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Home Vasodialators Psychotropic-benzisothiazole-derivatives

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 Psychotropic benzisothiazole derivatives

Details
Inventors: Stack, Gary P.; Abou-Gharbia, Magid A.; Golobish, Thomas D.;
Assignee: American Home Products Corporation (New York, NY)
Primary Examiner: Bond; Robert T.
Assistant Examiner:
Attorney, Agent or Firm: Patton; Walter

Disclosed herein are novel benzisothiazole derivatives having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of a variety of central nervous system disorders.

DETAILED DESCRIPTION We claim: 1.
The compounds of formula (I) ##STR7## wherein R.
sup.
1 is hydrogen, hydroxy, cyano, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, halo or trifluoromethyl; (O) represents optional oxidation of sulfur; n is 2 to 5 and Z is ##STR8## wherein X is alkylene of 1 to 4 carbon atoms or alkylidene of 2 to 4 carbon atoms; Q is alkylene of 1 to 4 carbon atoms, alkylidene of 2 to 4 carbon atoms, or ##STR9## or a pharmaceutically acceptable salt thereof.
2.
The compounds according to claim 1 wherein R.
sup.
1 is hydrogen, hydroxy, methoxy, bromo or chloro; n is 4; Z is (II) wherein X is ethenylene and Q is methylene or ethenylene; or Z is (III) wherein X is methylene and Q is ##STR10## or Z is (IV) or (V) or a pharmaceutically acceptable salt thereof.
3.
A compound of claim 2 which is decahydro-3-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,5-metha no-6,7,9-metheno-2H-pentaleno[1,2-d]azepine-2,4(3H)-dione or a pharmaceutically acceptable salt thereof.
4.
A compound of claim 2 which is 2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-3a,4,4a,6a,7,7a-hex ahydro-4,7-etheno-1H-cyclobut[f]isoindole-1,3(2H)-dione or a pharmaceutically acceptable salt thereof.
5.
A compound of claim 2 which is 2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-4,4a,5,5a,6,6a-hexa hydro-4,6-ethenocycloprop[f]isoindole-1,3(2H,3aH)-dione or a pharmaceutically acceptable salt thereof.
6.
A compound of claim 2 which is 2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-1H-isoindole-1,3(2H )-dione or a pharmaceutically acceptable salt thereof.
7.
A compound of claim 2 which is (exo)-octahydro-2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-4,5 ,7-metheno-1H-pentaleno[1,2-c]pyrrole-1,3(1H)-dione or a pharmaceutically acceptable salt thereof.
8.
A compound of claim 2 which is (endo)-octahydro-2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-4, 5,7-metheno-1H-pentaleno[1,2-c]pyrrole-1,3(2H)-dione or a pharmaceutically acceptable salt thereof.




Description:
BACKGROUND OF THE INVENTION U



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