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US4070465A
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Various 2-(substituted piperazinyl)-1H-benz [de]isoquinoline-1,3 (2H) -diones
Assignee: ER Squibb and Sons LLC
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Filing: 1976-06-24
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Granted: 1978-01-24
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Expires: 1996-06-24
Abstract
Abstract Compounds of the following formula and their acid addition salts ##STR1## Z is ##STR2## A is straight or branched chain alkylene of 2 to 6 carbons; B is straight chain alkylene of 2 to 4 carbons; X is straight or branched chain alkyl of 1 to 8 carbons, phenyl, benzyl, phenethyl, substituted phenyl, substituted benzyl, or substituted phenethyl, R 1 and R 2 are located at the 7 or 8 and 5 or 6 position respectively and are independently selected from the group consisting of hydrogen, straight or branched chain alkyl of 1 to 4 carbons, straight or branched chain alkoxy of 1 to 4 carbons, Cl, Br, F, amino, nitro, CF 3 , and cyano; are disclosed. These compounds possess antiprotozoal activity.
Inventors
- 👤 Peter C. Wade
- 👤 Berthold Richard Vogt
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 17:37
CPC Classifications
C; C07; C07D; C07D221/00; C07D221/02; C07D221/04; C07D221/06; C07D221/14
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
159 words
A compound of the formula: ##STR47## wherein Z is ##STR48## A is straight or branched chain alkylene of 2 to 6 carbons; B is straight chain alkylene of 2 to 4 carbons; X is straight or branched chain alkyl of 1 to 8 carbons, phenyl, benzyl, phenethyl, substituted phenyl, substituted benzyl or substituted phenethyl wherein said phenyl ring substituent is straight or branched chain alkyl of 1 to 4 carbons, straight or branched chain alkoxy of 1 to 4 carbons, Cl, Br, F, CF 3 , nitro, di(Cl), di(Br), di(methyl), di(methoxy), or tri(methoxy); R 1 and R 2 are located at the 7 or 8 and 5 or 6 position respectively and are independently selected from the group consisting of hydrogen, straight or branched chain alkyl of 1 to 4 carbons straight or branched chain alkoxy of 1 to 4 carbons Cl, Br, F, amino, nitro, CF 3 , and cyano; and a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
159 words
A compound of the formula: ##STR47## wherein Z is ##STR48## A is straight or branched chain alkylene of 2 to 6 carbons; B is straight chain alkylene of 2 to 4 carbons; X is straight or branched chain alkyl of 1 to 8 carbons, phenyl, benzyl, phenethyl, substituted phenyl, substituted benzyl or substituted phenethyl wherein said phenyl ring substituent is straight or branched chain alkyl of 1 to 4 carbons, straight or branched chain alkoxy of 1 to 4 carbons, Cl, Br, F, CF 3 , nitro, di(Cl), di(Br), di(methyl), di(methoxy), or tri(methoxy); R 1 and R 2 are located at the 7 or 8 and 5 or 6 position respectively and are independently selected from the group consisting of hydrogen, straight or branched chain alkyl of 1 to 4 carbons straight or branched chain alkoxy of 1 to 4 carbons Cl, Br, F, amino, nitro, CF 3 , and cyano; and a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
39 words
The compound of claim 1 wherein R 1 and R 2 are independently selected from the group consisting of hydrogen, methyl, methoxy, Cl, Br, and F; and A is straight or branched chain alkylene of 2 to 4 carbons.
Claim 4
Dependent Claim
9 words
The compound of claim 2 wherein Z is ##STR49##
Claim 5
Dependent Claim
25 words
The compound of claim 3 wherein R 1 and R 2 are both hydrogen and A is straight chain alkylene of 2 to 4 carbons.
Claim 6
Dependent Claim
7 words
The compound of claim 4, 2-[2-[4-(2-hydroxyethyl)-1-piperazinyl]ethyl]-1H-benz[de]isoquinoline-1,3(2H)-dione, hydrochloride.
Claim 7
Dependent Claim
9 words
The compound of claim 2 wherein Z is ##STR50##
Claim 8
Dependent Claim
25 words
The compound of claim 6 wherein R 1 and R 2 are both hydrogen and A is straight chain alkylene of 2 to 4 carbons.
Claim 9
Dependent Claim
7 words
The compound of claim 7, 2-[2-[4-(3,4,5-trimethoxybenzoyl)-1-piperazinyl]ethyl]-1H-benz[de]isoquinoline-1,3(2H)-dione, hydrochloride.
Claim 10
Dependent Claim
7 words
The compound of claim 7, 2-[2-[4-(1-oxo-2-propylpentyl)-1-piperazinyl]ethyl]-1H-benz[de]isoquinoline-1,3(2H)-dione, hydrochloride.
Claim 11
Dependent Claim
26 words
A pharmaceutical composition useful for treating mammals having a protozoa infection comprising a compound or mixture of compounds of claim 1 and a pharmaceutically acceptable carrier.
Claim 12
Dependent Claim
21 words
The method of treating a mammal having a protozoa infection comprising administering an effective amount of the compound of claim 10.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-01-23 | 1981-07-25 | 1982-01-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-01-23 | 1985-07-25 | 1986-01-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-01-23 | 1989-07-25 | 1990-01-24 | $7700.00 | Window Closed / Lapsed |