Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...
Patent
1996-06-24
1999-03-02
Bernhardt, Emily
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitrogen attached directly or indirectly to the purine ring...
544229, 544375, 544376, 544364, 540575, 546148, 546196, 546202, 5462827, 5462831, 435140, 514218, 514253, 514320, 514324, 514319, 514337, 514345, 514352, A61K 31495, C07D40506, C07D40514, C07F 710
Patent
active
058773177
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
1. Field of the Invention
The invention relates to Isochroman-alkyl-piperazinyl-aryl compounds useful as anti-psychotic agents.
2. Description of the Related Art
Chromans (also known as 1-benzopyrans, where the oxygen atom is attached to the aromatic ring) and isochromans (also known as 2-benzopyrans, where the oxygen atom is not attached to the aromatic ring) are known in the art, as are aryl-piperazines (or aminopiperidines). Chromans and aryl piperazines linked together with an alkyl chain are also known. European Patent 300,908 discloses (1-benzopyran)!-alkyl-(piperazinyl or aminopiperidine)-aryls useful as antiarrythmics and anti-fibrillatory agents. The compounds of this invention require -alkyl-piperazinyl (or aminopiperidinyl)-aryl at carbon 1 of an 2- benzopyran ring which are useful for CNS and cardiovascular disorders.
Various isochromans, thioisochromans, benzoxepines, and benzothiepines with hydroxy, alkoxy, or o-methylenedioxy substitution on their aromatic rings, and linked to aryl piperazines(piperidines) by alkyl chains are known. These compounds are disclosed as being useful as antipsychotics and hypotensives. The compounds of this invention do not permit oxygen substitution on the aromatic ring of the isochroman, thioisochroman, benzoxepin, or benzothiepin ring system for their usefulness in CNS and cardiovascular disorders.
Another group of isochromans, thioisochromans, benzoxepines and benzothiepines with hydroxy, alkoxy, or o-methylenedioxy functionality attached to their aromatic rings, and linked to aryl piperazines(piperidines) by alkyl chains are known, useful as antipsychotics and hypotensives. The compounds of this invention do not permit oxygen substitution on the aromatic ring of the isochroman, thioisochroman, benzoxepin, or benzothiepin ring system for their usefulness in CNS and cardiovascular disorders.
U.S. Pat. No. 4,179,510 and the many divisionals thereof discloses isochromanalkyl-piperazinyl (or aminopiperidinyl)-aryls requiring oxygen as a substituent on the isochroman aromatic ring. These compounds are disclosed as being useful as hypotensive and antipsychotic agents.
Also disclosed are isochroman-, isothiochroman-, 2-benzoxepin-, and -2-benzothiepin-alkyloxyethanols as being useful for preparing the above compounds. More specifically 7,8-dimethoxybenzoxepines are disclosed as disclosed are 2-benzoxepine-alkyl-piperazine(aminopiperidine)-aryls, 2-benzothiepins and 2-benzoxepines all requiring an oxygen atom as a substituent on the aromatic ring and useful for the same purposes.
Dutch Patent 8,001,981 discloses l)ethyl!piperazine useful as an antipsychotic agent.
International Patent Publication WO 9218089 discloses isochroman-alkyl-piperazinyl (aminopiperidinyl)-aryls, with the requirement that oxygen be present on the aromatic ring of the isochroman which are useful in sensitizing cells against multi-drug resistance.
International Patent Publication WO 8808424 discloses isochromans-alkyl-piperazinyl (or aminopiperidinyl)-aryls, with the requirement that oxygen be present on the aromatic ring of the isochroman, useful in the treatment of head injury, spinal trauma, and stroke.
International Patent Publication WO 9015056 and U.S. Pat. No. 5,140,040 disclose isochromans, tetralins, and dihydroanaphthalenes substituted with various alkyl amines for the treatment of glaucoma, depression, hypertension, congestive heart failure and vascular spastic conditions.
U.S. Pat. No. 4,994,486 discloses isochroman-alkyl-amines for treating psychoses, Parkinson's disease, and addictive behavior.
Japanese Patent 61083180 discloses isochroman-alkyl-(alkyl)amines as antiulcer agents.
European Patent 404,197 discloses isochroman-alkyl-piperazine-alkyl-keto (alcohol)-aryls with bronchodilator and antiallergy activity.
Japanese Patent 51125287 (J 52083846) discloses isochroman-alkyl-amines(piperazine) with antidepressive, analgesic, diuretic, antiinflammatory, and anti-asthma activity.
German Patent DE 2,624,693 and Great Britain Patent GB 1552004 discloses is
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Ennis Michael D.
Lahti Robert A.
TenBrink Ruth E.
Bernhardt Emily
Pharmacia & Upjohn Company
Stein Bruce
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