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    Prodrugs of selective androgen receptor modulators and methods of use thereof
    61.
    发明授权
    Prodrugs of selective androgen receptor modulators and methods of use thereof 有权
    选择性雄激素受体调节剂的前药及其使用方法

    公开(公告)号：US07595402B2

    公开(公告)日：2009-09-29

    申请号：US11013214

    申请日：2004-12-16

    申请人： Duane D. Miller ,  Mitchell S. Steiner ,  Karen A. Veverka ,  James T. Dalton

    发明人： Duane D. Miller ,  Mitchell S. Steiner ,  Karen A. Veverka ,  James T. Dalton

    IPC分类号： C07D215/38

    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.

    摘要翻译： 本发明提供选择性雄激素受体调节剂（SARM）的前药，以及它们在治疗或降低骨质疏松症发生率，多种激素相关病症，与老年男性（ADAM）雄激素衰退相关的病症中的用途。 与雄激素降低（ADIF）相关的病症，肌肉消瘦症，肥胖症，干眼症和前列腺癌。 前药还可用于口服雄激素替代疗法和男性避孕。

    Selective androgen receptor modulators
    63.
    发明授权
    Selective androgen receptor modulators 失效
    选择性雄激素受体调节剂

    公开(公告)号：US07518013B2

    公开(公告)日：2009-04-14

    申请号：US11353225

    申请日：2006-02-14

    申请人： James T. Dalton ,  Duane D. Miller ,  Yali He ,  Donghua Yin

    发明人： James T. Dalton ,  Duane D. Miller ,  Yali He ,  Donghua Yin

    IPC分类号： C07C255/49 ,  A61K31/275

    CPC分类号： C07C255/60

    摘要： The present invention relates to androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity, which are nonsteroidal ligands for the androgen receptor. The selective androgen receptor modulators (SARM) 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; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas.

    摘要翻译： 本发明涉及雄激素和合成代谢活性的雄激素受体靶向剂（ARTA），其是雄激素受体的非甾体配体。 选择性雄激素受体调节剂（SARM）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; e）降低前列腺癌的发生率，停止或导致消退; f）口服雄激素替代和/或其他临床治疗和/或诊断领域。

    Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy
    64.
    发明授权
    Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy 失效
    放射性标记的选择性雄激素受体调节剂及其在前列腺癌成像和治疗中的应用

    公开(公告)号：US07344700B2

    公开(公告)日：2008-03-18

    申请号：US10371210

    申请日：2003-02-24

    申请人： James T. Dalton ,  Duane D. Miller ,  Leonid I. Kirkovsky ,  Arnab Mukherjee

    发明人： James T. Dalton ,  Duane D. Miller ,  Leonid I. Kirkovsky ,  Arnab Mukherjee

    IPC分类号： A61K51/00

    CPC分类号： A61K51/04 ,  A61K51/0402 ,  A61K51/0406 ,  A61K51/0446 ,  A61K51/0455 ,  A61K51/0459

    摘要： Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and in treating or preventing prostate cancer. The agents define a new-subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention. The present invention further provides a method of producing the radiolabeled SARM compounds, and precursor compounds useful in the preparation of the radiolabeled SARM compounds.

    摘要翻译： 提供了一类用于前列腺癌成像和治疗或预防前列腺癌的放射性标记的雄激素受体靶向剂（ARTA）。 这些试剂定义了一种放射性标记化合物的新亚类，它们是选择性雄激素受体调节剂（SARM），其表现出雄激素受体的非甾族化合物的抗雄激素活性和/或不依赖于雄激素受体的结合。 本发明进一步提供a）用于a）成像受试者中的癌症的方法，b）使受试者中含有雄激素受体的组织成像，c）受试者体内成像，d）治疗患有前列腺癌的受试者，e ）延迟患有前列腺癌的受试者的前列腺癌的进展，f）预防患有前列腺癌的受试者中前列腺癌的复发，以及g）治疗患有前列腺癌的受试者中前列腺癌的复发，其包括 使用本发明的放射性标记的化合物。 本发明还提供了一种制备放射性标记的SARM化合物的方法，以及可用于制备放射性标记的SARM化合物的前体化合物。

    Methylene-bridged selective androgen receptor modulators and methods of use thereof
    65.
    发明授权
    Methylene-bridged selective androgen receptor modulators and methods of use thereof 有权
    亚甲基桥接选择性雄激素受体调节剂及其使用方法

    公开(公告)号：US07253210B2

    公开(公告)日：2007-08-07

    申请号：US10683157

    申请日：2003-10-14

    申请人： James T. Dalton ,  Duane D. Miller ,  Igor Rakov

    发明人： James T. Dalton ,  Duane D. Miller ,  Igor Rakov

    IPC分类号： A61K31/16 ,  A61K31/165 ,  C07C255/00 ,  C07C67/02 ,  C07C233/00

    CPC分类号： C07C237/22 ,  A61K31/167 ,  C07C235/38 ,  C07C255/60

    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。

    Heterocyclic selective androgen receptor modulators and methods of use thereof
    66.
    发明授权
    Heterocyclic selective androgen receptor modulators and methods of use thereof 失效

    公开(公告)号：US07214693B2

    公开(公告)日：2007-05-08

    申请号：US10683125

    申请日：2003-10-14

    申请人： James T. Dalton ,  Duane D. Miller

    发明人： James T. Dalton ,  Duane D. Miller

    IPC分类号： C07D401/02 ,  C07D213/02 ,  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.

    Selective androgen receptor modulators
    67.
    发明授权
    Selective androgen receptor modulators 失效
    选择性雄激素受体调节剂

    公开(公告)号：US07205437B2

    公开(公告)日：2007-04-17

    申请号：US11125159

    申请日：2005-05-10

    申请人： James T. Dalton ,  Duane D. Miller ,  Yali He ,  Donghua Yin

    发明人： James T. Dalton ,  Duane D. Miller ,  Yali He ,  Donghua Yin

    IPC分类号： C07C233/05 ,  C07C255/00

    CPC分类号： C07C235/24

    摘要： The present invention relates to androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity, which are nonsteroidal ligands for the androgen receptor. The selective androgen receptor modulators (SARM) 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; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas.

    摘要翻译： 本发明涉及雄激素和合成代谢活性的雄激素受体靶向剂（ARTA），其是雄激素受体的非甾体配体。 选择性雄激素受体调节剂（SARM）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; e）降低前列腺癌的发生率，停止或导致消退; f）口服雄激素替代和/或其他临床治疗和/或诊断领域。

    N-bridged selective androgen receptor modulators and methods of use thereof
    68.
    发明授权
    N-bridged selective androgen receptor modulators and methods of use thereof 有权
    N-桥接的选择性雄激素受体调节剂及其使用方法

    公开(公告)号：US07022870B2

    公开(公告)日：2006-04-04

    申请号：US10462837

    申请日：2003-06-17

    申请人： James T. Dalton ,  Duane D. Miller ,  Craig A. Marhefka ,  Wenqing Gao

    发明人： James T. Dalton ,  Duane D. Miller ,  Craig A. Marhefka ,  Wenqing Gao

    IPC分类号： C07C255/00 ,  C07C67/02 ,  C07C233/02

    CPC分类号： C07D211/72 ,  A61K31/415 ,  A61K31/44 ,  A61K31/505 ,  A61K31/65 ,  C07C237/10 ,  C07C255/60 ,  C07D233/44 ,  C07D239/02

    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; 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，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。

    Non-steroidal agonist compounds and their use in male hormone therapy
    69.
    发明授权
    Non-steroidal agonist compounds and their use in male hormone therapy 失效
    非甾体激动剂化合物及其在男性激素治疗中的应用

    公开(公告)号：US6160011A

    公开(公告)日：2000-12-12

    申请号：US86699

    申请日：1998-05-29

    申请人： Duane D. Miller ,  Leonid I. Kirkovsky ,  James T. Dalton ,  Arnab Mukherjee

    发明人： Duane D. Miller ,  Leonid I. Kirkovsky ,  James T. Dalton ,  Arnab Mukherjee

    IPC分类号： A61K31/167 ,  A61K31/277 ,  C07C235/16 ,  C07C255/60 ,  C07C317/46 ,  C07C323/60 ,  A61K31/275

    CPC分类号： C07C323/60 ,  A61K31/167 ,  A61K31/277 ,  C07C235/16 ,  C07C255/60 ,  C07C317/46

    摘要： The present invention relates to a nonsteroidal agonist compound having the formula: ##STR1## where R.sub.1, R.sub.2, and R.sub.3 are the same or different and are a hydrogen, a nitro, a cyano, a carbamoyl, a halogen, a perfluoroalkyl, a haloalkylamido, an isothiocyanate, an azide, a diazocarbonyl, a substituted oxirane, or a .beta.-chloroethylamine; R.sub.4 is a hydrogen, an alkyl, or is joined to R.sub.5 ; R.sub.5 is a hydrogen, a hydroxy, an alkoxy, an acyloxy, an amino, an alkylamino, a halogen, an alkyl, a haloalkyl, or is joined to R.sub.4 ; R.sub.6 is a hydrogen, an alkyl, or a haloalkyl; A.sub.1 and A.sub.2 is the same or different, each is direct link or an alkylene; X.sub.1 is an oxygen, a sulfur, a sulphinyl, a sulphonyl, an amino, an alkylimino, or an alkylene; R.sub.7 is a hydrogen, a halogen, an alkoxy, a haloalkoxy, an acyloxy, a haloacyloxy, an aryloxy, a thioalkyl, a thioraryl, an amino, an alkylimino, an alkylamido group, a haloalkylamido group, or a phenyl optionally substituted with a halogen, a nitro group, an alkyl, a haloalkyl, a cyano, a hydroxyl, a carboxylic group, an amino, an alkylamino group, a dialkylamino group, a bisalkylamino group, a haloalkylamino group, a dihaloalkylamino group, a bishaloalkylamino group, an acylamido group, a diacylamido group, an alkylacylamido group, a haloacylamido group, a bis(haloacyl)imido group, or an alkylhaloacylamido group. The present invention further relates to a method of producing the non-steroidal agonist compound, a composition containing the non-steroidal agonist compound, and methods of binding an androgen receptor, suppressing spermatogenesis, and providing hormonal therapy for androgen-dependent conditions.

    摘要翻译： 本发明涉及具有下式的非甾体激动剂化合物：其中R1，R2和R3相同或不同，为氢，硝基，氰基，氨基甲酰基，卤素，全氟烷基，卤代烷基酰氨基，异硫氰酸酯 ，叠氮化物，重氮羰基，取代的环氧乙烷或β-氯乙胺; R4是氢，烷基，或与R5连接; R5是氢，羟基，烷氧基，酰氧基，氨基，烷基氨基，卤素，烷基，卤代烷基，或与R4结合; R6是氢，烷基或卤代烷基; A1和A2相同或不同，各自为直链或亚烷基; X1是氧，硫，亚磺酰基，磺酰基，氨基，烷基亚氨基或亚烷基; R 7是氢，卤素，烷氧基，卤代烷氧基，酰氧基，卤代酰氧基，芳氧基，硫代烷基，芳基，氨基，烷基亚氨基，烷基酰氨基，卤代烷基酰氨基或任选被 卤素，硝基，烷基，卤代烷基，氰基，羟基，羧基，氨基，烷基氨基，二烷基氨基，双烷基氨基，卤代烷基氨基，二卤代烷基氨基，二卤代烷基氨基， 酰基酰氨基，二酰氨基，烷基酰氨基，卤代酰氨基，双（卤代酰基）亚氨基或烷基卤代酰胺基。 本发明还涉及生产非甾体激动剂化合物的方法，含有非甾体激动剂化合物的组合物，和结合雄激素受体的方法，抑制精子发生，以及为雄激素依赖性条件提供激素疗法。