发明名称 GASTRIN AND CHOLECYSTOKININ RECEPTOR LIGANDS (II)
摘要 <p>Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently =N-, -N(R5)- (R5 being selected from H, Me, Et, Pr, Bn, -OH and -CH¿2COOR?6, wherein R6 represents H, Me, Et, Pr or Bn), =CH-, -S-, or -O-; R1 is H or C¿1?-C15 hydrocarbyl wherein up to three C atoms may optionally be replaced by N, O and/or S atoms, and up to three H atoms may optionally be replaced by halogen atoms; R?2¿ is selected from H, Me, Et, Pr and OH, each R2 being independently selected from H, Me, Et, Pr and OH when n is greater than 1; R3 (when n is 1) is selected from H, Me, Et and Pr; or (when n is greater than 1) each R3 is independently selected from H, Me, Et and Pr, or two R3 groups on neighbouring carbon atoms are linked to form a C¿3? to C6 carbocyclic ring, or two R?3¿ groups are absent from neighbouring carbon atoms which are linked by a double bond; or R?2 and R3¿ on the same carbon atom together represent an =O group; R4 is H or C¿1?-C15 hydrocarbyl wherein up to three C atoms may optionally be replaced by N, O and/or S atoms, and up to three H atoms may optionally be replaced by halogen atoms; Z is a diradical derived from an optionally substituted aromatic or non-aromatic C5 or C6 carbocycle, wherein 1, 2 or 3 C atoms are optionally replaced by N, O and/or S; Q is a 6-membered aromatic carbocycle (optionally substituted with 1 or 2 V groups and/or 1, 2 or 3 T groups) wherein 1, 2 or 3 C atoms are optionally replaced by N; V is -CO-NH-SO2-Ph, -SO2-NH-CO-Ph, -CH2OH, or a group of the formula -R?7¿U, (wherein U is -COOH, tetrazolyl, -CONHOH or -SO¿3?H; and R?7¿ is a bond; C¿1? to C6 hydrocarbylene, optionally substituted by hydroxy, amino or acetamido; -O-(C1 to C3 alkylene)-; -SO2NR?8-CHR9¿-; -CO-NR?8-CHR9-, R8 and R9¿ being independently selected from H and methyl; or -NH-(CO)¿c?-CH2-, c being 0 or 1); T is C1 to C6 hydrocarbyl, -NR?10R11¿ (wherein R?10 and R11¿ are independently selected from H, Me, Et, Pr or Bn), -OMe, -OH, -CH¿2?OH, halogen or trihalomethyl. Compositions comprising a compound of formula (I) are also described.</p>
申请公布号 WO2001085723(A1) 申请公布日期 2001.11.15
申请号 GB2001001964 申请日期 2001.05.04
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