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1. 发明申请

US20130116277A1 ALDO-KETO REDUCTASE SUBFAMILY 1C3 (AKR1C3) INHIBITORS 审中-公开
标题翻译： ALDO-KETO还原亚型1C3（AKR1C3）抑制剂
公开(公告)号：US20130116277A1
公开(公告)日：2013-05-09
申请号：US13607633
申请日：2012-09-07
申请人： James T. DALTON , Duane D. Miller , Ramesh Narayanan , Muralimohan Yepuru , Christopher C. Coss , Michael L. Mohler , Zhongzhi Wu
发明人： James T. DALTON , Duane D. Miller , Ramesh Narayanan , Muralimohan Yepuru , Christopher C. Coss , Michael L. Mohler , Zhongzhi Wu
IPC分类号： C07D217/24
CPC分类号： C07D217/24 , A61K31/4709 , A61K31/472 , C07D217/22
摘要： The present invention relates to a novel class of AKR1C3 inhibitors, to compositions containing them, to methods for their preparation, and to methods of use thereof. The AKR1C3 inhibitors may be useful in the treatment of, for example, prostate cancer, benign prostate hyperplasia (BPH), lung cancer, acne, seborrhea, hirsuitism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, uterine cancer, uterine fibroids, endometriosis, myeloma and leiomyoma.
摘要翻译：本发明涉及新一类的AKR1C3抑制剂，含有它们的组合物，其制备方法及其使用方法。 AKR1C3抑制剂可用于治疗例如前列腺癌，良性前列腺增生（BPH），肺癌，痤疮，皮脂溢，多发性脱发，秃发，脱发，早熟性青春期，肾上腺肥大，多囊卵巢综合征，乳腺癌，子宫癌，子宫肌瘤，子宫内膜异位症，骨髓瘤和平滑肌瘤。

2. 发明申请

US20120157539A1 NUCLEAR RECEPTOR BINDING AGENTS 失效
标题翻译：核受体结合剂
公开(公告)号：US20120157539A1
公开(公告)日：2012-06-21
申请号：US13362242
申请日：2012-01-31
申请人： James T. DALTON , Christina BARRETT , Duane D. MILLER , Seoung-Soo HONG , Yali HE , Michael L. MOHLER , Ramesh NARAYANAN , Zhongzhi WU
发明人： James T. DALTON , Christina BARRETT , Duane D. MILLER , Seoung-Soo HONG , Yali HE , Michael L. MOHLER , Ramesh NARAYANAN , Zhongzhi WU
IPC分类号： A61K31/165 , C07C237/40 , A61P19/10 , A61P9/00 , A61P3/06 , A61P15/00 , A61P25/28 , A61P17/00 , A61P35/00 , A61P29/00 , A61P35/02 , A61P9/10 , A61P31/12 , A61P13/12 , A61P3/10 , A61P19/08 , C07K14/705
CPC分类号： A61K31/138 , A61K31/40 , A61K31/445 , A61K31/55 , C07C233/60 , C07C233/65 , C07C233/75 , C07C233/84 , C07C235/38 , C07C235/56 , C07C235/66 , C07C251/48 , C07C255/57 , C07C311/29 , C07C2601/14 , C07D221/12 , C07D265/34 , Y02A50/402 , Y02A50/411 , Y02A50/414 , Y02A50/423
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.
摘要翻译：本发明涉及新型选择性雌激素受体调节剂（SERM）。 SERM化合物可用于预防和/或治疗各种疾病和病症，包括预防和治疗诸如前列腺和乳腺癌，骨质疏松症，激素相关疾病，潮热或血管舒缩症状，神经系统疾病，心血管疾病和肥胖。

3. 发明申请

US20120071524A1 COMPOUNDS FOR TREATMENT OF CANCER 有权
标题翻译：用于治疗癌症的化合物
公开(公告)号：US20120071524A1
公开(公告)日：2012-03-22
申请号：US13216927
申请日：2011-08-24
申请人： Yan Lu , Chien-Ming Li , Zhao Wang , Jianjun Chen , Wei Li , James T. DALTON , Duane D. Miller , Charles Duke , Sunjoo Ahn
发明人： Yan Lu , Chien-Ming Li , Zhao Wang , Jianjun Chen , Wei Li , James T. DALTON , Duane D. Miller , Charles Duke , Sunjoo Ahn
IPC分类号： A61K31/427 , C07D263/32 , C07D413/12 , C07D233/22 , C07D403/04 , A61P35/02 , A61K31/426 , A61K31/421 , A61K31/4178 , A61K31/4174 , A61P35/00 , C07D277/42 , C07D403/12
CPC分类号： A61K31/425 , A61K45/06 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/56 , C07D417/04 , A61K2300/00
摘要： The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.
摘要翻译：本发明涉及具有抗癌活性的新化合物，制备这些化合物的方法及其用于治疗癌症和药物抗性肿瘤的用途，例如，黑素瘤，转移性黑素瘤，耐药性黑素瘤，前列腺癌和耐药前列腺癌。

4. 发明申请

US20100280107A1 TREATING BENIGN PROSTATE HYPERPLASIA WITH SARMS 失效
标题翻译：用SARMS处理BENIGN PROSTATE HYPERPLASIA
公开(公告)号：US20100280107A1
公开(公告)日：2010-11-04
申请号：US12826842
申请日：2010-06-30
申请人： James T. DALTON , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Wenqing Gao
发明人： James T. DALTON , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Wenqing Gao
IPC分类号： A61K31/277 , A61P13/08 , A61P17/14 , A61K31/167
CPC分类号： A61K31/277 , A61K31/00 , A61K31/167 , A61K31/56
摘要： This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, 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. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-α reductase enzyme type 1 and/or type 2 inhibitor, wherein said inhibitor is 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. This invention also provides a method of inhibiting a 5-α reductase type 1 and/or type 2 enzyme, comprising contacting the enzyme with an effective 5-α reductase inhibitory amount of 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.
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）和/或其类似物，衍生物，异构体，代谢物来治疗，预防，抑制或降低男性患者良性前列腺增生的发生率的方法，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。本发明还提供了一种治疗脱发患者的方法，包括向受试者施用治疗有效量的1型和/或2型抑制剂的5-α还原酶的步骤，其中所述抑制剂是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。本发明还提供抑制1型和/或2型5α还原酶的方法，包括使酶与有效的5-α还原酶抑制量的选择性雄激素受体调节剂（SARM）和/或其类似物接触，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。

5. 发明申请

US20120022121A1 INDOLES, DERIVATIVES AND ANALOGS THEREOF AND USES THEREFOR 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：US20120022121A1
公开(公告)日：2012-01-26
申请号：US13190150
申请日：2011-07-25
申请人： James T. DALTON , Duane D. MILLER , Sunjoo AHN , Charles DUKE , Dong Jin HWANG , Jun YANG
发明人： James T. DALTON , Duane D. MILLER , Sunjoo AHN , Charles DUKE , Dong Jin HWANG , Jun YANG
IPC分类号： A61K31/404 , C07D209/12 , C07D277/64 , C07D263/57 , A61P35/04 , A61K31/4184 , A61K31/423 , A61K31/428 , A61P35/00 , C07D403/10 , C07D235/22
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 analogous 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 cancer, metastatic cancer, resistant cancer or multidrug resistant cancer, including inter-alia: prostate cancer, breast cancer, melanoma, colon cancer and bladder cancer.
摘要翻译：提供吲哚衍生物和类似化合物以及包含其的药物组合物。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，转移性癌症，耐药性癌症或多重耐药性癌症的方法，其中包括：前列腺癌，乳腺癌，黑素瘤，结肠癌和膀胱癌。

6. 发明申请

US20100137430A1 TREATING ANDROGEN DECLINE IN AGING MALE (ADAM)-ASSOCIATED CONDITIONS WITH SARMS 有权
标题翻译：治疗老年男性（ADAM）的SARS治疗条件恶化
公开(公告)号：US20100137430A1
公开(公告)日：2010-06-03
申请号：US12632619
申请日：2009-12-07
申请人： James T. DALTON , Duane D. Miller , Donghua Yin , Yali He
发明人： James T. DALTON , Duane D. Miller , Donghua Yin , Yali He
IPC分类号： A61K31/277 , A61K31/167 , A61P5/26
CPC分类号： C07C235/24 , A61K31/16 , A61K31/167 , A61K31/277 , C07C255/60
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.
摘要翻译：本发明提供了用于治疗和抑制雄性雄性雄激素降低（ADAM）相关病症的男性受试者的方法，例如性功能障碍，性欲性降低，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，认知改变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，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。

7. 发明申请

US20120136052A1 SUBSTITUTED ACYLANILIDES AND METHODS OF USE THEREOF 有权
标题翻译：取代的ACYLANILID及其使用方法
公开(公告)号：US20120136052A1
公开(公告)日：2012-05-31
申请号：US13302988
申请日：2011-11-22
申请人： James T. DALTON , Duane D. Miller
发明人： James T. DALTON , Duane D. Miller
IPC分类号： A61K31/277 , A61P15/16 , A61P5/26 , A61P27/02 , A61P3/08 , A61P1/16 , A61P9/00 , C07C255/60 , A61P3/10
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。

8. 发明申请

US20120077845A1 ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF 有权
标题翻译：雌激素受体配体及其使用方法
公开(公告)号：US20120077845A1
公开(公告)日：2012-03-29
申请号：US13215679
申请日：2011-08-23
申请人： James T. DALTON , Mitchell S. STEINER , Ronald A. MORTON
发明人： James T. DALTON , Mitchell S. STEINER , Ronald A. MORTON
IPC分类号： A61K31/137 , A61P5/26 , A61K31/4453 , A61K31/167 , A61P35/00
CPC分类号： A61K31/167 , A61K31/137 , A61K31/4453 , A61K45/06 , A61K2300/00
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 cancer, and castration-resistant prostate cancer (CRPC) and palliative treatment of prostate cancer, advanced prostate cancer and castration-resistant prostate cancer (CRPC). The compounds of this invention suppress free or total testosterone levels to castrate levels which may be used to treat prostate cancer, advanced prostate cancer, and CRPC without causing bone loss, decreased bone mineral density, increased risk of bone fractures, increased body fat, hot flashes and/or gynecomastia.
摘要翻译：本发明涉及通过减少黄体激素（LH）或独立于男性受试者的LH水平来降低睾酮水平的方法以及治疗，抑制，降低发病率，降低严重性或抑制前列腺癌，晚期前列腺癌的方法，抗阉割前列腺癌（CRPC）和姑息治疗前列腺癌，晚期前列腺癌和去势抗原前列腺癌（CRPC）。本发明的化合物抑制游离或总睾丸激素水平的阉割水平，其可用于治疗前列腺癌，晚期前列腺癌和CRPC，而不引起骨丢失，骨矿物质密度降低，骨折的增加风险，增加的身体脂肪，热闪烁和/或男子女子气概

9. 发明申请

US20090088480A1 SOLID FORMS OF SELECTIVE ANDROGEN RECEPTOR MODULATORS 有权
标题翻译：选择性受体调节剂的固体形式
公开(公告)号：US20090088480A1
公开(公告)日：2009-04-02
申请号：US12209137
申请日：2008-09-11
申请人： James T. DALTON , David A. Dickason , David Hong , Thomas G. Bird , Tai Ahn
发明人： James T. DALTON , David A. Dickason , David Hong , Thomas G. Bird , Tai Ahn
IPC分类号： A61K31/165 , C07C237/14 , A61P5/26
CPC分类号： C07C255/60 , C07B2200/13
摘要： The present invention relates to solid forms of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same.
摘要翻译：本发明涉及（S）-N-（4-氰基-3-（三氟甲基）苯基）-3-（4-氰基苯氧基）-2-羟基-2-甲基丙酰胺的固体形式及其制备方法。

10. 发明申请

US20100267773A1 ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF 有权
标题翻译：雌激素受体配体及其使用方法
公开(公告)号：US20100267773A1
公开(公告)日：2010-10-21
申请号：US12710693
申请日：2010-02-23
申请人： James T. DALTON , Mitchell S. Steiner , Jeetendra Eswaraka
发明人： James T. DALTON , Mitchell S. Steiner , Jeetendra Eswaraka
IPC分类号： A61K31/4453 , A61K31/167 , A61K31/136 , A61P43/00
CPC分类号： C07D211/06 , A61K31/137 , A61K31/167 , A61K31/445 , A61K31/4453 , C07C215/82 , C07C233/75 , C07C235/56 , C07D221/12 , C07D295/155
摘要： The present invention relates to methods of treating androgen deprivation therapy (ADT) induced hot flashes and severe hot flashes in a subject.
摘要翻译：本发明涉及治疗雄激素剥夺疗法（ADT）诱发受试者的热潮红和严重潮热的方法。

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