Patents Assigned to Ortho-McNeil Pharmaceutical, Inc.
  • Polynucleotide and polypeptide sequences of Canine Cathepsin S
    Patent number: 6780985
    Abstract: DNAs encoding canine Cathepsin S have been cloned and characterized. The recombinant protein is capable of forming biologically active protein. The cDNA's have been expressed in recombinant host cells that produce active recombinant protein. The recombinant protein is also purified from the recombinant host cells. In addition, the recombinant host cells are utilized to establish a method for identifying modulators of the receptor activity, and receptor modulators are identified.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: August 24, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Robin Thurmond, Lars Karlsson, Sherry Baker
  • Phthalimido arylpiperazines useful in the treatment of benign prostatic hyperplasia
    Patent number: 6780994
    Abstract: This invention relates to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.
    Type: Grant
    Filed: July 29, 2002
    Date of Patent: August 24, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Gee-Hong Kuo, William V. Murray, Catherine P. Prouty
  • Ligand binding assays for vanilloid receptors
    Patent number: 6780650
    Abstract: The present invention describes an assay in which pH alters RTX affinity to VR1 receptors. The RTX affinity was increased with increasing pH from 4.1 to 8.6. Both the RTX affinity and apparent number of RTX binding sites were decreased with increasing pH from 8.6 to 10.6. The high pH may be causing the cell membranes to denature. These pH conditions (pH 8.0 to pH 9.0) provide a high signal to noise ratio, give a more robust assay and require use of less experimental materials.
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: August 24, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Sui-Po Zhang, Ellen E. Codd
  • 1,3,8-Triazaspiro[4.5]decan-4-one derivatives useful for the treatment of ORL-1 receptor mediated disorders
    Patent number: 6777421
    Abstract: The present invention is directed to novel 1,3,8-triazaspiro[4.5]decan-4-one derivatives of the general formula wherein all variables are as defined herein, useful in the treatment of disorders and conditions mediated by the ORL-1 G-protein coupled receptor. More particularly, the compounds of the present invention are useful in the treatment of disorders and conditions such as anxiety, depression, substance abuse, neuropathic pain, acute pain, migraine, asthma, cough and for improved cognition.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: August 17, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Alfonzo Jordan, Allen B. Reitz, Kevin Pan
  • Taste masked pharmaceutical compositions
    Patent number: 6767557
    Abstract: A taste masked pharmaceutical composition comprising a microcapsule, wherein the microcapsule comprises a pharmaceutically active agent core coated with a taste masking effective amount of a water-insoluble enteric coating, wherein the coating comprises a weakly acidic methacrylic acid-ethyl acrylate copolymer.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: July 27, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Stephen A. Ulrich, Karen R. Zimm
  • 7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives useful as antagonists of gonadotropin releasing hormone
    Patent number: 6765011
    Abstract: The present invention is directed to novel 7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives of the general formula (I) or (II) wherein all variables are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions associated with gonadotropin releasing hormone (GnRH). The compounds of the invention are antagonists of GnRH, useful in the treatment of the infertility, prostate cancer, benign prostate hyperplasia (BPH) and as contraceptives.
    Type: Grant
    Filed: April 3, 2003
    Date of Patent: July 20, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Zhihua Sui, Mark Macielag, James C. Lanter
  • Indoloazepines as vasopressin receptor antagonists
    Patent number: 6765004
    Abstract: The invention is directed to tricyclic indoloazepine compounds useful as vasopressin receptor antagonists, pharmaceutical compositions comprising the compounds of the present invention and methods of treating conditions involving increased vascular resistance and cardiac insufficiency which include hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis or water retention in a subject in need thereof.
    Type: Grant
    Filed: June 12, 2000
    Date of Patent: July 20, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: William J. Hoekstra, Michael N. Greco, Leonard R. Hecker, Bruce E. Maryanoff, Jay M. Matthews
  • Substituted amino acids as erythropoietin mimetics
    Patent number: 6750369
    Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: June 15, 2004
    Assignee: Ortho McNeil Pharmaceutical, Inc.
    Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
  • DNA encoding human serine protease D-G
    Patent number: 6750034
    Abstract: Here we describe the molecular identification of a cDNA encoding a novel serine protease we have termed D-G. The deduced amino acid sequence, and it's alignment with other well characterized serine proteases clearly indicates that it is a member of the S1 serine protease family. We have found that the protease D-G mRNA is widely expressed in several tissues throughout the body including epidermis, fibroblasts, keratinocytes, colon, small intestine, stomach, lung, kidney, bone marrow, lymph node, thymus, ovary, prostate, uterus and spinal cord. Interestingly, this protease contains a hydrophobic stretch of amino acids which is a putative transmembrane near the NH2-terminus. Thus, this serine protease is thought to be synthesized as a type II integral protein.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: June 15, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Andrew L. Darrow, Jenson (Jian-Shen) Qi, Patricia Andrade-Gordon
  • Low dose estrogen interrupted hormone replacement therapy
    Patent number: 6747019
    Abstract: A hormone replacement therapy, comprising a plurality of daily doses of a pharmaceutical preparation, the doses being administered continuously and consecutively in alternating phases of three daily doses, a relatively dominant estrogenic activity phase comprising three daily doses of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17&bgr;-estradiol per day, and a relatively dominant progestagenic activity phase of a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17&bgr;-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 &mgr;g per day of norgestimate.
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: June 8, 2004
    Assignees: Jencap Research, Ltd., Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Robert F. Casper, Gary A. Shangold, Militza K. Ausmanas
  • Antibody immunologically reactive with serine protease EOS
    Patent number: 6747134
    Abstract: Here we describe the molecular identification of a cDNA encoding a novel serine protease we have termed protease EOS. The deduced amino acid sequence, and it alignment with other well-characterized serine proteases indicates that it is a member of the S1 serine protease family. We have found that the protease EOS mRNA is expressed in platelets and leukocytes and more specifically eosinophils. Although this protease is abundantly expressed in ovary, retina and stomach, where it may perform important functions, its expression in platelets and certain cells of the immune system suggests that it may play roles in thrombosis and in the immune process. Enzymatically active protease EOS is amenable to further biochemical analyses for the identification of physiological substrates and specific modulators.
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: June 8, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Andrew Darrow, Jenson Qi, Patricia Andrade-Gordon
  • Pharmacokinetic and pharmacodynamic modeling of erythropoietin administration
    Patent number: 6747002
    Abstract: The present invention relates to systems and methods for obtaining optimized EPO dosage regimens for a desired pharmacodynamic/pharmacokinetic response. The system includes choosing one or more EPO dosage regimens, then using a PK/PD model to determine the pharmacodynamic/pharmacokinetic profile of one or more EPO dosage regimens, and finally selecting one of the EPO dosage regimens for administration to achieve the desired pharmacodynamic/pharmacodynamic response based on the EPO profile.
    Type: Grant
    Filed: May 10, 2000
    Date of Patent: June 8, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Wing Cheung, David Gibson, Christine Cote, Els Vercammen
  • Substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators
    Patent number: 6747127
    Abstract: The invention is directed to substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators, their use in wound healing and preventing platelet aggregation. Pharmaceutical compositions comprising the substituted heterocyclic acyl-tripeptides of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
    Type: Grant
    Filed: May 5, 2000
    Date of Patent: June 8, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: David F. McComsey, Bruce E. Maryanoff, Michael J. Hawkins
  • Aminomethyl-pyrroloquinazoline compounds as thrombin receptor antagonists
    Patent number: 6740657
    Abstract: The invention is directed to novel aminomethyl-pyrroloquinazoline compounds and pharmaceutical compositions thereof which are useful thrombin receptor or PAR-1 antagonists, methods for production thereof and methods for treating thrombin or PAR-1 mediated disorders.
    Type: Grant
    Filed: January 29, 2002
    Date of Patent: May 25, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Bruce E. Maryanoff, Han-Cheng Zhang, David F. McComsey
  • 6-O-carbamate-11,12-lacto-ketolide antimicrobials
    Patent number: 6713455
    Abstract: 6-O-Carbamate-11,12-lacto-ketolide antimicrobials of the formula: wherein R1, R2, R3 R7, and R8 are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
    Type: Grant
    Filed: September 16, 2002
    Date of Patent: March 30, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Eugene B. Grant, III, Todd C. Henninger, Mark J. Macielag, Deodialsingh Guiadeen
  • Tricyclic benzodiazepines as vasopressin receptor antagonists
    Patent number: 6713475
    Abstract: The invention is directed to tricyclic benzodiazepines useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising tricyclic benzodiazepines of the present invention and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.
    Type: Grant
    Filed: July 24, 2001
    Date of Patent: March 30, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: William J. Hoekstra, Alexey B. Dyatkin, Bruce E. Maryanoff, Jay M. Matthews
  • Pyrazine derivatives as modulators of tyrosine kinases
    Patent number: 6710048
    Abstract: The present invention provides pyrazine derivatives that inhibit tyrosine kinase activity. Certain pyrazine derivatives are selective inhibitors of vascular endothelial growth factor (VEGF) receptor tyrosine kinase. The present invention also provides pharmaceutical formulations containing the pyrazine derivatives and methods of use of these formulations as anti-tumor agents and to treat solid-tumor cancers, angiogenesis, diabetic retinopathy, rheumatoid arthritis, endometriosis and psoriasis.
    Type: Grant
    Filed: September 19, 2001
    Date of Patent: March 23, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Gee-Hong Kuo, Peter J. Connolly, Catherine Prouty, Alan DeAngelis, Aihua Wang, Linda Jolliffe, Steve Middleton, Stuart Emanuel
  • Pharmaceutical composition of topiramate
    Patent number: 6696091
    Abstract: The invention is directed to a pharmaceutical composition of topiramate an anticonvulsant which is useful for treating epilepsy. More specifically, the present invention provides a solid dosage formulation of topiramate intended primarily for use by pediatric patients, or for patients who have difficulty swallowing tablets. Processes for preparing the pharmaceutical composition are also described.
    Type: Grant
    Filed: March 1, 1999
    Date of Patent: February 24, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Madhav S. Thakur, Pramod M. Kotwal, Irwin S. Gibbs
  • Pharmaceutical compositions of erythropoietin
    Patent number: 6696056
    Abstract: The present invention provides aqueous pharmaceutical formulations of erythropoietin that are free of human serum blood products, stabilized with a quantity of an amino acid and a sorbitan mono-9-octadecenoate poly(oxy-1,2-ethanediyl) derivative. The present invention also provides aqueous stable, preserved pharmaceutical formulations of erythropoietin that contain an antimicrobial quantity of cresol and a quantity of an amino acid.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: February 24, 2004
    Assignee: Ortho McNeil Pharmaceutical, Inc.
    Inventors: Wing K. Cheung, Jaya Natarajan, Marilyn Sanders, Els Vercammen, Selima Begum, Basant Sharma
  • Methods for the synthesis of highly substituted 2,4-dioxopiperidine libraries
    Patent number: 6686503
    Abstract: The invention relates to methods of synthesizing libraries of diverse and complex highly substituted 2,4-dioxopiperidine compounds of the general formula: wherein R1, R2 and R3 are as herein described, novel intermediates useful for synthesizing such 2,4-dioxopiperidine compounds and methods for identifying and isolating the compounds.
    Type: Grant
    Filed: June 13, 2001
    Date of Patent: February 3, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Wenying Chai, William V. Murray