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    • 6. 发明专利
    • Gastrin and cholecystokinin receptor ligands (iii)
    • AU5241301A
    • 2001-11-20
    • AU5241301
    • 2001-05-04
    • BLACK JAMES FOUNDATION
    • KALINDJIAN SARKIS BARRETBUCK ILDIKO MARIALOW CAROLINE MINLI RACHELTOZER MATTHEW JOHN
    • A61K31/415A61K31/42A61K45/06A61P1/04C07D403/04C07D413/04
    • Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently -N-, -N(R 5 )-(R 5 being selected from H, Me, Et, Pr, Bn, OH and -CH 2 COOR 6 , wherein R 6 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; R 1 is H or C 1 to C 15 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 R 2 being independently selected from H, Me, Et, Pr and OH when n is greater than 1; R 3 (when n is 1) is selected from H, Me, Et and Pr; or (when n is greater than 1) each R 3 is independently selected from H, Me, Et and Pr, or two R 3 groups on neighbouring carbon atoms are linked to form a C 3 to C 6 carbocylic ring, or two R 3 groups are absent from neighbouring carbon atoms which are linked by a double bond; or R 2 and R 3 on the same carbon atom together represent an -O group; R 4 is C 1 to C 15 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-SO 2 -Ph, -SO 2 -NH-CO-PH, -CH 2 OH, 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 C 6 hydrocarbylene optionally substituted by hydroxy, amino or acetamido; -O-(C 1 to C 3 alkylene)-; -SO 2 NR 8 -CHR 9 -; -CO-NR 8 -CHR 9 -, R 8 and R 9 being independently selected from H and methyl; or -NH-(CO) c -CH 2 , c being 0 or 1); or a pharmaceutically acceptable salt thereof. Compositions comprising a compound a formula (I) are also described