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    Gastrin and cholecystokinin receptor ligands(II)
    2.
    发明授权
    Gastrin and cholecystokinin receptor ligands(II) 失效

    公开(公告)号：US06878734B2

    公开(公告)日：2005-04-12

    申请号：US10275741

    申请日：2001-05-04

    申请人： Sarkis Barret Kalindjian ,  Ildiko Maria Buck ,  Katherine Isobel Mary Steel ,  Paul Trevor Wright ,  Matthew John Tozer ,  Michael John Pether ,  Caroline Minli Rachel Low

    发明人： Sarkis Barret Kalindjian ,  Ildiko Maria Buck ,  Katherine Isobel Mary Steel ,  Paul Trevor Wright ,  Matthew John Tozer ,  Michael John Pether ,  Caroline Minli Rachel Low

    IPC分类号： A61K31/42 ,  A61K45/06 ,  A61P1/04 ,  C07D233/54 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  A61K31/415 ,  C07D233/06 ,  C07D237/08 ,  C07D247/02 ,  C07D405/04 ,  C07D413/02

    CPC分类号： C07D233/64 ,  A61K31/42 ,  A61K45/06 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  A61K2300/00

    摘要： Ligands for the gastrin and cholecystokinin (CCK) receptors are provided, together with methods for preparing such ligands, and compounds which are useful intermediates in such methods. Pharmaceutical compositions comprising such ligands, methods for preparing such pharmaceutical compositions, and methods of treatment using these compositions also are provided. The ligands have the formula (I): where n is from 1 to 3; X and Y are independently ═N— or —N(R5)— where R5 is selected from the group consisting of H, Me, Et, Pr, Bn, —OH and —CH2COOR6, where R6 represents H, Me, Et, Pr or Bn; R1 is H or a C1-C15 saturated carbocylic ring optionally substituted with OMe, NMe2, CF3, Me, F, Cl, Br or I where 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 is selected from the group consisting of H, Me, Et and Pr when n is 1; or, when n is greater than 1, each R3 is independently selected from the group consisting of 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 H or a C3 to C10 alicyclic ring where up to three H atoms may optionally be replaced by halogen atoms; Z is selected from the group consisting of: Q is a 6-membered aromatic carbocycle substituted with 1 or 2 V groups and optionally substituted with 1, 2 or 3 T groups; V is selected from the group consisting of —CO—NH—SO2—Ph, —SO2—NH—CO—Ph, —CH2OH, or a group of the formula —R7U, where U is selected from the group consisting of —COOH, tetrazolyl, —CONHOH and —SO3H; and R7 is selected from the group consisting of a bond; C1 to C6 hydrocarbylene, optionally substituted by hydroxy, amino or acetamido; —O—(C1 to C3 alkylene)-; —SO2NR8—CHR9—; —CO—NR8—CHR9—, where R8 and R9 are independently selected from H and methyl; and —NH—(CO)c—CH2—, where c is 0 or 1.

    CCK and gastrin receptor ligands
    7.
    发明授权
    CCK and gastrin receptor ligands 失效

    公开(公告)号：US5939437A

    公开(公告)日：1999-08-17

    申请号：US737317

    申请日：1996-12-20

    申请人： Sarkis Barret Kalindjian ,  Katherine Isobel Mary Steel ,  David John Dunstone ,  Ildiko Maria Buck

    发明人： Sarkis Barret Kalindjian ,  Katherine Isobel Mary Steel ,  David John Dunstone ,  Ildiko Maria Buck

    IPC分类号： C07C237/22 ,  C07C237/36 ,  C07C237/42 ,  C07D207/34 ,  C07D209/08 ,  C07D213/82 ,  C07D307/68 ,  A61K31/165

    CPC分类号： C07D213/82 ,  C07C237/22 ,  C07C237/36 ,  C07C237/42 ,  C07D207/34 ,  C07D209/08 ,  C07D307/68 ,  C07C2101/18 ,  C07C2103/74

    摘要： Compounds of formula (I) and their pharmaceutically active salts are gastrin and CCK receptor ligands, where Ar is a monocyclic aromatic group, R.sup.1 is halo, amino, nitro, cyano, sulphamoyl, sulphonyl, trifluoromethyl, C.sub.1 to C.sub.3 alkyl, C.sub.1 to C.sub.3 alkylamino, C.sub.1 to C.sub.3 dialkylamino, phenyl, substituted phenyl, C.sub.1 to C.sub.3 alkoxy, hydroxy, esterified hydroxy, C.sub.1 to C.sub.3 hydroxyalkyl, C.sub.1 to C.sub.3 alkylcarboxyamino, carboxy, esterified carboxy and amidated carboxy, m is 0, 1, 2, 3, or 4, provided that m is not more than 2 unless R.sup.1 is exclusively halo, x+y=0 or 1, R.sup.2 and R.sup.4 independently are II, or C.sub.1 to C.sub.3 alkyl, R.sup.3 is H or C.sub.1 to C.sub.15 hydrocarbyl, where one or more hydrogen atoms of die hydrocarbyl group may be replaced by a halogen atom, and where up to two of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom, provided that R.sup.3 does not contain a --O--O-- group, R.sup.5 is H or C.sub.1 to C.sub.3 alkyl, U is a cyclic moiety, selected from the group consisting of aryl, aromatic heterocyclic, non-aromatic heterocyclic, and cycloalkyl groups, where the aryl or aromatic group contains up to 3 substituents selected from the group consisting of halo, amino, nitro, cyano, sulphamoyl, sulphonyl, trifluoromethyl, C.sub.1 to C.sub.3 alkyl, C.sub.1 to C.sub.3 alkylamino, C.sub.1 to C.sub.3 dialkylamino, phenyl, C.sub.1 to C.sub.3 alkoxy, hydroxy, esterified hydroxy, C.sub.1 to C.sub.3 hydroxyalkyl, C.sub.1 to C.sub.3 alkylcarboxyamino, carboxy, esterified carboxy and amidated carboxy, Z is a group of the formula (IIa) or (IIb) where R.sup.6 is H or C.sub.1 to C.sub.3 alkyl, X is --CO.sub.2 H, esterified carboxy, amidated carboxy, tetrazolyl, hydroxy, cyano, amidino, --CH.sub.2 OH, --SO.sub.2 NHCOR.sup.7, --SONHCOR.sup.7, --COR.sup.7, --NHSO.sub.2 R.sup.7, --CONHSO.sub.2 R.sup.7,--NHCOR.sup.7 or --SO.sub.2 NHR.sup.8, where R.sup.7 is C.sub.1 to C.sub.6, alkyl, C.sub.1 to C.sub.6 aryl or substituted aryl, and R.sup.8 is --OH, --CN, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 haloalkyl, aryl or substituted aryl, Y is H or a group selected from those recited above for X, and a is 0, 1, or 2. ##STR1##