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    • 1. 发明专利
    • Pharmaceutical compositions comprising proton pump inhibitors and gastrin/cholecystokinin receptor ligands
    • GB2379387B
    • 2004-10-06
    • GB0225706
    • 2001-05-04
    • BLACK JAMES FOUNDATION
    • KALINDJIAN SARKIS BARRETBLACK JAMES WHYTEHULL ROBERT ANTONY DAVIDSHANKLEY NIGEL PAULMESENS JEAN LOUISANDRIES LUC JOSEPH
    • A61K31/415A61K31/44A61P1/00A61P1/04
    • Pharmaceutical compositions comprising a proton pump inhibitor and a compound of the formula (I) or its pharmaceutically acceptable salts, are useful in treating gastrointestinal disorders. 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-, S- or -O-; n is from 1 to 4; 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 which are linked by a double bond; or R 2 >and R 3 >on the same carbon atom 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 two H atoms may optionally be replaced by halogen atoms; Z is -(NR 7>) a -CO-(NR 8>) b - (wherein a is 0 or 1, b is 0 or 1, and R 7 >and R 8 >are independently selected from the groups recited above for R 6>), -CO-NR 7>—CH 2 -CO-NR 8>—, -CO-O-, -CH 2 -CH 2 -, -CH=CH-, -CH 2 -NR- or a bond; Q is -R 9>V, or (II) (wherein R 9 >is -CH 2 -; -CH 2 -CH 2 -; or (III) R 9 >and R 8>, together with the nitrogen atom to which R 8 >is attached, form a piperidine or pyrrolid
    • 2. 发明专利
    • Pharmaceutical compositions comprising proton pump inhibitors and gastrin/cholecystokinin receptor ligands
    • GB2379387A
    • 2003-03-12
    • GB0225706
    • 2001-05-04
    • BLACK JAMES FOUNDATION
    • KALINDJIAN SARKIS BARRETBLACK JAMES WHYTEHULL ROBERT ANTONY DAVIDSHANKLEY NIGEL PAULMESENS JEAN LOUISANDRIES LUC JOSEPH
    • A61K31/415A61K31/44A61P1/00A61P1/04
    • Pharmaceutical compositions comprising a proton pump inhibitor and a compound of the formula (I) or its pharmaceutically acceptable salts, are useful in treating gastrointestinal disorders. 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-, -S- or -O-; n is from 1 to 4; 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 which are linked by a double bond; or R 2 and R 3 on the same carbon atom 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 two H atoms may optionally be replaced by halogen atoms; Z is -(NR 7 ) a -CO-(NR 8 ) b - (wherein a is 0 or 1, b is 0 or 1, and R 7 and R 8 are independently selected from the groups recited above for R 6 ), -CO-NR 7 -CH 2 -CO-NR 8 -, -CO-O-, -CH 2 -CH 2 -, -CH=CH-, -CH 2 -NR 8 - or a bond; Q is -R 9 V, or (II) (wherein R 9 is -CH 2 -; -CH 2 -CH 2 -; or (III) R 9 and R 8 , together with the nitrogen atom to which R 8 is attached, form a piperidine or pyrrolidine ring which is substitued by V; V is -CO-NH-SO 2 -Ph, SO 2 -NH-CO-Ph, -CH 2 OH, or a group of the formula -R 10 U, (wherein U is -COOH, tetrazolyl, -CONHOH- or -SO 3 H; and R 10 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 11 -CHR 12 -;-CO-NR 11 -CHR 12 -, R 11 and R 12 being independently selected from H and methyl; or -NH-(CO) c -CH 2 -, c being 0 or 1); T is C 1 to C 6 hydrocarbyl, -NR 6 R 7 (wherein R 6 and R 7 are as defined above), -OMe, -OH, -CH 2 OH, halogen or trihalomethyl; m is 1 or 2; p is from 0 to 3; and q is from 0 to 2, with the proviso that q is 1 or 2 when Z is a bond).