Novel peptide derivatives and their pharmaceutical use

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 5/04 (2006.01) A61K 31/425 (2006.01) A61K 38/04 (2006.01) C07D 277/06 (2006.01) C07D 417/12 (2006.01) C07K 5/06 (2006.01) C07K 5/062 (2006.01) C07K 5/065 (2006.01) C07K 5/097 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2049390

ABSTRACT Peptide derivatives of the following formula Image wherein R1 and R2 are the same or different and respectively mean hydrogen atom, a C1-5 alkyl group or phenyl, X is -NH- or -CH2-, Y is hydrogen atom, a benzyl group wherein phenyl may be substituted by hydroxyl, or a C1-5 alkyl group which may be substituted by -SH, -SR3, -SO2R3, -CONH2, Image , -OR6 or- Image (wherein R3 means a C1-5 alkyl group or an aryl group, R4 and R5 are the same or different and respec- tively mean hydrogen atom, a C1-5 alkyl group or an amino protecting group and R6 is hydrogen atom, a C1-5 alkyl group or a hydroxyl protecting group), Z is -CH2- or -S-, and n is 1 or 2, provided that when X is -NH-, R1 and R2 are not hydrogen atoms at the same time, pharmaceutically acceptable acid addition salts thereof and pharmaceutical use thereof. Since the compounds of the present invention possess stronger actions on central nervous system, they are of use as a therapeutic medicament for central nervous disorders.

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