.

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: 7,692,028

« Back to Dashboard

Details for Patent: 7,692,028

Title:2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses
Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, ##STR00001## wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.
Inventor(s): Differding; Edmond (Louvain-la-Neuve, BE), Kenda; Beno t (Emines, BE), Lallemand; Benedicte (Waimes, BE), Matagne; Alain (Gerpinnes, BE), Michel; Philippe (Beersel, BE), Pasau; Patrick (Chastre, BE), Talaga; Patrice (Watermael-Boitsfort, BE)
Assignee: UCB Pharma, S.A. (Brussels, BE)
Filing Date:Dec 13, 2007
Application Number:12/000,512
Claims:1. A compound of formula (AA-XIX) ##STR00072## wherein X is --CA.sup.1NR.sup.5R.sup.6, --CA.sup.1OR.sup.7, --CA.sup.1-R.sup.8 or --CN; A.sup.1 is oxygen, sulfur or --NR.sup.9; R.sup.1 is hydrogen, alkyl, aryl or --CH.sub.2--R.sup.1a wherein R.sup.1a is aryl, halogen, hydroxy, amino, nitro or cyano; R.sup.2 and R.sup.4 are hydrogen; R.sup.3 is halogen, thiol, nitro, nitrooxy, cyano, azido, carboxy, amido, sulfonic acid, sulfonamide, alkyl, alkenyl, alkynyl, ester, ether, aryl, tetrazolyl, thiazolyl, thienyl, furyl, pyrrolyl, pyridinyl, alkynyloxy, acyloxy, oxyester, oxyamido, alkylsulfonyloxy, alkylsulfinyloxy, arylsulfonyloxy, arylsulfinyloxy, aryloxy, aralkoxy, alkylthio, alkenylthio, alkynylthio, arylthio, formyl, acetyl, propionyl, isobutyryl, valeryl, lauroyl, heptanedioyl, cyclohexanecarbonyl, crotonoyl, furmaroyl, acyloyl, benzoyl, naphtoyl, 4-carboxybutanoyl, oxalyl, ethoxalyl, cysteinyl, oxamoyl, alkylsulfonyl, alkenylsulfonyl, alkynylsulfonyl, arylsulfonyl, alkylsulfinyl, alkenylsulfinyl, alkynylsulfinyl or arylsulfinyl; R.sup.5, R.sup.6, R.sup.7 and R.sup.9 are the same or different and each is independently hydrogen, hydroxy, alkyl, aryl, alkoxy, alkenyloxy, alkynyloxy, acyloxy, oxyester, oxyamido, alkylsulfonyloxy, alkylsulfinyloxy, arylsulfonyloxy, arylsulfinyloxy, aryloxy or arylakoxy; and R.sup.8 is hydrogen, hydroxy, thiol, halogen, alkyl, aryl, alkylthio, alkenylthio, or alkynylthio.

2. A compound of formula (AA-XIX) according to claim 1 wherein X is --CA.sup.1NR.sup.5R.sup.6; A.sup.1 is oxygen; R.sup.1 is alkyl; R.sup.2 and R.sup.4 are hydrogen; R.sup.3 is alkyl; and R.sup.5 and R.sup.6 are hydrogen.

3. A compound of formula (AA-XIX) according to claim 1 wherein when the carbon atom to which R.sup.1 is attached is asymmetric, said carbon atom is in the "S"-configuration.

4. A method of preparation of compound of formula (I) ##STR00073## wherein X is --CA.sup.1NR.sup.5R.sup.6, --CA.sup.1OR.sup.7, --CA.sup.1-R.sup.8 or --CN; A.sup.1 is oxygen, sulfur or --NR.sup.9; R.sup.1 is hydrogen, alkyl, aryl or --CH.sub.2--R.sup.1a wherein R.sup.1a is aryl, halogen, hydroxy, amino, nitro or cyano; R.sup.3 is halogen, thiol, nitro, nitrooxy, cyano, azido, carboxy, amido, sulfonic acid, sulfonamide, alkyl, alkenyl, alkynyl, ester, ether, aryl, tetrazolyl, thiazolyl, thienyl, furyl, pyrrolyl, pyridinyl, alkynyloxy, acyloxy, oxyester, oxyamido, alkylsulfonyloxy, alkylsulfinyloxy, arylsulfonyloxy, arylsulfinyloxy, aryloxy, aralkoxy, alkylthio, alkenylthio, alkynylthio, arylthio, formyl, acetyl, propionyl, isobutyryl, valeryl, lauroyl, heptanedioyl, cyclohexanecarbonyl, crotonoyl, furmaroyl, acyloyl, benzoyl, naphtoyl, 4-carboxybutanoyl, oxalyl, ethoxalyl, cysteinyl, oxamoyl, alkylsulfonyl, alkenylsulfonyl, alkynylsulfonyl, arylsulfonyl, alkylsulfinyl, alkenylsulfinyl, alkynylsulfinyl or arylsulfinyl; R.sup.3a is hydrogen; R.sup.5, R.sup.6, R.sup.7 and R.sup.9 are the same or different and each is independently hydrogen, hydroxy, alkyl, aryl, alkoxy, alkenyloxy, alkynyloxy, acyloxy, oxyester, oxyamido, alkylsulfonyloxy, alkylsulfinyloxy, arylsulfonyloxy, arylsulfinyloxy, aryloxy or arylakoxy; and R.sup.8 is hydrogen, hydroxy, thiol, halogen, alkyl, aryl, alkylthio, or alkenylthio, alkynylthio; with the proviso that when the compound is a mixture of all possible isomers, X is --CONR.sup.5R.sup.6 and R.sup.1 is hydrogen, methyl, ethyl or propyl then R.sup.3 and R.sup.3a substitution is other than mono-, di-methyl or mono-ethyl; and that when R.sup.1 and R.sup.3a are both hydrogen and X is --CONR.sup.5R.sup.6 then R.sup.3 is different from carboxy, ester, amido, substituted oxo-pyrrolidine, alkynyloxy, acyloxy, oxyester, oxyamido, alkylsulfonyloxy, alkylsulfinyloxy, arylsulfonyloxy, arylsulfinyloxy, aryloxy, aralkoxy, methyl, naphtyl, phenyl optionally substituted by oxy derivatives or in the para position by an halogen atom; which comprises reduction of a compound of formula (AA-XIX) ##STR00074## .sup.4 according to claim 1.

5. The method of preparation of compound of formula (I) according to claim 4 wherein the reduction is performed in the presence of Pd/C.
« 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