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1. 发明授权

US06503896B1 Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use 有权
公开(公告)号：US06503896B1
公开(公告)日：2003-01-07
申请号：US09872826
申请日：2001-05-31
申请人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
发明人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC分类号： A61K3156
CPC分类号： C07J41/0072 , A61K9/02 , C07J41/0077 , C07J43/003
摘要： 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.

2. 发明授权

US06281205B1 Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use 有权
标题翻译：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：US06281205B1
公开(公告)日：2001-08-28
申请号：US09220408
申请日：1998-12-24
申请人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
发明人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC分类号： A61K3156
CPC分类号： C07J41/00 , A61K9/02 , C07J41/0072 , C07J41/0077 , C07J43/003
摘要： 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.
摘要翻译：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。

3. 发明授权

US06455517B1 Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use 有权
标题翻译：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
申请人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
发明人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC分类号： A61K3156
CPC分类号： C07J41/00 , A61K9/02 , C07J41/0072 , C07J41/0077 , C07J43/003
摘要： 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.
摘要翻译：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。

4. 发明授权

US06747018B2 Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use 有权
标题翻译：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
申请人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
发明人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC分类号： A61K3156
CPC分类号： C07J41/0072 , A61K9/02 , C07J41/0077 , C07J43/003
摘要： 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.
摘要翻译：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。

5. 发明授权

US6054446A Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use 失效
公开(公告)号：US6054446A
公开(公告)日：2000-04-25
申请号：US998877
申请日：1997-12-24
申请人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
发明人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC分类号： 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分类号： C07J41/00 , C07J41/0072 , C07J41/0077 , C07J43/003 , A61K9/02
摘要： 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.

6. 发明授权

US06548491B2 Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use 有权
标题翻译：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
申请人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
发明人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC分类号： A61K3156
CPC分类号： C07J41/0072 , A61K9/02 , C07J41/0077 , C07J43/003
摘要： 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.
摘要翻译：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。

7. 发明授权

US07666897B2 Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents 有权
标题翻译：吲哚-3-甲醇代谢物的类似物作为化学治疗和化学预防剂
公开(公告)号：US07666897B2
公开(公告)日：2010-02-23
申请号：US12205532
申请日：2008-09-05
申请人： Ling Jong , Wan-Ru Chao
发明人： Ling Jong , Wan-Ru Chao
IPC分类号： A61K31/40 , C07D209/00
CPC分类号： C07D487/04 , C07D209/08 , C07D209/30 , C07D209/42
摘要： Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds has the structure of formula (IV) wherein: R1, R2, R3, R4, R5, R6, R7, R8, R5A, R6A, R7A, R8A, R22 and R23 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
摘要翻译：提供了可用作化学治疗和化学预防剂的新型化合物。化合物是吲哚-3-甲醇代谢物的类似物，其中选择化合物的结构和取代基以增强化合物的总体功效，特别是关于治疗活性，口服生物利用度，长期安全性，患者耐受性和治疗窗口。这些化合物不仅可用于治疗癌症，还可用于预防癌症。新型化合物的一类优选具有式（Ⅳ）的结构，其中R1，R2，R3，R4，R5，R6，R7，R8，R5A，R6A，R7A，R8A，R22和R23定义如下。还提供药物组合物，以及合成和使用的方法。

8. 发明授权

US06800655B2 Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents 有权
标题翻译：吲哚-3-甲醇代谢物的类似物作为化学治疗和化学预防剂
公开(公告)号：US06800655B2
公开(公告)日：2004-10-05
申请号：US10224979
申请日：2002-08-20
申请人： Ling Jong , Wan-Ru Chao
发明人： Ling Jong , Wan-Ru Chao
IPC分类号： A61K31403
CPC分类号： C07D487/04 , C07D209/08 , C07D209/30 , C07D209/42
摘要： Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds have the structure of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
摘要翻译：提供了可用作化学治疗和化学预防剂的新型化合物。化合物是吲哚-3-甲醇代谢物的类似物，其中选择化合物的结构和取代基以增强化合物的总体功效，特别是关于治疗活性，口服生物利用度，长期安全性，患者耐受性和治疗窗口。这些化合物不仅可用于治疗癌症，还可用于预防癌症。一类优选的化合物具有式（I）的结构，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7， R 8，R 9，R 10，R 11和R 12如本文所定义。还提供药物组合物，以及合成和使用的方法。

9. 发明授权

US07429610B2 Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents 有权
标题翻译：吲哚-3-甲醇代谢物的类似物作为化学治疗和化学预防剂
公开(公告)号：US07429610B2
公开(公告)日：2008-09-30
申请号：US11350232
申请日：2006-02-07
申请人： Ling Jong , Wan-Ru Chao
发明人： Ling Jong , Wan-Ru Chao
IPC分类号： A61K31/40 , C07D209/00
CPC分类号： C07D487/04 , C07D209/08 , C07D209/30 , C07D209/42
摘要： Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds have the structure of formula (III) wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, R20, and R21 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
摘要翻译：提供了可用作化学治疗和化学预防剂的新型化合物。化合物是吲哚-3-甲醇代谢物的类似物，其中选择化合物的结构和取代基以增强化合物的总体功效，特别是关于治疗活性，口服生物利用度，长期安全性，患者耐受性和治疗窗口。这些化合物不仅可用于治疗癌症，还可用于预防癌症。一类优选的化合物具有式（III）的结构，其中R 1，R 2，R 3，R 3， R 4，R 5，R 6，R 7，R 8，R 8， 11，R 12，R 20和R 21在本文中定义。还提供药物组合物，以及合成和使用的方法。

10. 发明授权

US07078427B2 Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents 有权
标题翻译：吲哚-3-甲醇代谢物的类似物作为化学治疗和化学预防剂
公开(公告)号：US07078427B2
公开(公告)日：2006-07-18
申请号：US10772036
申请日：2004-02-03
申请人： Ling Jong , Wan-Ru Chao
发明人： Ling Jong , Wan-Ru Chao
IPC分类号： A61K31/40 , C07D209/02
CPC分类号： C07D487/04 , C07D209/08 , C07D209/30 , C07D209/42
摘要： Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds have the structure of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
摘要翻译：提供了可用作化学治疗和化学预防剂的新型化合物。化合物是吲哚-3-甲醇代谢物的类似物，其中选择化合物的结构和取代基以增强化合物的总体功效，特别是关于治疗活性，口服生物利用度，长期安全性，患者耐受性和治疗窗口。这些化合物不仅可用于治疗癌症，还可用于预防癌症。一类优选的新化合物具有式（I）的结构，其中R 1，R 2，R 3，R 3， R 4，R 5，R 6，R 7，R 8，R 8， 9，R 10，R 11和R 12在本文中定义。还提供药物组合物，以及合成和使用的方法。

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