US5354776A
Expired / Lapsed
US
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Acetylenes disubstituted with a heteroaromatic group and a tetralin group and having retinoid-like activity
Assignee: Acuityads Us Inc
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Filing: 1993-06-29
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Granted: 1994-10-11
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Expires: 2013-06-29
Abstract
Abstract Retinoid-like activity is exhibited by compounds of the formula ##STR1## where R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH or an ester or amide thereof, --CH 2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR 1 or a ketal derivative thereof where R 1 is --(CH 2 ) m CH 3 where m is 0-4; or a pharmaceutically acceptable salt thereof.
Inventors
- 👤 Roshantha A. S. Chandraratna
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 18:16
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/06; C07D213/60; C07D213/78; C07D213/79; C07D213/80; A; A61; A61P; A61P17/00; A61P27/00; A61P27/02; A61P27/14; A61P29/00; A61P37/00; A61P37/08
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
84 words
A compound of the formula ##STR6## where R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH 2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR 1 or a ketal derivative thereof where R 1 is -(CH 2 ) m CH 3 where m is 0-4; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
84 words
A compound of the formula ##STR6## where R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH 2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR 1 or a ketal derivative thereof where R 1 is -(CH 2 ) m CH 3 where m is 0-4; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
21 words
The compound of claim 1 where R is hydrogen or methyl, n is 0, 1 or 2 and A is furyl.
Claim 4
Dependent Claim
18 words
The compound of claim 2 where B is --COOH or a pharmaceutically acceptable salt, ester or amide thereof.
Claim 5
Dependent Claim
87 words
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula ##STR7## where R is hydrogen or lower alkyl; A is furyl; n is 0-5; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH 2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR 1 or a ketal derivative thereof where R 1 is --(CH 2 ) m CH 3 where m is 0-4; or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim
87 words
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula ##STR7## where R is hydrogen or lower alkyl; A is furyl; n is 0-5; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH 2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR 1 or a ketal derivative thereof where R 1 is --(CH 2 ) m CH 3 where m is 0-4; or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
12 words
A composition according to claim 4 having anti-psoriatic activity in a mammal.
Claim 8
Independent Claim
104 words
A method for treating psoriasis in a mammal which method comprises administering alone or in conjunction with a pharmaceutically acceptable excipient, a therapeutically effective amount of a compound of the formula ##STR8## where R is hydrogen or lower alkyl; A is furyl; n is 0-5; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH 2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR 1 or a ketal derivative thereof where R 1 is --(CH 2 ) m CH 3 where m is 0-4; or a pharmaceutically acceptable salt thereof.
Claim 9
Independent Claim
104 words
A method for treating psoriasis in a mammal which method comprises administering alone or in conjunction with a pharmaceutically acceptable excipient, a therapeutically effective amount of a compound of the formula ##STR8## where R is hydrogen or lower alkyl; A is furyl; n is 0-5; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH 2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR 1 or a ketal derivative thereof where R 1 is --(CH 2 ) m CH 3 where m is 0-4; or a pharmaceutically acceptable salt thereof.
References Cited (Backward Citations)
US4269848A
Cited
US5248221A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1997-10-10 | 1998-04-11 | 1998-10-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-10-10 | 2002-04-11 | 2002-10-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-10-10 | 2006-04-11 | 2006-10-11 | $7700.00 | Window Closed / Lapsed |