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1. 发明授权

US06187766B1 Steroid sulphatase inhibitors 失效
标题翻译：类固醇硫酸酶抑制剂
公开(公告)号：US06187766B1
公开(公告)日：2001-02-13
申请号：US09238345
申请日：1999-01-27
申请人： Michael John Reed , Barry Victor Potter
发明人： Michael John Reed , Barry Victor Potter
IPC分类号： A61K31165
CPC分类号： A61K31/37 , C07D311/16 , C07D311/30 , C07D311/32 , C07D311/36 , C07J41/0072
摘要： A method of inhibiting steroid sulphatase activity in a subject in need of same as described. The method comprises administering to said subject a steroid sulphatase inhibiting amount of a ring system compound; which ring system compound comprises a ring to which is attached a sulphamate group of the formula wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); and if the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37° C. it would provide a Km value of less than 50 &mgr;M.
摘要翻译：一种抑制需要与上述相同的对象的类固醇硫酸酯酶活性的方法。该方法包括向所述受试者施用抑制甾类硫酸酯酶的量的环系化合物; 所述环系化合物包含与R 1和R 2各自独立地选自H，烷基，烯基，环烷基和芳基的或者一起表示任选含有一个或多个杂原子或基团的亚烷基亚烷基链; 并且其中所述化合物是具有类固醇硫酸酯酶活性的酶的抑制剂（E.C.3.1.6.2）; 并且如果所述化合物的氨基磺酸酯基团被硫酸根基团替代以形成硫酸盐化合物，并在pH 7.4和37℃下与类固醇硫酸酶（EC3.1.6.2）一起温育，则其将提供小于 50亩。

2. 发明申请

US20070225256A1 COMPOUND 审中-公开
标题翻译：复合
公开(公告)号：US20070225256A1
公开(公告)日：2007-09-27
申请号：US11689936
申请日：2007-03-22
申请人： Matthew Leese , Atul Purohit , Michael Reed , Fabrice Jourdan , Barry Victor Potter , Christian Bubert
发明人： Matthew Leese , Atul Purohit , Michael Reed , Fabrice Jourdan , Barry Victor Potter , Christian Bubert
IPC分类号： A61K31/675 , A61K31/58 , C07J43/00 , C07J41/00
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 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) —SO2R5, 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)R3, wherein R3 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 —NO2R4 is present and/or R1 is present as a sulphamate group, and when R3 is —C(═O)R3R4 is present and R1 is present as a sulphamate group.
摘要翻译：本发明提供了包含甾族环系统和选自-OH，氨基磺酸盐基团，膦酸盐基团，硫代膦酸盐基团，磺酸盐基团或磺酰胺基团中的任何一个的任选基团R1的化合物; 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 L 3，其中L是任选的连接基团，R 3选自以下基团，或其中包含一个的（i）-SO 2 R 5，其中R 5是H，连接到D环上的烃基或键或基团 ; （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 3，其中R 3是H或烃基; （vii）-C≡CR9，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）R 3 3 R 4时，存在R 1和R 2 >以氨基磺酸盐基团存在。

3. 发明申请

US20070105886A1 Steroidal compounds for inhibiting steroid sulphatase 失效
标题翻译：用于抑制类固醇硫酸酶的甾体化合物
公开(公告)号：US20070105886A1
公开(公告)日：2007-05-10
申请号：US11329982
申请日：2006-01-11
申请人： Barry Victor Potter , Michael Reed , Lok Wai Woo
发明人： Barry Victor Potter , Michael Reed , Lok Wai Woo
IPC分类号： C07D221/18 , A61K31/473
CPC分类号： C07J1/0051 , C07J63/00 , C07J63/008
摘要： There is provided a compound having Formula (I) wherein G is H or a substituent, and wherein R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group, capable of inhibiting steroid sulphatase.
摘要翻译：提供具有式（I）的化合物，其中G是H或取代基，其中R 1是氨基磺酸酯基，膦酸酯基，硫代膦酸酯基，磺酸酯基或磺胺类，能够抑制类固醇硫酸酯酶。

4. 发明申请

US20060074060A1 Compound 失效
标题翻译：复合
公开(公告)号：US20060074060A1
公开(公告)日：2006-04-06
申请号：US11234868
申请日：2005-09-23
申请人： Nigel Vicker , Harshani Lawrence , Gillian Allan , Christian Bubert , Delphine Sophie Fischer , Alan Purohit , Michael Reed , Barry Victor Potter
发明人： Nigel Vicker , Harshani Lawrence , Gillian Allan , Christian Bubert , Delphine Sophie Fischer , Alan Purohit , Michael Reed , Barry Victor Potter
IPC分类号： A61K31/58 , C07J71/00
CPC分类号： C07J71/00 , C07J41/00
摘要： There is provided a compound of Formula (I) wherein (I) R2 is 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) alkylheteroaryl 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 alkyl heterocycle group, alkenyl heterocycle group, alkylheteroaryl group, alkenylheteroaryl group, heteroaryl group, alkylamine group, alkyloxyalkyl group, alkylaryl group, straight or branched alkyl group, (xi) —CHO so that R1 together with R3 provide the enol tautomer (a); OR R2 together with R3 form (xii) a pyrazole wherein (a) R4 is ═N—O-alkyl or ═N—O—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 —O-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）化合物，其中（I）R 2选自（ⅰ）烷氧基烷基（ⅱ）腈基，其中R2能够形成氢键（ⅲ）烷基芳基，其中芳基基团被取代的芳基（ⅴ）烷基杂芳基以外的C 1-10基团（ⅳ）链烯基芳基取代，其中当杂芳基仅在环中仅包含C和N时，芳基被除了甲基（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-CH2- 或-C 2 -C 12 - ，（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，烷基胺基，烷氧基烷基中的至少一个基团，烷基芳基，直链或支链烷基，（xi）-CHO，使得R1起始与R3提供烯醇互变异构体（a）; OR 2与R 3一起形成（xii）吡唑，其中（a）R4是-NO-烷基或-NOH基，（b）吡唑被烷基-OH基，烷基酯基，烷氧基烷基，支链烷基基团和酰胺和/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）R2选自能够形成氢键的基团，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; 和（III）R 3选自-OH，-O或C（-O） - 模仿物。

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