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    Synthesis of selective androgen receptor modulators
    64.
    发明授权
    Synthesis of selective androgen receptor modulators 有权
    选择性雄激素受体调节剂的合成

    公开(公告)号：US06995284B2

    公开(公告)日：2006-02-07

    申请号：US10277108

    申请日：2002-10-22

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

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

    IPC: C07C233/05 ,  C07C231/12

    CPC classification number: C07D215/227 ,  A61K31/167 ,  A61K31/404 ,  A61K31/4706 ,  A61K31/661 ,  C07C235/24 ,  C07D209/08 ,  C07D271/12 ,  G01N30/7233 ,  G01N33/5438 ,  G01N33/74 ,  G01N2030/8813

    Abstract: The present invention relates to a synthetic process for the preparation of 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; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

    Abstract translation: 本发明涉及一种用于制备新型雄激素受体靶向剂（ARTA）的合成方法，其表现出雄激素受体的非甾族化合物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; e）降低前列腺癌的发生率，停止或导致消退; f）口服雄激素替代和/或其他临床治疗和/或诊断领域。 本发明的方法适用于大规模制备，因为所有步骤都产生高纯度的化合物，因此避免了复杂的纯化方法，从而降低产率。 因此，本发明提供了可用于工业大规模合成的非甾体激动剂化合物的合成方法，并以高产率提供高纯度产品。

    Selective androgen receptor modulators and methods of use thereof
    65.
    发明授权
    Selective androgen receptor modulators and methods of use thereof 失效
    选择性雄激素受体调节剂及其使用方法

    公开(公告)号：US06492554B2

    公开(公告)日：2002-12-10

    申请号：US09935044

    申请日：2001-08-23

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

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

    IPC: C07C23305

    CPC classification number: A61K31/167 ,  C07C235/24 ,  G01N33/5438 ,  G01N33/74

    Abstract: The present invention relates to 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 male hormone therapy such as oral testosterone replacement therapy, treating prostate cancer, imaging prostate cancer.

    Abstract translation: 本发明涉及一种新型雄激素受体靶向剂（ARTA），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。 这些试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，可用于男性激素治疗，如口服睾酮替代疗法，治疗前列腺癌，成像前列腺癌。

    Non-steroidal radiolabeled agonist/antagonist compounds and their use in prostate cancer imaging
    67.
    发明授权
    Non-steroidal radiolabeled agonist/antagonist compounds and their use in prostate cancer imaging 失效

    公开(公告)号：US6019957A

    公开(公告)日：2000-02-01

    申请号：US90425

    申请日：1998-06-04

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

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

    IPC: A61K51/04 ,  C07B59/00 ,  C07C235/16 ,  C07C255/60 ,  C07C317/46 ,  C07C323/60 ,  C07D295/28 ,  A61K51/00

    CPC classification number: C07D295/30 ,  A61K51/0402 ,  A61K51/0406 ,  A61K51/0453 ,  C07B59/001 ,  C07C235/16 ,  C07C255/60 ,  C07C317/46 ,  C07C323/60 ,  A61K2123/00 ,  C07B2200/05 ,  C07B2200/07

    Abstract: The present invention relates to a radiolabeled non-steroidal compound having the formula: ##STR1## where R.sub.1, R.sub.2, and R.sub.3, are the same or different and are a radioactive or nonradioactive halogen, a nitro, a cyano, a carbamoyl, a hydrogen, a perfluoroalkyl, a haloalkylamido, an isothiocyanate, an azide, a diazocarbonyl, a substituted oxirane, or a .beta.-chloroethylamine;R.sub.4 is a hydrogen, an alkyl, or is joined to R.sub.5 ;R.sub.5 is a radioactive or nonradioactive halogen, a hydrogen, a hydroxy, an alkyl, a haloalkyl, an alkoxy, an acyloxy, an amino, an alkylamino, a thio, a thioalkyl, or is joined to R.sub.4 ;R.sub.6 is a hydrogen, an alkyl, a halogen, or a haloalkyl;A.sub.1 and A.sub.2 are the same or different, and each is a direct link or an alkylene;X.sub.1 is a radioactive or nonradioactive halogen, an oxygen, a sulfur, a sulphinyl, a sulphonyl, an amino, an alkylimino, or alkylene;R.sub.7 is a radioactive or nonradioactive halogen, a hydrogen, an alkoxy, a haloalkoxy, an acyloxy, a haloacyloxy, an aryloxy, a thioalkyl, a thioraryl, an alkylsulphinyl, an arylsulphinyl, an alkylsulphonyl, an arylsulphonyl, an amino, an alkylimino, an alkylamido group, a radioactive or nonradioactive haloalkylamido group, a phenyl optionally substituted with a radioactive or nonradioactive halogen, a nitro group, an alkyl, a radioactive or nonradioactive haloalkyl, a cyano, a hydroxyl, a carboxyl group, an amino, an alkylamino group, a dialkylamino group, a bisalkylamino group, a radioactive or nonradioactive haloalkylamino group, a radioactive or nonradioactive dihaloalkylamino group, a radioactive or nonradioactive bishaloalkylamino group, an acylamido group, a diacylamido group, an alkylacylamido group, a radioactive or nonradioactive haloacylamido group, a radioactive or nonradioactive bis(haloacyl)imido group, or a radioactive or nonradioactive alkylhaloacylamido group.

    Methods of treating meibomian gland dysfunction
    69.
    发明授权
    Methods of treating meibomian gland dysfunction 有权
    治疗睑板腺功能障碍的方法

    公开(公告)号：US08791158B2

    公开(公告)日：2014-07-29

    申请号：US13004764

    申请日：2011-01-11

    Applicant: James T. Dalton ,  Jeetendra Eswaraka

    Inventor： James T. Dalton ,  Jeetendra Eswaraka

    IPC: A01N37/34 ,  A61K31/275

    CPC classification number: A61K31/277

    Abstract: The present invention includes methods for treating Meibomian gland dysfunctions. The invention also includes methods for improving tear lipid composition, for treating abnormal Meibomian gland secretion and for normalizing Meibomian gland secretions.

    Abstract translation: 本发明包括治疗睑板腺功能障碍的方法。 本发明还包括改善泪液脂质组成，治疗异常睑板腺分泌物和使睑板腺分泌物正常化的方法。

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