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    Oestrogen derivatives as inhibitors of steroid sulphatase
    3.
    发明授权
    Oestrogen derivatives as inhibitors of steroid sulphatase 失效
    雌激素衍生物作为类固醇硫酸酯酶的抑制剂

    公开(公告)号：US07893284B2

    公开(公告)日：2011-02-22

    申请号：US11233945

    申请日：2005-09-23

    申请人： Matthew Leese ,  Atul Purohit ,  Michael John Reed ,  Simon Paul Newman ,  Surinder Kuman Chander ,  Fabrice Jourdan ,  Barry Victor Lloyd Potter

    发明人： Matthew Leese ,  Atul Purohit ,  Michael John Reed ,  Simon Paul Newman ,  Surinder Kuman Chander ,  Fabrice Jourdan ,  Barry Victor Lloyd Potter

    IPC分类号： C07J3/00 ,  C07J1/00

    CPC分类号： C07J43/00 ,  C07J41/00

    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 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 a nitrite group, an alcohol, an ester, an ether, an amine and an alkene, provided that when R3 is or comprises an alcohol, L is present; and wherein the A ring of the steroidal ring system is substituted at position 2 or 4 with a group R4, wherein R4 is a hydrocarbyl 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; 其中甾族环体系的D环被式-L-R3的基团R 2取代，其中L是任选的连接基团，并且R 3选自亚硝酸根基团，醇， 酯，醚，胺和烯烃，条件是当R3是或包含醇时，存在L; 并且其中所述甾族环系统的A环在位置2或4与基团R 4取代，其中R 4是烃基。

    COMPOUND
    4.
    发明申请
    COMPOUND 审中-公开
    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。

    Oestrogen derivatives as inhibitors of steroid sulphatase
    5.
    发明申请
    Oestrogen derivatives as inhibitors of steroid sulphatase 失效
    雌激素衍生物作为类固醇硫酸酯酶的抑制剂

    公开(公告)号：US20060094696A1

    公开(公告)日：2006-05-04

    申请号：US11233945

    申请日：2005-09-23

    申请人： Mathew Leese ,  Alan Purohit ,  Michael Reed ,  Simon Newman ,  Surinder Chander ,  Fabrice Jourdan ,  Barry Potter

    发明人： Mathew Leese ,  Alan Purohit ,  Michael Reed ,  Simon Newman ,  Surinder Chander ,  Fabrice Jourdan ,  Barry Potter

    IPC分类号： A61K31/66 ,  C07J51/00 ,  A61K31/56

    CPC分类号： C07J43/00 ,  C07J41/00

    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 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 a nitrite group, an alcohol, an ester, an ether, an amine and an alkene, provided that when R3 is or comprises an alcohol, L is present; and wherein the A ring of the steroidal ring system is substituted at position 2 or 4 with a group R4, wherein R4 is a hydrocarbyl 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; 其中所述甾体环体系的D环被式-LR 3 SO 2的基团R 2取代，其中L是任选的连接基团，R 3 选自亚硝酸根基团，醇类，酯类，醚类，胺类和烯烃中的一种或其中之一的基团，条件是当R 3是或包含一个或多个 酒精，L存在; 并且其中所述甾族环系统的A环在位置2或4被基团R 4取代，其中R 4为烃基。

    Microcin B17 Analogs And Methods For Their Preparation And Use
    6.
    发明申请
    Microcin B17 Analogs And Methods For Their Preparation And Use 审中-公开
    Microcin B17类似物及其制备和使用方法

    公开(公告)号：US20080234132A1

    公开(公告)日：2008-09-25

    申请号：US11667385

    申请日：2005-11-18

    申请人： Laurence Coquin ,  Fabrice Jourdan ,  Olivier Pierrat ,  David John Lowe ,  Anthony Maxwell ,  Christopher John Pickett ,  Melisa Wall

    发明人： Laurence Coquin ,  Fabrice Jourdan ,  Olivier Pierrat ,  David John Lowe ,  Anthony Maxwell ,  Christopher John Pickett ,  Melisa Wall

    IPC分类号： A01N43/36 ,  C07K7/06 ,  A61K38/08 ,  A61P35/00 ,  A01P1/00 ,  A01P21/00 ,  A61P31/04 ,  C12N9/99

    CPC分类号： C07K5/1024 ,  C07D207/38 ,  C07D261/18 ,  C07K5/0819 ,  C07K7/02 ,  C07K7/08 ,  C07K14/001

    摘要： The present invention pertains to synthetic analogues of microcin B17 component units, methods of making and using these analogues, including, for example, as inhibitors of DNA gyrase. More particularly, the present invention pertains to compounds of the Formula wherein: W is independently: —H or a peptide group; Z is independently: —OH or a peptide group; wherein each peptide group, if present, is: an amino acid group and comprises exactly one amino acid, or: a poly(amino acid) group and comprises two or more amino acids; RN3 is independently: —H, C1-6alkyl, C2-6alkenyl, C3-6cycloalkyl, or C3-6cycloalkenyl, C6-14-carboaryl, C5-14heteroaryl, C6-14carboaryl-C1-6alkyl, C5-14heteroaryl-C1-6alkyl, and is optionally substituted; the circle represents a mono-heterocycle or a bis-heterocycle, wherein the heterocycle, or each of the two heterocycles, is a five membered ring having at least a first ring heteroatom that is N, and optionally a second ring heteroatom that is selected from N, O, and S; and the heterocycle, or each of the two heterocycles, is optionally substituted with one or more substituents; and pharmaceutically acceptable salts, amides, esters, solvates, and hydrates thereof. The present invention also pertains to uses of such compounds, for example, to inhibit DNA Gyrase activity in a cell and in methods of therapy, for example, to treat a disease or condition that is ameliorated by the inhibition of DNA Gyrase, such as a bacterial infection, cancer, etc.; as a herbicide; as a microbicide; as a bactericide; etc.

    摘要翻译： 本发明涉及细胞因子B17组分单元的合成类似物，制备和使用这些类似物的方法，包括例如DNA促旋酶的抑制剂。 更具体地说，本发明涉及下式的化合物：其中：W独立地是：-H或肽基; Z独立地为：-OH或肽基团; 其中每个肽基团（如果存在的话）是：氨基酸基团并且仅包含一个氨基酸，或者：聚（氨基酸）基团并且包含两个或更多个氨基酸; R 3 N 3独立地为：-H，C 1-6烷基，C 2-6链烯基，C 3-6亚烷基， 或C 3-6亚环烷基，C 6-14芳烃基，C 5-14杂芳基，C 6 -14碳芳基-C 1-6烷基，C 5-14杂芳基-C 1-6烷基，并且任选地 取代 该环表示单杂环或双杂环，其中杂环或两个杂环中的每一个为具有至少第一环杂原子为N的五元环，并且任选地为选自以下的第二环杂原子： N，O和S; 并且杂环或两个杂环中的每一个任选被一个或多个取代基取代; 和其药学上可接受的盐，酰胺，酯，溶剂合物和水合物。 本发明还涉及这样的化合物的用途，例如抑制细胞中的DNA促旋酶活性和治疗方法，例如治疗通过抑制DNA促旋酶改善的疾病或病症，例如 细菌感染，癌症等; 作为除草剂; 作为杀微生物剂; 作为杀菌剂; 等等