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    • 8. 发明授权
      US07034048B2 Gastrin and cholecystokinin receptor ligands (III) 失效
    • Gastrin and cholecystokinin receptor ligands (III)
    • US07034048B2
    • 2006-04-25
    • US10275613
    • 2001-05-04
    • Sarkis Barret Kalindjian , Ildiko Maria Buck , Caroline Minli Rachel Low , Matthew John Tozer
    • Sarkis Barret Kalindjian , Ildiko Maria Buck , Caroline Minli Rachel Low , Matthew John Tozer
    • A61K31/4164 , A61K31/404 , C07D403/04
    • C07D403/04 , A61K31/415 , A61K31/42 , A61K45/06 , C07D413/04 , A61K2300/00
    • 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)—(R5 being selected from H, Me, Et, Pr, Bn, OH and —CH2COOR6, wherein R6 represents H, Me, Et, Pr or Bn), ═CH—, —O— or —S—; n is from 1 to 4; A is an optionally substituted 5- or 6-membered carbocyclic ring wherein (a) 1 or 2 C atoms may optionally be replaced by N, O and/or S atoms, (b) A is fused with the aromatic group in formula (I) to form a fused bicycle, and (c) the ring containing X and Y is linked to a C atom of A; R1 is H or C1 to C15 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; 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 (when n is 1) 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 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 C1 to C15 hydrocarbyl wherein up to two 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; V is —CO—NH—SO2—Ph, —SO2—NH—CO—PH, —CH2OH, or a group of the formula —R7U, (wherein U is —COOH, tetrazolyl, —CONHOH or —SO3H; and R7 is a bond; C1 to C6 hydrocarbylene optionally substituted by hydroxy, amino or acetamido; —O—(C1 to C3 alkylene)—; —SO2NR8—CHR9—; —CO—NR8—CHR9—, R8 and R9 being independently selected from H and methyl; or —NH—(CO)c—CH2, c being 0 or 1); or a pharmaceutically acceptable salt thereof. Compositions comprising a compound a formula (I) are also described
    • 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 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明授权
      US5939437A CCK and gastrin receptor ligands 失效
    • CCK and gastrin receptor ligands
    • US5939437A
    • 1999-08-17
    • US737317
    • 1996-12-20
    • Sarkis Barret Kalindjian , Katherine Isobel Mary Steel , David John Dunstone , Ildiko Maria Buck
    • Sarkis Barret Kalindjian , Katherine Isobel Mary Steel , David John Dunstone , Ildiko Maria Buck
    • C07C237/22 , C07C237/36 , C07C237/42 , C07D207/34 , C07D209/08 , C07D213/82 , C07D307/68 , A61K31/165
    • C07D213/82 , C07C237/22 , C07C237/36 , C07C237/42 , C07D207/34 , C07D209/08 , C07D307/68 , C07C2101/18 , C07C2103/74
    • 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##
    • 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
    • 10. 发明授权
      US06355665B1 1H-4(5)-substituted imidazole derivatives, their preparation and their use as histamine H3 receptor ligands 失效
    • 1H-4(5)-substituted imidazole derivatives, their preparation and their use as histamine H3 receptor ligands
    • 1H-4（5） - 取代咪唑衍生物，其制备及其作为组胺H3受体配体的用途
    • US06355665B1
    • 2002-03-12
    • US09463012
    • 2000-03-14
    • Matthew John Tozer , Sarkis Barret Kalindjian , Ian Duncan Linney , Katherine Isabel Mary Steel , Michael John Pether , Tracey Cooke
    • Matthew John Tozer , Sarkis Barret Kalindjian , Ian Duncan Linney , Katherine Isabel Mary Steel , Michael John Pether , Tracey Cooke
    • C07D23354
    • C07D233/64 , C07D417/04
    • A compound of the formula wherein R2 is an optionally substituted Cz to Cg alkylene or alkylene chain; R3 is C2 to C15 optionally substituted hydrocarbyl; X is a bond or —NR4—, wherein R4 is hydrogen or non-aromatic C1 to C5 optionally substituted hydrocarbyl, or aryl(C1 to C3)alkyl, or a pharmaceutically acceptable salt thereof. A method of modifing histamine activity in a patient comprising administering to said patient a pharmaceutical composition containing an effective amount of a compound of formula wherein R1 is selected from C1 to C6 alkyl, C1 to C6 alkoxy, C1 to C6 alkylthio, carboxy, carboxy(C1 to C6)alkyl, formyl, C1 to C6 alkylcarbonyl, C1 to C6 alkylcarbonylalkoxy, nitro, trihalomethyl, hydroxy, amino, C1 to C6 alkylcarbonylalkoxy, nitro, trihalomethyl, hydroxy, amino, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, aryl, C1 to C6 alkylaryl, halo, sulfamoyl and cyano; R2 is optionally substituted C2 to C20 hydrocarbylene, in which one or more hydrogen atoms may be replaced by halogen atoms and up to 6 carbon atoms may be replaced by oxygen or nitrogen atoms, R2 being in the form of an optionally substituted C2 to C8 alkylene or alkenylene chain; R3 is hydrogen or C1 to C15 optionally substituted hydrocarbyl; X is a bond or —NR4—; and a is from 0 to 2, or a pharmaceutically acceptable salt thereof.
    • 化学式R 2的化合物是任选取代的C 1至C 8亚烷基或亚烷基链; R3是C2至C15任选取代的烃基; X是键或-NR 4 - ，其中R 4是氢或非芳族C 1至C 5任选取代的烃基或芳基（C 1至C 3）烷基或其药学上可接受的盐。1，一种修饰患者组胺活性的方法， 向所述患者施用含有有效量的蛔虫素R1化合物的药物组合物选自C1至C6烷基，C1至C6烷氧基，C1至C6烷硫基，羧基，羧基（C1至C6）烷基，甲酰基，C1至C6 烷基羰基，C 1至C 6烷基羰基烷氧基，硝基，三卤代甲基，羟基，氨基，C 1至C 6烷基羰基烷氧基，硝基，三卤甲基，羟基，氨基，C 1至C 6烷基氨基，二（C 1至C 6烷基）氨基，芳基，C 1至C 6烷基芳基， ，氨磺酰基和氰基; R2是任选取代的C 2至C 20亚烃基，其中一个或多个氢原子可以被卤素原子取代，并且最多6个碳原子可被氧或氮原子取代，R 2为任选取代的C 2至C 8亚烷基 或亚烯基链; R 3是氢或C 1至C 15任选取代的烃基; X是键或-NR4-; 和a为0至2，或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 Espacenet 法律信息 同族专利 专利引用
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