Tetrahydroisoquinoline compounds for use as &bgr;3-adrenoreceptor agonists
    21.
    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

    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。

    Substituted acylanilides and methods of use thereof
    23.
    发明授权
    Substituted acylanilides and methods of use thereof 有权
    取代的酰基酰苯胺及其使用方法

    公开(公告)号:US08846756B2

    公开(公告)日:2014-09-30

    申请号:US13868768

    申请日:2013-04-23

    IPC分类号: A61K31/275 C07C255/60

    CPC分类号: C07C255/60 C07B2200/07

    摘要: This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.

    摘要翻译: 本发明提供了SARM化合物及其用于治疗受试者中的多种疾病或病症的用途,所述疾病或病症尤其包括肌肉消瘦疾病和/或病症或骨相关疾病和/或病症。

    Regenerable MgO promoted metal oxide oxygen carriers for chemical looping combustion
    24.
    发明授权
    Regenerable MgO promoted metal oxide oxygen carriers for chemical looping combustion 有权
    可再生的MgO促进金属氧化物氧载体进行化学循环燃烧

    公开(公告)号:US08807988B2

    公开(公告)日:2014-08-19

    申请号:US13477274

    申请日:2012-05-22

    IPC分类号: F23D3/40

    摘要: The disclosure provides an oxygen carrier comprised of a plurality of metal oxide particles in contact with a plurality of MgO promoter particles. The MgO promoter particles increase the reaction rate and oxygen utilization of the metal oxide when contacting with a gaseous hydrocarbon at a temperature greater than about 725° C. The promoted oxide solid is generally comprised of less than about 25 wt. % MgO, and may be prepared by physical mixing, incipient wetness impregnation, or other methods known in the art. The oxygen carrier exhibits a crystalline structure of the metal oxide and a crystalline structure of MgO under XRD crystallography, and retains these crystalline structures over subsequent redox cycles. In an embodiment, the metal oxide is Fe2O3, and the gaseous hydrocarbon is comprised of methane.

    摘要翻译: 本公开提供了由与多个MgO促进剂颗粒接触的多个金属氧化物颗粒构成的氧载体。 当在大于约725℃的温度下与MgO气体烃接触时,MgO助催化剂颗粒增加了金属氧化物的反应速率和氧气利用率。促进的氧化物固体通常包含小于约25wt。 %MgO,并且可以通过物理混合,初始润湿浸渍或本领域已知的其它方法制备。 氧载体在XRD晶体学下表现出金属氧化物的结晶结构和MgO的结晶结构,并且在随后的氧化还原循环中保留这些晶体结构。 在一个实施方案中,金属氧化物是Fe 2 O 3,并且气态烃由甲烷组成。

    Substituted acylanilides and methods of use thereof
    25.
    发明授权
    Substituted acylanilides and methods of use thereof 有权
    取代的酰基酰苯胺及其使用方法

    公开(公告)号:US08080682B2

    公开(公告)日:2011-12-20

    申请号:US11892595

    申请日:2007-08-24

    IPC分类号: C07C255/50 A61K31/275

    CPC分类号: C07C255/60 C07B2200/07

    摘要: This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.

    摘要翻译: 本发明提供了SARM化合物及其用于治疗受试者中的多种疾病或病症的用途,所述疾病或病症尤其包括肌肉消瘦疾病和/或病症或骨相关疾病和/或病症。

    SARMS and method of use thereof
    27.
    发明授权
    SARMS and method of use thereof 有权
    SARMS及其使用方法

    公开(公告)号:US07772433B2

    公开(公告)日:2010-08-10

    申请号:US11785250

    申请日:2007-04-16

    IPC分类号: C07C233/05 A61K31/165

    摘要: This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, muscle wasting diseases and/or disorders, bone-related diseases and/or disorders, diabetes, cardiovascular disease, renal disease and others.

    摘要翻译: 本发明提供了SARM化合物及其用于治疗受试者中各种疾病或病症的用途,包括肌肉消耗疾病和/或病症,骨相关疾病和/或病症,糖尿病,心血管疾病,肾脏疾病 和别的。

    Multi-substituted selective androgen receptor modulators and methods of use thereof
    28.
    发明授权
    Multi-substituted selective androgen receptor modulators and methods of use thereof 有权
    多取代的选择性雄激素受体调节剂及其使用方法

    公开(公告)号:US07705182B2

    公开(公告)日:2010-04-27

    申请号:US10371155

    申请日:2003-02-24

    IPC分类号: C07C233/05 A61K31/16

    CPC分类号: C07C235/24

    摘要: This invention provides 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。