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1. 发明申请

WO2004062612A3 LARGE-SCALE SYNTHESIS OF SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：选择性雄激素受体调节剂的大规模合成
公开(公告)号：WO2004062612A3
公开(公告)日：2004-11-04
申请号：PCT/US2004000618
申请日：2004-01-12
申请人： GTX INC , STEINER MITCHELL S , CHUNG KIWON , DALTON JAMES , MILLER DUANE D , VEVERKA KAREN A
发明人： STEINER MITCHELL S , CHUNG KIWON , DALTON JAMES , MILLER DUANE D , VEVERKA KAREN A
IPC分类号： C07C231/12 , C07C235/24 , C07C231/00
CPC分类号： C07C231/12 , C07C235/24
摘要： 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, and alterations in mood and cognition; 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 and endometriosis, 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 replacement; g) preventing and/or treating dry eye conditions; h) treatment and/or prevention of begnin prostate hyperplasia (BPH); I) inducing apoptosis in a cancer cell; j) treatment and/or prevention of cancers of female sexual organs such as breast cancer, uterine cancer and ovarian cancer; and/or other clinical therapeutic 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.
摘要翻译：本发明涉及一种制备新型雄激素受体靶向剂（ARTA）的合成方法，其显示了雄激素受体的非甾体配体的雄激素和合成代谢活性。这些药物定义了一种新的亚类化合物，它们是选择性雄激素受体调节剂（SARM），其可用于a）男性避孕; b）治疗多种激素相关病症，例如与衰老男性（ADAM）中的雄激素降低相关的病症，例如疲劳，抑郁症，性欲减退，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，肥胖症，肌肉减少症，骨质减少症，骨质疏松症以及情绪和认知改变; c）治疗与女性雄激素降低（ADIF）有关的病症，例如性功能障碍，性欲减退，性腺机能减退，肌肉减少症，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖症和子宫内膜异位症，d ）治疗和/或预防慢性肌肉消瘦; e）降低前列腺癌的发病率，停止或导致其消退; f）口服雄激素替代物; g）预防和/或治疗干眼症; h）治疗和/或预防begnin前列腺增生（BPH）; I）诱导癌细胞凋亡; j）治疗和/或预防女性性器官的癌症，如乳腺癌，子宫癌和卵巢癌; 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，因为所有步骤产生高纯度化合物，因此避免了复杂的纯化程序，最终降低了收率。因此，本发明提供了用于合成非甾体激动剂化合物的方法，其可以用于工业大规模合成，并且以高收率提供高纯度产物。

2. 发明申请

WO03074473A2 IRREVERSIBLE SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：不可逆选择性的雄激素受体调节剂及其使用方法
公开(公告)号：WO03074473A2
公开(公告)日：2003-09-12
申请号：PCT/US0303121
申请日：2003-02-24
申请人： UNIV TENNESSEE RES CORP , DALTON JAMES , MILLER DUANE D , CHUNG KIWON , HE YALI , STEINER MITCHELL S , VEVERKA KAREN A
发明人： DALTON JAMES , MILLER DUANE D , CHUNG KIWON , HE YALI , STEINER MITCHELL S , VEVERKA KAREN A
IPC分类号： A61K31/16 , A61K31/26 , A61K31/275 , C07C261/02 , C07C265/12 , C07C331/10 , C07C331/28 , C07C233/05 , C07C255/50
CPC分类号： 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化合物是与雄激素受体不可逆地结合的雄激素受体拮抗剂。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。

3. 发明申请

WO2005037201A3 TREATING BONE-RELATED DISORDERS WITH SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：用选择性的雄激素受体调节剂治疗骨骼相关疾病
公开(公告)号：WO2005037201A3
公开(公告)日：2005-10-06
申请号：PCT/US2004033395
申请日：2004-10-12
申请人： GTX INC , DALTON JAMES , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A , KEARBY JEFFREY
发明人： DALTON JAMES , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A , KEARBY JEFFREY
IPC分类号： A61K20060101 , C07F7/22
CPC分类号： A61K31/167 , A61K31/00 , A61K31/165 , A61K31/21 , A61K31/32 , A61K31/405 , A61K31/4704 , A61K31/66
摘要： This invention provides method of treating, preventing, suppressing, inhibiting, or reducing the risk of developing a bone-related disorder, for example osteoporosis, osteopenia, increased bone resorption, bone fracture, bone frailty and/or loss of bone mineral density (BMD), by administrating a therapeutically effective amount of a selective androgen receptor modulator (SARM) and/or its analogue, derivative, isomer, metabolite pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof. The invention also provides methods of decreasing fat mass (FM) and increasing lean mass, comprising administering same.
摘要翻译：本发明提供了治疗，预防，抑制，抑制或降低骨相关病症发生风险的方法，例如骨质疏松症，骨质减少，增加的骨吸收，骨折，骨质脆弱和/或骨矿物质密度的丧失（BMD ），通过施用治疗有效量的选择性雄激素受体调节剂（SARM）和/或其类似物，衍生物，异构体，代谢物药学上可接受的盐，药物产品，水合物，N-氧化物或其任何组合。本发明还提供降低脂肪量（FM）和增加瘦肉质量的方法，包括施用它们。

4. 发明申请

WO2013043304A9 ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：雌激素受体配体及其使用方法
公开(公告)号：WO2013043304A9
公开(公告)日：2014-04-24
申请号：PCT/US2012052141
申请日：2012-08-23
申请人： GTX INC , DALTON JAMES , STEINER MITCHELL S , COSS CHRISTOPHER C
发明人： DALTON JAMES , STEINER MITCHELL S , COSS CHRISTOPHER C
IPC分类号： A01N37/18 , A61K31/165
CPC分类号： A61K31/137 , A61K31/167
摘要： The present invention relates to methods for reducing testosterone levels by reduction of luteinizing hormone (LH) or independent of LH levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate (5) cancer, castration resistant prostate cancer (CRPC), metastatic castration resistant prostate cancer (mCRPC) and palliative treatment of prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC) and metastatic castration resistant prostate cancer (mCRPC), and methods of reducing high or increasing PSA levels and/or increasing SHBG levels in a subject suffering from prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC) and metastatic (10) castration resistant prostate cancer (mCRPC). The compounds of this invention suppress free or total testosterone levels despite castrate levels secondary to ADT and reduce high or increasing PSA levels.
摘要翻译：本发明涉及通过降低男性受试者的黄体生成素（LH）或LH水平而降低睾酮水平的方法以及治疗，抑制，降低发病率，降低严重程度或抑制前列腺癌，晚期前列腺（ 5）癌症，去势抗性前列腺癌（CRPC），转移性阉割抗性前列腺癌（mCRPC）和姑息治疗前列腺癌，晚期前列腺癌，去势抗性前列腺癌（CRPC）和转移性阉割抗性前列腺癌（mCRPC）在前列腺癌，晚期前列腺癌，阉割抗性前列腺癌（CRPC）和转移性（10）抗阉割前列腺癌（mCRPC）的受试者中降低PSA水平升高和/或增加SHBG水平。本发明的化合物尽管阉割水平继发于ADT并降低高水平或增加PSA水平，但抑制游离或总睾丸激素水平。

5. 发明申请

WO0216310A9 SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：选择性雄激素受体调节剂及其使用方法
公开(公告)号：WO0216310A9
公开(公告)日：2002-07-18
申请号：PCT/US0126328
申请日：2001-08-23
申请人： GTX INC , DALTON JAMES , MILLER DUANE D , YIN DONGHUA , HE YALI
发明人： DALTON JAMES , MILLER DUANE D , YIN DONGHUA , HE YALI
IPC分类号： A61P5/28 , A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , A61P7/06 , A61P13/08 , A61P15/00 , A61P15/08 , A61P15/16 , A61P19/10 , A61P35/00 , C07C235/24 , C07D209/08 , C07D215/22 , C07D215/227 , C07D271/12 , G01N33/543 , G01N33/74 , C07C233/15 , A01N31/16 , A01N37/18 , C07C233/33 , C07C233/48 , C07C235/26 , C07C237/14 , A01N31/165
CPC分类号： C07D215/227 , A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D271/12 , G01N33/5438 , G01N33/74
摘要： This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of non-steroidal agonist compounds. The invention further provides compositions containing the selective androgen modulator compounds or the non-steroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.
摘要翻译：本发明提供了一类新的雄激素受体靶向剂（ARTA）。这些代理定义了一种化合物的新亚类，它们是组织选择性雄激素受体调节剂（SARM），其可用于口服睾酮替代疗法，男性避孕，维持女性性欲，治疗前列腺癌和成像前列腺癌。这些药剂对于雄激素受体的非甾体配体的雄激素和合成代谢活性具有意想不到的体内活性。这些药物可以单独活性或与孕激素或雌激素联合使用。本发明进一步提供了一类新型的非甾体激动剂化合物。本发明进一步提供了含有选择性雄激素调节剂化合物或非甾体激动剂化合物的组合物以及结合雄激素受体，调节精子发生，治疗和成像前列腺癌以及提供雄激素依赖性病症的激素疗法的方法。

6. 发明申请

WO2006062857A3 COMPOSITIONS HAVING A HIGH ANTIVIRAL AND ANTIBACTERIAL EFFICACY 审中-公开
标题翻译：具有高抗病毒和抗细菌效能的组合物
公开(公告)号：WO2006062857A3
公开(公告)日：2006-12-14
申请号：PCT/US2005043794
申请日：2005-12-05
申请人： DIAL CORP , TAYLOR TIMOTHY , TOWNER HARRY ERNEST , FULS JANICE LYNN , COX BRUCE RUSSELL , FISCHLER GEORGE E , FOX PRISCILLA S , RODGERS NANCY DAY , DALTON JAMES
发明人： TAYLOR TIMOTHY , TOWNER HARRY ERNEST , FULS JANICE LYNN , COX BRUCE RUSSELL , FISCHLER GEORGE E , FOX PRISCILLA S , RODGERS NANCY DAY , DALTON JAMES
IPC分类号： A01N37/36
CPC分类号： A01N37/36 , A01N2300/00
摘要： A method of providing a rapid, broad spectrum bacterial control, and a rapid persistent antiviral control on a surface, and particularly a mammalian skin surface, is disclosed. In the method, a compound or composition capable of lowering skin pH to less than about 4 is applied to the skin, and preferably is allowed to remain on the skin.
摘要翻译：公开了一种在表面特别是哺乳动物皮肤表面提供快速，广谱的细菌控制和快速持续的抗病毒控制的方法。在该方法中，将能够将皮肤pH降低至小于约4的化合物或组合物施用于皮肤，优选保留在皮肤上。

7. 发明申请

WO2009070645A1 INDOLES, DERIVATIVES, AND ANALOGS THEREOF AND USES THEREOF 审中-公开
标题翻译：吲哚，衍生物及其类似物及其用途
公开(公告)号：WO2009070645A1
公开(公告)日：2009-06-04
申请号：PCT/US2008084801
申请日：2008-11-26
申请人： OHIO UNIVERSITY RES FOUNDATION , UNIV TENNESSEE RES FOUNDATION , DALTON JAMES , MILLER DUANE , AHN SUNJOO , DUKE CHARLES , HWANG DONG JIN , YANG JUN
发明人： DALTON JAMES , MILLER DUANE , AHN SUNJOO , DUKE CHARLES , HWANG DONG JIN , YANG JUN
IPC分类号： C07D401/00
CPC分类号： C07D209/04 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/14 , C07D405/04 , C07D405/06 , C07D409/04 , C07D417/06
摘要： Indole derivatives and analog compounds and pharmaceutical compositions comprising the same are provided. Also provided are methods of using these compounds to inhibit tubulin polymerization in a cell associated with a proliferative disease or to treat a cancer.
摘要翻译：提供了吲哚衍生物和类似物以及包含它们的药物组合物。还提供了使用这些化合物抑制与增殖性疾病相关的细胞中的微管蛋白聚合或治疗癌症的方法。

8. 发明申请

WO2007139847A2 METHOD OF ENHANCING THE CONTROL OF VIRUSES ON SKIN 审中-公开
标题翻译：提高皮肤病毒控制的方法
公开(公告)号：WO2007139847A2
公开(公告)日：2007-12-06
申请号：PCT/US2007012321
申请日：2007-05-23
申请人： DIAL CORP , FULS JANICE LYNN , RODGERS NANCY DAY , FOX PRISCILLA S , DALTON JAMES , TOWNER HARRY ERNEST , PEDERSEN DANIEL E , ROLANDO JOHN J , STAUB RICHARD K
发明人： FULS JANICE LYNN , RODGERS NANCY DAY , FOX PRISCILLA S , DALTON JAMES , TOWNER HARRY ERNEST , PEDERSEN DANIEL E , ROLANDO JOHN J , STAUB RICHARD K
CPC分类号： A01N31/02 , A01N25/00 , A01N37/04 , A01N37/36 , A61K31/045 , A61K31/192 , A61K31/194 , A61K31/78 , A01N35/02 , A01N47/36 , A01N37/02 , A01N2300/00
摘要： A method of imparting a rapid antiviral effectiveness, and a persistent antiviral effectiveness, to an animate surface is disclosed. The method includes first treating the animate surface with a preconditioning composition, followed by treating the animate surface with an antiviral composition.
摘要翻译：公开了赋予动画表面的快速抗病毒效力和持久的抗病毒效能的方法。该方法包括用预处理组合物首先处理动画表面，然后用抗病毒组合物处理动画表面。

9. 发明申请

WO2007044032A3 COMPOSITIONS HAVING A HIGH ANTIVIRAL AND ANTIBACTERIAL EFFICACY 审中-公开
标题翻译：具有高抗病毒和抗细菌效能的组合物
公开(公告)号：WO2007044032A3
公开(公告)日：2008-03-06
申请号：PCT/US2005043910
申请日：2005-12-05
申请人： DIAL CORP , FULS JANICE LYNN , TAYLOR TIMOTHY J , FOX PRISCILLA S , RODGERS NANCY DAY , TOWNER HARRY ERNEST , DALTON JAMES
发明人： FULS JANICE LYNN , TAYLOR TIMOTHY J , FOX PRISCILLA S , RODGERS NANCY DAY , TOWNER HARRY ERNEST , DALTON JAMES
IPC分类号： A01N31/02 , A01N37/04 , A01N37/10 , A61K31/045 , A61K31/19 , A61K31/60 , A61K31/78 , A61P1/00
CPC分类号： A61K31/19 , A01N31/02 , A61K31/045 , A61K31/60 , A61K31/78 , A01N37/02 , A01N37/04 , A01N37/36 , A01N2300/00 , A61K2300/00
摘要： Antimicrobial compositions having a rapid antiviral and antibacterial effectiveness, and a persistent antiviral effectiveness, are disclosed. The antimicrobial compositions contain (a) a disinfecting alcohol, (b) an organic acid, and (c) water, wherein the composition has a pH of about 5 or less.
摘要翻译：公开了具有快速抗病毒和抗菌效力以及持久的抗病毒效果的抗微生物组合物。抗微生物组合物含有（a）消毒醇，（b）有机酸和（c）水，其中所述组合物的pH为约5或更低。

10. 发明申请

WO2006065789A3 METHOD AND SYSTEM FOR SECURELY AUTHORIZING ANONYMOUS PEERS OF VOIP NETWORKS 审中-公开
标题翻译：用于安全地授权VOIP网络的匿名对等体的方法和系统
公开(公告)号：WO2006065789A3
公开(公告)日：2007-04-19
申请号：PCT/US2005045013
申请日：2005-12-13
申请人： TRANSNEXUS INC , DALTON JAMES , ISAKBAYEV DMITRY
发明人： DALTON JAMES , ISAKBAYEV DMITRY
IPC分类号： H04L12/66
CPC分类号： H04L12/14 , H04L12/1446 , H04L12/1471 , H04L29/12018 , H04L61/10 , H04L63/123 , H04L63/126 , H04L65/104 , H04L65/105 , H04L65/1069 , H04L65/1073 , H04L65/80 , H04L67/104 , H04M3/42008 , H04M7/0063 , H04M7/0078 , H04M15/56 , H04M2215/202
摘要： A peering authority or settlement clearinghouse (Fig. 2A, 300) can be used to control access, collect session accounting information and provide financial settlement of interconnect or session fees among anonymous Internet Protocol (IP) peers (120, 230) or networks. The addition of peering policy criteria, such as price and quality of service, to peer to peer route discovery mechanisms enable a trusted intermediary, such as the settlement clearinghouse (300), to authorize acceptable interconnection or peeing sessions between anonymous IP peers (120, 230). Any financial settlement transactions which result from the peering sessions may be subsequently executed by the settlement clearinghouse (300).
摘要翻译：可以使用对等机构或结算交换所（图2A，300）来控制访问，收集会话会计信息，并在匿名互联网协议（IP）对等体（120,230）或网络之间提供互连或会话费用的财务结算。将对等政策标准（如价格和服务质量）添加到对等路由发现机制中，使诸如结算信息交换所（300）之类的信托中介机构授权匿名IP对等体之间可接受的互联或对讲会话（120， 230）。结算交易所（300）可能会由对方会议导致的任何财务结算交易。

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