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    • 5. 发明申请
      WO1992011284A1 TETRAPEPTIDE DERIVATIVES AND ANALOGUES 审中-公开
    • TETRAPEPTIDE DERIVATIVES AND ANALOGUES
    • 四肽衍生​​物和类似物
    • WO1992011284A1
    • 1992-07-09
    • PCT/GB1991002249
    • 1991-12-17
    • THE JAMES BLACK FOUNDATION LIMITED , KALINDJIAN, Sarkis, Barret , BROUGHTON, Howard, Barff , LOW, Caroline, Minli, Rachel , McDONALD, Iain, Mair , HULL, Robert, Antony, David , SHANKLEY, Nigel, Paul , BUCK, Ildiko, Maria , STEEL, Katherine, Isobel, Mary , DAVIES, Jonathan, Michael, Richard
    • THE JAMES BLACK FOUNDATION LIMITED
    • C07K05/10
    • C07K14/595
    • The invention provides compounds which display antagonist or partial agonist activity at gastrin and/or cholecystokinin receptors. The compounds are of formula (I), wherein R1 is H or (a) R2, R3, R4, R5 and R6 are independently H or methyl, R7, is H, methyl, ethyl, benzyl or formyl, R8 and R10 are independently C1 to C3 alkylene or are absent, R9 is C1 to C3 alkylene or is linked to R6 to form a 3- to 6-membered cycloalkyl group or is absent, R11 is an N-blocking group and R12 is H or methyl, or R11 and R12 are linked to form an N-blocking group, B1, B2 and B3 are independently -CH2- or a carbonyl group, Y is -CO2H, tetrazole or CONR13R14 (wherein R13 and R14 are independently H or C1 to C6 hydrocarbyl), Z1 and Z2 (which may be the same or different) are optional and each represents one or more substituents in the aromatic ring system, such substituents being independently selected from C1 to C6 alkyl (two such alkyl substituents optionally forming a ring fused to one or both of the aromatic rings), C1 to C6 alkoxy, C1 to C6 thioalkoxy, carboxy, C1 to C6 carboalkoxy, nitro, trihalomethyl, hydroxy, -NR15R16 (wherein R15 and R16 are independently H or C1 to C6 alkyl), C1 to C6 alkylaryl, C1 to C6 alkyl(substituted aryl), halo, sulphonamide and cyano, and D is -O-R17-Q or (b), (wherein Q is H or a carbocyclic or heterocyclic group which may optionally be substituted; R17 is absent or is C1 to C10 hydrocarbylene, optionally substituted by -OH, -SH, halogen, -CO2R19 or -CONR19R20 (wherein R19 and R20 are independently H or C1 to C6 hydrocarbyl), and optionally having up to three carbon atoms replaced by -O-, -S- or -NR21- (wherein R21 is H or an N-blocking group), provided that R17 contains at least one carbon atom if Q is H and that R17 does not contain -O-O-; and R18 is H or C1 to C6 alkyl or forms an alkylene (eg C1 to C4 alkylene) link to Q) and pharmaceutically acceptable salts thereof.
    • 本发明提供了在胃泌素和/或胆囊收缩素受体中显示拮抗剂或部分激动剂活性的化合物。 化合物为式（I），其中R 1为H或（a）R 2，R 3，R 4，R 5和R 6独立地为H或甲基，R 7为H，甲基，乙基，苄基或甲酰基，R 8和R 10独立地为 C1至C3亚烷基或不存在，R 9为C 1至C 3亚烷基或连接至R 6以形成3-至6-元环烷基或不存在，R 11为N-封闭基团，R 12为H或甲基或R 11 和R 12连接形成N-封闭基团，B1，B2和B3独立地是-CH2-或羰基，Y是-CO 2 H，四唑或CONR 13 R 14（其中R 13和R 14独立地是H或C 1至C 6烃基） Z 1和Z 2（其可以相同或不同）是任选的，并且各自表示芳环体系中的一个或多个取代基，这样的取代基独立地选自C 1至C 6烷基（两个这样的烷基取代基，任选地形成与一个或多个 两个芳环），C1至C6烷氧基，C1至C6硫代烷氧基，羧基，C1至C6烷氧羰基，硝基，三卤代甲基，羟基，-NR15R16（其中 n R 15和R 16独立地为H或C 1至C 6烷基），C 1至C 6烷基芳基，C 1至C 6烷基（取代的芳基），卤素，磺酰胺和氰基，D为-O-R 17 -Q或（b） Q是H或可任选被取代的碳环或杂环基; 任选被-OH，-SH，卤素，-CO 2 R 19或-CONR 19 R 20（其中R 19和R 20独立地为H或C 1至C 6烃基）和任选地具有至多3个碳原子被取代的C 1 -C 10亚烃基 如果Q为H且R 17不含-OO-，则R 17含有至少一个碳原子;（其中R 21为H或N-封闭基团） 并且R 18是H或C 1至C 6烷基或与Q形成亚烷基（例如C 1至C 4亚烷基））及其药学上可接受的盐。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      WO1995030647A1 CCK AND GASTRIN RECEPTOR LIGANDS 审中-公开
    • CCK AND GASTRIN RECEPTOR LIGANDS
    • CCK和GASTRIN受体配体
    • WO1995030647A1
    • 1995-11-16
    • PCT/GB1995000997
    • 1995-05-02
    • JAMES BLACK FOUNDATION LIMITED , KALINDJIAN, Sarkis, Barret , BUCK, Ildiko, Maria , DUNSTONE, David, John , STEEL, Katherine, Isobel, Mary
    • JAMES BLACK FOUNDATION LIMITED
    • C07C237/22
    • C07D213/82 , C07C237/22 , C07C237/36 , C07C237/42 , C07C2601/18 , C07C2603/74 , C07D207/34 , C07D209/08 , C07D307/68
    • Compounds of formula (I), wherein Ar is a monocyclic aromatic group, R (or each R group, when m is 2 or more) is selected from halo, amino, nitro, cyano, sulphamoyl, sulphonyl, trifluoromethyl, C1 to C3 alkyl, C1 to C3 alkylamino, C1 to C3 dialkylamino, phenyl, substituted phenyl, C1 to C3 alkoxy, hydroxy, esterified hydroxy, C1 to C3 hydroxyalkyl, C1 to C3 alkylcarboxyamino, carboxy, esterified carboxy and amidated carboxy; m is from 0 to 4, provided that m is not more than 2 unless R is exclusively halo, x + y = 0 or 1, R and R are independently H, C1 to C3 alkyl or a C1 to C3 alkylene link to an ortho carbon atom in the aromatic ring, R is H or C1 to C15 hydrocarbyl, in which one or more hydrogen atoms of the hydrocarbyl group may be replaced by a halogen atom, and up to two of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom, provided that R does not contain a -O-O- group, R is H or C1 to C3 alkyl, U is aryl, substituted aryl, heterocyclic, substituted heterocyclic or cycloalkyl, and Z is a group of formulae (IIa or IIb) (wherein R is H or C1 to C3 alkyl, X is -CO2H, esterified carboxy, amidated carboxy, tetrazolyl, hydroxy, cyano, amidino, -CH2OH, -SO2NHCOR , -SONHCOR , -COR , -NHSO2R , -CONHSO2R , -NHCOR or -SO2NHR , in which R is alkyl (e.g. C1 to C6 alkyl), haloalkyl (e.g. C1 to C6 haloalkyl), aryl or substituted aryl, and R is -OH, -CN, or a group selected from those recited above for R , Y is H or a group selected from those recited above for X, and a is from 0 to 2) and pharmaceutically acceptable salts thereof are CCK and gastrin receptor ligands.
    • 式（I）化合物其中Ar为单环芳基，R 1（或每个R 1基团，当m为2以上时）选自卤素，氨基，硝基，氰基，氨磺酰基，磺酰基， 三氟甲基，C1至C3烷基，C1至C3烷基氨基，C1至C3二烷基氨基，苯基，取代苯基，C1至C3烷氧基，羟基，酯化羟基，C1至C3羟基烷基，C1至C3烷基羧基氨基，羧基，酯化羧基和酰胺化羧基; m为0至4，条件是m不大于2，除非R 1仅为卤素，x + y = 0或1，R 2和R 4独立地为H，C 1至C 3烷基或 与芳环中原子碳原子的C1-C3亚烷基连接，R 3是H或C 1至C 15烃基，其中一个或多个烃基的氢原子可以被卤素原子代替，直到 R 3可以被氮，氧或硫原子替代，条件是R 3不含有-OO-基，R 5是H或C 1至C 3烷基，U是芳基，取代的芳基 ，杂环，取代的杂环或环烷基，Z为式（IIa或IIb）（其中R 6为H或C 1至C 3烷基，X为-CO 2 H，酯化羧基，酰胺基羧基，四唑基，羟基，氰基 ，脒基，-CH 2 OH，-SO 2 NHCOR 7，-SONHCOR 7，-COR 7，-NHSO 2 R 7，-CONHSO 2 R 7，-NHCOR 7或-SO 2 NHR 8，其中 R 7是烷基（例如C 1 -C 6烷基），卤代烷基（例如C 1至C 6卤代烷基），芳基或取代的芳基，R 8是-OH，-C N或选自上述R 7的基团，Y为H或选自上述X的基团，a为0至2的基团）及其药学上可接受的盐为CCK和胃泌素受体配体。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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