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1. 发明专利

AU5240601A Pharmaceutical compositions comprising proton pump inhibitors and gastrin/cholecystokinin receptor ligands 未知
公开(公告)号：AU5240601A
公开(公告)日：2001-11-20
申请号：AU5240601
申请日：2001-05-04
申请人： BLACK JAMES FOUNDATION , JANSSEN PHARMACEUTICA NV
发明人： KALINDJIAN SARKIS BARRET , BLACK JAMES WHYTE , HULL ROBERT ANTONY DAVID , SHANKLEY NIGEL PAUL , MESENS JEAN LOUIS , ANDRIES LUC JOSEPH
IPC分类号： A61K31/415 , A61K31/44 , A61P1/00 , A61P1/04
摘要： 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

AU1061500A Gastrin and cholecystokinin receptor ligands 未知
公开(公告)号：AU1061500A
公开(公告)日：2000-05-29
申请号：AU1061500
申请日：1999-11-09
申请人： BLACK JAMES FOUNDATION
发明人： KALINDJIAN SARKIS BARRET , BUCK ILDIKO MARIA , LINNEY IAN DUNCAN , WRIGHT PAUL TREVOR , MCDONALD IAIN MAIR , STEEL KATHERINE ISOBEL MARY , HULL ROBERT ANTONY DAVID , ROBERTS SONIA PATRICIA , GAFFEN JOHN DAVID , VINTER JEREMY GILBERT , WALKER MARTIN KEITH , BLACK JAMES WHYTE , WATT GILLIAN FAIRFULL , HARPER ELAINE ANNE , SHANKLEY NIGEL PAUL , TOZER MATTHEW JOHN , DUNSTONE DAVID JOHN , PETHER MICHAEL JOHN , LILLEY ELLIOT JAMES , SYKES DAVID ANDREW , LOW CAROLINE MINLI RACHEL , GRIFFIN ERIC PETER , WRIGHT LAURENCE
IPC分类号： A61K31/40 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/421 , A61K31/426 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/454 , A61P1/14 , A61P1/18 , A61P25/04 , A61P25/18 , A61P25/22 , A61P35/00 , C07B61/00 , C07D207/34 , C07D233/54 , C07D233/88 , C07D233/90 , C07D263/34 , C07D277/20 , C07D277/42 , C07D277/56 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04
摘要： 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)-=CH-, -S- or -O-. n is from 1 to 4; R1 is H or C1 to C15 hydrocarbyl R2 is selected from H, Me, Et, Pr and OH, R3 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 R2 and R3 on the same carbon atom together represent an =O group; R4 is C1 to C15 hydrocarbyl Z is -(NR7)a-CO-(NR8)b- (wherein a is 0 or 1, b is 0 or 1, -CO-NR7-CH2-CO-NR8-, -CO-O-, -CH2-CH2-, -CH=CH-, -CH2-NR8- or a bond; Q is -R9V, or (II), (wherein R9 is -CH2-; -CH2-CH2-; or (III), R9 and R8, together with the nitrogen atom to which R8 is attached, form a piperidine or pyrrolidine ring which is substituted by V; V is -CO-NH-SO2-Ph, -SO2-NH-CO-Ph, -CH2OH, or a group of the formula -R10U, (wherein U is -COOH, tetrazolyl, -CONHOH- or -SO3H; and R10 is a bond; C1 to C6 hydrocarbylene, -O-(C1 to C3 alkylene)-; -SO2NR11-CHR12-; -CO-NR11-CHR12-, or -NH-(CO)c-CH2-, c being 0 or 1).

3. 发明专利

CA2346108A1 GASTRIN AND CHOLECYSTOKININ RECEPTOR LIGANDS 未知
公开(公告)号：CA2346108A1
公开(公告)日：2000-05-18
申请号：CA2346108
申请日：1999-11-09
申请人： BLACK JAMES FOUNDATION
发明人： GRIFFIN ERIC PETER , HULL ROBERT ANTONY DAVID , PETHER MICHAEL JOHN , WRIGHT PAUL TREVOR , LOW CAROLINE MINLI RACHEL , WALKER MARTIN KEITH , KALINDJIAN SARKIS BARRET , WRIGHT LAURENCE , BUCK ILDIKO MARIA , SHANKLEY NIGEL PAUL , WATT GILLIAN FAIRFULL , BLACK JAMES WHYTE , STEEL KATHERINE ISOBEL MARY , TOZER MATTHEW JOHN , DUNSTONE DAVID JOHN , LILLEY ELLIOT JAMES , GAFFEN JOHN DAVID , HARPER ELAINE ANNE , ROBERTS SONIA PATRICIA , VINTER JEREMY GILBERT , LINNEY IAN DUNCAN , SYKES DAVID ANDREW , MCDONALD IAIN MAIR
IPC分类号： A61K31/40 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/421 , A61K31/426 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/454 , A61P1/14 , A61P1/18 , A61P25/04 , A61P25/18 , A61P25/22 , A61P35/00 , C07B61/00 , C07D207/34 , C07D233/54 , C07D233/88 , C07D233/90 , C07D263/34 , C07D277/20 , C07D277/42 , C07D277/56 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04
摘要： Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independent ly =N-, -N(R5)- =CH-, -S- or -O-. n is from 1 to 4; R1 is H or C1 to C15 hydrocarbyl R2 is selected from H, Me, Et, Pr and OH, R3 is selected from H, Me, Et and Pr; or (when n is greater than 1) each R3 is independently select ed 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 R2 and R3 on the same carbon atom together represent an =O group; R4 is C1 to C15 hydrocarbyl Z is -(NR7) a- CO-(NR8)b- (wherein a is 0 or 1, b is 0 or 1, -CO-NR7-CH2-CO-NR8-, -CO-O-, - CH2-CH2-, -CH=CH-, -CH2-NR8- or a bond; Q is -R9V, or (II), (wherein R9 is - CH2-; -CH2-CH2-; or (III), R9 and R8, together with the nitrogen atom to whi ch R8 is attached, form a piperidine or pyrrolidine ring which is substituted b y V; V is -CO-NH-SO2-Ph, -SO2-NH-CO-Ph, -CH2OH, or a group of the formula -R10 U, (wherein U is -COOH, tetrazolyl, -CONHOH- or -SO3H; and R10 is a bond; C1 to C6 hydrocarbylene, -O-(C1 to C3 alkylene)-; -SO2NR11-CHR12-; -CO-NR11-CHR12- , or -NH-(CO)c-CH2-, c being 0 or 1).

6. 发明专利

GB2379387B Pharmaceutical compositions comprising proton pump inhibitors and gastrin/cholecystokinin receptor ligands 未知
公开(公告)号：GB2379387B
公开(公告)日：2004-10-06
申请号：GB0225706
申请日：2001-05-04
申请人： BLACK JAMES FOUNDATION
发明人： KALINDJIAN SARKIS BARRET , BLACK JAMES WHYTE , HULL ROBERT ANTONY DAVID , SHANKLEY NIGEL PAUL , MESENS JEAN LOUIS , ANDRIES LUC JOSEPH
IPC分类号： A61K31/415 , A61K31/44 , A61P1/00 , A61P1/04
摘要： 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

8. 发明专利

GB2379387A Pharmaceutical compositions comprising proton pump inhibitors and gastrin/cholecystokinin receptor ligands 未知
公开(公告)号：GB2379387A
公开(公告)日：2003-03-12
申请号：GB0225706
申请日：2001-05-04
申请人： BLACK JAMES FOUNDATION
发明人： KALINDJIAN SARKIS BARRET , BLACK JAMES WHYTE , HULL ROBERT ANTONY DAVID , SHANKLEY NIGEL PAUL , MESENS JEAN LOUIS , ANDRIES LUC JOSEPH
IPC分类号： A61K31/415 , A61K31/44 , A61P1/00 , A61P1/04
摘要： 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).

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