Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...
Patent
1990-05-21
1991-12-31
Shen, Cecilia
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitrogen attached directly or indirectly to the purine ring...
544230, 544232, 544368, 544398, 544373, 548371, 548372, 548373, C07D40304, C07D40314, C07D41300, C07F 902
Patent
active
050774050
ABSTRACT:
This invention relates to 3-(1-substituted-4-piperazinyl)-1H-indazoles having the following formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, arylloweralkyl, acyl, cycloalkylloweralkylene, and phenylsulfonyl; and R.sub.2 is hydrogen, lower alkyl, hydroxyloweralkyl of the formula -(loweralkylene)-OH, arylloweralkyl, acyl, cycloalkylloweralkylene, ##STR2## where Z is selected from hydrogen, halogen, loweralkoxy, CF.sub.3, NO.sub.2, and NH.sub.2 ; ##STR3## where Z is as defined above; ##STR4## where Z is as defined above; ##STR5## where R.sub.3 and R.sub.4 are each independently hydrogen and loweralkyl; ##STR6## where Z is as defined above; ##STR7## where R' and R" are each independently hydrogen and loweralkyl; X is hydrogen, loweralkyl, hydroxyl, halogen, loweralkoxy, CF.sub.3, NO.sub.2 and amino; n is an integer of 1 to 4, with the further proviso that R.sub.2 is not loweralkyl when R.sub.1 is hydrogen or acyl and X is chloro; the pharmaceutically acceptable acid addition salts thereof and where appropriate the geometric isomers, the stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic and antipsychotic agents.
REFERENCES:
patent: 3501482 (1970-03-01), Le Von
patent: 4549023 (1985-10-01), Ibuki et al.
patent: 4710573 (1987-12-01), Strupczewski
patent: 4775761 (1988-10-01), Strupczewski
March, Advanced Org. Chem. 3rd Edition, pp. 815-816.
Bordeau Kenneth J.
Strupczewski Joseph T.
Hoechst-Roussel Pharmaceuticals Incorporated
Korsen Elliott
Shen Cecilia
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