Method of treating anxiety and depression with 1-phenyl-2(1H,3H)-indolone psycho-therapeutic agents
First Claim
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1. A method of treating anxiety in a hyperanxious person which comprises treating said person with an anxiolytic amount of a compound of the formula ##STR8## wherein, in a first alternative,A2 is hydrogen or methyl, and B1 and C1 are each independently hydrogen, (C1 -C2)alkyl, phenyl or benzyl;
- in a second alternative,A2 is hydrogen or methyl, and B1 and C1 together with the nitrogen atom to which they are attached form a piperidine, pyrrolidine, morpholine or imidazole ring;
in a third alternative,A2 and B1 together are 1,3-propylene, 1,4-butylene or 1,5-pentylene, and C1 is hydrogen, (C1 -C2)alkyl, phenyl or benzyl;
W is hydrogen, (C1 -C2)alkyl, (C1 -C2)alkoxy, chloro or fluoro;
W1, X1 and Y1 are each independently hydrogen, (C1 -C2)alkyl, (C1 -C2)alkoxy, (C1 -C2)alkylthio, bromo, chloro, fluoro, trifluoromethyl, hydroxy, formyl, carboxamido, (C1 -C2)alkylcarboxamido, di(C1 -C2)alkylcarboxamido, cyano, nitro, amino, (C1 -C2)alkylamino or di(C1 -C2)alkylamino;
with the proviso that when A2 is hydrogen or methyl, B1 and C1 are each independently hydrogen, (C1 -C2)alkyl, phenyl or benzyl, and any one of W1, X1 and Y1 is 4-chloro, at least one of W1, X1 and Y1 is other than hydrogen.
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Abstract
Certain substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones are highly potent gabaergic agents, valuable in the treatment of individuals suffering from schizophrenia or reversing the side effects of a previously or concurrently administered neuroleptic agent; or in the treatment of epilepsy. A wider class of substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones, together with 1-phenyl-3-(2-pyrrolidinylidene)-2(1H,3H)-indolones, and homologs thereof, are valuable in the treatment of anxiety.
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Citations
14 Claims
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1. A method of treating anxiety in a hyperanxious person which comprises treating said person with an anxiolytic amount of a compound of the formula ##STR8## wherein, in a first alternative,
A2 is hydrogen or methyl, and B1 and C1 are each independently hydrogen, (C1 -C2)alkyl, phenyl or benzyl; -
in a second alternative, A2 is hydrogen or methyl, and B1 and C1 together with the nitrogen atom to which they are attached form a piperidine, pyrrolidine, morpholine or imidazole ring; in a third alternative, A2 and B1 together are 1,3-propylene, 1,4-butylene or 1,5-pentylene, and C1 is hydrogen, (C1 -C2)alkyl, phenyl or benzyl; W is hydrogen, (C1 -C2)alkyl, (C1 -C2)alkoxy, chloro or fluoro; W1, X1 and Y1 are each independently hydrogen, (C1 -C2)alkyl, (C1 -C2)alkoxy, (C1 -C2)alkylthio, bromo, chloro, fluoro, trifluoromethyl, hydroxy, formyl, carboxamido, (C1 -C2)alkylcarboxamido, di(C1 -C2)alkylcarboxamido, cyano, nitro, amino, (C1 -C2)alkylamino or di(C1 -C2)alkylamino; with the proviso that when A2 is hydrogen or methyl, B1 and C1 are each independently hydrogen, (C1 -C2)alkyl, phenyl or benzyl, and any one of W1, X1 and Y1 is 4-chloro, at least one of W1, X1 and Y1 is other than hydrogen. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
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13. A method of treating a person suffering from depression which comprises administration to said person 1-(4-methoxyphenyl-3-(1-methyl-2-pyrrolidinylidene-2(1H,3H)-indolone or a pharmaceutically acceptable salt thereof in an amount sufficient to alleviate said depression.
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14. A method of treating a person suffering from epileptic seuzures which comprises administrating to said person an epileptic seizure preventing amount of 1-(4-methoxyphenyl)-3-(1-methyl-2-pyrrolidinylidene)-2-(1H,3H)-indolone or a pharmaceutically acceptable salt thereof.
Specification
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Current AssigneePfizer Inc.
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Original AssigneePfizer Inc.
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InventorsHoward, Harry R. Jr., Sarges, Reinhard
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Primary Examiner(s)Cashion, Jr., Merrell C.
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Assistant Examiner(s)Kishore, G. S.
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Application NumberUS07/382,614Time in Patent Office510 DaysField of Search514/415, 514/418, 548/486US Class Current514/418CPC Class CodesC07C 43/225 containing halogenC07D 209/08 with only hydrogen atoms or...C07D 209/34 in position 2C07D 209/38 in positions 2 and 3, e.g. ...
