Spiro azepane-oxazolidinones as Kv1.3 potassium channel blockers

A compound of formula (v):

• wherein
• each of R1 and R2 is chosen from hydrogen, deuterium, fluorine, CF3, and alkyl(C1-3), which may be unsubstituted or substituted with one or more fluorine atoms,
• n is an integer chosen from 0, 1, and 2, and
• R3 is chosen from halogen, alkyl(C1-3), CF3, CN, NH2, NHAc, OH, OCH3, and OCF3.

A compound of formula (vi):

• wherein
• each of R1 and R2 is chosen from hydrogen, deuterium, fluorine, CF3, and alkyl(C1-3), which may be unsubstituted or substituted with one or more fluorine atoms,
• n is an integer chosen from 0, 1, and 2, and
• R3 is chosen from halogen, alkyl(C1-3), CF3, CN, NH2, NHAc, OH, OCH3, and OCF3.

A compound of formula (vii):

• wherein
• each of R1 and R2 is chosen from hydrogen, deuterium, fluorine, CF3, and alkyl(C1-3), which may be unsubstituted or substituted with one or more fluorine atoms,
• n is an integer chosen from 0, 1, and 2, and
• R3 is chosen from halogen, alkyl(C1-3), CF3, CN, NH2, NHAc, OH, OCH3, and OCF3,
• with the proviso that the compound of formula (vii) is not 3-[(S)-1-phenyl-ethyl]-1-oxa-3,8-diazaspiro[4.6]undecan-2-one.

A method for treating at least one condition chosen from diabetes, psoriasis, obesity, transplant rejection, and inflammatory neuropathies, -cell mediated autoimmune diseases, rheumatoid arthritis, and multiple sclerosis, the method comprising administering a compound of formula (1) to a patient in need of such treatment, wherein the compound of formula (1) is:

• wherein:
• each of R1 and R2 is chosen from hydrogen, deuterium, fluorine, CF3, and alkyl(C1-3), which may be unsubstituted or substituted with one or more fluorine atoms,
• n is an integer chosen from 0, 1, and 2,
• R3 is chosen from halogen, alkyl(C1-3), CF3, CN, NH2, NHAc, OH, OCH3, and OCF3,
• m is an integer chosen from 0, 1, 2, and 3, and
• R4 is chosen from halogen, alkyl(C1-3), CF3, CN, NH2, NHAc, OH, OCH3, and OCF3, or
• (R4)m and the phenyl ring to which it is attached form a naphthyl group,
• or a tautomer, a stereoisomer, or a pharmacologically acceptable salt of any of the foregoing.

A pharmaceutical composition comprising at least one pharmaceutically acceptable carrier, or at least one pharmaceutically acceptable auxiliary substance, or a combination of two or more thereof;

• and a pharmacologically active amount of at least one compound of formula (1):
• or a pharmacologically acceptable salt thereof, wherein:
• each of R1 and R2 are chosen from hydrogen, deuterium, fluorine, CF3, and alkyl(C1-3), unsubstituted or substituted with one or more fluorine atoms,
• n is an integer chosen from 0, 1, and 2, R3 is chosen from halogen, alkyl(C1-3), CF3, CN, NH2, NHAc, OH, OCH3, and OCF3,
• m is an integer chosen from 0, 1, 2, and 3, and
• R4 is chosen from halogen, alkyl(C1-3), CF3, CN, NH2, NHAc, OH, OCH3, and OCF3, or
• (R4)m and the phenyl ring to which it is attached form a naphthyl group.