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    • 34. 发明申请
    • Treating wasting disorders with selective androgen receptor modulators
    • 用选择性雄激素受体调节剂治疗浪费障碍
    • US20060111441A1
    • 2006-05-25
    • US11220414
    • 2005-09-07
    • James DaltonDuane MillerMitchell SteinerKaren Veverka
    • James DaltonDuane MillerMitchell SteinerKaren Veverka
    • A61K31/277
    • A61K31/277
    • 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.
    • 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。
    • 36. 发明申请
    • Irreversible selective androgen receptor modulators and methods of use thereof
    • 不可逆选择性雄激素受体调节剂及其使用方法
    • US20060035966A1
    • 2006-02-16
    • US10995567
    • 2004-11-24
    • James DaltonDuane MillerMitchell SteinerKaren VeverkaLeonid KirkovskyDong HwangArnab Mukherjee
    • James DaltonDuane MillerMitchell SteinerKaren VeverkaLeonid KirkovskyDong HwangArnab Mukherjee
    • C07C331/28
    • C07C323/60A61K31/16A61K31/26A61K31/275C07C261/02C07C265/12C07C331/10C07C331/28
    • 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.
    • 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。
    • 37. 发明申请
    • Formulations comprising selective androgen receptor modulators
    • 包含选择性雄激素受体调节剂的制剂
    • US20060004042A1
    • 2006-01-05
    • US11029022
    • 2005-01-05
    • James DaltonDuane MillerKaren Veverka
    • James DaltonDuane MillerKaren Veverka
    • A61K31/4706A61K31/405A61K31/165
    • A61K31/165A61K31/4706
    • 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.
    • 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。