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1. 发明授权

US06376687B1 Steroid sulfatase inhibitors and methods for making and using the same 失效
标题翻译：类固醇硫酸酯酶抑制剂及其制备和使用方法
公开(公告)号：US06376687B1
公开(公告)日：2002-04-23
申请号：US09490302
申请日：2000-01-24
申请人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
发明人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
IPC分类号： C07J300
CPC分类号： C07J41/0072 , C07J41/0005 , C07J41/0011 , C07J41/0066 , C07J71/0094
摘要： Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient 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化合物。这些化合物通常包含在C17位置取代的类固醇核。还公开了合成这些化合物并将其用于治疗和/或预防性治疗患者的方法。

2. 发明授权

US06638923B2 Estra-1,3,5(10),16-tetraene derivatives 失效
标题翻译： Estra-1,3,5（10），16-四烯衍生物
公开(公告)号：US06638923B2
公开(公告)日：2003-10-28
申请号：US09859599
申请日：2001-05-18
申请人： Yoji Ino , Nobuyoshi Amishiro , Taisuke Nakata , Hiroyuki Ishida , Shiro Akinaga , Chikara Murakata , Pui-Kai Li
发明人： Yoji Ino , Nobuyoshi Amishiro , Taisuke Nakata , Hiroyuki Ishida , Shiro Akinaga , Chikara Murakata , Pui-Kai Li
IPC分类号： A61K3156
CPC分类号： C07J3/00
摘要： Estra-1,3,5(10),16-tetraene derivatives represented by the following formula (I): (wherein R1 is as defined by the present specification.
摘要翻译：由下式（I）表示的Estra-1,3,5（10），16-四烯衍生物:(其中R 1如本说明书所定义）。

3. 发明授权

US06399595B1 Steroid sulfatase inhibitors and methods for making and using the same 失效
公开(公告)号：US06399595B1
公开(公告)日：2002-06-04
申请号：US09921668
申请日：2001-08-03
申请人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
发明人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
IPC分类号： A61K3156
CPC分类号： C07J41/0072 , C07J41/0005 , C07J41/0011 , C07J41/0066 , C07J71/0094
摘要： Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.

4. 发明授权

US06288050B1 Steroid sulfatase inhibitors and methods for making and using the same 失效
标题翻译：类固醇硫酸酯酶抑制剂及其制备和使用方法
公开(公告)号：US06288050B1
公开(公告)日：2001-09-11
申请号：US09236842
申请日：1999-01-25
申请人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
发明人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
IPC分类号： A61K3154
CPC分类号： C07J41/0072 , C07J41/0005 , C07J41/0011 , C07J41/0066 , C07J71/0094
摘要： Sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.
摘要翻译：公开了可用于治疗雌激素依赖性疾病的硫酸酯酶抑制剂化合物。这些化合物通常包含在C17位置取代的类固醇核。还公开了合成这些化合物并将其用于治疗和/或预防性治疗患者的方法。

5. 发明授权

US06262043B1 Estra-1,3,5(10),16-tetraene derivatives 失效
标题翻译： Estra-1,3,5（10），16-四烯衍生物
公开(公告)号：US06262043B1
公开(公告)日：2001-07-17
申请号：US09548930
申请日：2000-04-13
申请人： Yoji Ino , Nobuyoshi Amishiro , Taisuke Nakata , Hiroyuki Ishida , Shiro Akinaga , Chikara Murakata , Pui-Kai Li
发明人： Yoji Ino , Nobuyoshi Amishiro , Taisuke Nakata , Hiroyuki Ishida , Shiro Akinaga , Chikara Murakata , Pui-Kai Li
IPC分类号： A61K3156
CPC分类号： C07J3/00
摘要： Estra-1,3,5(10),16-tetraene derivatives represented by the following formula (I): (wherein R1 represents hydroxy, alkoxy, or NR2R3 (wherein R2 and R3 are the same or different, and each represents hydrogen, straight-chain lower alkyl having 1 to 3 carbon atoms, or branched-chain lower alkyl having 3 to 8 carbon atoms)), or pharmaceutically acceptable salts thereof.
摘要翻译：由下式（I）表示的Estra-1,3,5（10），16-四烯衍生物:(其中R1表示羟基，烷氧基或NR2R3（其中R2和R3相同或不同，各自表示氢，具有1至3个碳原子的直链低级烷基或具有3至8个碳原子的支链低级烷基））或其药学上可接受的盐。

6. 发明授权

US06436918B1 Steroid sulfatase inhibitors and methods for making and using the same 失效
公开(公告)号：US06436918B1
公开(公告)日：2002-08-20
申请号：US10005516
申请日：2001-11-08
申请人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
发明人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
IPC分类号： A61K3156
CPC分类号： C07J41/0072 , C07J41/0005 , C07J41/0011 , C07J41/0066 , C07J71/0094
摘要： Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.

7. 发明授权

US06288107B1 Compounds for the treatment of estrogen-dependent illnesses and methods for making and using the same 失效
标题翻译：用于治疗雌激素依赖性疾病的化合物及其制备和使用方法
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。

8. 发明授权

US5866603A Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use 失效
标题翻译：雌1,3,5（10）三烯-17-酮，3-氨基化合物的衍生物及其用途
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。

9. 发明申请

US20110212911A1 TRANSCRIPTION FACTOR INHIBITORS AND RELATED COMPOSITIONS, FORMULATIONS AND METHODS 有权
标题翻译：转录因子抑制剂及相关成分，制剂和方法
公开(公告)号：US20110212911A1
公开(公告)日：2011-09-01
申请号：US12954038
申请日：2010-11-24
申请人： Pui-Kai Li , Chenglong Li , Jiayuh Lin
发明人： Pui-Kai Li , Chenglong Li , Jiayuh Lin
IPC分类号： A61K31/18 , C07C311/29 , C07C303/38 , C12N5/00 , A61K31/704 , A61K31/7068 , C12Q1/02 , C12Q1/68 , A61P35/00
CPC分类号： C07C311/16 , A61K31/18 , A61K31/704 , A61K31/7068 , C07C303/38 , C07C303/40 , C07C311/29 , C07C2603/22 , G01N33/5008
摘要： The present invention provides small molecules useful to affect cancer cells, along with related methods. The present compounds, formulations, kits and methods are useful for a variety of research, diagnostic and therapeutic purposes. STAT3 inhibitors, particularly LLL12, are disclosed. The STAT3 inhibitors are useful to treat breast cancer in general and breast cancer initiating cells in particular.
摘要翻译：本发明提供了可用于影响癌细胞的小分子以及相关方法。本发明的化合物，制剂，试剂盒和方法可用于各种研究，诊断和治疗目的。公开了STAT3抑制剂，特别是LLL12。 STAT3抑制剂一般可用于治疗乳腺癌，特别是乳腺癌起始细胞。

10. 发明授权

US07960548B2 Keratinocyte growth factor receptor—tyrosine specific inhibitors for the prevention of cancer metastatis 失效
标题翻译：角质形成细胞生长因子受体 - 酪氨酸特异性抑制剂用于预防癌症转移
公开(公告)号：US07960548B2
公开(公告)日：2011-06-14
申请号：US11414890
申请日：2006-05-01
申请人： J. Thomas Pento , Pui-Kai Li , Robert W. Brueggemeier , John C. Hackett
发明人： J. Thomas Pento , Pui-Kai Li , Robert W. Brueggemeier , John C. Hackett
IPC分类号： C07D471/02 , C07D215/22 , C07D215/227
CPC分类号： C07D209/34 , C07D215/22 , C07D215/227 , C07D215/48 , C07D403/06 , C07D491/04
摘要： Compounds and methods for treating, inhibiting, or delaying the onset of cancer in a subject by administering a therapeutically effective amount of a keratinocyte growth factor receptor tyrosine kinase (KGFR TK) inhibitor to the subject in need of such treatment. Also provided are compounds and methods for the treating, inhibiting, or delaying the onset of metastasis in a subject with cancer by administering a therapeutically effective amount of a KGFR TK inhibitor to the subject in need of such treatment.
摘要翻译：通过向需要这种治疗的受试者施用治疗有效量的角质形成细胞生长因子受体酪氨酸激酶（KGFR TK）抑制剂来治疗，抑制或延迟受试者的癌症发作的化合物和方法。还提供了通过向需要这种治疗的受试者施用治疗有效量的KGFR TK抑制剂来治疗，抑制或延迟患有癌症的受试者的转移起始的化合物和方法。

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