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31. 发明申请

WO2011140228A1 NUCLEAR RECEPTOR BINDING AGENTS 审中-公开
标题翻译：核受体结合剂
公开(公告)号：WO2011140228A1
公开(公告)日：2011-11-10
申请号：PCT/US2011/035206
申请日：2011-05-04
申请人： GTX, INC. , NARAYANAN, Ramesh , YEPURU, Muralimohan , DALTON, James, T.
发明人： NARAYANAN, Ramesh , YEPURU, Muralimohan , DALTON, James, T.
IPC分类号： A01N43/42 , A61K31/47
CPC分类号： A61K31/4709 , A61K31/472 , C07D217/22 , C07D217/24
摘要： The present invention relates to methods for prevention and/or treatment of metabolic disorders, post-menopausal obesity and conditions associated with high fat diet consumption including, obesity, body weight gain, fat mass formation, bone mineral content reduction, white adipose tissue weight gain, increased cholesterol levels, increased leptin levels, insulin resistance, type II diabetes, increased blood glucose levels, inflammatory diseases, cardiovascular diseases, fatty liver condition (accumulation of fat in the liver), decreased uncoupling protein- 1 (UCP-1) levels and increased lipogenesis.
摘要翻译：本发明涉及用于预防和/或治疗代谢紊乱，绝经后肥胖症和与高脂肪饮食消费相关的病症的方法，包括肥胖，体重增加，脂肪量形成，骨矿物质含量减少，白人脂肪组织体重增加，增加的胆固醇水平，瘦素水平升高，胰岛素抵抗，II型糖尿病，血糖水平升高，炎症性疾病，心血管疾病，脂肪肝状况（脂肪在肝脏中的积累），减少的解偶联蛋白-1（UCP-1）水平并增加脂肪生成。

32. 发明申请

WO2008008433A3 SUBSTITUTED ACYLANILIDES AND METHODS OF USE THEREOF 审中-公开
标题翻译：取代的ACYILILIDES及其使用方法
公开(公告)号：WO2008008433A3
公开(公告)日：2008-09-25
申请号：PCT/US2007015895
申请日：2007-07-12
申请人： UNIV TENNESSEE RES FOUNDATION , DALTON JAMES T , MILLER DUANE D
发明人： DALTON JAMES T , MILLER DUANE D
IPC分类号： C07C391/00 , C07C275/40
CPC分类号： C07C255/60
摘要： This invention provides substituted acylanilide 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：本发明提供取代的酰苯胺化合物及其用于治疗受试者中的各种疾病或病症，尤其包括肌肉萎缩疾病和/或病症或骨相关疾病和/或病症的用途。

33. 发明申请

WO2007143081A3 THERAPEUTIC AGENTS FOR THE TREATMENT OF LYMPHOID MALIGNANCIES 审中-公开
标题翻译：用于治疗淋巴细胞恶性肿瘤的治疗药物
公开(公告)号：WO2007143081A3
公开(公告)日：2008-02-21
申请号：PCT/US2007012921
申请日：2007-06-01
申请人： UNIV OHIO STATE RES FOUND , BYRD JOHN C , PERROTTI DANILO , CHEN CHING-SHIH , DALTON JAMES T , FRISSORA FRANK , ZHAO XIAOBIN , LIU QING , MUTHUSAMY NATARAJAN
发明人： BYRD JOHN C , PERROTTI DANILO , CHEN CHING-SHIH , DALTON JAMES T , FRISSORA FRANK , ZHAO XIAOBIN , LIU QING , MUTHUSAMY NATARAJAN
IPC分类号： A61K31/135
CPC分类号： A61K31/137 , A61K45/06
摘要： Methods- for treatment and prevention of lymphoid malignancies, including, but not limited to acute lymphoblastic leukemia (ALL), chronic lymphocytic leukemia (CLL), B-cell lymphoma, Acute Myeloid leukemia (AML), and mantle cell lymphoma (MCL). The methods include administration of a therapeutically effective amount of FTY720 (2-Amino-2-[2-(4- octylphenyl) ethyl] propane 1, 3-diol hydrochloride) or a derivative, pharmaceutically acceptable salt thereof, or a prodrug thereof to a subject.
摘要翻译：方法 - 用于治疗和预防淋巴恶性肿瘤，包括但不限于急性淋巴细胞性白血病（ALL），慢性淋巴细胞白血病（CLL），B细胞淋巴瘤，急性骨髓性白血病（AML）和套细胞淋巴瘤（MCL）。所述方法包括将治疗有效量的FTY720（2-氨基-2- [2-（4-辛基苯基）乙基]丙烷-1,3-二醇盐酸盐）或其衍生物，药学上可接受的盐或其前药给予课程。

34. 发明申请

WO2007081696A3 TREATING ANDROGEN DECLINE IN AGING MALE (ADAM)-ASSOCIATED CONDITIONS WITH SARMS 审中-公开
公开(公告)号：WO2007081696A3
公开(公告)日：2007-07-19
申请号：PCT/US2007/000052
申请日：2007-01-04
申请人： GTX, INC. , DALTON, James, T. , MILLER, Duane, D. , STEINER, Mitchell, S. , VEVERKA, Karen, A.
发明人： DALTON, James, T. , MILLER, Duane, D. , STEINER, Mitchell, S. , VEVERKA, Karen, A.
IPC分类号： A01N37/34 , A61K31/275
摘要： This invention provides methods for treatment and inhibition of a male subject having an Androgen Decline in Aging Male (ADAM)-associated condition, for example sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, an alteration in cognition and mood, depression, anemia, hair loss, obesity, muscle loss, dry eye, memory loss, benign prostate hyperplasia and/or prostate cancer, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, pro-drug, polymorph, crystal, or any combination thereof.

35. 发明申请

WO2007062230A3 NUCLEAR RECEPTOR BINDING AGENTS 审中-公开
公开(公告)号：WO2007062230A3
公开(公告)日：2007-05-31
申请号：PCT/US2006/045451
申请日：2006-11-28
申请人： GTX, INC. , DALTON, James, T. , BARRETT, Christina , HE, Yali , HONG, Seoung-Soo , MILLER, Duane, D. , MOHLER, Michael, L. , NARAYANAN, Ramesh , WU, Zhongzhi
发明人： DALTON, James, T. , BARRETT, Christina , HE, Yali , HONG, Seoung-Soo , MILLER, Duane, D. , MOHLER, Michael, L. , NARAYANAN, Ramesh , WU, Zhongzhi
IPC分类号： C07C233/65 , A61K31/165
摘要： The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.

36. 发明申请

WO2004066922A2 A METHOD OF TREATING BREAST CANCER WITH ANDROGEN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：一种用雄激素受体拮抗剂治疗乳腺癌的方法
公开(公告)号：WO2004066922A2
公开(公告)日：2004-08-12
申请号：PCT/US2004/001313
申请日：2004-01-20
申请人： GTX INC. , STEINER, Mitchell, S. , DALTON, James, T. , MILLER, Duane, D. , VEVERKA, Karen, A.
发明人： STEINER, Mitchell, S. , DALTON, James, T. , MILLER, Duane, D. , VEVERKA, Karen, A.
IPC分类号： A61K
CPC分类号： A61K31/66 , A61K31/21 , A61K31/26
摘要： This invention relates to the prevention and treatment of breast cancer in a subject, for example a female subject. Accordingly, this invention provides methods of a) treating a subject suffering from breast cancer; b) preventing, suppressing, inhibiting or reducing the incidence of breast cancer in a subject; c) delaying the progression of breast cancer in a subject suffering from breast cancer; d) preventing the recurrence of breast cancer in a subject; e) treating the recurrence of breast cancer in a subject suffering from breast cancer; and/or f) treating, preventing, suppressing or inhibiting metastasis in a subject suffering from breast cancer, by administering to the subject a therapeutically effective amount of an Androgen Receptor Antagonist and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, phatmaceutical product, hydrate, N-Oxide, crystal polymorph, prodrug or any combination thereof, as described herein.
摘要翻译：本发明涉及预防和治疗受试者，例如女性受试者的乳腺癌。因此，本发明提供了a）治疗患有乳腺癌的受试者的方法; b）预防，抑制，抑制或降低患者乳腺癌的发生率; c）延缓乳腺癌患者乳腺癌的进展; d）预防受试者乳腺癌的复发; e）治疗乳腺癌患者乳腺癌的复发; 和/或f）通过向受试者施用治疗有效量的雄激素受体拮抗剂和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，治疗，预防，抑制或抑制患有乳腺癌的受试者的转移，药物产品，水合物，N-氧化物，晶体多晶型物，前药或其任何组合。

37. 发明申请

WO2004035738A3 METHYLENE-BRIDGED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：亚甲基桥选择性受体调节剂及其使用方法
公开(公告)号：WO2004035738A3
公开(公告)日：2004-07-15
申请号：PCT/US0332511
申请日：2003-10-14
申请人： UNIV TENNESSEE RES FOUNDATION , DALTON JAMES T , MILLER DUANE D
发明人： DALTON JAMES T , MILLER DUANE D
IPC分类号： A61K31/167 , A61K31/44 , A61K31/60 , C07C205/00 , C07D215/16
CPC分类号： C07C237/22 , A61K31/167 , C07C235/38 , C07C255/60
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; 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：本发明提供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）。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; 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。

38. 发明申请

WO2004034978A3 TREATING OBESITY WITH SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：选择性雄激素受体调节剂治疗肥胖
公开(公告)号：WO2004034978A3
公开(公告)日：2004-07-15
申请号：PCT/US0332509
申请日：2003-10-14
申请人： GTX INC , DALTON JAMES T , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A
发明人： DALTON JAMES T , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A
IPC分类号： A61K31/165 , A61K31/405 , A61K31/4706 , A61K31/675
CPC分类号： A61K31/165
摘要： This invention relates to the prevention and treatment of obesity. More particularly, this invention relates to a method of: a) treating, preventing, suppressing, inhibiting, or reducing obesity; b) promoting, increasing or facilitating weight loss; c) decreasing, suppressing, inhibiting or reducing appetite; d) altering the body composition, e) altering lean body mass or fat free body mass, f) converting fat to lean muscle; g) treating, preventing, suppressing, inhibiting, or reducing an obesity-associated metabolic disorder, for example hypertension, osteoarthritis, Type II diabetes mellitus, increased blood pressure, stroke, or heart disease; h) decreasing, suppressing, inhibiting or reducing adipogenesis; i) altering stem cell differentiation; and/or j) altering the level of leptin; comprising administering a therapeutically effective amount of a selective androgen receptor modulator and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, crystal, or any combination thereof, as described herein.
摘要翻译：本发明涉及肥胖症的预防和治疗。更具体地说，本发明涉及一种方法：a）治疗，预防，抑制，抑制或减少肥胖; b）促进，增加或促进体重减轻; c）减少，抑制，抑制或减少食欲; d）改变身体组成，e）改变瘦体重或无脂肪体重，f）将脂肪转化为瘦肌肉; g）治疗，预防，抑制，抑制或减轻与肥胖相关的代谢病症，例如高血压，骨关节炎，II型糖尿病，血压升高，中风或心脏病; h）减少，抑制，抑制或减少脂肪形成; i）改变干细胞分化; 和/或j）改变瘦素水平; 包括给予治疗有效量的选择性雄激素受体调节剂和/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，前药，多晶型物，晶体或其任何组合于此。

39. 发明申请

WO2004035739A2 TREATING ANDROGEN DECLINE IN AGING MALE (ADAM)-ASSOCIATED CONDITIONS WITH SARMS 审中-公开
标题翻译：治疗老年男性（ADAM）的SARS治疗条件恶化
公开(公告)号：WO2004035739A2
公开(公告)日：2004-04-29
申请号：PCT/US2003/032513
申请日：2003-10-14
申请人： GTX, INC. , DALTON, James, T. , MILLER, Duane, D. , STEINER, Mitchell, S. , VEVERKA, Karen, A.
发明人： DALTON, James, T. , MILLER, Duane, D. , STEINER, Mitchell, S. , VEVERKA, Karen, A.
IPC分类号： C12N
CPC分类号： C07K14/721
摘要： The present invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of an Androgen Decline in Aging Male (ADAM)- associated condition in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, crystal, or any combination thereof. The present invention further provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, benign prostate hyperplasia or prostate cancer due to ADAM in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, crystal, or any combination thereof.
摘要翻译：本发明提供了通过向受试者施用选择性雄激素受体调节剂（SARM）化合物来治疗，预防，抑制或抑制雄性雄性雄激素降低（ADAM）相关病症的男性受试者的发生率的方法和/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，前药，多晶型物，晶体或其任何组合。本发明还提供了治疗，预防，抑制或降低性功能障碍，性欲降低，勃起功能障碍，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，脱发通过向受试者施用选择性雄激素受体调节剂（SARM）化合物和/或其类似物，衍生物，异构体，代谢产物，药学上可接受的盐，药物产品，由此引起的ADAM在男性受试者中的肥胖，良性前列腺增生或前列腺癌。水合物，N-氧化物，前药，多晶型物，晶体或其任何组合。

40. 发明申请

WO2003049675A3 TREATING MUSCLE WASTING WITH SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2003049675A3
公开(公告)日：2003-06-19
申请号：PCT/US2002/036147
申请日：2002-12-05
申请人： GTX, INC. , STEINER, Mitchell, S. , VEVERKA, Karen, A. , DALTON, James, T. , MILLER, Duane, D. , CHEN, Jiyun , FISHER, Scott , KIM, Juhyun , OKOLICANY, Juraj , MARHEFKA, Craig , HWANG, Dong Jin , CHUNG, Kiwon
发明人： STEINER, Mitchell, S. , VEVERKA, Karen, A. , DALTON, James, T. , MILLER, Duane, D. , CHEN, Jiyun , FISHER, Scott , KIM, Juhyun , OKOLICANY, Juraj , MARHEFKA, Craig , HWANG, Dong Jin , CHUNG, Kiwon
IPC分类号： A61K31/32
摘要： This invention provides: a method of treating a subject suffering from a muscle wasting disorder; a method of preventing a muscle wasting disorder in a subject; a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 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 its analog, derivative isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide or any combination thereof, as described herein.

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