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1. 发明公开

EP1631579A2 17BETA-HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译： 17BETA-HYDROXYSTERIDID DEHYDROGENASE INHIBITOREN
公开(公告)号：EP1631579A2
公开(公告)日：2006-03-08
申请号：EP04722316.9
申请日：2004-03-22
申请人： Sterix Limited
发明人： VICKER, Nigel, Sterix Limited , LAWRENCE, Harshani Rithma R., Sterix Limited , ALLAN, Gillian Margaret, Sterix Limited , BUBERT, Christian, Sterix Limited , FISCHER, Delphine Sophie Marion, Sterix Limited , PUROHIT, Alan, Sterix Limited , REED, Michael John, Sterix Limited , POTTER, Barry Victor Lloyd, Sterix Limited
IPC分类号： C07J1/00 , A61K31/56 , A61K31/566 , C07J41/00
CPC分类号： C07J71/00 , C07J41/00
摘要： There is provided a compound of Formula (I) wherein (I) R1 is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, and wherein R2 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 R3 form (xii) a pyrazole wherein (a) R4 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) R2 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) R3 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，其中R 2能够形成氢键（iii）烷基芳基，其中芳基被其它芳基取代的（C 1〜C 10）烯基芳基（ⅴ）烷基杂芳基取代，其中当杂芳基仅在环中仅包含C和N时，芳基被除（vi）烯基杂芳基，（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）烷基酰胺的烷基是-CH 2 - 或-CH 2 CH 2 - ，（b）酰胺是二取代的和/或（c）酰胺被烷基杂环基，烯基杂环基，烷基杂芳基，烯基杂芳基，杂芳基，烷基胺中的至少一个所取代基团，烷氧基烷基，烷基芳基，直链或支链烷基，（xi）-CHO，使得 R 1与R 3一起提供烯醇互变异构体OR R 1和R 3形式（xii）吡唑，其中（a）R 4是= NO-烷基或= NOH基，（b）吡唑被烷基 -OH基，烷基酯基，烷氧基烷基，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（II）化合物R 2选自能够形成氢键，氨基磺酸酯基，膦酸酯基，硫代膦酸酯基，磺酸酯基和磺酰胺基的基团; 和（III）R 3选自-OH，= O或-C（= O） - 模拟物

2. 发明授权

EP1446388B1 1,2,4-TRIAZOLE DERIVATIVES CONTAINING A SULPHAMATE GROUP AS AROMATASE INHIBITORS 有权
标题翻译：含有作为芳香化酶抑制剂的亚磺酸盐基团的1,2,4-三唑衍生物
公开(公告)号：EP1446388B1
公开(公告)日：2013-01-09
申请号：EP02777569.1
申请日：2002-11-20
申请人： Sterix Limited
发明人： POTTER, Barry Victor Lloyd, Sterix Limited , WOO, Lok Wai Lawrence, Sterix Limited , PUROHIT, Atul, Sterix Limited , REED, Michael John, Sterix Limited , SUTCLIFFE, Oliver, Brook Sterix Limited , BUBERT, Christian Sterix Limited
IPC分类号： C07D249/08 , C07D413/12 , C07D417/12 , C07D403/12 , A61K31/4196 , A61P35/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D413/12 , C07D417/12

3. 发明授权

EP1399221B1 COMPOSITIONS COMPRISING OESTRONE-3-O-SULPHAMATE AND TRAIL (TNF-RELATED APOPTOSIS INDUCING LIGAND) 有权
标题翻译： ZUSAMMENSETZUNGEN MIT OESTRONE-3-O-SULFAMAT UND TRAIL（TNF-related APOPTOSIS INLIGAND LIGAND）
公开(公告)号：EP1399221B1
公开(公告)日：2009-07-29
申请号：EP02735595.7
申请日：2002-06-06
申请人： Sterix Limited
发明人： PACKHAM, Graham Keith, Sterix Limited , REED, Michael John, Sterix Limited , POTTER, Barry Victor Lloyd, Sterix Limited
IPC分类号： A61P35/00 , A61K38/19 , A61K31/565
CPC分类号： A61K45/06 , A61K31/565 , A61K38/177 , Y02A50/465 , A61K2300/00
摘要： The present invention provides a composition comprising (i) a compound comprising a sulphamate group ("a sulphamate compound"); and (ii) an apoptosis inducer.

4. 发明公开

EP1794176A2 2-SUBSTITUTED ESTROGEN SULPHAMATES FOR INHIBITION OF STEROID SULPHATASE 审中-公开
标题翻译： 2-取代ÖSTROGENSULFAMATE用于抑制类固醇
公开(公告)号：EP1794176A2
公开(公告)日：2007-06-13
申请号：EP05784415.1
申请日：2005-09-21
申请人： Sterix Limited
发明人： LEESE, Mathew, Sterix Limited , PUROHIT, Alan, Sterix Limited , REED, Michael John, Sterix Limited , JOURDAN, Fabrice, Sterix Limited , POTTER, Barry Victor Lloyd, Sterix Limited , BURBERT, Christian, Sterix Limited
IPC分类号： C07J41/00 , C07J43/00 , C07J31/00 , C07J3/00 , C07J7/00 , A61K31/565 , A61K31/566 , A61K31/57 , A61K31/58 , A61P5/32
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 R1 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 R4 which may be a suitable subtituent wherein the D ring of the steroidal ring system is substituted by a group R2 of the formula -L-R3, wherein L is an optional linker group and R3 is selected from groups which are or which comprise one of (i) -S02R5, wherein R5 is H, a hydrocarbyl group or a bond or group attached to the D ring; (ii) -NO2; (iii) -SOR6, wherein R6 is H or a hydrocarbyl group; (iv) -R7, wherein R7 is a halogen; (v) - alkyl; (vi) -C(=O)R8, wherein R8 is H or hydrocarbyl; (vii) -C≡CR9, wherein R9 is H or hydrocarbyl; (viii) -OC(=O)NR10R11 wherein R10 and R11 are independently selected from H and hydrocarbyl; (ix), (x), (xi), (xii) and (xiii) are formulae wherein when R3 is -alkyl, R4 is present as a hydrocarbon group, when R3 is -NO2 R4 is present and/or R1 is present as a sulphamate group, and when R3 is -C(=O)R8 R4 is present and R1 is present as a sulphamate group.

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