US 7,378,397 B2 | ||
TRH-degrading ectoenzyme inhibitors | ||
Julie A. Kelly, Ballsbridge (Ireland) | ||
Assigned to The Provost, Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen Elizabeth Near Dublin, Dublin (Ireland) | ||
Filed on Feb. 01, 2006, as Appl. No. 11/345,649. | ||
Application 11/345649 is a continuation of application No. 10/223590, filed on Aug. 19, 2002, abandoned. | ||
Application 10/223590 is a continuation in part of application No. PCT/IE01/00027, filed on Feb. 16, 2001. | ||
Claims priority of application No. 000135 (IE), filed on Feb. 17, 2000; and application No. 000240 (IE), filed on Mar. 30, 2000. | ||
Prior Publication US 2006/0293247 A1, Dec. 28, 2006 | ||
Int. Cl. A61K 38/06 (2006.01); A61K 38/07 (2006.01); A61K 38/08 (2006.01); A61K 31/397 (2006.01); A61K 31/40 (2006.01); C07D 417/02 (2006.01); C07D 413/02 (2006.01) |
U.S. Cl. 514—22 [514/2; 514/18; 514/17; 514/210.02; 530/300; 530/329; 530/330; 530/331; 548/180; 548/200; 548/215] | 18 Claims |
1. A compound of formula I:
wherein:
R1 is 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, N, or S;
X1 is —CO— or —CS— or —CH2CO— or CH(R4) wherein R4 is H or optionally substituted alkyl or —COOH or —COOR11 wherein R11 is optionally substituted alkyl;
X2 and X3 are independently —CO— or —CS—;
Z is —CH2— or —S— or —O— or —NH—;
Q is O or S;
R2 is H or optionally substituted alkyl or an optionally substituted carbocyclic ring;
R3 is 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 R2 and R3 together form an optionally substituted mono- or polycyclic ring optionally having one or more heteroatoms in the ring(s)
and optionally being a fused ring;
R5 and R6 are independently H, or lower alkyl;
R7 and R8 are independently H, or optionally substituted lower alkyl;
R9 and R10 are independently 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 R2 and R3 form part of the ring n is 0;
provided that when R1 is:
and X1, X2 and X3 are —CO—
and R5, R6, R7, R8, R9, R10 are H
and Z is —CH2—
and Q is O
and Y is —(CH2)n— where n is 0,
then R2 and R3 are not both H;
and pharmaceutically acceptable salts thereof.
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