US4757074A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Piperazinyl benzyl acids having antihistamine activity
Assignee: SmithKline Beecham Corp
•
Filing: 1986-02-24
•
Granted: 1988-07-12
•
Expires: 2006-02-24
Abstract
Abstract The present invention provides compounds of the formula (I): ##STR1## or salts, esters or amide derivatives thereof, wherein R 1 is --CO 2 H, --CH═CH--CO 2 H, --(CH 2 ) n CO 2 H, or --O--(CH 2 ) n CO 2 H (n=1 to 4); R 2 is C 1 ∝ alkyl or benzyl which is optionally substituted by a C 1-4 alkyl group or groups; R 3 is C 1-4 alkoxy, C 1-4 alkyl or halogen. Also provided are pharmaceutical formulations containing the compounds of the formula (I) and methods for the preparation of the compounds. The above mentioned compounds have antihistaminic activity.
Inventors
- 👤 Geoffrey G. Coker
- 👤 John W. A. Findlay
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 16:58
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/04; C07D295/08; C07D295/096; A; A61; A61P; A61P43/00; C07D295/14; C07D295/155
Claims Analysis
Total Claims: 4
Claim 1
Independent Claim
34 words
A compound selected from the group comprising: (E)-3-(4-chloro-α-(4-methyl-1-piperazinyl)benzyl)-cinnamic acid; 3-(4-chloro-α-(4-methyl-1-piperazinyl)benzyl)benzoic acid; 2-(4-chloro-α-(4-methyl-1-piperazinyl)benzyl)benzoic acid; 4-(4-chloro-α-(4-methyl-1-piperazinyl)benzyl)benzoic acid; 3-(4-methoxy-α-(4-methyl-1-piperazinyl)benzyl)benzoic acid; 3-(4-chloro-α-(4-methyl-1-piperazinyl)benzyl)phenoxyacetic acid; 3-(4-chloro-α-(4-(3-methylbenzyl)-1-piperazinyl)benzyl)phenoxyacetic acid; 3-(4-chloro-α-(4-(4-tert-butylbenzyl-1-piperazinyl)benzyl phenoxyacetic acid; and pharmaceutically acceptable acid addition salt, esters and amides thereof.
Claim 2
Dependent Claim
34 words
A compound selected from the group comprising: (E)-3-(4-chloro-α-(4-methyl-1-piperazinyl)benzyl)-cinnamic acid; 3-(4-chloro-α-(4-methyl-1-piperazinyl)benzyl)benzoic acid; 2-(4-chloro-α-(4-methyl-1-piperazinyl)benzyl)benzoic acid; 4-(4-chloro-α-(4-methyl-1-piperazinyl)benzyl)benzoic acid; 3-(4-methoxy-α-(4-methyl-1-piperazinyl)benzyl)benzoic acid; 3-(4-chloro-α-(4-methyl-1-piperazinyl)benzyl)phenoxyacetic acid; 3-(4-chloro-α-(4-(3-methylbenzyl)-1-piperazinyl)benzyl)phenoxyacetic acid; 3-(4-chloro-α-(4-(4-tert-butylbenzyl-1-piperazinyl)benzyl phenoxyacetic acid; and pharmaceutically acceptable acid addition salt, esters and amides thereof.
Claim 3
Dependent Claim
35 words
A method of treating a human having elevated histamine levels which comprises administering to said human an effective antihistamine amount of the compound, pharmaceutically acceptable salt, ester or amide of claim 1 to said human.
Claim 4
Dependent Claim
36 words
A method of treating a human having elevated histamine levels which comprises administering to said human an effective antihistamine amount of the compound or a pharmaceutically acceptable acid addition salt of claim 1 to said human.
References Cited (Backward Citations)
US2709169A
Cited
US2630435A
Cited
US2636032A
Cited
US2861072A
Cited
GB980251A
Cited
US3868377A
Cited
GB1528862A
Cited
US4146582A
Cited
EP0058146A1
Cited
US4397855A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-07-12 | 1992-01-11 | 1992-07-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-07-12 | 1996-01-11 | 1996-07-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-07-12 | 2000-01-11 | 2000-07-12 | $7700.00 | Window Closed / Lapsed |