TRH-degrading ectoenzyme inhibitors

Details TRH-degrading ectoenzyme inhibitors TRH-degrading ectoenzyme inhibitors

2008-05-27

2008-05-27

Gupta, Anish (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Lignin or derivative doai

C514S002600, C514S018700, C514S017400, C514S210020, C530S300000, C530S329000, C530S330000, C530S331000, C548S180000, C548S200000, C548S215000

Reexamination Certificate

active

11345649

ABSTRACT:
Peptide derivatives useful as inhibitors of activity of thyrotropin-releasing hormone-degrading ectoenzyme (TRH-DE) are of formula Ia:wherein:R1is an optionally substituted 4-, 5- or 6-membered heterocyclic ring having one or more heteroatoms, in which at least one carbon atom of the ring is substituted with O or S;X1is —CO— or —CS— or —CH2CO— or CH(R4) wherein R4is H or optionally substituted alkyl or —COOH or —COOR11wherein R11is optionally substituted alkyl;X2and X3(which may be the same or different) are —CO— or —CS—;Z is —CH2— or —S— or —O— or —NH—;Q is O or S;R2is H or optionally substituted alkyl or an optionally substituted carbocyclic ring;R3is H or optionally substituted alkyl or an optionally substituted mono- or polycyclic ring, optionally having one or more heteroatoms in the ring(s) and optionally being a fused ring; or R2and R3together form an optionally substituted mono- or polycyclic ring optionally having one or more heteroatoms in the ring(s) and optionally being a fused ring;R5and R6(which may be the same or different) are H, or lower alkyl;R7and R8(which may be the same or different) are H, or optionally substituted lower alkyl;R9and R10(which may be the same or different) are H, or optionally substituted alkyl, or an optionally substituted carbocyclic ring;Y is —(CH2)n— where n is 0, 1, 2 or 3 provided that when R2and R3form part of the ring n is 0;and pharmaceutically acceptable salts thereof.

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