6- (2, 3, 4, 5-Tetrahydro-1H-Benzo [D] Azepin-7-Yloxy) -Nicotamide Derivatives as Radio Labelled Ligands
AssigneeGlaxo Group Limited
InventorChristophe Plisson
Life of this patent
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Abstract
The present invention relates to radiolabelled compounds of formula (I), which are useful for the labelling and diagnostic imaging of histamine H3 receptor functionality.
Claims17
A compound of formula (I):
- for use as an histamine H3 ligand, wherein:
- R1 is a radiolabelled group incorporating or consisting of a radionuclide selected from 3H, 11C, 13N, 15O76Br, 18F, 123I, 125I, 131I, 75B, 76Br, 77Br, and 82Br and X is C;
- or R1 is C2-6alkyl and X is 11C;
- or a pharmaceutically acceptable salt thereof.
[11C—N-methyl]6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy-nicotamide.
[11C-carbonyl] 6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-methylnicotamide.
Use of a compound of formula (I) or [11C-carbonyl] 6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-methylnicotamide for the manufacture of a medicament for the treatment or prophylaxis of neurological diseases including Alzheimer's disease, dementia, age-related memory dysfunction, mild cognitive impairment, cognitive deficit, epilepsy, neuropathic pain, inflammatory pain, migraine, Parkinson's disease, multiple sclerosis, stroke and steep disorders including narcolepsy;
- psychiatric disorders including schizophrenia (particularly cognitive deficit of schizophrenia), attention deficit hypereactivity disorder, depression and addiction;
- and other diseases including obesity, asthma, allergic rhinitis, nasal congestion, chronic obstructive pulmonary disease and gastro-intestinal disorders.
Dependencies are inferred from the claim text.