公开(公告)号：US06479531B1

公开(公告)日：2002-11-12

申请号：US09831385

申请日：2001-08-02

申请人： Sarkis Barret Kalindjian ,  Ildiko Maria Buck ,  Ian Duncan Linney ,  Paul Trevor Wright ,  Iain Mair McDonald ,  Katherine Isobel Mary Steel ,  Robert Antony David Hull ,  Sonia Patricia Roberts ,  John David Gaffen ,  Jeremy Gilbert Vinter ,  Martin Keith Walker ,  James Whyte Black ,  Gillian Fairfull Watt ,  Elaine Anne Harper ,  Nigel Paul Shankley ,  Matthew John Tozer ,  David John Dunstone ,  Michael John Pether ,  Elliot James Lilley ,  David Andrew Sykes ,  Caroline Minli Rachel Low ,  Eric Peter Griffin ,  Laurence Wright

发明人： Sarkis Barret Kalindjian ,  Ildiko Maria Buck ,  Ian Duncan Linney ,  Paul Trevor Wright ,  Iain Mair McDonald ,  Katherine Isobel Mary Steel ,  Robert Antony David Hull ,  Sonia Patricia Roberts ,  John David Gaffen ,  Jeremy Gilbert Vinter ,  Martin Keith Walker ,  James Whyte Black ,  Gillian Fairfull Watt ,  Elaine Anne Harper ,  Nigel Paul Shankley ,  Matthew John Tozer ,  David John Dunstone ,  Michael John Pether ,  Elliot James Lilley ,  David Andrew Sykes ,  Caroline Minli Rachel Low ,  Eric Peter Griffin ,  Laurence Wright

IPC分类号： C07D40306

CPC分类号： C07D233/64 ,  C07D207/34 ,  C07D233/88 ,  C07D233/90 ,  C07D263/34 ,  C07D277/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  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).

摘要翻译： 式（I）化合物及其药学上可接受的盐是胃泌素和/或胆囊收缩素受体的配体。 X和Y独立地为= N-，-N（R 5） - = CH - ， - S-或-O-。 n为1至4; R1为H或C1至C15烃基R2选自H，Me，Et，Pr和OH，R3选自H，Me，Et和Pr; 或（当n大于1时），每个R 3独立地选自H，Me，Et和Pr，或相邻碳原子上的两个R 3基团连接形成C 3至C 6碳环，或在相同碳上的R 2和R 3 原子一起代表a = O组; R4为C1〜C15烃基Z为 - （NR7）a-CO-（NR8）b-（其中a为0或1，b为0或1，-CO-NR7-CH2-CO-NR8-，-CO- O，-CH 2 -CH 2 - ， - CH = CH - ， - CH 2 -NR 8 - 或键; Q为-R 9 V或（II）（其中R 9为-CH 2 - ; -CH 2 -CH 2 - III），R9和R8与R8所连接的氮原子一起形成被V取代的哌啶或吡咯烷环; V是-CO-NH-SO 2-Ph，-SO 2 -NH-CO-Ph， -CH 2 OH或式-R 10 U的基团（其中U为-COOH，四唑基，-CONHOH-或-SO 3 H; R 10为键; C 1至C 6亚烃基，-O-（C 1至C 3亚烷基） - ; -SO2NR11-CHR12-; -CO-NR11-CHR12-或-NH-（CO）c-CH2-，c为0或1）。