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11. 发明申请

US20050209320A1 Anti-cancer compounds and methods of use thereof 审中-公开
公开(公告)号：US20050209320A1
公开(公告)日：2005-09-22
申请号：US10963991
申请日：2004-10-14
申请人： Duane Miller , Mitchell Steiner , Karen Veverka , Christina Barrett , Seoungsoo Hong
发明人： Duane Miller , Mitchell Steiner , Karen Veverka , Christina Barrett , Seoungsoo Hong
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.

12. 发明申请

US20060019989A1 Compositions comprising 5-alpha reductase inhibitors and SERMs and methods of use thereof 审中-公开
标题翻译：包含5-α还原酶抑制剂和SERM的组合物及其使用方法
公开(公告)号：US20060019989A1
公开(公告)日：2006-01-26
申请号：US10895401
申请日：2004-07-21
申请人： Mitchell Steiner , Karen Veverka , Duane Miller
发明人： Mitchell Steiner , Karen Veverka , Duane Miller
IPC分类号： A61K31/138 , A61K31/47
CPC分类号： A61K31/138 , A61K31/47 , A61K31/56 , A61K45/06 , A61K2300/00
摘要： This invention provides for combinations of 5 alpha reductase inhibitors and SERMs. These combinations are useful in: 1) preventing prostate carcinogenesis in a subject; 2) preventing the recurrence of, suppressing, inhibiting or reducing the incidence of prostate carcinogenesis in a subject; 3) treating a subject with prostate cancer; 4) suppressing, inhibiting or reducing the incidence of prostate cancer in a subject; 5) treating a subject with pre-malignant lesions of prostate cancer; 6) suppressing, inhibiting or reducing the incidence of pre-malignant lesions of prostate cancer in a subject; 7) reducing the incidence, inhibiting, suppressing, preventing and/or treating androgen-deprivation induced conditions in men suffering from prostate cancer, such as androgen-deprivation induced osteoporosis, bone fractures, loss of bone mineral density (BMD), hot flashes and/or gynecomastia; and 8) treating polycystic ovarian syndrome and reducing the incidence, inhibiting, suppressing, preventing and/or treating diabetes, cardiovascular disease, breast cancer and endometrial cancer in women suffering from polycystic ovarian syndrome.
摘要翻译：本发明提供了5种α还原酶抑制剂和SERMs的组合。这些组合可用于：1）预防受试者的前列腺癌发生; 2）预防受试者中前列腺癌发生的复发，抑制，抑制或降低; 3）用前列腺癌治疗受试者; 4）抑制或抑制受试者前列腺癌的发生率; 5）用前列腺癌的恶性前病变治疗受试者; 6）抑制，抑制或降低患者前列腺癌恶变前病变的发生率; 7）降低患有前列腺癌的男性的雄激素剥夺诱导的骨质疏松症，骨折，骨矿物质密度（BMD），潮热的闪烁和/或损伤的发生，抑制，抑制，预防和/或治疗雄激素剥夺诱导的病症 /或男子乳房发育症和8）治疗多囊卵巢综合征，降低发生，抑制，抑制，预防和/或治疗患有多囊卵巢综合症的妇女的糖尿病，心血管疾病，乳腺癌和子宫内膜癌。

13. 发明申请

US20060258628A1 Compositions comprising 5-alpha reductase inhibitors, and SARMs and methods of use thereof 审中-公开
标题翻译：包含5-α还原酶抑制剂的组合物和SARM及其使用方法
公开(公告)号：US20060258628A1
公开(公告)日：2006-11-16
申请号：US11184037
申请日：2004-07-20
申请人： Mitchell Steiner , Karen Veverka , Duane Miller
发明人： Mitchell Steiner , Karen Veverka , Duane Miller
IPC分类号： A61K31/555 , A61K31/44 , A61K31/4172 , A61K31/506 , A61K31/415 , A61K31/32 , A61K31/277 , A61K31/165 , A61K31/66
CPC分类号： A61K31/165 , A61K31/277 , A61K31/32 , A61K31/415 , A61K31/4172 , A61K31/44 , A61K31/506 , A61K31/555 , A61K31/66
摘要： This invention provides a composition comprising a 5-alpha reductase inhibitor and a class of androgen receptor targeting agents (ARTA), which are selective androgen receptor modulators (SARM). The compositions of this invention are useful for, inter-alia, a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment of polycystic ovarian disease; e) treatment and/or prevention of acute and/or chronic muscular wasting conditions; f) preventing and/or treating dry eye conditions; g) oral androgen replacement therapy; h) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or i) inducing apoptosis in a cancer cell.
摘要翻译：本发明提供包含5-α还原酶抑制剂和作为选择性雄激素受体调节剂（SARM）的一类雄激素受体靶向剂（ARTA）的组合物。本发明的组合物尤其可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低相关的病症（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌癌症，子宫癌和卵巢癌; d）治疗多囊卵巢疾病; e）治疗和/或预防急性和/或慢性肌肉消瘦病症; f）预防和/或治疗干眼症状; g）口服雄激素替代疗法; h）降低前列腺癌的发生率，停止或导致消退; 和/或i）诱导癌细胞中的细胞凋亡。

14. 发明申请

US20050080143A1 Treatment of androgen-deprivation induced osteoporosis 审中-公开
标题翻译：雄激素剥夺诱导的骨质疏松症的治疗
公开(公告)号：US20050080143A1
公开(公告)日：2005-04-14
申请号：US10944465
申请日：2004-09-20
申请人： Mitchell Steiner , Karen Veverka , Sharan Raghow
发明人： Mitchell Steiner , Karen Veverka , Sharan Raghow
IPC分类号： A61K31/138
CPC分类号： A61K31/135 , A61K9/0014 , A61K9/0019 , A61K9/0021 , A61K9/0024 , A61K9/0053 , A61K31/138
摘要： The present invention provides methods for reducing the incidence of, inhibiting, suppressing, reducing the incidence of, and treating androgen-deprivation induced osteoporosis, bone fractures and/or loss of bone mineral density (BMD) in men having prostate cancer, comprising administering to a male human subject having prostate cancer a toremifene and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof. The present invention also provides methods of treating, preventing, suppressing, inhibiting, or reducing the incidence of hot flashes, gynecomastia, and/or hair loss in male humans having prostate cancer, comprising same.
摘要翻译：本发明提供了减少在具有前列腺癌的男性中发生，抑制，抑制，降低发生和治疗雄激素剥夺诱导的骨质疏松症，骨折和/或骨矿物质密度（BMD）丧失的方法，包括给予具有前列腺癌托泊米芬和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，药物产品，水合物，N-氧化物或其任何组合的男性受试者。本发明还提供了治疗，预防，抑制或抑制具有前列腺癌的男性人群中的潮热，男子女性发育和/或脱发的发生的方法。

15. 发明申请

US20070197664A1 Prevention and treatment of androgen-deprivation induced osteoporosis 审中-公开
标题翻译：预防和治疗雄激素剥夺诱导的骨质疏松症
公开(公告)号：US20070197664A1
公开(公告)日：2007-08-23
申请号：US11656566
申请日：2007-01-23
申请人： Mitchell Steiner , Sharan Raghow , Karen Veverka
发明人： Mitchell Steiner , Sharan Raghow , Karen Veverka
IPC分类号： A61K31/135
CPC分类号： A61K31/138 , A61K31/135
摘要： This invention provides a method of treatment, prevention, suppression, inhibition, or reduction of risk of developing androgen-deprivation induced skeletal-related events (SRE), such as pathologic fractures, surgery to bone, radiation to bone, spinal cord compression, change in antineoplastic therapy, including changes in hormonal therapy, new bone metastases, bone loss, or a combination thereof in men suffering from prostate cancer, comprising administering to a male subject suffering from prostate cancer a selective estrogen receptor modulator (SERM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof.
摘要翻译：本发明提供了治疗，预防，抑制，抑制或降低发展中的雄激素剥夺诱导的骨骼相关事件（SRE）的风险的方法，例如病理性骨折，骨骼手术，对骨骼的放射，脊髓压迫，变化包括对患有前列腺癌的男性的激素治疗，新骨转移，骨丢失或其组合的改变，包括对患有前列腺癌的男性受试者施用选择性雌激素受体调节剂（SERM）和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，药物产品，水合物，N-氧化物或其任何组合。

16. 发明申请

US20060287282A1 Compositions comprising a SARM ad GnRH agonist or a GnRH antagonist, and methods of use thereof 审中-公开
标题翻译：包含SARM-GnRH激动剂或GnRH拮抗剂的组合物及其使用方法
公开(公告)号：US20060287282A1
公开(公告)日：2006-12-21
申请号：US11003938
申请日：2004-12-06
申请人： Mitchell Steiner , Karen Veverka
发明人： Mitchell Steiner , Karen Veverka
IPC分类号： A61K31/675 , A61K31/555 , A61K31/277 , A61K31/32 , A61K31/165
CPC分类号： A61K31/165 , A61K31/277 , A61K31/32 , A61K31/555 , A61K31/675
摘要： The present invention relates to compositions comprising a selective androgen receptor modulators (SARM) and a gonadotropin releasing hormone (GnRH) agonist or a GnRH antagonist, and their use, inter-alia for treating hormone-associated conditions in males and females, which arise as a result of androgen decline, suppression or abrogation, or in treating, suppressing, inhibiting or preventing prostate cancer.
摘要翻译：本发明涉及包含选择性雄激素受体调节剂（SARM）和促性腺激素释放激素（GnRH）激动剂或GnRH拮抗剂的组合物，以及它们用于治疗男性和女性的激素相关病症，其出现为雄激素降低，抑制或消除的结果，或治疗，抑制，抑制或预防前列腺癌的结果。

17. 发明申请

US20060269611A1 Prevention and treatment of androgen-deprivation induced osteoporosis 审中-公开
标题翻译：预防和治疗雄激素剥夺诱导的骨质疏松症
公开(公告)号：US20060269611A1
公开(公告)日：2006-11-30
申请号：US11329393
申请日：2006-01-11
申请人： Mitchell Steiner , Sharan Raghow , Karen Veverka
发明人： Mitchell Steiner , Sharan Raghow , Karen Veverka
IPC分类号： A61K9/14 , A61K31/138
CPC分类号： A61K31/138
摘要： This invention provides a method of treating androgen-deprivation induced osteoporosis, bone fractures or loss of bone mineral density (BMD) in a male human subject suffering from prostate cancer by administering a pharmaceutical composition comprising Toremifene and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof, to the subject.
摘要翻译：本发明提供了一种通过给药含有托瑞米芬和/或其类似物，衍生物，异构体的药物组合物来治疗患有前列腺癌的男性人体中的雄激素剥夺诱导的骨质疏松症，骨折或骨矿物质密度（BMD）丧失的方法，代谢产物，药学上可接受的盐，药物产品，水合物，N-氧化物或其任何组合。

18. 发明申请

US20060270641A1 Method for chemoprevention of prostate cancer 审中-公开
标题翻译：化学预防前列腺癌的方法
公开(公告)号：US20060270641A1
公开(公告)日：2006-11-30
申请号：US11140255
申请日：2005-05-31
申请人： Mitchell Steiner , Sharan Raghow
发明人： Mitchell Steiner , Sharan Raghow
IPC分类号： A61K31/56 , A61K31/453 , A61K31/138
CPC分类号： A61K31/138 , A61K31/453 , A61K31/56
摘要： This invention relates to the chemoprevention of prostate cancer and, more particularly, to a method of suppressing or inhibiting latent prostate cancer comprising administering to a mammalian subject a chemopreventive agent, for example raloxifene, or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, ester, or N-oxide, or mixtures thereof. The chemopreventive agent prevents, prevents recurrence of, suppresses or inhibits prostate carcinogenesis and treats prostate cancer.
摘要翻译：本发明涉及前列腺癌的化学预防，更具体地，涉及一种抑制或抑制潜伏性前列腺癌的方法，包括向哺乳动物受试者施用化学预防药物，例如雷洛昔芬或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，酯或N-氧化物，或其混合物。化学预防剂防止，预防复发，抑制或抑制前列腺癌发生和治疗前列腺癌。

19. 发明申请

US20060287400A1 Method for treatment and chemoprevention of prostate cancer 审中-公开
标题翻译：前列腺癌的治疗和化学预防方法
公开(公告)号：US20060287400A1
公开(公告)日：2006-12-21
申请号：US11132425
申请日：2005-05-19
申请人： Mitchell Steiner , Sharan Raghow
发明人： Mitchell Steiner , Sharan Raghow
IPC分类号： A61K31/138 , A61K31/05 , A61K31/02
CPC分类号： A61K45/06 , A61K31/00 , A61K31/015 , A61K31/02 , A61K31/05 , A61K31/138 , A61K31/4535 , A61K31/565
摘要： This invention relates to the treatment and prevention of prostate cancer More particularly, the present invention provides 1) methods of preventing prostate carcinogenesis in a subject; 2) methods of preventing the recurrence of, suppressing, inhibiting or reducing the incidence of prostate carcinogenesis in a subject, 3) methods of treating a subject with prostate cancer; 4) methods of suppressing, inhibiting or reducing the incidence of prostate cancer in a subject; 5) methods of treating a subject with pre-malignant lesions of prostate cancer, and 6) methods of suppressing, inhibiting or reducing the incidence of pre-malignant lesions of prostate cancer in a subject by administering to the subject a compound of formula (I) or an analog or metabolite thereof, its N-oxide, ester, pharmaceutically acceptable salt, hydrate, or any combination thereof as described herein. The present invention provides a safe and effective method for suppressing or inhibiting prostate cancer, e.g. latent prostate cancer, and is particularly useful for treating subjects having an elevated risk of developing prostate cancer, for example, those having benign prostatic hyperplasia, prostate intraepithelial neoplasia (PIN), or an abnormally high level of circulating prostate specific antibody (PSA), or having a family history of prostate cancer.
摘要翻译：本发明涉及治疗和预防前列腺癌。更具体地，本发明提供1）预防受试者中前列腺癌发生的方法; 2）预防受试者的前列腺癌发生发生的复发，抑制，抑制或降低的方法，3）用前列腺癌治疗受试者的方法; 4）抑制或抑制受试者前列腺癌发病率的方法; 5）治疗患有前列腺癌的恶性前病变的受试者的方法，以及6）通过向受试者施用式（I）的化合物来抑制，抑制或降低患者前列腺癌的恶性前病变发病率的方法）或其类似物或代谢物，其N-氧化物，酯，药学上可接受的盐，水合物或其任何组合。本发明提供了一种安全有效的抑制或抑制前列腺癌的方法，例如，潜伏性前列腺癌，并且特别可用于治疗具有升高的前列腺癌风险的受试者，例如具有良性前列腺增生，前列腺上皮内瘤变（PIN）或异常高水平的循环前列腺特异性抗体（PSA）的受试者，或具有前列腺癌的家族史。

20. 发明申请

US20050171073A1 Composition and method for treatment and chemoprevention of prostate cancer 审中-公开
标题翻译：前列腺癌的治疗和化学预防的组合物和方法
公开(公告)号：US20050171073A1
公开(公告)日：2005-08-04
申请号：US11038468
申请日：2005-01-21
申请人： Mitchell Steiner , Sharan Raghow
发明人： Mitchell Steiner , Sharan Raghow
IPC分类号： A61K31/00 , A61K31/015 , A61K31/138 , A61K31/4535 , A61K31/565 , A61K45/06 , A61K31/58 , A61K31/57
CPC分类号： A61K45/06 , A61K31/00 , A61K31/015 , A61K31/02 , A61K31/05 , A61K31/138 , A61K31/4535 , A61K31/565
摘要： This invention relates to compositions and methods of use thereof in the prevention of prostate carcinogenesis in a subject; prevention of the recurrence of, suppression, inhibition or reduction of the incidence of prostate carcinogenesis in a subject; treatment of a subject with prostate cancer; suppression, inhibition or reduction of the incidence of prostate cancer in a subject; treatment of a subject with pre-malignant lesions of prostate cancer; and/or suppression, inhibition or reduction of the incidence of pre-malignant lesions of prostate cancer in a subject.
摘要翻译：本发明涉及其用于预防受试者中前列腺癌发生的组合物及其方法; 预防受试者中前列腺癌发生发生的复发，抑制，抑制或减少; 治疗患有前列腺癌的受试者; 抑制，抑制或减少受试者中前列腺癌的发生率; 治疗患有前列腺癌恶变前病变的受试者; 和/或抑制，抑制或降低受试者中前列腺癌的恶性前病变的发生率。

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