Prodrug derivatives of thyrotropin-releasing hormone (trh)

Details Prodrug derivatives of thyrotropin-releasing hormone (trh) Prodrug derivatives of thyrotropin-releasing hormone (trh)

C - Chemistry, Metallurgy

07

K

C07K 5/097 (2006.01) A61K 38/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2066449

2066449 9103487 PCTABS00003 Compounds of formula (I), wherein R1 is selected from the group consisting of an alkyl group, an aralkyl group, an alkenyl group, a cycloalkyl group, in which the alkyl, aralkyl, alkenyl or cycloalkyl group is unsubstituted or substituted with one or more substituents selected from the group consisting of a halogen atom, e.g. Cl or Br, a hydroxyl group or a straight or branched-chain alkoxy group containing from 1 to 6 carbon atoms; and the pharmaceutically acceptable acid addition salts thereof. Such compounds are prodrugs of TRH and are characterized by having a higher lipophilicity than TRH and possessing a high resistance toward degradation by TRH-inactivating enzymes. Such compounds will after administration be converted into TRH.

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