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40 results about "Lhrh antagonist" patented technology

LHRH antagonist is a specific type of antagonist used in prostate cancer hormone therapy. LHRH antagonist mimics natural LHRH or luteinizing hormone-releasing hormone and plugs into the receptors of the pituitary gland.

Immobilized and activity-stabilized complexes of LHRH antagonists and processes for their preparation

In this invention, a release-delaying system is to be developed for LHRH 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 polyamino acids 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 P2O5 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 activity 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 suppression 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.
Owner:ZENTARIS GMBH

Process for the preparation of immobilized and activity-stabilized complexes of LHRH antagonists

In this invention, a release-delaying system is to be developed for LHRH 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 polyamino acids 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 P2O5 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 activity 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 suppression 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.
Owner:ZENTARIS GMBH

Luteinizing hormone-releasing hormone (LHRH) antagonist derivative, preparation method of LHRH antagonist derivative and application of LHRH antagonist derivative

InactiveCN102675418AGood LHRH antagonist activityLow histamine releasing activityPeptide/protein ingredientsLuteinising hormone-releasing hormoneDiseaseSexual hormones
The invention belongs to the field of medicine and chemistry and particularly relates to a luteinizing hormone-releasing hormone (LHRH) antagonist derivative which is represented as formula (I), a preparation method of the LHRH antagonist derivative and application for preparation of drugs curing related sex hormone diseases or contraceptives. The invention also relates to a stereoisomeride of the LHRH antagonist derivative which is represented as the formula (I), a solvate of the LHRH antagonist derivative which is represented as the formula (I), or physio-toxicity-free salt of the LHRH antagonist derivative which is represented as the formula (I) and a pharmaceutical composition which contains compounds such as the LHRH antagonist derivative, the stereoisomeride, the solvate or the salt. An LHRH antagonist is modified with a water soluble group and a water soluble vitamin structure, the obtained LHRH antagonist derivative can maintain the activity of original antagonists, has low histamine-releasing activity and is beneficial to the clinic application and the water solubility is increased. The formula (I) is R-D-NAI-D-Cpa-D-Aaa3-Ser-Aaa5-Aaa6-Leu-Aaa8-Pro-D-Ala-B.
Owner:INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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