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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。

2. 发明申请

WO2006032885A3 2-SUBSTITUTED ESTROGEN SULPHAMATES FOR INHIBITION OF STEROID SULPHATASE 审中-公开
标题翻译： 2-取代的雌激素用于抑制甾体硫酸酯酶
公开(公告)号：WO2006032885A3
公开(公告)日：2006-08-24
申请号：PCT/GB2005003641
申请日：2005-09-21
申请人： STERIX LTD , LEESE MATHEW , PUROHIT ALAN , REED MICHAEL JOHN , JOURDAN FABRICE , POTTER BARRY VICTOR LLOYD , BURBERT CHRISTIAN
发明人： LEESE MATHEW , PUROHIT ALAN , REED MICHAEL JOHN , JOURDAN FABRICE , POTTER BARRY VICTOR LLOYD , BURBERT CHRISTIAN
IPC分类号： C07J41/00 , A61K31/565 , A61K31/566 , A61K31/57 , A61K31/58 , A61P5/32 , C07J3/00 , C07J7/00 , C07J31/00 , C07J43/00
CPC分类号： C07J43/003 , C07J3/00 , C07J7/0005 , C07J31/006 , C07J41/0005 , C07J41/0072
摘要： The present invention provides a compound comprising a steroidal ring system and an optional group R 1 selected from any one of -OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the A ring of the steroidal ring system is optionally substituted at position 2 or 4 with a group R 4 which may be a suitable subtituent wherein the D ring of the steroidal ring system is substituted by a group R 2 of the formula -L-R 3 , wherein L is an optional linker group and R 3 is selected from groups which are or which comprise one of (i) -S0 2 R 5 , wherein R 5 is H, a hydrocarbyl group or a bond or group attached to the D ring; (ii) -NO 2 ; (iii) -SOR 6 , wherein R 6 is H or a hydrocarbyl group; (iv) -R 7 , wherein R 7 is a halogen; (v) - alkyl; (vi) -C(=O)R 8 , wherein R 8 is H or hydrocarbyl; (vii) -C=CR 9 , wherein R 9 is H or hydrocarbyl; (viii) -OC(=O)NR 10 R 11 wherein R 10 and R 11 are independently selected from H and hydrocarbyl; (ix), (x), (xi), (xii) and (xiii) are formulae wherein when R 3 is -alkyl, R 4 is present as a hydrocarbon group, when R 3 is -NO 2 R 4 is present and/or R 1 is present as a sulphamate group, and when R 3 is -C(=O)R 8 R 4 is present and R 1 is present as a sulphamate group.
摘要翻译：本发明提供了包含选自-OH，氨基磺酸酯基，膦酸酯基，硫代膦酸酯基，磺酸酯基或磺酰胺中的任何一种的甾体环系和任选的基团R 1的化合物组; 其中所述甾族环系统的A环任选在位置2或4处被基团R 4取代，所述基团R 4可以是合适的取代基，其中所述甾族环系统的D环被基团R 其中L是任选的连接基团，R 3选自以下基团：其中R 1，R 2，R 3，（i）-S 0 2 R 5，其中R 5是H，连接到D环的烃基或键或基团; （ii）-NO 2 2; （iii）-SOR 6，其中R 6是H或烃基; （iv）-R 7，其中R 7为卤素; （ⅴ） - 烷基; （vi）-C（= O）R 8，其中R 8为H或烃基; （vii）-C = CR 9，其中R 9是H或烃基; （viii）-OC（= O）NR 10 R 11，其中R 10和R 11独立地选自由H和烃基组成; （ix），（x），（xi），（xii）和（xiii）是其中当R 3为 - 烷基时，R 4为烃，当R 3为-NO 2 R 4存在时，和/或R 1存在作为并且当R 3为-C（= O）时，存在R 8 R 4和R 4，并且R 1〜 >作为氨基磺酸盐基团存在。

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