Novel Medicaments

• US 20090312309A1
• Filed: 06/30/2006
• Published: 12/17/2009
• Est. Priority Date: 07/04/2005
• Status: Active Grant

• Current Assignee: vTv Therapeutics LLC (vTv Therapeutics, Inc.)
• Original Assignee: High Point Pharmaceuticals, LLC
• Inventors: Hohlweg, Rolf, Lundbeck, Jane Marie, Andersen, Knud Erik, Sorensen, Jan Lindy
• Granted Patent: US 8,501,739 B2
• Time in Patent Office: Days
• US Class Current: 514/218
• 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 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 213/74 Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• CPC Class Codes: C07D 213/84 Nitriles
• CPC Class Codes: C07D 213/87 in position 3
• CPC Class Codes: C07D 237/20 Nitrogen atoms nitro radicals C07D237/12
• CPC Class Codes: C07D 403/04 directly linked by a ring-member-to-ring-member bond
• CPC Class Codes: C07D 403/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 417/10 linked by a carbon chain containing aromatic rings

Abstract

Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

Claims

1. A compound of formula I:

2. A compound according to claim 1 with the following provisos h)-m):

h) R¹ is different from possibility i), when the ring containing W, X, Y and Z is a pyridazine or a pyrimidine ring, i) R¹¹ is different from hydrogen and methyl, j) R² is different from cyano, k) at least one of W, X, Y and Z is a moiety of the formula —

C(R²)═

wherein R² is as defined herein,

     1) R¹ is not a group of formula II when the ring containing W, X, Y and Z is a pyridazine ring, and m) A is different from pyrazol-1-yl when the ring containing W, X, Y and Z is a pyridazine ring.

4. A pharmaceutical composition comprising, as an active ingredient, at least one compound according to claim 1 together with one or more pharmaceutically acceptable carriers or recipients, which composition comprises from about 0.05 mg to about 1000 mg, from about 0.1 mg to about 500 mg, or from about 0.5 mg to about 200 mg, of the compound.

16. A method for the treatment of disorders and diseases related to the histamine H3 receptor, wherein the disorders and diseases are selected from:

overweight or obesity, eating disorders, anorexia, bulimia, binge eating, IGT, type 2 diabetes, delaying or preventing the progression from IGT to type 2 diabetes, delaying or prevention of the progression from non-insulin requiring type 2 diabetes to insulin requiring type 2, allergic rhinitis, ulcer, Alzheimer'"'"'s disease, narcolepsy or attention deficit disorders the method comprising administering to a subject in need thereof a therapeutically effective amount of a compound according to claim 1 or a pharmaceutical composition thereof.

18. A method for the reduction of weight, suppression of appetite, or for satiety induction, comprising:

administering to an individual in need thereof a therapeutically effective amount of a compound according to claim 1, or a pharmaceutical composition thereof.

3. (canceled)

5. (canceled)

6. (canceled)

7. (canceled)

8. (canceled)

9. (canceled)

10. (canceled)

11. (canceled)

12. (canceled)

13. (canceled)

14. (canceled)

15. (canceled)

17. (canceled)