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103 条记录 (耗时 0.031 秒)

    Yohimbine derivatives and use thereof
    14.
    发明授权
    Yohimbine derivatives and use thereof 失效
    育亨宾衍生物及其用途

    公开(公告)号：US07470703B1

    公开(公告)日：2008-12-30

    申请号：US11210206

    申请日：2005-08-23

    申请人： Duane D. Miller ,  Bob M. Moore, II ,  Suni Mustafa ,  Dennis R. Feller ,  Supriya A. Bavadekar

    发明人： Duane D. Miller ,  Bob M. Moore, II ,  Suni Mustafa ,  Dennis R. Feller ,  Supriya A. Bavadekar

    IPC分类号： A61K31/4745 ,  C07D471/16

    CPC分类号： C07D471/16

    摘要： Yohimbine derivatives are disclosed having modification of the C-16 carboxyl group to include a sidechain and where the resulting derivative does not possess a second yohimbine pharmacophore (i.e., the compound is not a yohimbine dimer). The yohimbine derivatives of the present invention are preferably characterized by selective activity as α2c-AR antagonists. Use of the compounds, or pharmaceutical composition containing them, for treating or preventing an α2c adrenergic receptor mediated condition or disorder, and for antagonizing activity of an α2c adrenergic receptor are also disclosed.

    摘要翻译： 公开了育亨宾衍生物，其具有C-16羧基的修饰以包括侧链，并且其中所得衍生物不具有第二育亨宾药效团（即，该化合物不是育亨宾二聚体）。 优选本发明的育亨宾衍生物的特征在于作为α2c-AR拮抗剂的选择性活性。 还公开了化合物或含有它们的药物组合物用于治疗或预防α2c肾上腺素能受体介导的病症或病症以及拮抗α2c肾上腺素能受体的活性的用途。

    Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy
    15.
    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

    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： A61K51/04 ,  C07C233/07

    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
    17.
    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

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

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

    IPC分类号： C07C255/50 ,  A61K31/275

    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; 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。

    Tetrahydroisoquinoline compounds for use as &bgr;3-adrenoreceptor agonists
    18.
    发明授权
    Tetrahydroisoquinoline compounds for use as &bgr;3-adrenoreceptor agonists 失效
    用作β3肾上腺素受体激动剂的四氢异喹啉化合物

    公开(公告)号：US06596734B1

    公开(公告)日：2003-07-22

    申请号：US10269438

    申请日：2002-10-11

    申请人： Dennis R. Feller ,  Duane D. Miller

    发明人： Dennis R. Feller ,  Duane D. Miller

    IPC分类号： C07D22102

    CPC分类号： C07D217/20

    摘要： The invention provides compounds of formula: wherein R1 is —NHS(O)mR, wherein R is alkyl, substituted alkyl, alkoxy, substituted alkoxy, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, or substituted heterocycle; X is independently selected from the group consisting of halo, alkyl, substituted alkyl, alkoxy, substituted alkoxy, hydroxy, nitro, amino, and substituted amino; R2 is benzyl or benzyl substituted with one or more substituents selected from the group consisting of halo, CF3, hydroxy, nitro, alkoxy, substituted alkoxy, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, substituted heterocycle, amino, and substituted amino of formula —NHR' or —NR′R′, wherein each R′ is alkyl, substituted alkyl, —C(O)Y, —C(O)NHY, or —C(O)SY, wherein Y is alkyl or substituted alkyl; R3 is H or alkyl; n is 0-3; m is 1-2; p is 1-4; the sum of n and p is 1-4; and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明提供下式的化合物：其中R1是-NHS（O）mR，其中R是烷基，取代的烷基，烷氧基，取代的烷氧基，环烷基，取代的环烷基，芳基，取代的芳基，杂芳基，取代的杂芳基，杂环或取代的杂环 ; X独立地选自卤素，烷基，取代的烷基，烷氧基，取代的烷氧基，羟基，硝基，氨基和取代的氨基; R 2是被一个或多个选自卤素，CF 3，羟基，硝基，烷氧基，取代的烷氧基，烷基，取代的烷基，环烷基，取代的环烷基，芳基，取代的芳基，杂芳基，取代的杂芳基， 杂环，取代的杂环，氨基和式-NHR'或-NR'R'的取代的氨基，其中每个R'是烷基，取代的烷基，-C（O）Y，-C（O）NHY或-C O）SY，其中Y是烷基或取代的烷基; R3是H或烷基; n为0-3; m是1-2; p为1-4; n和p的和为1-4; 及其药学上可接受的盐。