公开(公告)号：US5880115A

公开(公告)日：1999-03-09

申请号：US897247

申请日：1997-07-18

申请人： Pui-Kai Li ,  Kyle W. Selcer

发明人： Pui-Kai Li ,  Kyle W. Selcer

IPC分类号： A61K31/56 ,  A61K31/565 ,  A61P5/32 ,  A61P35/00 ,  A61P43/00 ,  C07J41/00 ,  C07J3/00

CPC分类号： C07J41/0005 ,  C07J41/0072

摘要： Sulfatase inhibitor compounds having the formula: ##STR1## wherein X, Y, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification. The compounds are useful in the treatment of estrogen dependent illnesses. Methods for synthesizing these compounds are also disclosed.

摘要翻译： 具有下式的硫酸酯酶抑制剂化合物：其中X，Y，R 1，R 2和R 3如说明书中所定义。 该化合物可用于治疗雌激素依赖性疾病。 还公开了合成这些化合物的方法。

公开(公告)号：US06248780B1

公开(公告)日：2001-06-19

申请号：US09164889

申请日：1998-10-01

申请人： Pui-Kai Li ,  Kyle W. Selcer

发明人： Pui-Kai Li ,  Kyle W. Selcer

IPC分类号： A61K31255

CPC分类号： C07C307/02

摘要： Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.

公开(公告)号：US06288107B1

公开(公告)日：2001-09-11

申请号：US09536331

申请日：2000-03-24

申请人： Pui-Kai Li ,  Kyle W. Selcer

发明人： Pui-Kai Li ,  Kyle W. Selcer

IPC分类号： A61K3138

CPC分类号： C07C307/02

摘要： Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.

摘要翻译： 公开了用于治疗雌激素依赖性疾病的新型硫酸酯酶抑制剂/雌激素受体阻断剂化合物。 化合物通常包含氨基磺酸酯部分和芳族的雌激素受体阻断剂部分。 还公开了合成这些化合物并将其用于治疗和/或预防性治疗雌激素依赖性疾病的方法。

公开(公告)号：US5866603A

公开(公告)日：1999-02-02

申请号：US476360

申请日：1995-06-07

申请人： Pui-Kai Li ,  Kyle W. Selcer

发明人： Pui-Kai Li ,  Kyle W. Selcer

IPC分类号： C07J41/00

CPC分类号： C07J41/0005

摘要： This invention discloses compounds useful as steroid sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R is selected from the group consisting of hydrogen, a lower alkyl group, an alkoxy group, halogen, NH.sub.2, NO.sub.2, C.tbd.N and N.dbd.C.dbd.S; and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiols, estradiolesters, pregnenolone, substituted estrones, substituted dehydroepiandrosterones, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The compounds also comprise the formula (5) ##STR2## wherein (a) R.sub.1 is hydrogen and R.sub.2 is selected from the group consisting of SO.sub.2 CF.sub.3, SO.sub.2 NH.sub.2, SO.sub.2 (C.sub.1 -C.sub.6 -alkyl), COCF.sub.3, CONH.sub.2, CO(C.sub.1 -C.sub.6 -alkyl); and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiol, estradiolester, pregnenolone, substituted estrones, substituted dehydroepiandrosterone, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The invention also discloses methods of treating a patient therapeutically and prophylactically for estrogen dependent diseases with the compounds of this invention.

摘要翻译： 本发明公开了可用作类固醇硫酸酯酶抑制剂的化合物。 化合物包括式（1）其中（a）R选自氢，低级烷基，烷氧基，卤素，NH 2，NO 2，C 3 N 3，N = C = S; 环系ABCD是选自雌酮，脱氢表雄酮，雌二醇，雌二醇，孕烯醇酮，取代的雌酮，取代的脱氢表雄甾酮，取代的雌二醇，取代的雌二醇酯和取代的孕烯醇酮的类固醇核。 化合物还包括式（5）其中（a）R 1是氢，R 2选自SO 2 CF 3，SO 2 NH 2，SO 2（C 1 -C 6烷基），COCF 3，CONH 2，CO（ C 1 -C 6 - 烷基）; 环系ABCD是选自雌酮，脱氢表雄酮，雌二醇，雌二醇，孕烯醇酮，取代的雌酮，取代的脱氢表雄酮，取代的雌二醇，取代的雌二醇酯和取代的孕烯醇酮的类固醇核。 本发明还公开了用本发明化合物治疗和预防性治疗雌激素依赖性疾病的方法。

公开(公告)号：US06716880B2

公开(公告)日：2004-04-06

申请号：US10174092

申请日：2002-06-18

申请人： Pui-Kai Li ,  Kyle W. Selcer

发明人： Pui-Kai Li ,  Kyle W. Selcer

IPC分类号： A61K3118

CPC分类号： C07C307/02

摘要： Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.

摘要翻译： 公开了用于治疗雌激素依赖性疾病的新型硫酸酯酶抑制剂/雌激素受体阻断剂化合物。 化合物通常包含氨基磺酸酯部分和芳族的雌激素受体阻断剂部分。 还公开了合成这些化合物并将其用于治疗和/或预防性治疗雌激素依赖性疾病的方法。

公开(公告)号：US5677292A

公开(公告)日：1997-10-14

申请号：US607797

申请日：1996-02-27

申请人： Pui-Kai Li ,  Kyle W. Selcer

发明人： Pui-Kai Li ,  Kyle W. Selcer

IPC分类号： C07J41/00 ,  A61K31/565

CPC分类号： C07J41/0005

摘要： This invention discloses compounds useful as steroid sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R is selected from the group consisting of hydrogen, a lower alkyl group, an alkoxy group, halogen, NH.sub.2, NO.sub.2, C.tbd.N and N.dbd.C.dbd.S; and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiols, estradiolesters, pregnenolone, substituted estrones, substituted dehydroepiandrosterones, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The compounds also comprise the formula (5) ##STR2## wherein (a) R.sub.1 is hydrogen and R.sub.2 is selected from the group consisting of SO.sub.2 CF.sub.3, SO.sub.2 NH.sub.2, SO.sub.2 (C.sub.1 -C.sub.6 -alkyl), COCF.sub.3, CONH.sub.2, CO(C.sub.1 -C.sub.6 -alkyl); and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiol, estradiolester, pregnenolone, substituted estrones, substituted dehydroepiandrosterone, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The invention also discloses methods of treating a patient therapeutically and prophylactically for estrogen dependent diseases with the compounds of this invention.

摘要翻译： 本发明公开了可用作类固醇硫酸酯酶抑制剂的化合物。 化合物包括式（1）其中（a）R选自氢，低级烷基，烷氧基，卤素，NH 2，NO 2，C 3 N 3，N = C = S; 环系ABCD是选自雌酮，脱氢表雄酮，雌二醇，雌二醇，孕烯醇酮，取代的雌酮，取代的脱氢表雄甾酮，取代的雌二醇，取代的雌二醇酯和取代的孕烯醇酮的类固醇核。 化合物还包括式（5）其中（a）R 1是氢，R 2选自SO 2 CF 3，SO 2 NH 2，SO 2（C 1 -C 6烷基），COCF 3，CONH 2，CO（ C 1 -C 6 - 烷基）; 环系ABCD是选自雌酮，脱氢表雄酮，雌二醇，雌二醇，孕烯醇酮，取代的雌酮，取代的脱氢表雄酮，取代的雌二醇，取代的雌二醇酯和取代的孕烯醇酮的类固醇核。 本发明还公开了用本发明化合物治疗和预防性治疗雌激素依赖性疾病的方法。

公开(公告)号：US06433000B1

公开(公告)日：2002-08-13

申请号：US09845850

申请日：2001-04-30

申请人： Pui-Kai Li ,  Kyle W. Selcer

发明人： Pui-Kai Li ,  Kyle W. Selcer

IPC分类号： C07D20944

CPC分类号： C07C307/02

摘要： Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.

摘要翻译： 公开了用于治疗雌激素依赖性疾病的新型硫酸酯酶抑制剂/雌激素受体阻断剂化合物。 化合物通常包含氨基磺酸酯部分和芳族的雌激素受体阻断剂部分。 还公开了合成这些化合物并将其用于治疗和/或预防性治疗雌激素依赖性疾病的方法。

公开(公告)号：US5571933A

公开(公告)日：1996-11-05

申请号：US341410

申请日：1994-11-17

申请人： Pui-Kai Li ,  Kyle W. Selcer

发明人： Pui-Kai Li ,  Kyle W. Selcer

IPC分类号： C07J41/00

CPC分类号： C07J41/0005

摘要： This invention discloses compounds useful as steroid inhibitors. The compounds comprise the formula (5) ##STR1## wherein (a) R.sub.1 is hydrogen and R.sub.2 is selected from the group consisting of SO.sub.2 CF.sub.3, SO.sub.2 NH.sub.2, SO.sub.2 (C.sub.1 -C.sub.6 -alkyl), COCF.sub.3, CONH.sub.2, CO(C.sub.1-C.sub.6 -alkyl); and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiol, estradiolester, pregnenolone, substituted estrones, substituted dehydroepiandrosterone, substituted estradiols, substituted estradiolesters and substituted pregnenolone. Preferably the steroid nucleus is selected from the group consisting of estrone, dehydropeiandrosterone and pregnenolone. The invention also discloses methods of treating a patient therapeutically and prophylactically for estrogen dependent diseases with the compounds of this invention.

摘要翻译： 本发明公开了可用作类固醇抑制剂的化合物。 化合物包括式（5）其中（a）R 1是氢，R 2选自SO 2 CF 3，SO 2 NH 2，SO 2（C 1 -C 6 - 烷基），COCF 3，CONH 2，CO（C 1 -C 1-6 - 烷基）; 环系ABCD是选自雌酮，脱氢表雄酮，雌二醇，雌二醇，孕烯醇酮，取代的雌酮，取代的脱氢表雄酮，取代的雌二醇，取代的雌二醇酯和取代的孕烯醇酮的类固醇核。 优选地，类固醇核选自雌酮，脱水雄酮和孕烯醇酮。 本发明还公开了用本发明化合物治疗和预防性治疗雌激素依赖性疾病的方法。