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    Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy
    41.
    发明申请
    Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy 审中-公开
    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：US20080193380A1

    公开(公告)日：2008-08-14

    申请号：US11984838

    申请日：2007-11-21

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

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

    IPC: A61K51/04 ,  C07C233/07

    CPC classification number: A61K51/04 ,  A61K51/0402 ,  A61K51/0406 ,  A61K51/0446 ,  A61K51/0455 ,  A61K51/0459

    Abstract: 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.

    Abstract translation: 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），其表现出非甾类配体对雄激素受体的抗雄激素活性和/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。

    Halogenated selective androgen receptor modulators and methods of use thereof
    43.
    发明授权
    Halogenated selective androgen receptor modulators and methods of use thereof 失效
    卤代选择性雄激素受体调节剂及其使用方法

    公开(公告)号：US07026500B2

    公开(公告)日：2006-04-11

    申请号：US10371213

    申请日：2003-02-24

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

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

    IPC: C07C255/50 ,  A61K31/275

    CPC classification number: C07D215/227 ,  A61K31/165 ,  A61K31/404 ,  A61K31/4706 ,  A61K31/661 ,  C07C235/16 ,  C07C235/24 ,  C07C255/60 ,  C07C335/18 ,  C07D209/08 ,  C07D271/12

    Abstract: 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.

    Abstract translation: 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。

    ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF
    46.
    发明申请
    ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF 有权
    雌激素受体配体及其使用方法

    公开(公告)号：US20150087712A1

    公开(公告)日：2015-03-26

    申请号：US14523333

    申请日：2014-10-24

    Applicant: James T. Dalton ,  Mitchell S. Steiner ,  Christopher C. Coss ,  Robert H. Getzenberg

    Inventor： James T. Dalton ,  Mitchell S. Steiner ,  Christopher C. Coss ,  Robert H. Getzenberg

    IPC: C07C235/64 ,  C07C215/50 ,  A61K31/137 ,  A61K45/06 ,  A61K31/167 ,  C07C233/75 ,  C07C215/82

    CPC classification number: C07C235/64 ,  A61K31/136 ,  A61K31/137 ,  A61K31/167 ,  A61K45/06 ,  C07C215/50 ,  C07C215/82 ,  C07C233/75 ,  C07D295/088

    Abstract: The present invention relates to methods for reducing testosterone levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC), metastatic castration resistant prostate cancer (mCRPC), and methods of reducing high or increasing PSA levels and/or increasing SHBG levels in a subject suffering from prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC) and metastatic castration resistant prostate cancer (mCRPC). The compounds of this invention suppress free or total testosterone levels despite castrate levels secondary to ADT and reduce high or increasing PSA levels. This reduction in testosterone levels may be used to treat prostate cancer, advanced prostate cancer, CRPC and mCRPC without causing bone loss, decreased bone mineral density, increased risk of bone fractures, increased body fat, hot flashes and/or gynecomastia.

    Abstract translation: 本发明涉及降低男性受试者睾丸激素水平的方法以及治疗，抑制，降低发病率，降低严重程度或抑制前列腺癌，晚期前列腺癌，抗阉割前列腺癌（CRPC），转移性阉割抗性前列腺的方法 癌症（mCRPC），以及在患有前列腺癌，晚期前列腺癌，抗阉割前列腺癌（CRPC）和转移性阉割抗性前列腺癌（mCRPC）的受试者中降低高水平或增加PSA水平和/或增加SHBG水平的方法。 本发明的化合物尽管阉割水平继发于ADT并降低高水平或增加PSA水平，但抑制游离或总睾丸激素水平。 睾丸激素水平的降低可用于治疗前列腺癌，晚期前列腺癌，CRPC和mCRPC，而不会引起骨丢失，骨矿物质密度降低，骨折的风险增加，身体脂肪增加，潮热和/或男子乳房发育。

    Compounds for treatment of cancer
    48.
    发明授权
    Compounds for treatment of cancer 有权
    化合物治疗癌症

    公开(公告)号：US08592465B2

    公开(公告)日：2013-11-26

    申请号：US12485881

    申请日：2009-06-16

    Applicant: Duane D. Miller ,  Wei Li ,  Zhao Wang ,  Yan Lu ,  Jianjun Chen ,  James T. Dalton ,  Chien-Ming Li

    Inventor： Duane D. Miller ,  Wei Li ,  Zhao Wang ,  Yan Lu ,  Jianjun Chen ,  James T. Dalton ,  Chien-Ming Li

    IPC: C07D277/04 ,  C07D277/24 ,  A61K31/426

    CPC classification number: C07D403/04 ,  A61K31/421 ,  A61K31/426

    Abstract: Compounds according to formula (I) are disclosed where Q is S, N, or O; X is optional, and can be O═, S═, ═N—NH2, ═N—OH, or —OH; Y is optional and can be —N(H)—, O, or C1 to C20 hydrocarbon; and R1 and R2 are each independently substituted or unsubstituted single-, fused- or multiple-ring aryl or (hetero)cyclic ring systems. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.

    Abstract translation: 公开了根据式（I）的化合物，其中Q是S，N或O; X是任选的，并且可以是O =，S =，= N-NH 2，= N-OH或-OH; Y是任选的，可以是-N（H） - ，O或C 1 -C 20烃; 且R 1和R 2各自独立地为取代或未取代的单，稠环或多环芳基或（杂）环系。 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。

    Treating androgen decline in aging male (ADAM)-associated conditions with SARMs
    49.
    发明授权
    Treating androgen decline in aging male (ADAM)-associated conditions with SARMs 有权
    老年男性（ADAM）治疗雄激素相关性SARS的情况下降

    公开(公告)号：US08445534B2

    公开(公告)日：2013-05-21

    申请号：US12632619

    申请日：2009-12-07

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

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

    IPC: A61K31/275

    CPC classification number: C07C235/24 ,  A61K31/16 ,  A61K31/167 ,  A61K31/277 ,  C07C255/60

    Abstract: 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.

    Abstract translation: 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。

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