Luteinizing hormone releasing hormone analogs

Details Luteinizing hormone releasing hormone analogs Luteinizing hormone releasing hormone analogs

C - Chemistry, Metallurgy

07

K

C07K 7/23 (2006.01) A61K 38/09 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2095932

This invention consists of two aspects: 1) the method of design and synthesis of LHRH antagonists; 2) the products there- after obtained by using the above method: Taking (NAc-D2Nal1, DpClPhe2, D3Pal3, Ser4, Tyr5, DArg6, Leu7, Arg3; Pro9; DA- la10)NH2 as the parent compound, a series of new analogs expressed as (NAc- D2Nal1, AA2, AA3, Ser4, AA5, AA6, Leu7, AA3,Pro9; DAla10)NH2 are obtained by fine modification of both lipophilic area and alkaline area of the molecule of the parent compound.In this way, the high antiovulatory activity of the parent compound can be maintained and the histamine- releasing activity can be reduced to the level so as to meet the clinical requirement.

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