METHODS OF TREATMENT USING SELECTIVE 5-HT2A INVERSE AGONISTS

• US 20170165273A9
• Filed: 03/21/2011
• Published: 06/15/2017
• Est. Priority Date: 03/06/2000
• Status: Active Grant

• Current Assignee: Allan Kjaersgaard Uldam, Carl-Magnus A. Andersson, Eva Louise Hansen, Glenn Croston
• Original Assignee: Carl-Magnus A. Andersson
• Inventors: ANDERSSON, Carl-Magnus A., Croston, Glenn, Hansen, Eva Louise, Uldam, Allan Kjaersgaard
• Granted Patent: US 9,765,053 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/40 having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 7/02 Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/08 Vasodilators for multiple indications
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: A61P 9/12 Antihypertensives
• CPC Class Codes: C07D 207/14 Nitrogen atoms not forming part of a nitro radical
• CPC Class Codes: C07D 211/26 with hydrocarbon radicals, substituted by nitrogen atoms
• CPC Class Codes: C07D 211/58 attached in position 4
• CPC Class Codes: C07D 401/06 : linked by a carbon chain containing only aliphatic carbon atoms
• CPC Class Codes: C07D 401/12 : linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 407/06 : linked by a carbon chain containing only aliphatic carbon atoms
• CPC Class Codes: C07D 407/12 : linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 409/06 : linked by a carbon chain containing only aliphatic carbon atoms
• CPC Class Codes: C07D 409/12 : linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 417/12 : linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 451/02 : containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
• CPC Class Codes: C07D 451/06 : Oxygen atoms
• CPC Class Codes: C07D 487/08 : Bridged systems

Abstract

Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.

Claims

1-17. -17. (canceled)

18. A method for the treatment of psychosis, comprising administering an effective amount of a selective 5-HT2A inverse agonist to a human in need of such treatment, wherein the compound has little or no activity at 5-HT1A, 5-HT1B, dopaminergic, histaminergic, adrenergic or muscarinergic receptors.

22. The method of claim 18, wherein the disease or disorder is psychosis associated with Alzheimer'"'"'s disease.

23. The method of claim 18, wherein the disease or disorder is psychosis associated with Parkinsonism.

24. The method of claim 18, wherein the selective 5-HT2A receptor inverse agonist is a small molecule.

25. The method of claim 18, wherein the compound or pharmaceutical composition is in the form of a dosage unit that contains from about 0.01 mg to about 50 mg of the selective 5-HT2A receptor inverse agonist.

26. The method of claim 25, wherein the dosage unit that contains from about 1 mg to about 10 mg of the selective 5-HT2A receptor inverse agonist.

27. The method of claim 25, wherein about 0.001 mg/kg to about 10 mg/kg of body weight per day of the selective 5-HT2A receptor inverse agonist is administered.

19. A method for the treatment of schizophrenia, comprising administering an effective amount of a selective 5-HT2A inverse agonist to a human in need of such treatment, wherein the compound has little or no activity at 5-HT1A, 5-HT1B, dopaminergic, histaminergic, adrenergic or muscarinergic receptors.

20. A method for the treatment of depression, comprising administering an effective amount of a selective 5-HT2A inverse agonist to a human in need of such treatment, wherein the compound has little or no activity at 5-HT1A, 5-HT1B, dopaminergic, histaminergic, adrenergic or muscarinergic receptors.

21. A method for the treatment of bipolar disorder, comprising administering an effective amount of a selective 5-HT2A inverse agonist to a human in need of such treatment, wherein the compound has little or no activity at 5-HT1A, 5-HT1B, dopaminergic, histaminergic, adrenergic or muscarinergic receptors.