.

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: 5,183,889

« Back to Dashboard

Details for Patent: 5,183,889

Title: Benzonaphtahalene derivatives, a process for their preparation and their use in therapeutic and cosmetic compositions
Abstract:A benzonphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy. This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjuctive tissues. The compound also possesses anti-tumor activity.
Inventor(s): Shroot; Braham (Antibes, FR), Eustache; Jacques (Grasse, FR), Bernardon; Jean-Michel (Nice, FR)
Assignee: Centre International de Recherches Dermatologiques (CIRD) (Valbonne, FR)
Filing Date:Dec 09, 1991
Application Number:07/803,965
Claims:1. A benzonaphthalene compound of the formula: ##STR11## wherein r' and r" taken together form a heterocycle selected from the group consisting of piperidino, piperazino, morpholino and pyrrolidino,

R.sub.2 represents hydrogen, branched or straight chain alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical,

R.sub.3 represents hydrogen, hydroxy, branched or straight chain alkyl, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical selected from the group consisting of 1-methyl cyclohexyl and 1-adamantyl, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents linear or branched lower alkyl,

R.sub.4 and R.sub.5, each independently, represent hydrogen, lower alkyl, hydroxy or lower acyloxy,

or a salt thereof.

2. The compound of claim 1 wherein said alkyl is selected from the group consisting of methyl, ethyl, isopropyl, butyl and tert.butyl.

3. The compound of claim 1 wherein said alkoxy is selected from the group consisting of methoxy, ethoxy, isopropoxy, hexyloxy and decyloxy.

4. The compound of claim 1 wherein said lower acyloxy has 1-4 carbon atoms.

5. The compound of claim 4 wherein said lower acyloxy is selected from the group consisting of acetyloxy and propionyloxy.

6. The compound of claim 1 wherein said monohydroxyalkyl has 2 or 3 carbon atoms.

7. The compound of claim 6 wherein said monohydroxyalkyl is selected from the group consisting of 2-hydroxyethyl and 2-hydroxypropyl.

8. The compound of claim 1 wherein said polyhydroxyalkyl has 3-6 carbon atoms and 2-5 hydroxy groups.

9. The compound of claim 8 wherein said polyhydroxyalkyl is selected from the group consisting of 2,3-dihydroxypropyl, 1,3-dihydroxypropyl or a residue of pentaerythritol.

10. The compound of claim 1 wherein said thiocycloaliphatic radical is 1-adamantylthio.

11. The compound of claim 1 having the formula ##STR12## wherein r' and r" taken together form a heterocycle selected from the group consisting of piperidino, piperazino, morpholino and pyrrolidino,

R'.sub.2 represents hydrogen, alkyl having 1-5 carbon atoms, alkoxy having 1-4 carbon atoms or 1-adamantyl, and

R'.sub.3 represents hydrogen, hydroxy, alkoxy having 1-10 carbon atoms, alkyl having 1-4 carbon atoms or 1-adamantylthio.

12. The compound of claim 1 which is the morpholide of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid.
« Back to Dashboard

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

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