.

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: 5,212,303

« Back to Dashboard

Details for Patent: 5,212,303

Title: Benzonaphthalene derivatives, a process for their preparation and their use in therapeutic and cosmetic compositions
Abstract:A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents (i) ##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 --0--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 acitivity.
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:Sep 28, 1992
Application Number:07/952,341
Claims:1. A process for preparing a compound having the formula ##STR11## comprising coupling, in an anhydrous solvent and in the presence of, as a reaction catalyst, a transition metal or a complex thereof, a magnesium, lithium or zinc derivative of a compound of the formula ##STR12## with a halogenated naphthalene compound of the formula ##STR13## wherein R.sub.1 represents (i) ##STR14## or (ii) --CH.sub.2 OH, R.sub.6 represents ##STR15## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' and R" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or an amino sugar selected from the group consisting of glucosamine, galactosamine and mannosamine, or 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 having 1-4 carbon atoms, 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, and

X and Y represent Cl, Br, F or I.

2. The process of claim 1 carried out at a temperature ranging from -20.degree. to +30.degree. C.
« 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