Methods of treating inflammation or neuropathic pain
AssigneeH. Lundbeck A/S
InventorsJacqueline Lorayne BLANKMAN, Jason Robert CLAPPER, R. Alan B. EZEKOWITZ, Iain Peter FRASER, Cheryl A. GRICE, Todd K. JONES, Gary Paul O'NEILL, Archie Wayne THURSTON, JR., Channing Rodney BEALS
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Abstract
Provided herein are methods of treating inflammation or neuropathic pain using an effective dose of a monoacylglycerol lipase inhibitor or a composition thereof.
Claims75
A method of treating inflammation or neuropathic pain in a patient in need thereof, comprising administering to the patient in need thereof an effective dose of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, wherein the effective dose is from about 1 mg to about 500 mg.
A method of treating Epilepsy/Seizure Disorder, Multiple Sclerosis, Neuromyelitis Optica (NMO), Tourette Syndrome, Alzheimer Disease, or abdominal pain associated with Irritable Bowel Syndrome in a patient in need thereof, comprising administering to the patient in need thereof an effective dose of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, wherein the effective dose is from about 1 mg to about 100 mg.
A method of treating acute pain, inflammatory pain, cancer pain, pain caused by peripheral neuropathy, central pain, fibromyalgia, migraine, vasoocclussive painful crises in sickle cell disease, spasticity or pain associated with multiple sclerosis, functional chest pain, rheumatoid arthritis, osteoarthritis, or functional dyspepsia in a patient in need thereof, comprising administering to the patient in need thereof an effective dose of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, wherein the effective dose is from about 1 mg to about 100 mg.
A method of treating inflammation or neuropathic pain in a patient in need thereof, comprising administering to the patient in need thereof an effective dose of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, wherein a fragment of Compound 1 is covalently attached to at least 30% of MGLL in PBMCs from the patient after administration of the effective dose.
A method of treating inflammation or neuropathic pain in a patient in need thereof, comprising administering to the patient in need thereof an effective dose of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, wherein the plasma AUC0-inf of Compound 1 is at least 0.05 μM·hr after administration of the effective dose.
A method of treating inflammation or neuropathic pain in a patient in need thereof, comprising administering to the patient in need thereof an effective dose of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, wherein the steady state plasma AUC0-inf of Compound 1 is at least 0.05 μM·hr after administration of the effective dose.
A method of treating inflammation or neuropathic pain in a patient in need thereof, comprising administering to the patient in need thereof a composition comprising 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, wherein administration of the composition provides a plasma AUC0-inf of at least 0.05 μM·hr.
A method of treating Epilepsy/Seizure Disorder, Multiple Sclerosis, Neuromyelitis Optica (NMO), Tourette Syndrome, Alzheimer Disease, or abdominal pain associated with Irritable Bowel Syndrome in a patient in need thereof, comprising administering to the patient in need thereof a composition comprising 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, wherein administration of the composition provides a plasma AUC0-inf of at least 0.05 μM·hr.
A method of treating acute pain, inflammatory pain, cancer pain, pain caused by peripheral neuropathy, central pain, fibromyalgia, migraine, vasoocclussive painful crises in sickle cell disease, spasticity or pain associated with multiple sclerosis, functional chest pain, rheumatoid arthritis, osteoarthritis, or functional dyspepsia in a patient in need thereof, comprising administering to the patient in need thereof a composition comprising 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, wherein administration of the composition provides a plasma AUC0-inf of at least 0.05 μM·hr.
A method of treating inflammation or neuropathic pain in a patient in need thereof, comprising administering to the patient in need thereof a composition comprising 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, wherein administration of the composition provides at least 30% of MGLL in PBMCs from the patient to be covalently attached to a fragment of Compound 1.
A method of treating Epilepsy/Seizure Disorder, Multiple Sclerosis, Neuromyelitis Optica (NMO), Tourette Syndrome, Alzheimer Disease, or abdominal pain associated with Irritable Bowel Syndrome in a patient in need thereof, comprising administering to the patient in need thereof a composition comprising 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, wherein administration of the composition provides at least 30% of MGLL in PBMCs from the patient to be covalently attached to a fragment of Compound 1.
A method of binding MGLL with 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1) in PBMCs in a subject after administration of an effective dose of Compound 1, or a pharmaceutically acceptable salt thereof, to the subject, wherein a fragment of Compound 1 is covalently attached to at least 30% MGLL in PBMCs.
A pharmaceutical composition for the treatment of inflammation or neuropathic pain, wherein the pharmaceutical composition comprises an effective dose of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient, wherein the effective dose is from about 1 mg to about 500 mg.
A pharmaceutical composition for the treatment of Epilepsy/Seizure Disorder, Multiple Sclerosis, Neuromyelitis Optica (NMO), Tourette Syndrome, Alzheimer Disease, or abdominal pain associated with Irritable Bowel Syndrome, wherein the pharmaceutical composition comprises an effective dose of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient, wherein the effective dose is from about 1 mg to about 100 mg.
A pharmaceutical composition for the treatment of acute pain, inflammatory pain, cancer pain, pain caused by peripheral neuropathy, central pain, fibromyalgia, migraine, vasoocclussive painful crises in sickle cell disease, spasticity or pain associated with multiple sclerosis, functional chest pain, rheumatoid arthritis, osteoarthritis, or functional dyspepsia, wherein the pharmaceutical composition comprises an effective dose of 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (Compound 1), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient, wherein the effective dose is from about 1 mg to about 100 mg.
Dependencies are inferred from the claim text.