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公开(公告)号：US06017904A
公开(公告)日：2000-01-25
申请号：US44984
申请日：1998-03-20
IPC分类号： A61K31/565 , A61K31/56 , A61K31/566 , A61K31/661 , A61K31/663 , A61P35/00 , A61P43/00 , C07F9/145 , C07J31/00 , C07J51/00 , C07J53/00 , C12N9/16 , A61K31/66
CPC分类号： C07J51/00 , C07J31/006
摘要： Phosphate esters of formula: ##STR1## for use in the inhibition of steroid sulfatase enzyme, wherein R is as defined in the specification and the -O-polycycle represents a residue of a sterol.
摘要翻译： 磷酸酯，其用于抑制类固醇硫酸酯酶，其中R如说明书中所定义，-O-多环代表固醇的残基。
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公开(公告)号：US6011024A
公开(公告)日：2000-01-04
申请号：US111927
申请日：1998-07-08
IPC分类号： A61K31/37 , C07D311/16 , C07D311/30 , C07D311/32 , C07D311/36 , C07J41/00 , A61K31/165
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 is 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 ##STR1## wherein each of R.sub.1 and R.sub.2 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.degree. C. it would provide a K.sub.m value of less than 50 .mu.M.
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公开(公告)号：US20100120789A1
公开(公告)日：2010-05-13
申请号：US12554943
申请日：2009-09-07
IPC分类号： A61K31/497 , C07C233/00 , A61K31/165 , A61K31/4365 , C07D495/04 , C07D405/02 , C12Q1/32
CPC分类号： C11D3/0073 , C11D3/2086 , C11D3/33 , C11D7/265 , C11D7/3245 , C11D11/0041
摘要： There is provided a compound having Formula I R1—Z—R2 Formula I wherein R1 is a group selected from optionally substituted fused polycyclic groups, substituted alkyl groups, branched alkyl groups, and optionally substituted cycloalkyl groups Z is a linker which is or comprises a carbonyl group or a isostere of a carbonyl group R2 is selected from optionally substituted aromatic rings and optionally substituted heterocyclic rings wherein (a) R2 is a 2-substituted thiophene group, and/or (b) Z is a group of the formula —C(═O)—CR3R4—X—(CR5R6)n-, wherein X is selected from NR7, S, O, S═O, and S(═O)2, wherein n is 0 or 1 and/or (c) R1 is an adamantyl group and Z is or comprises an amide group, and/or (d) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR8R9)p- NR10—S(═O)2—(CR11R12)q-, wherein p is 0 or 1 and q is 0 or 1 and/or (e) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR13R14)v-Y—(CR15R16)w- where Y is a heteroaryl group in which a bond in the heteroaryl ring is a isostere of a carbonyl group, wherein v is o or 1 and w is 0 or 1; wherein each of R3, R4, R5, R6, R8, R9, R11, R12, R13, R14, R15 and R16, are independently selected from H, hydrocarbyl and halogen, wherein each of R7 and R10 are independently selected from H and hydrocarbyl.
摘要翻译： 提供了具有式I的化合物R1-Z-R2式Ⅰ其中R1是选自任选取代的稠合多环基团，取代的烷基，支链烷基和任选取代的环烷基的基团Z是一种或多种 羰基或羰基的等排基团选自任选取代的芳环和任选取代的杂环，其中（a）R 2是2-取代的噻吩基团，和/或（b）Z是式-C （= O）-CR 3 R 4 -X-（CR 5 R 6）n - ，其中X选自NR 7，S，O，S = O和S（= O）2，其中n为0或1和/或（c） R1是金刚烷基，Z是或包含酰胺基，和/或（d）R1是金刚烷基，Z是或包含式 - （CR8R9）对NR10-S（= O）2- （CR11R12）q-，其中p为0或1，q为0或1，和/或（e）R1为金刚烷基，Z为或包含式 - （CR13R14）vY-（CR15R16）w- 在哪里 Y是杂芳基环中的键是羰基的等离子体的杂芳基，其中v是0或1，w是0或1; 其中R 3，R 4，R 5，R 6，R 8，R 9，R 11，R 12，R 13，R 14，R 15和R 16各自独立地选自H，烃基和卤素，其中R 7和R 10各自独立地选自H和烃基 。
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公开(公告)号：US07276513B2
公开(公告)日：2007-10-02
申请号：US11329982
申请日：2006-01-11
IPC分类号： A61K31/473 , C07D221/18
CPC分类号： C07J1/0051 , C07J63/00 , C07J63/008
摘要： There is provided a compound of formula XII, wherein G is H or a substituent, and wherein R1 is a sulphamate group.
摘要翻译： 提供了式XII化合物，其中G是H或取代基，其中R 1是氨基磺酸酯基。
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公开(公告)号：US07098199B2
公开(公告)日：2006-08-29
申请号：US10084235
申请日：2002-02-25
IPC分类号： A61K31/56
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 is 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 μM.
摘要翻译： 描述了在需要相同的受试者中抑制类固醇硫酸酯酶活性的方法。 所述方法包括向所述受试者施用抑制甾族硫酸酯酶的量的环系化合物; 该环系化合物包含连接下式的氨基磺酸酯基团的环，其中R 1和R 2各自独立地选自H，烷基，烯基，环烷基 或芳基，或一起表示亚烷基链中任选含有一个或多个杂原子或基团的亚烷基; 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取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）一起孵育，则其将提供K 值小于50μM。
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56.发明授权Steroid 3-O-sulphamate derivatives as inhibitors of oestrone sulphatase 失效类固醇3-O-氨基磺酸酯衍生物作为雌二醇硫酸酯酶的抑制剂公开(公告)号：US06949561B1
公开(公告)日：2005-09-27
申请号：US09572246
申请日：2000-05-17
IPC分类号： A61K31/565 , A61K31/185 , A61K31/255 , A61K31/365 , A61K31/435 , A61K31/47 , A61K31/473 , A61K31/58 , A61P35/00 , A61P37/00 , A61P43/00 , C07D221/18 , C07D221/22 , C07J41/00 , C07J63/00 , C07J73/00
CPC分类号： C07J73/003 , A61K31/366 , A61K31/435 , A61K31/56 , C07J41/0016 , C07J73/00 , C07J73/005 , C07J75/00
摘要： A sulphamate compound suitable for use as an inhibitor of oestrone sulphatese (E.C.3.1.6.2) is described. The compound is a polycyclic compound comprising at least two ring components, wherein the polycyclic compound comprises at least one sulphamate group attached to at least one of the ring components, and wherein at least one of the ring components of the polycyclic structure is a heterocyclic ring.
摘要翻译： 描述适用于硫酸亚甲酯（E.C.3.1.6.2）抑制剂的氨基磺酸盐化合物。 化合物是包含至少两个环组分的多环化合物，其中多环化合物包含至少一个与至少一个环组分连接的氨基磺酸酯基团，并且其中多环结构的至少一个环组分是杂环 。
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公开(公告)号：US06921776B1
公开(公告)日：2005-07-26
申请号：US09638314
申请日：2000-08-14
IPC分类号： A61K31/37 , C07D311/16 , A61K31/352 , C07D311/78
CPC分类号： C07D311/78 , A61K31/37 , C07D311/16
摘要： A compound is described. In particular, a non-steroidal sulphamate compound is described. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound is of general Formula (A), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof, but wherein at least one of R1-R6 is a sulphamate group; and wherein X is any one of S, NH, a substituted N, CH2, or a substituted C.
摘要翻译： 描述化合物。 特别地，描述了非甾体氨基磺酸盐化合物。 该化合物适合用作奥斯汀硫酸酯酶的抑制剂。 该化合物为通式（A），其中R 1至R 6独立地选自H，卤素，羟基，氨基磺酸酯，烷基和取代的变体或其盐， 但其中R 1 -R 6中的至少一个为氨基磺酸酯基; 并且其中X是S，NH，取代的N，CH 2或任何一个取代的C
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公开(公告)号：US06903084B2
公开(公告)日：2005-06-07
申请号：US09794853
申请日：2001-02-27
IPC分类号： A61K31/37 , C07D311/16 , C07D311/30 , C07D311/32 , C07D311/36 , C07J41/00 , A61K31/56 , C07J1/00
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 is 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 allylene 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 μM.
摘要翻译： 描述了在需要相同的受试者中抑制类固醇硫酸酯酶活性的方法。 所述方法包括向所述受试者施用抑制甾族硫酸酯酶的量的环系化合物; 该环系化合物包含连接下式的氨基磺酸酯基团的环，其中R 1和R 2各自独立地选自H，烷基，烯基，环烷基 或芳基，或一起代表任选地在亚烷基链中含有一个或多个杂原子或基团的烯丙基; 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取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）一起孵育，则其将提供K 值小于50μM。
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公开(公告)号：US06642397B1
公开(公告)日：2003-11-04
申请号：US09579163
申请日：2000-05-25
IPC分类号： C07J100
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 is 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 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： 描述了在需要相同的受试者中抑制类固醇硫酸酯酶活性的方法。 所述方法包括向所述受试者施用抑制甾族硫酸酯酶的量的环系化合物; 所述环系化合物包含连接在其上的环，其中R 1和R 2各自独立地选自H，烷基，烯基，环烷基和芳基，或一起表示任选地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。
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60.发明授权Compounds that inhibit oestrone sulphatase and/or aromatase and methods for making and using 失效抑制雌二醇硫酸酯酶和/或芳香酶的化合物及其制备和使用方法公开(公告)号：US06506792B1
公开(公告)日：2003-01-14
申请号：US09638315
申请日：2000-08-14
IPC分类号： A61K31352
CPC分类号： C07D311/30 , C07D311/32 , C07D311/36
摘要： The instant invention relates to sulphamate compounds of formula I, wherein A represents a ring structure, B represents a ring structure, D a ring structure, C is a bond, E is a link joining ring structure B to the ring structure D, X represents a suitable first group, and Y represents a suitable second group; wherein one ring of the compound is a phenolic ring; and wherein any one of ring structures A, B and D has a bound thereto a sulphamate group.
摘要翻译： 本发明涉及式I的氨基磺酸酯化合物，其中A表示环结构，B表示环结构，D表示环结构，C为键，E为环结构B与环结构D的连接，X表示 合适的第一组，Y表示合适的第二组; 其中所述化合物的一个环是酚醛环; 并且其中环结构A，B和D中的任何一个具有与其结合的氨基磺酸酯基团。
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