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1. 发明授权

US06413951B2 20-fluoro-17(20)-vinyl steroids 失效
标题翻译： 20-氟-17（20） - 乙烯基类固醇
公开(公告)号：US06413951B2
公开(公告)日：2002-07-02
申请号：US09886818
申请日：2001-06-21
申请人： Norton P. Peet , Philip M. Weintraub , Joseph P. Burkhart , Cynthia A. Gates
发明人： Norton P. Peet , Philip M. Weintraub , Joseph P. Burkhart , Cynthia A. Gates
IPC分类号： A61K3156
CPC分类号： C07J13/007
摘要： The invention relates to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-5,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17 (20)-dien-3-one, 20&xgr;-fluoropregna-5,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide. The compounds of the invention have the following general formulae:
摘要翻译：本发明涉及20和xgr-氟孕烷-4,17（20） - 二烯-21-蓖麻油酸乙酯，20＆xgr-氟-3β-羟基孕烯-5,17（20） - 二烯-21-酸（20） - 二烯-3-酮，20和xgr-氟孕烷-5,17（20） - 二烯-3β，21-二醇及相关化合物，并与掺入这些化合物的组合物以及C17,20裂解酶，5α-还原酶和C17-羟化酶的抑制，以及这些化合物在治疗雄激素和雌激素介导或依赖性疾病（包括良性前列腺增生症，前列腺癌）中的用途，乳腺癌和DHT介导的疾病如痤疮和多毛症。还包括治疗与过度合成皮质醇有关的疾病，例如库欣综合征。雄激素依赖性疾病的治疗还包括与已知的雄激素受体拮抗剂如氟他胺的联合治疗。本发明化合物具有以下通式：

2. 发明授权

US5977094A Methods and compositions using .DELTA..sup.16 unsaturated C.sub.17 heterocyclic steroids useful as steroid C.sub.17-20 lyase inhibitors 失效
标题翻译：使用可用作类固醇C17-20裂解酶抑制剂的DELTA 16不饱和C17杂环类固醇的方法和组合物
公开(公告)号：US5977094A
公开(公告)日：1999-11-02
申请号：US72779
申请日：1998-05-06
申请人： Norton P. Peet , Joseph P. Burkhart , Cynthia A. Gates
发明人： Norton P. Peet , Joseph P. Burkhart , Cynthia A. Gates
IPC分类号： A61K31/58 , A61P43/00 , C07J17/00 , C07J33/00 , C07J43/00
CPC分类号： C07J17/00 , C07J33/002 , C07J43/003 , Y10S514/88
摘要： The present invention relates to methods and compositions using .DELTA..sup.16 unsaturated steroids which are useful as steroid C.sub.17-20 lyase inhibitors.
摘要翻译：本发明涉及使用可用作类固醇C17-20裂解酶抑制剂的DELTA16不饱和类固醇的方法和组合物。

3. 发明授权

US5965548A .increment..sup.16 unsaturated C.sub.17 heterocyclic steroids useful as steroid C.sub.17-20 lyase inhibitors 失效
标题翻译：增加16种不饱和C17杂环类固醇可用作类固醇C17-20裂解酶抑制剂
公开(公告)号：US5965548A
公开(公告)日：1999-10-12
申请号：US72778
申请日：1998-05-06
申请人： Norton P. Peet , Joseph P. Burkhart , Cynthia A. Gates
发明人： Norton P. Peet , Joseph P. Burkhart , Cynthia A. Gates
IPC分类号： A61K31/58 , A61P43/00 , C07J17/00 , C07J33/00 , C07J43/00
CPC分类号： C07J17/00 , C07J33/002 , C07J43/003 , Y10S514/88
摘要： The present invention relates to .DELTA..sup.16 unsaturated steroids which are useful as steroid C.sub.17-20 lyase inhibitors.
摘要翻译：本发明涉及可用作类固醇C17-20裂解酶抑制剂的DELTA 16不饱和类固醇。

4. 发明授权

US5677293A 16 unsaturated C17 heterocyclic steroids useful as steroid C17-20 lyase inhibitors 失效
标题翻译： 16种不饱和C17杂环类固醇可用作类固醇C17-20裂解酶抑制剂
公开(公告)号：US5677293A
公开(公告)日：1997-10-14
申请号：US624395
申请日：1996-07-15
申请人： Norton P. Peet , Joseph P. Burkhart , Cynthia A. Gates
发明人： Norton P. Peet , Joseph P. Burkhart , Cynthia A. Gates
IPC分类号： A61K31/58 , A61P43/00 , C07J17/00 , C07J33/00 , C07J43/00
CPC分类号： C07J17/00 , C07J33/002 , C07J43/003 , Y10S514/88
摘要： The present invention relates to .DELTA..sup.16 unsaturated C.sub.17 heterocyclic steroids which are useful as steroid C.sub.17-20 lyase inhibitors.
摘要翻译： PCT No.PCT / US94 / 11030 Sec。 371日期：1996年7月15日 102（e）日期1996年7月15日PCT 1994年9月29日PCT公布。公开号WO95 / 11914 日期1995年5月4日本发明涉及可用作类固醇C17-20裂解酶抑制剂的DELTA16不饱和C17杂环类固醇。

5. 发明授权

US5990328A Process for the preparation of 4-amino-.DELTA.4-3-ketosteroids via 4-nitro-.DELTA.4-3-ketosteroids 失效
标题翻译：通过4-硝基-DTTA 4-3-酮类固醇制备4-氨基-TATA 4-3-酮类固醇的方法
公开(公告)号：US5990328A
公开(公告)日：1999-11-23
申请号：US256353
申请日：1999-02-24
申请人： Philip M. Weintraub , Michael R. Angelastro , Cynthia A. Gates , Gary Alan Flynn , Timothy Thomas Curran , Chi-Hsin Richard King
发明人： Philip M. Weintraub , Michael R. Angelastro , Cynthia A. Gates , Gary Alan Flynn , Timothy Thomas Curran , Chi-Hsin Richard King
IPC分类号： A61K31/56 , A61P37/04 , C07J41/00
CPC分类号： C07J41/0005 , C07J41/0011 , C07J41/0066
摘要： The present invention provides 4-nitro-.DELTA..sup.4 -3-ketosteroids, their use as steroid C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and to a novel process for preparing a compound of the formula: ##STR1## comprising sequentially: a) reacting a starting compound of the formula ##STR2## with an effective amount of a strong base at an elevated or suitable temperature for a time sufficient to create the corresponding thermodynamic dienolate, followed by addition of a neutral nitrating agent to produce the 4-nitrosteroid; and then;b) reacting the 4-nitrosteroid with a suitable reducing agent.
摘要翻译：本发明提供了4-硝基-DTTA 4-3-酮类固醇，它们用作类固醇C17-20裂合酶和5α-还原酶抑制剂，以及制备下式化合物的新方法：包括：a）使起始化合物与有效量的强碱在升高或合适的温度下反应足以产生相应的热力学二烯醇化物的时间，然后加入中性硝化剂以生产4-硝基甾类; 接着; b）使4-硝基甾类与合适的还原剂反应。

6. 发明授权

US5965550A Process for the preparation of 4-amino-.DELTA..sup.4 -3-ketosteroids via 4-nitro-.DELTA..sup.4 -3-ketosteroids 失效
标题翻译：通过4-硝基-DTTA 4-3-酮类固醇制备4-氨基-TATA 4-3-酮类固醇的方法
公开(公告)号：US5965550A
公开(公告)日：1999-10-12
申请号：US10974
申请日：1998-01-22
申请人： Philip M. Weintraub , Michael R. Angelastro , Cynthia A. Gates , Timothy Thomas Curran , Gary Alan Flynn , Chi-Hsin Richard King
发明人： Philip M. Weintraub , Michael R. Angelastro , Cynthia A. Gates , Timothy Thomas Curran , Gary Alan Flynn , Chi-Hsin Richard King
IPC分类号： A61K31/56 , A61P37/04 , C07J41/00
CPC分类号： C07J41/0005 , C07J41/0011 , C07J41/0066
摘要： The invention discloses 3-ketosteroids of the following formula used to inhibit steroid C.sub.17-20 lyase: ##STR1## wherein R is OH, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkanol, COCH.sub.2 OH, CO.sub.2 H, CONR.sub.7 R.sub.8, cyclopropyloxy, cyclopropylamino, acetylthioalkane, 2,2-dimethyldioxolan4-yl, 1,2-dihydroxyethyl and C.sub.1-4 alkylthiol;R.sub.1 is hydrogen, hydroxy or C.sub.1-6 alkyl;R and R.sub.1 together may indicate .dbd.O, that is an oxygen double bonded to the 17 carbon;R.sub.2, R.sub.3, and R.sub.4 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 and R.sub.6 are each independently hydrogen or OH;R.sub.5 and R.sub.6 together may indicate .dbd.O, that is an oxygen double bonded to the 11 carbon;R.sub.7 is hydrogen or C.sub.1 -C.sub.8 alkyl;R.sub.8 is C.sub.1 -C.sub.8 alkyl; andwith the proviso that, when R is OH, then R.sub.1 is hydrogen; andwith the proviso that, when R.sub.5 is OH, then R.sub.6 is hydrogen.
摘要翻译：本发明公开了用于抑制类固醇C17-20裂解酶的下式的3-酮甾烷：其中R是OH，C 1 -C 6烷酰基，C 1 -C 6烷酰氧基，C 1 -C 4烷醇，COCH 2 OH，CO 2 H，CONR 7 R 8，环丙氧基，环丙基氨基，乙酰基硫代烷，2,2-二甲基二氧戊环-4-基，1,2-二羟基乙基和C 1-4烷基硫醇; R1是氢，羟基或C1-6烷基; R和R 1可以表示= O，即与17碳双键键合的氧; R2，R3和R4各自独立地为氢或C1-C6烷基; R5和R6各自独立地为氢或OH; R5和R6一起可以表示= O，即与11碳双键结合的氧; R7是氢或C1-C8烷基; R8是C1-C8烷基; 并且条件是当R是OH时，则R1是氢; 并且条件是当R5是OH时，则R6是氢。

7. 发明授权

US5486511A 4-amino-17.beta.-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17.beta.-(cyclopropylamino)androst-4-en-3-one and related compounds as C.sub.17-20 lyase and 5.alpha.-reductase 失效
标题翻译： 4-氨基-17β-（环丙氧基）雄甾-4-烯-3-酮，4-氨基-17β-（环丙基氨基）雄甾-4-烯-3-酮和相关化合物，如C17-20裂合酶和5α - 还原酶
公开(公告)号：US5486511A
公开(公告)日：1996-01-23
申请号：US231434
申请日：1994-05-02
申请人： Philip M. Weintraub , Cynthia A. Gates , Michael R. Angelastro , Timothy T. Curran , J. O'Neal Johnston
发明人： Philip M. Weintraub , Cynthia A. Gates , Michael R. Angelastro , Timothy T. Curran , J. O'Neal Johnston
IPC分类号： A61K31/565 , C07J41/00 , C07J71/00 , C07J1/00
CPC分类号： C07J41/0011 , C07J41/0027 , C07J71/001
摘要： This invention is directed to 4-amino-17.beta.-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17.beta.-(cyclopropylylamino)androst-4-en-3-one and related compounds, a process for their synthesis, a pharmaceutical composition having C.sub.17-20 lyase and 5.alpha.-reductase inhibitory activity, the use of the present compounds as C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and also to a method for using such compounds in the treatment of androgen and/or estrogen dependent disorders, including bengin prostatic hyperplasia, breast cancer and prostatic cancer. The 4-amino compounds are prepared by the reaction of the appropriate 4,5-epoxide with sodium azide in an inert solvent in the presence of a catalytic amount of strong acid under appropriate reaction conditions. Alternatively, the 4-amino compounds are prepared by first nitration and then reduction of the appropriate steroid under appropriate reaction conditions.
摘要翻译：本发明涉及4-氨基-17β-（环丙氧基）雄甾-4-烯-3-酮，4-氨基-17β-（环丙基氨基）雄甾-4-烯-3-酮及相关化合物，一种方法为了合成，具有C17-20裂合酶和5α-还原酶抑制活性的药物组合物，本发明化合物用作C17-20裂合酶和5α-还原酶抑制剂，以及使用这些化合物治疗雄激素和/或雌激素依赖性疾病，包括前列腺增生，乳腺癌和前列腺癌。在合适的反应条件下，在惰性溶剂中，在催化量的强酸存在下，通过适当的4,5-环氧化物与叠氮化钠的反应来制备4-氨基化合物。或者，4-氨基化合物通过首先硝化然后在合适的反应条件下还原合适的类固醇来制备。

8. 发明授权

US5750744A Process for the preparation of 4-amino- 4-3-ketosteroids via 4-nitro- 4-3-ketosteroids 失效
标题翻译：通过4-硝基-4- 3-酮类固醇制备4-氨基-4- 3-酮类固醇的方法
公开(公告)号：US5750744A
公开(公告)日：1998-05-12
申请号：US737031
申请日：1997-02-11
申请人： Philip M. Weintraub , Cynthia A. Gates , Michael R. Angelastro , Gary Alan Flynn , Chi-Hsin Richard King , Timothy Thomas Curran
发明人： Philip M. Weintraub , Cynthia A. Gates , Michael R. Angelastro , Gary Alan Flynn , Chi-Hsin Richard King , Timothy Thomas Curran
IPC分类号： A61K31/56 , A61P37/04 , C07J41/00 , C07J1/00
CPC分类号： C07J41/0005 , C07J41/0011 , C07J41/0066
摘要： The present invention provides 4-nitro-.DELTA..sup.4 -3-ketosteroids, their use as steroid C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and to a novel process for preparing a compound of the formula: ##STR1## comprising sequentially: a) reacting a starting compound of the formula ##STR2## with an effective amount of a strong base at an elevated or suitable temperature for a time sufficient to create the corresponding thermodynamic dienolate, followed by addition of a neutral nitrating agent to produce the 4-nitro-steroid; and then; b) reacting the 4-nitrosteroid with a suitable reducing agent.
摘要翻译： PCT No.PCT / US95 / 04399 Sec。 371日期1997年2月11日 102（e）1997年2月11日PCT PCT 1995年4月11日PCT公布。公开号WO95 / 29932 日期：1995年11月9日本发明提供4-硝基-D3TA 4-3-酮类固醇，它们用作类固醇C17-20裂合酶和5α-还原酶抑制剂，以及制备下式化合物的新方法： I顺序地包括：a）在升高的或合适的温度下使式Ⅰ的起始化合物与有效量的强碱反应足以产生相应的热力学二烯醇化物的时间，然后加入中性硝化剂以产生4-硝基类固醇; 接着; b）使4-硝基甾类与合适的还原剂反应。

9. 发明授权

US5143909A Aminosteroids in a method for inhibiting C17-20 lyase 失效
标题翻译：用于抑制C17-20LYASE的方法中的氨基酸
公开(公告)号：US5143909A
公开(公告)日：1992-09-01
申请号：US671555
申请日：1991-03-19
申请人： Philip M. Weintraub , Cynthia A. Gates , Thomas R. Blohm
发明人： Philip M. Weintraub , Cynthia A. Gates , Thomas R. Blohm
IPC分类号： A61K31/57 , A61P13/02 , A61P15/00 , C07J41/00 , C07J71/00
CPC分类号： C07J41/0011 , C07J41/0005 , C07J71/001
摘要： The present invention relates to a method for the inhibition of C.sub.17-20 lyase enzyme which comprises administering to a patient in need of such inhibition, an effective amount of certain 4-amino-17-(hydroxyalkyl or dihydroxyalkyl)steroids or their esters or ethers. Certain of the aminosteroids used in the process are novel compounds.

10. 发明授权

US06365597B1 4-aza steroids 失效
标题翻译： 4-氮杂类固醇
公开(公告)号：US06365597B1
公开(公告)日：2002-04-02
申请号：US08798258
申请日：1997-02-11
申请人： James R. Pribish , Cynthia A. Gates , Philip M. Weintraub
发明人： James R. Pribish , Cynthia A. Gates , Philip M. Weintraub
IPC分类号： A61K3144
CPC分类号： A61K31/568 , C07D221/18
摘要： The invention related to 4-aza-17&bgr;-(cyclopropoxy)-androst-5&agr;-androstan-3-one, 4-aza-17&bgr;-(cyclopropylamino)-androst-4-en-3-one and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17-20 lyase, 5&agr;-reductase and C17&agr;-hydroxylase and to the use of these compounds in the treatment of androgen and estrogen mediated disorders, including benign prostatic hyperplasia, androgen mediated prostate cancer, estrogen mediated breast cancer and to DHT-mediated disorders such as acne. Disorders relating to the oversynthesis of cortisol, for example, Cushing's Syndrome, are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide. The compounds of the invention have the following general formula:
摘要翻译：本发明涉及4-氮杂-17β-（环丙氧基） - 雄甾-5α-雄甾烷-3-酮，4-氮杂-17β-（环丙基氨基） - 雄甾-4-烯-3-酮及相关化合物，这些化合物，以及C17-20裂解酶，5α-还原酶和C17alpha-羟化酶的抑制以及这些化合物在治疗雄激素和雌激素介导的疾病中的应用，包括良性前列腺增生，雄激素介导的前列腺癌，雌激素介导乳腺癌和DHT介导的疾病如痤疮。与皮质醇过度合成有关的疾病，例如库欣综合征，也包括在内。雄激素依赖性疾病的治疗还包括与已知的雄激素受体拮抗剂如氟他胺的联合治疗。本发明的化合物具有以下通式：

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