Benzimidazolone derivatives with central dopaminergic activity
First Claim
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1. A compound of the formula ##STR4## wherein X1, X2 and X3 are independently selected from carbon and nitrogen;
- R0, R1 and R2 are independently selected from hydrogen, halo, (C1 -C6)alkyl optionally substituted with from one to three fluorine atoms and (C1 -C6)alkoxy optionally substituted with from one to three fluorine atoms;
R3 is hydrogen, (C1 -C6)alkyl or benzyl, wherein the phenyl moiety of said benzyl group may optionally be substituted with from one or more substituents, independently selected from halo, cyano, (C1 -C6)alkyl optionally substituted with from one to three fluorine atoms, (C1 -C6)alkoxy optionally substituted with from one to three fluorine atoms, (C1 -C6)alkylsulfonyl, (C1 -C6)alkylamino, amino, di-(C1 -C6)alkylamino and (C1 -C6)carboxamido;
R4, R5 and R6 are independently selected from hydrogen, halo, cyano, (C1 -C6)alkyl optionally substituted with from one to three fluorine atoms, (C1 -C6)alkoxy optionally substituted with from one to three fluorine atoms, (C1 -C6)alkylsulfonyl, (C1 -C6)acylamino, (phenyl) (C1 -C6)acyl!amino, amino, (C1 -C6)alkylamino and di-(C1 -C6)alkylamino; and
the dashed line represents an optional double bond;
with the proviso that when X3 is nitrogen, R2 is absent;
or a pharmaceutically acceptable salt thereof.
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Abstract
This invention relates to novel, pharmaceutically active benzimidazolone derivatives of the formula ##STR1## wherein the dashed line, R0 through R6 and X1 through X3 are defined as in the specification. These compounds exhibit central dopaminergic activity and are u in the treatment of CNS disorders.
66 Citations
15 Claims
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1. A compound of the formula ##STR4## wherein X1, X2 and X3 are independently selected from carbon and nitrogen;
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R0, R1 and R2 are independently selected from hydrogen, halo, (C1 -C6)alkyl optionally substituted with from one to three fluorine atoms and (C1 -C6)alkoxy optionally substituted with from one to three fluorine atoms; R3 is hydrogen, (C1 -C6)alkyl or benzyl, wherein the phenyl moiety of said benzyl group may optionally be substituted with from one or more substituents, independently selected from halo, cyano, (C1 -C6)alkyl optionally substituted with from one to three fluorine atoms, (C1 -C6)alkoxy optionally substituted with from one to three fluorine atoms, (C1 -C6)alkylsulfonyl, (C1 -C6)alkylamino, amino, di-(C1 -C6)alkylamino and (C1 -C6)carboxamido; R4, R5 and R6 are independently selected from hydrogen, halo, cyano, (C1 -C6)alkyl optionally substituted with from one to three fluorine atoms, (C1 -C6)alkoxy optionally substituted with from one to three fluorine atoms, (C1 -C6)alkylsulfonyl, (C1 -C6)acylamino, (phenyl) (C1 -C6)acyl!amino, amino, (C1 -C6)alkylamino and di-(C1 -C6)alkylamino; and the dashed line represents an optional double bond; with the proviso that when X3 is nitrogen, R2 is absent; or a pharmaceutically acceptable salt thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15)
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Specification