专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20060035966A1 Irreversible selective androgen receptor modulators and methods of use thereof 审中-公开
标题翻译：不可逆选择性雄激素受体调节剂及其使用方法
公开(公告)号：US20060035966A1
公开(公告)日：2006-02-16
申请号：US10995567
申请日：2004-11-24
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka , Leonid Kirkovsky , Dong Hwang , Arnab Mukherjee
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka , Leonid Kirkovsky , Dong Hwang , Arnab Mukherjee
IPC分类号： C07C331/28
CPC分类号： C07C323/60 , A61K31/16 , A61K31/26 , A61K31/275 , C07C261/02 , C07C265/12 , C07C331/10 , C07C331/28
摘要： In one embodiment, this invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). The SARM compounds have unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. In one embodiment, the SARM compounds bind irreversibly to the androgen receptor In another embodiment, the SARM compounds are androgen receptor antagonists, which bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds are alkylating agents. The SARM compounds, either alone or as a composition, are useful for 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 and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.
摘要翻译：在一个实施方案中，本发明提供了一类雄激素受体靶向剂（ARTA）。这些药剂定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。 SARM化合物对雄激素受体的非甾体配体具有意想不到的抗雄激素活性。在一个实施方案中，SARM化合物不可逆地与雄激素受体结合。在另一个实施方案中，SARM化合物是雄激素受体拮抗剂，其不可逆地结合雄激素受体。在另一个实施方案中，SARM化合物是烷化剂。 SARM化合物，单独或作为组合物，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）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; g）降低前列腺癌的发生率，停止或导致消退; 和/或h）诱导癌细胞中的细胞凋亡。

2. 发明申请

US20050033074A1 Multi-substitued selective androgen receptor modulators and methods of use thereof 失效
标题翻译：多取代的选择性雄激素受体调节剂及其使用方法
公开(公告)号：US20050033074A1
公开(公告)日：2005-02-10
申请号：US10861905
申请日：2004-06-07
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka , Dong Hwang , Jiyun Chen
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka , Dong Hwang , Jiyun Chen
IPC分类号： C07C235/24 , C07F7/24 , C07C275/40 , C07C391/00
CPC分类号： C07C235/24
摘要： This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are usefull for 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 and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.
摘要翻译：本发明提供一类雄激素受体靶向剂（ARTA）。这些药剂定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。已经发现几种SARM化合物对雄激素受体具有非甾类化合物的意想不到的雄激素和合成代谢活性。已经发现其他SARM化合物对雄激素受体具有非甾类配体的意想不到的抗雄激素活性。 SARM化合物，单独或作为组合物，对于a）男性避孕是有用的; 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）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; 和/或g）降低前列腺癌的发生率，停止或导致消退。

3. 发明申请

US20060183931A1 Multi-substituted selective androgen receptor modulators and methods of use thereof 有权
标题翻译：多取代的选择性雄激素受体调节剂及其使用方法
公开(公告)号：US20060183931A1
公开(公告)日：2006-08-17
申请号：US10371155
申请日：2003-02-24
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka , Dong Hwang , Jiyun Chen
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka , Dong Hwang , Jiyun Chen
IPC分类号： C07F9/02 , C07F7/22 , C07C395/00 , C07C255/60 , C07C237/10
CPC分类号： C07C235/24
摘要： This invention provides androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for 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 and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer
摘要翻译：本发明提供雄激素受体靶向剂（ARTA）。这些药剂定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。已经发现几种SARM化合物对雄激素受体具有非甾类化合物的意想不到的雄激素和合成代谢活性。已经发现其他SARM化合物对雄激素受体具有非甾类配体的意想不到的抗雄激素活性。 SARM化合物，单独或作为组合物，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）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; 和/或g）降低前列腺癌的发生率，停止或导致消退

4. 发明申请

US20050032750A1 Treating androgen deficiency in female (ADIF)-associated conditions with SARMS 审中-公开
标题翻译：女性（ADIF）相关SARS治疗雄激素缺乏症
公开(公告)号：US20050032750A1
公开(公告)日：2005-02-10
申请号：US10759538
申请日：2004-01-20
申请人： Mitchell Steiner , Karen Veverka , James Dalton , Duane Miller
发明人： Mitchell Steiner , Karen Veverka , James Dalton , Duane Miller
IPC分类号： A61K20060101 , A61K31/165 , A61K31/166 , A61K31/195 , A61K31/22 , A61K31/277 , A61K31/66
CPC分类号： A61K31/22 , A61K31/166
摘要： The present invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of an Androgen Deficiency in Female (ADIF)-associated condition in a female subject, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, crystal, polymorph, prodrug, or any combination thereof. The present invention further provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, fatigue, depression, anemia, muscle weakness, hair loss, obesity, polycystic ovarian disease, endometriosis, breast cancer, uterine cancer and ovarian cancer due to ADIF in a female subject, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, crystal, polymorph, prodrug, or any combination thereof.
摘要翻译：本发明提供了通过向受试者施用选择性雄激素受体调节剂（SARM）化合物和治疗雌激素受体调节剂（SARM）化合物的方法来治疗，预防，抑制，抑制或降低女性受试者中雄激素缺乏症（ADIF）相关病症的发生率或其类似物，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，晶体，多晶型物，前药或其任何组合。本发明还提供一种治疗，预防，抑制或降低性功能障碍，性欲降低，性腺机能减退，肌肉减少症，骨质减少症，骨质疏松症，认知和情绪改变，疲劳，抑郁，贫血，肌肉无力等的发生的方法，通过向受试者施用选择性雄激素受体调节剂（SARM）化合物和/或其类似物，衍生物异构体，通过对雌性受试者的ADIF引起的脱发，肥胖，多囊卵巢疾病，子宫内膜异位症，乳腺癌，子宫癌和卵巢癌，代谢物，药学上可接受的盐，药物产品，水合物，N-氧化物，晶体，多晶型物，前药或其任何组合。

5. 发明申请

US20060276539A1 Treating Androgen Decline in Aging Male (ADAM)- associated conditions with SARMS 审中-公开
标题翻译：老年男性（ADAM）治疗雄激素下降 - 与SARMS相关的病症
公开(公告)号：US20060276539A1
公开(公告)日：2006-12-07
申请号：US11324753
申请日：2006-01-04
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
IPC分类号： A61K31/277
CPC分类号： A61K31/277 , C07K14/721
摘要： This invention provides methods for treatment and inhibition of a male subject having an Androgen Decline in Aging Male (ADAM)-associated condition, for example sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, an alteration in cognition and mood, depression, anemia, hair loss, obesity, muscle loss, dry eye, memory loss, benign prostate hyperplasia and/or prostate cancer, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, pro-drug, polymorph, crystal, or any combination thereof.
摘要翻译：本发明提供了用于治疗和抑制雄性雄性雄激素降低（ADAM）相关病症的男性受试者的方法，例如性功能障碍，性欲性降低，勃起功能障碍，性腺机能减退，肌肉减少症，骨质减少症，骨质疏松症，认知改变通过向受试者施用选择性雄激素受体调节剂（SARM）化合物和/或其类似物，通过向受试者施用选择性雄激素受体调节剂（SARM）化合物和/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，前药，多晶型物，晶体或其任何组合。

6. 发明申请

US20050080054A1 Treating androgen decline in aging male (ADAM)-associated conditions with SARMS 审中-公开
标题翻译：老年男性（ADAM）治疗雄激素相关性SARS的病情下降
公开(公告)号：US20050080054A1
公开(公告)日：2005-04-14
申请号：US10683161
申请日：2003-10-14
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
IPC分类号： C07K14/72 , A61K31/66 , A61K31/165 , A61K31/195 , A61K31/21 , A61K31/277 , A61K31/32
CPC分类号： C07K14/721
摘要： The present invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of an Androgen Decline in Aging Male (ADAM)-associated condition in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, crystal, or any combination thereof. The present invention further provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, benign prostate hyperplasia or prostate cancer due to ADAM in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, crystal, or any combination thereof.
摘要翻译：本发明提供了通过向受试者施用选择性雄激素受体调节剂（SARM）化合物，治疗，预防，抑制，抑制或降低男性受试者的老年男性（ADAM）相关状态的雄激素下降的发生率的方法和/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，前药，多晶型物，晶体或其任何组合。本发明还提供了治疗，预防，抑制或降低性功能障碍，性欲降低，勃起功能障碍，性腺机能减退，肌肉减少症，骨质减少症，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发通过向受试者施用选择性雄激素受体调节剂（SARM）化合物和/或其类似物，衍生物，异构体，代谢产物，药学上可接受的盐，药物产品，由此引起的ADAM在男性受试者中的肥胖，良性前列腺增生或前列腺癌。水合物，N-氧化物，前药，多晶型物，晶体或其任何组合。

7. 发明申请

US20060111441A1 Treating wasting disorders with selective androgen receptor modulators 有权
标题翻译：用选择性雄激素受体调节剂治疗浪费障碍
公开(公告)号：US20060111441A1
公开(公告)日：2006-05-25
申请号：US11220414
申请日：2005-09-07
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
IPC分类号： A61K31/277
CPC分类号： A61K31/277
摘要： This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.
摘要翻译：本发明提供：1）治疗患有肌肉消瘦障碍的受试者的方法; 2）预防受试者的肌肉消瘦障碍的方法; 3）治疗，预防，抑制，抑制或减轻患有肌肉消瘦障碍的受试者的肌肉损失的方法; 4）一种治疗，预防，抑制，减少或抑制患有肌肉消瘦障碍的受试者的肌肉消瘦的方法; 和/或5）通过向受试者施用选择性雄激素受体调节剂（SARM）和/或类似物衍生物，治疗，预防，抑制，减少或抑制患有肌肉消瘦疾病的受试者的肌肉蛋白分解代谢的方法，所述SARM化合物的异构体，代谢物，药学上可接受的盐，药物产品，水合物，N-氧化物，前药，多晶型物，杂质或晶体，或其任何组合。

8. 发明申请

US20050080055A1 Method of treating breast cancer with androgen receptor antagonists 审中-公开
标题翻译：用雄激素受体拮抗剂治疗乳腺癌的方法
公开(公告)号：US20050080055A1
公开(公告)日：2005-04-14
申请号：US10760152
申请日：2004-01-20
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
IPC分类号： A61K20060101 , A61K31/165 , A61K31/21 , A61K31/26 , A61K31/277 , A61K31/32 , A61K31/66 , A61P35/00
CPC分类号： A61K31/66 , A61K31/21 , A61K31/26
摘要： This invention relates to the prevention and treatment of breast cancer in a subject, for example a female subject. Accordingly, this invention provides methods of a) treating a subject suffering from breast cancer; b) preventing, suppressing, inhibiting or reducing the incidence of breast cancer in a subject; c) delaying the progression of breast cancer in a subject suffering from breast cancer; d) preventing the recurrence of breast cancer in a subject; e) treating the recurrence of breast cancer in a subject suffering from breast cancer; and/or f) treating, preventing, suppressing or inhibiting metastasis in a subject suffering from breast cancer, by administering to the subject a therapeutically effective amount of an Androgen Receptor Antagonist and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, crystal, polymorph, prodrug or any combination thereof, as described herein.
摘要翻译：本发明涉及预防和治疗受试者，例如女性受试者的乳腺癌。因此，本发明提供了a）治疗患有乳腺癌的受试者的方法; b）预防，抑制，抑制或降低患者乳腺癌的发生率; c）延缓乳腺癌患者乳腺癌的进展; d）预防受试者乳腺癌的复发; e）治疗乳腺癌患者乳腺癌的复发; 和/或f）通过向受试者施用治疗有效量的雄激素受体拮抗剂和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，治疗，预防，抑制或抑制患有乳腺癌的受试者的转移，药物产品，水合物，N-氧化物，晶体，多晶型物，前药或其任何组合。

9. 发明申请

US20050038110A1 Selective androgen receptor modulators and methods of use thereof 审中-公开
标题翻译：选择性雄激素受体调节剂及其使用方法
公开(公告)号：US20050038110A1
公开(公告)日：2005-02-17
申请号：US10863524
申请日：2004-06-09
申请人： Mitchell Steiner , James Dalton , Duane Miller , Karen Veverka
发明人： Mitchell Steiner , James Dalton , Duane Miller , Karen Veverka
IPC分类号： A61K31/277 , A61K31/32 , C07F7/24
CPC分类号： C07C255/60 , C07C235/24 , C07C255/54
摘要： This invention provides a class of androgen receptor targeting agents. The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM).
摘要翻译：本发明提供一类雄激素受体靶向剂。这些药剂定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。

10. 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.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式