3-(l,3-BENZODIOXOL-5-YL)-6-(4-CYCLOPROPYLPIPERAZIN-l-YL)-PYRIDAZINE, ITS SALTS AND SOLVATES AND ITS USE AS HISTAMINE H3 RECEPTOR ANTAGONIST

• US 20090176793A1
• Filed: 05/22/2007
• Published: 07/09/2009
• Est. Priority Date: 05/29/2006
• Status: Active Grant

• Current Assignee: vTv Therapeutics LLC (vTv Therapeutics, Inc.)
• Original Assignee: High Point Pharmaceuticals, LLC
• Inventors: Hohlweg, Rolf
• Granted Patent: US 8,378,097 B2
• Time in Patent Office: Days
• US Class Current: 514/252.20
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: C07D 405/04 directly linked by a ring-member-to-ring-member bond

Abstract

3-(1,3-Benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine and salts and solvates thereof, (I) having histamine H3 antagonistic activity can be used in pharmaceutical compositions.

Claims

1. 3-(1,3-Benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine or a pharmaceutically acceptable salt or solvate thereof.

2. The compound according to claim 1, wherein the solvate is a hydrate.

3. The compound according to claim 1, wherein the salt is the dihydrochloride.

4. The compound according to claim 2, wherein the hydrate is the monohydrate.

5. The compound according to claim 1, wherein the compound is in the form of the dihydrochloride monohydrate.

6. (canceled)

7. (canceled)

8. A pharmaceutical composition comprising:

3-(1,3-Benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine, or a pharmaceutically acceptable salt or solvate thereof; and

a pharmaceutically acceptable carrier or diluent.

11. The pharmaceutical composition according to claim 8, wherein the 3-(1,3-Benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine is in the form of a free base.

12. The pharmaceutical composition according to claim 8, wherein the solvate is a hydrate.

13. The pharmaceutical composition according to claim 8, wherein the salt is the dihydrochloride.

14. The pharmaceutical composition according to claim 12, wherein the hydrate is the monohydrate.

15. The pharmaceutical composition according to claim 8, wherein the 3-(1,3-Benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine is in the form of the dihydrochloride monohydrate.

16. The pharmaceutical composition according to claim 8, wherein the 3-(1,3-Benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine is in the form of a free base.

9. A method of treatment of disorders or diseases related to the H3 histamine receptor, the method comprising administering to a subject in need thereof a therapeutically effective amount of 3-(1,3-Benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine, or a pharmaceutically acceptable salt or solvate thereof.

17. The method according to claim 9, wherein the disorder or disease is selected from the group selected from obesity, dyslipidaemia, coronary heart disease, gallbladder disease, osteoarthritis, eating disorders, IGT, type 2 diabetes, airway disorders, narcolepsy, attention deficit disorders, epilepsy, motion sickness, vertigo, irritable bowel syndrome, dementia, Alzheimer'"'"'s disease, allergic rhinitis, ulcer and anorexia.

18. The method according to claim 9, wherein the disorder or disease is selected from obesity, type 2 diabetes and eating disorders.

10. (canceled)