2-arylamidothiazole derivatives with CNS activity

Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...

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544295, 544364, 544369, 546112, 546133, 548195, C07D27746, C07D41714, C07D41706, C07D45302

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active

055104789

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.

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K. Fukuda et al., TiPS 4-10 Dec. 1989 Supplement.
T. I. Bonner, TiPS 11-15 Dec. 1989 Supplement.
T. T. Soncrant et al., Psychopharmacology 112:421-427 (1993)**.
M. Williams, Curr. Opin. Invest. Drugs 2(5):541-544 (May 1993).
R. T. Bartus et al., Science 217:408-417 (Jul. 1982).

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