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公开(公告)号:US08158828B2
公开(公告)日:2012-04-17
申请号:US11785251
申请日:2007-04-16
申请人: James T. Dalton , Christina Barrett , Yali He , Seoung-Soo Hong , Duane D. Miller , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
发明人: James T. Dalton , Christina Barrett , Yali He , Seoung-Soo Hong , Duane D. Miller , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
IPC分类号: C07C233/65 , A61K31/165
CPC分类号: A61K31/138 , A61K31/40 , A61K31/445 , A61K31/55 , C07D221/12
摘要: The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
摘要翻译: 本发明涉及新型选择性雌激素受体调节剂(SERM)。 SERM化合物可用于预防和/或治疗各种疾病和病症,包括预防和治疗诸如前列腺和乳腺癌,骨质疏松症,激素相关疾病,潮热或血管舒缩症状,神经系统疾病, 心血管疾病和肥胖。
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公开(公告)号:US08637706B2
公开(公告)日:2014-01-28
申请号:US13362242
申请日:2012-01-31
申请人: James T. Dalton , Christina Barrett , Duane D. Miller , Seoung-Soo Hong , Yali He , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
发明人: James T. Dalton , Christina Barrett , Duane D. Miller , Seoung-Soo Hong , Yali He , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
IPC分类号: C07C233/65 , A61K31/165
CPC分类号: A61K31/138 , A61K31/40 , A61K31/445 , A61K31/55 , C07C233/60 , C07C233/65 , C07C233/75 , C07C233/84 , C07C235/38 , C07C235/56 , C07C235/66 , C07C251/48 , C07C255/57 , C07C311/29 , C07C2601/14 , C07D221/12 , C07D265/34 , Y02A50/402 , Y02A50/411 , Y02A50/414 , Y02A50/423
摘要: The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
摘要翻译: 本发明涉及新型选择性雌激素受体调节剂(SERM)。 SERM化合物可用于预防和/或治疗各种疾病和病症,包括预防和治疗诸如前列腺和乳腺癌,骨质疏松症,激素相关疾病,潮热或血管舒缩症状,神经系统疾病, 心血管疾病和肥胖。
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公开(公告)号:US20090062341A1
公开(公告)日:2009-03-05
申请号:US11604884
申请日:2006-11-28
申请人: James T. Dalton , Christina Barrett , Yali He , Seoung-Soo Hong , Duane D. Miller , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
发明人: James T. Dalton , Christina Barrett , Yali He , Seoung-Soo Hong , Duane D. Miller , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
IPC分类号: A61K31/4545 , C07C233/64 , A61K31/166 , A61K31/445 , C07D401/02 , C07K14/72 , C07D211/60 , C07D213/81 , A61K31/44
CPC分类号: A61K31/138 , A61K31/40 , A61K31/445 , A61K31/55 , C07D221/12
摘要: The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
摘要翻译: 本发明涉及新型选择性雌激素受体调节剂(SERM)。 SERM化合物可用于预防和/或治疗各种疾病和病症,包括预防和治疗诸如前列腺和乳腺癌,骨质疏松症,激素相关疾病,潮热或血管舒缩症状,神经系统疾病, 心血管疾病和肥胖。
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公开(公告)号:US20070265296A1
公开(公告)日:2007-11-15
申请号:US11785251
申请日:2007-04-16
申请人: James Dalton , Christina Barrett , Yali He , Seoung-Soo Hong , Duane Miller , Michael Mohler , Ramesh Narayanan , Zhongzhi Wu
发明人: James Dalton , Christina Barrett , Yali He , Seoung-Soo Hong , Duane Miller , Michael Mohler , Ramesh Narayanan , Zhongzhi Wu
IPC分类号: A61K31/167 , A61K31/136 , A61K31/192 , A61K31/445 , A61P19/00 , A61P19/10 , A61P3/00 , A61P35/00 , A61P37/00 , A61P5/00 , C07C211/54 , C07C233/11 , C07C63/00 , C07D211/00 , C07D221/12
CPC分类号: A61K31/138 , A61K31/40 , A61K31/445 , A61K31/55 , C07D221/12
摘要: The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
摘要翻译: 本发明涉及新型选择性雌激素受体调节剂(SERM)。 SERM化合物可用于预防和/或治疗各种疾病和病症,包括预防和治疗诸如前列腺和乳腺癌,骨质疏松症,激素相关疾病,潮热或血管舒缩症状,神经系统疾病, 心血管疾病和肥胖。
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公开(公告)号:US20050209320A1
公开(公告)日:2005-09-22
申请号:US10963991
申请日:2004-10-14
IPC分类号: A61K20060101 , A61K31/165 , A61K31/277 , A61K31/325 , A61K39/395 , C07C235/24 , C07C255/60 , C07C271/24 , C07C309/87 , C07C317/40 , C07C323/60 , C07D207/448 , C07F9/09
CPC分类号: C07D207/448 , C07C215/76 , C07C235/16 , C07C235/24 , C07C255/60 , C07C271/24 , C07C309/87 , C07C317/46 , C07C323/60 , C07D233/74
摘要: The present invention relates to a novel class of anti-cancer compounds which selectively target androgen receptor (AR)-expressing cancer cells, such as prostate cancer cells and breast cancer cells. These agents comprise an androgen receptor (AR) binding moiety, which selectively targets the compounds to (AR)-expressing cancer cells, and a cytotoxic ablating moiety, such as a nitrogen mustard moiety. The inherent high density expression of the androgen receptor in certain cancers, such as prostate cancer and breast cancer, is thus used as a tool to selectively increase the intracellular concentration of cytotoxic compounds, such as alkylating agents, e.g. DNA alkylating agents, by selectively targeting the agents to the AR-expressing cancer cells. These agents, either alone or in a composition, are thus useful for treating, delaying the progression of, treating the recurrence of, suppressing, inhibiting or reducing the incidence of cancers characterized by the presence of AR-expressing cells, such as prostate cancer. Accordingly, the present invention provides a) methods of selectively killing an (AR)-expressing cancer cell; b) methods of inducing apoptosis in an (AR)-expressing cancer cell; c) methods of treating a cancer characterized by the presence of AR-expressing cells in a subject; d) methods of delaying the progression of a cancer characterized by the presence of AR-expressing cells in a subject; e) methods of treating the recurrence of a cancer characterized by the presence of AR-expressing cells in a subject; f) methods of suppressing, inhibiting or reducing the incidence of a cancer characterized by the presence of AR-expressing cells in a subject; and g) methods of treating metastasis of a cancer characterized by the presence of AR-expressing cells in a subject; by administering to the subject or by contacting the cancer cells with a compound comprising an androgen receptor ligand moiety and an alkylating moiety, such as the novel compounds described herein.
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