Primary amines and derivitves thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto

Patent metadata

Field	Value
Publication number	US-9987252-B2
Application number	US-201615236722-A
Country	US
Kind code	B2
Filing date	Aug 15, 2016
Priority date	May 18, 2006
Publication date	Jun 5, 2018
Grant date	Jun 5, 2018

Abstract

The present invention pertains to certain compounds of Formula (Ia),

and pharmaceutical compositions thereof that modulate the activity of the 5-HT 2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infraction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

First claim

What is claimed is:

1. A method for modulating an activity of a 5-HT 2A serotonin receptor by contacting the receptor with N-[4-(2-amino-ethoxy)-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide, comprising administering to an individual in need thereof a therapeutically effective amount of an isolated compound that is N-[4-(2-amino-ethoxy)-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide, or a pharmaceutically acceptable salt thereof.

2. A method for treating a 5-HT 2A associated disorder in an individual comprising administering to the individual in need thereof a therapeutically effective amount of an isolated compound that is N-[4-(2-amino-ethoxy)-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide, or a pharmaceutically acceptable salt thereof.

3. The method according to claim 2 , wherein said 5-HT 2A associated disorder is a sleep disorder.

4. The method according to claim 2 , wherein said 5-HT 2A associated disorder is progressive multifocal leukoencephalopathy.

5. The method according to claim 2 , wherein said 5-HT 2A associated disorder is hypertension.

6. The method according to claim 2 , wherein said 5-HT 2A associated disorder is pain.

7. The method according to claim 2 , wherein said 5-HT 2A associated disorder is claudication.

8. The method according to claim 2 , wherein said 5-HT 2A associated disorder is peripheral artery disease.

9. The method according to claim 2 , wherein said 5-HT 2A associated disorder is vasoconstriction.

10. The method according to claim 2 , wherein said 5-HT 2A associated disorder is vasospasm.

11. The method according to claim 2 , wherein said 5-HT 2A associated disorder is thrombosis.

12. The method of claim 2 , wherein the individual has coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, or a symptom of any of the foregoing.

13. The method according to claim 2 , wherein said 5-HT 2A associated disorder is a symptom of stroke or stroke.

14. A method for reducing risk of blood clot formation in an angioplasty or coronary bypass surgery patient, or a patient suffering from atrial fibrillation, comprising administering to the individual in need thereof a therapeutically effective amount of an isolated compound that is N-[4-(2-amino-ethoxy)-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide, or a pharmaceutically acceptable salt thereof.

15. A method for reducing platelet aggregation in an individual comprising administering to the individual in need thereof a therapeutically effective amount of an isolated compound that is N-[4-(2-amino-ethoxy)-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide, or a pharmaceutically acceptable salt thereof.

Assignees

• Arena Pharm Inc

Inventors

• Teegarden Bradley
• Chapman Dennis
• Choi Juyi
• Feichtinger Konrad
• Han Sangdon
• Jayakumar Honnappa
• Tran Thuy-Anh
• Xu Jay
• Zou Ning

Classifications

• A61P7/02

  Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors · CPC title

• A61P7/00

  Drugs for disorders of the blood or the extracellular fluid · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title