Patents Represented by Attorney, Agent or Law Firm Ellen Ciambrone Coletti
  • Patent number: 7166601
    Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.
    Type: Grant
    Filed: April 26, 2006
    Date of Patent: January 23, 2007
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Sigmond G. Johnson, Ralph A. Rivero
  • Patent number: 6967199
    Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.
    Type: Grant
    Filed: November 8, 2002
    Date of Patent: November 22, 2005
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Sigmond G. Johnson, Ralph A. Rivero
  • Patent number: 6908908
    Abstract: The invention is directed to 4h-benzo[1,4]oxazin-3-ones useful as peroxisome proliferator activated receptor gamma (PPAR?) agonists or antagonists. Pharmaceutical compositions comprising compounds of the present invention and methods of treating conditions such as NIDDM and obesity are also disclosed.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: June 21, 2005
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Thomas P. Burris, Donald W. Combs, Philip J. Rybczynski, Joseph Dudash, Jr.
  • Patent number: 6743792
    Abstract: The present invention is concerned with the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p represents 0, 1, 2 or 3; q represents 0, 1, 2, 3 or 4; R1 represents hydrogen, C1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, mercapto, C1-6alkylthio, C3-7cycloalkyl, aryl or C1-6alkyl substituted with mono- or di(C1-6alkyl)-amino, C1-6alkyloxy, aryl or Het; R2 represents cyano or a radical of formula —C(═X)—Y—R5; wherein X represents O or S; Y represents O, S, NR6 or a direct bond; R5 represents hydrogen; C3-7cycloalkyl; aryl or optionally substituted C1-6alkyl; and where Y is a direct bond, R5 may also be halo or Het; R3 and R4 each independently represents halo, haloC1-6alkyl, C1-6alkyl, hydroxy, C1-6alkyloxy, C1-6alkylcarbonyloxy, mercapto, C1-6alkylthio, C1-6alkylsulfonyl, C1-6alkylsulfinyl, haloC1-6alkylsulfonyl, aryl, cyano, nitro, amino, mono- and di(C1-6alkyl)amino o
    Type: Grant
    Filed: May 14, 2001
    Date of Patent: June 1, 2004
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eddy Jean Edgard Freyne, Gustaaf Maria Boeckx, Jean Pierre Frans Van Wauwe, Gaston Stanislas Marcella Diels
  • Patent number: 6562867
    Abstract: This invention is directed to a method for preventing or treating bipolar disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1 and R2 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).
    Type: Grant
    Filed: February 21, 2002
    Date of Patent: May 13, 2003
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Carlos R. Plata-Salaman, Boyu Zhao, Roy E. Twyman, Yong Moon Choi, Robert Gordon
  • Patent number: 6476018
    Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula —X—COOR5, —X—CONR6R7 or —X—COR10 wherein —X— is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is —CH2—, —CH2—CH2—, —CH═CH—, —CHOH—CH2&mdas
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: November 5, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Francois Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux
  • Patent number: 6451802
    Abstract: The present invention relates to compounds of formula (I) the N-oxides, the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts, wherein n is 1 or 2, R1 is hydrogen, C1-6alkyl or halo; R2 is hydrogen or halo; R3 is C1-8alkyl or C3-6cycloalkyl; Hetis an optionally substituted triazole, imidazole, or thiazole; and —A—B— is a bivalent radical of formula —CH═CH—, —N═CH—, —CH═N—, wherein optionally one of the hydrogen atoms is replaced by C1-4alkyl; having apolipoprotein B inhibiting activity and concomitant lipid lowering activity.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: September 17, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Cornelus Gerardus Maria Janssen, Peter Walter Maria Roevens, Jozef Bertha August Thijssen
  • Patent number: 6452013
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyl-oxy; R2 is hydrogen, C1-6alkyl C1-6alkyloxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, -Alk-Y—C(═O)—R9, or -Alk-Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 an
    Type: Grant
    Filed: January 5, 2000
    Date of Patent: September 17, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
  • Patent number: 6440440
    Abstract: This invention concerns compounds of formula. stereochemically isomeric forms thereof, acid or base addition salts thereof, N-oxides thereof, or quaternary ammonium derivatives thereof, wherein the dotted line is an optional bond; X is a direct bond when the dotted line represents a bond, or X is hydrogen or hydroxy, when the dotted line does not represent a bond; R1, R2, R5 and R6 are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, —SO3H, and the like; R3 and R4 are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, nitro, amino, cyano, trifluoromethyl, or trifluoromethoxy; L is a radical of formula wherein A1 is a direct bond or C1-6alkanediyl; A2 is C2-6alkanediyl; and R7 to R11 are hydrogen, C1-6alkyl, aminoC1-6alkyl and the like; having biocidal properties; their preparation, compositions containing them and their use as a biocide.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: August 27, 2002
    Inventors: Lieven Meerpoel, Mark Arthur Josepha Van der Flaas, Louis Jozef Elisabeth Van Der Veken, Jan Heeres
  • Patent number: 6413988
    Abstract: The present invention is concerned with the an oral aqueous solution comprising prucalopride or pharmaceutically acceptable acid addition salts thereof having good organoleptic properties.
    Type: Grant
    Filed: October 26, 2001
    Date of Patent: July 2, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventor: Eddy André Josée De Proost
  • Patent number: 6403589
    Abstract: This invention concerns the use of nucleoside transport inhibitors, more particularly compounds of formula an N-oxide form, a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein R1 is C1-4alkyl, aminocarbonyl or mono- or di(C1-4alkyl)aminocarbonyl, Ar is a phenyl or pyridinyl derivative and L is a radical of formula wherein Ar1 is a phenyl derivative; Ar2 is a phenyl or pyridinyl derivative; and Alk is C1-4alkanediyl; for the manufacture of a medicine for the treatment of warm-blooded animals suffering from pain.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: June 11, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Theo Frans Meert, Herman Van Belle
  • Patent number: 6384031
    Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
    Type: Grant
    Filed: March 9, 2001
    Date of Patent: May 7, 2002
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Robert H. Chen, Min A. Xiang
  • Patent number: 6384233
    Abstract: A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III which is reacted with a compound of formula IV to form a compound of V and reacting with an alcohol to form the corresponding ester of formula VI and reacting the ester with N-methylhydroxylamine.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: May 7, 2002
    Inventors: Ahmed F. Abdel-Magid, Bruce D. Harris, Cynthia A. Maryanoff
  • Patent number: 6372246
    Abstract: The invention relates to a substrate coating for the electrostatic deposition of dry powder medicaments for use in the manufacture of pharmaceutical dosage forms comprising micronized polyethylene glycol (PEG), with A molecular weight in the range of 1,000 to 20,000, and having a particle size of 1-100 &mgr;m. The invention also relates to pharmaceutical compositions having such a substrate coating, and processes for manufacturing such pharmaceutical compositions. The invention also relates to the technology of reversing negative charge of medicaments so that they can be electrostatically deposited on a negatively charged substrate.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: April 16, 2002
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Shifeng Bill Wei, Herling Uang
  • Patent number: 6310077
    Abstract: The present invention is concerned with a novel benzamide of formula (I). Pharmaceutical compositions comprising said novel compounds, process for preparing compounds and compositions, and the use thereof as a medicine, in particular in the treatment of conditions involving a decreased motility of the intestine are described.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: October 30, 2001
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Jean-Paul René Marie André Bosmans, Joannes Adrianus Jacobus Schuurkes
  • Patent number: 6291481
    Abstract: Compounds of formula I the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the substituents are as described in the specification, and process for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
    Type: Grant
    Filed: August 27, 1998
    Date of Patent: September 18, 2001
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jean-Paul René Marie Bosmans, Christopher John Love, Marc Gustaaf Celine Verdonck, Joannes Adrianus Jacobus Schuurkes
  • Patent number: 6274599
    Abstract: The present invention concerns extended release formulations comprising cisapride-(L)-tartrate, in particular an oral formulation, the use thereof as a medicine, especially in treating gastrokinetic disorders.
    Type: Grant
    Filed: October 18, 1999
    Date of Patent: August 14, 2001
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eugene Marie Jozef Jans, Paul Marie Victor Gilis
  • Patent number: 6258956
    Abstract: A process for the synthesis of a compound of the formula wherein R1 is aryl, heteroaryl, substituted aryl or substituted heteroaryl and R2 is hydrogen, alkyl or aralkyl, or salt thereof.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: July 10, 2001
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Ahmed F. Abdel-Magid, Judith H. Cohen, Cynthia A. Maryanoff, Frank John Villani, Jr., Hua M. Zhong
  • Patent number: 6235745
    Abstract: The present invention is concerned with the use of 5HT3 antagonists for promoting intestinal lavage, especially in combination with an osmotic agent.
    Type: Grant
    Filed: October 15, 1999
    Date of Patent: May 22, 2001
    Assignee: Janssen Pharmaceutica N.V.
    Inventor: Antonius A. H. P. Megens
  • Patent number: 6224905
    Abstract: A method for preparing solid rapidly disintegrating dosage forms shaped as biconvex tablets having symmetrical top and bottom surfaces and dosage forms obtainable thereby.
    Type: Grant
    Filed: December 3, 1998
    Date of Patent: May 1, 2001
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Janice Lawrence, Gary Posage