# US 5,455,259 A · Compounds for the treatment of neurodegenerative disorders > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 5,455,259 A - Document ID: US5455259A - Status: Granted - Kind: A - Application number: 08/221,076 - Filed: 1994-03-31 - Granted: 1995-10-03 - Earliest claimed: 1987-02-06 - Assignees: Fisons Limited - Inventors: Ronald C. Griffith; Robert J. Murray; Michael Balestra; Donald Mathisen - Web page: https://patentgrep.com/patent/US5455259A ## CPC - A61K 31/16: Amides, e.g. hydroxamic acids - A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)} - A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide - A61K 31/245: Amino benzoic acid types, e.g. procaine, novocaine (salicylic acid esters A61K31/60) - A61K 31/275: Nitriles; Isonitriles - A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof - C07C 211/27: having amino groups linked to the six-membered aromatic ring by saturated carbon chains - C07C 211/29: the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups - C07C 215/52: linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring - C07C 217/60: linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring - C07C 237/00: Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups - C07C 237/06: having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms - C07C 237/08: having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms - C07C 237/10: having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups - C07C 255/58: containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton - C07C 271/12: to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals - C07D 213/38: having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom - C07K 5/06: Dipeptides - 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) - C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS - C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08) - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) ## Abstract (S)-.alpha.-phenyl-2-pyridineethanamine, and its pharmaceutically acceptable derivatives, are useful in the treatment of neurodegenerative disorders, and exhibit linear pharmacokinetics. ## Claims ### Claim 1 (S)-.alpha.-phenyl-2-pyridineethanamine, which is greater than 90% enantiopure, and pharmaceutically acceptable derivatives thereof. ### Claim 2 (S)-.alpha.-phenyl-2-pyridineethanamine, which is greater than 99% enantiopure, and pharmaceutically acceptable derivatives thereof. ### Claim 3 (S)-.alpha.-phenyl-2-pyridineethanamine, and pharmaceutically acceptable derivatives thereof. ### Claim 4 (depends on 1, 2, 3) A pharmaceutical formulation including (S)-.alpha.-phenyl-2-pyridineethanamine as defined in any one of claims 1 to 3, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. ### Claim 5 (depends on 1, 2, 3) A method of treatment of a neurodegenerative disorder, selected from the group consisting of epilepsy, stroke, cerebral ischacmia and anoxia which comprises administering an NMDA blocking, antihypoxia, antiepileptic or anti-ischemic effective amount of (S)-.alpha.-phenyl-2-pyridineethanamine, as defined in any one of claims 1 to 3, or a pharmaceutically acceptable derivative thereof, to a patient. ### Claim 6 (depends on 5) A method of treatment as claimed in claim 5, wherein the dose of the compound administered is linearly proportional to the blood plasma concentration of the compound desired. ### Claim 7 (S)-.alpha.-phenyl-2-pyridineethanamine (S)-malate which is greater than 90% enantiopure. ### Claim 8 (S)-.alpha.-phenyl-2-pyridineethanamine (S)-malate which is greater than 99% enantiopure. ### Claim 9 (S)-.alpha.-phenyl-2-pyridineethanamine (S)-malate. ### Claim 10 (depends on 7, 8, 9) A pharmaceutical formulation including (S)-.alpha.-phenyl-2-pyridineethanamine (S)-malate as defined in any one of claims 7 to 9, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. ### Claim 11 (depends on 7, 8, 9) A method of treatment of a neurodegenerative disorder, selected from the group consisting of epilepsy, stroke, cerebral ischaemia and anoxia which comprises administering an NMDA blocking, antihypoxia, antiepileptic or anti-ischemic effective amount of (S)-.alpha.-phenyl-2-pyridineethanamine (S)-malate, as defined in any one of claims 7 to 9, to a patient. ### Claim 12 (depends on 11) A method of treatment as claimed in claim 11, wherein the dose of the compound administered is linearly proportional to the blood plasma concentration of the compound desired. ### Claim 13 (S)-.alpha.-phenyl-2-pyridineethanamine benzoate which is greater than 90% enantiopure. ### Claim 14 (S)-.alpha.-phenyl-2-pyridineethanamine benzoate which is greater than 99% enantiopure. ### Claim 15 (S)-.alpha.-phenyl-2-pyridineethanamine benzoate. ### Claim 16 (depends on 13, 14, 15) A pharmaceutical formulation including (S)-.alpha.-phenyl-2-pyridineethanamine benzoate as defined in any one of claims 13 to 15, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. ### Claim 17 (depends on 13, 14, 15) A method of treatment of a neurodegenerative disorder, selected from the group consisting of epilepsy, stroke, cerebral ischacmia and anoxia which comprises administering an NMDA blocking, antihypoxia antiepileptic or anti-ischemic effective amount of (S)-.alpha.-phenyl-2-pyridineethanamine benzoate as defined in any one of claims 13 to 15, to a patient. ### Claim 18 (depends on 17) A method of treatment as claimed in claim 17, wherein the dose of the compound administered is linearly proportional to the blood plasma concentration of the compound desired.