Non-natural galanin receptor ligands
AssigneeKemia, Inc.
InventorsKulliki Saar, Tamas Bartfai, Ulo Langel, Gerd Hallnemo, Sven Hellberg
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Abstract
Compounds which are non-natural galanin receptor ligands are disclosed. The ligands are of small size, have agonist or antagonist galanin activity and may cross the blood-brain barrier to displace galanin from galanin receptors. The ligands are useful as medicaments for treatment of convulsions (e.g. in epilepsy), diseases and disorders related to endocrinology (e.g., growth hormone, insulin or prolactin release), tumors expressing galanin receptors, feeding disorders pain, allodynia, psychiatric disorders such as depression (involving e.g., noradrenaline or serotonin), cognitive disorders (e.g. Alzeimer's disease), and the like.
Claims59
A compound which is a galanin receptor ligand having the formula:
- wherein:
- R1, R1′, and R1″ are each independently hydrogen or lower alkyl,
- R2 is an optionally substituted hydrocarbyl moiety containing at least about four carbon atoms,
- R2′ is an optionally substituted hydrocarbyl moiety containing at least four carbon atoms,
- E is optional, and, if present, is O or S,
- X is a lysine side chain,
- Ar is an optionally substituted aromatic or heteroaromatic moiety having at least about three carbon atoms, and
- n is 1 to 3.
A compound which is a galanin receptor ligand having the formula:
- wherein:
- R1, R1′, and R1″ are each independently hydrogen or lower alkyl,
- One of R2 and R2′ is an optionally substituted polycyclic hydrocarbyl moiety containing at least about four carbon atoms, and the other of R2 and R2′ is an optionally substituted hydrocarbyl moiety containing at least about four carbon atoms,
- E is optional, and, if present, is O or S,
- X is a hydrocarbyl moiety bearing at least one substituent, wherein at least one of said substituents bears a positive charge,
- Ar is an optionally substituted aromatic or heteroaromatic moiety having at least about three carbon atoms, and n is 1 to 3.
Dependencies are inferred from the claim text.