| Title of Invention | NOVEL COMPLEXES OF LHRH ANTAGONISTS WITH POLYAMINO ACID. |
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| Abstract | IN THIS INVENTION, A RELEASE-DELAYING SYSTEM IS TO BE DEVELOPED FOR LHRN ANTAGONISTS, IN PARTICULAR FOR CETRORELIX, WHICH ALLOWS THE ACTIVE COMPOUND TO BE RELEASED IN A CONTROLLED MANNER OVER SEVERAL WEEKS BY COMPLEXATION WITH SUITABLE BIOPHILIC CARRIERS. THE ACIDIC POLYGLUTAMIC ACID AND POLYASPARTIC ACID WERE SELECTED FOR COMPLEXATION WITH CETRORELIX. THE CETRORELIX POLYAMINO ACID COMPLEXES ARE PREPARED FROM AQUEOUS SOLUTIONS BY COMBINATION OF THE SOLUTIONS AND PRECIPITATION OF THE COMPLEXES, WHICH ARE SUBSEQUENTLY CENTRIFUGED OFF AND DRIED OVER p205 IN VACUO. IF COMPLEXES HAVING A DEFINED COMPOSITION ARE TO BE OBTAINED, LYOPHILIZATION PROVES TO BE A SUITABLE METHOD. THE CETRORELIX-CARBOXYLIC ACID COMPLEXES WERE ALSO PREPARED FROM THE AQUEOUS SOLUTIONS. IN THE RANDOM LIBERATION SYSTEM, THE ACIDIC POLYAMINO ACIDS POLY-GLU AND POLY-ASP SHOWED GOOD RELEASE-DELAYING PROPERTIES AS A FUNCTION OF THE HYDROPHOBICITY AND THE MOLECULAR MASS OF THE POLYAMINO ACID. IN ANIMAL EXPERIMENTS, IT WAS POSSIBLE TO CONFIRM THE ACITIVITY OF THE CETRORELIX-POLYAMINO ACID COMPLEXES AS A DEPOT SYSTEM IN PRINCIPLE. IT IS THUS POSSIBLE BY COMPLEXATION OF CETRORELIX WITH POLYAMINO ACIDS TO ACHIEVE TESTOSTERONE SUPPERSSION IN MALE RATS OVER 600 HOURS. THE RELEASE OF ACTIVE COMPOUND HERE CAN BE CONTROLLED BY THE NATURE AND THE MOLECULAR MASS OF THE POLYMERS. |
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480-cal-1998-granted-abstract.pdf
480-cal-1998-granted-claims.pdf
480-cal-1998-granted-correspondence.pdf
480-cal-1998-granted-description (complete).pdf
480-cal-1998-granted-drawings.pdf
480-cal-1998-granted-form 1.pdf
480-cal-1998-granted-form 18.pdf
480-cal-1998-granted-form 2.pdf
480-cal-1998-granted-form 3.pdf
480-cal-1998-granted-form 5.pdf
480-cal-1998-granted-letter patent.pdf
480-cal-1998-granted-priority document.pdf
480-cal-1998-granted-reply to examination report.pdf
480-cal-1998-granted-specification.pdf
480-cal-1998-granted-translated copy of priority document.pdf
| Patent Number | 212139 | |||||||||||||||||||||
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| Indian Patent Application Number | 480/CAL/1998 | |||||||||||||||||||||
| PG Journal Number | 47/2007 | |||||||||||||||||||||
| Publication Date | 23-Nov-2007 | |||||||||||||||||||||
| Grant Date | 20-Nov-2007 | |||||||||||||||||||||
| Date of Filing | 23-Mar-1998 | |||||||||||||||||||||
| Name of Patentee | ZENTARIS GMBH | |||||||||||||||||||||
| Applicant Address | WEISMULLERSTRASSE 45, 60314 FRANKFURT/MAIN | |||||||||||||||||||||
Inventors:
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| PCT International Classification Number | A61K 47/48 | |||||||||||||||||||||
| PCT International Application Number | N/A | |||||||||||||||||||||
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PCT Conventions:
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