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    Non-steroidal radiolabeled agonist/antagonist compounds and their use in prostate cancer imaging
    52.
    发明授权
    Non-steroidal radiolabeled agonist/antagonist compounds and their use in prostate cancer imaging 失效

    公开(公告)号：US6019957A

    公开(公告)日：2000-02-01

    申请号：US90425

    申请日：1998-06-04

    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： A61K51/04 ,  C07B59/00 ,  C07C235/16 ,  C07C255/60 ,  C07C317/46 ,  C07C323/60 ,  C07D295/28 ,  A61K51/00

    CPC分类号： C07D295/30 ,  A61K51/0402 ,  A61K51/0406 ,  A61K51/0453 ,  C07B59/001 ,  C07C235/16 ,  C07C255/60 ,  C07C317/46 ,  C07C323/60 ,  A61K2123/00 ,  C07B2200/05 ,  C07B2200/07

    摘要： The present invention relates to a radiolabeled non-steroidal compound having the formula: ##STR1## where R.sub.1, R.sub.2, and R.sub.3, are the same or different and are a radioactive or nonradioactive halogen, a nitro, a cyano, a carbamoyl, a hydrogen, 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 radioactive or nonradioactive halogen, a hydrogen, a hydroxy, an alkyl, a haloalkyl, an alkoxy, an acyloxy, an amino, an alkylamino, a thio, a thioalkyl, or is joined to R.sub.4 ;R.sub.6 is a hydrogen, an alkyl, a halogen, or a haloalkyl;A.sub.1 and A.sub.2 are the same or different, and each is a direct link or an alkylene;X.sub.1 is a radioactive or nonradioactive halogen, an oxygen, a sulfur, a sulphinyl, a sulphonyl, an amino, an alkylimino, or alkylene;R.sub.7 is a radioactive or nonradioactive halogen, a hydrogen, an alkoxy, a haloalkoxy, an acyloxy, a haloacyloxy, an aryloxy, a thioalkyl, a thioraryl, an alkylsulphinyl, an arylsulphinyl, an alkylsulphonyl, an arylsulphonyl, an amino, an alkylimino, an alkylamido group, a radioactive or nonradioactive haloalkylamido group, a phenyl optionally substituted with a radioactive or nonradioactive halogen, a nitro group, an alkyl, a radioactive or nonradioactive haloalkyl, a cyano, a hydroxyl, a carboxyl group, an amino, an alkylamino group, a dialkylamino group, a bisalkylamino group, a radioactive or nonradioactive haloalkylamino group, a radioactive or nonradioactive dihaloalkylamino group, a radioactive or nonradioactive bishaloalkylamino group, an acylamido group, a diacylamido group, an alkylacylamido group, a radioactive or nonradioactive haloacylamido group, a radioactive or nonradioactive bis(haloacyl)imido group, or a radioactive or nonradioactive alkylhaloacylamido group.

    MULTI-SUBSTITUTED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
    54.
    发明申请
    MULTI-SUBSTITUTED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
    多选择性选择性受体调节剂及其使用方法

    公开(公告)号：US20110082212A1

    公开(公告)日：2011-04-07

    申请号：US12880389

    申请日：2010-09-13

    申请人： James T. Dalton ,  Duane D. Miller ,  Mitchell S. Steiner ,  Karen A. Veverka ,  Dong Jin Hwang ,  Jiyun Chen

    发明人： James T. Dalton ,  Duane D. Miller ,  Mitchell S. Steiner ,  Karen A. Veverka ,  Dong Jin Hwang ,  Jiyun Chen

    IPC分类号： A61K31/167 ,  C07C233/15 ,  A61P15/16 ,  A61P35/00 ,  A61P27/04

    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 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。

    Treating benign prostate hyperplasia with SARMS
    56.
    发明授权
    Treating benign prostate hyperplasia with SARMS 失效
    用SARMS治疗良性前列腺增生

    公开(公告)号：US07776921B2

    公开(公告)日：2010-08-17

    申请号：US10359270

    申请日：2003-02-06

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

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

    IPC分类号： A61K31/16

    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-α 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, N-oxide, or any combination thereof as described herein. This invention also provides a method of inhibiting a 5-α reductase type 1 and/or type 2 enzyme, comprising contacting the enzyme with an effective 5-α 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-α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，N-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-α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。

    Prodrugs of selective androgen receptor modulators and methods of use thereof
    58.
    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。

    Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy
    60.
    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。