Abstract: The invention is directed to 4h-benzo[1,4]oxazin-3-ones useful as peroxisome proliferator activated receptor gamma (PPAR&ggr;) 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:
May 11, 2001
Date of Patent:
April 29, 2003
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Thomas P. Burris, Donald W. Combs, Philip J. Rybczynski
Abstract: This invention is directed to 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives useful as &dgr;-opioid or &mgr;-opioid receptor modulators. Depending on their agonist or antagonist effect, the compounds are useful analgesics, immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.
Type:
Grant
Filed:
February 22, 2001
Date of Patent:
April 22, 2003
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Robert E. Boyd, John R. Carson, Steven J. Coats, Lou Anne Neilson, Philip M Pitis, Wu-Nan Wu
Abstract: DNA encoding human acid sensing ion channel BnaC4 has 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:
March 3, 2000
Date of Patent:
April 15, 2003
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Adrienne Elizabeth Dubin, Jayashree Pyati, Rene Huvar, Mark G. Erlander
Abstract: This invention provides compounds having the following general structure:
This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.
Type:
Grant
Filed:
June 12, 2000
Date of Patent:
April 8, 2003
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
James C. Lanter, Suying Zhang, Boyu Zhao
Abstract: This invention is directed to a method for preventing or treating psychotic disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II):
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, R2, R3, R4, R5 and R6 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:
April 1, 2003
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Carlos R. Plata-Salaman, Boyu Zhao, Roy E. Twyman
Abstract: The present invention is directed to compounds useful as selective serine protease or dual-serine protease inhibitors, compositions thereof and methods for treating serine protease or dual-serine protease mediated disorders.
Type:
Grant
Filed:
March 5, 2002
Date of Patent:
March 25, 2003
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Michael N. Greco, Bruce E. Maryanoff, Michael J. Hawkins, Robert E. Boyd
Abstract: The present invention relates to an oil-in-water emulsion containing tretinoin and the use thereof in mitigating skin disorders such as acne, photodamaged skin, wrinkles, mottled hyperpigmentation, tactile roughness, and yellowing of facial skin.
Abstract: This invention relates to a series of substituted imidazoles of Formula I
pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention inhibit the production of a number of inflammatory cytokines, and are useful in the treatment of diseases associated with overproduction of inflammatory cytokines.
Type:
Grant
Filed:
November 3, 2000
Date of Patent:
February 18, 2003
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Scott A. Beers, Elizabeth A. Malloy, Michael P. Wachter, Wei Wu
Abstract: Piperidinyloxy, pyrrolidinyloxyl and azetidinyloxy compounds of the formula:
wherein R1 is a piperidinyl, pyrrolidinyl or azetidinyl moiety 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:
December 5, 2000
Date of Patent:
February 11, 2003
Assignee:
Ortho McNeil Pharmaceutical, Inc.
Inventors:
Michele A. Weidner-Wells, Christine Boggs, Dennis Hlasta, Erin Nelson
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.
Abstract: This invention is directed to methods of synthesizing densely functionalized pyrrolidine compounds through the use of intramolecular Diels Alder reactions.
Type:
Grant
Filed:
March 12, 2002
Date of Patent:
January 28, 2003
Assignee:
Ortho McNeil Pharmaceutical, Inc.
Inventors:
Pranab Mishra, Sengen Sun, William V. Murray
Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:
Type:
Grant
Filed:
January 8, 2002
Date of Patent:
January 21, 2003
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
Abstract: This invention provides a convenient process for preparing an oral contraceptive liquid formulation having improved solubility, bioavailability and stability useful as a reference standard.
Abstract: Anticonvulsant compounds of the general formula I:
where X, R1, R2, R3, R4, R5, and R6 are as herein defined; are useful in treating acute ischemia-induced neurodegeneration, such as occurs during and after stroke, head trauma, spinal injury, non-fatal cardiac arrest, or major surgical procedures. Furthermore, pharmaceutical compositions containing a compound of formula I as well as methods for their use are disclosed.
Type:
Grant
Filed:
July 20, 2000
Date of Patent:
December 17, 2002
Assignee:
Ortho McNeil-Pharmaceutical, Inc.
Inventors:
Michael J. Costanzo, Bruce E. Maryanoff, Richard P. Shank
Abstract: The present invention relates to novel &bgr;-carboline derivatives of the general formula
wherein all the variables are as described within the specification, useful as phosphodiesterase inhibitors. The present invention further relates to use of the described derivatives for the treatment of diseases and conditions related to PDE, for example male erectile dysfunction.
Abstract: The invention features methods of using pharmaceutically-active 2- or 3-aryl substituted imidazopyridines for the treatment of histamine H3 receptor-mediated disorders.
Type:
Grant
Filed:
March 29, 2001
Date of Patent:
December 3, 2002
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
J. Guy Breitenbucher, Nicholas I. Carruthers, Xiaobing Li, Timothy W. Lovenberg
Abstract: The invention is directed to nonpeptide substituted benzodiazepines of Formula I,
wherein A, X, Z, Bp, W, n, R1 and R2 are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising a compound of Formula I 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.
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.
Type:
Grant
Filed:
August 31, 1999
Date of Patent:
November 26, 2002
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Andrew Darrow, Jenson Qi, Patricia Andrade-Gordon