2-arylamidothiazole derivatives with CNS activity
AssigneeAmerican Home Products Corporation
InventorAnnmarie L. Sabb
Life of this patent
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Abstract
The compound of the formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are, independently, H, alkyl, halo, perhaloalkyl, hydroxy, alkoxy, aryl or arylalkyl; n is an integer from 0-5; R is azabicyclo 2.2.2!octyl or azabicyclo 2.2.1!heptyl when n.sub.1 is zero, or R is NR.sub.4 R.sub.5 when n.sub.1 is 1, 2, 3, 4, or 5, in which R.sub.4 and R.sub.5 are alkyl or R.sub.4 and R.sub.5, taken with the nitrogen atom to which they are attached, are N-(substituted aryl)piperazinyl in which said substituent is alkoxy, halo, or perhaloalkyl; N-(pyridyl)piperazinyl; N-(pyrimidinyl)piperazinyl; or 3-azabicyclo- 3.2.2!non-3-yl; X is oxygen or NH; n and n.sub.1 are, independently, one of the integers 0, 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof are centrally active muscarinic agents.
Claims21
A compound of the formula:
- ##STR4## where R.sub.1, R.sub.2 and R.sub.3 are, independently, H, alkyl of 1 to 6 carbon atoms, halo, perhaloalkyl of 1 to 6 carbon atoms, hydroxy, alkoxy of 1 to 6 carbon atoms, aryl of 6 to 10 carbon atoms or arylalkyl of 7 to 12 carbon atoms;
- n is one of the integers 0, 1, 2, 3, 4 or 5;
- R is azabicyclo 2.2.2!octyl or azabicyclo 2.2.1!heptyl when n.sub.1 is zero, or R is NR.sub.4 R.sub.5 when n.sub.1 is 1, 2, 3, 4, or 5, in which R.sub.4 and R.sub.5 are alkyl of 1 to 6 carbon atoms or R.sub.4 and R.sub.5, taken with the nitrogen atom to which they are attached, are N-(substituted aryl)piperazinyl in which said substituent is alkoxy of 1 to 6 carbon atoms, halo, or perhaloalkyl of 1 to 6 carbon atoms, and the aryl group contains 6 to 10 carbon atoms;
- N-(pyridyl)piperazinyl;
- N-(pyrimidinyl)piperazinyl;
- or 3-azabicyclo- 3.2.2!non-3-yl;
- X is oxygen or NH;
- n and n.sub.1 are, independently, one of the integers 0, 1, 2, 3, 4 or 5;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.