Ortho-mcneil Pharmaceutical Corp.

Janssen Pharmaceutica Nv

Other

Janseen Pharmacautica Nv

Ellen Codd

Mark E McDonnell

James J McNally

Ning Qin

John R Carson

Sui-Po Zhang

Scott L Dax

Mark Andrew Youngman

Michele C Jetter

Andrea Blum Works

Christine M Razler

Michael R D'Andrea

Susan K Yagel

Philip Michael Pitis

Christopher M Flores

Carlos Plata-Salaman

Boyu Zhao

Kathryn E Rogers

Rebecca P Martinez

Mark Mcdonnell

Michele Jetter

Mark Mcdonell

This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to &#x3b2;-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.

Aminotetralin-derived urea modulators of vanilloid VR1 receptor

This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to quinoline-derived amides that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.

Quinoline-derived amide modulators of vanilloid VR1 receptor

The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic &#x3b4;-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.

Tricyclic &#x3b4;-opioid modulators

Thiozanthene derivatives as delta-opioid modulators

The invention provides an assay system for detecting a molecule that interacts with a membrane channel, the assay system including cell membranes including one or more membrane channels; support bodies including scintillant and a coupling agent that associates with the cell membrane; a ligand that is selected to bind the membrane channel, the ligand including a scintillant-activating label. According to the invention, association of the support bodies with the cell membrane and binding of the ligand to the membrane channel results in emission from the scintillant of the support bodies, and, in the presence of a test molecule that interacts with the membrane channel, the emission from the scintillant of the support bodies changes. Methods of identifying a molecule that interacts with a cell membrane channel are also described.

Assay systems and methods for detecting molecules that interact with membrane channels

The present invention provides nucleic acid and polypeptide sequences describing an isoform of the &#x3b1;2&#x3b4;-4 subunit of a voltage gated calcium channel. The nucleic acids described herein can be used to produce functional &#x3b1;2&#x3b4;-4 protein. The calcium channel &#x3b1;2&#x3b4;-4 protein may be isolated for the purposes of binding experiments or may be used in cells to form a functional calcium channel complex.

CDNA encoding the human &#x3b1;2 &#x3b4;4 calcium channel subunit

Disclosed are compounds, compositions and methods for treating various diseases and conditions, including pain. Such compounds are represented by Formula I as follows: wherein A, Z, Y, R-Rare defined herein.

Tricyclic-bridged piperidinylidene derivatives as 8-opioid modulators

CDNA encoding the human alpha2 delta4 calcium channel subunit

The present invention provides nucleic acid and polypeptide sequences describing a neve isozyme of the cyclooxygenase enzyme, herein named as human cyclooxygenase 3. The isolated nucleic acid or polypeptide molecule of the invention can be used in detection assays, gene therapy, and screening assays.

Human cyclooxygenase-3 enzyme and uses thereof

DNAs encoding human voltage gated sodium channel &#x3b2;1A subunit 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.

Human voltage gated sodium channel &#x3b2;1A subunit and methods of use

This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to naphthol, quinoline and isoquinoline-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.

Naphthol, quinoline and isoquinoline-derived urea modulators of vanilloid VR1 receptor

The present invention provides nucleic acid and polypeptide sequences describing a novel isoform of the &#x3b1;2&#x3b4; subunit of a voltage gated calcium channel, herein named as &#x3b1;2&#x3b4;-4. The isolated nucleic acid or polypeptide molecule of the invention can be used in diagnosing and treating a disease or disorder associated with a defective &#x3b1;2&#x3b4;-4 subunit, such as seizure-related syndromes, anxiety, multiple sclerosis, and the like.

This invention is directed to a method for preventing or treating neuropathic pain and cluster and migraine headache-associated pain 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 independently selected from the group consisting of fluorine, chlorine, bromine and iodine; and; R, R, Rand Rare independently selected from the group consisting of hydrogen and C&#x2013;Calkyl; wherein C&#x2013;Calkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of hydrogen, halogen, C&#x2013;Calkyl, C&#x2013;Calkoxy, amino, nitro and cyano).

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Blue Bell, PA, United States of America

Ellen Codd