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公开(公告)号：US08394825B2
公开(公告)日：2013-03-12
申请号：US12593560
申请日：2008-03-27
申请人： Matthew Leese , Fabrice Jourdan , Meriel Kimberley , Atul Purohit , Barry Victor Lloyd Potter , Gillian Reed
发明人： Matthew Leese , Fabrice Jourdan , Meriel Kimberley , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
IPC分类号： A61K31/47 , A61K31/472 , C07D217/00
CPC分类号： A61K31/40 , A61K31/403 , A61K31/435 , A61K31/47 , A61K31/55
摘要： The present invention involves tetrahydroisoquinoline compounds and their use in the inhibition and/or prevention of tumor growth.
摘要翻译： 本发明涉及四氢异喹啉化合物及其在抑制和/或预防肿瘤生长中的用途。
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公开(公告)号：US20190102850A1
公开(公告)日：2019-04-04
申请号：US15720305
申请日：2017-09-29
申请人： David McMakin Wheeler , Ned M. Smith , Thimas Barnes Abels , Michael John Reed , Clair Michael Bowman , Thomas John Barnes
发明人： David McMakin Wheeler , Ned M. Smith , Thimas Barnes Abels , Michael John Reed , Clair Michael Bowman , Thomas John Barnes
摘要： Embodiments involve using smart contracts in a decentralized network as a framework for a smart city commodity exchange. In at least one embodiment, consumers and service providers negotiate terms and conditions of a smart contract for providing goods or services to the consumer. The service provider may provide all requested goods and services or bundle goods and services provided from multiple vendors. Verification of smart contract fulfillment may be assisted by information from sensors or other independent data collection. The service provider may provide discounted services in exchange for information to provide to a third party. Resources of both the consumer and service provide are committed during smart contract negotiations until completion of the smart contract, or rejection of the offered terms. Resource commitments, smart contract generation, performance of the smart contract and intermediate transactions are recorded in public ledgers according to Blockchain protocols. Other embodiments are described and claimed.
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公开(公告)号：US20080312266A1
公开(公告)日：2008-12-18
申请号：US11855603
申请日：2007-09-14
IPC分类号： A61K31/435 , C07D221/18 , C12Q1/34 , A61P35/00
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： 提供了具有式（I）的化合物，其中G是H或取代基，并且其中R 1是能够抑制类固醇硫酸酯酶的氨基磺酸酯基，膦酸酯基，硫代膦酸酯基，磺酸酯基或磺酰胺基中的任何一种 。
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34.发明授权17-aryl linker derivatised estrogen 3-sulphamates as inhibitors of steroid sulphatase 失效17-芳基连接体衍生化的雌激素3-磺酰胺酸酯作为类固醇硫酸酯酶的抑制剂公开(公告)号：US07067503B2
公开(公告)日：2006-06-27
申请号：US10367622
申请日：2003-02-14
CPC分类号： A61K31/565 , A61K31/37
摘要： There is provided a compound comprising a steroidal ring system and a group R1 selected from any one of 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 an aromatic hydrocarbyl group.
摘要翻译： 提供了包含选自氨基磺酸盐基团，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甾体环系统和基团R 1的化合物; 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 芳香族烃基。
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公开(公告)号：US06677325B2
公开(公告)日：2004-01-13
申请号：US10082007
申请日：2002-02-21
IPC分类号： A61K3135
CPC分类号： A61K31/37 , C07D311/16 , C07D311/30 , C07D311/32 , C07D311/36 , C07J41/0072
摘要： A method for controlling estrone or estrodiol production comprising administering a ring system compound comprising a sulphamic acid ester group; wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein if the sulphamic acid ester group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH 7.4 and 37° C. it provides a Km value of less than 50 &mgr;M. A method to target the estrogen metabolic pathway comprising administering a ring system compound comprising a sulphamic acid ester group; wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein if the sulphamic acid ester group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH 7.4 and 37° C. it provides a Km value of less than 50 &mgr;M.
摘要翻译： 用于控制雌酮或雌二醇生产的方法，包括施用包含氨基磺酸酯基团的环系化合物; 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（EC 3.1.6.2）; 并且其中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（EC 3.1.6.2）温育，则其提供Km值 小于50亩。 靶向雌激素代谢途径的方法，包括施用包含氨基磺酸酯基团的环系化合物; 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（EC 3.1.6.2）; 并且其中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（EC 3.1.6.2）温育，则其提供Km值 小于50亩。
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公开(公告)号：US06670353B2
公开(公告)日：2003-12-30
申请号：US09572237
申请日：2000-05-17
IPC分类号： A61K3156
CPC分类号： A61K31/565
摘要： A sulphamate compound suitable for use as an inhibitor of oestrone sulphatase (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 oxime group is attached to or is part of at least one of the ring components.
摘要翻译： 描述了适合用作奥斯汀硫酸酯酶抑制剂（E.C.3.1.6.2）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连接至至少一个环组分的氨基磺酸酯基团，并且其中至少一个肟基团连接至至少一个 的环组件。
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公开(公告)号：US06476011B1
公开(公告)日：2002-11-05
申请号：US09193970
申请日：1998-11-18
IPC分类号： A61K3156
CPC分类号： A61K31/37 , C07D311/16 , C07D311/30 , C07D311/32 , C07D311/36 , C07J41/0072
摘要： The invention pertains to methods for introducing an estrogenic compound into a subject in need thereof involving administering an effective amount of a ring system compound having the formula (II) wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, and at least one of R1 and R2 is H, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and the ring system ABCD represents a substituted or unsubstituted, saturated or unsaturated steroid nucleus selected from the group consisting of oestrones, dehydroepiandrosterones, substituted oestrones, oestradiols, substituted oestradiols, oestriols, substituted dehydroepiandrosterones, or substituted oestriols; wherein the compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3,1,6,2), or a pharmceutically acceptable salt thereof.
摘要翻译： 本发明涉及向有需要的受试者中引入雌激素化合物的方法，包括给予有效量的具有式（II）的环系化合物，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，并且R 1和R 2中的至少一个为H，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; 环系ABCD代表选自以下组中的取代或未取代的饱和或不饱和类固醇核：地塞米松，脱氢表雄酮，取代的雌二醇，雌二醇，取代的雌二醇，雌三醇，取代的脱氢表雄甾酮或取代的雌三醇; 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（EC 3,1,6,2）或其药学上可接受的盐。
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公开(公告)号：US5861390A
公开(公告)日：1999-01-19
申请号：US456122
申请日：1995-05-31
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
CPC分类号： C07J51/00 , C07J31/006
摘要： Steroid sulphatase inhibitors and pharmaceutical compositions containing them for use in the treatment of oestrone dependent tumors, especially breast cancer. The steroid sulphatase inhibitors are phosphonate esters of formula (I) ##STR1## where R is alkyl, alkenyl, cycloalkyl or aryl; and --O--polycycle represents the residue of a polycyclic alcohol such as a sterol, preferably a 3-sterol.
摘要翻译： 类固醇硫酸酯酶抑制剂和含有它们的药物组合物用于治疗依赖于雌激素的肿瘤，特别是乳腺癌。 类固醇硫酸酯酶抑制剂是式（I）的膦酸酯，其中R是烷基，烯基，环烷基或芳基; -O-多环表示多环醇的残基，例如固醇，优选3-固醇。
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公开(公告)号：US08124614B2
公开(公告)日：2012-02-28
申请号：US11855603
申请日：2007-09-14
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 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： 提供了具有式（I）的化合物，其中G是H或取代基，并且其中R 1是能够抑制类固醇硫酸酯酶的氨基磺酸酯基，膦酸酯基，硫代膦酸酯基，磺酸酯基或磺酰胺基中的任何一种 。
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公开(公告)号：US6159960A
公开(公告)日：2000-12-12
申请号：US193969
申请日：1998-11-18
IPC分类号： A61K31/565 , A61K31/00 , A61K31/145 , A61K31/56 , A61K31/566 , A61K31/567 , A61K31/5685 , A61P5/30 , A61P5/32 , A61P5/36 , A61P35/00 , A61P43/00 , C07C307/02 , C07J1/00 , C07J31/00 , C07J41/00 , C07J43/00 , C12N9/16
CPC分类号： A61K31/565 , C07J41/0033 , 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.
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; 该环系化合物包括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，环烷基和芳基，或一起表示任选含有一个或多个杂原子或基团的亚烷基 在亚烷基链中; 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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