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    Haloacetamide and azide substituted compounds and methods of use thereof
    1.
    发明申请
    Haloacetamide and azide substituted compounds and methods of use thereof 审中-公开
    卤代乙酰胺和叠氮化物取代的化合物及其使用方法

    公开(公告)号：US20050137172A1

    公开(公告)日：2005-06-23

    申请号：US10963761

    申请日：2004-10-14

    申请人： James Dalton ,  Duane Miller ,  Vipin Nair ,  Huiping Xu

    发明人： James Dalton ,  Duane Miller ,  Vipin Nair ,  Huiping Xu

    IPC分类号： A61K31/165 ,  A61K31/21 ,  A61K31/277 ,  A61K31/655 ,  A61K31/66 ,  C07C235/24 ,  C07C255/60 ,  C07D207/44 ,  C07D207/452 ,  A61K31/195 ,  A61K31/32 ,  A61K31/4015

    CPC分类号： C07D207/452 ,  C07C235/24 ,  C07C255/60

    摘要： The present invention relates to a novel class of anti-cancer compounds, which contain a haloacetamide or azide moiety and are, in one embodiment, alkylating agents. These agents, either alone or in a composition, are useful for treating cancer, preventing cancer, delaying the progression of cancer, treating and/or preventing the recurrence of cancer, suppressing, inhibiting or reducing the incidence of cancer, or inducing apoptosis in a cancer cell. Accordingly, the present invention provides a) methods of treating cancer in a subject; b) methods of preventing cancer in a subject; c) methods of delaying the progression of cancer in a subject; d) methods of treating the recurrence of cancer in a subject; e) methods of preventing the recurrence of cancer in a subject; f) methods of suppressing, inhibiting or reducing the incidence of cancer in a subject; and g) methods of inducing apoptosis in a cancer cell; by administering to the subject an anti-cancer compound of the present invention or an analog or metabolite thereof, its N-oxide, ester, pharmaceutically acceptable salt, hydrate, or any combination thereof as described herein.

    摘要翻译： 本发明涉及一类新的抗癌化合物，其含有卤代乙酰胺或叠氮化物部分，在一个实施方案中是烷化剂。 这些药物单独或组合物可用于治疗癌症，预防癌症，延缓癌症进展，治疗和/或预防癌症复发，抑制，抑制或降低癌症发生率或诱导癌细胞凋亡 癌细胞。 因此，本发明提供了a）在受试者中治疗癌症的方法; b）预防受试者癌症的方法; c）延缓受试者癌症进展的方法; d）治疗患者癌症复发的方法; e）预防受试者癌症复发的方法; f）抑制或抑制受试者癌症发病率的方法; 和g）诱导癌细胞凋亡的方法; 通过向受试者施用本文所述的抗癌化合物或其类似物或代谢物，其N-氧化物，酯，药学上可接受的盐，水合物或其任何组合。

    Heterocyclic selective androgen receptor modulators and methods of use thereof
    4.
    发明申请
    Heterocyclic selective androgen receptor modulators and methods of use thereof 审中-公开
    杂环选择性雄激素受体调节剂及其使用方法

    公开(公告)号：US20070265290A1

    公开(公告)日：2007-11-15

    申请号：US11723957

    申请日：2007-03-22

    申请人： James Dalton ,  Duane Miller

    发明人： James Dalton ,  Duane Miller

    IPC分类号： A61K31/505 ,  A61K31/16 ,  A61K31/40 ,  A61K31/41 ,  C07D221/22 ,  C07D239/00 ,  C07D277/00 ,  C07D401/00 ,  C07D263/02 ,  C07D233/00 ,  A61K31/506 ,  A61K31/4164 ,  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.

    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。

    Treating wasting disorders with selective androgen receptor modulators
    5.
    发明申请
    Treating wasting disorders with selective androgen receptor modulators 有权
    用选择性雄激素受体调节剂治疗浪费障碍

    公开(公告)号：US20060111441A1

    公开(公告)日：2006-05-25

    申请号：US11220414

    申请日：2005-09-07

    申请人： James Dalton ,  Duane Miller ,  Mitchell Steiner ,  Karen Veverka

    发明人： James Dalton ,  Duane Miller ,  Mitchell Steiner ,  Karen Veverka

    IPC分类号： A61K31/277

    CPC分类号： A61K31/277

    摘要： This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.

    摘要翻译： 本发明提供：1）治疗患有肌肉消瘦障碍的受试者的方法; 2）预防受试者的肌肉消瘦障碍的方法; 3）治疗，预防，抑制，抑制或减轻患有肌肉消瘦障碍的受试者的肌肉损失的方法; 4）一种治疗，预防，抑制，减少或抑制患有肌肉消瘦障碍的受试者的肌肉消瘦的方法; 和/或5）通过向受试者施用选择性雄激素受体调节剂（SARM）和/或类似物衍生物，治疗，预防，抑制，减少或抑制患有肌肉消瘦疾病的受试者的肌肉蛋白分解代谢的方法 ，所述SARM化合物的异构体，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，杂质或晶体，或其任何组合。

    Irreversible selective androgen receptor modulators and methods of use thereof
    7.
    发明申请
    Irreversible selective androgen receptor modulators and methods of use thereof 审中-公开
    不可逆选择性雄激素受体调节剂及其使用方法

    公开(公告)号：US20060035966A1

    公开(公告)日：2006-02-16

    申请号：US10995567

    申请日：2004-11-24

    申请人： James Dalton ,  Duane Miller ,  Mitchell Steiner ,  Karen Veverka ,  Leonid Kirkovsky ,  Dong Hwang ,  Arnab Mukherjee

    发明人： James Dalton ,  Duane Miller ,  Mitchell Steiner ,  Karen Veverka ,  Leonid Kirkovsky ,  Dong Hwang ,  Arnab Mukherjee

    IPC分类号： C07C331/28

    CPC分类号： C07C323/60 ,  A61K31/16 ,  A61K31/26 ,  A61K31/275 ,  C07C261/02 ,  C07C265/12 ,  C07C331/10 ,  C07C331/28

    摘要： In one embodiment, 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). The SARM compounds have unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. In one embodiment, the SARM compounds bind irreversibly to the androgen receptor In another embodiment, the SARM compounds are androgen receptor antagonists, which bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds are alkylating agents. 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： 在一个实施方案中，本发明提供了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）。 SARM化合物对雄激素受体的非甾体配体具有意想不到的抗雄激素活性。 在一个实施方案中，SARM化合物不可逆地与雄激素受体结合。在另一个实施方案中，SARM化合物是雄激素受体拮抗剂，其不可逆地结合雄激素受体。 在另一个实施方案中，SARM化合物是烷化剂。 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。

    Formulations comprising selective androgen receptor modulators
    8.
    发明申请
    Formulations comprising selective androgen receptor modulators 审中-公开
    包含选择性雄激素受体调节剂的制剂

    公开(公告)号：US20060004042A1

    公开(公告)日：2006-01-05

    申请号：US11029022

    申请日：2005-01-05

    申请人： James Dalton ,  Duane Miller ,  Karen Veverka

    发明人： James Dalton ,  Duane Miller ,  Karen Veverka

    IPC分类号： A61K31/4706 ,  A61K31/405 ,  A61K31/165

    CPC分类号： A61K31/165 ,  A61K31/4706

    摘要： The present invention relates to pharmaceutical compositions and formulations comprising 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, 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; and/or e) decreasing the incidence of, halting or causing a regression of prostate cancer. The present invention provides pharmaceutical compositions comprising the selective androgen receptor modulator compounds, together with pharmaceutically acceptable excipients.

    摘要翻译： 本发明涉及包含新型雄激素受体靶向剂（ARTA）的药物组合物和制剂，其表现出雄激素受体的非甾体配体的雄激素和合成代谢活性。 这些药剂定义了一种新的选择性雄激素受体调节剂（SARM）的化合物亚类，它们可用于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; 和/或e）降低前列腺癌的发生率，停止或导致消退。 本发明提供了包含选择性雄激素受体调节剂化合物以及药学上可接受的赋形剂的药物组合物。

    Method of treating breast cancer with androgen receptor antagonists
    9.
    发明申请
    Method of treating breast cancer with androgen receptor antagonists 审中-公开
    用雄激素受体拮抗剂治疗乳腺癌的方法

    公开(公告)号：US20050080055A1

    公开(公告)日：2005-04-14

    申请号：US10760152

    申请日：2004-01-20

    申请人： James Dalton ,  Duane Miller ,  Mitchell Steiner ,  Karen Veverka

    发明人： James Dalton ,  Duane Miller ,  Mitchell Steiner ,  Karen Veverka

    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, pharmaceutical 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。