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1. 发明申请

WO2004035739A3 TREATING ANDROGEN DECLINE IN AGING MALE (ADAM)-ASSOCIATED CONDITIONS WITH SARMS 审中-公开
标题翻译：用SARMS治疗老年男性（ADAM）相关病症的雄激素降低
公开(公告)号：WO2004035739A3
公开(公告)日：2004-09-30
申请号：PCT/US0332513
申请日：2003-10-14
申请人： GTX INC , DALTON JAMES T , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A
发明人： DALTON JAMES T , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A
IPC分类号： C07K14/72 , A61K31/165 , A61K31/40 , A61K31/41 , A61K31/435 , A61K31/44
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）化合物来治疗，预防，抑制，抑制或减少男性受试者中老化雄性（ADAM）相关病症中雄激素降低的发生的方法和/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。本发明进一步提供治疗，预防，抑制，抑制或减少性功能障碍，性欲减退，勃起功能障碍，性腺机能减退症，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，贫血症，脱发（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，药物产品或药物产品给予受试者，所述受试者是男性受试者中由于ADAM引起的肥胖，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。

2. 发明申请

WO03065992A2 TREATING BENIGN PROSTATE HYPERPLASIA WITH SARMS 审中-公开
标题翻译：用SARMS处理BENIGN PROSTATE HYPERPLASIA
公开(公告)号：WO03065992A2
公开(公告)日：2003-08-14
申请号：PCT/US0303447
申请日：2003-02-06
申请人： GTX INC , STEINER MITCHELL S , VEVERKA KAREN A , MILLER DUANE D , DALTON JAMES T , CHUNG KIWON , GAO WENQING
发明人： STEINER MITCHELL S , VEVERKA KAREN A , MILLER DUANE D , DALTON JAMES T , CHUNG KIWON , GAO WENQING
IPC分类号： A61K45/00 , A61K31/00 , A61K31/167 , A61K31/277 , A61K31/56 , A61P13/08 , A61P43/00 , A61K
CPC分类号： A61K31/277 , A61K31/00 , A61K31/167 , A61K31/56
摘要： This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, by administering to the subject a selective androgen receptor modulator(SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-a reductase enzyme type 1 and /or type 2 inhibitor, wherein said inhibitor is a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite,pharmaceutically acceptable salt, pharmaceutical product, hydrate, Woxide, or any combination thereof as described herein. This invention also provides a method of inhibiting a 5-a reductase type 1 and/or type 2 enzyme, comprising contacting the enzyme with an effective 5-a reductase inhibitory amount of a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof, as described herein.
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）和/或其类似物，衍生物，异构体，代谢物来治疗，预防，抑制或降低男性患者良性前列腺增生的发生率的方法，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。本发明还提供了一种治疗脱发患者的方法，包括向受试者施用治疗有效量的1型和/或2型抑制剂的5-a还原酶的步骤，其中所述抑制剂是选择性雄激素受体调节剂（SARM）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，氧化物或其任何组合。本发明还提供抑制1型和/或2型5α还原酶的方法，包括使酶与有效的5-a还原酶抑制量的选择性雄激素受体调节剂（SARM）和/或其类似物接触，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。

3. 发明申请

WO2004034978A3 TREATING OBESITY WITH SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：选择性雄激素受体调节剂治疗肥胖
公开(公告)号：WO2004034978A3
公开(公告)日：2004-07-15
申请号：PCT/US0332509
申请日：2003-10-14
申请人： GTX INC , DALTON JAMES T , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A
发明人： DALTON JAMES T , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A
IPC分类号： A61K31/165 , A61K31/405 , A61K31/4706 , A61K31/675
CPC分类号： A61K31/165
摘要： This invention relates to the prevention and treatment of obesity. More particularly, this invention relates to a method of: a) treating, preventing, suppressing, inhibiting, or reducing obesity; b) promoting, increasing or facilitating weight loss; c) decreasing, suppressing, inhibiting or reducing appetite; d) altering the body composition, e) altering lean body mass or fat free body mass, f) converting fat to lean muscle; g) treating, preventing, suppressing, inhibiting, or reducing an obesity-associated metabolic disorder, for example hypertension, osteoarthritis, Type II diabetes mellitus, increased blood pressure, stroke, or heart disease; h) decreasing, suppressing, inhibiting or reducing adipogenesis; i) altering stem cell differentiation; and/or j) altering the level of leptin; comprising administering a therapeutically effective amount of a selective androgen receptor modulator and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, crystal, or any combination thereof, as described herein.
摘要翻译：本发明涉及肥胖症的预防和治疗。更具体地说，本发明涉及一种方法：a）治疗，预防，抑制，抑制或减少肥胖; b）促进，增加或促进体重减轻; c）减少，抑制，抑制或减少食欲; d）改变身体组成，e）改变瘦体重或无脂肪体重，f）将脂肪转化为瘦肌肉; g）治疗，预防，抑制，抑制或减轻与肥胖相关的代谢病症，例如高血压，骨关节炎，II型糖尿病，血压升高，中风或心脏病; h）减少，抑制，抑制或减少脂肪形成; i）改变干细胞分化; 和/或j）改变瘦素水平; 包括给予治疗有效量的选择性雄激素受体调节剂和/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，晶体或其任何组合于此。

4. 发明申请

WO2007081696A2 TREATING ANDROGEN DECLINE IN AGING MALE (ADAM)-ASSOCIATED CONDITIONS WITH SARMS 审中-公开
标题翻译：治疗老年男性（ADAM）的SARS治疗条件恶化
公开(公告)号：WO2007081696A2
公开(公告)日：2007-07-19
申请号：PCT/US2007000052
申请日：2007-01-04
申请人： GTX INC , DALTON JAMES T , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A
发明人： DALTON JAMES T , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A
IPC分类号： A61K31/277 , C07K14/72
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。

5. 发明申请

WO2004066922A3 A METHOD OF TREATING BREAST CANCER WITH ANDROGEN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：一种用雄激素受体拮抗剂治疗乳腺癌的方法
公开(公告)号：WO2004066922A3
公开(公告)日：2005-09-15
申请号：PCT/US2004001313
申请日：2004-01-20
申请人： GTX INC , STEINER MITCHELL S , DALTON JAMES T , MILLER DUANE D , VEVERKA KAREN A
发明人： STEINER MITCHELL S , DALTON JAMES T , MILLER DUANE D , VEVERKA KAREN A
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, phatmaceutical 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。

6. 发明申请

WO2004064747A2 TREATING ANDROGEN DEFICIENCY IN FEMALE (ADIF)-ASSOCIATED CONDITIONS WITH SARMS 审中-公开
标题翻译：女性（ADIF）治疗SARS治疗条件缺陷
公开(公告)号：WO2004064747A2
公开(公告)日：2004-08-05
申请号：PCT/US2004001359
申请日：2004-01-20
申请人： GTX INC , STEINER MITCHELL S , VEVERKA KAREN A , DALTON JAMES T , MILLER DUANE D
发明人： STEINER MITCHELL S , VEVERKA KAREN A , MILLER DUANE D
IPC分类号： A61K20060101 , A61K31/165 , A61K31/166 , A61K31/195 , A61K31/22 , A61K31/277 , A61K31/66 , A61K
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。

7. 发明申请

WO2004035736A3 HALOGENATED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：选择性受体选择性受体调节剂及其使用方法
公开(公告)号：WO2004035736A3
公开(公告)日：2004-07-15
申请号：PCT/US0332507
申请日：2003-10-14
申请人： UNIV TENNESSEE RES FOUNDATION , DALTON JAMES T , MILLER DUANE D , YIN DONGHUA , HE YALI , STEINER MITCHELL S , VEVERKA KAREN A
发明人： DALTON JAMES T , MILLER DUANE D , YIN DONGHUA , HE YALI , STEINER MITCHELL S , VEVERKA KAREN A
IPC分类号： A61K31/165 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/16 , C07C235/24 , C07C255/60 , C07C335/18 , C07D209/08 , C07D215/22 , C07D215/227 , C07D271/12 , C07C233/05 , A61K31/275 , C07C255/50
CPC分类号： C07D215/227 , A61K31/165 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/16 , C07C235/24 , C07C255/60 , C07C335/18 , C07D209/08 , C07D271/12
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化合物对于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化合物对于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）治疗多种激素相关病症，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有关的疾病（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）诱导癌细胞凋亡。

8. 发明申请

WO2006010162A2 COMPOSITIONS COMPRISING 5-ALPHA REDUCTASE INHIBITORS, AND SERMs AND METHODS OF USE THEREOF 审中-公开
标题翻译：包含5-ALPHA还原酶抑制剂的组合物及其使用方法
公开(公告)号：WO2006010162A2
公开(公告)日：2006-01-26
申请号：PCT/US2005025840
申请日：2005-07-21
申请人： GTX INC , STEINER MITCHELL S , VEVERKA KAREN A , MILLER DUANE D
发明人： STEINER MITCHELL S , VEVERKA KAREN A , MILLER DUANE D
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发生的复发，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 /或男子母乳喂养和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。

9. 发明申请

WO2004062612A3 LARGE-SCALE SYNTHESIS OF SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：选择性雄激素受体调节剂的大规模合成
公开(公告)号：WO2004062612A3
公开(公告)日：2004-11-04
申请号：PCT/US2004000618
申请日：2004-01-12
申请人： GTX INC , STEINER MITCHELL S , CHUNG KIWON , DALTON JAMES , MILLER DUANE D , VEVERKA KAREN A
发明人： STEINER MITCHELL S , CHUNG KIWON , DALTON JAMES , MILLER DUANE D , VEVERKA KAREN A
IPC分类号： C07C231/12 , C07C235/24 , C07C231/00
CPC分类号： C07C231/12 , C07C235/24
摘要： The present invention relates to a synthetic process for the preparation of 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, and alterations in mood and cognition; 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 and endometriosis, d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen replacement; g) preventing and/or treating dry eye conditions; h) treatment and/or prevention of begnin prostate hyperplasia (BPH); I) inducing apoptosis in a cancer cell; j) treatment and/or prevention of cancers of female sexual organs such as breast cancer, uterine cancer and ovarian cancer; and/or other clinical therapeutic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.
摘要翻译：本发明涉及一种制备新型雄激素受体靶向剂（ARTA）的合成方法，其显示了雄激素受体的非甾体配体的雄激素和合成代谢活性。这些药物定义了一种新的亚类化合物，它们是选择性雄激素受体调节剂（SARM），其可用于a）男性避孕; b）治疗多种激素相关病症，例如与衰老男性（ADAM）中的雄激素降低相关的病症，例如疲劳，抑郁症，性欲减退，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，肥胖症，肌肉减少症，骨质减少症，骨质疏松症以及情绪和认知改变; c）治疗与女性雄激素降低（ADIF）有关的病症，例如性功能障碍，性欲减退，性腺机能减退，肌肉减少症，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖症和子宫内膜异位症，d ）治疗和/或预防慢性肌肉消瘦; e）降低前列腺癌的发病率，停止或导致其消退; f）口服雄激素替代物; g）预防和/或治疗干眼症; h）治疗和/或预防begnin前列腺增生（BPH）; I）诱导癌细胞凋亡; j）治疗和/或预防女性性器官的癌症，如乳腺癌，子宫癌和卵巢癌; 和/或其他临床治疗和/或诊断领域。本发明的方法适用于大规模制备，因为所有步骤产生高纯度化合物，因此避免了复杂的纯化程序，最终降低了收率。因此，本发明提供了用于合成非甾体激动剂化合物的方法，其可以用于工业大规模合成，并且以高收率提供高纯度产物。

10. 发明申请

WO2005037201A3 TREATING BONE-RELATED DISORDERS WITH SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：用选择性的雄激素受体调节剂治疗骨骼相关疾病
公开(公告)号：WO2005037201A3
公开(公告)日：2005-10-06
申请号：PCT/US2004033395
申请日：2004-10-12
申请人： GTX INC , DALTON JAMES , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A , KEARBY JEFFREY
发明人： DALTON JAMES , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A , KEARBY JEFFREY
IPC分类号： A61K20060101 , C07F7/22
CPC分类号： A61K31/167 , A61K31/00 , A61K31/165 , A61K31/21 , A61K31/32 , A61K31/405 , A61K31/4704 , A61K31/66
摘要： This invention provides method of treating, preventing, suppressing, inhibiting, or reducing the risk of developing a bone-related disorder, for example osteoporosis, osteopenia, increased bone resorption, bone fracture, bone frailty and/or loss of bone mineral density (BMD), by administrating a therapeutically effective amount of a selective androgen receptor modulator (SARM) and/or its analogue, derivative, isomer, metabolite pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof. The invention also provides methods of decreasing fat mass (FM) and increasing lean mass, comprising administering same.
摘要翻译：本发明提供了治疗，预防，抑制，抑制或降低骨相关病症发生风险的方法，例如骨质疏松症，骨质减少，增加的骨吸收，骨折，骨质脆弱和/或骨矿物质密度的丧失（BMD ），通过施用治疗有效量的选择性雄激素受体调节剂（SARM）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。本发明还提供降低脂肪量（FM）和增加瘦肉质量的方法，包括施用它们。

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