sub.1-6 alkyl; or R.sup.4 is --O--R.sup.7 or --NH--R.sup.8 ; R.sup.5 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.
    Type: Grant
    Filed: March 19, 1999
    Date of Patent: April 18, 2000
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Eddy Jean Edgard Freyne, Francisco Javier Fernandez-Gadea, Jose Ignacio Andres-Gil
  • Patent number: 5994376
    Abstract: The present invention describes 1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one compounds and their use for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases.
    Type: Grant
    Filed: September 29, 1997
    Date of Patent: November 30, 1999
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Eddy Jean Edgard Freyne, Gaston Stanislas Marcella Diels, Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea
  • Patent number: 5990123
    Abstract: The present invention is concerned with compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein .dbd.a.sub.1 --a.sub.2 .dbd.a.sub.3 --a.sub.4 .dbd. is a bivalent radical of formula .dbd.N--CH.dbd.CH--CH.dbd. (a), .dbd.CH--N.dbd.CH--CH.dbd. (b), .dbd.CH--CH.dbd.N--CH.dbd. (c), .dbd.CH--CH.dbd.CH--N.dbd. (d), wherein one or two hydrogen atoms can be substituted by halo, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is C.sub.1-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a five- or six-membered heterocyclic ring containing at least one nitrogen atom or a radical of formula --C(NR.sup.5 R.sup.6).dbd.C--R.sup.4 wherein R.sup.4 is hydrogen, cyano, aminocarbonyl or C.sub.1-6 alkyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.
    Type: Grant
    Filed: August 6, 1997
    Date of Patent: November 23, 1999
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Guy Rosalia Eugene Van Lommen, Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea, Maria Encarnacion Matesanz-Ballesteros
  • Patent number: 5952510
    Abstract: The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6 or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo?2.2.1!-2-heptenyl; bicyclo?2.2.1!heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-6 alkyloxy; R.sup.4 is hydrogen; cyano; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkyloxycarbonyl or aryl; R.sup.5 is hydrogen; cyano; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkyloxycarbonyl or aryl; Y is a direct bond or C.sub.1-3 alkanediyl; --A--B-- is a bivalent radical of formula --CR.sup.6 .dbd.CR.sup.7 -- or --CHR.sup.6 --CHR.sup.7 --; L is hydrogen; optionally substituted C.sub.
    Type: Grant
    Filed: September 30, 1997
    Date of Patent: September 14, 1999
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Eddy Jean Edgard Freyne, Gaston Stanislas Marcella Diels, Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea
  • Patent number: 5869515
    Abstract: The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo?2.2.1!-2-heptenyl; bicyclo?2.2.1!heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R3 is hydrogen, halo or C.sub.1-6 alkyloxy ##STR2## is a bivalent radical of formula ##STR3## Alk is C1-4alkanediyl; --A--B-- is a bivalent radical of formula: --CR.sup.6 .dbd.CR.sup.7 -- or --CHR.sup.6 --CHR.sup.7 --; L is hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; optionally substituted C.sub.3-6 alkenyl; optionally substituted piperidinyl; C.sub.
    Type: Grant
    Filed: September 29, 1997
    Date of Patent: February 9, 1999
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eddy Jean Edgard Freyne, Gaston Stanislas Marcella Diels, Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea
  • Patent number: 5773433
    Abstract: This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. ##STR1## wherein: R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; C.sub.1-6 alkyl substituted with hydroxy, C.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkyloxycarbonyl or aryl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R.sup.3 to R.sup.10 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; R.sup.11 is hydrogen, C.sub.1-6 alkyl, or trifluoromethyl; R.sup.12 is hydrogen, C.
    Type: Grant
    Filed: April 25, 1997
    Date of Patent: June 30, 1998
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Francisco Javier Fernandez-Gadea, Victor Karel Sipido, Jose Ignacio Andres-Gil, Theo Frans Meert
  • Patent number: 5691344
    Abstract: The present invention is concerned with compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, the N-oxides thereof and the stereochemically isomeric forms thereof, wherein .dbd.a.sub.1 --a.sub.2 .dbd.a.sub.3 --a.sub.4 .dbd. is a bivalent radical of formula:.dbd.N--CH.dbd.CH--CH.dbd. (a),.dbd.CH--N.dbd.CH--CH.dbd. (b),.dbd.CH--CH.dbd.N--CH.dbd. (c),.dbd.CH--CH.dbd.CH--N.dbd. (d),wherein in said bivalent radicals one or two hydrogen atoms can be substituted by halo, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is C.sub.1-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a five- or six-membered heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## wherein R.sup.4 is hydrogen, cyano, aminocarbonyl or C.sub.1-6 alkyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.
    Type: Grant
    Filed: January 24, 1996
    Date of Patent: November 25, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Guy Rosalia Eugene Van Lommen, Francisco Javier Fernandez-Gadea, Jose Ignacio Andres-Gil, Maria Encarnacion Matesanz-Ballesteros