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1. 发明申请

WO2004085457A3 17BETA-HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译： 17BETA-HYDROXYSTERIDID DEHYDROGENASE抑制剂
公开(公告)号：WO2004085457A3
公开(公告)日：2005-02-03
申请号：PCT/GB2004001234
申请日：2004-03-22
申请人： STERIX LTD , VICKER NIGEL , LAWRENCE HARSHANI RITHMA RUCHI , ALLAN GILLIAN MARGARET , BUBERT CHRISTIAN , FISCHER DELPHINE SOPHIE MARION , PUROHIT ALAN , REED MICHAEL JOHN , POTTER BARRY VICTOR LLOYD
发明人： VICKER NIGEL , LAWRENCE HARSHANI RITHMA RUCHI , ALLAN GILLIAN MARGARET , BUBERT CHRISTIAN , FISCHER DELPHINE SOPHIE MARION , PUROHIT ALAN , REED MICHAEL JOHN , POTTER BARRY VICTOR LLOYD
IPC分类号： A61K31/56 , A61K31/566 , C07J20060101 , C07J41/00 , C07J71/00
CPC分类号： C07J71/00 , C07J41/00
摘要： There is provided a compound of Formula (I) wherein (I) R is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, and wherein R is capable of forming a hydrogen bond (iii) alkylaryl group, wherein the aryl group is substituted by other than a C1-10 group (iv) alkenylaryl group wherein the aryl group is substituted (v) alkyiheteroaryl group, wherein when heteroaryl group comprises only C and N in the ring, the aryl group is substituted by other than a methyl group (vi) alkenylheteroaryl group, (vii) =N-O-alkyl or =N-O-H group (viii) branched alkenyl (ix) alkyl-alcohol group (x) amide or alkylamide wherein (a) the alkyl of the alkylamide is - CH2- or -CH2CH2-, (b) the amide is di-substituted and/or (c) the amide is substituted with at least one of a I kyl heterocycle group, al ke nyl heterocycle group, alkylheteroaryl group, alkenylheteroaryl group, heteroaryl group, alkylamine group, alkyloxyalkyl group, alkylaryl group, straight or branched alkyl group, (xi) -CHO so that R, together with R3 provide the enol tautomer (a); OR R1 together with R form (xii) a pyrazole wherein (a) R is =N-0-alkyl or =N-0-H group, (b) the pyrazole is substituted with one of alkyl-OH group, alkyl ester group, alkyloxyalkyl. group, branched alkyl group, and an amide and/or (c) the 2 position is substituted with a group selected from -OH and -0-hydrocarbyl (xiii) a heteroaryl ring to provide a compound of the formula (b); (II) R is selected from groups capable of forming a hydrogen bond, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group and a sulphonamide group; and (III) R is selected from -OH, =O, or a -C(=O)- mimetic.
摘要翻译：提供式（I）的化合物，其中（I）R 1选自（i）烷氧基烷基（ii）腈基，并且其中R 2能够形成氢键（iii ）烷基芳基，其中芳基被除了其中芳基被取代的（C）芳基取代的（C 1 -C 6）烯基芳基以外的其它芳基取代;（ⅴ）芳基杂芳基，其中当杂芳基仅在环中仅包含C和N时，芳基（vii）= NO-烷基或= NOH基（viii）支链烯基（ix）烷基醇基（x）酰胺或烷基酰胺，其中（a）烷基的烷基酰胺是-CH 2 - 或-CH 2 CH 2 - ，（b）酰胺是二取代的，和/或（c）酰胺被I烷基杂环基，烯基杂环基，烷基杂芳基中的至少一个取代，烯基杂芳基，杂芳基，烷基胺基，烷氧基烷基，烷基芳基，直链或支链烷基，（xi）-CHO so t 与R 3一起提供烯醇互变异构体（a）; 或R 1与R 3一起形成（xii）吡唑，其中（a）R 4是= N-O-烷基或= N-O-H基，（b）吡唑被烷基 - OH基，烷基酯基，烷氧基烷基。基团，支链烷基和酰胺和/或（c）2位被选自-OH和-O-烃基（xiii）杂芳基环的基团取代，以提供式（b）的化合物; （II）R 2选自能够形成氢键的基团，氨基磺酸酯基团，膦酸酯基团，硫代膦酸酯基团，磺酸酯基团和磺酰胺基团; 和（III）R 3选自-OH，= O或-C（= O） - 模拟物。

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