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公开(公告)号：US6054446A
公开(公告)日：2000-04-25
申请号：US998877
申请日：1997-12-24
Applicant: Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
Inventor： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC: A61K31/57 , A61K9/02 , A61K31/56 , A61K31/575 , A61K31/58 , A61P3/06 , A61P5/32 , A61P11/00 , A61P19/10 , A61P35/00 , A61P43/00 , C07J13/00 , C07J41/00 , C07J43/00 , C07J5/00
CPC classification number: C07J41/00 , C07J41/0072 , C07J41/0077 , C07J43/003 , A61K9/02
Abstract: Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.
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2.发明授权Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use 有权抗雌激素类固醇，以及相关的药物组合物和使用方法公开(公告)号：US06747018B2
公开(公告)日：2004-06-08
申请号：US10327401
申请日：2002-12-19
Applicant: Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
Inventor： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC: A61K3156
CPC classification number: C07J41/0072 , A61K9/02 , C07J41/0077 , C07J43/003
Abstract: Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.
Abstract translation: 提供了新的抗雌激素化合物，其可用于治疗多种疾病，特别是雌激素依赖性疾病。 优选的化合物具有1,3,5-三亚甲基核，并且在C-17或C-11位置被分子部分取代，这使得化合物有效地竞争性阻断雌激素与其受体的结合。 特别优选的化合物是17-脱氧-1,3,5-雌三烯。 也提供治疗方法和药物组合物。
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3.发明授权Estrone sulfamate inhibitors of estrone sulfatase, and associated pharmaceutical compositions and methods of use 失效雌酮硫酸酯酶的氨基磺酸盐抑制剂及其相关药物组合物和使用方法
公开(公告)号：US6046186A
公开(公告)日：2000-04-04
申请号：US997416
申请日：1997-12-24
Applicant: Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
Inventor： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
IPC: A61K31/565 , A61K31/57 , A61K31/575 , A61P35/00 , A61P43/00 , C07J41/00 , A61K31/56 , A61K31/58 , C07J9/00 , C07J43/00
CPC classification number: C07J41/0072 , C07J41/0005 , C07J41/0094
Abstract: Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen and lower alky, or together form a cyclic substituent (II) ##STR1## wherein Q is NH, O or CH.sub.2, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.
Abstract translation: 提供了可用作雌酮硫酸酯酶抑制剂的新型化合物。 化合物具有结构式（I），其中r1是任选的双键，R 1和R 2选自氢和低级烷基，或一起形成其中Q是NH，O或CH 2的环状取代基（II） 而其它各种取代基如本文所定义。 还提供了使用式（I）化合物治疗雌激素依赖性疾病的药物组合物和方法。
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4.发明授权Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use 有权抗雌激素类固醇，以及相关的药物组合物和使用方法公开(公告)号：US06455517B1
公开(公告)日：2002-09-24
申请号：US09918890
申请日：2001-07-30
Applicant: Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
Inventor： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC: A61K3156
CPC classification number: C07J41/00 , A61K9/02 , C07J41/0072 , C07J41/0077 , C07J43/003
Abstract: Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.
Abstract translation: 提供了新的抗雌激素化合物，其可用于治疗多种疾病，特别是雌激素依赖性疾病。 优选的化合物具有1,3,5-三亚甲基核，并且在C-17或C-11位置被分子部分取代，这使得化合物有效地竞争性阻断雌激素与其受体的结合。 特别优选的化合物是17-脱氧-1,3,5-雌三烯。 也提供治疗方法和药物组合物。
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5.发明授权Steroid inhibitors of estrone sulfatase and associated pharmaceutical compositions and methods of use 失效甾体硫酸酯酶的类固醇抑制剂及其相关药物组合物和使用方法
公开(公告)号：US5861388A
公开(公告)日：1999-01-19
申请号：US1601
申请日：1997-12-31
Applicant: Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
Inventor： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
CPC classification number: C07J71/0094
Abstract: Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) ##STR1## wherein X and Y, or Y and Z, form an oxathiazine dioxide ring or a dihydro-oxathiazine dioxide ring, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.
Abstract translation: 提供了可用作雌酮硫酸酯酶抑制剂的新型化合物。 化合物具有结构式（I）其中X和Y或Y和Z形成氧噻嗪二氧化物环或二氢 - 噻吩二氧化物环，其它各种取代基如本文所定义。 还提供了使用式（I）化合物治疗雌激素依赖性疾病的药物组合物和方法。
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Patent Agency Ranking6.发明授权Steriod inhibitors of estrone sulfatase and associated pharmaceutical compositions and methods of use 失效雌酮硫酸酯酶的Steriod抑制剂及其相关药物组合物和使用方法
公开(公告)号：US5763432A
公开(公告)日：1998-06-09
申请号：US794229
申请日：1997-01-29
Applicant: Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
Inventor： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
CPC classification number: C07J71/0094
Abstract: Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) ##STR1## wherein X and Y, or Y and Z, form an oxathiazine dioxide ring or a dihydro-oxathiazine dioxide ring, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.
Abstract translation: 提供了可用作雌酮硫酸酯酶抑制剂的新型化合物。 化合物具有结构式（I）其中X和Y或Y和Z形成氧噻嗪二氧化物环或二氢 - 噻吩二氧化物环，其它各种取代基如本文所定义。 还提供了使用式（I）化合物治疗雌激素依赖性疾病的药物组合物和方法。
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7.发明授权Synthesis of anti-estrogenic and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one 有权从21-羟基-19-去甲孕烯-4-烯-3-酮合成抗雌激素和其它治疗类固醇公开(公告)号：US06784170B2
公开(公告)日：2004-08-31
申请号：US09780990
申请日：2001-02-09
Applicant: Richard H. Peters , Jyanwei Liu , John G. Johansson , Kenneth J. Ryan , Wan-Ru Chao , Masato Tanabe
Inventor： Richard H. Peters , Jyanwei Liu , John G. Johansson , Kenneth J. Ryan , Wan-Ru Chao , Masato Tanabe
IPC: A61K3156
Abstract: Syntheses of steroids such as 3-hydroxy-7&agr;-methyl-21-[2′-methoxy-4′-(diethylaminomethyl)-phenoxy]-19-norpregna-1,3,5(10)triene citrate (“SR 16234”) and analogs thereof are provided, wherein 21-hydroxy-19-norpregna-4-en-3-one serves as a starting material or intermediate. The latter compound may be readily prepared from estrone-3-methyl ether. Certain intermediates in these syntheses also have value as therapeutic agents, for example in the treatment of prostate disorders such as prostatic cancer.
Abstract translation: 类固醇如3-羟基-7α-甲基-21- [2'-甲氧基-4' - （二乙基氨基甲基） - 苯氧基] -19-去甲基-1,3,5（10）三烯柠檬酸盐（“SR 16234” ）及其类似物，其中21-羟基-19-去甲基-4-烯-3-酮用作原料或中间体。 后一种化合物可以容易地由雌酮-3-甲基醚制备。 这些合成中的某些中间体也具有作为治疗剂的价值，例如在前列腺疾病如前列腺癌的治疗中。
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8.发明授权Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use 有权抗雌激素类固醇，以及相关的药物组合物和使用方法公开(公告)号：US06548491B2
公开(公告)日：2003-04-15
申请号：US09872825
申请日：2001-05-31
Applicant: Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
Inventor： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC: A61K3156
CPC classification number: C07J41/0072 , A61K9/02 , C07J41/0077 , C07J43/003
Abstract: Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5(10)-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5(10)-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.
Abstract translation: 提供了新的抗雌激素化合物，其可用于治疗多种疾病，特别是雌激素依赖性疾病。 优选的化合物具有1,3,5（10） - 三亚甲基核，并且在C-17或C-11位置被分子部分取代，这使得化合物有效地竞争性阻断雌激素与其受体的结合。 特别优选的化合物是17-脱氧-1,3,5（10） - 雌三烯。 也提供治疗方法和药物组合物。
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9.发明授权Stereoisomerically pure 17.alpha.-ethynyl-estra-2-en-17.beta.-ol and the 17.beta. esters thereof, methods of preparation and uses 失效立体异构纯的17α-乙炔基 - 雌-2-烯-17β-醇及其17β-酯，其制备方法和用途
公开(公告)号：US5116830A
公开(公告)日：1992-05-26
申请号：US873074
申请日：1986-06-02
Applicant: Masato Tanabe , David F. Crowe , Richard H. Peters , John G. Johansson
Inventor： Masato Tanabe , David F. Crowe , Richard H. Peters , John G. Johansson
Abstract: This invention relates to a stereoisomerically pure .DELTA..sup.2 compound of the formula (I): ##STR1## wherein: R.sup.1 is hydrogen or --(C.dbd.O)--R.sup.2, wherein:R.sup.2 is an organic substituent selected from the group consisting of alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkylalkylenes, haloalkyls, aryls, haloaryls and arylalkylenes, and their product by the process of:(a) reacting the 17.beta.-hydroxy group of 17.beta.-hydroxy-5.alpha.-estr-1-en-3-one with dihydropyran to produce the 3-keto-17.beta.-ether;(b) reducing the 3-keto-17.beta.-ether product of step (a) with lithium in ammonia;(c) reacting the product of step (b) with dialkyl chlorophosphate to produce the 3-substituted phosphate;(d) reducing the product of step (c) with lithium and ammonia to produce the .DELTA..sup.2 -protected-17.beta.-ether product;(e) hydrolysis of the produce of step (d) to product the .DELTA..sup.2 -17.beta.-hydroxy compound;(f) oxidizing the 17.beta.-hydroxy product of step (e) to produce the 17-keto compound;(g) reacting the 17-keto derivative of step (f) with acetylene magnesium halide to produce the compound of formula I where R.sup.1 is hydrogen; and(h) optionally reacting the product of step (g) with an acyl halideThe invention described herein was made in the course of work under a contract from the U.S. National Institutes of Health No. NOl-HD-2809 of the Department of Health and Human Resources.
Abstract translation: 本发明涉及式（I）的立体异构纯的DELTA 2化合物：其中：R 1是氢或 - （C = O）-R 2，其中：R 2是有机取代基，其选自 烷基，链烯基，炔基，环烷基，环烷基亚烷基，卤代烷基，芳基，卤代芳基和芳基亚烷基，以及它们的产物通过以下方法：（a）使17β-羟基-5α-雌甾-1-烯的17β-羟基与 en-3-酮与二氢吡喃反应生成3-酮-17β-醚; （b）用氨在氨中还原步骤（a）的3-酮-17β-醚产物; （c）使步骤（b）的产物与氯磷酸二烷基酯反应，生成3-取代的磷酸酯; （d）用锂和氨还原步骤（c）的产物以产生DELTA 2-保护的-17β-醚产物; （e）步骤（d）的产物的水解以产生DELTA2-17β-羟基化合物; （f）氧化步骤（e）的17β-羟基产物以制备17-酮化合物; （g）使步骤（f）的17-酮衍生物与乙炔卤化镁反应，生成其中R 1为氢的式Ⅰ化合物; 和（h）任选地使步骤（g）的产物与酰卤或酰基酸酐反应以制备其中R 1为酰基的式I化合物。 本发明还涉及用于口服给药的药物组合物，其包含式I化合物和在雌性哺乳动物中实现避孕（生育控制）的方法。 式I的化合物在雌性哺乳动物中具有抗雌激素活性，并且可用于控制生育力，基本上没有不期望的副作用。
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10.发明授权19-Norpregna- 1,3,5(10)-trien-3-ol and loweralkyl homologs thereof having postcoital antifertility activity 失效具有后肠抗生育活性的19-诺珀孕酮-1,3,5（10） - 三烯-3-醇及其低级烷基同系物
公开(公告)号：US3946052A
公开(公告)日：1976-03-23
申请号：US587256
申请日：1975-06-16
Applicant: David F. Crowe , Richard H. Peters , Masato Tanabe , George Detre
Inventor： David F. Crowe , Richard H. Peters , Masato Tanabe , George Detre
CPC classification number: C07J9/00 , C07J13/007 , C07J3/00 , C07J7/0005 , Y10S514/843
Abstract: 19-Norpregna-1,3,5(10)-trien-3-ol and loweralkyl homologs thereof wherein the alkyl group attached in the 17.beta. position contains from 2 to 7 carbon atoms. Said compounds, along with the corresponding known 17.beta.-methyl derivative, are found to have antifertility activity, and particularly postcoital antifertility activity, along with very low estrogenic activity, when administered orally to mammals.
Abstract translation: 19-诺贝格纳1,3,5（10） - 三烯-3-醇及其低级烷基同系物，其中连接在17β位的烷基含有2至7个碳原子。 发现所述化合物连同相应的已知的17β-甲基衍生物具有抗生育活性，特别是后生的抗生育活性，以及当向哺乳动物口服施用时具有非常低的雌激素活性。
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