Abstract: A Compound of formula (wherein X is O or S and R1-R5 are disclosed herein) or a pharmaceutically acceptable salt thereof (each being a “Piperazine Compound”), pharmaceutical compositions comprising a Piperazine Compound and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperazine Compound are disclosed.

Abstract: This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel aryl-substituted pyrimidine compounds of Formula I: or a pharmaceutically acceptable salt, or solvate thereof, wherein A, R1, R2, R3 and R4 are defined in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: This invention relates aryl substituted thiazolidinones of Formula I: or a pharmaceutically acceptable salt, or solvate thereof, wherein R1 and R2, are defined in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: A Compound of formula (wherein X is O or S and R1–R5 are disclosed herein) or a pharmaceutically acceptable salt thereof (each being a “Piperazine Compound”), pharmaceutical compositions comprising a Piperazine Compound and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperazine Compound are disclosed.

Abstract: This invention relates aryl substituted benzimidazoles of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1, R2, R10 and n are defined in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: A compound of formula: (wherein X is O or S and R1, R3, R4, and R5 are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Thiadiazolylpiperazine Compound”), pharmaceutical compositions comprising a Thiadiazolylpiperazine Compound, and methods for treating or preventing pain in a patient comprising administering to a patient in need thereof an effective amount of a Thiadiazolylpiperazine Compound are disclosed.

Abstract: This invention relates aryl substituted thiazolidinones of Formula I: or a pharmaceutically acceptable salt, or solvate thereof, wherein R1 and R2, are defined in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: A compound of formula (wherein A, R1, R2, R6, m and n are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Piperazine Compound”); pharmaceutical compositions comprising a Piperazine Compound; and methods for treating pain, urinary incontinence (UI), an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia and depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperazine Compound are disclosed.

Abstract: The present invention relates to peptidomimetic ORL-1 receptor ligands containing certain conformationally constrained amino acids that favor alpha-helix or extended beta-strand conformations. Preferably, the ORL-1 receptor ligands of the present invention have one or more residues in an “address” segment to promote alpha-helix formation. The ligands of the present invention include ORL-1 receptor agonists that may be used as analgesics to treat pain in a patient in need of such treatment, and also may be used to treat anxiety, addiction, withdrawal and drug tolerance, as well as to enhance memory and learning.

Abstract: This invention relates to N-substituted hydromorphones of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is C1-6 alkyl. These compounds act as &mgr; opioid receptor agonists. The invention is also directed to the use of compounds of Formula I for the treatment, prevention or amelioration of both acute and chronic pain.

Abstract: A compound of formula: 1

Abstract: This invention relates aryl substituted thiazolidinones of Formula I: 1

Abstract: This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel 2-substituted bicyclic benzoheterocyclic compounds of Formula I: 1

Abstract: This invention relates aryl substituted benzimidazoles of Formula I: 1

Abstract: This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel aminoalkyl-substituted aryl compounds of Formula I: 1

Abstract: A compound of formula: 1

Abstract: This invention relates to aryl substituted hydantoins of Formula I: 1

Abstract: This invention relates to N-substituted hydromorphones of Formula I: 1

Abstract: A compound of formula 1

Abstract: A Compound of formula 1