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11. 发明申请

US20060009488A1 Prodrugs of selective androgen receptor modulators and methods of use thereof 有权
公开(公告)号：US20060009488A1
公开(公告)日：2006-01-12
申请号：US11013214
申请日：2004-12-16
申请人： Duane Miller , Mitchell Steiner , Karen Veverka
发明人： Duane Miller , Mitchell Steiner , Karen Veverka
IPC分类号： A61K31/4704 , C07D215/36
CPC分类号： C07F9/091 , A61K31/4704 , A61K47/548 , C07C235/24
摘要： The present invention provides prodrugs of selective androgen receptor modulators (SARMs), and their use in treating or reducing the incidence of osteoporosis, a variety of hormone-related conditions, conditions associated with Androgen Decline in Aging Male (ADAM); conditions associated with Androgen Decline in Female (ADIF), and muscular wasting conditions, obesity, dry eye conditions, and prostate cancer. The prodrugs are also useful in oral androgen replacement therapy and male contraception.

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

US20060035965A1 Selective androgen receptor modulators and methods of use thereof 有权
公开(公告)号：US20060035965A1
公开(公告)日：2006-02-16
申请号：US11146427
申请日：2005-06-07
申请人： James Dalton , Duane Miller , Karen Veverka
发明人： James Dalton , Duane Miller , Karen Veverka
IPC分类号： A01N37/34 , A61K31/277
CPC分类号： A61K31/277
摘要： This invention provides SARM compounds and their use in treating a variety of diseases or conditions in a subject, including, inter-alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.

15. 发明申请

US20060004042A1 Formulations comprising selective androgen receptor modulators 审中-公开
标题翻译：包含选择性雄激素受体调节剂的制剂
公开(公告)号：US20060004042A1
公开(公告)日：2006-01-05
申请号：US11029022
申请日：2005-01-05
申请人： James Dalton , Duane Miller , Karen Veverka
发明人： James Dalton , Duane Miller , Karen Veverka
IPC分类号： A61K31/4706 , A61K31/405 , A61K31/165
CPC分类号： A61K31/165 , A61K31/4706
摘要： The present invention relates to pharmaceutical compositions and formulations comprising a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which 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 chronic muscular wasting; and/or e) decreasing the incidence of, halting or causing a regression of prostate cancer. The present invention provides pharmaceutical compositions comprising the selective androgen receptor modulator compounds, together with pharmaceutically acceptable excipients.
摘要翻译：本发明涉及包含新型雄激素受体靶向剂（ARTA）的药物组合物和制剂，其表现出雄激素受体的非甾体配体的雄激素和合成代谢活性。这些药剂定义了一种新的选择性雄激素受体调节剂（SARM）的化合物亚类，它们可用于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/或预防慢性肌肉消瘦; 和/或e）降低前列腺癌的发生率，停止或导致消退。本发明提供了包含选择性雄激素受体调节剂化合物以及药学上可接受的赋形剂的药物组合物。

16. 发明申请

US20070265290A1 Heterocyclic selective androgen receptor modulators and methods of use thereof 审中-公开
标题翻译：杂环选择性雄激素受体调节剂及其使用方法
公开(公告)号：US20070265290A1
公开(公告)日：2007-11-15
申请号：US11723957
申请日：2007-03-22
申请人： James Dalton , Duane Miller
发明人： James Dalton , Duane Miller
IPC分类号： A61K31/505 , A61K31/16 , A61K31/40 , A61K31/41 , C07D221/22 , C07D239/00 , C07D277/00 , C07D401/00 , C07D263/02 , C07D233/00 , A61K31/506 , A61K31/4164 , A61K31/44
CPC分类号： C07D213/75 , C07D213/84 , C07K14/721
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 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：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，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。

17. 发明申请

US20060040998A1 Thiazolidinone amides, thiazolidine carboxylic acid amides, methods of making, and uses thereof 有权
标题翻译：噻唑烷酮酰胺，噻唑烷羧酸酰胺，其制备方法和用途
公开(公告)号：US20060040998A1
公开(公告)日：2006-02-23
申请号：US10992175
申请日：2004-11-18
申请人： Duane Miller , Veeresa Gududuru , James Dalton , Eunju Hurh
发明人： Duane Miller , Veeresa Gududuru , James Dalton , Eunju Hurh
IPC分类号： A61K31/427 , C07D417/02
CPC分类号： C07D277/06 , C07D277/14 , C07D277/20 , C07D277/34 , C07D277/56 , C07D417/04
摘要： Substituted thiazolidinone carboxylic acid amides and substituted thiazolidine carboxylic acid amides according to formulae (I) and (II) are disclosed where the various substituent groups are as defined in the specification. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.
摘要翻译：公开了根据式（I）和（II）的取代的噻唑烷酮羧酸酰胺和取代的噻唑烷羧酸酰胺，其中各种取代基如说明书中所定义。还公开了制备这些化合物的方法，含有这些化合物的药物组合物及其用途，特别是用于治疗或预防癌症的方法。

18. 发明申请

US20080076829A1 Substituted acylanilides and methods of use thereof 有权
标题翻译：取代的酰基酰苯胺及其使用方法
公开(公告)号：US20080076829A1
公开(公告)日：2008-03-27
申请号：US11892595
申请日：2007-08-24
申请人： James Dalton , Duane Miller
发明人： James Dalton , Duane Miller
IPC分类号： C07C255/51 , A61K31/167 , A61P15/16
CPC分类号： C07C255/60 , C07B2200/07
摘要： This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.
摘要翻译：本发明提供了SARM化合物及其用于治疗受试者中的多种疾病或病症的用途，所述疾病或病症尤其包括肌肉消瘦疾病和/或病症或骨相关疾病和/或病症。

19. 发明申请

US20080057068A1 SARMS and method of use thereof 有权
标题翻译： SARMS及其使用方法
公开(公告)号：US20080057068A1
公开(公告)日：2008-03-06
申请号：US11785250
申请日：2007-04-16
申请人： James Dalton , Duane Miller
发明人： James Dalton , Duane Miller
IPC分类号： A61K31/167 , A61K31/17 , A61K31/4985 , A61K31/56 , A61K38/16 , A61K38/28 , A61K38/47 , A61K39/395 , A61P15/16 , A61P35/00 , C07C233/04
CPC分类号： C07C255/60 , A61K38/09 , A61K38/24 , A61K38/35 , A61K2300/00
摘要： This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, muscle wasting diseases and/or disorders, bone-related diseases and/or disorders, diabetes, cardiovascular disease, renal disease and others.
摘要翻译：本发明提供了SARM化合物及其用于治疗受试者中各种疾病或病症的用途，包括肌肉消耗疾病和/或病症，骨相关疾病和/或病症，糖尿病，心血管疾病，肾脏疾病和别的。

20. 发明申请

US20060241180A1 Selective androgen receptor modulators and methods of use thereof 有权
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：US20060241180A1
公开(公告)日：2006-10-26
申请号：US11394181
申请日：2006-03-31
申请人： James Dalton , Duane Miller , Craig Marhefka , Wenqing Gao
发明人： James Dalton , Duane Miller , Craig Marhefka , Wenqing Gao
IPC分类号： A61K31/66 , A61K31/277 , A61K31/165 , A61K31/32 , C07F9/28 , C07C255/20 , C07C235/24
CPC分类号： A61K31/275 , A61K31/277 , A61K31/415 , A61K31/421 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/505 , A61K31/557 , A61K31/65 , A61K31/66 , C07C255/60 , C07D211/72 , C07D233/44 , C07D239/02
摘要： This invention provides a class of androgen receptor targeting agents (ARTA). The compounds are selective androgen receptor modulators (SARM) useful for, inter-alia, suppressing spermatogenesis, treating a subject having a hormone related condition, treating a subject suffering from prostate cancer, delaying the progression of prostate cancer, preventing the recurrence of prostate cancer, and treating the recurrence of prostate cancer.
摘要翻译：本发明提供一类雄激素受体靶向剂（ARTA）。这些化合物是选择性雄激素受体调节剂（SARM），其用于除其他外抑制精子发生，治疗具有激素相关病症的受试者，治疗患有前列腺癌的受试者，延缓前列腺癌的进展，预防前列腺癌的复发，并治疗前列腺癌的复发。

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