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1. 发明申请

WO2003106401A1 N-BRIDGED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译： N-桥选择性受体调节剂及其使用方法
公开(公告)号：WO2003106401A1
公开(公告)日：2003-12-24
申请号：PCT/US2003/016219
申请日：2003-06-17
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION , DALTON, James , MILLER, Duane, D. , MARHEFKA, Craig, A. , GAO, Wenqing
发明人： DALTON, James , MILLER, Duane, D. , MARHEFKA, Craig, A. , GAO, Wenqing
IPC分类号： C07C233/05
CPC分类号： C07D211/72 , A61K31/415 , A61K31/44 , A61K31/505 , A61K31/65 , C07C237/10 , C07C255/60 , C07D233/44 , C07D239/02
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, and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.
摘要翻译：本发明提供了一类雄激素受体靶向剂（ARTA）。该药物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）治疗与雄激素降解有关的疾病（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌肉减少症，骨质减少症，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，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）降低前列腺癌的发作，停止或导致消退。

2. 发明申请

WO2009070645A8 INDOLES, DERIVATIVES, AND ANALOGS THEREOF AND USES THEREOF 审中-公开
公开(公告)号：WO2009070645A8
公开(公告)日：2009-06-04
申请号：PCT/US2008/084801
申请日：2008-11-26
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , UNIVERSITY OF TENNESSEE RESEARCH 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
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.

3. 发明申请

WO2004062612A2 LARGE-SCALE SYNTHESIS OF SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：选择性受体调节剂的大规模合成
公开(公告)号：WO2004062612A2
公开(公告)日：2004-07-29
申请号：PCT/US2004/000618
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： A61K
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）化合物的亚类，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，肥胖症，肌肉减少症，骨质减少症，骨质疏松症，情绪和认知的改变; 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，肌肉减少，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖和子宫内膜异位症）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; g）预防和/或治疗干眼病症; h）治疗和/或预防前列腺增生（BPH）; I）诱导癌细胞凋亡; j）治疗和/或预防女性性器官如乳腺癌，子宫癌和卵巢癌的癌症; 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。

4. 发明申请

WO2003074450A3 RADIOLABELED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND THEIR USE IN PROSTATE CANCER IMAGING AND THERAPY 审中-公开
公开(公告)号：WO2003074450A3
公开(公告)日：2003-09-12
申请号：PCT/US2003/003124
申请日：2003-02-24
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION , 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： A61K31/40
摘要： Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and n treating or preventing prostate cancer. The agents define a new subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention. The present invention further provides a method of producing the radiolabeled SARM compounds, and precursor compounds useful in the preparation of the radiolabeled SARM compounds.

5. 发明申请

WO2003074450A2 RADIOLABELED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND THEIR USE IN PROSTATE CANCER IMAGING AND THERAPY 审中-公开
标题翻译：放射性选择性原癌基因调节因子及其在前列腺癌成像和治疗中的应用
公开(公告)号：WO2003074450A2
公开(公告)日：2003-09-12
申请号：PCT/US2003/003124
申请日：2003-02-24
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION , 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： C07C
CPC分类号： A61K51/04 , A61K51/0402 , A61K51/0406 , A61K51/0446 , A61K51/0455 , A61K51/0459
摘要： Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and n treating or preventing prostate cancer. The agents define a new subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention. The present invention further provides a method of producing the radiolabeled SARM compounds, and precursor compounds useful in the preparation of the radiolabeled SARM compounds.
摘要翻译：提供了一类用于前列腺癌成像和治疗或预防前列腺癌的放射性标记的雄激素受体靶向剂（ARTA）。这些试剂定义了一种放射性标记化合物的新亚类，它们是选择性雄激素受体调节剂（SARM），其表现出非甾类配体对雄激素受体的抗雄激素活性和/或不依赖于雄激素受体的结合。本发明进一步提供a）用于a）成像受试者中的癌症的方法，b）使受试者中含有雄激素受体的组织成像，c）受试者体内成像，d）治疗患有前列腺癌的受试者，e ）延迟患有前列腺癌的受试者的前列腺癌的进展，f）预防患有前列腺癌的受试者中前列腺癌的复发，以及g）治疗患有前列腺癌的受试者中前列腺癌的复发，其包括使用本发明的放射性标记的化合物。本发明还提供了一种制备放射性标记的SARM化合物的方法，以及可用于制备放射性标记的SARM化合物的前体化合物。

6. 发明申请

WO2005037201A2 TREATING BONE-RELATED DISORDERS WITH SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：用选择性雄激素受体调节剂治疗骨关节疾病
公开(公告)号：WO2005037201A2
公开(公告)日：2005-04-28
申请号：PCT/US2004/033395
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： A61K
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，抑制或降低发生骨相关病症的风险的方法，例如骨质疏松症，骨质减少，骨再吸收增加，骨折，骨脆弱和/ 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。本发明还提供了降低脂肪量（FM）和增加瘦体重的方法，包括给予相同的方法。

7. 发明申请

WO2003074473A3 IRREVERSIBLE SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2003074473A3
公开(公告)日：2003-09-12
申请号：PCT/US2003/003121
申请日：2003-02-24
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION , 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： C07C233/05
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.

8. 发明申请

WO2003074471A1 HALOACETAMIDE AND AZIDE SUBSTITUTED COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：羟基乙酰胺和酰胺取代的化合物及其使用方法
公开(公告)号：WO2003074471A1
公开(公告)日：2003-09-12
申请号：PCT/US2003/003122
申请日：2003-02-24
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION , DALTON, James , MILLER, Duane, D.
发明人： DALTON, James , MILLER, Duane, D.
IPC分类号： C07C231/00
CPC分类号： A61K31/165 , A61K31/215 , A61K31/275 , A61K31/655 , C07C235/16 , C07C235/24 , C07C247/16 , C07F9/46 , C07F9/5004 , C07F9/5022 , C07F9/52
摘要： The present invention relates to a novel class of androgen receptor targeting agents (ARTA), which contain a haloacetamide or azide moiety and are alkylating agents. These agents which define a new subclass of compounds, namely selective androgen receptor modulators (SARMs) which, either alone or in 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：本发明涉及含有卤代乙酰胺或叠氮化物部分并且是烷化剂的新一类雄激素受体靶向剂（ARTA）。这些定义新化合物亚类的药剂，即选择性雄激素受体调节剂（SARM），其单独或组合物可用于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。

9. 发明申请

WO2022155543A1 PHARMACEUTICAL COMPOSITIONS FOR TREATING BREAST CANCERS AND METHODS OF USES THEREOF 审中-公开
公开(公告)号：WO2022155543A1
公开(公告)日：2022-07-21
申请号：PCT/US2022/012631
申请日：2022-01-14
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： STEINER, Mitchell , NARAYANAN, Ramesh , AHN, Sunjoo , DALTON, James
IPC分类号： A61K31/167 , A61K31/277 , A61K35/00
摘要： This invention relates to the treatment of breast cancer in a subject. Including methods of: treating by first determining the 18F-16Beta-fluoro-5alpha-dihydrotestosterone (18F-DHT) tumor uptake and identifying said subject as having AR-positive breast cancer based on F-DHT tumor uptake, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound and a cyclin-dependent kinase 4/6 (CDK 4/6) inhibitor.

10. 发明申请

WO2006015149A1 BAR SOAP COMPOSITIONS WITH ENHANCED LATHER PROPERTIES 审中-公开
标题翻译：具有增强皮革性能的BAR皂组合物
公开(公告)号：WO2006015149A1
公开(公告)日：2006-02-09
申请号：PCT/US2005/026845
申请日：2005-07-28
申请人： THE DIAL CORPORATION , DEMSON, Robert , DALTON, James , PATEL, Jayesh
发明人： DEMSON, Robert , DALTON, James , PATEL, Jayesh
IPC分类号： A61K7/00
CPC分类号： C11D10/04 , C11D1/92 , C11D3/3707 , C11D17/006
摘要： This invention relates to solid soap compositions which have greatly improved lather creaminess (lotion like feel) and bar slip in use. These improvements are achieved through a synergistic combination of high and low molecular weight polyols along with a co-surfactant. More specifically, it ha been found that a vegetable based fatty acid soap when combined with about 0.10 to 5.00% by weight of cocoamidopropyl hydroxy sultaine (amphoteric co-surfactant) and about 0.10 to about 4.00% by weight of PEG-12 (low molecular weight polyol) and about 0.01% to about 1.00% by weight of PEG-90M (high molecular weight polyol) results in a soap composition with greatly improved lather creaminess and slip in use.
摘要翻译：本发明涉及在使用中极大改善泡沫乳液（洗剂样感觉）和棒滑的固体肥皂组合物。这些改进通过高分子量和低分子量多元醇与辅助表面活性剂的协同组合来实现。更具体地，已经发现，当与约0.10至5.00重量％的椰油酰氨基丙基羟基磺基甜菜碱（两性助表面活性剂）和约0.10至约4.00重量％的PEG-12（低分子量重量多元醇）和约0.01％至约1.00％（重量）的PEG-90M（高分子量多元醇）导致皂组合物在使用中具有极大改善的泡沫霜和滑爽性。

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