Gastrin and cholecystokinin receptor ligands (III)

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 -CH2COOR6, wherein R6 represents H, Me, Et, Pr or Bn), -CH-, -O- or -S-; n is from 1 t...

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Hauptverfasser: LOW CAROLINE MINLI RACHEL, KALINDJIAN SARKIS BARRET, BUCK ILDIKO MARIA, TOZER MATTHEW JOHN
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creator LOW CAROLINE MINLI RACHEL
KALINDJIAN SARKIS BARRET
BUCK ILDIKO MARIA
TOZER MATTHEW JOHN
description 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 -CH2COOR6, wherein R6 represents H, Me, Et, Pr or Bn), -CH-, -O- or -S-; n is from 1 to 4; A is an optionally substituted 5- or 6-membered carbocyclic ring wherein (a) 1 or 2 C atoms may optionally be replaced by N, O and/or S atoms, (b) A is fused with the aromatic group in formula (I) to form a fused bicycle, and (c) the ring containing X and Y is linked to a C atom of A; R1 is H or C1 to 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; R2 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 C3 to C6 carbocylic ring, or two R3 groups are absent from neighbouring carbon atoms which are linked by a double bond; or R2 and R3 on the same carbon atom together represent an -O group; R4 is C1 to C15 hydrocarbyl wherein up to two 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; V is -CO-NH-SO2-Ph, -SO2-NH-CO-PH, -CH2OH, or a group of the formula -R7U, (wherein U is -COOH, tetrazolyl, -CONHOH or -SO3H; and R7 is a bond; C1 to C6 hydrocarbylene optionally substituted by hydroxy, amino or acetamido; -O-(C1 to C3 alkylene)-; -SO2NR8-CHR9-; -CO-NR8-CHR9-, R8 and R9 being independently selected from H and methyl; or -NH-(CO)c-CH2, c being 0 or 1); or a pharmaceutically acceptable salt thereof. Compositions comprising a compound a formula (I) are also described
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X and Y are independently -N-, -N(R5)-(R5 being selected from H, Me, Et, Pr, Bn, OH and -CH2COOR6, wherein R6 represents H, Me, Et, Pr or Bn), -CH-, -O- or -S-; n is from 1 to 4; A is an optionally substituted 5- or 6-membered carbocyclic ring wherein (a) 1 or 2 C atoms may optionally be replaced by N, O and/or S atoms, (b) A is fused with the aromatic group in formula (I) to form a fused bicycle, and (c) the ring containing X and Y is linked to a C atom of A; R1 is H or C1 to 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; R2 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 C3 to C6 carbocylic ring, or two R3 groups are absent from neighbouring carbon atoms which are linked by a double bond; or R2 and R3 on the same carbon atom together represent an -O group; R4 is C1 to C15 hydrocarbyl wherein up to two 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; V is -CO-NH-SO2-Ph, -SO2-NH-CO-PH, -CH2OH, or a group of the formula -R7U, (wherein U is -COOH, tetrazolyl, -CONHOH or -SO3H; and R7 is a bond; C1 to C6 hydrocarbylene optionally substituted by hydroxy, amino or acetamido; -O-(C1 to C3 alkylene)-; -SO2NR8-CHR9-; -CO-NR8-CHR9-, R8 and R9 being independently selected from H and methyl; or -NH-(CO)c-CH2, c being 0 or 1); or a pharmaceutically acceptable salt thereof. 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X and Y are independently -N-, -N(R5)-(R5 being selected from H, Me, Et, Pr, Bn, OH and -CH2COOR6, wherein R6 represents H, Me, Et, Pr or Bn), -CH-, -O- or -S-; n is from 1 to 4; A is an optionally substituted 5- or 6-membered carbocyclic ring wherein (a) 1 or 2 C atoms may optionally be replaced by N, O and/or S atoms, (b) A is fused with the aromatic group in formula (I) to form a fused bicycle, and (c) the ring containing X and Y is linked to a C atom of A; R1 is H or C1 to 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; R2 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 C3 to C6 carbocylic ring, or two R3 groups are absent from neighbouring carbon atoms which are linked by a double bond; or R2 and R3 on the same carbon atom together represent an -O group; R4 is C1 to C15 hydrocarbyl wherein up to two 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; V is -CO-NH-SO2-Ph, -SO2-NH-CO-PH, -CH2OH, or a group of the formula -R7U, (wherein U is -COOH, tetrazolyl, -CONHOH or -SO3H; and R7 is a bond; C1 to C6 hydrocarbylene optionally substituted by hydroxy, amino or acetamido; -O-(C1 to C3 alkylene)-; -SO2NR8-CHR9-; -CO-NR8-CHR9-, R8 and R9 being independently selected from H and methyl; or -NH-(CO)c-CH2, c being 0 or 1); or a pharmaceutically acceptable salt thereof. Compositions comprising a compound a formula (I) are also described</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Gastrin and cholecystokinin receptor ligands (III)
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