# US 2014/0179707 A1 · Novel ergoline derivatives and uses thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2014/0179707 A1 - Document ID: US20140179707A1 - Status: Published application - Kind: A1 - Application number: 14/134,127 - Filed: 2013-12-19 - Published: 2014-06-26 - Earliest claimed: 2012-12-21 - Assignees: MAP Pharmaceuticals, Inc. - Applicants: Map Pharmaceuticals, Inc. - Inventors: Thomas Armer; Shashidhar Kori; Libo Wu - Web page: https://patentgrep.com/patent/US20140179707A1 ## CPC - A61K 31/4985: Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems - A61P 25/00: Drugs for disorders of the nervous system - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract Provided herein are 8′-Hydroxy-2-CF3-dihydroergotamine (8′OH-2-CF3-DHE) compounds, compositions, and dosage forms containing such compositions. Also provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein. ## Claims ### Claim 1 A 8′-Hydroxy-2-CF3-dihydroergotamine (8′OH-2-CF3-DHE) composition suitable for use in the treatment of a disease, condition or disorder selected from the group consisting of migraine, amyotrophic lateral sclerosis (ALS), Parkinson's disease, stress/anxiety, nausea, emesis, aggression, pain, neuropathic pain, sleeplessness, insomnia, restless leg syndrome and depression. ### Claim 2 (depends on 1) The 8′OH-2-CF3-DHE composition of claim 1, wherein said composition comprises an 8′OH-2-CF3-DHE compound in the form of a pharmaceutically acceptable salt, solvate, ester, or hydrate. ### Claim 3 (depends on 1) The 8′OH-2-CF3-DHE composition of claim 1, wherein said composition comprises an 8′OH-2-CF3-DHE compound in a solid form. ### Claim 4 (depends on 3) The 8′OH-2-CF3-DHE composition of claim 3, wherein the 8′OH-2-CF3-DHE compound is in the form of amorphous, semi-crystalline or crystalline particles. ### Claim 5 (depends on 4) The 8′OH-2-CF3-DHE composition of claim 4, wherein the amorphous, semi-crystalline or crystalline particles of the 8′OH-2-CF3-DHE compound are suitable for administration via inhalation. ### Claim 6 (depends on 1) The 8′OH-2-CF3-DHE composition of claim 1, wherein said composition comprises a pharmaceutically acceptable vehicle. ### Claim 7 (depends on 1) The 8′OH-2-CF3-DHE composition of claim 1, wherein said composition comprises a pharmaceutically acceptable excipient. ### Claim 8 (depends on 1) The 8′OH-2-CF3-DHE composition of claim 1, wherein said composition comprises an 8′OH-2-CF3-DHE derivative. ### Claim 9 (depends on 1) The 8′OH-2-CF3-DHE composition of claim 1, wherein said composition is in the form of a solution, suspension, tablet, dispersible tablet, pill, capsule, powder, sustained release composition, an elixir, a sterile solution or suspension suitable for parenteral administration, a topical dosage form, a transdermal dosage form, a nasal dosage form, or a pulmonary dosage form suitable for inhalation administration. ### Claim 10 (depends on 1) The 8′OH-2-CF3-DHE composition of claim 1, wherein said composition is suitable for administration using a nebulizer, a dry powder inhaler (DPI) device, a metered dose inhaler (MDI) device, or a pressurized metered dose inhaler (pMDI). ### Claim 11 A method for treating, preventing or ameliorating one or more symptoms of a disease, condition or disorder selected from the group consisting of migraine, amyotrophic latereral sclerosis (ALS), Parkinson's disease, stress/anxiety, nausea, emesis, aggression, pain, neuropathic pain, sleeplessness, insomnia, restless leg syndrome and depression, said method comprising administering a therapeutically effective dose of an 8′OH-2-CF3-DHE composition to a subject in need of such treatment. ### Claim 12 (depends on 11) The method of claim 11, wherein said treatment comprises a reduction in at least one symptom of the disease, condition or disorder. ### Claim 13 (depends on 11) The method of claim 11, wherein said treatment comprises provision of partial relief from at least one symptom of the disease, condition or disorder. ### Claim 14 (depends on 13) The method of claim 13, wherein said treatment further comprises provision of sustained relief from at least one symptom of the disease, condition or disorder. ### Claim 15 (depends on 11) The method of claim 11, wherein said treatment is further characterized by not inducing one or more drug-induced side effect. ### Claim 16 (depends on 15) The method of claim 15, wherein said treatment is further characterized by not inducing one or more drug-induced side effect selected from nausea, emesis, chest tightness, and cardiovascular effects. ### Claim 17 (depends on 11) The method of claim 11, wherein said 8′OH-2-CF3-DHE composition is administered in the form of a solution, suspension, tablet, dispersible tablet, pill, capsule, powder, sustained release composition, an elixir, a sterile solution or suspension suitable for parenteral administration, a topical dosage form, a transdermal dosage form, a nasal dosage form, or a pulmonary dosage form suitable for inhalation administration. ### Claim 18 (depends on 11) The method of claim 11, wherein said 8′OH-2-CF3-DHE composition is administered using a nebulizer, a DPI device, a MDI device, or a pMDI device. ### Claim 19 A molecule having the structure ### Claim 20 (depends on 19) A composition comprising the molecule of claim 19 in the form of a pharmaceutically acceptable salt, solvate, ester or hydrate.