Gastrin and cholecystokinin receptor ligands(II)

Details Gastrin and cholecystokinin receptor ligands(II) Gastrin and cholecystokinin receptor ligands(II)

2005-04-12

2005-04-12

Desai, Rita (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C548S125000, C548S345100, C548S364100

Reexamination Certificate

active

06878734

ABSTRACT:
Ligands for the gastrin and cholecystokinin (CCK) receptors are provided, together with methods for preparing such ligands, and compounds which are useful intermediates in such methods. Pharmaceutical compositions comprising such ligands, methods for preparing such pharmaceutical compositions, and methods of treatment using these compositions also are provided. The ligands have the formula (I):where n is from 1 to 3;X and Y are independently ═N— or —N(R5)— where R5is selected from the group consisting of H, Me, Et, Pr, Bn, —OH and —CH2COOR6, where R6represents H, Me, Et, Pr or Bn;R1is H or a C1-C15saturated carbocylic ring optionally substituted with OMe, NMe2, CF3, Me, F, Cl, Br or I where up to three H atoms may optionally be replaced by halogen atoms;R2is selected from H, Me, Et, Pr and OH, each R2being independently selected from H, Me, Et, Pr and OH when n is greater than 1;R3is selected from the group consisting of H, Me, Et and Pr when n is 1; or, when n is greater than 1, each R3is independently selected from the group consisting of H, Me, Et and Pr, or two R3groups on neighbouring carbon atoms are linked to form a C3to C6carbocylic ring, or two R3groups are absent from neighbouring carbon atoms which are linked by a double bond; or R2and R3on the same carbon atom together represent an ═O group;R4is H or a C3to C10alicyclic ring where up to three H atoms may optionally be replaced by halogen atoms;Z is selected from the group consisting of:Q is a 6-membered aromatic carbocycle substituted with 1 or 2 V groups and optionally substituted with 1, 2 or 3 T groups;V is selected from the group consisting of —CO—NH—SO2—Ph, —SO2—NH—CO—Ph, —CH2OH, or a group of the formula —R7U, where U is selected from the group consisting of —COOH, tetrazolyl, —CONHOH and —SO3H; and R7is selected from the group consisting of a bond; C1to C6hydrocarbylene, optionally substituted by hydroxy, amino or acetamido; —O—(C1to C3alkylene)-; —SO2NR8—CHR9—; —CO—NR8—CHR9—, where R8and R9are independently selected from H and methyl; and —NH—(CO)c—CH2—, where c is 0 or 1.

REFERENCES:
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