.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 5,677,451

« Back to Dashboard

Details for Patent: 5,677,451

Title: Disubstituted acetylenes bearing heterobicyclic groups and heteroaromatic or phenyl groups having retinoid like activity
Abstract:Compounds of the formula ##STR1## where R.sub.1 and R.sub.2, independently are alkyl groups having 2 to 8 carbons; R.sub.3 is hydrogen or lower alkyl; X is S, O or N-R.sub.4 where R.sub.4 is hydrogen or lower alkyl; Y is phenyl or pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH.sub.2).sub.n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub. 2OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR11OR.sub.10 O, where R.sub.5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.8 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.9 is lower alkyl, R.sub.10 is divalent alkyl radical of 2-5 carbons and R.sub.11 is alkyl, cycloalkyl or alkenyl containing 1 to 5 carbons, have retinoic acid like activity.
Inventor(s): Chandraratna; Roshantha A. S. (El Toro, CA)
Assignee: Allergan (Waco, TX)
Filing Date:Jun 06, 1995
Application Number:08/466,003
Claims:1. A compound of the formula ##STR11## wherein R.sub.1 and R.sub.2, independently are n-alkyl groups having 2 to 8 carbons, or cyclo or branch-chained alkyl groups of 3 to 8 carbons;

R.sub.3 is hydrogen or lower alkyl;

X is S, O or N-R.sub.4 where R.sub.4 is hydrogen or lower alkyl;

Y is phenyl or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl;

A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3 to 6 carbons, cycloalkyl having 3 to 6 carbons, alkenyl having 2 to 6 carbons and I or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds;

B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub.2 OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR.sub.11 OR.sub.10 O, where R.sub.5 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.8 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.9 is lower alkyl, R.sub.10 is divalent alkyl radical of 2-5 carbons and R.sub.11 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons.

2. A compound in accordance with claim 1 where X is NH.

3. A compound in accordance with claim 1 where X the R.sub.1 and R.sub.2 groups are identical with one another.

4. A compound in accordance with claim 1 where the R.sub.1 and R.sub.2 groups are both n-alkyl.

5. A compound in accordance with claim 1 where Y is selected from a group consisting of [pyridyl,] thienyl, furyl.

6. A compound in accordance with claim 5 where Y is selected from a group consisting of pyridyl and thienyl.

7. A compound of the formula ##STR12## where R.sub.1 and R.sub.2, independently are n-alkyl groups having 2 to 8 carbons;

R.sub.3 is hydrogen or lower alkyl;

Z is S or O;

A is (CH.sub.2).sub.n where n is 0-5, and

B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub.2 OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR.sub.11 OR.sub.10 O, where R.sub.5 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.8 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.9 is lower alkyl, R10 is divalent alkyl radical of 2-5 carbons and R.sub.11 is an alkyl, cycloalkyl or alkenyl group containing i to 5 carbons.

8. A compound in accordance with claim 7 where A is (CH.sub.2).sub.n and where n is 0.

9. A compound in accordance with claim 8 where B is COOH, COOR.sub.5, CONR.sub.6 R.sub.7 or a pharmaceutically. acceptable salt thereof.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc