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US 6,545,022 B1Granted
4(3)substituted-4(3)-aminomethyl-(thio)pyran or piperidine derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders
AssigneePfizer Inc.
InventorsJustin Stephen Bryans, David Christopher Horwell, Clare Octavia Kneen, David Juergen Wustrow
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Abstract
Novel amines of formulas 1D and 1E are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.
Claims15
The compound of the invention are those of formula
- or a pharmaceutically acceptable salt thereof wherein:
- n is an integer of from 0 to 2;
- R is a heterocycle selected from
- and
- X is —O—, —S—, —S(O)—, —S(O)2—, or NR′1 is hydrogen, straight or branched alkyl of from 1 to 6 carbons, benzyl, —C(O)R′2 is straight or branched alkyl of 1 to 6 carbons, benzyl or phenyl or —CO2R′3 wherein R′3 is straight or branched alkyl of from 1 to 6 carbons, or benzyl wherein the benzly or phenyl groups can be unsubstituted or substituted by from 1 to 3 substituents selected from halogen trifluoromethyl, and nitro.
2 more elements
Dependencies are inferred from the claim text.